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Chronic angina l
~octumal Anginal
Or
Vasospastic angin
Coronary artery Diseases
The most common complications associated with Coronary artery disease include: Angina pectoris,
Myocardial infarction, post Myocardial infarction,and Ischemic stroke. Insufficient supp ly of oxygen
to heart can lead to Ischemic conditions.
Myocardial ischem ia is usually caused by coronary vessel atheroscleros is (High LDL
and high cholesterol is the most common risk facto r). As the vessel lumen nalTOws blood
flow is reduced.
Other causes that limit coronary blood How include: Arterial thrombi and Spasm
A ngina Pectoris
Angina are those symptoms of myocardial ischem ia that occur when myocardial oxygen availability
is insufficient to meet myocardial oxygen demand.
These symptoms include:
Chest discomfort often described as heaviness, pressure, and squeezing. The sensation is
localized typically in the sternal region.
Symptoms often last one to five minutes. Angina can radiate to the left shoulder, to both anns
(ulnar surfaces of the foreann and hand), and can radiate to the neck,jaw, teeth, epigastrium and
back.
Types of angina
Angina Pectoris
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Types of angina
pectoris
Nocturnal
angina (angina
decubitus)
Prinzmetal
angina
(vasospastic or
variant angina)
Coronary artery spasm that reduces blood flow precipitates this angina.
Secondary to coronary artery spasm
Usually occurs at rest (pain may disrupt sleep)
Calcium channel blockers are most effective
Stable angina or
classical
Unstable
angina/resting!
Crescendo
I Vasod ilators I
INitrates I
I Cardiac depressants I
Short duration
Inhaled amyl nitrite
Sublingual
Nitroglycerine
Isosorbide dinitrite
Intennediate
Oral regular or sustainedrelease Nitroglycerine
lsosorbide dinitrite
~-blockers
Proponolol
Long duration
Transdermal
Ntiroglycerine patch
Treatment of angina
The following beta-blockers are used in treatment of angina:
Beta-blockers with Selective Intrins ic Sympathomimetic Activity (ISA) :
Acebutolol hydrochloride Beta-blockers with Non-I SA: Atenolol
and Metoprolol tartrate can be used.
Beta-blockers w ith Nonselective, ISA: Pindolol
Beta-blockers with Nonselective, Non-ISA: Nadolol, Propranolol hydrochloride,
Timolol maleate
Calcium Channel Blockers are used in treatment of angina:
Amlodipine besylate, Diltiazem hydrochloride, Nifedipine, Verapamil hydrochloride
The following Coronary Vasodilators, Nitrates are used in treatment of angina:
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Nitrates
Ht
Nitri tes
rl t
1-+1t cGMP
~
V",So<l'l._~'
Nitrates
Organic nitrates act primarily by vasod ilation (especially venod ilation), which reduces
myocardial preload and therefore myocardial oxygen demand.
Nitrates also promote redistribution of blood flow to relative ischemic areas.
Mechanism
ft~~~;::cts\
~-""
~)
Storage
Conditions
Drug
interactions
Dosage forms
fU-W)
Nitrites
Therapeutic use
Side effects
><
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calcium-channel blocking agents block the entrance of calcium into the muscle, the muscle will not
contract. This will allow themuscle to relax and subsequently reduce the blood pressure. Other
therapeutic uses: angina, migraine, antiarrhythmic.
Non
dihydropyridines
Diltiazem hydrochloride
Verapamil hydrochloride
DHP
NDHP
Cause Bradycardia
Cause Heart blockade
Myocardial vasodilation
Negative (-ve) inotropic
effect (worsening CHF)
iltiazem
Coronary Dilatation ~
(GFJ)
Side effects: flushing, profound low blood pressure, swelling oflegs and feet, constipation and
stomach upset. Ifedema (swelling) of the legs and feet occur, a diuretic may be added to the
regimen.
Nifedipine (Adalat)
Mechanism
Therapeutic use
Side Effects
Amlodipine (Norvasc)
Mechanism
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Therapeutic use
Sidc Effects
Diltiazem (Cardizem)
Mechanism
Therapeutic use
Side Effects
ASA
Post MI
M9i01en~
tlc\opldme
~Iood
A = AnalgesIcs
.IIU
A = AntipyretIcs
Anglo1enslnl
A = Antiinflammatory
~An9~'ln
conwrtlng
A = Anllplatelets (6081 mg/day)
Kidney
fn>yMe
lung
Aspi rin decrease morbidity and mortality
AngIoIensltl ll
fj-"" "'- t
oCCB
ft
Vasocon.-"
tAldost_ _ 1on
Thrombolytic used for coronary
t ADH $Ietlon
perfusion, eg: streptok inase
lThI."
Also Glycoprotein lIB, lilA inhibitors such Ttrofiban can be used
i:.. e-..p
:::--r )
!J ~
\r
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The most common side effect ofni lroglycerine is headache; therefore nitroglycerine should be
taken while sitting position .
Nitroglycerine patch can cause tolerance, to avoid tolerance use nitrate free period.
What drugs effective in MI prevention and treatIl}ent -7 "t.,~). .f\ ')
J
What drugs should be avoided in MI -7 ~\ ?\~u..\.\IJ
~ c ~_ 1'1 _ I M Severe C.hest pain associated with Ml treatedb~ -7 \'\};~ ~
0 0 ~ -
-r\ ()
H, -) -:;.
M,
STEM] -)
~ ;":-'-~ ~
NSTEMl -) ,,",0'" S..
~ MAt what dose ASA act as Antiplatelet -7 b C> _ {1 \)
,
ASA act as irreversible Antiplatelet drug
Nitrates -7 Increase nitrites -7 Increase N itric oxide (NO) -7 vascular smooth muscle relaxation
Low-density Lipoprotein
Angiotensin-Converting Enzvme
Acetyl Saliaylate
ST-Segment Elevation Ml
non-ST-Se ment Elevation MI
Levitra
Viagra
Cialis
Nitrooress
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Vasodilators
I
Cardioic
g1ycosides
Digoxin
Digitoxin
Quabain
p-agonists,
Dobutamine
POE inhibitors
Amrinone
ACE inhibitors
Captopril
Enalapril
Lisinopril
Nitrates,
Nitroprusside,
Hydralazine,
POE inhibitors
Milrinone
Congestive heart failure is characterized by reduced cardiac output so that the heart is not able to
pum p sufficient oxygenated blood strongly enough to reach the tissues. The heart beat is weak and
rapid and the heart muscles may hypertrophy (grow larger) to compensate for reduced cardiac output.
Atrial fibrillation occurs when the atria beat rapidly and out of sequence.
Cardiac Heart failure due to:
Increased sympathetic activity
Fluid retention (edema)
Decrease in heart muscle contractil ity
Due to negative (-ve) inotropic effect
Due to +ve chronotropic effects
Left systolic dysfunction
Left sided failure (systolic failure)
This is the most common type of heart failure, Often due to hypertension. Due left ventricular
(systolic) dysfunction leads to pulmonary edema; Symptoms: SOB (Dyspnea), Wheezing. Can be
treated by ACE l, and beta blockers (rarely in chronic), only carvedilol (PI , P2 and 0.1).
The Most common etiology of left sided heart failu re is:
Due to impaired pumping abi lity of the heart
Usually occurs in Left ventricular ejection fraction
May be present without CHF
Ejection fraction is lower than 35%, it is Left ventricular dysfunction (systolic failure)
Right Sided Heart failure (diastolic failure)
Due to chronic lung d isease, Diastolic filling is impaired this can leads to peripheral edema.
Symptoms: edema in veins, legs, bowel. Diuretics or Dihydropyridine cess treats ri ght-sided
heart failure.
Ejection fraction is greater than 45%, it is Right ventricular dysfunction (Diastolic fa ilure)
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Cardiac glycosides
Mechanism
Positive Inotropic
effect
Negative
chronotropic effect
Vagomimetic effect
Side effects
Digoxin (Lanoxin)
Digoxin
Bioavailability
Therapeutic use
+-r.~9i\""'a/K ATPase
+---;:=:f;-Na
Reduced Na
gradient ~)OW~
Caremoval
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Side effects
Monitor
Decreases wa ll tension
ECG
Counselling
Improves Oxygenation
j lnotropy
(Desired)
Tachyarrhythrnias
(S ide effect)
Bradyarrhythmias
(Side effecl)
! Heart Rate
(Desired)
Digitalis toxicity
Digitalis
toxicity
Predisposing
factors
Toxicities of digoxin
increased by renal failure
(decrease excretion)
Hypokalemia, or
hyperkalemia (potentiates
drug effect)
Hypothyroidism, hypoxia,
renal failure and myocarditis
also predisposing factors for
digitalis toxicities.
Drugs that ! K+
levels
Thiazides
Loop diuretics
Corticosteroids
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Digital is toxicity: Reduced
potassium levels
Digitalis toxicity can be
managed by: discontinue
digoxin, monitor blood
potassium levels. Sever
tachycardia may require
the use ofFAS antibodies.
Which bind to inactive
digoxin
Di gifab
Digital is
toxicity
Management
Antidote
P,_L
P
Di itoxin
Binds strongly to
proteins extravascular
space, resulting in
large volume of
distribution.
Digoxin eliminated
largely unchanged in
Urine
Extensively
metabolized by liver
before it excrete in
feces.
_u - N,
-e....,
e.
li
~
Vc,....~O\.1.I""'J;c..
IJ
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Antiarrhythmic Drugs
T
Class II
P-blockers
Esmolol
(Propranolol)
TImolol
Atenolol
Metoprolol
Nadolol
Class I
la-Na! channel
blockers
Quinidine
Procainamide
DisoQY!iIll ide
\.;.\miodaronO
Ib: Lidocaine
Mcxilctinc
Tocainide
Ic: Flecainide
ropafenone
la
Ib
Ie
II
III
IV
Class III
K+ channel
inhibitors
Amiodarone
(Cordarone)
Bretylium
Dofetilide
Sotolol
N a+ channel blocker
N a+ channel blocker
N a+ channel blocker
Beta blockers
K+ channel blockers
Cal+ channel
Class rv
Ca 1+ channel
blockers
Verapamil
Diltiazem
Nifedipine
(procardia, Adalat)
Miscellaneous
Adenosine
Magnesium
Arrhythmias
Arrhythmias develop because of abnormal impulse generation, propagation or both.
Cardiac arrhythmias are related to abnormal electrical activity within the heart resulting in either
altered rhythm or impulse conduction.
Dysrhythmia--disturbed heart rhythm
Arrhythmia - absence of rhythm
Bradycardia - a heart rate that is lower than nonnal 60 beats/min).
Tachycardia - a heart rate that is higher than normal (> 100 beats/min).
Paroxysmal - an arrhythmia that suddenly begins and ends (may occur with fever)
Sinus bradycardia - low sinus rate <60 beats/min ( between the pacemaker and atria).
Sinus tachycardia - high sinus rate of 100-180 beats/min as occurs during exercise or other
conditions that lead to increased SA nodal firing rate.
Atrial flutter - sinus rate of250-350 beats/min.
Sick sinus syndrome - a disturbance of SA nodal function that results in a markedly variable
rhythm (cycles of bradycardia and tachycardia).
Atrial tachycardia - a series of3 or more consecutive atrial premature beats occurring at a
frequency> I OO/min; usually due to abnormal focus within the atria and paroxysmal in nature.
This type of rhythm includes paroxysmal atrial tachycardia (PAT).
Atrial fibrillation - uncoordinated atrial depolarizations.
Junctional escape rhythm - SA node suppression can result in AV node-generated rhythm of 4060 beats/min (not preceded by p-wave).
AV nodal blocks - a conduction block within the AV node (or occasionally in the bundle of Hi s)
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Antiarrhythmic Drugs
Heart blockade:
The el ectrical impulses are partially or fully blocked between the atria and the ventricles . The SA
node in the right atrium ' fires' at the normal rate, but the rate at which the ventricles contract (pulse
rate) depends on how many impulses get through to the ventricl es.
Three types:
1it degree ---blockage of pulsation
2nd degree ----blockage of pulsation
3rd degree---complete heart block
First-degree heart block means there is a slight delay in each impulse going from the atria to the
ventricles. But, each impulse does get through and the heart rate is nonnal.
Second-degree heart block means that some impulses from the atria are not conducted through to
the ventricles. The rate that the ventricles contract can then be slow.
Third degree or ' complete heart block' means that no impulses are conducted through. The
ventricles then comract at their own intrinsic rate of about 20-40 beats per minute. So, you have a
very slow pulse.
Myocard ial Action Potential Curve
Myocardial action potential curve reflects action potential, which describe electrical activity of five
phases.
This occurs in atrial and ventricular myocytes and Purkinje fibers
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Antiarrhythmic Drugs
mV
3
IJ,,~
"
~ '-.
~----~=~~-~~~~
Myocardial action pOlential curve
Torsade de pointes
A problem in one of the ion channels can prolong the Q-T interval. A prolonged Q-T interval can
increase ri sk for a type of arrhythmia called torsade de pointes. When torsade de pointes occurs,
heart cannot pump enough oxygen-rich blood to the rest of body, especially your brain. Torsade de
pointes can also lead to ventricular fibrillation, a dangerous fonn of arrhythmia that causes rapid,
uncoordinated contractions in the muscle fibers of the ventricles. With ventricular fibrillation, the
heart cannot pump oxygen-rich blood to the rest of the body, wh ich can lead to death.
Drugs and diseases that can lead to QT-prolongation
Phenothiazines and haloperidol -7 anti psychotics
Type III antiarrhythmic drugs
In patients with hepatic fai lure.
Electrocardiograph Wave Forms
The electrical acti vity occurred during depolarization and
repolarization transmitted through electrodes attached to
the body and transformed by an electrocardiograph (ECG)
in to series ofwavefonns;
P WAVE: indicated atrial depolarization
PR INTERVAL : indicates the spread of the impulse from the atria through Purkenje fibres.
QRS complex: indicates ventricular depolarization
ST segment: indicates phase 2 or the action potential- the absolute refractory period.
T wave: shows phase 3 of the action potential-ventricular repolarization.
Q-T interval -7 mechani cal contraction of the ventricles (Torse de pointes)
U wave -7 caused by hypokalem ia
Arrhythmias Treatment
Class I
Class la
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Class la
Therapeutic use
Class Ib
Therapeutic use
Class Ic
Therapeutic use
Class II
Beta blockers
Therapeutic use
Class III
K ~ channel
blockers
Class IV
Ca2+ channel
blockers
Therapeutic use
Digoxin
Therapeutic use
Antiarrhythmic Drugs
Pharmacological action;
Slow the phase 0 (slow entry of Sodium ion)
Prolong re-polarization
Prolong effective refractory period
Indicated to treat SVT, VT
Lidocaine
Tocainamide
Mexiletine
Pharmacological action:
Min imal effect on Phase 0 Slow phase -III repolarization (decrease K
pump o ut)
Indicated to treat VT, VA
iv Lidocaine: used to treat cardioversion related arrhythm ias
Encainide,
Propafenone ~ decrease 25-50% digoxin
Flecainide
Pharmacological action:
Very effective on slowing phase 0 depolarization
Little effect on repoiarization
Indicated to treat VA
Propranolol
Atenolol
Timolol
Pharmacological action:
Competitively block catecholamine induced stimulation of Beta
receptor thereby
Suppress phase I V depolarization
Indicated to treat AT, SVT, VT, VA
Amiodarone ~ blue skin, photosensitivity, photophobia
Bretyl ium
Sotalol
Prolong Phase II I repolarization (Prolong QT interval) ~ Torose de
pointes
Indicated to treat VA
Verapamil
Diltiazem
Nifedipine
Pharmacological action: Shortens action potential
Indicated to treat SVA, VA
Pharmacological aClion: Effects vagotonic response (vegomimetic)
thereby increases AV nodal refractoriness.
It is contraindicated in ventricular fibrillation.
Ventricular taChycardia may result from digitalis toxicities
Indicated to treat SVA (atrial arrhythmias) only
Contraindicated in ventricular arrhythmias
Quinidine (Quinaglute)
Mechanism
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Therapeutic use
Drug-Drug
interaction
Side Effects
Counselling
Antiarrhythmic Drugs
Atrial, AV junctional, and ventricular tachycardia.
Maintain sinus rhythm after direct atrial flutter or fibrillation.
Antihypertensive, Anticoagulant - Quinidine may increase the effects of
these
drugs.
Phenobarbital and Phenytoin - reduce the effect of quinidine
Digoxin-Quinidine increases the effects of digoxin (decrease 50% digoxin
dose).
SA and AV block or asystole, nausea, vomiting, diarrhea (cinchonism-large
doses-blurred vision, tinnitus, headache, disorientation and psychosis. Torsos
De pointes (VA)
Toxic level ~induce ventricular tachycardia.
Increases steady state concentration of digoxin by displacing PPB
Report tinnitus, blurred vision immediately
Avoid concurrent use of aluminum containing antacids
Keep out of reach of children
Administer after meal to minimize gastric distress
Don ' t crush tablets because drug irritates mucosa.
Procainamide (Pronestyl)
Mechanism
Side Effects
Amiodarone (Cordarone)
ofT~ toT]
Counseling
Blue skin color gn:aentation), corneal deposits, hepatic toxicity, optic neuritis,
erectile dysfunc IOn~otophobia
Avoid exposure to sunlight, use sunscreen
Avoid grapefruit juice
Digoxin (Lanoxin)
Therapeutic use
Contraind icated
Atrial arrhythmias
Ventricular fibrillation and hypokalimic patients
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Counseling
Antiarrhythmic Drugs
May be taken with or without food
Meals wI bran fiber, antacids may reduce amt of drug absorbed
Store between15-25 0 C in a tight container and protect from light
t;
'(',,~
'A,
SA
AV
PVC
ECG
PPB
LVD
BS
Cordarone
Lanoxin
Procaine SR
No aceCR
Enkaid
Rhythmol
Lanoxin
uinagiute, Quinidex
Pronestvl Procan Procanbid
Tambocor
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Antiarrhythmic Drugs
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MoA
LM\V H
oJ:. 4
":' looo~ {"~~~
~ <0 Ct~ ;.JJ ;u
% -t~,,,,,,1,,::... '(lY-~
bO~ ~
~~
L",I,;\'ilcrv +pr~-:~'=~ Y--
<>---~~
~
....1l
6~J
n<
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1:.jlL
MO~tS l?A.~lT
---~-yOU
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r (,i\~ T __ \",d.l,"" )
y\~
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Anticoagulants
Anticoagulants
I Anticoagulants I
I
I Antithrombin III I
Mucopolysaccharide
I
",.J
Protein C
' . "'--
W -0--
Endogenous
Anticoagulant
Vitamin K
~ analogue
':>1
~ ~'~-- I Warfarin
LMWH
I
L
'~
\
IntnnSlc
"
Pal hway
1 ....
Damaged surface
l
Kininogcn,Kallikrein
XII"'"
VJ
Extrinsic Pathway
Trauma
1. .
"Xll a
IX "
.. lXa
VII
Vila
...
..X a
,.
Final
Common
Pathway
Prothrombin (II)
lv.
FibrinogTn(l)
Fibrin (La)
lXIII.
Cross-l inked
fibrin clot
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Anticoagulants
Mechanism
Therapeutic use
Drug-Drug
interaction
Side Effects
Contraindications
Monitori ng
_I
Advantage
Therapeutic
Monitoring
Side effects
Enoxaparin
Dalteparin
Tinzaparin
Ardeparin
LMWH are not interchangeable with heparin in their actions and
use. Because these highly acidic. These administered parenterally as
sodium salt. Because poorly absorbed from Gl tract.
The prevention of DVT or PE
Does not change Prothrombin Levels
Act longer and do not require close blood monitoring as Heparin does
Hypersensitivity reaction (chills, fever, urticaria etc),
Bleeding
Heparin induce Thrombocytopenia
Osteoporosis
Warfarin (Coumadin)
Mechanism
v, t 'k ~-)
ltv~
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(~~~
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Therapeutic
Drug-Drug
interactions
Side Effects
Monitoring
lI,'arfann
~.o.
isY~'hes.. of dOl""
,-
Ccfomindole
c.._
Ccf",otan
Ccfame1arole
Due 10 additm.
<ff~
..,.",
~,~
'T'hrornbo/y1,c
~~"
Vitamin K
Antidote
Parenteral
Mech
Enhances the
serum protease
antithrombin
In results in
inactivation of
fators Ha, rXa, Xa,
Xla XlIa XllIa
Protamin sulfate
Antidote
Vitamin K ,
t ohvtanadione
Site of
action
In vitro, In vivo
Onset of
action
Pregnancy
Faster (minutes)
Yes
NO (Terotogenic)
I Warfarin I
~r
t~
Chronic
alcohol
Barbiturates
Rifampin
Vitam in K
Dark g reen
Ve!etables
AtIJ~
~-",-/:,~~
,)
====~~~~----------~.
p'I" o l <:,o<,
Heparin antidote -7
Patient taking heparin
1\
7- --
Y:'
I 1
Heparinactioninclude~ \t... V,\i,,_ \I , y "
What is the safest anticoagulant in pregnancy ~
What are the factors heparin inhibits -7 d-o, I q
Monitor warfarin through ~ I tv F.. ~
I
) IOc, I ,I c:,
~"
(y~
r lc..
" ~ ...,
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~.
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WhatdoyoumonitorinLMWH 7 "," 0
~ lN~
Vitamin K supplements and green vegetable effect on INR by '-:"
Increase in IN R can increase risk of 7 6..L ,J.......,-, / l~A
Heparin antidote action is due to 7 (\.l...u..t-r ~&~ -l ~ --t b~
,
If patient taking warfarin and INR is 4 -~5, what is appropriat~ recommendation 7 ~
ASA interact with warfarin by 7
1 ~ ~ t~ ~
Warfarin act on what factors ~ ;). c, ) 7,\ )
I0 ~
Patient after 2 days, air flight, reports pain ?n h!s legs.. His me~ical qistory ~c1 udes , DVT and
l _~
currently using warfarin 7 "'" '"'rI \.,: <:. ~ \; l:t t< ~, '
Recurrance of~eparin induced TKrombocytop~nia syndrome can be prevented by using7
ty-
9 " -)
cv
t(up
, l.L.vVhOI ~
PE
PT
INR
TIA
STEM]
MI
aPIT
,,' ,t \{ cruJ-;
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Anticoagulants
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10
Antiplatelet Drugs
Antiplatelet Drugs
ASA
Dipyridamole
f\L ",brb,i"
Ticlopidine
&
Clopidogrel
Glycoprotein
inhibitors
Eptifibatide
Tirrofiban
Prostaglandin
.n.IOr
Epoprostenol
("PlLbjllk
l '" l" 1,; t; "'"
Platelets, of the elements of blood cells, tend to clump together. The following drugs interfe re with
the coagulation by inhibiting platelet aggregation. Heart attacks and strokes occur when a blood
clot that forms in a narrowed portion of an artery blood flow and cuts off the supply of oxygen and
nutrients to the tissue that lies beyond the site of the clot.
ASA (Salicylates)
ClopidogreJ
Ticlopidine
Theonopyridine
Dipyridamole
Dipiperdino dinitro pyrimidine
Fab fragments of human monoclonal antibody to the Glycoproteine (GPllbIllIa) receptors
(Abciximab, tirofiban, eptifibatide).
Tielopidine (Tielid)
Mechanism
Therapeutic use
Side effects
Contraindications
Storage conditions
Dosage
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Clopidogrel (Plavix)
An antiplatelet drugs that is used to prevent blood clots from fonning.
It reduces the tendency of platelet to stick together when blood flow
disrupted.
Drug of choice for Transient Ischemic attacks (TIA), and stroke .
Bruising and nosebleeds
Increase the effects of ASA in platelets, as will the risk ofG l bleeding
when Clopidogrel is taken with ASA and other NSAID's.
Not recommended with infants and children
Bleedi ng
Mechan ism
Therapeutic use
Side Effects
Drug-Drug
interacti on
Contraindication
Monitoring
Antiplatelet summary
A,<:'", (c....-.t:.'<-~)
IS
an alternate drug
of chOice -) U--<si" ~
~ ~ ~_~
If patient is allergic to aspIrin what is alternate drug ~ C
1-\...~ ~
Drug of choice for trans ient Ischemic attack {TIA) ~ (~ L
What IS the effcct of aspirin on warfann ~ \' U 99.D"::J
a
What dose of aspirin act as Antiplatelet ~ b<...-
a.l A SA
&.'0
Acetvl Saliavlate
Transient Ischemic attack
Nonsteroidal Anti-Inflammatory Drug
I Ticlid
Plavix
L,'", ,"l~
T icQ :ct
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Thrombolytic Drugs
11
Thrombolytic Drugs
Thrombolytic Drugs
Streptokinase
(Strepto protein from
Group CB-hemplytic
steptococci bacteria
tissue
plasminogen
activator tPA
Clot selective
Mechan ism
('
Anlstreptase Ammase)
PrOOrug of streptokinase
U ro k'mase
t~pa
(AbTlOnase)
Alteplase
Reteplase
Tenecteplase
Streptokinase
Urokinase
Anistreplase
Facilitate conversion of
plasminogen to plasmin that
subsequently hydrolyzes fibrin
to dissolve clots
Recombinant DNA derivatives
oftissue plasminogen activator
Side Effects
Thrombin TIa
Fibril!
,T~h;e~ra;p~e~U~I;~C____--!A~cu
~l~e~MW1~a~n~d'l!a~c~u
~,e~mJas~sl;vLe~O ~
pulmon
bolism PE D - /
<"
Prothrombin (II) _
(IPA),
They contain 527 and 355 am ino
acids of natural tPA.
tPA catalyzes the conversion of
lasminogen to plasmin
y'"
rl"-X
B<"",
_ xu.
/.1
~
ypersensitivity reactIons
Internal GI bleeding, retroperitoneal
bleeding, superficial bleeding at catheter injection site.
Nausea and vomiting
Streptokinase (Streptase)
Mechanism
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Thrombolytic Drugs
Therapeutic use
D rug-Drug
interactions
Side Effects
Monitoring
Urokinase (Abbokinase)
Mechanism
Therapeutic use
Side effects
Anistreplase (Eminase)
Mechanism
Therapeutic use
Thrombolytics Tips
f\ ~ ) ~~b~
I- PAsa,e -7
DOC for ST segment elevation myocardial infarction (ST EM I)
EmbOlUS -7 ~ ~ ~
Streotase
Abbokinase
Eminase
. ~4 -~~~
an'}h~L"\J"'o'Ib<.li.....b .
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_ ~ 1,- ,) 0 Q
Antidepressants
12
@j l f '~
Antidepressants
Classification of Antidepressants
I
Monoamine Oxidase ( MAO)
Inhibi tors
Irreversible MAO
Phenelzine (Nardi !)
Tranylcypromine (Parnate)
Isocarboxazid
Clorgyline
I
Amine reuptake
inhibitors drugs
5HT, NE, D
I
5HT, N E
Tricyclics (TCA's)
Tertiary ami ne type (S HT<NE)
Amitripty line
Imipramine
Secondary amine type
(5HT=NE)
Desipramine
Nortriptyline
receptor inhibitors
I
Non-selective
(12
Dual action
SNRl
Venlafaxine
sNDRl
Bupropion
5HT only
Selective serotonin
Reuptake inhibitors (SSRI 's)
Fluoxetine (Prozac)
Fluvoxamine
Paroxetine
Sertraline
Citalopram
e--ei-rnlopram
fI::U"i~ \-
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Antidepressants
Classes of antidepressant drugs include: tricyclic compounds (TCAs), monoamine oxidase inhibitors
(MAOls), selective serotonin re-uptake inhibitors (SSRIs) and reversible inhibitors of monoamine
ox idase (RIMAs).
Mechanism
Citalopram (Celexa)
E-citalopram
Fluoxetine (Prozac)
Fluvoxamine (Luvox)
Paroxeline (Paxil)
Sertraline (Zoloft)
Selective serotonin reuptake inhibitors:lncrease serotonin levels
Metabolic enzymes
Therapeutic use
Antidepressant
Antianxiety
Sexual dysfunction (orgasmic delay) ~ Alprostad i l may be helpful
GI 7 Nausea (Most common)
Headache
Insomnia
ervousness
Fatigue
Side effects
Advantage
Serotonergic
syndrome
(Contraindications)
Discont inued
syndrome
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Antidepressants
Tips
Most anorexic~Fluoxetine
Most nauseating ~ Fluvoxamine
Most weight gain ~ Mirtazapine
Citalopram ~ SE: Somnolence
All SSRJs have common SE: Nausea
Antidepressants with Less sexual dysfunction ~ Bupropion,
Mirtazapine, moclobemide
Onset of action
It normally takes 2-4 weeks for antidepressant to have an effect.
Wash out period
Two SSRI's or SSRl with TCA or MAOI should not combine
If switch from one SSRI to other (SS RI , TCA or MAOI), waiting period
required (washout period)
All SSRls have washout period for 2 weeks, Except: Fluoxetine (require
5 weeks)
Tramadol
Meperidine
Amphetamine
Dopamine
Cocaine
Methyldopa
MAO Inhibitors
Dextromethorphan
SS RI
Caffeine
TCA
Lithium
SSRI
MAO Inhibitors
TCAs
St.John wort
serotonergic symptoms
Hyperpyrexia (Fever)
Agitation
Neuromuscular pains/myoclonus hyper refiexia
Hypotension
Tremors I Shivering
Seizure
Coma, and death
Tricyclic Antidepressants
TCA
Mechanism
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Therapeutic use
Side effects
Contraindications
Overdose symptoms
Overdose treatment
Tips
Antidepressants
Antidepressant
Neuropathy pain ~ Amitriptyline
Enuresis in children (Bedweuing)
Anxiety disorder (OCD)
Imipramine
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MAO Inhi bitors
Mechanism
Therapeutic use
Side effects
Drug interactions
Can cause
Serotonergic
syndrome
Serotonergic
syndrome
Hypertensive
cris is
Food to avoid
Antidepressants
TCA
Dopamine
Cocaine
Methyldopa
Dextromethorphan
Caffeine
Pseudoephridine
Lithium
Serotonin syndrome symptoms includes:
Hyperpyrexia
Agitation
Neuromuscular pains
Hypotension
Coma, and death
Caused by combination of MAOI's with SSRI or TCA's or narcotics
(meperidine).
Use washout period for 2 weeks before administering SSRI.
Inhibitions of MAO I in brain causes catalyze oxidative deamination of toxic
substances such as tyramine.
Tyramine is present in foods such as fermented food cheese, wine etc.
Aged cheese (cheddar, blue and Swiss), yogurt, smoked meats, wine, liquor,
yeast, raisins, chocolate, dry salami, pepperoni, sausage, bananas, figs, tea and
coffee.
Drugs: Sympathomimectis, ephedrine, pseudoephridine.
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Antidepressants
Bupropion
Venlafaxine
Mirtazapine
Bupropion
Venlafaxine
Minazapine
Trazodone and Nefazadone
Serotonin (very little), Dopamine and Norepinephrine reuptake inhibitor
(sNDRI)
SE: Stimulant affect (tachycardia, agitation), aggravation of psychosis,
aggravation of seizure (Reduce seizure threshold)
Also used for sm'o king cessation (Zyban)
1" line treatment for Major depression
Least sexual dysfunction and weight gain
Inhibits Serotonin and Norepinephrine, Some degree of dopamine reuptake
inhibitor (SNRI)
Stimulant aITt::l.:l -7 Anxit::ty, agilaliulI, ht::adadLt::, ill~u lILLLia
At higher dose 225 mg / day, it has cardiovascular side effects, such as dose
dependent hypertension.
At lower dose (75 and 150mg) it acts on 5HT only, higher dose (225mg)
5HT ,NE and Dopamine.
Alph~ antagonist and potent 5HT2 receptor antagonist
Increases release of norepinephrine and serotonins.
Side effects: Increase appetite, Sedation
Increase serum cholesterol levels
Lithium (Lithobid)
Therapeutic use
Pharmacokinetics
Therapeutic levels
Dose
Side effects
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L~-t."'~ +J....:..\A\'"'~ ~
_'
t ,::... r..
~W
Antidepressants
Drowsiness
In coordination
Dizziness
Blurred vision
Confusion
Seizures
Monitoring
Fluid retenti on
Change in heart rate or rhythm
Li thium serum levels
Renal Function tests
Thyroid Function Tests
(:{~g;::t~ ,,~~'S(~~E~~i7~ ~ 1~ ~~
Antidepressant Tips
_ ',
dCt;;: () ~ u, ~ ""l=K
SSRI onset of action is ~ J - ~ I....ll./ ~\ ~
fl -..r ;
lc.J\
l' _.
MAO is classified as -7
n....t,.-., ~ ......0
-0 ~
i: '"D~
r.
,.... 0
L\l~ \. ""'-
It-
-">
Lt~~!O~? ~
tOile. .........
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Antidepressants
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NDRl
RlMA
TCA
OCD
CVD
GAD
5HT
Monoamine Oxidase
Selective serotonin reuptake inhibitor
Dopamine
Norepinephrine
Serotonin ore ine hrine Reu take Inhibitors
Norepinephrine Dopamine Reu take Inhibitor
Reversible Inhibitors of Monoamine oxidase
Tricyclic Antidepressants
Obsessive-Compulsive Disorder
Cardiovascular Disease
General Anxiety Disorde
5-hydroxy tryptamine Serotonin
Celexa
Proxac
Luvox
Paxil
Zolof't
Anafranil
No ramin
Sinequan
Tofranil
Aventyl
Sunnontil
Nardil
Pamate
Wellbutrin SR
Effexor
Remeron
Desvrel
Lithobid
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13
~I
Non-benzodiazepines
Zaleplon
Zopiclone
Zolpidem
Other anxiolytics:
Buspirone, Hydroxyzine
Barbiturates
Benzodiazepines
I
Long action
Diazepam
Fluorazepam
Clorazepate
[ntermediat
Alprazolam
Lorazepam
Temazepam
Estazolam
Short acting
Oxazepam
Triazulam
Midazolam
I\LT{..
~\-
Ultra-shon
action
Th iopental
Intermediate
Amobarbital
Secobarbital
Pentobarbital
Long action
Phenobarbital
Sedatives (anxiolytic agents): Reduce anxiety with linle effect on motor or mental functions.
Hypnotics: Produce drowsiness and reduce onset of sleep.
Insom nia - disturbed or fragmented sleep, often associ ated with physical or emotional illness
Anxiolytic - a drug that decreases anxiety
Sedatives
~~
Benzodinzepines
Others sedatives
Barbiturates
r-----~------_r------_.~------.
Aldehyde
derivative
Antihistamine
, :t\~ ~\'"
~Short acting
Midazolam
Estazolam
Triazolam (Halcion)
Cyc1opyrolones
Pyrazolopyrimidincs
Benzodiazepines
Hypnotic &
Sedatives
I
........ -0J.
l.a
Long acting
Diazepam (generics)
Flurazepam (Dal mane)
Clonazepam,
Chlordiazepoxide
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Benzodiazepine are minor tranquilizers are used to treat insomnia and anxiety. The following are
tenns that are used to describe some conditions dealing with anxiety or sleep disorders. Anxiolytic a
drug that decreases anxiety: insomnia - disturbed or fragmented sleep, often associated with physical
or emotional ill ness: sedative - a drug which causes drowsiness but not sleep, reduces anxiety and
irritability; hypnotic - a drug which will produce sleep. Sometimes a larger dose of a sedative will
cause a hypnotic action .
Mechanism
Benzodiazepine
therapeutic actions
Reduce anxiety
Insomnia; Sedative and hypnotic action
Anticonvulsant action
Muscle relaxant action
Flurazepam (no rebound insomnia)
Quazt;pam (No rebound insomnia)
Temazepam
Triazolam used for insomnia ~ often rebound insomn ia
Alprazolam (used in treatment of panic disorders)
Clonazepam (useful in treating absence seizures)
D iazep am ~ status epi lepticus
D iazep am ~ muscle spasm, muscle degenerative disease
Physical and psychological dependence (at high doses)
Withdrawal symptoms upon abrupt discontinuation
Long acting withdrawal symptoms occurs after number of days
Short acti ng benzodiazepine associated wi th immediate withdrawal
symptoms if it is Slopped abruptly.
Confus ion, anx iety, agitation, restlessness, insomnia, and tension.
Rapid development of tolerance and withdraw I symptoms occurs
with short acting.
Flumazenil
Anticonvulsant action
Muscle relaxant action
Dependence
Wi thdrawal symptoms
Benzodiazepine antidote
Other sedatives
Mechanism
Therapeutic use
Zaleplon
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Zopiclone
Zolpidem
Zolpidem (Ambien)
Mechan ism
Therapeutic use
Advantages
Side effects
Barbiturates
Barbiturates
I
Ultra-short action
Thiopental
Short acting
Amobarbital
Secobarbital
Pentobarbital
Long action
Phenobarbital
Barbiturates are used much less commonly than before. They are effective only for a few weeks
since they alter the length oftime spent in R.E.M. sleep. They should only be used for short-term
therapy as sedative or hypnotics.
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Barbiturates
Mechanism
Metabolic Enzymes
Therapeutic use
Withdrawal
symptoms
Poisoning
Poisoning
management
Barbiturates
antagonist
Miscellaneous
Non-barbiturate
sedatives
Chloralhydrate
Antihistami ne
Chloralhydrate
Alcohol
Antihistamine
Buspirone
Tri chlorinated derivative of acetaldehyde
Doxy lamine and other antihistamine are used as OTe treatment of sleep
disorders
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Autocoids
at 9 and II. Subscripts relate to the number of double bond present in aliphatic chains
Platelet aggregation, Relax bronchial and GI smooth muscles, Relax smooth muscles, Inhibit gastric
acid secretion, Pain, Edema, Inflammation
Prostaglandin analogs
1
PGF zu
PGl,
Dinoprostone
Latanoprost
Epoprostenol
Thromboxane A2
Branchial &
smooth
muscle
dilatation
Branchial &
smooth
muscle
constriction
Blood vessels
dilatation
Platelet
aggregation
PGE,
PGE,
Misoprostol
Alprastadil
Branchial &
smooth
muscle
dilatation
TxA2
Inhibit
aggrega.tion
Receptors
PGI;:
Actions
Vasodilation
Decrease platelets aggregation
Maintaining renal blood flow
NSAID. Aspirin. coXI1
POE l
PGF 2
Pmstagl.aadins G
l~.--
Bronchoconstriction
Contraction of uterus
Vasodialtion
Inhibition of platelets aggregation
Increase Platelets aggregation
Vasoconstriction
ProSlaCycIill (PGIIl
'."'et aggrtgation
Vascular lone
Bnlnchiill tone
UtenDt l(lllt
IX
Thrombounc A
t Uterint tont
t V&SCular lOJle
t Bronchill tonc
t Pa1t:1Cl 1IggJC&
f Vascular l(IIlt
PGEAnalogs
PGE. analogs
Misoprostol (Cytotec): is used for prevention ofNSAID induced GI ulcers.
Chemically it is ecosonides
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Autocoids
Leukotrienes
Physiological functions
LTC and LTD antagonists
Play important role in numerous
physiological functions.
Slow reacting suhstance of anaphylaxis.
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Autocoids
tract ~
Neutrophil chemotaxis
(LTC~
and LTD4 )
e. g. Zafirlukast (Accolate) and montelukast (Si ngu lair) ~ Peptid mimetic structure. Indicated in
prophylaxis of asthma.
Zafirlukast (Accolate)
Therapeutic use: For the prophy laxis and chronic treatment of asthma in adults and children
12 years of age and older. Side effects include: G I upset, liver dysfunction.
Take empty stomach to enhance it absorption
Montel ukast (Singulair)
Similar profi le to that of Zafi rlukast.
Can be used in children over 2-year age
Montelukast may be taken without regard of food.
Available as chewable tablet (once daily in the evening).
Administer granules directly into mouth or mix with teaspoon of cold or room temperature
applesauce, carrot, rice or ice cream.
Do not take aspirin or NSAlDs while on this medication.
PGF
LTC
LTD
POI
OAG
lOP
Cytotec
Caverject, Prostin Vi{ pediatrics
Prostin E2, Prepidil , Cerv idil
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Latanoprost
Travoprost
Bimatoprost
Unoprostone
Carboprost
Epoprostenol
Zafirlukast
Montelukast
Autocoids
Xalatan
Travatan
Lumigan
Rescula
Hemabate
Prostcyclin, Fl olan
Accolate
Singulair
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Autocoids
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23
I Ultra rapid I
I Insulin lispro I
Rapid
I I Intennediate I
Regular
Semilente
NPH
Longacting
I
Ultralente
Protamine Zinc
Glargine
Lente
Types of insulin are categorized by their onset of action, and these relat
their effectiveness and their duration of action as well.
..
ue for
/~
r Sulfo~y[ureas l
I" Generation
Tolbutamide
Tolazamide
Chlorpropamide
I
Nonsulfonylurea insul in
secretagogue
Meglitinides
Repaglinide
Neglitinide
Biguanide
Metfonnin
2.... Generation
Glyburide
Glipizide
Gl imepiride
aglucosidase
inhibitor
*Acarbose
Thiazolidinedione
*Pioglitazone
*Rosiglitazone
Very short
(fastest)
iv fonn
Onset
(hours)
Peak
(hours)
5-\0
min
30-40
min
Usual Effecti ve
Duration of Action
I (hours)
2-3 h
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Regular (R)
(suitabl e for iv dose). Both
human and animal source
NPH (N) Isophane
Amorphous precipitate of
insulin wI zinc ion acetate
buffer
Ultralente
Zinc suspension crystals
in acetate buffer contain
large particles that are slow
dissolve
Long
(70%)
Slowest onset of
action but Longest
hypoglycemic effect.
4-5 h
13 h
5-7 (dose-dependent;
may be longer)
6- 10 h
14- 18 h
not suitable for iv
dose
18-28 h
Juvemle onset
I Adult onset (4U yrs)
Milder fonn
_
Destruction of p-cells in pancreas
No production of insulin Associated Very strong genetic predisposition
with treatment is by Diet and
Inabil ity of beta cells to produce adequate
insulin.
insulin and doesn't meet the body's
Ketoacidosis occurs
requirements.
Mainly due insul in resistance
ulet
I inSUlin
Oral hypoglyccmics
Oral hypoglycemics + insulin
I
I reatment
I ural
hypoglycemics
i lin.,,
. .
Diagnosis (Diabetic)
I-Symptoms
2-Random Blood sugar levels> 14.0 mmollL
3-Fasting Blood sugar levels> 11. 1mmoUL
4-Post prandial BSL > 14.0 mmollL
5-G lycosy lated hemoglobin (HbA I c) > 7%
Normal Blood sugar levels (BSL)
Fasting BSL 5-6 mmoUL
Random BSL 11.1 mmollL
Post prandial 14.0 mmollL
HbAI C is 4 - 6%
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Oral antidibetics
HypgJycemic drugs: Sulfony lureas, Meglitinides
Antihyperglycemics: Biguanides, Thizolinediones
Medication
Mechanism
Side effects
Contraindications
Sulfony lureas
Glyburide (DiaBeta)
Chlorpropamide
(Diabinese)
Gliclazide
Stimulate release of
endogenous insulin
Hypoglycemia
Nausea
GI discomfort
Weight gain
Meglitinides
Repaglinide (Gluconorm)
Stimulate release of
endogenous insulin
(rapid-acting, better
post-prandial glucose control): Must
take before meals,
because
Decrease postprandial glucose levels.
I-Reduce gluconeogenesis,
2-increase glucose
utilization
Hepatic or renal
Impairment
Chlorpropamide not a good
choice in elderly (long half
life)
Not used in Ty pe I OM
Pregnancy
It is important to Avoid
alcohol, it can cause disulfiram tvoe reactions.
Hypersensitivity
Diabetic Ketoacidosis
(DKA)
Not indicated in type I diabetes
Contraindicated Pregnancy
Biguanides
Metformin (Gluco-
phage)
Lactic acidosis, in
hepatic and renal disease patients
GI discomfort Anorexia, nausea, diarrhea, metallic taste
Due to anorexia
caused by metformin
this drugs used for
weight loss.
Hepatic or renal
Impairment
Alcoholism
Advanced age
Previous lactic acidosi s
DOC in obese
Therapeutic uses also inelude: To treat Infertility
For weight loss
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Thiazolidinediones
Ros iglitazone
(Avandia)
Pioglitazone
(Actos)
Glucosidase
Inhibitors
Acarbose
(Prandase)
Flatulence
Abdominal
Cramping, nausea
Diarrhea.
Decrease metformin
bioavailability.
Uver disease,
Congestive heart fai lure
(CHF)
DKA,
Inflammatory Bowel
Disease (LBO)
Pregnancy & Lactation,
Li ver cirrhosis
With first bite of meaL
Diarrhea
Steatorrhea (Fatty
stools)
Abdominal discom-
fon
Oily leakage
Chlorpropamide (Diabinese)
Mechanism
Therapeutic use
Contraindications
Side Effects
Repaglinide (Glucononn)
Mechanism
Therapeutic use
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Contraindications
Side Effects
Gliclazide (Diamicron)
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Monitoring
Stimulates the production and secretion of insulin from the islet cells of
pancreas .
Treat adult (maturity-onset) diabetes mellitus
Faintness and confusion
Weakness and tremor
Sweating, constipation and diarrhea
Corticosteroids, estrogens, diuretics, rifampin, other drugs may reduce
the effect of gJiclazide.
Alcohol
Not recommended to pregnant, lactating mothers. and children.
Regular testing of sugar levels in the blood and urine is required.
Periodic assessment of the eyes, heart, and kidneys may also be
advised.
Metformin (Glucophage)
Mechan ism
Therapeutic use
Side Effects
Contraindication
Drug-Drug
interactions
Does not stimulate secretion of insulin like sulfony l ureas. Rather decreases
hepatic glucose output by inhibition of gluconeogenesis.
Reduces LDL, VLDL, cholesterol levels
To control hyperglycemia
For the treatment of obese diabetic patients.
No weight gain side effect.
Preferred in obese patients
Lactic acidosis (in hepatic or renal failure patient), metallic taste, N, D and
anorexia
Contraindicated in renal and hepatic impainnents.
During pregnancy
Patient with history of Lactic acidosis, irrespective or precipitating factors
Alcohol potentiates effects, avoid alcohol
Potentiates other oral hypoglycemics
Rosiglitazone (Avandia)
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Mechanism
Therapeutic Effects
Pioglitazone (Actos)
Mechan ism
Therapeutic use
Contraindications
Side Effects
Drug-Drug
interactions
Acarbose (Prandase)
Mechanism
Therapeutic
use
Drug-Drug
interaction
Dose
Side Effects
Monitoring
Onistat (Xenical)
Mechani sm
Therapeutic use
Drug-Drug
interaction
Dose
Side Effects
Blocks the action of stomach and pancreatic enzymes (Iipases) that digest fats,
so fats and oiher fat so luble vitamins ADEK are not absorb in the body but pass
through and excreted in the feces.
Reduces fats stores and produce weight loss.
Orlistat increases blood levels and toxicity of pravastatin
120-360mg daily
Di arrhea, abdominal discomfort, oi ly leakage
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DiaBeta
Diabinese
Glucononn
Avandia
Actos
Prandase
Xenical
Orinase, Diabinese, Insulase
Diamicron
Starlix
Glucophage
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24
Thyroid disorders
I Drugs Used In Thyroid Disease I
I
I
I Hypothyroids I
IHyperthyroids I
I
Thyroxine (T4).
Dess icated thyroi
hormone.
Svnthroid
I
ITriidothyronine CT,)I
Thioamides:
Methimazole
Propylthiouracil
Symptoms
Treatment
Monitoring
Pregnancy
I
Iodide
Lugol solution :
(lU+!)
~ I lpod," I
Hypothyroid ism
Sensitivity to cold
Constipation
Bradycardia
Weight gain
Dry flaky skin
Coarse hai r
Slowed speech
Puffy face , hands, feet
Hearing loss
Decreased libido
Slow return of deep tendon
reflexes
If untreated myxedema and coma
will develop
Thyroxin (T4)
Triiodothyronine (T])
Hvperthvroidism
Intolerance to heat
Diarrhea
Tachycardia
Weight loss
Nervousness
Heart palpitation
More common in pregnancy
Thioamides
Methimazole
Propylthiouracil
Iodide
Radioacti ve iodide
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Thyroids Disorders
Drug-drug
interaction
Over dose
Monitoring
Methimazole (Tapazo!e)
Thioamides
Mechanism
Pharmacokinetics
Similarities between
Carbimazole and
Methimazole
Do not prevent the uptake ofT by the gland they inhibit the synthesis of
T3 and T 4 by inhibiting the iodination of tyrosine in the thyroglobulin
Blocks the coupling of the iodo thyroxine
Inhibits the conversion ofT. to T J
Therefore thyroid hormone synthesis is decreased.
Obvious effects are very slow since it takes 3-4 weeks before the
hormone levels show a decrease
Well absorbed,
Slow excretion
tll2 is 6 hours
Both drugs accumulate in the plasma
Both cross the placental barrier and can accumulate in the thyroid gland
of the fetus
Propylthiouracil (Propyl-Thyracil)
Mechanism
Therapeutic use
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Thyroids Disorders
Side Effects
Phannacokinetics
Disadvantage
Contraind ication
Monitoring
Tapazole
Propy l-Thyracil
Drug of Choice
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Thyroids Disorders
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25
ITestes I
I Ova')' I
Estrogen
Ethinyl estradiol
Mestranol (prodrug)
Progesterone
Norethidrone
Norgestrel
Norethynodrel
Norgestimate
-rlesogestrel
Included in this category are: androgens (male sex hormones), estrogens (female sex hormones) and
progestins. These chemicals are needed for the development. maintenance and function of the sexual
organs and are necessary for normal pregnancy to occur, be maintained and for birth
Clinical Uses for Various Estrogen Preparations
Palliative treatment of
advanced prostate cancer
IDiethylstilbestrol
Estrogen
Conjugated estrogens
Estradiol
I Estradiol transdermal
Estrogens are female sex honnones that are used primarily to decrease bone loss and to treat the
symptoms of menopause. Estrogen is used to reduce or prevent osteoporosis in susceptible women.
Estrogens decrease the frequency and severity of hot flashes as well as the dryness in the vagina that
many post-menopausal women experience.
Estradiol ~ Exist in body in eqUilibrium with estrone
Estriol
Estrone
Ethinyl estradiol ~ 17 alpha estradiol
Mestranol
Quinestrol~ used for estrogen replacement therapy (HRT)
Diethylstilbestrol ~ Non steroidal synthetic estrogen (sti lbene derivatives)
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Therapo;;:utic use
Side effects
GI? Nausea and vomiting are the most common, weight gai n, d iarrhea
CNS ? Headache, Breast tenderness
CV ? Edema, Hypertension, stroke, MI, Increased risk of thromboembolic
diseases
Contraindicated in
Antiestrogens
Mechanism
Therapeutic use
Tamoxifen
Clomiphene
Inh ibit or modify the action of estrogen
These drugs are non-steroidal antiestrogcnic compounds equally effective in
oral or injection.
Tamoxifen ? Breast cancer
Clomiphene? Fertility drugs
Tamoxifen
Mechanism
Indication
Side effects
Clomiphene (Clomid)
Mechanism
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Therapeutic use
Contraind ication
Side effects
Progestins
Progestins are female sex hormones that may be used with estrogens in oral contraceptive pi lls,
hormone replacement therapy, and treat menstrual irregularities, and as cancer treatment.
Classification of progestins
Two types ofprogestins
17 -alpha hydroxyprogesterone
A. Medroxyprogesterone acetate
B. Megestrol aceta
17-alpha ethinylandrogens (more potent)
A. Norethindrone
B. Norethynodrel
Commonly used in oes
Potent oral activity
More lipid soluble
Less first pass metabolism
Progestins are produced in males from testes.
Mechanism
Adrenal cortex produced progestins in males and females.
Progestins in females promote the development of a secretor endometrium that
can accommodate implantation of newly formed embryo.
The high level ofprogestins produced in second half of menstrual cycle inhibits
the production of gonadotropins and thereby further ovulation.
Therapeutic
Major clinical use in contraception, general ly used with estrogen.
use
Not widely used as alone because of its rapid metabolism results in low
bioavailability.
Progestins are indicated in uterine bleeding, dysmenorrhea, suppress ion of
postpartum lactone, and endometrium cancer.
Endometriosis
Side Effects
Edema
Depression
Menstrual irregularities (breakthrough bleeding, amenorrhea)
Androgen like progestins can increase LDL and HDL ratio cholesterol , weight
gain and edema,
Hirsutism, and acne can cause thrombophJebitis (inflammation of wall of vein)
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Therapeutic use
Side Effects
Androgens
Testosterone is the androgen that leads to the development of male secondary sexual characteristics
and maintains the male reproductive system.
Androgens are used to treat delayed puberty in males who do not develop normal testicular function.
They are also used ill egally by athletes to build muscle mass. They are very dangerous when used for
this as they may lead to aggressive behaviour, and may cause liver and/or brain tumours and death.
Androgens
Danazol
Nandrolone
Stanozolol
Fluoxymesterone
Mechanism
Therapeutic use
Side effects
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Antiandrogens- Finasteride
Mechanism
Therapeutic use
Finasteride
Dutasteride
FJutamide
Cyproterone acetate
Inhibit the synthesis of androgen.
Finasteride: steroid like drug approved for BPH treatment.
Finasteride : inhibits the S-alpha reductase: Competitive and specific
inhibitor of type II S-alpha reductase
Indicated in BPH, and to treat men who have lost scalp hair.
Side effects
Decrease libido.
Sexual dysfunction
Breast tenderness
Hirsutism
Hypersensitive reactions like rashes, pruritic, swelling face and lips
Testicular pain
Dose
Contraindication
~ofindicated
Diabetes Insipidus
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Nolvadex, Soltamox
Clomid
Mifeprex
Danocrine
Durabolin, Kabolin
Winstrol
Halotestin, Android-F, Ora-Testryl.
Avodal1
Eulexin
Diane
Avodant
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Adrenal Corticosteroids
26
Adrenal Corticosteroids
The adrenal hormones, or corticosteroids, are drugs with powerful anti-inflammatory effects. These
are used for replacement therapy in conditions such as, Addisons disease, a condition of adrenal
insufficiency. In replacement therapy, the adverse effects are minimal since hormones are being
replaced and are not added to those already in the body.
Corticosteroids are used for their anti-infl ammatory, anti-allergic and anti-stress effects. Prednisone
is used 'as replacement therapy and also for its anti-inflammatory effects in many conditions, such as
arthritis, allergies and asthma.
Glucocorticoids
Classification
Short acting (812 hour)
Intermediate acting (18-36
hours)
Mechanism
Side Effects
Hydrocortisone
Cortisone
Prednisone
Prednisolone
Methylprednisolone
Triamcilone
Betamethasone
Dexamethasone
Paramethasone
Promote normal intennediately metabol ism
Increase resistant to stress
Alter blood cell levels in plac;ma
Anti-inflammatory action by inhibiting IgE
High doses stimulate gastric acid and pepsin production and may
cause peptic ulcers.
Chronic use causes sever bone loss (Due to decrease in calcium)
and myopathy leads to weakness
Concentration of topical Glucocorticoids depends on site of use
on the body.
Take with food
Should not be stopped suddenly, taper off or gradually decrease
dose.
Diabetic drugs ~ glyburide, chlorpropamide, gl ipizide,
tolbutamide, and tolzamide.
Can rise blood sugar noticeably
Monitor blood sugar levels
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Side effects
I Adrenal
Corticosteroid
I L-ortlcoster010
biosynthesis
inhi bitors
I Mccnamsm
InD icatIOns
of Adrenal
corticosteroids
Adrenal Corticosteroids
Cortisone
Hydrocortisone
Betamethasone
Beclomethasone
Prednisolone
Prednisone
Triamcilone
Methylprednisolone
tl..etoconaZOle
Spi ronolactone
Mifepristone
Metyrapone
Aminoglutethimide
l'or antl-mnammatory cortlco~as: .li lucocOrtlCOIOS cnccts on mc o~ stfloutJon,
concentration, and function of leukocytes. These include decrease in
concentration oflymphocytes T and B cell s) and increase in concentration of
neutrophils.
Decrease basophils, eosinophils and monocytes, and inhibition of the ability
ofleukocyte and macrophages to responds mitogen and antigen.
The above Inhibitory response also results in reduce the amount of histamine
release from basophil s to inhibit kinins.
InDIcatIOns ot aDrenal cortlcoster01DS
Addison's disease (caused by dysfunction of adrenal cortex}-hydrocortisone.
Cushing' syndrome (caused by hypersecretion of glucocorticoids that is due
to excess secretion of corticotropi n by anterior pituitary to adrenal tumor. dexamethasone test is used in diagnosis .
Congenital adrenal hyperplasia (CAH}-results from enzyme defectsadministration of sufficient corticosteroids .
Indicated in inflammatory symptoms of rheumatoi d arthritis, osteoarthritis,
skin condition. Redness, swelling, heat, and tenderness that commonly treated
by adrenal corticoids
Indicated in treatment of allergies.
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Adrenal Corticosteroids
I FormulatIOns
. Systemic:
lM -7 Cortisone, triamcinolone, desoll.ycorticostt:rum::
IV and 1M -7 Dexamethasone, hydrocortisone, methylprednisolone,
prednisolone.
Inhaled -7 Aerosol -7 Beclomethasone, flunisolide. fluticasone, triamcinolone
Topical -7 Hydrocortisone, beclomethasone, dexamethasone, triamcinolone,
Oral: All corticosteroids can be administered orally.
I Long term use OsteoporosIs --> IS due negative calcIUm balance
Side effects
Increase risk of infection due to impaired wound healing and immunosuppression
associated with Diabetes -7 due to hyperglycemia SE
oral steroids
Increased appetite can cause we ight gain
Hypertensi on is due to increase water retention (Edema)
Peptic ulcers
Euphoria
Psychosis
Immunosuppression -7 due to suppression ofh!:E.
Adrenocorticoids Tips
Increase in cortisone cause -->
Decrease corticosteroids Gause~>
What is steroid sparing drug -->
Aldosterone are secreted from -->
lOP
Cortone
A-hvdroCort, Ala-Cort, Ala-Scalpt, Anu-Med HC
Oi rosone. Oi rolene
Beclovent Beconase A Beconase. var Vancenase
AX-Pred Bubbli-Pred Econo red Econo red Plus
Oeltasone. Predone. Stera red Stera red OS
A-Methanred Cortimed De medalone De o-Medrol Medralone
Extina Kuric Nizoral Shamnoo Nizoral Nizoral A-D Xolepel
Aldactone Snirono
Mife rex
Meto irone
Amino lutethimide
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Oral Contraceptives
27
Oral Contraceptives
Oral contraceptives (birth control pills) are combinations of estrogen and progestins.
The combination preparations may be monophasic, biphasic or triphasic. They contain various
estrogens and progestins . Some common ones are listed:
Drugs that Causes Of
OC Failure
Contraindications
Precautions
Starting Hormonal
Contraceptives
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Starting Hormonal
Contraceptives
Miss pills
Plan B (Levonorgestrel
O.7Smg per dose)
Or Minipill
Or Morning after pill
or
Emergency
contraception
Side effects plan B
Oral Contraceptives
Starting Depo-Provera: im
Should be inj ected during the first 5 days of menstrual cycle rule out
pregnancy
Repeat injection ql2 weeks - effective for up to 14 wks
Breakthrough bleeding - most common in 1st 3 months; if persists
beyond 3-6mon check for other causes (eg. chlamydia). Change to
oe with 1 estrogen/progestin depending on when BTB occurs in the
cycle; may also be related to poor compliance, smoking, DIs
Breast tendemess - if persists beyond 1st 3months rule oul pathologic
causes; change to oe with! estrogen/progestin
Weight gain - may i appetite in 1st month but overall weight gain is
minimal with low dose oes & within nonnal limits for age-related
gain; may be cyclical due to Na & H20 retention
Nausea - often subsides within 3 months; take at hs with food or change
to lower estrogen content
Headache - tension headaches unaffected but honnone related or
vascular migraines may i!; if precipitated or exacerbated by oes
should avoid their use
Acne - sometimes worsens initially but usually improves in the long
tenn; change to ! androgenic OC or use topical therapy
Chloasma - irreversible and idiosyncratic; exacerbated by sunlight so
use sunscreen and reduce exposure; ! estrogen dose
Miss one pill: Take as soon as you remember and take usual pill next
day. This means that you might take two pills in a day.
Miss two pills in a row:
First two weeks : Take two pills the day you remember and two pills
next day. Then take one pill until you finish pack.
Use back up method of birth control, if you have sex in next seven
days of missing pill.
Third week: Safely dispose remained pills and start new pack same day.
(If you're on Sunday start schedule continue one pill until Sunday).
You may not have periods this month.
If you miss two periods in a row call doctor.
Progestin only
Very efective within 24hrs and can be used upto 5 days unprotected
inter course.
Schedule 2 (Phannacist intervention)
Contains 2 pills (use 2nd pill after 12 hours of I " pill)
To treat Nausea and vomiting associated with this pill can be treated
by Gravol (dimenhydrinate)
Nausea (23.1%), Vomiting (5%), Dizziness, fatigue
DVT
BTB
Oral Contraceptive
Deep Veinthrombosis
Break Through Bleeding
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Oral Contraceptives
Alesse
Brevicon
Demulen
Diane35
Ortho Cept
Marvelon
Ortho
M inOvral
Triphasil
Svnphasic
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Oral Contraceptives
;;>
O--~
M'J~ ~ ~~
\-1et-~o tra~
~~ \v,1:)~ ~
4 'l.--<-:J
~ if J
J. ('
-~
Mo.Yc_-/~'
"t () fr.-vo.!
sf
D1rj. 6j
'b~;
\)
L~
~-"-h
; <>-- S
II
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Osteoarthritis
~,-,l."'~
~ I", -h ,; """"--t, .
28
0",
Osteoarthritis
1Osteoarthritis I
Nonsteroidal Anti~
inflammatory Drugs
Pain Therapy,
Topical
Tonical
Synovial Fluid
Replacement
Corticosteroids
Betamethasone valerate
Dic10fenac sodium
Capsaicin
Hylan GF 20
(pennsaid)
Methy l salicylate
Menthol
Triethanolamine
salicvlate
Sodium hyaluronate
Viscous supplements
Intraarticular injections
~ , "'~ \~,-b,
Glucoconiooids
Cortisone acetate
Dexamethasone
Dexamethasone sodium
phosphate
Methyl prednisolone
acetate
Prednisolone
Triamcinolone
Triamcinolone diacetate
t Prostaglandins
of C}1otoxic .
t Cytokines
T cells
~.
r.-\ ~S
.L' "'\~..\,
\
J-
Activation of
B cells
Production of
IgRF
autoimmune
complex
Joint
inflammation
Synoviocytc
prolifcrnlion,
Bone and
cartilage
destruction
antibodies
Diclofenac (Voltaren)
Therapeutic use
Side Effects
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Drug-Drug
interaction
Contraind ication
Monitoring
Osteoarthritis
Osteoarthritis Tips
Allergic to aspirin -7
Aspirin use in children with flu symptoms can cause -7
Peptobismol (Bismuth subsalicylate) can cause Rye syndrome in childrem.
Ibuprofen is safe in children under 12 years (No Rye syndrome)
Misprostol is -7
Azotemia -7
Topical pain relievers -7
Hylorunan injections (synovial fluid replacement) act as viscous supplement given -7
Misoprostol is -7
What type of exercise in osteoarthitis -7
Acetaminophen is least used in -7
Risk factors for renal toxicity associated with NSAIDs and COX II inhibitors include -7 .
Counseling of Capscicin -7
Corticosteroids are used primarily for their action as -7
Symptoms
Stiffness
Localized
Pain
lnftammation
Risk factor
Osteoarthritis
Morning or after inactivity (l ast 30
min)
Limited affected joints.
Worsens With Activity Or
After Prolong Use, (weight bearing
activity) .
Uncommon
>65 years
Degenerative joint disease caused
by breakdown of the cartilage b/w
bones, degradation of articular
cartilage in ~ynov ialjoints
Rheumatoid Arthritis
In the morning (last I hour)
Not localized
Worsens with prolong inacti vity. (Usually
improves with activity).
Common
Autoimmune inflammatory condition
Chronic systemic
Symmetrical synovitis affecting similar
joints bilateral.
Cataflam, Solaraze
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M~"'OL~() ..
LC)
ll~
/ --:-,
<:.- 1
'-'-
29
O :~ ,
, '""""'
DMARD'S
r
Gold preparations
Cytotoxics
Other DMARDs
:\
Aurothioglucose
Sodium
aurothioglucose
Azathiopnne
Methotrexate
sodium ~ Gold
Standards for
treatment ofRA
""Cyclosponne
Hydroxychloroquine--,.
sulfate ~ SE: Corneal &
retinal deposition
Biological response
modifiers
Adalimumab
Anakinra
Etanercept
lnflixirnab
~~~LeflunOmide-7 ~
pregnancy
H~~ 'i
Penic;lIamme
Sulfasalazine ~ ell: ASA
."
~"up
A chronic inflammatory disease with frequent acute attacks. The immune system is involved in
attacking the joints and surrounding structures such as muscle tendons and most other connective
tissue. There is inflammation of the synovial membrane.
Biological
Response Modifiers
:::':,
"
...."
""
lnflix.imab
Etanercept
lnfliximab
lnflix.imab (Remicade)
Etanercept (Embrel)
Anakinra (Kineret) .
Binds to the Tumor Necrosis Factor (TN Fa.)
Inhibit interleukin- l (IL-!), a key mediator of inflammatory NF
synoviti s as well as bone and cartilage destruction.
Improve the sign and symptom of active RA
Must be given with Methotrexate to prevent fonnatian of antibodies.
Binds to the Tumor Necrosis Factor (TNF alpha and beta)
Given SC twice weekly
Side effects: Most common: Respiratory tract infections
Given every 8 week by iv
Most common SE is Respiratory tract infections (Pneumonitis)
Storage: Refrigerator (2 - 8OC)
~
Do not freeze
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Methotrexate (Rheumatrex)
Mechanism
Therapeutic use
Side effects
Nausea, diarrhea
Flu-like aches
Oral ulcers (mouth ulcer): Treated by folic acid or folinic supplements.
Bone marrow and liver toxicity
Immunosuppression
Hepatotoxicity
Renal failure
Leukopenia
Abnormal LFT
Pulmonary toxicities in children
Susceptible to Infections (P. carinii)
Starting 7. 5 - 15 mg po Q wk. Increase by 2.5 - 5 mg Q 2 - 4 wk.
Maximwn 25 mg! wk
Maintenance dose: 7.5 - 20 mg po, sc or 1M Q wk (s ingle dose if
tolerated or divided in 2 or 3 doses Q 12 h)
Effectiveness seen after 2- 6 weeks
Administer; PO, 1M, SC
IfG] upset occurs: 2.5 mg start ~ (12 h after) 2. 5 mg ~ (1 2 h after) 2.5
Dose
mg
Monitoring
CBC
LFT's
Creatinin Q 1-2 months
Azathioprine (Imuran)
Refractory RA
Mefabolism
Therapeutic use
Side effects
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Contraindications
Hydroxychloroguine (Plaguenil)
Therapeutic use
Side Effects
Overdose
management
Sulfasalazine (Azulfidine)
Mechanism
Therapeutic use
Side effects
Dose
Pharmacokinetics
Contraindications
Allergies
ASA
Furosemide
Thiazide diuretics
Carbonic anhydrase inhibitors,
Sulfonamides -7 sulfapyridine
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Counselling
Leflunomide (Arava)
Mechanism
Therapeutic use
Side Effects
Monitoring
Washout
Cyclosporine (Neoral)
Cyclosporin PO
3- 10 mg/Kg/day for RA
Therapeutic use
Side effects
Precautions
Drug interactions
(Cyclosporin is
metabolized by
CYP3A4)
Kidney transplantation
Organ transplantation rejection
PsoriasislRheumatoid Arthritis/Nephrotic Syndrome
Renal 7 Very common : renal dysfunction
Cardiovascular 7 Very common: hypertension (particularly in heart
transplant patients)
Nervous System7 Very common: tremor, headache
Metabolic7 Very common: hyperlipidemia
NSAlD therapy should be discontinued where possible. As nonsteroidal
anti-inflammatory drugs alone can have an adverse effect on renal
function, addition of these drugs to N eora! or Sandimmune LV. therapy
or an increase in their dosage should be accompanied by particular close
monitoring of renal function .
Drugs that increase cyclosporin serum concentration :
Ketoconazole
Fluconazole, Itraconazole
Macrolide antibiotics (mainly erythromyci n and c\arithromycin)
Corticosteroids, Oral contraceptives
Norethisterone or danazo l
Calcium channel blockers: Diltiazem, Verapamil, N icardipine
Metoclopramide
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Drug interactions
(Cyclosporin is
metabolized by
CYP3A4)
Minocycline (Minocin)
Minocycl ine
Therapeutic use
Side Effects
Contraindication
D-penicillamine (Cuprimine)
Mechanism
Chelating agent
Therapeutic usc
Side Effects
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Side Effects
Most common
Skin rashes
Proteinuria (after 1M admin.)
Nitritoid reaction (low blood pressure and syncope after injections)
Pruritis (pruriginous), dermatitis
Angioedema
Thrombocytopenia
Aplastic anemia
Diarrhea
Stomatitis
Proteinuria
ASA
TNF
LFT
esc
uc
NSAID
SJS
OA
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~ 30
Gout and Hyper uricemia
I
Hyperuricemia
TheraDV
Antimitotics and
anti-inflammatory
action
Colchicine
Corticosteroids
Nonsteroidal
Anti-inflammatory
Drugs (NSA IDs)
UricosuricS71ncrease
excretion of uric acid
Xanthine oxidase
inhibitors " prevents
conversion of purine to
uric acid
Dexamethasone
Dexamethasone sodium phosphate
Hydrocortisone sodium succinate
Methylprednisolone acetate
Prednisone
Triamcinolone
H,O
SuJfinpyrazone7 Take with full
glass of HP
Allopurinol" Take
with full glass of HP
r...........
lL
/-M-o-r-e-c-o=m::'m~o-n-=:in~:~M::e~n~o:v~e~r-4-0-y-e-a-r~o=f=a:g=e~;;~
R~
..-.
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Hereditary metabolic disease that is a fonn of acute arthritis and is marked by inflammation of the
- Joints.
Gout is associated with increased body stores of uric acid.
Acute attacks involve joint inflammation caused by precipitation of uric acid crystals.
Hyperuricemi a ~
Urate crystal in joints -?
inflammatory response
Acute gout arthritis
Abrupt onset of excruciating pain and inflammation of joint during the night or early morning.
Patient cannot tolerate even light pressure such as a bed sheet on the affected j oint.
Attacks often resolve spontaneously over 3- 10 days. J.IIline treatment is N SAID's
For sever pain a Intra-articular inj ection of corticosteroid. (especially in patient with polyarticular
gout)
Colchicinea It relieves pain withjn 24 hours in 90% patients if treated within few hours of attacks.
Side effects: Gl ~ abdominal pain, cramps, diarrhea, N and V
Rarely a Neuropathy, myopathy, bone marrow suppression
Intercritical gout: Most patient have second attack within 6 - 24 months .
Chronic tophaceous gout: May occur after 12 year of first attack.
3~ '~
Mechanism
Therapeutic use
Side effects
Drug-Drug
interactions
Indomethacin (Indocin)
Mechanism
Therapeutic use
Side effec ts
Probenecid (Benemid)
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Mechanism
Therapeutic use
Side effects
Counselling
Take plenty of water
Sulfinpyrazone (Anturane)
Mechanism
Allopurinol (Zyloprim)
Metabolism
Therapeutic
use
Side effects
C 1.< . ; : " , ,,
&" .~"'~ ~,
Sulfinpyrazone partially inhibits both the active secretion and the active
reabsorption
Inhibits platelet aggregation
Gout arthriti s
Urate crystal formation
Take plenty of water
Therapeutic use
Side effects
Counselling
Mechan ism
en ~
Rlbo," -
P + ATP
Inosinic Acid
j
Hypersensitivity rashes
Inosine
Peripheral neuritis and necrotizing
j 1
vasculitis
Hyroxilnthinp
GI intolerance, diarrhea
Ir.X~M-'~h~I"-,-o-xo~d-,,'eI
In condition with large purine turnover xanthine
Xanthine
stone formation may occur
Ir.X~M----'th~'"-,-o-xo~d-,,'eI
Alkalinize the urine to increase solubi lity
With 6~merca topurine (but not thioguanine)
Uric Acid
Must decrease by 2 I use Wit a opurm .
Xanthine oxidase is main biotransforming enzyme for 6-mercaptopurine.
Example of6-mercaptopurines is azathioprine, an anticancer drug
Take plenty of water
!
!
Counselling
T}>~"--.A
a
~,}
t'"
l\~t,,,J:)
<;Jf"'V'o""'~
-J
,
~ ,
f l' \ ~
~ ~ o...L..o-...C;~l 0
"'l
,0
'j
'"'.(1<1)
Co
l'\. _ ~
'1'J4-
c..
Pharn>acY"e 'vvlot
t.
o!
'? ~ ~\
d...
-Lj)
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Sulfinpyrazone is used as ~
A uricosuric drug is one that -7
Colchicine is mainly used for ~
I xo
I xanthine oxidase
lndocin
Benemid, Probalan
Anturane
Zyloprim
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Osteoporosis
31
Osteoporosis
I
Osteoporosis Treatment
I
Calcium Supplements
Anti parathyroid
Hormones
calcitoni~
Bisphosphonates
Benzothiophene
"\
Parathyroid hormonesl
Alendronate
- l-
~tidronate
Non Modifiable
I
Selected Estrogen
Receptor Modul ators
"(SERM s)
Calci um carbonate
Calcium gluconate
Risedronate
Age> 65 y
Vertebral compression fractures
Postmenopausal woman (not on estrogen
therapy)
Premature menopause 45 years)
Gender (Female)
Family history
Thin and small boned (overweight is NOT a
risk factor)
Hypogonadism
Race: Caucasians, Asians
Hyperparathyroidism
Hypocalcemia
In esled
Teriparatide
Raloxifene
hydrochloride
Modifiab le
Low calcium intake 1000 mg
elemental calcium per day)
Inadequate sun exposure.
Gigarette smoking
Excessive Alcohol intake ~
Caffeine contai ning beverages.
Sedentary life sty le
Excessive heparin therapy
Oral Corticosteroid therapy
V.'t D
( )
) ~.~~~
(
(
(~ )
Fe<:al
Ca"
_s,_cro_;_,,_---'
LI
Filtration
Reabsorptl
~
I'TH
~rmary Ca'-excretlon
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-~
www
'---=-- c::.
0 2,
~,,<<<-)
ac Pre .Com
j'
'~'1J ~,-\' J ~ ~~
Osteoporosis
Dose of Vitamin D
s\::::
Bisphosphonates
L-.". ~ ~
l' ~ Y) r s 'v,.~ -~
"C<A..
! \ I.) <.l""'O
'r~ -?t"-V4-2>~po<...toi.s
Bisphosphonates
Mechanism
Therapeutic use
Osteoporosis Prevention
Treatment of post menopause bone loss
Treatment of osteoporosis
Treatment of Glucocorticoid induced osteoporosis
Paget's disease = Excessive activity of osteoclasts.
Metastatic bone cancer
Bisphosphonates have decreased rate of bone fracture in osteoporosis
and Paget's disease patients
Bisphosphonates have anti resorptive activity.
Risedronate has highest anti resorptive activity and than alendronate.
Etidronate has lowest anti resorptive activity
Side Effects
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Dose
Alendronate
Counseling
Osteoporosis
Alendronate (Fosamax) available in a once weekly 70mg tablet
Available dosage forms: 5 mg, IOmg, 35 mg, 40 mg, 70 mg
Prevention of osteoporosis in postmenopausal women - once 5 mg
daily
Treatment of osteoporosis in women 10 mg once daily or 70 mg tablet
once weekJy
Treatment and prevention of glucocorticoid induced osteoporosis in
men and women- 5 mg once daily
Treatment of osteoporosis in men one 10 mg tablet once daily or 70 mg
once a week.
Risedronate (Actonel) = Available dosage forms: 5 mg, 35 mg,
Take first thing in the morning empty stomach
Take with plenty of water
Do not lie down for 30~45 min after medications (slay upright)
Calcium supplements should be separated by 2hours before or after
Raloxifene (Evista)
Mechanism
Therapeutic use
Side Effects
Calcitonin salmon
Calcitonin is a hormone secreted from thyroid gland
Calcitonin hormone helps bone formation by transporting Ca from blood to bones
Mechanism: Directly effect on osteoclast and decrease bone resorption through direct effect.
Two products are available
Miacalcin
200 JU/day intranasally
Common SE is nasal irritation
Calcimar, caltine
50 - 100 JU sc/day or Q 2,.j day or 5days/wk
Not approved for osteoporosis
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Osteoporosis
Osteoporosis Tips
present~ 0 ~ ft- ~ _n
_r
rO~4~ ~
Riskfactorsofosteoporosis~ ~ost_~ ~.- ~Ot>~_-' \_- ',t:
~e!~
o....~
OJ
Ff 0 I 4
Elderlymayabsorbcalciumpoorlydueto \~ ~ o....<'l'd... ~ ~~~ ~j\\I.Q \J~
Calci u~ supplement in elderly ~ C6..... (
Paget O>sease-7 D
~ -l
lh ~t- ~ c c:.....
c.c ~
_0-::\ '< .
~"- '""~ J l>'("'4l!.:. '\:)
~~
.~
V t
~
..,
(..
n.
M ~.
SERM
LDL
HOL
TO
OVT
t. O<;.IAY;
Evista
Fosamax
Didronel
Actonel
Alendronate
-')
--:::,
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32
Bronchodilators
Methyl
xanthene
Mast cell
stabilizers
Aerosol
corticos-
teroids
'5t \. yo d.
~--:-::-:-~~/ a. V., La:
~eophylli.ne
Fluticasone
Beclamethasone
antagonist
PR~r'-I-----"';;;=;-----J
Leukotriene
receptors
antagonist
Inhibitory
of5-lipo /
Ammophyll~
rM-u-sc-ar-;--'n-;c'
~2-adrenergic
agonist
Anti-inflammatory drugs
ox~enas~
enZ)'
2...~ l( S
()\.os.~
\0'0
Ii
Zafirlukast
Montelukast
I z;yu~
,
S~>-t
:,nort actmg
Albuterol (salbutamol)
Isoproterenol
Isoetharine
Metaprotereno]
T
Long acting
Fonneterol
Salmeterol
~Tj]jrigi9giOi.rs"---------------lN~,,\vvrtlt< ~ CO P D
Early asthmatic response- Symptoms only (i.e., bronchoconstriction)
Cold ai r
Exercise
Emotional stress
Late asthmatic response- Worsening asth ma
Allcrgens (Pollens. cockroach, molds, animal dandur)
Respiratory viruses
Occupational chemicals
Drugs - ASA, NSAIDs
Food additives - sulfites, tartrazine
Air pollution (including cigarette smoke)
GERD
Sinusitis
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~ ~~
c.....tto
~'--'
Q(5
c::::::
-.
Salmeterol
""~
Fonnoterol (short ~ I- 3 min and long duration 12 hours)
Mechanism
Bronchodilation
Vasodilatation
Slightly decrease peripheral resistance
Increase muscle and liver glycogenolysis
Relax uterine muscles
Increase release of glucagon
Therapeutic use
Treat Asthma
SE
Salbutamol (Ventolin)
Mechanism
Therapeutic use
Side effects
Recommendation
Contraindication
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10-20 minutes
Duration of
bronchodilation
4-5 hours
Salmeterol (Serevent)
Mechanism
Therapeutic use
Side effects
Drug-drug intemclion
Metaproterenol (Alupent)
Mechanism
Therapeutic use
Asthma
5-10 Minutes
Onset of
bronchodilation
Duration of action
4-5 Hours
Terbutaline (Bricanyl)
Mechanism
Therapeutic use
Side effects
Drug-drug
. interaction
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Corticosteroids
Corticosteroids
Mechanism
Therapeutic use
Side effects
Recommendation
Combination
products
PrednisoneJPrednisolone (Inflamase)
Mechanism
Therapeutic use
Side effects
Drug-Drug interaction
Recommendation
Fluticasone (Flovent)
Mechani sm
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Mechanism
Therapeutic use
Side effects
Monitoring
Periodic checks of adrenal funct ions may be required if large doses are
being taken.
Therapeutic use
Side effects
Drug-Drug
interaction
Ketoconazole and other azole antifungals can increase the blood level
of oral Budesonide.
Monitoring
Beclomethasone (Qvar)
Mechanism
Therapeutic use
Side effects
Recommendation
Monitoring
When large doses are being used, periodic checks is required to ensure
that the adrenal glands are functioning healthy.
Anticholinergics
Ipratropium Bromide
Atrovem
Mechanism
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Therapeutic use
Side effects
Onset of effect
515 minutes
Duration of action
8 hours
Tiotropi um (Spiriva)
Combivent
All MDI
Leukotriene inhibitors
Zafirlukast
Mechanism
Leukotriene inhibitors
Inhibitors ofLTC 4 and LTD4 receptors
Steroid sparing properties
Therapeutic use
Side effects
Drug.Food
interaction
Montelukast
Singulair
Chewable tablets and G ranules
Mechanism
Therapeutic use
Side effects
Headache
Nausea and diarrhea
Abdominal pain
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Drug-Food
interaction
Therapeutic use
Antiinflammatory action
Chronic asthma----mainly decreases symptoms
Bronchitis and emphysema
Use as a preventive measure, and is added to standard therapy
Side Effects
Recommendation
Monitoring
-.
Periodic checks on blood levels are requires especially the Serum level
Theophyllines are contraindicated in patients with hypersensitivity to
xanthine compounds.
Cuation in patient with peptic ulcers and seizure diseases
Increase theophylline clearance (decrease levels): age: 1-9 years, '::,
High protein diet, smoking (tobacco, Qlarijuana), fever, drugs such as
carbamazepine, Phenobarbital, phenytoin and nfampl~
.
Decrease theophylline clearance (Increase levels): Age (elderly,
infants, under 6 months age, premature neonates), CHF, Fatty food,
High carbohydrated diet, Liver dysfunction and Drugs such as: Oral
contraceptives, Non selective beta blockers, CCBs, Macrolide antibiotics,
Clindamycin, Zafirlukast, Allopurinol.
~obllr1J
tartmmillipirle
RrtamplCln
cyt:losporin
l'
Theophylline
ke:Dc~naztll
~,~
smoking
U
phenytoin
anbcoagulam
~~~nitidlne
ropilll'(Jloi
"
ftuconilzol
obesity
lmonary aedema
COf'
allopurinol
uncosul'llic drugs
Erylhromyt:in
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Side Effects
EMPHYSEMA is a disease in which the small air exchange sacs (alveoli) in the lungs become
permanently enlarged and damaged (alveoli walls destroyed) decreas ing oxygen absorption and
resulting in shortness of breathe.
CHRONIC BRONCfITTIS is an inflammation of the airways in the lungs that causes your lungs to
produce excessive amounts of mucus (phlegm). This reduces the flow of air to the lungs .
Onset age 45 years
Risk Factors that Cause COPD
Smoking (8090%)
Family History
Occupational exposures to ceI1ain ducts and fumes
Air Pollution
Second Hand Smoke
Asthma
Drug used for the treatment of CO PO
PDt:.
Theophylline inhibit activity of -7
Leukotrienes are chemical derivatives of -7
""L,,<J::;;:;
!\ y<>--.i.; JO",I'C
AuJ
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l~ t 01-\..\ O~ t:..4 ~
Patient has COPD and pneumonia, what is DOC -7 O()"'\'\'0 ~~: -4 0'- "2...~ ~'( v \0....."" "KOral contraceptive effect on theophylline -7
l-.Q.~.J~
Dry cough is caused by accumulation of -7 ~T ......J,.qk\'" 1l-\3
What is differentiating symptoms of-asthma from CO'P'D -7
'.J ~<....t. L.. J;
Smoking is very high risk factor for -7 COPD
U
What asthma devices do not require shaking 7, 1I \ c:;, I< ~ ~ '\::"''':r
~ 0
Polycythemia -7
R. I!>c-'> ll..,,,,,,boV, ~ OL str.,.Q,(
<..
~
Asthma exacerbations are NOT triggered by~ H
1\ t....Y' ~
Q..
Obstruction of airways in lungs is referred as~ \'ry <;. ~
Pennanent enlargement of alveoli is referred as ~ Q...."-. P\..Q ~
Highest clearance of theophylline in which Me $fouP~rt l ~ q 'f r $
When can we use leukotriene inhibitors ~ '" '!Il::-QY'O\Q d.o~
What is important to counsel in patient using steroid inhalers ~ 'c
So--e....
Histamines are released from ~ ""o...~ ~
ba..\o~~,~What kinds of changes can you expect to see in aminophylline solutions exposed to air? ~ C \'\l~ 3u~
Uq:
l'
b _) l . . . t
l'
crt
\th
COMT
EIA
CO PO
CHF
CCB
Ventolin
Advir, Serevent
Alupent
Brenthin Bricanv l
Inflamase Pedia ril Win red
Flonase Flovent
Entocort Pulmicort Rhinocort Rh inocortA ua
Ati-Beclomethasone var Rivanase A
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33
Action of DNA
Damage DNA
I
I
Alkylation:
Mechlorethamine
Cyclophosphamide
Ifosfamide
Chlorambucil
Melphalan
Busulfan
Lomustine
Cannustine
Streptozolin
Cisplatin
Carboplatin
Dacarbazine
Procarbazine
Altretaminel
Hexamelhylmelamine
Mitomycin
Others
Actinomycin 0
Etoposide
Teniposide
Amsacrine
I Free
radicals: I
Bleomycin
Inhibit
synthesis or
functions
A,,~ b;~IC
Topoisomerase
inhibitors
Doxorubicin
Daunorubicin
Topotecan
lrinotecan
I
Antimetabolites
5f1uorouracil
Cytarabine
Mercaptopurine
Thioguanine-Thioguanine
Methotrexate
Action on steroid
Hormones
Agonists
Androgens
Estrogens
Progestins
Lcuprotide
Goscrclin
Narfarclin
Atagonist
Tamoxifen
Toremifcnc
Flutamide
Anastrozole
Letrozole
Cancer estimated
deaths in men
Cancer estimated
deaths in women
Warning signs of
cancers
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Cell Cycle Phases
G1 : synthesis of
cellular componenlS
required for mitosis
I s:replicated
DNA is
phase ~
radiation,
G,: resting
state where cell
is not dividing
h/1
G/ : synthesis
of ellZ)mes
necds for DNA
smthesis
~
~
Class
Examples
Mechanisms
Melphalan, Chlorambucil,
Cisplatin, Carmustine
Antimetabolites
Fl uoroucil, Methotrexate
cytarabine, Mercaptopurine
fludarabine
Antibiotics
Doxorubin, Bleomycin,
Mitomyci n C, Dacti nomycin
Mitotic inhibitors
Vincristine, Vinblastine,
Paclitaxel . Docetaxel
Topoisomerase
inh ibitors
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Alopecia is a counseling issue! The extent of hair loss varies, but is usually starts at 2-4 weeks and
is reversible when the drugs are discontinued. Doxorubicin and paclitaxel tend to cause the most
alopecia, but it is common with most combination regimens. Patients may wear wigs, hats, or may
just go bald.
Neurotoxicity: Vincristine has as its dose-limiting toxicity autonomic dysfunction and peripheral
neuropathy, both sensory and motor.
Pulmonary toxicity; Bleomycin causes a generally irreversible pulmonary fibrosis at higher lifetime
doses.
Clophosphamide (Cytoxan)
Mechanism
Therapeutic use
Side Effects
Drug-Drug
interaction
Contraindication
Monitoring
Side effects
Doxorubicin (Adriamycin)
Mechanism
Therapeutic use
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Side effects
Irreversible cardiotoxicity
Myelosuppression
Stomatitis
Alopecia
Nausea and vom iting
Compounding
Dactinomycin (Cosmegen)
Mechanism
Anticancer antibiotics
Form stable DNA complex and interfere with DNA dependent RNA polymerase
Side effects
Mechlorethamine (Mustargen)
Mechanism
Alkylating agent
Therapeutic use
Side effects
Side effects
Myelosuppression
Paralytic ileus
Alopecia
Stomatitis
Paclitaxel (Taxol)
Mechanism
Side effects
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Chemotherapy
c9.J
The treatment of cancer with drugs is called chemotherapy. Antineoplastic drugs, also referred to as
chemotherapeutic agents, are drugs that are used to treat cancer.
Side effects of chemotherapy:
Acute:
Extravasation (effects the adjacent tissue)
Vessicant drugs (damage to tissue / necrosis) Example: Bleomycin, cisplatin,
dactinomycin, domorubicin, vincri stine, vinblastin etc.
Thrombophlebitis (inflammation associated with thrombus): Patient with cancer can
develop thrombosis after chemotherapy. Due to activation of fibrinogen.
Hypersensitive reactions. Example: Etopisi de, peclitaxol, ritux.imab, trastuzumab.
Rapid tumor lysis syndrome
Nausea and vomiting
Alopecia is the loss of hair: Drug that cause alopecia is doxorubicin, daunorubicin,
cyclophosphamide, vincristine, and paclitaxel.
Vessicant agents include: dactinomycin, doxorubicin, mechlorethamine, mitomycin, vincristine, and
vinblastine.
Hair regrowth occurs after \-2 months after stopping chemotherapy.
Xerostomia: Dry mouth is one of the most common complication associated with radiation therapy.
Reversible after 6-12 months of therapy.
Can be managed by: Sugar free hard candy, chewing sugar free gum stimulate salivation.
Commercially available saliva substitute. Ice chi ps . Cholinergic agonist ~ Pilocarpine Smg tab.
Bone marrow depression (Myelosuppression):
Bone marrow depression ~ Neutropenia, Thrombocytopenia
Neutropenia 7 treated by colony stimulating factors (O-CSF and OM - CSF): Filgrastim or
pegfiJgrastim
Thrombocytopenia ~ for prevention use Oprelvekin (Inerleukin-ll)
Complications: Bone marrow suppression is the most dose limiting side effect of cancer
Myelosuppression in general the onset is 7 ~ 10 days and peak is I 0 ~ 14 days. Recovery count
occurs usually occurs in 2 ~ 3 weeks.
Megaloblastic anemia by methotrexate ~ Fo l inic acid (leucovorin, 5-fonnyltetrahydrofolic acid)
Neutropenia associated anticancer drugs ~ can be treated by filgrastim (human granulocyte
colony stimulating factor)
Least bone marrow depression anticancer drugs is: Bleomycin
Cancer patient with anemia -7 Erythropoeitins are useful
Cardiotoxicity:
Ri sk ofC HF, commonly seen with doxorubicin, daunorubicin. epirubicin, mitoxantrone.
5-FU, capecitabine; Cause coronary spasms, mimicking a myocardial infarction (avoid in know
coronary artery disease patients)
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Pulmonary toxicity:
Pneumonitis, pulmonary fibrosis commonly seen with Bleomycin, Cannustine, Cyclophosphamide,
Mitomycin, Methotrexate, vinca alkaloids,
Symptoms of pulmonary toxicity include: SOB, non-productive cough, and rarely low grade fever.
Neurotoxicity:
Common with vincristine, vinblastine, Cytarabines, Methotrexate (very little), 5FU, interferon
alpha
Peripheral neuropathies associated with: Vincristine, peclitaxel: Peresthesia (numbness and
tingling) can occur with vincristine, which often appears within few weeks of therapy.
Hi gh dose of cytarabin may produce cerebllar toxicity that manifest initially as loss of eye-hand
coord ination and progress to coma.
Fludrabine cause severe neurotoxicity
Caramustine and other alkylating agents cause little or no neurotoxicity.
GI toxicity
Mucositis or stomatitis:
Mucositis: Generalized burning, and pain on the ventral surface of tongue. Floor of tongue, mouth
looks erythromatus.
Stomatitis: generalized inflammation of oral mucosa.
Mucositis or stomatitis: Common with Doxorubicin, Methotrexate, 5-Huorouracil, Actinomycin,
Bleomycin capecitabine.
Recommend mouth hygiene, xylocaine, viscous sucralfate, nystatin, sod ium bicarbonate, for
severe cases pelifonnin (growth factor) can be used.
Avoid alcohol, antihitamine, steroids, spicy food
Mucositis treatment and prevention:
Topical anesthetics: Viscous Lidocaine, or dyclonineHCL 0.5 or 1%
Corticosteroid provide anti-inflammatory action
Capscisin: Produces burning and pain and ultimately desensitizes pain.
Sucralfate suspens ion may provide benefit by coating.
-For Localized effect: use benzocain in orabase
Mucositis prevention:
Chlorhexidine gluconate 0.12% (peridex, Periogard) may reduce severity and frequency
of mucositis infections.
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Hepatotoxicity
Hepatotoxicity monitor LFT, jaundice, or hepatitis: Asparaginase, cytarabine, mercaptopurine, and
methotrexate.
Nephropathy:
_
Elevate BUN and electrolyte abnonnalities: methotrexate may precipitate in kidney. Cisplatin and
streptozocin. Amifostine..may be used to protect the kidney from the...nephrotoxicity associated
with cisplatin.
Sexual dysfunction:
Cyclophosphamide, melphalan, and procarbazine associated with significant infertility in men and
women.
Hemorrhagic cystitis G-It is a bladder toxicity that is seen most commonly after administration of cyclophosphamide and
ifosfamide.
These drugs produce a metabolite called acrolein, w~ ich cr u ~e chemical irritation in bladder
mucosa, resulting in bleeding.
\.--"J b~
Hemorrhagic cystitis caused by Acrolein can be prevented by excessive hydration and subsequent
frequent urination. The other method is by administering uroprotecting agent called MESNA,
which bind acroleine and prevent from contacting the bladder mucosa.
Pulmonary toxicities:
The most common with bleomycin, mitomycin, cannustine
Rationale for combination therapy: Overcoming or preventing resistance, Cytotoxicity to resting and
dividing cells' Biochemical enhancement of effect. Beneficial drug interactions' Rescue host cells
Some agents can be administered intrathecally: Methotrexate, Cytarabine' Thiotepa
Warning: Vincristine should be labelled as Intravenous only. Intrathecally vincristine causes death.
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'S\.(~~
Melonoma is ?
r
Metoc!opramide and dexamethaso,(lc are more effective Rausea r~lated, to ? e.o
~ ~ "
Methotrexate is used for ?
t\ 1 c........ ~) ,~S uT , c... S. i .s
f
Which anticancer d..(ugs cause pulIl,lonary fibrosis~ ~~:..- ~ u:J.....-4Il _ ~ 0 . f\
Hypenropy is -7
L.Q.~'"'~ ~~SI:;"'O -. r --::;~
Hyperplasia is -7 l'
'#-_
~
.
J ,,--, \.0 .....
Least emetic anticancer drug is ~ l'
0.' {o.......... I:l~
Cancer patient on cancer fihemotherapy, reports shortness of breath, non productive cough, she
may be using drug ~ b~
DOC for delayed Nausea and vomiting ~
Mesna is ~
Doxorubicin preparation should be perfonned in ~
Hypertrepy-is -7
1iyperpIasia..i.s ~
Melatonin ~
Peclitaxel and docetaxel act on ~
c..
fl.--
'l'''''-U s,
<..o..U...
e, . .
'0" ,"-
CSF
LFT
MESNA
Alkeran
Leukeran
Platinol
BiCNU
Adruc il Carae Efudex Fluoronlex
Rheumatrex TrexaJl
Cvtosar
Fludara
Btenoxane
Mitozytrex Mutamycin
Oncovin Yincasar PFS
Velban
TaxotereT
Etopophos Toposar VePesid
Camotosar
Hvcamtin
Oncovin
Cytoxan Procytox
Purinethol
Adriamycin Rubex
Cosmegen
Mustargen
Taxol
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Gastrointestinal Drugs
34
Gastrointestinal Dru s
GERD
Mild GERD, relief of symptoms is with antacids, algi nates or non-prescription strength H1 RA.
Severe GERD: PPI are the Drug of choice. Use PPJ for 2 - 4 weeks
The goal is to raise the intragastric pH 4 during periods when reflux is likely to occur.
peptic ulcer.;
Gastric ulcers - Due to reflux since has weak pyloric sphincter
Duodenal ulcers - Excessive secretion from parietal cells
Acute stress ulcers (Curling's ulcer) - Tumors
Pathologic acid-hypersecretory states (Zollinger- Ellison syndrome)
Treatment of peptic ulcers
Neutralization of gastric acid a Antacids
Reduction of gastric secretion a H. antagonist, Proton Pump Inhibitors (PP I)
Cytoprotection a Sucralfate
Eradication of Helicobacter pyloria 2 Antibiotics + PPJ (triple therapy)
To eradicate H. pylori
Triple therapy: 2 antibiotics + 1 PPJ
Losee 1-2-3 A: Amoxicillin + Clarithromycin + Omeprazole
Losee 1-2-3 M: Metronidazole + Clarithromycin + Omeprazole
Quadruple therapy: Tetracycline+ Metronidazole + Bismuth subsalicylate + Omeprazole
Antacids
Antacids are used to treat stomach upset, acid indigestion (heartburn) and sometimes ulcers. They
are simple chemical compounds that are mildly alkaline, and some also act as chemical buffers. They
act by neutralizing stomach and coating the mucosal lining of the stomach. Simethicone is an agent
added to antacids that helps relieve gas.
Types of antacids
.
.
Aluminum
compounds
Has prolonged action and widely used especially for the treatment of
indigestion and dyspepsia.
Side effects: constipation.
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Gastrointestinal Drugs
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Mg bicarbonate
Na bicarbonate
Combined
preparations
Calcium Carbonate
Constipation
H?receptor antagonists
A,"
_r_
Gastrin
Histamine
AUOPine
M~receptor
Cimetidine
H , receptor
H2-receptor antagonists inhibit the action of a special type of histamine receptor present in the
stomach. Th is reduces the amount of gastric acid production, which helps heal ulcers.
H2 receptor
antagonists
Cimetidine (Tagamet)
Ranitidine (Zantac)
Famotidine (pepcid)
N izatidine (Axid)
Acid must be produced to digest protein
Gastric acid secretion is controlled by histamine from enterochromaffin-like
cells, acetylcholine neurons and gastrin-G cells in the antrum
Therapeutic use
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Gastrointestinal Drugs
Side effects
Tips
Ranitidine (Zantac)
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Advantage from
other drugs
Sore throat/fever
Cimetidine
Mechanism
Therapeutic use
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Gastrointestinal Drugs
Side Effects
Diarrhea
Dizziness
Drug-Drug
interaction
Contraindication
Discuss with physician about using the drugs for pregnant and
lactating mothers.
Mo nitori ng
PPJ
Omeprazole
Lansoprazoie
Rabeprazole
Pantoprazole
Mechanism
Therapeutic use
Duration
Side effects
Abdominal pain
Diarrhea
Headache
Omeprazole (Losee)
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Rash
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Gastrointestinal Drugs
Lansoprazole (Prevacid)
Mechanism
Therapeutic use
Side Effects
Drug-drug
interaction
Contraindication
Mechanism
Therapeutic use
Side effects
Causes constipation
Dose
Dose Ig qid
Drug interactions
Bismuth Compounds
Mechanism
Therapeutic use
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Shoul d not be given in renal disease and pregnancy
Contraindications
GI disorder Tips
Lactulose is used in what type of chronic liver disorder ~
An example of ecosanide is~
Misoprostol is ~
Type of pain in GERD is ~
Increase in bilirubin cause ~
Aluminum salts can cause SE ~
Magnesium antacids cause SE ~
H pylori will cause ~
What type of hepatitis is chronic ~
What is treatment of hepatitis ~
NSA lDs induced ulcers can be treated by ~
Independent risk factors for peptic ulcers are: H.pylori and NSAI Ds
Chronic hepatiris?
Epsom salt is?
Ul cerative colitis occurs at?
Antiftatulance agent?
What vaccine can be used for traveler 's diarrhea?
Na bicarbonate is contraindicated in-patient with hypertension, CHF, severe renal disease,
and edema. This also contraindicated in ulcers.
CaC03 antacids have rebound acidity due 10 stimulation of acid secretion.
CaCOJ antacids avoid in hypercalcemia patients .
Hypophosphetemia and osteomalacia can occur with long-tenn use of Aluminum containing
antacids.
Antacids bind with Tetracyclins, and fluroqu inolone and reduce absorption.
Antacids may destroy coating of enteric-coated drugs.
Mg antacids can cause cathartic SE.
GERD
Losee
Prevacid
Tagamet
Axid
Zantac
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35
I
Cell Wall synthesis
inhibitors
Peni cillins
Cephalosporins
Vancomycin
Protein Synthesis
inhibitors
Am inoglycosides
Macrol idcs
Tetracycline 's
Lincosamide
I
DN A Synthesis
inhibitors
Quinolonesl
Fluoroquinolones
Metronidazole
Penicillins
Acid labile (ac id sensitive)
Penicillin G ......... J!-lactamasc sensitive
Methicillin ........ . ~- lactamase resistant
Nafcillin .... .. ... .... ~-lactamase resistant
Penicillin G
Penicill in V
Methicillin
Nafcill in
Oxacillin
Carbenicillin
Ticarcillin
Piperacillin
Aminopcnicillins
Amox icillin
Ampicillin
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Mechanism
Therapeutic uses
Side effects
Penicillins G
Mechan ism
Therapeutic uses
Side effects
Side effects
management
Drug interactions
Penicillin V
Mechanism
Uses
Side Effects
SE management
Drug interactions
Side Effects
Drug interaction
Amoxicillin (Amoxil)
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Therapeutic use
Gram + ve (mainly)
Gram - ve Ne isseria
Synergi stic effect with aminoglycoside
Side Effects
Hypersensitivity, Anaphylaxis
GI affects ~ Nausea& Vomiting, P Colitis (diarrhea).
Blood related ~
Thrombocytopenia
Leucopenia
Agranulocytosis
Drug interaction
Allopurinol-Increases rashes
Honnonal contraceptive-Decreases contraceptive effect.
Methotrexate-effects renal tubular absorption.
Ampicillin (Principen)
Clinical use
Gram + ve (mainly)
Gram -ve Neisseria
Drug interaction
- Side Effects
Hypersensitivity, Anaphylaxis
Gl -7 Nausea & Vomiting, P colitis (diarrhea).
Blood related ~ Thrombocytopenia
Leukopenia
Agranulocytosis
Cephalosporins
1 a.generation
Cefazolin
Cephalothin
Cephalexin
Cephapi rin
Cephrad ine
f.Dd.generation
Ccfadroxin
Oral
Cefaclor
CefamandoJe
Cefoxitin
Cefuroxime
sodium
Cefuroxime
auxetil
oral
Cefotetan
Cefproxi l
Oral
Cefonic id
Loracarbef
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lni.generation
Contain
methy lthiotetrazo le
side chain. Can cause
hypoprothrombonemia
and bleeding problems
Ilh.generation
Cefixime
Cefoperazone
Oral
Hepatic elimination only
Cefotaxime
Cefpodoxime
Ceftazidime
Ceftriaxone
Cefdinir
Oral
Ceftibuten
Oral
-+ Single dose
Cefepime
Cephalosporins _1 st Generation
I II Generation
Therapeutic use
Side effects
Dose
Cefazolin
Cephalothin
Surgical prophylaxis (best for Gram + ve)
Allergic reaction (5- 15%)
Anaphylaxis
Skin rash
Fever
Hemolytic anemia
Granulocytopenia
Local irritation at site of injection.
Seizure in high doses in IV form
IV and PO
Clinical use
Side effects
Dose
Cefaclor
Cefamandole
Cefoxitin
Cefuroxime
Gram Ave coverage.
Parenteral administration except cefaclor
Allergic reaction (5 -15%)7 Skin rash, Anaphylaxis
Fever,
Local irritation at site of injection
Blood related 7 Hemolytic anemia, Granulocytopenia
IV and PO
Cephalosporins-3 rd Generation
3'" Generation
Cefixime
Cefoperazone
Cefotaxime
Cefpodoxime
Ceftazidime
Ceftriaxone
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Clinical use
Side effects
Dose
Cefepime
Best for Gram -ve
Higher potency
Side effects
~ose
LVand~
Vancomycin (Vancocin)
Mechanism
Therapeutic use
Side effects
Precautions
Dosage
GI
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Pfizerpen
Beepen-VK, V-Cillin-K, Veetids
Pipraci l
Amoxi!, Dipermox, Trimox
Principen
Vancoc in, Vancol ed
Ancef, Kefzol
Keftin
Cec1or, Ceclor CD, RanicJor, RanicJor
Mefoxin
Alti, Ceftin, Kefurox, Zi nacef
Velosef
Duricef
Mefoxin
Ceftin
Cefotan
Cefzil
Lorabid
Suprax
Cefobid
Claforan
Banan, Vantin
Ceptaz, Fortaz, Tazicef, Tazidime
Rocephin
Omnicef
Rocephin
Cedax
Maxipime
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36
I
I
Chloramphenicol
Lincosamides
Clindamycin
Lincomycin
Aminoglycosides
Gentamycin
Streptomycin
Kanamycin
Macrol idcs
Erythromycin
Azithromycin
Clarithromycin
Tetracyclines
Oemec1ocycline
Doxycycline
Minocycline
Aminoglycosides
Gentamicin, Streptomycin, Tobramycin, Kanamycin, Amikacin
Phannacokinetics
All am inoglycosides renally eli minated
Halflife 2 - 4 hours .
Post dose antibiotic effect (PDAE)
Only k anamycin and neomycin have oral and topical
Commonly aminoglycosides used as 1M or IV
Streptomycin has only 1M
Pharmacokinetics is not completel y understood
Contain aminosugars structures and have low bioavailablity
Pri marily used in infections associated w ith gram - ve.
Aminoglycoside have little activity against anaerobic.
Gentamicin (Garamycin)
Therapeutic Uses
Gram-ve
Drug uptake depends of oxygen: active against aerobes
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 31d) to reduce resistance
Side Effects
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Streptomycin
Uses
Gram -ve
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 3rd ) to reduce resistance
Side Effects
Ototoxicity
Streptomycin = Kanamycin> amikacin = gentamycin = tobramcycin > netilmycin
Tobramycin (Tobrex)
Uses
Gram -ve
Second line treatment for tuberculosis (mainly streptomycin)
Treatment for plague (streptomycin).
Pseudomonas (streptomycin)
Combined with cephalosporins (2nd and 3rd ) to reduce resistance
Side Effects
Amikacin (Amikin)
Uses
Gram -ve
Second line treatment for tuberculosis (mai nly streptomycin)
Treatment for plague (streptomycin).
Pseudnmnna.~ (streptomycin)
Combined with cephalosporins (2 nd and 3rd) 10 reduce resistance
Side Effects
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Ototoxicity symptoms associated with gentamycin and streptomycin are: Vestibular damage this
can cause T innitus, vertigo, and ataxia.
Ototoxicity symptoms associated with ami kacin and kanamycin are: Auditory damage this can
cause hearing loss.
Tobramycin can cause both vestibular and auditory damage
To prevent serious side effects associated with aminoglycosides monitor: Blood drug levels,
BUN, Serum creatinin levels
Blood levels are monitored by peak and trough levels:
Trough levels of gentamycin greater than 2mcglml can cause nephrotox ic .
Macrolides
Erythromycin. C larithromycin, Azithromycin
Pharmacokinetics:
All of macrolides hepatical ly eliminated, except: clarithromycin, which is renally el iminated.
All macrolides have oral dosage and erythromycin gluceptate and lactobionate is IV.
Azithromycin has long half-life 68h and used single daily doses.
Erythromycin has short half-life 1.2 - 2 .6 hours .
Erythromycin are preferred drug for treatment of Mycoplasma infection.
Important alternate in patient allergic to penicill ins
Erythromycin estolate may cause cholestatic jaund ice in-pati ent used more than 10-14 days.
( Resolved after d iscontinued treatment)
Erythromycin is inhibitor ofCYP3A4, thereby potentiates toxicities of drugs that are metabolized
by CYP3A4. eg: digoxin, corticosteroids, lovastatin or CALS), Carbamazepine.
Clarithromycin increase warfarin INR (monitor PT), increases digoxin and theophylline levels.
Azithromycin is more active against gram - ve H .influenza than erythromycin.
Clarithromycin is effective for H .pylori (used along with PPls in triple therapy)
Erythromycin
+ ve (all of them), Gram -ve for Neisseria
Use
Gram
Side effects
Drug
Interactions
Clarithromycin (Biaxin)
Use
Side Effects
Contraindication
Azithromycin (Zithromax)
Use
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Side Effects
Epigastric distress.
Oral has less N and V.
Contraindicated
Counsell ing
Tetracycline
Tetracycline
Therapeutic Uses
Acne treatment
Chlamydia (lymphogranuloma, Psittacosis)
Rickettsia (Rocky mountain spotted fever)
Mycoplasma pneumonia
Lyme disease
Side Effects
Contraindication
Counselling
Doxycycline
Uses
Broad spectrum
Prophylaxis in travellers diarrhea
Lyme disease, Chlamydia (lymphogranuloma, Psittacosis), Rickettsia (Rocky
mountain spotted fever)
Mycoplasma pneumonia
Side Effects
Gastric discomfort.
Effect on calcified tissues (deposition in the bone and primary dentination
occurs during growing children.
Discoloration and hypoplasia of the teeth and temporary stunting of growth,
Fetal hepatotoxicity
PhototoxicitySevere sunburn
Super infection (over growth of candida in vagina or resistance to
Staphylococcus in intestine)
Contraindication
Counseling
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Minocycline
Minocycline
Therapeutic use
Side Effects
Less phototoxicity
Vestibular problems: dizziness, nausea, vomiting
Pregnancy, breast-feeding, children under 8 old
Contraindication
Clindamycin
Clindamycin
Uses
Side Effects
Contraindication
Counseling
Precaution
Biaxin
Azasite Zithromax Zmax
Emtet Panmycin Sumycin Tetra 250
Adoxa Pak Atridox Bio-Tab Doxy
Cleeravue Dvnacin Minocin Mvrac
Dalacin Clinacin Cleocin Evoclin
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37
3"'
Gatifloxacin
Moxifloxacin
Levofloxacin
4th Travofloxacin
Therapeutic Uses
UTI 7 E.coli
STD -7 Gonorrhea
Respiratory 7 alternate to ampicillin in pneumonia
G I infections 7 E.coli travellers diarrhea
Nephrotoxicity
Cartilage toxicity-Avoid under 18years and pregnancy
Tendonitis/tendon rupture-common in elderly and renal failure patient
Most common: Nausea and Vomiting, light-headedness.
Side Effects
Counseling
With or without food. The preferred time is 2 hours after meal (for faster
absorption)
With full glass of water. (avoid dairy products)
Avoid taking with antacid, iron, or calcium together
Phototoxicity
Ofloxacin (Floxin)
Mechanism
Uses
Mainly for E. coli in UTI and STD with exception syphi lis.
Alternate in gonorrhea
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Side effects
Counseling
Gatifloxacin (Tequin)
Mechanism
Therapeutic use
Side Effects
Q-T prolongation
Drug-drug
interaction
Contraindication
Monitoring
Metronidazole (Flagyl)
Metronidazole
Mechanism
Therapeutic use
Side effects
Drug-Drug
interaction
Precautions
Pregnancy and
lactations
Dosage
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38
Sulfamethoxazole
Sulfadiazine
Sulfisoxazole
Sulfasalazine
Trimethoprim
Combination
drugs
Cotrimoxazole
Mechanism
Folate Antagonists
Therapeutic Use
UTI ~ E. coli
Drug of choice in Traveller diarrhea
Trachoma-chlamydia trachoma-most
common cause of preventable blindness
Topical: Bums and wounds
Side effects
Counseling
Ptcridinc + PABA
1--Dihydroptcroic acid
1-
Dihydrofolic acid
""=;:
=-:':::::i.
1
l ~;on;~
THF cofactors
Thymine
DNA
Purines
DNA
Glycine
f-mct-tRNA
Proteins
Sulfasalazine (Salazopyrin)
Mechanism
Therapeutic use
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Side effects
Drugdrug
interactions
Monitoring
Periodic test of blood composition and liver function are usually required.
Blood disorders may occur with prolonged use of this drug.
Side effects
Counseling
Contraindications
Antibiotics Tips
Steven-johnson's Syndrome: Rash, sk in peeling, and sores on the mucus membrane. In Steven
Jhonson's syndrome, a person has blistering of m ucus membrane, typical ly in mouth, eyes and
vagina. Patchy areas of rash. SJS can occur in all age groups .
Due to: SASPAN
Sulfonylurea
Anticonvulsant (phenytoin)
Sulphonamide
Penicillin
Allopurinol
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NSA lDs
Sulfa drugs ~ Stevens Jhonsons Syndrome
Topical sulfa is contraindicated because it may cause disease like SJS, this disease is life threaten ing.
Treatment of SJS is Cortisone
Summary of Cell wall synthcsis inhibitors
Methicillin is only IV and 1M
Penicillin G benzathine has long half life ~
Naficillin is mainly hepatic elimination
Beta lactamase sensitive drugs: Pen G, Amoxi, Pen V and Ampicillin
Endocarditis prophylaxis is (Dental extraction prophylaxis) ~
A child less than 2 y allergic penicillin, what is the drug choice for otitis media treatment ~
A patient has heart diseases and undenvent prostatic valve surgery. Dentist plans to tooth
extraction, what antibiotic is suitable for endocarditis prophylaxis ~
Chewable antibiotics ~
Beta lactams that should be taken empty stomach ~
Aminopenicillins are:
Penicillin allergic patient, alternate drug of choice is?
Penicillins are ineffective in treatment of bacterial infections associated with ~
MRSA infections are treated by ~
P.colitis associated diarrhea is treated by ~
Bacteria is inhabitant in GI, what location ofGl tract is commonly fou nd ~
Type of bacteria mainly present in colon is ~
Macrolides Practice Test
Azithromycin suspension stored at 7
Clarithromycin suspension stored at -7
Which macroli de suspension have to refrigerate after reconstitution ~
What antibiotics should caution and require monitoring in patient receiving warfarin What antibiotic potentiate the effect of digoxin and can cause digitalis toxicity 7
Azithromycin is the drug of choice in traveler diarrhea for patient travel ing to ~
Tetracyclin Practice Tests
Tetracyclin are contraindicated are contraindicated in pregnancy and children.
Tetracyclin can stain teeth and discoloration.
Oral or topical tetracycline are drug of cho ice for acne treatment
Tetracyclin MUST BE taken empty stomach.
Tetracyclin binds ~
GI distress (abdominal discomfort, diarrhea) most common SE. This can be resolved by taking
with food or decreasing dose.
Expired tetracycline can lead 7
Doxycyclin is the DOC ~
Doxycyclin should be taken ~
Minocyclin may take with or without food.
Phototoxic reactions (sever skin lesions) can develop with exposure to sunlight. Photoxicity is the
most common with doxycyc1in or demec1ocyc1in.
Epimerization is a ~
Tetracyclins = Take empty stomach
Doxycyclins = Take with or after food
Minocyclins = Regardless of food
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THF
SMX
TMP
UTI
GAS
1M
JNR
rin EnTabs
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Antifungals
39
Antifungal agents
Mechanisms of Action and Classification of Antifungal Agents
Antifu gat Agents
After cell me1brane permeability
Azolr5
AlIyl. mint
Terbinafine
Nftftifin"
lm idazoles
.. Ketoconazole
.. Miconazole
- ClouimazoJc
Systemic
antifungals
Topical
Antifungals
Tria7.oles
P oly tnt
mRnol idt
a ntibiotic
Pyriml din t
An a log
I
I
Aucytosinc
Ptnir ill in
dtriva li vt
I
I
Griseofulvin
.. Amphotericin B
-Nystatin
Auconawlc
Itraconawle
Terbinafine hydrochloride
Antifungal Antibiotics
Amphotericin B
Amphotericin B (lipid-based)
Griseofulvin
Echinocandins
Caspofungin acetate
Imidazole
Ketoconazole
Pyrimidi nes
Flucytosine
Triazoles
Fluconazole
Itraconazole
Allylamines
Naftifine hydrochloride
Terbinafine hydrochloride
Antifungal Antibiotics
Nystatin
Imidazoles
Clotrimazoles
Econazole nitrate
Ketoconazole
Miconazole nitrate
Oxiconazole nitrate
Tioconazole
Chlorphenesin
Ciclopirox olamine
Clioquinol
Selenium sulfide
Tol naftate
Undecylenic acid
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Antifungals
Amphotericin 8 (Fungicidal)
Therapeutic use
Mechanism
Bind to ergosterol from pores resulting in the leakage of cell ular contents
Side effects
Contraindication
Allergies
WARN ING
Drug interaction
Prccauti"on
Counselling
When applying topicals on the skin, protect nails and clothes as it may stain
References
Nystatin
Category
Therapeutic use
Mechanism
Side effects
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Antifungals
Advantage
Drug interaction
Precaution
Counselling
Reference:
Ketoconazo!
Imidazole type antifungal
Inhibitor Ergosterol synthesis
Not a single dose
Doesn't penetrate eNS
SE: Hormonal effects such as gynecomastia and
menstrual disturbances
Interaction with cimetidine, antacids
Require acidic conditions for absorption (avoid
antacids concomitantly)
Potent inhibitor ofCYP 3A4 (high) and CYP
2C9
Ketoconazole taken with food or after food
(with cola beverage if achlorhydric or on acid
secrete suppressor)
Ketoconazole (Nizoral)
Ketoconazole (Imidazole type)
Miconazole; Clotrimazole
Therapeutic use
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Antifungals
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Mechanism
Side effects
Contraindication
Hypersensitivity; teratogenicity
WARNING
Precaution
Counsell ing
References
Fluconazole (Diflucan)
Mechani sm
Therapeutic use
Side effects
Skin Rash
GI Effects ? Nausea, Vomiting Diarrhea Or Commonly Causing G I
Disturbances.
Liver Effect ? Increase Liver Enzymes, Yellowing Of The Skin, And
Eyes, Flu-Like Symptoms,
CNS ? Dizziness, Headache, Exfol iative Skin Reactions, Altered Taste
Buds, Extreme Tiredness, Seizures.
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Antifungals
Drug interaction
Precaution
Reference:
Itraconazole (Sporanox)
Therapeutic use
Mechanism
Bl ock the synthes is of ergosterol 14a demethylase in the fungal CYP 450
complexz
Side effects
Contraindication
Warning
Cause CHF; heart attack; irregular heart beat! dse; lung! kidneylliver
disease or other serious problems; SOB; coughing up white phlegm;
weakness; excessive tiredness; fast heart beat; swelling ofthe feet, ankle or
leg; sudden weight gain
Drug interaction
Drug interaction
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Antifungals
Counselling
Oral solution: Sw ish 10ml (2tsp) in the mouth for a few seconds and
swallow. Repeat is necessary until entire dose is taken. The solution is
usually taken on an empty stomach once daily or 8lD for 1-4 weeks .
Tell Doctor if taking Itraconazole. Do not substitute the capsules for the
liquid because they have different use .
Reference:
Clotrimazole
Therapeutic use
Mechanism
Block the synthesis of ergosterol 14a demethylase in the fungal CYP 450
complex
Topical: blisters, edema, pruritus, burning, stinging, peeling skin tissue,
increase urinary frequency
Abdominal pain
Irritation
Abnormal liver function test in patient taking lozenge
Side effects
Contraindication
Management
Precaution
Reference
Miconazole
Category
Mechanism
Therapeutic use
Side effects
Contraindication
Sensitivity to any of the components of Miconazole, not for chi ldren> 2y/o
unless directed by a doctor, do not use for the infection of the nail
Drug interaction
Anticoagulants,
Phenytoin,
Terbinafine,
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Antifungals
Drug interaction
Atypical anti-psychotics,
Cyclosporins
Some statins
Availability
Application
Reference
Tolnaftate
Category
Fungistic, fungicidal
Mechanism
Therapeutic use
Side effects
Administration
Administration
Warning
Contraindication
y/o
Reference:
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Antifungals
Antifungals Tips
Nystatin is indicated -7
Ketoconazole require acidic conditions for higher bioavai lability therefore -7
Meningitis fungal infections other eNS infections can be treated bY-7
If a chi ld swallowed 5g of nystatin, and parents are panic, comes to your phannacy, what is
appropriate action -7
Nystatin is ineffective for -7
DOC for oral thrush-7
DOC for vaginal candidasi s
Topcal Drug of choice for Atheletes foot -7
Nystatin suspension counseling-7
Amphotericin - B is -7 act by inhibiting the cell membrane function
HTN
SJS
CSF
ACTH
AZT
OCP
NN RTI
IV
CYP
SOB
CBZ
BID
CPS
Fungistic, Fungicidal
Tri-Statin, Mycolog, Mytrex
Diftucan
Sppranox
Clotrimazole Cruex Lotrimin M celex
Aloe Vesta Cruex Desenex Jock Itch
Asorbine Afate. Genas ore Pitrex
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Ami-Mycobacterial Drugs
40
Anti-Mycobacterial Drugs
Antimycobacterial drugs
Isoniazid
Rifampin
Streptomycin
Pyrazinamide
Ethambutol
Capreomycin
Rifabutin
Tuberculosis treatment:
Goal of treatment is must eradicate mycobacterium.
Important issues in tuberculos is treatment are resistance to drugs .
.-Drugs that haveJowest resistancejs:lsoniazid, rifampin, streptomycin and combination of these
drugs with pyrazinamide, or ethambutol.
Drug of choice is combination of Isoniazid + rifampin + pyrazinamide.
Antimycobacterial Drugs
Rifampin
Chemical structure ofrifampin is a macrocyclin.
This drugs is bactericidal
Inhibits RNA synthesis
Mechanism
Therapeutic Use
Effective against M. tuberculosis, and M. leprae
Prophylactic for house hold members of exposed to meningitis caused by
meningococci or H. influenza type b
Side Effects
Seri ous liver toxicity (hepatotoxicity) thereby LIT should be performed
regularly
Gr SE: nausea, vomiting, abdomil!al pail!
CNS SE: Headache, drowsiness, confus ion, fatigue
Rifampin discolor urine, sweat, tears, saliva and feces to orange-red .
Drug interactions
Rifampin is inducer ofCYP IA2, 206, 2C9, 2C19, 3A4
Reduce efficacy oral contraceptive.
Isoniazid (INH)
Mechanism
Therapeutic Use
Side Effects
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Side Effects
Anti-Mycobacterial Drugs
Most common: Hepatitis: Most severe-fatal, the risk of hepatitis increases
with patient age and alcohol abuse. Monitor LFT
Blood dyscariasis (agranulocytosis, aplastic anemia, hemolytic anemia
Thrombocytopenia) thereby monitor CBC routinely
eNS toxicity due to decrease in pyridoxine levels: Administer 15 -50 mgldy
pyridoxine to minimize the peripheral neuropathy.
Symptoms of CNS toxicity are: insomnia, restlessness, hyperreflexia, and
convulsions.
Pyrazinamide (ZIN)
Mechanism
Therapeutic Use
Combination with INH and rifampin. Pyrazinamide has activity only against
M.Tuberculosis
Liver dysfunction
Urate retention .
May precipitate gouty attacks
Side effeclS
Antimycobacterials Tips
Drugs that discolor urine, tears, saliva, feces, sweat ?
Drug of choice to treat tuberculosis ?
Peripheral neuritis caused by isoniazid can managed by administering ?
XDR TB = Extensive Drug Resistance Tuberculosis.
All antitubercular drug should be taken on :
Isoniazid
Li ver Funtion Test
XDRTB
ZIN
CYP
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Anti-viral Drugs
41
Anti-viral Drugs
Antiviral Agents
Amant.din<
~Iovir
lidovudine
Ne,u apint
Rimantadirr
VolK)'Clow
Ganciclo, u
Didano<int
Delavitdint
Efavirenz
Neuroamindiase inhibitor
Osaltamavir
ZarJalllavir
Sl.wdin<
Antiretroviral
Amantadine
Ribavirin
Rimantadine
Zidovudine
Didanosine
Zalcitabine
Stavudine
Lamivudine
Nevirapine
Nucleoside Reverse
Transcriptase
Inhibitors (NRTI)
Foscarnet
Ribavirin
ACyclovir (zovirax)
NRTI
NNRTI
Lami" ..dint
Vidanbft
At.ca ....
Zalcilabino
TriOuridin<
lndina ....
Soquinaw
RitolUlvir
Ampre"" .....
Protease inhibitors
Zidovudine (AZT)
Stavudine
Lamivudine
Didanosine
Zalcitabine
Non-Nuc leoside
Reverse Transcriptase
Inhibitors (NNRTI)
Nevirapine
Efavirenz
Delavirdine
Protease Inhibitors
Saquinavir
Ritonavir
Indinavir
Mechanism
Therapeut ic use
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Anti-viral Drugs
Side effects
Advantage
Dosage
Oral
Topical (5% cream, ointment)7 Recurrent orolabial herpes infections
Antiretroviral drugs:
Retrovirus: Virus that contain reverse transcriptase enzyme such as HIV is referred as retrovirus
There are three classes of antiretroviral drugs: NRTl, NNRTI and Protease Inhibitors;
Nucleoside reverse transcriptase inhibitors (NRTI) phosphorylate by human cellular kinases .
Non nucleoside reverse transcriptase inhibitors (NNRTI}- phosphory late by human cell ul ar kinases.
Protease inhibitors : ! viral protease
Zidovudine (AZT)
Mechanism
Therapeutic use
Side effects
Didanosine (ddl)
Mechanism
Therapeutic use
Side effects
Monitor
Monitor 7 serum amylase and triglyerides
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Anti-viral Drugs
Zalcitabine (ddc)
Mechanism
Therapeutic use
Side effects
Monitor
Avoid
Stavudine (d4T)
Mechanism
-Side-effects
Monitor
Lamivudine (3TC)
Mechanism
Therapeutic use
Indicated to treat HIV and chronic hepatitis B in patients with active liver
inflammation
Side effects
Monitor
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Antiviral Drugs
HIV
AZT
HSV
RBC
ATP
RBC
Zovirax
AZT Retrovir
Videx Videx EC
Hivid
Zedt
Eoivir
Tamiflu
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Anti-Malarial Drugs
42
Anti-Malarial Drugs
Malaria is infection of red blood cells with the single-celled parasite Plasmodium, which causes
fever, an enlarged spleen, and anemia.
Four species of malaria parasites--Plasmodiumja[ciparum, Plasmodium vivax, Plasmodium ovale,
and Plasmodium mal(Jriae--can infect people.
Fa1ciparum malaria, caused by Plasmodium falciparum, is the most dangerous fonn of malaria and
can be fatal.
Blackwater fever is an uncommon complication of falciparum malaria.
Chloroquine is the drug of choice for treatment in a person who has malaria caused by Pl asmodi um
vivax, Plasmod ium ovale, or Plasmodium malariae--except in a very few areas where resistance to
chloroquine in people with Plasmodium vivax has been reponed.
Chloroquine is the preferred drug for prevention of malaria caused by Plasmodium falciparum in
Mexico, areas of Central America west of the Panama Canal, Haiti, the Dominican Republic, and
some areas of the Middle East.
Primaquine is added to kil! persistent parasites in the liver of a person infected with Plasmodium
vivax or Plasmodium ovale. Before primaquine is given, a blood test is done to look for a relatively
common enzyme deficiency (G6PD defic iency). People with G6PD deficiency who are given
primaquine may have a breakdown of their red blood cells.
Treatment of malaria
Prophylaxis
P. falciparum
P. malariae
Chloroquine
Chloroquine
P. vivax
Chloroquine + primaquine
P. ovale
Chloroquine + primaquine
Treatment
Retinopathy
Nausea, dizziness, and trouble sleeping, may rarely produce seizures
or psychiatric problems. Should al so be avoided in people with
certain heart conditions.
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AntiMalarial Drugs
Quinine
Atovaquone-proguanil
I Glucose-6-phosphate dehydrogenase
Ara;em
Radical cure
Adoxa Pak Adoxa. Alodox . Atridox Bio-Tab
Lariam
Malarone Malarone Pediatric
Oaraorim
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Travellers Diarrhea
43
Traveller's Diarrhea
Travellers diarrhea also known as infections diarrhea. Organisms commonly implicated in the
cause of Traveller's Diarrhea:
Escheri chia col i.
Shigella sp.
Compylobacter jejuni
Shigella diarrhea diarrhea characterized as dysentery (bloody diarrhea).
Effective drugs in the prevention of Traveller's Diarrhea:
Ciprofloxacin is the DOC for traveler's diarrhea.
Alternate DOC is Cotrimoxazole
Prevention~ Doxycycline or ciprofloxacin
Traveller to Thailand: Azithromycin is the DOC for traveler 's diarrhea
The antibiotic most commonJy recommended is ciprofloxacin.
Non prescription drugs:
Bismuth subsalicylate, a nonprescription drug. Causes black stools and tongue.
Loperamide (immodium): Treatment ofdiarrh"ea.
Bismuth subsalicylate can be used as prophylaxis or treatment. However loparamide is only used
upon appear of symptoms of diarrhea
When symptoms occur, treatment includes drinking plenty of fluids and eating a bland diet (for
example, cooked cereals, bananas, rice, applesauce, and toast). In addition, antib iotics (such as
ciprofloxacin) and antidiarrheal drugs (such as Lopramide or bismuth) are usually recommended.
Travelers are encouraged to seek medical care if they develop fever or blood in the stool.
I Drug of Choice
I lmmodium
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AntiHelments Drugs
44
Anti-HelminthicDrugs
Helminthic
Spec ies
Mode of
transmission
Treatment
Ascaris
lumbricoides
Round wonn
Ingestion
Pyrantel pamoate,
mebendazole
Necator
americanus
Hook wonn
Percutaneous
Pyrantel pamoate,
mebendazole
Trichuris trichuria
Whipwonn
Ingestion
Mebendazole
Enterobius
vermiculars
Pinwonn
Ingestioniinhalation
Strongyloides
Threadwonn
Ingestion
Pyrantel pamoate
Mebendazole
Thianendazole
Wuchereria
bancrofti
Filariasi s
Percutaneous
Diethylcarbamzine
Onchocerca
volvulus
River blindnessl
onchoceriasis
Percutaneous
Livermectin
Trichinosis
Ingestion
Thiabendazole
Taenia solium
Pork
Ingestion
Niclosamide
Taenia saginata
beef
ingestion
Niclosamide
Diphyllobothrium
latum
Fish
ingestion
Niclosamide
Hymenolepis nana
Dwarf
Intestinal
nematodes
Tissue nematodes
Ceslodes
(tapewonns)
Praziquantel, niclosamide
Trematodes
(flukes)
Schistosoma
mansoni
Schistosoma
haematobium
Blood
Clonorchis sinesis
Liver
ingestion
Praziquantel
Fasciolopsis
Intestinal
Ingestion
Praziquantel
Pragonimus
Lung
Ingestion
Praziquantel
Percutaneous
bilharziasis
Praziquanlel
Praziquantel
Mebendazole:
Mechanism: Inhibits microtubule synthesis and glucose uptake in nematodes
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Anti-Helments Drugs
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