Introduction to Pharmacology

Pharmacology
• the study of science of drugs
Drug
• any chemical that affects the processes of a living organism

I. Drug sources:
a. plants
b. animals
c. minerals
d. chemical synthesis/ biogenetic engineering

II. Drug uses:

• prevent diseases
• treat diseases
• diagnose diseases
• prevent pregnancy
• maintain health

III. Drug names

 Chemical name
o the drug’s chemical composition and molecular structure
o ex.( +/- ) – 2 – ( p-isobutylphenyl ) proponic acid

 Generic Name ( Nonproprietary name )

o name given by the United States Adopted Name Council
o universally accepted
o ex.ibuprofen

 Trade Name ( Brand name/ Proprietary name)

o the drug has a registered trademark ; use of the name restricted by the drug’s
owner
o ex. Motrin

IV. Drug Standards:

• same drug name must have same strength, quality & purity
• based on United States Pharmacopeia and National Formulary (USP-NF)

V. Drug references:
• American Hospital Formulary Service (AHFS) Drug Information
• Physicians’ Desk Reference (PDR)
• Package inserts
• Drug Facts and Comparisons
• Saunders/ Lipincott’s Nursing Drug Guide
• Journals
• Internet
VI. Phases of Drug Development
1. Preclinical trial
2. Phase 1
3. Phase 2
4. Phase 3
5. Phase 4

VII. Legal Regulation

A. Food and Drug Administration (FDA) Pregnancy Categories:

Category A  no risk to fetus

Category B  no risk in animal fetus; no human studies available
Category C  adverse effects to animal fetus; no human studies available
Category D  possible fetal risk in humans reported
Category X  fetal abnormalities reported; + evidence of fetal risk in animal/& human
studies.

B. Controlled Substances:
 controlled substances
 OTC drugs
 prescription drugs
 orphan drugs
  dependence

Drug Enforcement Agency (DEA) Schedules of Controlled Substances:

Schedule I Drugs
• high potential for abuse
• used for research only
• ex. heroin, marijuana, lysergic acid diethylamide (LSD)

Schedule II Drugs
• high abuse potential
• severe physical & psychologic dependence
• acceptable medical use, with restrictions
• ex. amphetamines, cocaine, mepiridine (Demerol) , morphine, anabolic steroids

Schedule III Drugs

• moderate potential for abuse
• psychological dependence , low physical dependence
• acceptable medical use, by prescription only
• ex. secobarbital (Seconal), Tylenol with codeine

Schedule IV
• low potential for abuse
• limited physical & psychological dependence
• ex. diazepam (Valium), phenobarbital, chlordiazepoxide (Librium)

Schedule V
• low potential for abuse
• acceptable medical use
• OTC narcotic drugs, sold only by registered pharmacists: buyer must be 18yo
• Ex. cough syrups with codeine eg. Guaifenesin,
diphenoxylate HCL with atropine ( Lomotil)
 Pharmacologic Principles

I. Drug Action:
 Pharmaceutics
 Pharmacokinetics
 Pharmacodynamics

II. Drug Effect:

 Pharmacotherapeutics

Pharmaceutics
• the study of how various drug forms influence pharmacokinetic and pharmacodynamic
activities.
o disintegration
o dissolution

Pharmacokinetics
• the study of what the body does to the drug:
o Absorption
o Distribution
o Metabolism or biotransformation
o Excretion or elimination

Pharmacodynamics
• the study of what the drug does to the body :
o the mechanism of drug action in living tissues.

Pharmacotherapeutics
• the use of drugs and the clinical indications for drugs to prevent and treat diseases.

Pharmacognosy
• the study of natural ( plant and animal ) drug sources.

I. The 3 Phases of Drug Action:

A. Pharmaceutic Phase
1. disintegration
2. dissolution

 Rate limiting – time it takes for drug to disintegrate & dissolve to be absorbed by the body

B. Pharmacokinetic Phase
1. Absorption:
• passage of a drug into the bloodstream from site of administration

 Processes of drug absorption:

 passive absorption
 active absorption
  pinocytosis
 Drug absorption of Oral Preparations:
Liquids, elixirs, syrups Fastest
Suspension solutions
Powders
Capsules
Tablets
Coated tablets
Enteric-coated tablets Slowest

 The rate at which the drug leaves its site of administration, and the extent to
which absorption occurs.
 Bioavailability

 Factors that affect absorption :

 solubility of drug
 food or fluids administered with the drug
 dosage formulation
 status of the absorptive surface
 rate of blood flow to the small intestine
 acidity of the stomach
 status of GI motility
 administration route of drug

 Routes :
• a drug’s route of administration affects the rate and extent of absorption of the
drug.
o Enteral
o Parenteral
o Topical

 Enteral Route
• drug is absorbed into the systemic circulation through
the oral or gastric mucosa, the small intestine, or rectum.
o oral
o sublingual*
o buccal
o rectal

 Parenteral Route
• Intravenous *
• Intramuscular
• Subcutaneous
• Intradermal
• Intrathecal
• Intraarticular

 Topical Route
• skin ( including transdermal patches )
• eyes, ears & nose
 • lungs ( inhalation )*
• vagina
First – Pass Effect
• the metabolism of a drug and its passage from the liver into the circulation.

 A drug given via the oral route may be extensively metabolized by the liver before
reaching the systemic circulation ( high first – pass effect ).

 The same drug – given IV – bypasses the liver, preventing the first – pass effect
from taking place, the more drug reaches the circulation.

• Routes that bypass the liver :

o sublingual transdermal
o buccal vaginal
o rectal* intramuscular
o intravenous subcutaneous
o intranasal inhalation

2. Distribution
• transport of a drug by the bloodstream to its site of action

 Factors affecting drug distribution:

• protein-binding
• water soluble vs fat soluble
• areas of rapid distribution
o heart, liver, kidneys, brain
• areas of slow distribution
o muscle, skin, fat

3. Metabolism or biotransformation
• the transformation of a drug into an inactive metabolite, a more soluble compound or a
more potent metabolite

 liver*
 others: kidneys, lungs, plasma ,intestinal mucosa

 Factors that decrease metabolism:

• cardiovascular problem
• renal problem
• starvation
• liver problem
• erythromycin or ketoconazole drug therapy

 Factors that increase metabolism:

• nicotine
• alcohol
• barbiturates & glucocorticoids
• rifampin therapy

 Half-life
 o time it takes for one half of the original amount of a drug in the body to be
removed.
o a measure the rate at which drugs are removed from the body
4. Excretion
• elimination of drugs from the body
 kidneys*
 others: lungs, exocrine glands (sweat, salivary or mammary glands),
skin & intestinal tract

C. Pharmacodynamics Phase

 Onset of Action
• time it takes for the drug to elicit a therapeutic response
 minimum effective concentration (MEC)

 Peak Action
• time it takes for drug to reach its maximum therapeutic response

 Duration of Action
• the time a drug concentration is sufficient to produce its therapeutic response

 Receptor Theory
• most receptors are found on cell membrane
• drug binding occurs on receptors
• lock & key interaction
:
 Agonist & antagonist:
 Agonists
• drugs that attracts to receptors  stimulate/ enhance a response
• ex. Insulin, isoproterenol – stimulate beta 1 receptor

 Antagonists
• drugs that attracts to receptors  block a response
• ex. cimetidine – blocks H2 receptor

 Nonspecific & Nonselective Drugs

 Nonspecific Drugs
• affect various sites of the body
• ex. Bethanecol  stim. cholinergic receptor  strengthen bladder
contraction,increases HR, decreases BP, bronchiole & pupil constriction

 Nonselective Drugs
• affect various receptors
• ex. Epinephrine  acts on alpha1, beta 1 & 2 receptors
 Categories of drug action:
a. depress cellular activities
b. stimulates cellular activities
c. inhibit or kill organisms
d. act as substitute for missing chemicals

 Therapeutic Index & therapeutic Range:

 Therapeutic Index (TI)
• relationship bw the drug’s therapeutic effects & its adverse effects

TI= LD50
ED50

• High TI  wide margin of safety

• Low TI  narrow margin of safety

 Therapeutic Range (therapeutic window)

• drug concentration bw therapeutic effect & toxic effect
• Ex. Digoxin = 0.5 to 2 ng/ml

 Peak & Trough Level

 Peak drug level
• highest plasma concentration of drug at a specific time
• indicate rate of absorption

 Trough level
• lowest plasma concentration
• indicate rate of elimination

 Loading dose
• large initial dose given for immediate response.
• given to achieve a rapid minimum effective concentration.
• Ex. Digoxin (digitalization)
II. Pharmacotherapeutics
• use of drugs to treat disease.

A. Types of Therapies:
1. acute therapy
• px is critically ill & requires immediate intensive therapy

2. empiric therapy
• based on practical experience rather than on pure scientific data
3. maintenance therapy
• chronic conditions that don’t resolve

4. supplemental or replacement therapy

• replenish or substitute missing substances in the body

5. supportive therapy
• Doesn’t treat the cause of disease but maintains other threatened body systems
until the patient’s condition resolve.

6. palliative therapy
• used for end-stage or terminal diseases to make the patient as comfortable as
possible

Drug Effects:
 Main effect
• desired therapeutic effect
• reason drug is administered

 Side effects
• physiologic effects that are not related to desired drug effects
• expected, well-known reactions that result in little or no change in patient intervention

 Adverse Reactions
• more severe than side effects
• undesirable & unexpected effects occurring even at normal dose

 Local vs Systemic drug effect

 Placebo Effect
• a therapeutic effect that results from a patient’s belief in the benefits of a medication
 Factors affecting Drug Effects:
• Age
• Size
• Sex
• Genetic factors
• Disease conditions
• Emotional conditions
• Route of administration
• Time of day
• Drug taking history
• Environmental conditions
• Drug-interactions
 Drug Interactions

Drug interactions
• occur bw drugs or bw drugs & foods

I. Drug – Drug Interactions:

1. additive drug effect 2 drugs produce equivalent effects when either drug is given alone
in higher doses.

ex. diuretic & beta blocker

aspirin & codeine

2. synergistic/potentiation – 2 drugs produce same effects but one drug enhances

the effect of the other drug  greater effect

ex. meperidine (Demerol) & promethazine

alcohol & sedatives

3. antagonistic – combined effects of 2 drugs are less than the effect produced by
the 2 individual drugs

ex. tetracycline & antacid

morphine & naloxone

4. Incompatibility – 2 drugs mixed together  chemically incompatible

ex. ampicillin & gentamicin

II. Drug – Food Interactions:

• tetracycline & dairy products

• levodopa & high protein meals
• monoamine oxidase inhibitor (MAO) inhibitor & tyramine-rich foods
• nitrofurantoin
• Metoprolol & food
• lovastatin
 Adverse Drug Reactions

I. Dose- related adverse reactions:

• Secondary effects
• Hypersensitivity or hypersusceptibility
• Overdose
• Iatrogenic
• Tolerance
• Dependence

II. Patient sensitivity-related adverse reactions

• Allergic reaction
• Idiosyncrasy

I. Dose-related adverse reactions:

a. Secondary effects
ex. morphine
antihistamine

b. Hypersensitivity or hypersusceptibility
• excessive therapeutic response even with usual therapeutic dose

ex. anticholinergics  dry mouth, blurring of vision, urinary retention & constipation
narcotic analgesic
oral contraceptives
digitalis
aspirin

c. Overdose & toxicity

• excessive dose  exaggerated response
• pediatric & elderly

ex. CNS depressants

digoxin

d. Iatrogenic effects
• adverse reactions that caused by drugs that are part of medical tx.
• drug-induced diseases

ex. antineoplastics, aspirin, corticosteroids  GI irritation & bleeding

propanolol
gentamicin
e. tolerance
• decrease response to drug over time

ex. psychoactive drugs (e.g. benzodiazepines)

propanolol
cocaine
 morphine

f. dependence
• strong physical & psychological
need for a certain drug

 habituation
 addiction

g. cumulation
• body cannot metabolize & excrete one dose of a drug completely before
the next dose.

II. Patient sensitivity-related adverse reactions:

• result from unusual & extreme sensitivity to a drug
a. Allergic reaction
• abnormal response due to antibodies against a certain drug
ex. antibiotics (penicillin) , aspirin, sulfonamides

Types:
1. Immediate allergic reaction :
 Urticaria
sxs:
• skin rash with severe itching
• swelling

 Anaphylaxis
sxs:
• dyspnea
• extreme weakness
• nausea & vomiting
• cyanosis
• hypotension
• circulatory collapse

2. Delayed allergic reaction

 Serum sickness
Sxs.
• itchy rash
• fever
• swollen & stiff joints
Interventions:
• notify prescriber & discontinue drugs
• emergency tx for anaphylactic shock
 • Epinephrine
• Antihistamines or topical corticosteroids
• Cool environment

b. Idiosyncratic reactions:
• unique or strange responses to certain drugs thought
to be caused by genetic factors

ex. succinylcholine
primaquine

III. Other drug- related effects:

a. Teratogenic
• produce organ defects in developing fetus

ex. marijuana/ cocaine

alcohol
aminoglycoside

b. Carcinogenic
• induce malignant changes in cells

ex. estrogen therapy

antineoplastics for pediatric leukemias

c. Mutagenic
• produce genetic mutations

IV. Drug-induced tissue & organ damage:

A. Dermatological reactions:
Sxs:
• hives/ urticaria
• rash
• exfoliative dermatitis
• Stevens- Johnson syndrome

Ex. procainamide - butterfly- rash

sulfonamide - Stevens-Johnson syndrome

Tx:
• frequent skin care
 • notify prescriber & discontinue drug
• topical corticosteroids, antihistamine & emollients

B. Stomatitis
S/sxs:
• swollen gums & tongue.
• difficulty swallowing
• bad breath
• pain in mouth & throat

ex. antineoplastic agents (eg fluorouracil)

Tx:
• frequent mouth care
• frequent, small meals

D. Gingival hyperplasia
S/sxs:
• red, & enlarged gums

ex. phenytoin (anticonvulsant)

E. Superinfections
S/sxs:
• fever
• diarrhea
• hairy tongue
• mucous membrane lesions
• vaginal discharge

ex. antibiotics

F. Blood dyscrasias
 agranulocytosis*
 anemia
 thrombocytopenia

s/sxs:
• fever & chills
• extreme weakness
• sore throat
• high risk to infection
• high risk for bleeding/hemorrhage

ex. antineoplastics & antipsychotics

antibiotics (eg. chloramphenicol, sulfonamides)
anti-inflammatory (eg non-steroidal anti-inflammatory drugs (NSAID)

tx.
• monitor blood counts
 • protect from exposure to infection
• avoid activities that result in injury or bleeding

G. Hepatotoxicity
s/sxs:
• jaundice*
• fever
• nausea & vomiting
• increase in liver enzymes (AST & ALT)
• altered bilirubin

ex. isoniazid (INH)

acetaminophen

H. Nephrotoxicity
s/sxs
• edema
• increase Crea & BUN
• decrease hematocrit
• electrolyte imbalances

ex. aminoglycosides (eg gentamicin)

sulfonamide

I. Ototoxicity
s/sxs
• dzziness
• ringing in ears
• loss of balance
• hearing problem

ex. aminoglycoside (eg. Gentamicin)

azithromycin, erythromycin
aspirin
quinidine

J. Ocular toxicity
s/sxs
• burring of vision
• color vision changes
• blindness

ex. chloroquine (anti-malarial )

K. Hypoglycemia
s/sxs
• headache
• tremors
• drowsiness
 • cold clammy skin
• seizures/coma

ex. antidiabetic agents (eg. Insulin, glipizide)

L. Hyperglycemia
s/sxs
• polyphagia
• polyuria
• polydipsia
• kussmaul’s respiration
• fruity breath

ex. ephedrine ( bronchodilator)

M. Hypokalemia
s/sxs
• serum K
• irregular, weak pulse
• weakness & numbness of extremities
• paralytic ileus
o absent bowel sounds
o abdominal distention

ex. loop diuretics (eg, furosemide)

N. Hyperkalemia
s/sxs
• same as hypokalemia

ex. potassium-sparing diuretics (eg. Spironolactone)

antineoplastic drugs

O. General CNS effects

s/sx
• anxiety
• insomnia
• nightmares
ex. beta-blockers (eg. Metoprolol)

P. Atropine- like (Cholinergic) effects

s/sxs
• dry mouth
• constipation
• urinary retention
• decrease sweating,
• hot dry skin

ex. antidepressants (eg. TCA)

Q. Extrapyramidal reactions/ parkinson- like syndrome
s/sxs
• immobility (akinesia)
• rigidity
• muscular tremors
• violent movement of head & arms (dystonia)
• restlessness (akathisia)

ex. antipsychotic drugs

R. Neuroleptic Malignant syndrome

s/sxs
• extrapyramidal symptoms
• hyperthermia

ex. general anesthetics

S. Photosensitivity
s/sxs
• itching
• scaling
• reddening of skin
Ex. sulfonamides, tetracycline

T. Cough - ACE inhibitors

U. Gray Baby Syndrome - chloramphenicol

V. Osteoporosis – corticosteroids, heparin

W. Pseudomembranous colitis – clindamycin

X. Discolors teeth – tetracycline

Y. Nasal stuffiness – reserpine

Z. cervical cancer – estrogen

hemorrhage – oral anticoagulants, heparin

The capacity to laugh at things, including ourselves at times,

means that we are still the masters of our fate…
 Adrenergics and Adrenergic Blockers

I. Adrenergics/ Sympathomimetics
• mimic effects of NE by stimulating SNS.

A. Effects of Adrenergics at receptor sites

Alpha 1 Receptors Alpha 2 receptors

• vasoconstriction (skin & mucous membrane) • decrease NE release

• increase BP • decrease BP
• pupil dilation • decrease GI motility
• closure of urinary bladder sphincter
• thickened salivary secretions
• goosebumps
• ejaculation

Beta 1 receptors Beta 2 receptors

 increase HR  bronchodilation
 Increase cardiac contraction  vasodilation (skeletal muscle)
 increase cardiac conduction  relaxation of uterus
 lipolylis  relaxation of GIT & decrease GI secretions
 relaxation fo urinary bladder
 increase blood sugar

B. Inactivation of NE:
1. reuptake of NE back into the neuron.
2. enzymatic degradation - MAO & COMT
3. diffusion away from transmitter

C. Classification of Adrenergics/ Sympathomimetics

I. Direct Acting Adrenergic

• epinephrine

II. Indirect Acting Adrenergic

• amphetamine

III. Mixed Acting Adrenergic

• ephedrine
 BODY TISSUE/ ORGAN

Eye

Lungs

Heart

Blood V

Gastroin

Bladder

Uterus

Salivary

* The sympathetic and parasympathetic nervous systems have opposite responses on body tissues and organs.
 Antidiabetic Drugs
I. Injectable hypoglycemics MOA Indication

Insulin Preparations > increase uptake of glucose, Type 1 & type2 DM

amino acids & free fatty acids
for storage
> synthesize glycogen, fats &
Proteins

A. Short acting/ rapid acting onset peak duration

1. Lispro (Insulin analog) 5 min O.5 – 1 h 2–4h
• Humalog

2. Crystalline Zinc Insulin (Regular) 0.5 – 1 h 2–4h 6–8h

• Humulin R, Novolin R

3. Semilente 1 – 1.5 h 1–4h 12 – 16 h

B. Intermediate/ short acting

1. NPH insulin 1–2h 6 -12 h 18 – 24 h H
• Humulin N, Novolin N
L
2. Lente insulin 1–2h 8 – 12 h 18 – 24 h
• Humulin L, Novolin L

C. Long-acting
1. Ultralente insulin 5–8h 14 – 20 h > 36 h
a. Humulin U

2. Protamine Zinc Insulin (PZI) 4 – 8 h 14 – 24 h 24 – 36 h

D. Combination
1. NPH + Regular insulin
• Humulin 70/30 0.5 h 4–8h 22 – 24 h
• Humulin 50/ 50 0.5 h 4–8h 24 h
• Humulin 75/25 15 min 0.5 – 6 h 20 – 24 h
 ANTIDYSRHYTHMIC DRUGS

Cardiac dysrhythmia

 deviation from normal rate & pattern of heartbeat.

 Atrial dysrhythmias  prevent proper filling of ventricles  decrease CO (1/3)

 Ventricular dysrhythmias  lifethreatening

 ineffective filling of ventricle  decrease or absent CO

Types of Arrhythmias:

1. Sinus Arrhythmias
• ANS influence SA node to change rate of firing to meet body’s demand for O2

 Sinus tachycardia
• faster than normal HR with normal- appearing ECG.

 Sinus bradycardia
• Slower than normal HR with normal- appearing ECG.

2. Supraventricular Arrhythmias
• arrhythmias that originate above ventricles but not in SA node.
• abnormal P wave but normal QRS complexes.

 Premature atrial contraction (PAC)

• ectopic focus in atria conducting impulse out of normal rhythm.

 Paroxysmal atrial tachycardia (PAT)

• sporadically occurring rapid HR originating in atria.

 Atrial flutter
• sawtoothed –shaped P waves
• regular fast atrial depolarization
• from a single ectopic focus

 Atrial fibrillation
• irregular P waves
• rapid, uncoordinated atrial depolarization
• from many ectopic foci
• bombardment of impulses at AV node  transmit many impulses to ventricles
 cause rapid, irregular & ineffective ventricular contraction.
Antineoplastics / Chemotherapeutic Agents
• Objectives:
1. to destroy all malignant cells without excessive destruction of normal cells.
2. to control tumor growth if cure is no longer possible.

• Affect neoplastic and normal cells  INTERVENTIONS: (CANCER)

CBC, platelets, uric acid – monitor
A. UNDESIRABLE effects: (BARFS)  WBC < 4000 cells/ ul
Bone marrow depression ( WBC, RBC, Plt Ct.)  Platelet Ct < 75,000
 Avoid crowd, protect from infection.  Uric acid > 8 mg/dl (hyperur
 Frequent rest periods. • Tx: Allopurinol
 Bleeding protocol, Avoid ASA • Low purine diet -->
 Consult MD before receiving vaccination.
Antiemetics before drug.
Alopecia • ondansetron, grani
 Reassure its temporary • dronabinol, halope
 Wigs • alprazolam, lorazep
• prochlorperazine
Retching –- nausea / vomiting
 Antiemetics 30-60 min before chemo drug. Nephrotoxicity / hemorrhagic cystitis –
 Replace fluids & electrolyte losses  provide 2-3 L of fluids per d
 Small, frequent meals
Counselling regarding reproductive is
Fear & anxiety  category X drugs ---> terato
 pretreatment counseling.  gonadal suppression --> inf

Stomatitis Encourage handwashing, avoid crowd

 good oral hygiene
 avoid hot & spicy foods. Recommend wig for alopecia.

B. INTERVENTIONS: (METABOLITE)
Monitor CBC & platelets weekly  Contraindications:
 Infection. -->Chemo drugs are immu
Evaluate renal function tests.  Recent surgery. --> They retard hea
 Impaired kidney/ liver function. --> n
Temperature assessment q 4-6 hrs.
 Pregnancy.--> congenital defects
Asepsis – strict  Bone marrow depression --> aggrav
Bleeding, anemia, infection & nausea – report

Oral hygiene – soft toothbrush

Lots of fluids (2 -3 L / day)

Intake & output, nutritional intake – monitor

The protocol for handling chemo drugs must be followed.

Emphasize protective isolation

 ANTISEIZURE DRUGS

I. Seizures / Epilepsy
• abnormal or uncontrolled neuronal brain discharges.
• sxs of underlying disease

Causes:
 head trauma
 brain infection
 fluid & electrolyte imbalance
 hypoxia
 stroke
 brain tumors
 high fever in children

II. Categories of Seizures:

A. Partial (Focal) Seizures

• Simple

• Complex

B. Generalized Seizures
• Absence (Petit mal)

• Tonic-Clonic (Grand mal)

• Myoclonic seizures

• Febrile seizures

• Status epilepticus

III. Antiseizure Drugs act by distinct mechanisms:

• increasing effect of GABA , inhibitory neurotransmitter
• delaying the influx of sodium and calcium ions into neurons

4 Major Chemical categories of antiseizure meds:

1. Barbiturates
2. Benzodiazepines
3. Hydantoin & phenytoin-like drugs
4. Succinimides
 ANTI-ULCER DRUGS

Type Examples Mechanism of Action Indication

1. Antacids a. Na- bicarbonate based Neutralize stomach acid relieveheartburn/ hyperacidity

( Alka-seltzer) gastritis , peptic ulcer
b. Ca- carbonate
(Tums)
c. Mg – hydroxide
(Milk of Magnesia)
d. Aluminum hydroxide
(Amphojel)
d. Combination
(Maalox, Mylanta,Novaluzid) ALL c
preven

2. Histamine 2 (H2) a. cimetidine (Tagamet) block H2 receptors peptic ulcer, gastritis,GERD

blockers b. famotidine (Pepcid)
c. nizatidine (Axid)
d. ranitidine (Zantac)

3. Proton Pump a. omeprazole (losec) inhibits acid production peptic ulcer, gastritis, GERD
Inhibitors b. lansoprazole (Prevacid) in parietal cells of stomach
c. esomeprazole (Nexium)
d. rabeprazole (Pariet)
e. pantoprazole (Pantoloc)

4. Miscellaneous
a. Sucralfate (Iselpin) forms polymers in acidic peptic ulcer disease (PUD)
environment &coats peptic stress- ulcer prophylaxis
ulcer from further acid attack
b. Bismuth subsalicylate (Pepto- Bismol) coats esophagus & acts as PUD, GERD
barrier to gastric acids

Tetracycline & Metronidazole eradicate Helicobacter pylori

c. Misoprostrol (Cytotec) secrete gastric mucous barrier prevent NSAID-induced pept
 DOSAGE CALCULATIONS

I. Systems of Measurement with Conversion

A. Metric System
B. Apothecary System
C. Household System
D. Avoirdupois System

Commonly accepted conversions:

_______________________________________________________________________
Metric Apothecary Household ______________
Solid measures:
1 kg 2.2 lb
454 g 1.0 lb
1 g = 1000 mg 15 gr (gr xv)
60 mg 1 gr (gr i )
30 mg ½ gr (gr ss)

Liquid measures:
1 L = 1000 mL about 1 quart
240 mL 8 f oz (f oz viii) 1c
30 mL 1 f oz ( f oz i) 2 tbsp
15 – 16 mL 4 f dr (f dr iv) 1 tbsp = 3 tsp
8 mL 2 f dr ( f dr ii) 2 tsp
4 – 5 mL 1 f dr (f dr ii) 1 tsp = 60 gtt
1 mL 15 -16 min
0.0 6 mL 1 min ( min i)

II. Calculating Dosage:

I. Oral Drugs
A. Basic formula:
Desired dose ( D) X V = Amount to be given (A)
On- hand dose (H)

Ex. Order: amoxicillin 100mg PO qid

Available: amoxicillin 250 mg / 5 mL

D x V = A 100 mg x 5 mL = 2 mL
H 250 mg

B. Ratio & Proportion

H : V= D :x

250 mg : 5 mL = 100 mg : x
250 x = 500
x = 2 mL
 Cholinergics and Cholinergic Blockers

I. Cholinergics / Parasympathomimetics
• mimics effects of acetylcholine, stimulating PSNS

A. Effects of Cholinergics at receptor sites:

Muscarinic receptor Nicotinic receptor

• pupil constriction • muscle contraction

• bronchoconstriction
• decrease HR, BP, & conduction
• increase GI peristalsis & secretions
• increase urinary bladder contraction, relax
urinary sphincters
• uterine contraction
• increase glandular secretions (sweat, tears,
saliva)
• erection

B. Inactivation of Acetylcholine
• Acetylcholinesterase

C. Classification of Cholinergics/ Parasympathomimetics

I. Direct acting cholinergics

 Muscarinic agonists
• bethanechol*
• carbachol
• pilocarpine
• metoclopramide (Reglan)

Indications: Tx of urinary retention, glaucoma, & gastroesophageal reflux

MOA: acts on muscarinic receptors to increase urination, constrict pupils & reduce
Intraocular pressure, increase GI peristalsis

CI : intestinal or urinary tract obstruction

 Cardiovascular Agents
1. Cardiac Glycosides:
Action: inhibit Na-K ATPase ---> increase cardiac contraction
Indic: CHF, atrial dysrhythmias

LIZZY DIGGY
digoxin (Lanoxin)
digitoxin

Therapeutic level of Digoxin: 0.5 - 2 ng/ ml

Dig level 2 ng/ml or greater is toxic!!!!

Increases myocardial contractility
GI or CNS signs indicate adverse effects
SE:
• GI- nausea & anorexia, vomiting & diarrhea
• CNS – vertigo , HA, drowsiness, confusion
• bradycardia --> cardiac dysrhythmias, heartblock
• photophobia, yellow-green halos around visual images, flashes of light

2. Nitrates:
ANDY ANGINA
nitroglycerin (Nitro-Bid, Nitrostat, Transderm- Nitro)
isosorbide dinitrate (Isordil)
isosorbide mononitrate (Imdur)

Action
Relaxes vascular smooth muscle
venous return
arterial BP
left ventricular workload
myocardial oxygen consumption

Indic: Angina Pectoris

SE: headache (MC), syncope, weakness, nausea & hypotension
SL: burning & tingling sensation in mouth
 DIURETICS

Diuretics
 increase the rate of urine formation  removal of sodium & water
 “ water pills”

2 main indications:
1. decrease blood pressure
2. decrease edema

Types of Diuretics:

1. Carbonic Anhydrase inhibitors

• acetazolamide (Diamox)* 4. Thiazide Diuretics
• methazolamide • hydrochlorothiazide (Hydrodiuril)
• dichlorphenamide • chlorothiazide

2. Osmotic Diuretics Thiazide –like diuretics

• mannitol • chlorthalidone
• urea • metolazone
• glycerin
• isosorbide 5. Potassium – sparing diuretics
• spironolactone
3. Loop Diuretics • amiloride
• furosemide (Lasix)* • Triamterene
• bumetanide
• torsemide
• ethacrynic
 DRUGS USED TO TREAT ANEMIA

Classification:

A. Erythropoietin
1. Darbopoeitin alfa
2. Epoetin alfa (Epogen, Procrit)

B. Iron Preparations
1. Ferrous fumarate
2. Ferrous gluconate
3. Ferrous sulfate
4. Ferrous sulfate exsiccated
5. Iron dextran
6. Iron sucrose
7. Sodium ferric gluconate complex

C. Folic Acid Derivatives

1. Folic Acid
2. Leucovorin

D. Vitamin B12
1. Cyanocobalamin
2. Hydroxocobalamin

I. A. Blood Components
Blood
 contains oxygen & nutrients essential for cell survival  delivers these to cells &
removes waste products from the tissues.

Blood- composed of :
a. Plasma  mostly water
• Also contain glucose, electrolytes & proteins for immune response & for blood
clotting.
b. Formed elements
• Leukocytes (WBC) – impt part of immune system.
• Erythrocytes (RBC) – carry O2 to tissues & remove CO2 for delivery to lungs.
• Platelets – impt. part of coagulation, blood clotting.

B. Erythropoiesis
• Process of RBC production.
• Produced in myeloid tissue of the bone marrow.
• Controlled by Erythropoeitin.
• Is a constant process  1% of body’s RBC are destroyed & replaced each day.

Erythropoeitin
 Released from kidneys in response to decreased blood flow in the kidneys.

Insert fig 49-1 p668

 ANTIPLATELETS, ANTICOAGULANTS, THROMBOLYTICS

I. Process of blood coagulation & thrombus formation

Blood vessel injury

Vasoconstriction Blood loss into tissues Intrinsic pathway Extrinsic pathway

to clot formation to clot formation

Platelet adhesion
to injured wall of bv &
platelet aggregation

decrease blood flow compression of platelet plug blood clot

at site of injury injured bv

thrombus

Decrease blood loss at site of injury

 Final step of clot formation:

Prothrombin thrombin

Fibrinogen Fibrin clot

 Clot dissolution:

Plasminogen plasmin (fibrinolysin)

Fibrin clot dissolution of clot

 DRUGS FOR CARDIAC DISORDERS

Congestive heart failure (CHF)

 condition when heart muscle fails to effectively pump blood through the heart & systemic
circulation  build-up of blood (congestion).

 Causes:
• damaged heart muscle
 atherosclerosis / coronary artery dse (CAD)
 cardiomyopathy

• increased demand to heart muscle to work harder

 hypertension
 valvular disease

• abnormal heart structure

 congenital cardiac defects

Left-sided Heart failure

 when LV does not contract sufficiently  excessive blood backs up into lung tissue.

 s/sxs
• pulmonary edema
o tachypnea
o dyspnea
o orthopnea
o hemoptysis
o rales /wheezes
• cardiomegaly, increase HR, S3
• anxiety
• decrease peripheral pulses

Right-sided Heart Failure

 when right side of the heart does not contract sufficiently  excessive blood backs up into
peripheral tissues.

 s/sxs:

o elevated jugular venous pressure

o hepatomegaly
o splenomegaly
o decrease renal perfusion when upright
o increase renal perfusion when supine  nocturia
o pitting edema
o weakness & fatigue
 Drugs for Parkinsonism and Parkinson’s Disease

I. Parkinsonism
• group of disorders that share four main symptoms:
1. tremors
2. rigidity
3. slowness of movement (bradykinesia)
4. poor balance and coordination.

Idiopathic Parkinson’s Disease

• loss of dopamine- secreting neurons in substantia nigra
• cause unknown (idiopathic)
• causal theories:
 viral infection
 head trauma
 atherosclerosis

Pseudoparkinsonism/ Drug –induced Parkinsonism

• causes:
 antipsychotics (phenothiazines)
 poisons (carbon monoxide, manganese)

Basal ganglia cells

INHIBITION STIMULATION

Type 1 drugs Type 2 drugs

Dopaminergics Anticholinergics

A. Dopaminergics
A. biperiden (Akineton)
• Levodopa* B. benztropine(Cogentin)
• Carbidopa- levodopa (Sinemet) C. diphenhydramine
(Benadryl)
D. procyclidine
B. MAO –B inhibitor
• Selegiline E. trihexyphenidyl
(Artane)
C. COMT inhibitors
• tolcapone
• entacapone

D. Dopamine Agonists
• amantadine pramipexole
• ropinirole pergolide
• bromocriptine
 Drugs for Parkinsonism and Parkinson’s Disease

I. Parkinsonism
• group of disorders that share four main symptoms:
1. tremors
2. rigidity
3. slowness of movement (bradykinesia)
4. poor balance and coordination.

Idiopathic Parkinson’s Disease

• loss of dopamine- secreting neurons in substantia nigra
• cause unknown (idiopathic)
• causal theories:
 viral infection
 head trauma
 atherosclerosis

Pseudoparkinsonism/ Drug –induced Parkinsonism

• causes:
 antipsychotics (phenothiazines)
 poisons (carbon monoxide, manganese)

Basal ganglia cells

INHIBITION STIMULATION

Type 1 drugs Type 2 drugs

Dopaminergics Anticholinergics

A. Dopaminergics
A. biperiden (Akineton)
• Levodopa* B. benztropine(Cogentin)
• Carbidopa- levodopa (Sinemet) C. diphenhydramine
(Benadryl)
D. procyclidine
B. MAO –B inhibitor
• Selegiline E. trihexyphenidyl
(Artane)
C. COMT inhibitors
• tolcapone
• entacapone

D. Dopamine Agonists
• amantadine pramipexole
• ropinirole pergolide
• bromocriptine
 Adrenergics and Adrenergic Blockers
I. Adrenergics
A. Function:
Adrenergics
Adrenergic agonists stimulate SNS
sympathomimetics

B. Effects of Adrenergics at receptor sites :

Beta1 receptor Beta2 receptor

Heart Kidney Smooth muscle Lungs Uterus Liver

( gastrointestinal
tract )

Increased Increased
heart renin
Activation of
contraction secretion Bronchodilation glycogenolysis

Decreased Relaxation of
Increased Increased
gastrointestinal uterine smooth
heart rate angiotensin
tone and motility muscle

Increased
Increased blood sugar
blood
pressure
 LIPID LOWERING DRUGS

I. HMG- CoA reductase inhibitors / Statins

• atorvastatin (Lipitor)
• simvastatin (Zocor)
• pravastatin

MOA: inhibits HMG- CoA reductase  inhib. Cholesterol synthesis  LDL

SE/ Adverse effects:

1. GIT upset
2. liver complications
3. rhabdomyolysis
4. cataract

CI: liver failure, pregnancy & lactation, allergy to fungal byproducts

II. Bile Acid sequestrants

• cholestyramine
• colestipol

MOA: binds bile acids in SI & promote increase disposal of cholesterol

SE:
1. CNS effects: HA, anxiety, drowsiness
2. GIT effects: nausea ,constipation, bloating & flatulence
3. increase bleeding
4. muscle aches & pains

III. Fibrates
• gemfibrozil
• clofibrate

MOA: decrease triglyceride & LDL synthesis  TG & LDL, HDL

SE:
1. same GIT effects
2. muscle aches & pains

IV. Nicotinic Acid / Vitamin B3 / Niacin

MOA:
1. inhib. release of fatty acids from adipose tissue
2. increase TG removal from plasma  TG & LDL, HDL

SE:
1. intense flushing, dizziness, fainting
2. GIT effects: nausea, abdominal pain
 Pain Medications
Types of analgesics:

A. Nonnarcotic Analgesics:
1. Non- steroidal antiinflamatorydrugs (NSAIDs)
• naproxen (Aleve) • diclofenac (Cataflam)
• ibuprofen ( Advil, Midol) • ketorolac ( Toradol)
• aspirin • ketoprofen (Orudis)
• mefenamic acid (Dolfenal, Ponstan) • piroxicam ( feldene)
 Indomethacin
MOA:
 Aspirin –> irreversibly inhibits cyclooxygenase (both COX I & COX II)
--> blocks prostaglandin (PG) synthesis

 other NSAIDs --> reversibly inhibit COX I & COX II --> block PG synthesis

Indication: analgesic ( mild pains, somatic pains antipyretic, anti-inflammatory

SE/ adverse effect:

1. gastric irritation
2. GI bleeding
3. nephrotoxic
4. aplastic anemia
5. hypersensitivity to ASA ( tinnitus, vertigo, bronchospasm, urticaria)
6. Reye’s syndrome
7. hyperventilation

New NSAID:
 COX – 2 inhibitors
• celecoxib (Celebrex)
• valdecoxib (Bextra)
• rofecoxib (Vioxx)

MOA: selectively inhibits COX-2

Indication: rheumatoid & osteoarthritis

SE: same as other NSAIDs but less GI toxicity

2. Acetaminophen (Tempra , Tylenol)

Acetaminophen combinations:
• Acetaminophen with codeine (Tylenol with Codeine)
• Acetaminophen with hydrocodone
• Acetaminophen with oxycodne

MOA: reversibly inhibits COX mostly in CNS

Indications: antipyretic, analgesic (moderate pain)

Adverse Effects: hepatotoxic

Antidote: acetylcysteine (Mucomyst)
 ANTIPSYCHOTICS

Psychosis
 symptomatic thought disorder.
 chemical imbalance within brain

Schizophrenia
 MC psychosis
 characterized by:

a. positive symptoms
 exaggeration of normal function
 incoherent speech
 hallucination
 delusion
 paranoia

b. negative symptoms
 loss in function & motivation
 poverty of speech content
 poor self-care
 social withdrawal

Antipsychotics
• block dopamine receptor  improve thought processes & behavior , EPS
• block chemoreceptor trigger zone & vomiting  antiemetic effect
SE:
1. drowsiness
2. hypotension
3. anticholinergic effects

4. extrapyramidal side effects (EPS)

a. dystonia
 spasms of tongue, neck, back & legs
 facial grimacing
 involuntary upward eye movement
 unnatural positioning of the neck
 excessive salivation

b. akathisia
 uncontrolled restlessness
 inability to sit & stand still
 foot tapping
 hand movements

c. pseudoparkinsonism
 muscle tremors at rest
 rigidity
 bradykinesia
 shuffling gait
 stooped posture
 pill-rolling motion of hand
 drooling
 SKELETAL MUSCLE RELAXANTS

Movement & control of muscles regulated by:

 Spinal reflexes
 Cerebral cortex
 Cerebellum
 Basal ganglia

Spinal reflexes
• Simple  incoming sensory neuron & an outgoing motor neuron.
• Complex  plus interneurons

Neuromuscular Abnormalities:
1. Muscle Spasm
 often results from injury to musculoskeletal system.
• overstretch muscle
• tear in ligament or tendon

2. Muscle Spasticity
 often results from damage to neurons within CNS.
 permanent condition
 due to increase muscle excitation or decrease inhibition within CNS  muscle
hyperactivity
• cerebral palsy
• paraplegia

SKELETAL MUSCLE RELAXANTS

• decrease muscle tone & movements by reducing skeletal muscle activity.

Classification:

I. Centrally Acting skeletal muscle relaxants

1. baclofen (Lioresal)
2. carisoprodol (Soma)
3. chlorphenesin (Maolate)
4. chlorzoxazone (Paraflex)
5. cyclobenzaprine ( Flexeril)
6. metaxalone (Skelaxin)
7. methocarbamol (Robaxin)
8. orphenadrine (Banflex, Norflex)
9. tizanidine (Zanaflex)

II. Direct-Acting skeletal muscle relaxants

1. dantrolene (Dantrium)
2. botulinum toxin type B (Myobloc)
3. botulinm toxin type A (Botox Cosmetic)
 RESPIRATORY TRACT drugs
MOA Indication S/E
1. Decongestants local vasoconstriction common cold, sinusitis,
decrease overproduction of allergic rhinitis, relief of OM
secretions
NasaL steroid local burning/irrita
a. Beclomethasone dryness of mucos
b. Budesonide
Topical
a. topical ehphedrine tachycardia, incr
b. phenylephrine cool & clammy s

Oral
a. pseudoephedrine

2. Antihistamines block histamine --> decrease allergic rhinitis, sinusitis sedation,

Inflammation skin dryness, uri
a. diphenhydramine
b. cetirizine (Virlix, Zytec)
c. hydroxyzine (Iterax)
d. loratadine (Claritin)

3. Expectorants increase productive cough to bronchitis, pneumonia GI upset

clear airways headache & dizzi
a. guiafenesin
b. terpin hydrate

4. Mucolytics liquefy secretions to clear GI upset, stomatit

Airways bronchospasm
a. acetylcysteine post-op clearing of secretions
b. dornase –alfa cystic fibrosis

5. Antitussives
a. codeine central acting--> reduce excitability resp depression
b. dextromethorphan of cough center addiction, C

c. benzonatate peripheral acting --> block signals constipation, dizzine

d. demulcents fr vagus & glossopharyngeal nerves
(honey, olive oil, glycerin)
 ANALGESICS

I. Pain
 occurs when there is tissue damage

release of kinins & prostaglandins

stimulate sensory nerves (A-delta & C fibers)

pain is perceived

 Gate-Control Theory

II. Non -Narcotic Analgesics

A. Nonsteroidal Antiinflammatory Drugs (NSAIDs)

• ibuprofen (Advil, Alaxan, Dolan, Muskelax, Midol)
• mefenamic acid (Dolfenal, Gardan, Ponstan)
• Naproxen (Flanax)
• Ketorolac (Toradol)
• ketoprofen (Orudis)
• diclofenac (Cataflam, Neopyrazone )
• indomethacin
• piroxicam
• Meloxicam (Mobic)

Indic:
 analgesic (arthritis, mild-moderate pain, dysmenorrhea)
 antipyretic

MOA: block prostaglandin (PG) synthesis

Side Effects:
1. gastric irritation & bleeding -MC
2. blood dyscrasias
3. dizziness
4. hypotension
5. pruritus
6. Na & water retention
7. tinnitus

B. Salicylates
• aspirin (ASA, Aspilet)

Indic:
 analgesic
 antipyretic
 anticoagulant (reduce risk of TIA, stroke, or MI)