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Typewritten #2.

Autacoids
Drug

Mechanism
of Action

Adverse Drug
Reaction

Pharmacokinetic
(ADME)

Pharmacodyn
amic

Drug
Interactions

Preparation
s

Atropine

Anticholiner
gic agent
which
competitivel
y blocks the
muscarinic
receptors in
peripheral
tissues such
as the heart,
intestines,
bronchial
muscles,
iris, and
secretory
glands.

Dry mouth,
difficulty
swallowing &
talking, thirst,
reduced
bronchial
secretions,
dilatations of
pupils or
mydriasis with
loss of
accommodation
or cyclopegia &
photophobia,
flushing, dry
skin, transient
bradycardia
followed by
tachycardia
with
palpitations &
arrhythmias,
difficulty in
micturition,
reduced GIT
tone & motility.
Conjunctivitis,
skin rash,
hyperthermia.
Tremor,
headache;
tachycardia.
Tab/Syr:
Palpitations,
muscle cramps.

Absorption:
Readily absorbed
from the GI tract;
also absorbed from
mucous
membranes, eye,
and through intact
skin
Distribution:
distributes
throughout the body
and crosses the
blood-brain barrier
Metabolism:
Incomplete
metabolism in the
liver
Excretion: Excreted
in the urine as
unchanged drug and
metabolites. Half-life
reported to be 4hr.

Atropine
reduces
secretions in
the mouth and
respiratory
passages,
relieves the
constriction
and spasm of
the respiratory
passages, and
may reduce the
paralysis of
respiration,
which results
from actions of
the toxic agent
on the central
nervous
system.

Enhanced effect
with drugs with
antimuscarinic
properties (eg,
amantadine,
antihistamines,
phenothizine
antipsychotics
& TCAs);
enhanced
antimuscarinic
effect with
MAOIs; effect
counteracted
by
parasympatheti
cs. may affect
absorption of
other drugs.

500ug/5mL
solution for
injection prefilled syringes

Absorption:
Readily absorbed
from the GIT.
Distribution: Binds
to and releases from
plasma proteins as
necessary.
Metabolism:
Hepatic and in the
gut wall.
Excretion: Via the
urine as metabolites

Selective B2adrenoceptor
agonist. At
therapeutic
doses, it acts
on the B2adrenoceptors
of bronchial
muscle, with
little or no
action on the
B1-

Non-selective
B-blockers (eg,
propranolol)
antagonize
Salbutamol
action;
Adrenergic
drugs
increase effects
of Salbutamol;
Digoxin
decreased

Tab 2mg,
Syringe 2
mg/5mL,
Rotacap
200ug,
Metered-dose
inhaler
100ug/inhalat
ion; Nebules
2.5mg/2.5mL

Salbutamo
l

Available
brands in the
Philippines
Anespin; Atropan;
Atroptal; Isopto
Atropine; Phil
Pharmawealth/Atl
antic Atropine;
Euro-Med Atropine
Sulfate

Actimed
Salbutamol;
Aerovit; AeroVent; Asfrenon;
Asmacaire CFCFree; Asmalin
MDI; Derihaler
100;
Hivent/Hivent DS;
Rhinol/Rhinol Plus;
Soluvent; Ventar;
Ventolin; RiteMED

Promethaz
ine

A
phenothiazin
e derivative,
blocks
postsynaptic
dopaminergi
c receptors
in the brain
and has a
strong aadrenergic
blocking
effect. It
competitivel
y binds to
H1receptors.

Bradycardia,
tachycardia,
transient minor
increase in BP &
occasional
hypotension.
Jaundice &
blood
dyscrasias,
extrapyramidal
effects (at high
doses). Venous
thrombosis at
IV inj site.
Arteriospasm &
gangrene
following
inadvertent IA
inj.

Loratadine

Nonsedating
antihistamin
e. It works
by
selectively
binding to
peripheral

Fatigue,
headache,
somnolence,
dry mouth,
rash. GI
disorders eg
nausea,
gastritis. Very

and unchanged
drug. Some
excretion in the
feces. Salbutamol IV
has t1/2 of 4-6 hrs.

adrenoceptors
of cardiac
muscle

serum Digoxin
with IV or Oral
Salbutamol;
Monoamine
Oxidase
Inhibitors
(MAOIs)
vasoconstrictio
n, hypotension;
Diuretics
hypokalemia,
ECG changes;

Salbutamol;
Resdil; Ventolax;
Efamed/Efamed
Plus; Bronhosar;

Absorption: well
absorbed (Oral/IM);
peak plasma
concentrations after
2-3hrs
Distribution:
widely distributed:
Brain, crosses the
placenta, enters
breast milk. Proteinbinding: 76-93%
Metabolism:
extensive hepatic
1st-pass
metabolism;
converted to
promethazine
sulfoxide, Ndesmethylprometha
zine
Excretion: via urine
and bile (as
metabolites); 5-14hr
t1/2
Absorption:
Absorbed rapidly
from the GI tract
(oral); peak plasma
concentrations after
1 hr. Absorption
delayed by the
presence of food.

H1-antagonist,
with
anticholinergic,
sedative, and
antiemetic
effects and
some local
anesthetic
properties.
Used as an
antiemetic or
to prevent
motion
sickness.

CNS
depressants
includine
alcohol,
barbiturates,
hypnotics,
opioid
analgesics,
anxiolytic
sedatives &
antipsychotics.
Other
antimuscarinic
drugs (eg,
atropine &
some
antidepressants
both tricyclic
and MAOIs)

Injection 25
mg/mL

Promet; Sylomet;
Promezin

Loratadine is a
long acting
second
generation
antihistamine
that is similar
in structure to
cyproheptadine

Ketoconazole,
erythromycin,
cimetidine may
increase plasma
conc of
loratadine. Coadministration
w/ drugs known

Syr 5
mg/5mL; Tab
10mg

Actidin; Allerta
Syrup; Antal;
Astena; Carin;
Claritin; Lorange;
Lorano; Loratyne;
Lorexa; Lorfast;
Ratalin; Toral;
Zylohist

Ranitidine

histamine
H1-receptors
on effector
cells.

rarely, alopecia,
anaphylaxis,
abnormal
hepatic
function,
tachycardia,
palpitations &
dizziness.

Distribution:
Enters breast milk,
does not cross the
blood-brain barrier.
Protein-binding:
98%.
Metabolism:
Extensively hepatic;
converted to
descarboethoxylorat
adine
(desloratadine).
Excretion: Via urine
and faeces (as
metabolites);elimina
tion half-life 8.4 hr
(loratadine) and 28
hr (desloratadine).

and azatadine.
The
pharmacology
of loratadine is
similar to other
antihistamines,
but unlike
other H1blockers,
loratidine is
shown to
exhibit
competitive,
specific, and
selective
antagonism of
H1 receptors.
The exact
mechanism of
this interaction
is unknown,
but disposition
of the drug
suggests that
loratadine's
prolonged
antagonism of
histamine may
be due to the
drug's slow
dissociation
from the
receptor or the
formation of
the active
metabolite,
desloratadine.
Loratadine
does not
penetrate the
CNS effectively
and has a low
affinity for CNS
H1-receptors.

to inhibit
hepatic
metabolism.

Blocks

Headache.

Absorption: ~50%

Ranitidine is a

(RiteMed

Tab 150mg,

Aciloc; Aglotac;

Sumatript
an

histamine
H2-receptors
in the
stomach and
prevents
histaminemediated
gastric acid
secretion. It
does not
affect pepsin
secretion,
pentagastrin
-stimulated
factor
secretion or
serum
gastrin.

Dizziness,
insomnia,
reversible
mental
confusion,
reversible
blurred vision,
arrhythmias,
constipation,
diarrhea,
nausea,
vomiting,
arthralgias,
myalgias.

bioavailability orally.
Distribution:
Widely distributed.
Crosses the
placental barrier
and enters breast
milk. Proteinbinding: 20%
Metabolism:
Hepatic; converted
to N-oxide, S-oxide,
and
desmethylranitidine.
Excretion: urine
(unchanged drug)
within 24hrs; feces;
2-3hr t1/2

Sumatriptan
is a selective
serotonin
agonist that
acts at 5HT1

Dizziness,
drowsiness,
sensory
disturbance
including
paresthesia &

Absorption:
Rapidly but
incompletely
absorbed from the
GIT (oral); peak
plasma

histamine H2receptor
antagonist
similar to
cimetidine and
famotidine. An
H2-receptor
antagonist,
often
shortened to
H2 antagonist,
is a drug used
to block the
action of
histamine on
parietal cells in
the stomach,
decreasing acid
production by
these cells.
These drugs
are used in the
treatment of
dyspepsia,
however their
use has waned
since the
advent of the
more effective
proton pump
inhibitors. Like
the H1antihistamines,
the H2
antagonists are
inverse
agonists rather
than true
receptor
antagonists.
Sumatriptan,
an
antimigraine
drug, is a
selective
agonist of

Ranitidine) Al- &


Mg-hydroxide
antacids,
propantheline
bromide,
warfarin,
paracetamol.
Triazolam,
ketoconazole.

300 mg, 75
mg

Clodine;
Contracid;
Dalycrid; Diranite;
Entac Ampoule;
Loracid; Pep-Bloc;
Peptica; Pharex
Ranitidine; Phil
Pharmawealth/Atl
antic Ranitidine;
Ramadine;
Ranifin; Raxide;
RiteMED
Ranitidine;
Ulcemed;
Ulcepac; Ulcerix;
Ulcin; Ulzim;
Zantac/Zantac 75;
Zeptag

Take
ergotaminecontaining prep
6 hr apart.
MAOIs, SSRIs,
triptans &

Tab 50mg

Imigran

Hydroxyzi
ne

receptors. It
causes
vasoconstric
tion of
cranial
arteries
and/or
inhibition of
neurogenic
inflammator
y processes
in the CNS.
A small but
significant
delay in
gastric
emptying
also occurs.

hypoesthesia,
transient
increase in BP,
flushing;
dyspnea;
nausea,
vomiting;
heaviness
sensation; pain,
heat or cold
sensation,
pressure or
tightness;
feeling of
weakness,
fatigue.

concentrations
reached in 2 hr
(oral), 25 min
(subcutaneous), 1.5
hr (intranasal).
Bioavailability for
oral is 14%,
subcutaneous 96%
and intranasal is
16% of that
achieved in
subcutaneous.
Distribution:
Enters breast milk.
Protein-binding: 1421%
Metabolism:
Extensive first-pass
metabolism by MAO
type A
Excretion: Mainly
via urine (as
inactive indole
acetic acid
derivative and its
glucuronide), via
faeces (as
unchanged drug and
metabolites).
Elimination half-life:
2hr.Imi

vascular
serotonin ((5hydroxytrypta
mine; 5-HT)
type 1-like
receptors,
likely the 5HT1D and 5HT1B subtypes.
It has no
significant
affinity (as
measured
using standard
radioligand
binding assays)
or
pharmacologic
al activity at 5HT2, 5-HT3
receptor
subtypes or at
alpha1-,
alpha2-, or
betaadrenergic;
dopamine1;
dopamine2;
muscarinic; or
benzodiazepine
receptors.

SNRIs.

Hydroxyzine
blocks
histamine
H1-receptors
on effector
cells of the
GI tract,
blood
vessels and
respiratory
tract; a
sedating
anihistamine
with

Somnolence,
headache,
fatigue, dry
mouth.

Absorption:
Absorbed rapidly
from the GI tract
(oral).
Distribution:
Protein binding: 93%
Metabolism:
Hepatic. Converted
to cetirizine (has
antihistaminic
properties).
Excretion: 20 hr
t1/2.

Hydroxyzine, a
piperazine
antihistamine
structurally
related to
buclizine,
cyclizine, and
meclizine, is
used to treat
histaminemediated
pruritus or
pruritus due to
allergy, nausea

CNS
depressants eg
alcohol,
anticholinergics
, betahistine,
anticholinestera
se drugs,
MAOIs,
epinephrine,
phenytoin,
cimetidine,
CYP2D6
substrates,
arrhythmogenic

Syr 2mg/mL;
Tab 10mg,
25mg

Iterax

antimuscari
nic and
significant
sedative
properties. It
also
possesses
skeletal
muscle
relaxing,
bronchodilat
or,
antiemetic
and
analgesic
properties.

Fluoxetine

Fluoxetine is
a potent and
highly
selective
inhibitor of
serotonin (5HT) reuptake. No
affinity for
adrenocepto
rs or
histamine,
GABA-B, or
muscarinic
receptors.

Dry mouth. GI
disturbances eg
nausea,
vomiting,
dyspepsia,
constipation &
diarrhea.
Anorexia & wt
loss.
Neurological
effects.
Excessive
sweating,
pruritus, skin
rashes &
urticaria.
Angioedema &
anaphylactic
shock.
Hyponatremia
particularly in
the elderly.
Hyperprolactine
mia,
galactorrhea,

Absorption: Oral
admin: Readily
absorbed from the
GI tract; peak
plasma
concentrations after
6-8 hr.
Distribution:
Widely distributed;
enters breast milk.
Protein-binding:
95%.
Metabolism:
Extensively hepatic
by demethylation to
norfluoxetine.
Excretion: Urine.
Elimination half-life:
1-3 days
(fluoxetine), 4-16
days (norfluoxetine).

and vomiting,
and, in
combination
with an opiate
agonist,
anxiolytic pain.
Hydroxyzine is
also used as a
perioperative
sedative and
anxiolytic and
to manage
acute alcohol
withdrawal.
Hydroxyzine's
active
metabolite,
cetirizine, is
also used as an
H1-antagonist.

drugs, alcohol
dehydrogenase
& CYP3A4/5
inhibitors.

Fluoxetine, an
antidepressant
agent
belonging to
the selective
serotonin
reuptake
inhibitors
(SSRIs), is used
to treat
depression,
bulimia
nervosa,
premenstrual
dysphoric
disorder, panic
disorder and
post-traumatic
stress.
According to
the amines
hypothesis, a
functional
decrease in the
activity of

Synergistic
effects w/
MAOIs.
Increases
benzodiazepine
plasma conc.
Elevates
plasma levels of
thioridazine &
anticonvulsants
, blood levels of
haloperidol &
clozapine.
Tryptophan,
lithium,
selegiline.

Cap 20mg

Adepssir;
Deprizac;
Magrilan;
Motivest;
Neuxetin; Prodin

arthralgia &
myalgia. Chest
pain & chills.

amines, such
as serotonin
and
norepinephrine
, would result
in depression;
a functional
increase of the
activity of
these amines
would result in
mood
elevation.
Fluoxetine's
effects are
thought to be
associated with
the inhibition of
5HT receptor,
which leads to
an increase of
serotonin level.
Antagonism of
muscarinic,
histaminergic,
and 1
adrenergic
receptors has
been
hypothesized
to be
associated with
various
anticholinergic,
sedative, and
cardiovascular
effects of
classical
tricyclic
antidepressant
(TCA) drugs.
Fluoxetine
binds to these
and other
membrane
receptors from

brain tissue
much less
potently in
vitro than do
the tricyclic
drugs.
References:
http://www.drugbank.ca/
http://www.mims.com/PHILIPPINES/home/Index