Anti Histamin

H 1 receptor
antagonists

Histami
ne
H1
Receptors
Ca2+

Smooth muscle
contraction
Increased capillary
permeability
Vasodilation
Sensory nerve endings
pain & itching

H2
Receptors
cAMP

Gastric acid
secretion
Blood vessels:
vasodilation
Increased capillary
permeability

H3 Receptors
(presynaptic auto
receptors)
cAMP

histamine release
secretion
Vasodilation

Type
H1 histamine
receptor

H2 histamine
receptor
H3 histamine

Location
Function
Vasodilation,
Smooth musclespasmodic contractions of Bronchoconstriction,
bronchial smooth
ileum, uterus, diarrhoea
Exocrine glandsmuscle contraction
pancreas, salivary,
separation of
lacrimal
endothelial cells
Endothelium
(responsible for
CNS tissue
hives), and pain and
itching due to insect
stings;
the primary
receptors involved in
allergic rhinitis
symptoms and
motion sickness;
sleep regulation.
Primarily stimulate
Located on parietal cells
gastric acid secretion
Decreased
Found on central nervous neurotransmitter
system and to a lesser
release: histamine,

Common allergic
reactions

Clinical Symptoms erythema,

Associated
With
urticaria,
Histamine Release and/or itching
Mild/cutaneous
Mild to moderate

Severe/anaphylac
tic

skin reactions,
tachycardia,
dysrhythmias, moderate
hypotension, mild
respiratory distress
severe hypotension,
ventricular fibrillations,
cardiac arrest,
bronchospasm,
respiratory arrest

Antihistamines
Antihistamines
are reversible competitive antagonists of histamine
at H1 receptor sites.
inhibits the action of histamine by either blocking its
attachment to histamine receptors, or
inhibiting the enzymatic activity of histidine
decarboxylase which catalyzes the transformation of
histidine into histamine

Classification
H 1 receptor antagonists
1st Generation:
dimenhydrinate, Diphenhydramine, Doxylamine,
Hydroxyzine, Promethazine
clemastine, Pyrilamine, Cyproheptadine,
Pheniramine,
chlorpheniramine, Triprolidine, Cyclizine,

2nd Generation:
Terfenadine, Astemizole, Cetirizine, Loratadine,
Mizolastine, Fexofenadine, Ebastine

3rd Generation:
Desloratadin, Levocetrizine ,
Note :
Terfenadine and astemizole were removed from the market due to serious
cardiovascular events related to torsade de pointes.

Perbedaan Antar generasi anti

histamin
1 st
generatio
n
Sedation
Anticholliner
gic property

2nd generation
-absence of sedation
-devoid of antichollinergic
effects

3rd generation

Second generation drugs

with decreased cardiac side
effect

Perbedaan Antar generasi anti

histamin

Klasifikasi anti histamin

berdasarkan struktur kimianya

H 1 receptor antagonists

Adverse effects

Sedation ,alertness

Motor incoordination
Tendency to fall sleep

Blurred vision

Anticholinergic

Urinary retention

Constipation
ABCD &
U

Dry mouth

H 1 receptor antagonists

USES

Allergic disorders

Urticaria , Angioedema ,
Conjunctivitis , Rhinitis
Itching (Pruritus)
Chlorpheniramine
Diphenhydramine

Common Cold

H 1 receptor antagonists

USES

Motion sickness

Promethazine , Diphenhydramine ,
Meclizine, dimenhydrinate

Morning sickness (vomiting of early pregnancy)

Doxylamine , Meclizine

H 1 receptor antagonists

USES

Vertigo

Dimenhydrinate , Promethazine

Perbedaan anti Histamin

generasi I, II dan III

Third

Terima Kasih