Anti Histamin

H1 receptor antagonists
 Histamine

H1 Receptors H2 Receptors H3 Receptors

(presynaptic auto
receptors)

↑ Ca2+ ↑ cAMP ↓ cAMP

Smooth muscle contraction ↑ Gastric acid secretion ↓ histamine release

Increased capillary Blood vessels: ↓secretion
permeability vasodilation Vasodilation
Vasodilation Increased capillary
Sensory nerve endings pain permeability
& itching
 Type Location Function
H1 histamine receptor •Smooth muscle-spasmodic  Vasodilation,
contractions of ileum, uterus,  Bronchoconstriction,
diarrhoea  bronchial smooth muscle
•Exocrine glands-pancreas, contraction separation of
salivary, lacrimal endothelial cells
• Endothelium (responsible for hives),
• CNS tissue and pain and itching due
to insect stings;
 the primary receptors
involved in allergic rhinitis
symptoms and motion
sickness;
 sleep regulation.

Primarily stimulate gastric

H2 histamine receptor Located on parietal cells
acid secretion
Decreased neurotransmitter
Found on central nervous system
release: histamine,
H3 histamine receptor and to a lesser extent peripheral
acetylcholine,
nervous system tissue
norepinephrine, serotonin
Common allergic
reactions
 Clinical Symptoms Associated With
Histamine Release
• Mild/cutaneous • erythema, urticaria, and/or
itching
• skin reactions, tachycardia,
• Mild to moderate
dysrhythmias, moderate
hypotension, mild respiratory
distress
• severe hypotension,
• Severe/anaphylactic 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
H1 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

2nd generation
1st
generation -absence of sedation
-devoid of antichollinergic effects
•Sedation
•Antichollinergic 3rd generation
property
Second generation drugs with
decreased cardiac side effect
Perbedaan Antar generasi anti histamin
 Klasifikasi anti histamin
berdasarkan struktur kimianya
 H1 receptor antagonists

Adverse effects
Sedation ,↓alertness
Motor incoordination
Tendency to fall sleep
 Anticholinergic
Blurred vision Constipation Dry mouth

Urinary retention ABCD & U

H1 receptor antagonists
USES
 Allergic disorders
Urticaria , Angioedema , Conjunctivitis , Rhinitis

Itching (Pruritus)
Chlorpheniramine
Diphenhydramine

Common Cold
 H1 receptor antagonists
USES
Motion sickness
Promethazine , Diphenhydramine , Meclizine,
dimenhydrinate

Morning sickness (vomiting of early pregnancy)

Doxylamine , Meclizine
 H1 receptor antagonists
USES
Vertigo
Dimenhydrinate , Promethazine
Perbedaan anti Histamin
generasi I, II dan III
Third
Terima Kasih