H1 receptor and its

antagonist
Dr darshna kumari
Histamie
• Histamine is a biogenic amine .
• It synthesis from substance histadine by decarboxylation process.
• Histadine Histamine
• After synthesis it stores in granules form in mast cell of lungs, GIT,
lungs, placenta.
• It release from mast cell in response of antigen antibody reaction
(allergic reaction).
• If there is allergy from food, drugs, venom, trauma causes histamine
to release.
Receptors
• It act on following receptors after releasing from the mast cell.
• 1) H1 receptor (Gq coupled) involve in anaphylactic shock and
inflammation
• 2)H2 receptor (Gs coupled)involve in gastric acid secretion)
• 3)H3 receptor (Gi coupled) involve in negative feedback mechanisam
• 4)H4 receptor(Gi coupled) involve in chemotaxis, cytokines reaction
H1 recptor
• When H1 receptor is stimulate in smooth muscels and endothelial cells it
release nitric oxide, which causes smooth muscels relaxation , result in fall
in blood pressure and vasodialation.
• It increase capillary permeability causes edema by activation f H1 receptor.
• On heart it causes negative dramotropic effect mean slow down rate of
electrical impulse due to decrease in AV conduction.
• By acting on H1 receptor in visceral smooth muscels it result in
bronchoconstriction and in GIT it causes abdominal cramps.
• In brain it result activate reticular activating system maintain the
wakefulness of individual.
H1 receptor antagonist
• They are competitive blocker of H1 receptor.
• They are lipid soluble and cross placenta and have teratogenic effect.
• They require hepatic metabolisam.
Classification of drugs
• First generation drugs.
• It is antimuscarnic cause urinary retention and constipation.
• It acts as local anesthetic because it have sodium channel blocking
effect.
• it is antimotion sickness because of blocking of M,N, H1 receptor in
vestibular apparatus and vomiting center in CNS.
• Antiparkinsonian and CNS depression due to H1 blocking.
drugs
• 1)Diphenhydramine.
Widely sold OTC drug.
2)Promethazine
It have local anesthetic action
3)Chlorpheniramine
Known for its CNS stimulation effect
Meclizine is use for motion sickness
uses
• Allergies (rhinitis, dermatitis, conjunctivitis and uriticaria.
• Motion sickness and vertigo due to its muscarinic and histamine
blocking effect.
• Nausea and vomiting in pregnancy and chemotherapy due to
antimuscarnic and antihistamine effect.
• OTC sleeping aids and cold medication.
• Acute management of extrapyramidal symptoms.
Kinetics
• Well absorbed afer oral and parenteral administration.
• Widely distributed and metabolize and excreted in urine.
Adverse effect.
Sedation
Drowsiness
Headache
Fatigue
Weakness
Nausea
Vomiting
Loss of appetite
Second generation drugs
• They cant cross blood brain barrier.
• They are only use in allergies.
• They have no antimuscarnic,antimotion and no sedation effet.
• Drugs.
• Cetarizine
• It block H1 receptor and block histamine release.
• Loratidine rarely cause cardiac arrhythmia.
• Fexofenadine. Same arrythmia
Adverse effect
• Headache
• Cough
• Tiredness
• Sore throat
• Abdominal pain/discomfort
• Nausea and vomiting