Histaminergic Agents Flashcards
H1
smooth muscle
Gq
increased IP3, DAG
pain and itching
bronchonstriction
vasodilation
local edema
H1 receptor antagonist
1st Generation
Diphenhydramine
Brompheniramine
Chlopheniramine
Promethazine
Cyproheptadine
Cyclizine
Meclizine
Buclizine
Dimenhydrinate
H1 receptor antagonist
1st Generation
allergic reactions, hay fever, angioedema, insomnia
Diphenhydramine
H1 receptor antagonist
1st Generation
cold medications
Brompheniramine
Chlopheniramine
H1 receptor antagonist
1st Generation
anti-emetic
decrease secretions during anesthetic induction
Promethazine
H1 receptor antagonist
1st Generation
serotonin syndrome
Cyproheptadine
H1 receptor antagonist
1st Generation
motion sickness
Cyclizine
Meclizine
H1 receptor antagonist
1st Generation
nausea, vomiting and dizziness
Dimenhydrinate
H1 receptor antagonist
2nd Generation
Cetirizine
Levocetirizine
Loratadine
Desloratadine
Fexofenadine
Terfenadine
Rupatadine
Astemizole
Azelastine
Ebastine
Bilastine
Carboxylated hydroxyzine
Cetirizine
H2
stomach
heart
mast cells
gastric acid secretion
cardiac stimulation
H2 receptor antagonist
nocturnal acid attacks
PUD
Cimetidine
Ranitidine
Famotidine
Nizatidine
CYP450 INHIBITOR - Cimetidine
SE: Cimetidine - gynecomastia
Strong antagonist of H3 receptor (inc levels of NT histamine, serotonin, acetylcholine, NE, GABA) and weak agonist of H1 receptor (local vasodilation and increased permeability to inner ear)
Used for balance disorders or to alleviate vertigo symptoms
Betahistine
Promotes cerebral blood flow
For nausea and vomiting d.t. motion sickness, chemotherapy, vertigo or Meniere’s disease
Cinnarizine
Triple Response of Lewis
classic demonstration of histamine effect
mediated by H1 and H2 receptors
wheal
flush
flare