Histamine and Serotonin Drugs Class/Mechanism Flashcards
(26 cards)
How are H1 receptor antagonists metabolized and how fast?
rapidly metabolized via liver microsomes
What are H1 receptor antagonists used for and what are their general side effects?
Use: allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids.
SE: sedation; anti-muscarinic action, poisoning (especially children) with convulsions, allergy, local anesthesia
Diphenhydramine (Benadryl)
class
mech
SE
Ether/ethanolamine derivative
H1 receptor antagonist
SE: anti-muscarinic, sedation
Tripelennamine
Class
Mech
Use
ethylenediamine derivative
H1 receptor antagonist
Use: OTC sleep aid
Cyclizine
Class
Mech
Use
Piperazine derivative
H1 receptor antagonist
Use: Motion sickness
Promethazine class mech use SE
phenothiazine derivative
H1 receptor antagonist
Use: Antiemetic
SE: Anti-muscarinic, sedation
Chlorpheniramine Class mech use SE
Alkylamine
H1 receptor antagonist
Use: Component of cold meds
SE: less sedation
Laratadine (claritin) class mech use SE
Piperidine derivative
2nd gen H1 receptor antagonist
Use: Allergic rhinitis
SE: no sedation, rare CV effects
Fexofenadine (allegra) Class mech use SE
Piperidine derivative
2nd gen H1 receptor antagonist
Use: Allergic rhinitis
SE: no sedation, rare CV effects
Azelastine
mech
use
SE
2nd gen H1 receptor antagonist
Use: allergic rhinitis (internasal spray), allergic conjunctivitis (opthalmic solution)
SE: No sedation
Cetirizine
mech
use
SE
2nd gen H1 receptor antagonist
Use: allergic rhinitis
SE: No sedation
Cimetidine
Mech
use
SE
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Use: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
SE: Antiandrogen (causing impotence and gynecomastia), inhibition of P450 enzymes
Ranitidine (Zantac)
Mech
Use
SE
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Use: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
SE: Liver toxicity
Famotidine
Mech
Use
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Use: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
Nizatidine
Mech
Use
H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Use: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
Why do second gen H1 antagonists cause less sedation?
poorly cross BBB
What is a possible SE of all H2 antagonists?
CNS dysfunction possible
Cyproheptadine
mech
Use
SE
Antihistaminic and antiserotinergic
Use: Skin allergies (urticaria, anti-5HT1)
Diarrhea of carcinoid syndrome (anti 5HT2)
SE: Sedation, antimuscarinic
Ketanserin
Mech
Use
Selective 5HT2A, 2C receptor antagonist as well as alpha 1 and H1 receptor antagonist
Use: Antihypertensive (Relaxes vascular and tracheal smooth muscle), antiplatelet aggregation
Odansetron
Mech
Use
5HT3 receptor antagonist
Use: Nausea and vomiting in chemotherapy
Ergot Alkaloids
Mech
SE
Agonist and antagonist actions at 5HT and alpha adrenergic receptors (also some dopamine)
SE: powerful hallucinations, smooth muscle contraction (vascular and uterine)
Ergotamine Class Mech Use SE
Ergot alkaloid
nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at alpha adrenergic receptors
Use: Prodrome of migraines
SE: N/V, cumulative and prolonged vasoconstriction
Methysergide Class Mech use SE
Ergot alkaloid
partial agonist at all 5HT1 receptors, antagonist at 5HT2
Use: Prophylaxis of migraines
SE: GI disturbances, inflammatory fibrosis (chronic use), hallucinations
Ergonovine
Class
Mech
Use
ergot alkaloid
alpha agonists
pospartum hemorrhage (Oxytocic)
