Histamine, Serotonin, and Antagonists Flashcards
Diphenhydramine (Benadryl)
Mechanism: H1 receptor antagonist
Therapeutics: Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids
Side Effects: Anti-muscarinic, sedating
Tripelennamine (Pyribenzamine)
Mechanism: H1 receptor antagonist
Therapeutics: OTC sleep aid
Side Effects: Anti-muscarinic, sedating
Cyclizine (Marezine)
Mechanism: H1 receptor antagonist
Therapeutics: Motion sickness
Side Effects: Anti-muscarinic, sedating
Promethazine (Phenergan)
Mechanism: H1 receptor antagonist
Therapeutics: Antiemetic
Side Effects: Anti-muscarinic, sedating
Chlorpheniramine (Chlor-Trimeton)
Mechanism: H1 receptor antagonist
Therapeutics: Component of “cold” medications
Side Effects: Less sedating
Loratadine (Claritin)
Mechanism: 2nd generation H1 receptor antagonist
Therapeutics: Allergic rhinitis
Side Effects: No sedation
Fexofenadine (Allegra)
Mechanism: 2nd generation H1 receptor antagonist
Therapeutics: Allergic rhinitis
Side Effects: No sedation
Azelastine (Astelin)
Mechanism: 2nd generation H1 receptor antagonist
Therapeutics: Allergic rhinitis (intranasal spray), allergic conjunctivitis (ophthalmic solution)
Side Effects: No sedation
Cetirizine (Zyrtec)
Mechanism: 2nd generation H1 receptor antagonist
Therapeutics: Allergic rhinitis
Side Effects: No sedation
Cimetidine (Tagamet)
Mechanism: H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Therapeutics: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
Side Effects: Antiandrogen (causing impotence and gynecomastia), inhibition of P450 enzymes
Ranitidine (Zantac)
Mechanism: H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Therapeutics: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
Side Effects: Liver toxicity
Famotidine (Pepcid)
Mechanism: H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Therapeutics: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
Nizatidine (Axid)
Mechanism: H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion)
Therapeutics: Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions
Cyproheptadine (Periactin)
Mechanism: Antihistaminic and antiserotinergic
Therapeutics: Skin allergies (urticaria, anti-5HT1), diarrhea of carcinoid syndrome (anti-5HT2)
Ketanserin
Mechanism: Selective 5HT2A,2C receptor antagonist, as well as α1 and H1 receptor antagonist
Therapeutics: Antihypertensive (relaxes vascular and tracheal smooth muscle), antiplatelet aggregation
Odansetron (Zofran)
Mechanism: 5HT3 receptor antagonist
Therapeutics: Nausea and vomiting in chemotherapy
Ergotamine (Ergomar)
Class: Ergot alkaloid
Mechanism: Nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at α-adrenergic receptors
Therapeutics: Prodrome of migraines
Methysergide (Cycloset)
Class: Ergot alkaloid
Mechanism: Partial agonist at all 5HT1 receptors, antagonist at 5HT2
Therapeutics: Prophylaxis of migraines
Ergonovine
Class: Ergot alkaloid
Therapeutics: Postpartum hemorrhage (Oxytocic)
Bromocriptine (Sansert)
Class: Ergot alkaloid
Mechanism: Dopamine agonist
Therapeutics: Hyperprolactinemia
Triptans
Class: Non-ergot serotonin analogs
Mechanism: 5HT1B,D receptor agonist
Therapeutics: Effective (70%) migraine treatment