Histadine, Seratonin

Question 1

Class;Mechanism;Therapeutics;SideEffects

H1 receptor antagonist

Answer 1

— H1 receptor antagonist; rapidly absorbed orally, widely distributed, rapidly metabolized via liver microsomes Allergic reactions, motion sickness, nausea and vomiting in pregnancy, sleep aids Sedation, anti-muscarinic action, poisoning (especially children) with convulsions, allergy, local anesthesia — Older agents cross CNS to cause central effects

Question 2

Class;Mechanism;Therapeutics;SideEffects

Diphenhydramine (Benadryl)

Answer 2

Ether/ethanolamine derivitive H1 receptor antagonist — Anti-muscarinic, sedating — —

Question 3

Class;Mechanism;Therapeutics;SideEffects

Tripelennamine (Pyribenzamine)

Answer 3

Ethylenediamine derivitive H1 receptor antagonist OTC sleep aid — — —

Question 4

Class;Mechanism;Therapeutics;SideEffects

Cyclizine (Marezine)

Answer 4

Piperazine derivative H1 receptor antagonist Motion sickness — — —

Question 5

Class;Mechanism;Therapeutics;SideEffects

Promethazine (Phenergan)

Answer 5

Phenothiazine derivative H1 receptor antagonist Antiemetic Anti-muscarinic, sedating — —

Question 6

Class;Mechanism;Therapeutics;SideEffects

Chlorpheniramine (Chlor-Trimeton)

Answer 6

Alkylamine derivitive H1 receptor antagonist Component of “cold” medications Less sedating — —

Question 7

Class;Mechanism;Therapeutics;SideEffects

Loratadine (Claritin)

Answer 7

Piperidine derivitive 2nd generation H1 receptor antagonist Allergic rhinitis No sedation Cardiovascular effects (rare, with high doses) Poorly crosses BBB, so fewer central and side effects

Question 8

Class;Mechanism;Therapeutics;SideEffects

Fexofenadine (Allegra)

Answer 8

Piperidine derivitive 2nd generation H1 receptor antagonist Allergic rhinitis No sedation Cardiovascular effects (rare, with high doses) Poorly crosses BBB, so fewer central and side effects

Question 9

Class;Mechanism;Therapeutics;SideEffects

Azelastine (Astelin)

Answer 9

— 2nd generation H1 receptor antagonist Allergic rhinitis (intranasal spray), allergic conjunctivitis (ophthalmic solution) No sedation — Poorly crosses BBB, so fewer central and side effects

Question 10

Class;Mechanism;Therapeutics;SideEffects

Cetirizine (Zyrtec)

Answer 10

2nd generation H1 receptor antagonist Allergic rhinitis No sedation – Poorly crosses BBB, so fewer central and side effects

Question 11

Class;Mechanism;Therapeutics;SideEffects

Cimetidine (Tagamet)

Answer 11

— H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion) Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions Antiandrogen (causing impotence and gynecomastia), inhibition of P450 enzymes CNS dysfunction possible Most side effects of H2-blocker class

Question 12

Class;Mechanism;Therapeutics;SideEffects

Ranitidine (Zantac)

Answer 12

— H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion) Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions Liver toxicity CNS dysfunction possible —

Question 13

Class;Mechanism;Therapeutics;SideEffects

Famotidine (Pepcid)

Answer 13

— H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion) Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions — CNS dysfunction possible —

Question 14

Class;Mechanism;Therapeutics;SideEffects

Nizatidine (Axid)

Answer 14

— H2 receptor antagonist; blocks gastric acid secretion (more so with nocturnal acid secretion than meal secretion) Dyspepsia, duodenal and gastric ulcers, hypersecretory conditions — CNS dysfunction possible Least side effects of H2-blocker class

Question 15

Class;Mechanism;Therapeutics;SideEffects

Cyproheptadine (Periactin)

Answer 15

— Antihistaminic and antiserotinergic Skin allergies (urticaria, anti-5HT1), diarrhea of carcinoid syndrome (anti-5HT2) — Sedation, antimuscarinic —

Question 16

Class;Mechanism;Therapeutics;SideEffects

Ketanserin

Answer 16

— Selective 5HT2A,2C receptor antagonist, as well as _1 and H1 receptor antagonist Antihypertensive (relaxes vascular and tracheal smooth muscle), antiplatelet aggregation — — —

Question 17

Class;Mechanism;Therapeutics;SideEffects

Odansetron (Zofran)

Answer 17

— 5HT3 receptor antagonist Nausea and vomiting in chemotherapy — — —

Question 18

Class;Mechanism;Therapeutics;SideEffects

Ergot alkaloids

Answer 18

— Agonist and antagonist actions at 5HT and _-adrenergic receptors — Powerful hallucinations, smooth muscle contraction (vascular and uterine) — —

Question 19

Class;Mechanism;Therapeutics;SideEffects

Ergotamine (Ergomar)

Answer 19

Ergot alkaloid Nonspecific partial agonist at all 5HT1,2 receptors; partial agonist at _-adrenergic receptors Prodrome of migraines — N/V, cumulative and prolonged vasoconstriction —

Question 20

Class;Mechanism;Therapeutics;SideEffects

Methysergide (Cycloset)

Answer 20

Ergot alkaloid Partial agonist at all 5HT1 receptors, antagonist at 5HT2 Prophylaxis of migraines — GI disturbances, inflammatory fibrosis (chronic use), hallucinations Withdrawn from U.S. market

Question 21

Class;Mechanism;Therapeutics;SideEffects

Ergonovine

Answer 21

Ergot alkaloid — Postpartum hemorrhage (Oxytocic) — — —

Question 22

Class;Mechanism;Therapeutics;SideEffects

Bromocriptine (Sansert)

Answer 22

Ergot alkaloid Dopamine agonist Hyperprolactinemia — — —

Question 23

Class;Mechanism;Therapeutics;SideEffects

Triptans

Answer 23

Non-ergot serotonin analogs 5HT1B,D receptor agonist Effective (70%) migraine treatment — — —