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Antiemetics

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zidazije's version from 2017-04-17 00:20

Section 1

Question Answer
Promethazine (Phenergan)antihistamine, 2nd line therapy in pregnancy
Meclizine (Bonine)antihistamine
Dimenhydrinate (Dramamine)antihistamine
Cyclizine (Marezine)antihistamine
Doxylamine, pyridoxine (Diclegis)combination used for morning sickness in pregnancy
Pyridoxime (Vitamin B6)1st line antiemetic in pregnancy
Scopolamine (Transderm Scop Patch)anticholinergic, Prophylaxis of motion sickness
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Serotonin receptor antagonists

Question Answer
Dolasetron (Anzemet)5-HT3 antagonist,
Granisetron (Kytril)5-HT3 antagonist, use 24-48 hrs prior to chemo, available as patch ($450/patch)
Ondansetron (Zofran)5-HT3 antagonist, class prototype, BID dosing
Palonosetron (Aloxi)5-HT3 antagonist, IV ONLY, Highest receptor affinity, positive cooperatively & insurmountable antagonism
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D2 antagonists

Question Answer
Prochlorperazine (Compazine) D2 receptor antagonist, used at lower dosage than antipsychotic
Metoclopramide (Reglan) D2 receptor antagonist, used at lower dosage than antipsychotic
ADRs of D2 antagonists anticholinergic, antimuscarinic, and extrapyramidal effects
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NK-1 antagonists

Question Answer
NK-1 antagonist MoA Blocks binding of substance P --> decreased perception of visceral pain
Aprepritant (Emend) NK-1 antagonist,
Rolapitant (Varubi) NK-1 antagonist,
Indications Delayed portions of CINV, also has long DoA 120 hrs with 90% receptor blockade
Netupitant, palonosetron (Akynzeo) prevention of both the acute and delayed phase of CINV, PO formulation
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