Medical Pharmacology: Gastrointestinal Pharmacology Practice Questions
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Emetogenic chemotherapy is associated with both an acute phase and a delayed phase. Agents belonging to this class of drugs are particularly effective for managing the acute phase.
? 5-HT3 receptor blockers ? Neurokinin 1 (NK1)
Emetogenic chemotherapy is associated with both an acute phase and a delayed phase. Agents belonging to this class of drugs are particularly effective for managing the delayed phase.
? Neurokinin receptor blockers (NK1 receptor antagonist) ? 5-HT3 receptor antagonists
NK1 receptors represent receptors for the neuropeptide substance P.
? True ? False
Example(s) of (an) NK1 receptor antagonist(s):
? Aprepitant (Emend) ? Rolapitant (Varubi; Varuby) ? Both ? Neither
Rolapitant exhibits an unusually long t1/2
(about four days).
? True ? Falls
Administration, plasma protein binding and metabolism of aprepitant:
? Aprepitant is typically given as monotherapy to manage delayed emesis. ? Aprepitant is substantially associated with plasma protein to >95%. ? Aprepitant is metabolized by the liver drug metabolizing system, the cytochrome P450 system mainly catalyzed by the CYP3A4 isoform. ? A & B ? B & C ? A & C ? A, B & C
Due to the possibility of life-threatening ECG QT prolongation, aprepitant should not be administered to patients receiving:
? Cisapride (Propulsid) ? Pimozide (Orap) ? Both ? Neither
Example(s) of drug(s) metabolized by CYP3A4 and thus subject to dose adjustment in individuals receiving aprepitant (CYP3A4 substrate)
? Methylprednisolone ? Warfarin ? Dexamethasone ? A & B ? B & C ? A & C ? A, B & C
Rolapitant:
? Administered typically in a single-dose, 1-2 hours before chemotherapy (in combination with dexamethasone and a 5-HT3 antagonist) ? Administration of rolapitant may be associated with adverse effects including neutropenia, dizziness, reduced appetite. ? Both ? Neither
A relatively recent approved drug combination involves netupitant along with palonosetron.
? True ? False
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