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Aprepitant

Aprepitant

It is an antiemetic chemical compound that belongs to a class of drugs called substance P antagonists. It mediates its effect by blocking the neurokinin (NK1) receptor. It is used for prevention of acute and delayed chemotherapy-induced nausea and vomiting and for prevention of postoperative nausea and vomiting.

Indications

Prophylaxis of chemotherapy-induced nausea and vomiting, Prophylaxis of Postoperative nausea and vomiting.


Dosage

(Oral) For Prophylaxis of chemotherapy-induced nausea and moviting, to go given for 3 days as part of a regimen containing a corticosteroid and a 5HT3 antagonist. Day 1:125mg (1 Hr before chemotherapy); days 2 and 3: 80mg once daily. For Prophylaxis of postoperative nausea and vomiting, 40mg within 3 hr prior to induction of anaesthesia.


Contra-Indications

Concomitant use with astemizole, cisapride, pimazole, terfinadine.


Special Precautions

Moderate to severe hepatic impairment. Concurrent use with strong/moderate CYP3A4 inhibitors, inducers or substrates. Monitor INR closely for patients on warfarin. Not recommended in lactation and Pregnancy.


Side Effects

Headache, dizziness, nausea, vomiting, hiccups, thirst, constipation, abdominal pain, dyspepsia, diarrhoea, dehydration, fatigue, cough, hypotension, hypertension, angioedema, elevated ALT and AST levels, proteinuria, increased BUN. Hypersensitivity reactions, Steven-Johnsons syndrome.


Drug Interactions

Concurrent use with CYP3A4 inhibitors (e.g. clarithromycin, troleandomycin, diltiazem, verapamil, itraconazole, ketoconazole, nefazodone, ritonavir, nelfinavir) may lead to increased plasma, levels of Aprepitant; concurrent use with CYP3A4 inducers (e.g. carbamazepine, phenytoin, rifampicin, primidone, phenobarbitol,) may lead to reduced efficacy of Aprepitant. May reduce efficacy of oral contraceptives, With other drugs, astemizole, cisapride, pimozide, terfenadine, phenytoin, tolbutamide, warf


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