Description

Aprepitant is a selective high affinity antagonist of human substance P neurokinin 1 (NK1) receptors. When substance P attaches to these receptors, it causes nausea and vomiting. Aprepitant stops substance P from binding to the NK1 receptors. By blocking the receptors, Aprepitant can prevent nausea and vomiting, which often happens after chemotherapy or as a complication of surgery.

Aprepitant is a substrate, a weak-to-moderate (dose dependent) inhibitor, and an inducer of CYP3A4. Aprepitant is also an inducer of CYP2C9. Precautions should be taken while coadministering Aprepitant with drugs that use CYP3A4 or CYP2C9, for example- Warfarin, Tolbutamide, Phenytoin, Ketoconazole, Itraconazole, Nefazodone, Troleandomycin, Clarithromycin, Ritonavir, Nelfinavir, Diltiazem, Rifampin, Carbamazepine etc.   Upon coadministration with Aprepitant, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or back-up methods of contraception should be used during treatment with Aprepitant and for 1 month following the last dose of Aprepitant.

Aprepitant is contraindicated in patients who are hypersensitive to any component of the product. Aprepitant should not be used concurrently with Pimozide, Terfenadine, Astemizole & Cisapride.

Constipation, Hypotension, Pruritus, Pyrexia

Pregnancy Category B. This drug should be used during pregnancy only if clearly needed. It is not known whether this drug is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug based on patient’s importance.

Patients with Renal Impairment: No dosage adjustment is necessary for patients with renal impairment or for patients with end-stage renal disease (ESRD) undergoing hemodialysis. Patients with Hepatic Impairment: No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment.