Aprepitant (Aprepitant)
Overview of Aprepitant
Aprepitant is a substance P/neurokinin 1 (NK1) receptor antagonist and prevents the stimulation of the vomiting center and chemotherapy receptor trigger zone in the brain, chemically described as 5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2dihydro-3H-1,2,4-triazol-3-one. Its empirical formula is C23H21F7N4O3. Fosaprepitant dimeglumine is a prodrug of aprepitant for Injection and may be substituted for oral.
Indication of Aprepitant
Aprepitant is primarily indicated in conditions like Nausea and vomiting (chemotherapy induced), Post operative vomiting.
Contraindication of Aprepitant
Aprepitant is contraindicated in conditions like Hypersensitivity to any component of product.
Side Effects of Aprepitant
The signs and symptoms that are produced after the acute overdosage of Aprepitant include Drowsiness, Headache.,The symptomatic adverse reactions produced by Aprepitant are more or less tolerable and if they become severe, they can be treated symptomatically, these include Nausea, Vomiting, Diarrhea, Constipation, Heart burn, Hiccups, Pain at injection site, Stomach pain.
Precautions of Aprepitant
Aprepitant a dose-dependent inhibitor of CYP3A4 should be used with caution in patients receiving concomitant medications that are primarily metabolized through CYP3A4. Moderate inhibition of CYP3A4 by aprepitant, 125 mg/80 mg regimen, could result in elevated plasma concentrations of these concomitant medications. Caution should be exercised when aprepitant is administered in sever hepatic impairment. This drug should be used during pregnancy only if clearly needed. Safety and effectiveness of aprepitant in pediatric patients have not been established.