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Aprepitant

CENTRAL NERVOUS SYSTEM

ANTIEMETICS & ANTINAUSEANTS - [ CENTRAL NERVOUS SYSTEM ]

Aprepitant is an antiemetic drug. It is an antagonist at the NK1 receptor of the substance P and useful in conditions of delayed vomiting which are at times not inhibited by serotonin antagonists.(1)

In combination with other antiemetic agents for the: prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin prevention of nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy For the prevention of postoperative nausea and vomiting (PONV).(2)

Hypersensitivity to the drug or any constituents of the formulation. Concomitant use with pimozide, terfenadine, astemizole, or cisapride.(2)

Asthenia, fatigue, dizziness, dehydration, abdominal pain, fever. Nausea, constipation, diarrhea, vomiting. Heartburn, gastritis and epigastric discomfort. Tinnitus, anorexia, insomnia, headache, hiccups.(2)

Drugs metabolized by CYP3A4: Increased levels of these drugs at higher doses of aprepitant. Dexamethasone, methylprednisolone: Increased levels of these drugs. Warfarin and tolbutamide: Decreased levels of these drugs.(2)

Safety and efficacy is not established in pediatric patients.(2)

Prevention of Chemotherapy Induced Nausea and Vomiting: Aprepitant is given for 3 days as part of the chemotherapy induced nausea and vomiting (CINV) regimen that includes a corticosteroid and a 5-HT3 antagonist. The recommended dose of Aprepitant is 125 mg orally 1 hour prior to chemotherapy treatment (Day 1) and 80 mg orally once daily in the morning on Days 2 and 3. Fosaprepitant dimeglumine for Injection may be substituted for oral aprepitnant (125 mg) on Day 1 only as part of the CINV regimen. Prevention of Postoperative Nausea and Vomiting: 40 mg within 3 hours prior to induction of anesthesia.(2)

1. Brunton LL, Chabner BA, Knollmann BC, editors. Goodman & Gilman’s The Pharmacological Basis of Therapeutics. 12th ed. China: McGraw Hill; 2011. 2. Emend [cited 2013 Sept 18]. Available from: http://www.accessdata.fda.gov/drugsatfda_docs/label/2013/021549s023lbl.pdf