In combination with other antiemetic agents to prevent acute and delayed nausea and vomiting associated with initial and repeat courses of moderately to highly emetogenic cancer chemotherapy, including high-dose cisplatin.
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.
Adjunct to dexamethasone and a 5HT3-receptor antagonist in preventing nausea and vomiting associated with moderately and highly emetogenic chemotherapy BY MOUTH Adult: Initially 125 mg, dose to be taken 1 hour before chemotherapy, then 80 mg once daily for 2 days, consult product literature for dose of concomitant corticosteroid and 5HT3-antagonist
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.
Common or very common Anorexia . asthenia . constipation . diarrhoea . dizziness . dyspepsia . headache . hiccups Uncommon Abdominal pain . abnormal dreams . acne . anaemia . anxiety . bradycardia . chills . colitis . confusion . conjunctivitis . cough . drowsiness . dry mouth . duodenal ulcer . dysuria . euphoria . flatulence . flushing . haematuria . hyperglycaemia . hyponatraemia . myalgia . neutropenia . oedema . palpitations . pharyngitis . photosensitivity . polyuria . pruritus . rash . sneezing . stomatitis . sweating . taste disturbance . thirst . tinnitus . weight changes Frequency not known Dysarthria . dyspnoea . insomnia . Stevens-Johnson syndrome . urticaria . visual disturbances
PREGNANCY Avoid unless potential benefit outweighs risk?no information available. BREAST FEEDING Avoid?present in milk in animal studies.
No specific information is available on the treatment of overdosage with Aprepitant. Single doses up to 600 mg of Aprepitant were generally well tolerated in healthy subjects. Drowsiness and headache can be seen due to overdose. In the event of overdose, Aprepitant should be discontinued. General supportive treatment and monitoring should be provided. Because of the antiemetic activity of Aprepitant, medicine-induced emesis may not be effective. Aprepitant cannot be removed by hemodialysis.
Keep below 30°C temperature, away from light & moisture. Keep out of the reach of children.
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