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Aprepitant information from DrugsUpdate  

See Available Brands of Aprepitant in India

P - Caution when used during pregnancy
L - Caution when used during lactation
FI - Food *

Aprepitant is an antiemetic chemical compound that belongs to a class of drugs called substance P antagonists (SPA). It mediates its effect by blocking the neurokinin 1 (NK1) receptor.

Pharmacodynamics

Aprepitant is an antiemetic which acts as a substance P/neurokinin 1 (NK1) receptor antagonist. It also enhances antiemetic activity of 5HT3 antagonists and corticosteroid.

Pharmacokinetics

 


Absorption: Absorbed in the GI tract. Plasma concentrations peak after about 4 hr. Bioavailability: About 60-65%.


Distribution: Vd: About 70 L; crosses the blood-brain barrier; plasma protein binding: >95%.


Metabolism: Undergoes extensive hepatic metabolism via oxidation by cytochrome P450 isoenzyme CYP3A4, the isoenzymes CYP1A2 and CYP2C19 mediate minor metabolic pathways.


Excretion: Primarily by metabolism. Terminal elimination half-life: About 9-13 hr.


 

Aprepitant Indications / Aprepitant Uses

In Prophylaxis of chemotherapy-induced nausea and vomiting and in Prophylaxis of postoperative nausea and vomiting

Aprepitant Adverse Reactions / Aprepitant 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.


Potentially Fatal: Hypersensitivity reactions, Steven-Johnsons syndrome.


 

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. Pregnancy.

Other 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, phenobarbital) may lead to reduced efficacy of Aprepitant. May decrease concentrations of CYP2C9 substrates e.g. phenytoin, tolbutamide, warfarin. May increase plasma levels of dexamethasone and methylprednisolone. May increase plasma levels of benzodiazepine (e.g. midazolam, diazepam, alprazolam). Serum concentrations of colchicine may increase with Aprepitant. May increase toxicity of chemotherapy drug metabolised by CYP3A4 e.g. docetaxel, etoposide, ifosfamide, imatinib, paclitaxel, vincristine, vinblastin. May increase levels of ergot derivatives resulting in ergotism. May reduce efficacy of oral contraceptives, use additional methods of contraception during treatment and for at least 1 mth following the last dose of Aprepitant.


Potentially Fatal: May result in increased serum levels of astemizole, cisapride, pimozide and terfenadine which can lead to life-threatening torsade de pointes arrhythmias.


 

Other Interactions

Avoid grapefruit juice, may raise serum concentrations of Aprepitant. St John's wort may decrease Aprepitant levels.

Dosage

 


Oral


Prophylaxis of chemotherapy-induced nausea and vomiting


Adult: To be given for 3 days as part of a regimen containing a corticosteroid and a 5HT3 antagonist. Day 1: 125 mg (1 hr before chemotherapy); days 2 and 3: 80 mg once daily. 


Oral


Prophylaxis of postoperative nausea and vomiting


Adult: 40 mg within 3 hr prior to induction of anaesthesia.


 

Food(before/after)

May be taken with or without food

List of Contraindications

Aprepitant and Pregnancy

Category B: Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Aprepitant and Lactation

Caution when used during lactation

Aprepitant and Children

Information Not Available

Aprepitant and Geriatic

Information Not Available

Aprepitant and Other Contraindications

Information Not Available

Storage

Oral: Store at room temperature 20-25°C (68-77°F)

Lab interference

Oral: Store at room temperature 20-25°C (68-77°F)

Aprepitant brands in India:

Aprecap Aprelief Apretero Apriset Apristar Empov Emvoid

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