Aprepitant

Drug #2233

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.

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Primary Characteristics

Molecular Weight: 534.43 · Solubility in Water: insoluble · Solubility in Alcohol: sparingly soluble in ethanol and isopropyl acetate and slightly soluble in acetonitrile · Non-proprietary name: Aprepitant.

Pharmacokinetics

Absorption: Aprepitant has an oral bioavailability is 62.5% (±2.5%).

Distribution: Aprepitant has a volume of distribution is 70 L at steady state. plasma protein binding is greater than 95%.

Elimination: it is metabolised via CYP3A4 with minor metabolism by CYP1A2 and CYP2C19, plasma half-life is 9 to 13 hours.

Indications

Aprepitant is primarily indicated in conditions like Nausea and vomiting (chemotherapy induced), Post operative vomiting.

Contraindications

Aprepitant is contraindicated in conditions like Hypersensitivity to any component of product.

Dosage

Aprepitant's dosage details are as follows:

Dose	Single Dose	Frequency	Route	Instructions
Adult Dosage
80 – 125 mg	—	—	PO	Aprepitant is given for 3 days as part of a regimen that includes a corticosteroid and a 5-HT3 antagonis for moderate to highly emetogenic cancer chemotherapy:. 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. It may be taken with or with out food.
40 mg	40 mg	—	PO	For prevention of postoperative nausea and vomiting (PONV): The recommended oral dosage of aprepitant is 40 mg within 3 hours prior to induction of anesthesia.
Paediatric Dosage (20kg)
No data.
Neonatal Dosage (3kg)
No data.

Drug Interactions

7 interactions

Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.

Side Effects

The signs and symptoms that are produced after acute overdosage of Aprepitant are Drowsiness, Headache.

Aprepitant is known to cause more or less tolerable side effects which are usually transient. These include Constipation , Diarrhea, Heart burn, Hiccups, Nausea, Pain at injection site, Stomach pain, Vomiting .

Warnings / Precautions

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.

Available Brands

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Single Ingredient

Caps

125 mg 40 mg 80 mg

Storage Conditions

Aprepitant should be stored Caps.

Drug Classification

1.17.2 — Antiemetics & antinauseants

Manufacturers

Manufacturers of Aprepitant in Pakistan:

Ferozson