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.


Adult Dose
Dose: 80 to 125 mg
Single Dose: 100 (102.5)
Frequency: As recommended.
Route: PO
Instructions: 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._x000D_It may be taken with or with out food.
Neonatal
Paedriatic
Characteristics
. The Molecular Weight of Aprepitant is 534.43.
Contraindications
Aprepitant is contraindicated in conditions like Hypersensitivity to any component of product.
Effects
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.
Indications
Aprepitant is primarily indicated in conditions like Nausea and vomiting (chemotherapy induced), Post operative vomiting.
Interactions
Aprepitant is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementDexamethasoneIncreased the AUC of dexamethasone, a CYP3A4 substrate, by 2.2-fold on Days 1 and 5 of chemotherpy when given in regimen. The oral dexamethasone doses should be reduced by approximately 50% when coadministered with aprepitant capsules)(125 mg/80 mg regimen), to achieve exposures of dexamethasone similar to those obtained when it is given without aprepitant capsules. A single dose of aprepitant capsules (40 mg) when coadministered with a single oral dose of dexamethasone 20 mg, increased the AUC of dexamethasone by 1.45-fold. Therefore, no dose adjustment is recommended.EthinyloestradiolUpon coadministration with aprepitant capsules, the efficacy of hormonal contraceptives during and for 28 days following the last dose of aprepitant capsules may be reduced. Alternative or back-up methods of contraception should be used during treatment with aprepitant capsules and for 1 month following the last dose of aprepitant.KetoconazoleIncrease the AUC and the mean terminal half-life of aprepitant. Concomitant administration of aprepitant capsules with strong CYP3A4 inhibitors should be approached cautiously.PimozideInhibition of CYP3A4 by aprepitant could result in elevated plasma concentrations of this drugs, potentially causing serious or life-threatening reactions. It should not be used concurrently with pimozide, terfenadine, astemizole, or cisapride.VORICONAZOLEmay increase the serum concentration of aprepitant by decreasing its metabolism.discounted or dose changedWarfarin (Na)Decrease in S(-) warfarin (a CYP2C9 substrate) trough concentration accompanied by a 14% decrease in the prothrombin time.In patients on chronic warfarin therapy, the prothrombin time (INR) should be closely monitored in the 2-week period, particularly at 7 to 10 days, following initiation of the 3-day regimen of aprepitant capsules with each chemotherapy cycle, or following administration of a single 40 mg dose of aprepitant capsules for the prevention of postoperative nausea and vomiting. These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Risks
Drug should not be given to Paediatrics, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Caps Store Between 20°C-25°C.
Warnings
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.
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