Emestop Capsule
Aprepitant
40mg
Incepta Pharmaceuticals Ltd.
| Pack size | 4's Pack |
|---|---|
| Dispensing mode | |
| Source | |
| Agent | |
| Retail Price | 50.00 AED |
Available as:
Indications
Emestop Capsule is used for:
Prevent nausea and vomiting caused by certain types of cancer medicines (chemotherapy), prevent nausea and vomiting after surgery.
Adult Dose
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.
Aprepitant (fosaprepitant dimeglumine) for Injection may be substituted for oral Aprepitant (125 mg) on Day 1 only as part of the CINV regimen.
Prevention of Postoperative Nausea and Vomiting
The recommended oral dosage of Aprepitant for the postoperative nausea and vomiting (PONV) indication is 40 mg within 3 hours prior to induction of anesthesia.
Child Dose
Chemotherapy-Induced Nausea & Vomiting
Indicated 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, and for moderately emetogenic cancer chemotherapy (MEC)
Oral suspension: Aged <6 months: Safety and efficacy not established
Capsule
<12 years or weight <30 kg: Safety and efficacy not established
>12 years or <12 years and weight ?30 kg
Day 1: 125 mg PO 1 hr prior to chemotherapy plus dexamethasone 12 mg PO (30 minutes before chemotherapy) and a 5-HT3 antagonist
Days 2 and 3: 80 mg PO 1 hr prior to chemotherapy plus dexamethasone 8 mg PO qAM
Day 4: Dexamethasone 8 mg PO in AM
Oral suspension
<6 months: Safety and efficacy not established
>6 months to <12 years
Day 1: 3 mg/kg PO 1 hr prior to chemotherapy
Days 2 and 3: 2 mg/kg PO 1 hr prior to chemotherapy
Administer with concomitant dexamethasone and 5-HT3 antagonist (eg, ondansetron)
Renal Dose
Renal impairment
Severe (CrCl <30 mL/min): Decreased AUC of total aprepitant (unbound and protein bound) by 21% and Cmax decreased by 32%, compared to healthy subjects (CrCl >80 mL/min)
ESRD undergoing hemodialysis: Decreased AUC of total aprepitant by 42% and Cmax decreased by 32%
Administration
May be taken with or without food.
Contra Indications
Coadministration of astemizole, cisapride, pimozide, or terfenadine; hypersensitivity to any component of the product.
Precautions
Coadministration of aprepitant with warfarin (a CYP2C9 substrate) may result in a clinically significant decrease in the International Normalized Ratio (INR) of prothrombin time.
The efficacy of hormonal contraceptives during and for 28 days following the last dose of Aprepitant may be reduced. Alternative or backup methods of contraception should be used.
Aprepitant is a dose-dependent inhibitor of CYP3A4, and should be used with caution in patients receiving concomitant medications that are primarily metabolized through CYP3A4.
Caution should be exercised when administered in patients with severe hepatic impairment.
Pregnancy-Lactation
Pregnancy
Insufficient data on use in pregnant women to inform a drug associated risk
Avoid aprepitant IV emulsion in pregnant women due to the alcohol content
Animal studies
No adverse developmental effects observed in rats or rabbits exposed during period of organogenesis to systemic drug levels (AUC) ~1.5 times adult human exposure at 125-mg/80-mg/80-mg regimen
Contraception
Aprepitant may reduce efficacy of hormonal contraceptives
Advise females of reproductive potential using hormonal contraceptives to use an effective alternative or back-up non-hormonal contraceptive (eg, condoms or spermicides) during treatment and for 1 month following the last dose of aprepitant
Lactation
Unknown whether drug is excreted in milk
A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother
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 drugs 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 month following the last dose of Aprepitant.
Potentially Fatal: This may result in increased serum levels of astemizole, cisapride, pimozide and terfenadine which can lead to life-threatening torsade de pointes arrhythmias.
Contraindicated (8)
chloramphenicol
darunavir
flibanserin
lomitapide
lonafarnib
pimozide
ribociclib
tipranavir
Adverse Effects
Side effects of Aprepitant :
>10% (only seen in CINV)
Oral (adults)
Fatigue (13%)
Oral (pediatrics)
Neutropenia (13%)
1-10%
Oral (adults)
Diarrhea (9%)
Asthenia (7%)
Dyspepsia (7%)
Abdominal pain (6%)
Hiccups (5%)
Decreased WBCs (4%)
ALT increased (3%)
Oral (pediatrics)
Headache (9%)
Diarrhea (6%)
Decreased appetite (5%)
Cough (5%)
Fatigue (5%)
Hemoglobin decreased (5%)
Dizziness (5%)
Hiccups (4%)
Mechanism of Action
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.
Note
Emestop 40mg Capsule manufactured by Incepta Pharmaceuticals Ltd.. Its generic name is Aprepitant. Emestop is availble in Bangladesh.
Farmaco BD drug index information on Emestop Capsule is not intended for diagnosis, medical advice or treatment; neither intended to be a substitute for the exercise of professional judgment.