Emestop(Aprepitant)
Therapeutic Group: Anti Emetic
Presentation
Emestop Capsule: Each capsule contains Aprepitant INN 40 mg.
Emestop 80 Capsule: Each capsule contains Aprepitant INN 80 mg.
Emestop 125 Capsule: Each capsule contains Aprepitant INN 125 mg.
Description
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.
Indications
Emestop is indicated for-
– Prevention of postoperative nausea and vomiting (PONV)
– Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)
Dosage & Administration
Post Operative Nausea and Vomiting
The recommended oral dosage of Emestop is 40 mg within 3 hours prior to induction of anesthesia.
Chemotherapy Induced Nausea and Vomiting
The following regimen should be used for the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy:
Day 1: Emestop 125mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): 24 mg 30 minutes before the start of chemotherapy.
Day 2: Emestop 80 mg orally, Dexamethasone 8 mg orally
Day 3: Emestop 80 mg orally, Dexamethasone 8 mg orally
Day 4: Dexamethasone 8 mg orally
*Emestop is administered orally 1 hour prior to chemotherapy treatment on Day 1 and in the morning on Days 2 and 3. **Dexamethasone is administered 30 minutes prior to chemotherapy treatment on Day 1 and in the morning on Days 2 through 4. The dose of dexamethasone accounts for drug interactions.
The following regimen should be used for the prevention of nausea and vomiting associated with moderately emetogenic cancer chemotherapy:
Day 1: Emestop 125mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): one 8 mg tablet 30 minutes before chemotherapy followed by an 8 mg dose 8 hours later.
Day 2: Emestop 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day
Day 3: Emestop 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day
*Emestop is administered orally 1 hour prior to chemotherapy treatment on Day 1 and in the morning on Days 2 and 3. **Dexamethasone is administered 30 minutes prior to chemotherapy treatment on Day 1. The dose of dexamethasone accounts for drug interactions.
Emestop may be taken with or without food. No dosage adjustment is necessary for the elderly patients.
Patients with Renal Impairment- No dosage adjustment is necessary for patients with renal impairment or for patients with end stage renal disease (ESRD) undergoing hemodialysis.
Patients with Hepatic Impairment-No dosage adjustment is necessary for patients with mild to moderate hepatic impairment. There are no clinical data in patients with severe hepatic impairment .
Side Effects
Constipation,Hypotension, Pruritus,Pyrexia
Precautions
N/A
Use in Pregnancy & Lactation
Pregnancy Category B: This drug should be used during pregnancy only if clearly needed.
It is not known whether this drug is excreted in human milk. A decision should be made whether to discontinue nursing or to discontinue the drug based on patient’s importance.
Drug Interaction
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.
Over Dose
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.
Commercial Pack
Emestop capsule: Each box contains 1 alu-alu blister strip of 4 capsules.
Emestop 80 capsule: Each box contains 1 alu-alu blister strip of 4 capsules.
Emestop 125 capsule: Each box contains 1 alu-alu blister strip of 4 capsules.
