Emestop
Generic Name
Aprepitant
Manufacturer
Square Pharmaceuticals Ltd.
Country
Bangladesh
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Price Details
Current market pricing information
| Variant | Unit Price | Strip Price |
|---|---|---|
| emestop 125 mg capsule | ৳ 150.00 | ৳ 600.00 |
Description
Overview of the medicine
Emestop 125 mg capsule, containing Aprepitant, is an antiemetic used to prevent nausea and vomiting associated with cancer chemotherapy.
Uses & Indications
Dosage
Adults
Highly Emetogenic Chemotherapy: 125 mg orally 1 hour before chemotherapy on Day 1, then 80 mg once daily on Days 2 and 3. Moderately Emetogenic Chemotherapy: 125 mg orally 1 hour before chemotherapy on Day 1, then 80 mg once daily on Days 2 and 3 (typically in combination with a corticosteroid and a 5-HT3 antagonist).
Elderly
No specific dosage adjustment is required for elderly patients.
Renal_impairment
No dosage adjustment is needed for patients with renal impairment (including end-stage renal disease on hemodialysis).
How to Take
Take the capsule orally with or without food. Swallow whole, do not open or crush.
Mechanism of Action
Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. It blocks the binding of substance P to the NK1 receptor, preventing chemotherapy-induced nausea and vomiting.
Pharmacokinetics
Onset
Peak plasma levels are achieved approximately 4 hours after oral administration.
Excretion
Excreted primarily in the feces (86%) and to a lesser extent in the urine (5%).
Half life
The mean plasma half-life is approximately 9-13 hours.
Absorption
Well absorbed orally, with an absolute bioavailability of approximately 60-65%. Peak plasma concentration is reached in approximately 4 hours.
Metabolism
Primarily metabolized by the liver, mainly through the cytochrome P450 3A4 (CYP3A4) isoenzyme. It is a moderate CYP3A4 inhibitor and a weak CYP2C9 inducer.
Side Effects
Contraindications
- Hypersensitivity to Aprepitant or any component of the formulation.
- Concomitant use with Pimozide, Terfenadine, Astemizole, or Cisapride due to the risk of increased plasma concentrations of these drugs, which are CYP3A4 substrates, potentially leading to serious and/or life-threatening reactions.
Drug Interactions
Warfarin
Aprepitant may decrease INR; monitor INR closely for 2 weeks after each chemotherapy cycle and Aprepitant initiation.
Oral Contraceptives
May decrease efficacy; use alternative or backup birth control methods for 28 days after the last dose of Aprepitant.
Corticosteroids (e.g., Dexamethasone)
May increase plasma concentrations of Dexamethasone; reduce Dexamethasone dose by approximately 50% when co-administered with Aprepitant.
Pimozide, Terfenadine, Astemizole, Cisapride
Contraindicated due to potential for serious and/or life-threatening reactions including QT prolongation.
CYP3A4 Substrates (e.g., Alfentanil, Fentanyl, Quinidine)
May increase plasma concentrations of these drugs; monitor closely.
Storage
Store below 30°C in a dry place, away from direct light and moisture. Keep out of reach of children.
Overdose
Limited experience with Aprepitant overdose. In case of overdose, discontinue the drug and institute general supportive measures. Due to the antiemetic activity of Aprepitant, drug-induced emesis may not be effective. Hemodialysis is unlikely to be effective in the treatment of overdose because of high plasma protein binding.
Pregnancy & Lactation
Pregnancy Category B. Studies in animals have not shown harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed. It is not known whether Aprepitant is excreted in human breast milk; therefore, caution should be exercised when administered to a nursing woman.
Side Effects
Contraindications
- Hypersensitivity to Aprepitant or any component of the formulation.
- Concomitant use with Pimozide, Terfenadine, Astemizole, or Cisapride due to the risk of increased plasma concentrations of these drugs, which are CYP3A4 substrates, potentially leading to serious and/or life-threatening reactions.
Drug Interactions
Warfarin
Aprepitant may decrease INR; monitor INR closely for 2 weeks after each chemotherapy cycle and Aprepitant initiation.
Oral Contraceptives
May decrease efficacy; use alternative or backup birth control methods for 28 days after the last dose of Aprepitant.
Corticosteroids (e.g., Dexamethasone)
May increase plasma concentrations of Dexamethasone; reduce Dexamethasone dose by approximately 50% when co-administered with Aprepitant.
Pimozide, Terfenadine, Astemizole, Cisapride
Contraindicated due to potential for serious and/or life-threatening reactions including QT prolongation.
CYP3A4 Substrates (e.g., Alfentanil, Fentanyl, Quinidine)
May increase plasma concentrations of these drugs; monitor closely.
Storage
Store below 30°C in a dry place, away from direct light and moisture. Keep out of reach of children.
Overdose
Limited experience with Aprepitant overdose. In case of overdose, discontinue the drug and institute general supportive measures. Due to the antiemetic activity of Aprepitant, drug-induced emesis may not be effective. Hemodialysis is unlikely to be effective in the treatment of overdose because of high plasma protein binding.
Pregnancy & Lactation
Pregnancy Category B. Studies in animals have not shown harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed. It is not known whether Aprepitant is excreted in human breast milk; therefore, caution should be exercised when administered to a nursing woman.
Frequently Asked Questions
Common questions about this medicine
Pack Sizes
Shelf Life
24 to 36 months from the date of manufacture, depending on manufacturer specifications.
Availability
Pharmacies, hospitals
Approval Status
Approved by relevant authorities (e.g., FDA, DGDA)
Patent Status
Patent expired, generics available
Clinical Trials
Aprepitant has been extensively studied in various Phase 2 and Phase 3 clinical trials demonstrating its efficacy and safety in preventing chemotherapy-induced nausea and vomiting (CINV) when used in combination with other antiemetics.
Lab Monitoring
- Monitor INR closely for 2 weeks after each chemotherapy cycle and Aprepitant initiation in patients receiving warfarin.
- Liver function tests may be considered if clinically indicated.
Doctor Notes
- Emestop (Aprepitant) is a valuable addition to antiemetic regimens for CINV. It should be used in combination with a 5-HT3 receptor antagonist and a corticosteroid for optimal efficacy in HEC and MEC.
- Careful monitoring for drug interactions is essential, particularly with CYP3A4 substrates like warfarin, oral contraceptives, and certain corticosteroids, requiring dose adjustments or alternative contraception.
Patient Guidelines
- Take Emestop 125 mg capsule exactly as prescribed by your doctor, usually for 3 days starting with chemotherapy.
- Do not discontinue the medication without consulting your healthcare provider.
- Report any unusual or severe side effects to your doctor immediately.
- If you are taking oral contraceptives, use an alternative or backup method of birth control for 28 days after your last dose.
Missed Dose Advice
If a dose is missed on Day 2 or 3, it should be taken as soon as possible after realizing the missed dose. Do not take a double dose to make up for a missed dose. Consult your doctor if uncertain.
Driving Precautions
Emestop may cause dizziness, fatigue, or somnolence. If you experience these effects, avoid driving or operating machinery.
Lifestyle Advice
- Maintain adequate hydration by drinking plenty of fluids, especially during chemotherapy. Follow any dietary recommendations from your healthcare team.
- Avoid alcohol and other substances that may worsen nausea or interact with your chemotherapy regimen.
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