Emestop Capsule 125 mg

Emestop Capsule 125 mg Uses, Dosage, Side Effects, Food Interaction and all others data.

Emestop Capsule 125 mg 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. Emestop Capsule 125 mg stops substance P from binding to the NK1 receptors. By blocking the receptors, Emestop Capsule 125 mg can prevent nausea and vomiting, which often happens after chemotherapy or as a complication of surgery.

Emestop Capsule 125 mg, an antiemetic, is a substance P/neurokinin 1 (NK1) receptor antagonist which, in combination with other antiemetic agents, is indicated for the prevention of acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy. Emestop Capsule 125 mg is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Emestop Capsule 125 mg has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CI NV).

Emestop Capsule 125 mg
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Emestop Capsule 125 mg
Availability	Prescription only
Generic	Aprepitant
Aprepitant Other Names	Aprepitant, Aprépitant, Aprepitantum
Related Drugs	lorazepam, ondansetron, Zofran, dexamethasone, Ativan, metoclopramide
Weight	125 mg
Type	Capsule
Formula	C₂₃H₂₁F₇N₄O₃
Weight	Average: 534.4267 Monoisotopic: 534.150187993
Protein binding	Protein binding is reported to be >95%.
Groups	Approved, Investigational
Therapeutic Class	Anti-emetic drugs
Manufacturer	Incepta Pharmaceuticals Ltd.
Available Country	Bangladesh
Last Updated:	October 19, 2023 at 6:27 am

Uses

Emestop Capsule 125 mg is used for-

- Prevention of postoperative nausea and vomiting (PONV)

- Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)

Emestop Capsule 125 mg is also used to associated treatment for these conditions: Nausea and vomiting

How Emestop Capsule 125 mg works

Emestop Capsule 125 mg has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with Emestop Capsule 125 mg have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Emestop Capsule 125 mg augments the antiemetic activity of the 5-HT₃-receptor antagonist ondansetron and the corticosteroid ethasone and inhibits both the acute and delayed phases of cisplatin induced emesis.

Dosage

Emestop Capsule 125 mg dosage

Post Operative Nausea and Vomiting

The recommended oral dosage of Emestop Capsule 125 mg 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 Capsule 125 mg 125mg orally, Dexamethasone 12 mg orally, 5-HT3 antagonist (Ondansetron): 24 mg 30 minutes before the start of chemotherapy.

Day 2: Emestop Capsule 125 mg 80 mg orally, Dexamethasone 8 mg orally

Day 3: Emestop Capsule 125 mg 80 mg orally, Dexamethasone 8 mg orally

Day 4: Dexamethasone 8 mg orally

*Emestop Capsule 125 mg 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 Capsule 125 mg 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 Capsule 125 mg 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day

Day 3: Emestop Capsule 125 mg 80 mg orally, 5-HT3 antagonist (Ondansetron): 8 mg tablet twice a day

*Emestop Capsule 125 mg 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 Capsule 125 mg 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

Interaction

Emestop Capsule 125 mg is a substrate, a weak-to-moderate (dose dependent) inhibitor, and an inducer of CYP3A4. Emestop Capsule 125 mg is also an inducer of CYP2C9. Precautions should be taken while coadministering Emestop Capsule 125 mg 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 Emestop Capsule 125 mg, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Emestop Capsule 125 mg may be reduced. Alternative or back-up methods of contraception should be used during treatment with Emestop Capsule 125 mg and for 1 month following the last dose of Emestop Capsule 125 mg.

Food Interaction

Take with or without food. The absorption is unaffected by food.

Emestop Capsule 125 mg Drug Interaction

Unknown: charcoal, charcoal, diphenhydramine, diphenhydramine, sulfamethoxazole / trimethoprim, sulfamethoxazole / trimethoprim, prochlorperazine, prochlorperazine, meperidine, meperidine, sodium iodide, sodium iodide, pregabalin, pregabalin, acetaminophen, acetaminophen, cholecalciferol, cholecalciferol, ondansetron, ondansetron

Emestop Capsule 125 mg Disease Interaction

Moderate: liver disease

Volume of Distribution

70 L

Elimination Route

The mean absolute oral bioavailability of aprepitant is approximately 60 to 65%.

Half Life

9-13 hours

Clearance

Apparent plasma cl=62-90 mL/min

Elimination Route

Emestop Capsule 125 mg is eliminated primarily by metabolism; aprepitant is not renally excreted. Emestop Capsule 125 mg is excreted in the milk of rats. It is not known whether this drug is excreted in human milk.

Pregnancy & Breastfeeding use

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.

Contraindication

Emestop Capsule 125 mg is contraindicated in patients who are hypersensitive to any component of the product. Emestop Capsule 125 mg should not be used concurrently with Pimozide, Terfenadine, Astemizole & Cisapride.

Special Warning

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 .

Acute Overdose

No specific information is available on the treatment of overdosage with Emestop Capsule 125 mg. Single doses up to 600 mg of Emestop Capsule 125 mg were generally well tolerated in healthy subjects. Drowsiness and headache can be seen due to overdose. In the event of overdose, Emestop Capsule 125 mg should be discontinued. General supportive treatment and monitoring should be provided. Because of the antiemetic activity of Emestop Capsule 125 mg, medicine-induced emesis may not be effective. Emestop Capsule 125 mg cannot be removed by hemodialysis.

Interaction with other Medicine

Emestop Capsule 125 mg is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4. Emestop Capsule 125 mg is also an inducer of CYP2C9. Precautions should be taken while coadministering Emestop Capsule 125 mg 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 Emestop Capsule 125 mg, the efficacy of hormonal contraceptives during and for 28 days following the last dose of Emestop Capsule 125 mg may be reduced. Alternative or back-up methods of contraception should be used during treatment with Emestop Capsule 125 mg and for 1 month following the last dose of Emestop Capsule 125 mg.