Apretero

Apretero Uses, Dosage, Side Effects, Food Interaction and all others data.

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

Apretero, 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. Apretero is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Apretero 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).

Trade Name Apretero
Availability Prescription only
Generic Aprepitant
Aprepitant Other Names Aprepitant, Aprépitant, Aprepitantum
Related Drugs lorazepam, ondansetron, Zofran, dexamethasone, Ativan, metoclopramide
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 Hetero Healthcare Limited
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Apretero
Apretero

Uses

Apretero is used for-

- Prevention of postoperative nausea and vomiting (PONV)

- Prevention of Chemotherapy Induced Nausea and Vomiting (CINV)

Apretero is also used to associated treatment for these conditions: Nausea and vomiting

How Apretero works

Apretero 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 Apretero have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies show that Apretero 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

Apretero dosage

Post Operative Nausea and Vomiting

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

Day 2: Apretero 80 mg orally, Dexamethasone 8 mg orally

Day 3: Apretero 80 mg orally, Dexamethasone 8 mg orally

Day 4: Dexamethasone 8 mg orally

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

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

*Apretero 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.

Apretero 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

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

Food Interaction

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

Apretero 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

Apretero is eliminated primarily by metabolism; aprepitant is not renally excreted. Apretero 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

Apretero is contraindicated in patients who are hypersensitive to any component of the product. Apretero 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 Apretero. Single doses up to 600 mg of Apretero were generally well tolerated in healthy subjects. Drowsiness and headache can be seen due to overdose. In the event of overdose, Apretero should be discontinued. General supportive treatment and monitoring should be provided. Because of the antiemetic activity of Apretero, medicine-induced emesis may not be effective. Apretero cannot be removed by hemodialysis.

Interaction with other Medicine

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

Innovators Monograph

You find simplified version here Apretero

Apretero contains Aprepitant see full prescribing information from innovator Apretero Monograph, Apretero MSDS, Apretero FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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