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Aprepitant

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Overview

What is Aprepitant?

Aprepitant Capsules, USP contain the active ingredient aprepitant, USP. Aprepitant, USP is a substance P/neurokinin 1 (NK) receptor antagonist, an antiemetic agent, chemically described as 5-[[(2,3)-2-[(1)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3-1,2,4-triazol-3-one.

Its empirical formula is CHFNO, and its structural formula is:

Aprepitant, USP is a white to off-white powder, with a molecular weight of 534.43. It is soluble in methanol and in acetone, sparingly soluble in ethanol, and practically insoluble in water.

Each capsule for oral administration contains either 40 mg, 80 mg, or 125 mg of aprepitant, USP and the following inactive ingredients: colloidal silicon dioxide, hydroxyethyl cellulose, microcrystalline cellulose, mannitol, poloxamer, povidone, sodium stearyl fumarate, vitamin E polyethylene glycol succinate, and purified water. The capsule shell excipients are gelatin, sodium lauryl sulphate and titanium dioxide. The 40-mg capsule shell also contains iron oxide yellow, and the 125-mg capsule also contains FD&C Red #3. Non-volatile solvents in the imprinting ink are shellac, iron oxide black and potassium hydroxide.

USP dissolution test pending.



What does Aprepitant look like?



What are the available doses of Aprepitant?

Aprepitant Capsules, USP: 40 mg; 80 mg; 125 mg ()

What should I talk to my health care provider before I take Aprepitant?

See Full Prescribing Information for a list of clinically significant drug interactions. (, , , , , )

Pediatric use information is approved for Merck Sharp & Dohme Corp.’s EMEND (aprepitant) capsules. However, due to Merck Sharp & Dohme Corp.’s marketing exclusivity rights, this drug product is not labeled with that information.

How should I use Aprepitant?

Aprepitant capsules, in combination with other antiemetic agents, are indicated for the prevention of:

Pediatric use information is approved for Merck Sharp & Dohme Corp.'s EMEND (aprepitant) capsules. However, due to Merck Sharp & Dohme Corp.'s marketing exclusivity rights, this drug product is not labeled with that information.

Adults

The recommended oral dosage of aprepitant capsules, dexamethasone, and a 5-HT antagonist in adults for the prevention of nausea and vomiting associated with administration of HEC or MEC is shown in Table 1 or Table 2, respectively.

*

[see Clinical Pharmacology ()]

*

[see Clinical Pharmacology ()].

Pediatric use information is approved for Merck Sharp & Dohme Corp.’s EMEND (aprepitant) capsules. However, due to Merck Sharp & Dohme Corp’s marketing exclusivity rights, this drug product is not labeled with that information.


What interacts with Aprepitant?

Sorry No Records found


What are the warnings of Aprepitant?

Sorry No Records found


What are the precautions of Aprepitant?

Sorry No Records found


What are the side effects of Aprepitant?

Sorry No records found


What should I look out for while using Aprepitant?

Aprepitant is contraindicated in patients:


What might happen if I take too much Aprepitant?

No specific information is available on the treatment of overdosage.

Drowsiness and headache were reported in one patient who ingested 1440 mg of aprepitant (approximately 11 times the maximum recommended single dose).

In the event of overdose, aprepitant should be discontinued and general supportive treatment and monitoring should be provided. Because of the antiemetic activity of aprepitant, drug-induced emesis may not be effective in cases of aprepitant overdosage.

Aprepitant is not removed by hemodialysis.


How should I store and handle Aprepitant?

SUSTIVA capsules and SUSTIVA tablets should be stored at 25°C (77°F); excursions permitted to 15°C-30°C (59°F-86°F) [see USP Controlled Room Temperature].Aprepitant Capsules, USP, 125 mg:Aprepitant Capsules, USP, 80 mg:Aprepitant Capsules, USP, 3-day pack (125-mg/80-mg/80-mg):Aprepitant Capsules, USP, 40 mg: Storage and HandlingStore at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].Aprepitant Capsules, USP, 125 mg:Aprepitant Capsules, USP, 80 mg:Aprepitant Capsules, USP, 3-day pack (125-mg/80-mg/80-mg):Aprepitant Capsules, USP, 40 mg: Storage and HandlingStore at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].Aprepitant Capsules, USP, 125 mg:Aprepitant Capsules, USP, 80 mg:Aprepitant Capsules, USP, 3-day pack (125-mg/80-mg/80-mg):Aprepitant Capsules, USP, 40 mg: Storage and HandlingStore at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].Aprepitant Capsules, USP, 125 mg:Aprepitant Capsules, USP, 80 mg:Aprepitant Capsules, USP, 3-day pack (125-mg/80-mg/80-mg):Aprepitant Capsules, USP, 40 mg: Storage and HandlingStore at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].Aprepitant Capsules, USP, 125 mg:Aprepitant Capsules, USP, 80 mg:Aprepitant Capsules, USP, 3-day pack (125-mg/80-mg/80-mg):Aprepitant Capsules, USP, 40 mg: Storage and HandlingStore at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].Aprepitant Capsules, USP, 125 mg:Aprepitant Capsules, USP, 80 mg:Aprepitant Capsules, USP, 3-day pack (125-mg/80-mg/80-mg):Aprepitant Capsules, USP, 40 mg: Storage and HandlingStore at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F) [see USP Controlled Room Temperature].


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Clinical Information

Chemical Structure

No Image found
Clinical Pharmacology

Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK) receptors. Aprepitant has little or no affinity for serotonin (5-HT), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV).

Aprepitant 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 aprepitant have shown that it crosses the blood brain barrier and occupies brain NK receptors. Animal and human studies show that aprepitant augments the antiemetic activity of the 5-HT-receptor antagonist ondansetron and the corticosteroid dexamethasone and inhibits both the acute and delayed phases of cisplatin-induced emesis.

Non-Clinical Toxicology
Aprepitant is contraindicated in patients:

Drug Interactions:

Aprepitant is a substrate, a weak-to-moderate (dose-dependent) inhibitor, and an inducer of CYP3A4.

See Table 10 and Table 11 for a listing of potentially significant drug interactions

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Reference

This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"

While we update our database periodically, we cannot guarantee it is always updated to the latest version.

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Professional

Clonazepam Description Each single-scored tablet, for oral administration, contains 0.5 mg, 1 mg, or 2 mg Clonazepam, USP, a benzodiazepine. Each tablet also contains corn starch, lactose monohydrate, magnesium stearate, microcrystalline cellulose, and povidone. Clonazepam tablets USP 0.5 mg contain Yellow D&C No. 10 Aluminum Lake. Clonazepam tablets USP 1 mg contain Yellow D&C No. 10 Aluminum Lake, as well as FD&C Blue No. 1 Aluminum Lake. Chemically, Clonazepam, USP is 5-(o-chlorophenyl)-1,3-dihydro-7-nitro-2H-1,4-benzodiazepin-2-one. It is a light yellow crystalline powder. It has the following structural formula: C15H10ClN3O3 M.W. 315.72
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Interactions

Interactions

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