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CINVANTI

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Overview

What is CINVANTI?

CINVANTI injectable emulsion contains the active ingredient, aprepitant. Aprepitant is a substance P/neurokinin 1 (NK1) receptor antagonist, an antiemetic agent, chemically described as 5-[[(2R,3S)-2-[(1R)-1-[3,5- bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3- one.

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

Aprepitant is a white to off-white crystalline solid, with a molecular weight of 534.43. It is practically insoluble in water. Aprepitant is sparingly soluble in ethanol and isopropyl acetate and slightly soluble in acetonitrile.

CINVANTI (aprepitant) injectable emulsion is a sterile, opaque, off-white to amber liquid in a single-dose vial for intravenous use. Each vial contains 130 mg aprepitant in 18 mL of emulsion. The emulsion also contains the following inactive ingredients: egg lecithin (2.6 g), ethanol (0.5 g), sodium oleate (0.1 g), soybean oil (1.7 g), sucrose (1 g), and water for injection (12 g).



What does CINVANTI look like?



What are the available doses of CINVANTI?

Injectable emulsion: 130 mg aprepitant in single-dose vial ()

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

Pregnancy

8.1

How should I use CINVANTI?

CINVANTI, in combination with other antiemetic agents, is indicated in adults for the prevention of:

Limitations of Use

The recommended dosages in adults of CINVANTI, dexamethasone, and a 5-HT antagonist for the prevention of nausea and vomiting associated with administration of HEC or MEC are shown in and , respectively.


What interacts with CINVANTI?

Sorry No Records found


What are the warnings of CINVANTI?

Sorry No Records found


What are the precautions of CINVANTI?

Sorry No Records found


What are the side effects of CINVANTI?

Sorry No records found


What should I look out for while using CINVANTI?

CINVANTI is contraindicated in patients:


What might happen if I take too much CINVANTI?

There is no specific information on the treatment of overdosage with aprepitant.

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

Aprepitant is not removed by hemodialysis.


How should I store and handle CINVANTI?

Store at 20° to 25°C (68° to 77°F) [See USP Controlled Room Temperature].CINVANTI injectable emulsion is supplied as an opaque, off-white to amber emulsion in a single-dose glass vial containing 130 mg/18 mL aprepitant:StorageCINVANTI injectable emulsion vials must be refrigerated, store at 2°C-8°C (36°F-46°F).CINVANTI injectable emulsion vials can remain at room temperature up to 60 days.Do not freeze.CINVANTI injectable emulsion is supplied as an opaque, off-white to amber emulsion in a single-dose glass vial containing 130 mg/18 mL aprepitant:StorageCINVANTI injectable emulsion vials must be refrigerated, store at 2°C-8°C (36°F-46°F).CINVANTI injectable emulsion vials can remain at room temperature up to 60 days.Do not freeze.CINVANTI injectable emulsion is supplied as an opaque, off-white to amber emulsion in a single-dose glass vial containing 130 mg/18 mL aprepitant:StorageCINVANTI injectable emulsion vials must be refrigerated, store at 2°C-8°C (36°F-46°F).CINVANTI injectable emulsion vials can remain at room temperature up to 60 days.Do not freeze.CINVANTI injectable emulsion is supplied as an opaque, off-white to amber emulsion in a single-dose glass vial containing 130 mg/18 mL aprepitant:StorageCINVANTI injectable emulsion vials must be refrigerated, store at 2°C-8°C (36°F-46°F).CINVANTI injectable emulsion vials can remain at room temperature up to 60 days.Do not freeze.


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Clinical Information

Chemical Structure

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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. 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
CINVANTI is contraindicated in patients:

The hypoglycemic action of sulfonylureas may be potentiated by certain drugs including nonsteroidal anti-inflammatory agents, some azoles, and other drugs that are highly protein bound, salicylates, sulfonamides, chloramphenicol, probenecid, coumarins, monoamine oxidase inhibitors, quinolones and beta adrenergic blocking agents. When such drugs are administered to a patient receiving glipizide, the patient should be observed closely for hypoglycemia. When such drugs are withdrawn from a patient receiving glipizide, the patient should be observed closely for loss of control. binding studies with human serum proteins indicate that glipizide binds differently than tolbutamide and does not interact with salicylate or dicumarol. However, caution must be exercised in extrapolating these findings to the clinical situation and in the use of glipizide with these drugs.

Certain drugs tend to produce hyperglycemia and may lead to loss of control. These drugs include the thiazides and other diuretics, corticosteroids, phenothiazines, thyroid products, estrogens, oral contraceptives, phenytoin, nicotinic acid, sympathomimetics, calcium channel blocking drugs, and isoniazid. When such drugs are administered to a patient receiving glipizide, the patient should be closely observed for loss of control. When such drugs are withdrawn from a patient receiving glipizide, the patient should be observed closely for hypoglycemia.

A potential interaction between oral miconazole and oral hypoglycemic agents leading to severe hypoglycemia has been reported. Whether this interaction also occurs with the intravenous, topical, or vaginal preparations of miconazole is not known. The effect of concomitant administration of fluconazole and glipizide has been demonstrated in a placebo-controlled crossover study in normal volunteers. All subjects received glipizide alone and following treatment with 100 mg of fluconazole as a single daily oral dose for 7 days. The mean percentage increase in the glipizide AUC after fluconazole administration was 56.9% (range: 35 to 81).

In studies assessing the effect of colesevelam on the pharmacokinetics of glipizide ER in healthy volunteers, reductions in glipizide AUC and C of 12% and 13%, respectively were observed when colesevelam was coadministered with glipizide ER. When glipizide ER was administered 4 hours prior to colesevelam, there was no significant change in glipizide AUC or C, -4% and 0%, respectively. Therefore, glipizide should be administered at least 4 hours prior to colesevelam to ensure that colesevelam does not reduce the absorption of glipizide.

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

See and 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

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Interactions

Interactions

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