Fosaprepitant

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

Fosaprepitant is an intravenously administered antiemetic drug. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment.

Fosaprepitant is a prodrug of Aprepitant. Once biologically activated, the drug acts as 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. Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant 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).

Fosaprepitant
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	Fosaprepitant
Availability	Prescription only
Generic	Fosaprepitant
Fosaprepitant Other Names	Fosaprépitant, Fosaprepitant, Fosaprepitantum
Related Drugs	lorazepam, ondansetron, Zofran, dexamethasone, Ativan, metoclopramide
Weight	150mg,
Type	Intravenous Powder For Injection, Intravenous
Formula	C₂₃H₂₂F₇N₄O₆P
Weight	Average: 614.4066 Monoisotopic: 614.116518403
Protein binding	95% +
Groups	Approved
Therapeutic Class
Manufacturer
Available Country	United States
Last Updated:	September 19, 2023 at 7:00 am

Uses

Fosaprepitant is an antiemetic drug used in combination with other antiemetic agents for the prevention of acute and delayed nausea and vomiting caused by chemotherapy.

For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy.

Fosaprepitant is also used to associated treatment for these conditions: Acute chemotherapy-induced nausea and vomiting, Delayed chemotherapy induced naused and vomiting

How Fosaprepitant works

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 NK1 receptors. Animal and human studies show that Aprepitant 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. In summary, the active form of fosaprepitant is as an NK1 antagonist which is because it blocks signals given off by NK1 receptors. This therefore decreases the likelihood of vomiting in patients experiencing.

Food Interaction

Exercise caution with grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of fosaprepitant, which may increase its serum concentration.
Exercise caution with St. John's Wort. This herb induces the CYP3A4 metabolism of fosaprepitant and may reduce its serum concentration.

Fosaprepitant Drug Interaction

Moderate: paclitaxel protein-bound, doxorubicin, dexamethasoneUnknown: pemetrexed, palonosetron, diphenhydramine, loratadine, prochlorperazine, acetaminophen / aspirin / caffeine, trastuzumab, loperamide, furosemide, metoprolol, polyethylene glycol 3350, morphine, pegfilgrastim, cyanocobalamin, pyridoxine, ascorbic acid, cholecalciferol

Fosaprepitant Disease Interaction

Moderate: QT prolongation, severe hepatic impairment

Half Life

9-13 hours

Elimination Route

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