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).

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
Fosaprepitant
Fosaprepitant

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 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.

Innovators Monograph

You find simplified version here Fosaprepitant

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