DESCRIPTION
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.
PHARMACODYNAMIC-
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.
MECHANISM OF ACTION
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.
METABOLISM-
Aprepitant is metabolized primarily by CYP3A4 with minor metabolism by CYP1A2 and CYP2C19. Seven metabolites of aprepitant, which are only weakly active, have been identified in human plasma.
HALF LIFE - 9TO 12 HOURS
PROTEIN BINDING - + 95%
ADVERSE EFFECT-
Dizziness
Anorexia
Headache
DRUG INTERACTION-
- FOSAPREPITANT+ASTEMIZOLE = Increase the level and effect of astemizole by affecting hepatic and intestinal enzyme CYP3A4 metabolism
- FOSAPREPITANT+ CARBAMAZEPINE =Carbamazepine will decrease the level and effect the fosaprepitant by affecting hepatic and intestinal enzyme CYP3A4 metabolism.
- FOSAPREPITANT + CISAPRIDE =increase the level of fosaprepitant.
- FOSAPREPITANT + CIMETIDINE =increase the level and effect of fosaprepitant.
REFERENCE-
Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no- 670
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