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EMPOV TAB ( STRIP , 3 )

Manufactured by: Dr. Reddy’s Laboratories Ltd

. 809.00/- . 1300.00/- 37.76 % OFF You Save : . 491.00/-
Availability : In stock

DESCRIPTION

Aprepitant, an antiemetic, is 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).

CATEGORIES

Alimentary Tract and Metabolism Antiemetics and Antinauseants Cytochrome P-450 CYP1A2 Inhibitors Cytochrome P-450 CYP2C9 Inhibitors Cytochrome P-450 CYP1A2 Inducers Cytochrome P-450 CYP2C9 Inducers Cytochrome P-450 CYP2C19 Inducers CYP3A4 Inhibitors

CHEMICAL FORMULA

C23H21F7N4O3

COMPOSITION

Aprepitant (1 cap) 125 mg + Aprepitant (2 caps) 80 mg.

INDICATION

For the prevention of nausea and vomiting associated with highly emetogenic cancer chemotherapy, including high-dose cisplatin (in combination with other antiemetic agents).

PHARMACODYNAMICS

Aprepitant, an antiemetic, is 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).

MECHANISM

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.

ABSORPTION

The mean absolute oral bioavailability of aprepitant is approximately 60 to 65%.

VOLUME DISTRIBUTION

70 L

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.

ROUTE ELIMINATION

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.

HALF LIFE

9-13 hours

FOOD INTERACTIONS

Take without regard to meals.

SIDE EFFECTS

fatigue and feeling listless constipation diarrhea loss of appetite hiccups heartburn or indigestion (sour stomach) pain at injection site (IV form) itching