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APREPITANT

 APREPITANT


BRAND NAME:- APRECAP, APRESET ,APRELIFE ,EMPOV 125mg (one cap) + 80mg (2caps) kit.


APREPITANT is a medication used to manage and treat chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV). It is in the neurokinin-1 antagonist class of medications. 



PHARMACOLOGY & MECHANISM OF ACTION:- 

It is a recently introduced selective , high affinity NK1 receptors antagonist that blocks the emetic action of substance P, with little effect on 5 HT3 and D2 or other receptors. Gastrointestinal motility is not affected. Oral aprepitant (125 mg + 80 mg + 80 mg over 3 days) combined with standard i.v. ondansetron+ dexamethasone regimen significantly enhanced the antiemetic efficacy against high emetogenic cisplatin based chemotherapy. Greater additional protection was afforded against delayed vomiting than against Acute vomiting. It was particularly useful in patients undergoing multiple cycles of chemotherapy. Adjuvant benefits of aprepitant has also been demonstrated in cyclophosphamide based moderately emetogenic chemotherapy. A single 40mg oral dose of aprepitant has been found equally effective as ondansetron in PONV as well.

     APREPITANT is well absorbed orally. It penetrates blood brain barrier and is metabolized in liver, mainly by CYP3A4 metabolites are eliminated via bile in faeces and in urine; t½ is 9-13 hours ,but clearance is reduced with increase in dose . Inducers and inhibitors of CYP3A4 are likely to interact with aprepitant. Dose of dexamethasone and warfarin needs to be reduced. Aprepitant should not be given with Q-T interval prolonging drugs like cisapride.


Tolerability of aprepitant is good.


USED:- 

To prevent the nausea and vomiting that may occur during cancer treatment (chemotherapy). Aprepitant capsules are also used to prevent nausea and vomiting that may occur after surgery .



ADVERSE EFFECTS:- 

Combined regimen were similar to those produced by ondansetron+ dexamethasone with out aprepitant. Symptoms attributed to aprepitant are Weakness, fatigue, flatulence and rarely rise in liver enzymes.


DOSE :- 

FOR CINV – 125mg before chemotherapy+ 80mg each on 2nd and 3rd day ( all oral ) along with i.v. ondansetron+ dexamethasone.

For PONV – 40mg (single dose) oral before abdominal or other surgery.





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