Skip to main content

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.





Comments

Popular posts from this blog

Chlorthalidone Uses, Side Effects, and More....

 Chlorthalidone  Brand name:- Hythalton 50,100mg , Hydrazide, Thalizide ( 12.5, 25) . Chlorthalidone is a diuretic which lowers blood pressure by removing extra water and certain electrolytes from the body. Over time it also relaxes blood vessels and improves blood flow. Pharmacodynamic:- Not 🚫 available.  Pharmacokinetics:- Chlortalidone is slowly absorbed from the gastrointestinal tract after oral ingestion. It has a long half-life and therefore a prolonged diuretic action, which results in continued diuretic effects despite a skipped dose. This prolonged action of chlortalidone despite missing doses may account for the higher efficacy of chlortalidone compared to the shorter half-life medication, hydrochlorothiazide. Chlortalidone is eliminated from the body mostly by the kidney, as unchanged drug. Thus, in persons with diminished kidney function, the clearance of chlortalidone is reduced and the elimination half-life is increased. As with other thiazide diuretics, ch...

Chlordiazepoxide Uses, Side Effects, and More

 Chlordiazepoxide Brand name:- Librium 10, 25 mg tabs; Equilibrium 10mg tab. Chlordiazepoxide is a benzodiazepine. It works by increasing the action of a chemical messenger (GABA) which suppresses the abnormal and excessive activity of the nerve cells in the brain. Pharmacodynamic:-  Chlordiazepoxide has antianxiety, sedative, appetite-stimulating and weak analgesic actions. The drug seems to block EEG arousal from stimulation in the brain stem reticular formation. The drug has been studied extensively in many species of animals and these studies are suggestive of action on the limbic system of the brain, which recent evidence indicates is involved in emotional responses. Hostile monkeys were made tame by oral drug doses which did not cause sedation. Chlordiazepoxide revealed a "taming" action with the elimination of fear and aggression. The taming effect of chlordiazepoxide was further demonstrated in rats made vicious by lesions in the septal area of the brain. The drug dos...

Know details about Dabigatran etexilate drug ?

 Dabigatran Etexilate