인디나빌

개요Crixivan was launched in Australia, Switzerland, the UK and the US as an orally-bioavailable HIV-1 protease inhibitor. The compound can be prepared by coupling an optically active piperazine derivative with an epoxide derivative (now commercially available). The synthesis of the proteins, reverse transcriptase, integrase, structural proteins and a protease, required by the virus to complete its lifecycle, can be interupted if the protease enzyme is not capable of cleaving a proform polypeptide chain into these components. lndinavir inhibits this process and is more potent than the first approved protease inhibitor saquinavir. This effect was noted by the increase in CD4+ cells and a decrease in HIV RNA levels. Since indinavir is metabolized by the CYP3A4 isozyme, care must be taken with patients with hepatic insufficiency and to sex-related differences in the level of this enzyme. Other than nephrolithiasis (5%), indinavir is relatively safe and well tolerated.

일반 설명When administered with a high-fat diet, indinavir(Crixivan) achieves a maximum serum concentration of77% of the administered dose. The drug is 60% bound inthe plasma. It is extensively metabolized by CYP3A4, andseven metabolites have been identified. Oral bioavailabilityis good, with a tmax of 0.8±0.3 hour. The half-life ofelimination is 1.8 hour, and the elimination products aredetectable in feces and urine. Indinavir also causes dyslipidemia.The available dosage forms are capsules of 200 mg,333 mg, and 400 mg.