Human immunodeficiency virus amprenavir

TC, lamivudine ABC, abacavir APV, amprenavir AST, aspartate aminotransferase ALT, alanine aminotransferase ATV, atazanavir CBC, complete blood cell count D/C, discontinue ddl, didano-sine d4T, stavudine EFV, efavirenz FTC, emtricitabine P1BV, hepatitis B virus F1CV, hepatitis C vims HIV, human immunodeficiency virus IDV, indinavir IV, intravenous LFT, liver function tests LPV/r, lopinavir + ritonavir NNRTI, nonnucleoside reverse transcriptase inhibitor NRTI, nucleoside reverse transcriptase inhibitor NVP, nevirapine PI, protease inhibitor PT, prothrombin time T.bili, total bilirubin TDF, tenofovir disoproxiI fumarate TPV, tipranavir ULN, upper limit of normal ZDV, zidovudine. 

Pharmacology Amprenavir is an inhibitor of human immunodeficiency virus (HIV)-I protease. Amprenavir binds to the active site of HIV-1 protease and thereby prevents the processing of viral gag and gag-pol polyprotein precursors, resulting in the formation of immature noninfectious viral particles. 

Amprenavir is an inhibitor of the human immunodeficiency virus (HIV) protease. The chemical name of amprenavir is (3 S)-tetrahydro-3-furyl N-[(1 S,2 R)-3-(4-amino-N-isobu-tylbenzenesulfonamido)-1 -benzyl-2-hydroxypropyl]car-bamate. Amprenavir is a single stereoisomer with the (3... 

Furfine, E. S., Baker, C. T., Hale, M. R., Reynolds, D. J., Salisbury, J. A., Searle, A. D., Studenberg, S. D., Todd, D., Tung, R. D., and Spaltenstein, A. (2004). Preclinical pharmacology and pharmacokinetics of GW433908, a water-soluble prodrug of the human immunodeficiency virus protease inhibitor amprenavir. Antimicrob. Agents Chemother. 48 791-798. 

At the present time, there are at least 14 compounds that have been formally approved for the treatment of human immunodeficiency virus (HIV) infections. There are six nucleoside reverse transcriptase inhibitors (NRTIs) that, after their intracellular conversion to the 5 -triphosphate form, are able to interfere as competitive inhibitors of the normal substrates (dNTPs). These are zidovudine (AZT), didanosine (ddl), zalcitabine (ddC), stavudine (d4T), lamivudine (3TC), and abacavir (ABC). There are three nonnucleoside reverse transcriptase inhibitors (NNRTIs) — nevirapine, delavirdine, and efavirenz — that, as such, directly interact with the reverse transcriptase at a nonsubstrate binding, allosteric site. There are five HIV protease inhibitors (Pis saquinavir, ritonavir, indinavir, nelfinavir, and amprenavir) that block the cleavage of precursor to mature HIV proteins, thus impairing the infectivity of the virus particles produced in the presence of these inhibitors. 

Veronese L, Rautaureau J, Sadler BM, et al. (2000) Single-dose pharmacokinetics of amprenavir, a human immunodeficiency virus type 1 protease inhibitor, in subjects with normal or impaired hepatic function. Antimicrob Agents Chemother 44 821-826. 

Sadler BM, Hanson CD, Chittick GE, Symonds WT, Roskell NS. Safety and pharmacokinetics of amprenavir (141W94), a human immunodeficiency virus (HIV) type 1 protease inhibitor, following oral administration of single doses to HIV-infected adults. Antimicrob Agents Chemother 1999 43(7) 1686-92. 

Sadler BM, Gillotin C, Lou Y, Eron JJ, Lang W, Haubrich R, Stein DS. Pharmacokinetic study of human immunodeficiency virus protease inhibitors used in combination with amprenavir. Antimicrob Agents Chemother 2001 45(12) 3663-8. 

B. M. Sadler, C. Gillotin, Y. Lou, and D. S. Stein, In vivo effect of alpha-l-acid glycoprotein on pharmacokinetics of amprenavir, a human immunodeficiency virus protease inhibitor. Antimicrob Agents Chemother 45 852-856 (2001). 

Duval X, Le Moing V, Longuet P, Leport C, Vilde J L, Lamotte C, Peytavin G, Farinotti R. Efavirenz-induced decrease in plasma amprenavir levels in human immunodeficiency virus-infected patients and correction hy ritonavir. Antimicrob Agents Cbemotber (2000) 44, 2593. 

Falloon J, Piscitelli S, Vogel S, Sadler B, Mitsuya H, KavUck MF, Yoshimura K, Rogers M, LaFon S, Manion DJ, Lane HC, Masur H. Comhination therapy with amprenavir, abacavir, and efavirenz in human immunodeficiency virus (HIV) infected patients failing a protease-inhibitor regimen pharmacokinetic drug interactions and antiviral activity. Clin bfect Dis (2000) 30, 313-18. 

Duval X, Lamotte C, Race E, Descamps D, Damond F, Clavel F, Leport C, Pe3rtavin G, Vilde J-L. Amprenavir inhibitory quotient and virolc ical response in human immunodeficiency virus-infected patients on an amprenavir-containing salvage regimen without or with ritonavir. Antimicrcb Agents Chemo ier (2002) 46,570-4. 

Goujard C, Vincent I, Meynard J-L, ChoudetN, Bollens D, Rousseau C, Demarles D, Gillotin C, Bidault R, Taburet A-M, Steady-state pharmacokinetics of amprenavir coadministered with ritonavir in human immunodeficiency virus type 1 -infected patients. Antimicrob Agents Chemother (2003) 47,118-23,... 

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