Lopinavir Indinavir

Zidovudine Didanosine Stavudine Lamivudine Abacavir Tenofovir Emtricitabine Nevirapine Efavirenz TMC125 Saquinavir Indinavir Lopinavir Fosamprenavir Atazanavir Tipranavir Darunavir Raltegravir Elvitegravir Enluvirtide Maraviroc Vicriviroc Bevirimat... 

Protease inhibitors (amprenavir, atazanavir, indinavir, lopinavir, nelfinavir, ritonavir, saquinavir) Rifampin... 

Azalides azithromycin Azoles fluconazole, itraconazole, ketoconazole, and voriconazole Macrolides erythromycin, clarithromycin Protease inhibitors amprenavir, indinavir, lopinavir/ritonavir, nelfinavir, ritonavir, and saquinavir Quinolones ciprofloxacin, gatifloxacin, levofloxacin, moxifloxacin. 

Cross-resistance Cross-resistance among Pis has been observed. Tipranavir had less than 4-fold decreased susceptibility against 90% (94 of 105) of HIV-1 isolates resistant to amprenavir, atazanavir, indinavir, lopinavir, nelfinavir, ritonavir, or saquinavir. Tipranavir-resistant viruses that emerged in vitro had decreased susceptibility to the Pis amprenavir, atazanavir, indinavir, lopinavir, nelfinavir, and ritonavir but remained sensitive to saquinavir. 

Ritonavir Amprenavir Indinavir Lopinavir Nelfinavir Saquinavir ... 

Fosamprenavir Abacavir, atazanavir, delavirdine, etravirine, indinavir, lopinavir, ritonavir, tipranavir, zidovudine Didanosine, efavirenz, nevirapine, saquinavir... 

Nevirapine is a moderate inducer of CYP3A metabolism, resulting in decreased levels of amprenavir, indinavir, lopinavir, saquinavir, efavirenz, and methadone (Table 49-4). Drugs that induce the CYP3A system, such as tipranavir, rifampin, rifabutin, and St. John s wort, can decrease levels of nevirapine, whereas those that inhibit CYP3A activity, such as fluconazole, ketoconazole, and clarithromycin, can increase nevirapine levels. 

Amprenavir, indinavir, lopinavir, nelflnavir, ritonavir and saquinavir... 

Preferred Pl-based regimens are lopinavir/ritonavir plus lamivudine or emtricitabine plus another NRTI, usually zidovudine, stavudine or abacavir. Alternative combinations include other Pis with or without ritonavir, and two NRTIs. The combination of a protease inhibitor with ritonavir provides inhibition of cytochrome p450 enzymes and permits less frequent dosing of amprenavir, indinavir, lopinavir and saquinavir. Use of ritonavir in this setting is also known as boosting. ... 

This class of agents affects a later part of the HIV cycle, by inhibiting the protease enzyme and leading to impaired assembly of mature HIV virions. Examples include amprenavir, atazanavir, darunavir, fosampre-navir indinavir, lopinavir, nelfinavir, ritonavir, and saquinavir. There have been no published reports of AKI or other direct kidney toxicity due to amprenavir, darunavir, fosamprenavir, and lopinavir. 

L. Dickinson, L. Robinson, J. Tjia, S. Khoo, D. Back, Simultaneous determination of HIV protease inhibitors amprenavir, atazanavir, indinavir, lopinavir, nelfinavir, ritonavir and saquinavir in human plasma by LC—AdS dS, J. Chromatogr. B, 829... 

Drugs in this dass, which inhibit HIV protease leading to impaired maturation of noninfectious HIV virions, indude amprenavir, indinavir, lopinavir, nelfi-navir, ritonavir, and saquinavir. There are no published reports of ARF or other direct renal toxidty due to amprenavir, nelfinavir, and lopinavir. 

In the following example the authors studied the thermodynamics of several HIV-protease inhibitors (Amperavir, Indinavir, Lopinavir, Nelfinavir, Ritonavir, Saquinavir) interacting with the immobiUzed protein [Ilj. In Fig. 5... 

In this example, investigative studies were conducted to address an issue of unconjugated hyperbilirubinemia in human subjects observed after administration of HIV protease inhibitors indinavir and atazanavir. The proposed hypothesis for hyperbilirubinemia was inhibition of glucuronidation of bilirubin by these two drugs, a key step in the excretion of bilirubin into bile. To test this hypothesis, a panel of HIV protease inhibitors, including atazanavir, indinavir, lopinavir, nelfinavir, ritonavir, and saquinavir, were... 

Amprenavir, Atazanavir, Darunavir, Fosamprenavir, Indinavir, Lopinavir, Nelfinavir, Ritonavir, Saquinavir, Tipranavir... 

Rifabutin bioavailability is increased by amprenavir, atazanavir, fosamprenavir/ritonavir, indinavir, lopinavir/ritonavir, nelfinavir, tipranavir/ritonavir, and especially ritonavir, with an increased risk of toxicity. Rifabutin modestiy decreases the bioavailability of indinavir, neifinavir, and particuiarly saquinavir (with an increased risk of therapeutic faiiure), but has no effect on amprenavir, atazanavir, and ritonavir-boosted fosamprenavir. The combination of rifabutin with protease inhibitors may be used, but dosage adjustments of rifabutin or both drugs are often necessary. 

Combination of 16 ARVs seven HIV protease inhibitors (amprenavir, atazanavir, indinavir, lopinavir, nelfmavir, ritonavir, and saquinavir), seven nucleoside reverse transcriptase inhibitors (abacavir, didanosine, emtricitabine, lamivudine, stavudine, zalcitabine, and zidovudine), and two nonnucleoside reverse transcriptase inhibitors (efavirenz and nevirapine)... 

Faux, J. Venisse, N. Le Motil, G. Dupuis, A. Bouquet, S. Simultaneous determination of six HIV protease inhibitors, one metabolite, and two non-nucleoside reverse transcriptase inhibitors in human plasma by isocratic reversed-phase liquid chromatography after solid-phase extraction, Chromatographia 2003, 58, 421-426. [amprenavir indinavir lopinavir nelflnavir ritonavir saquinavir efavirenz nevirapine prazepsun]... 

Keil, K. Frerichs, V.A. DiPrancesco, R. Morse, G. Reverse phase high-performance liquid chromatography method for the analysis of amprenavir, efavirenz, indinavir, lopinavir, nelflnavir and its active metabolite (M8), ritonavir, and saquinavir in heparinized human plasma, Ther.Drug Monit., 2003, 25, 340-346. 

Poirier, J.M. Robidou, P. JaiUon, P. Simultaneous determination of the six HIV protease inhibitors (amprenavir, indinavir, lopinavir, nelfinavir, ritonavir, and saquinavir) plus M8 nelfinavir metabolite and the nonnucleoside reverse trsinscription inhibitor efavirenz in hmnan plasma by solid-phase extraction and column liquid chromatography, Ther.Drug Monit., 2002,24, 302-309. 

Rentsch, K.M. Sensitive and specific determination of eight smtiretroviral agents in plasma by high-performance liquid chromatography-mass spectrometry, J.Chromatogr.B, 2003, 788, 339-350. [SPE amprenavir efavirenz indinavir lopinavir nelfinavir nevirapine ritonavir saquinavir]... 

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