Stavudine Saquinavir

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

Atazanavir or fosamprenavir or nelfinavir or saquinavir/ ritonavir, and zidovudine or stavudine or tenofovir or abacavir or didanosine, and lamivudine or emtricitabine... 

APV, amprenavir ATV, atazanavir CNS, central nervous system CVD, cardiovascular disease D/C, discontinue ddC, zalcitabine ddl, didanosine DEXA, dual-energy x-ray absorptiometry d4T, stavudine EFV, efavirenz HDL, high-density lipoprotein HIV, human immunodeficiency virus HTN, hypertension IDV, indinavir LDL, low-density lipoprotein LPV/r, lopinavir+ ritonavir MRI, magnetic resonance imaging NNRTI, nonnucleoside reverse transcriptase inhibitor NRTI, nucleoside reverse transcriptase inhibitor NVP, nevirapine PI, protease inhibitor RTV, ritonavir SQV, saquinavir TDF, tenofovir disoproxil fumarate TG, triglyceride TPV/r, tipranivir + ritonavir ZDV, zidovudine. 

Peptidases encoded by many viruses play essential roles at various stages of viral replication, including the coordinated assembly and maturation of virons [7a]. Viral peptidases have become important drug targets in the treatment of viral infections. Of note are inhibitors of proteases of the human immunodeficiency virus (HIV), particularly HIV-1 protease (HIV-1 retropepsin, EC 3.4.23.16) and HIV-2 protease [47-50], Drugs in this class, which include indinavir, ritonavir, and saquinavir, are useful in the treatment of AIDS, especially when administered as a cocktail together with one of the drugs that act on the viral retrotranscriptase (e.g., didanosine, stavudine, and zidovudine (AZT)). 

TC Lamivudine ABC Abacavir d4T Stavudine ddC Zalcitabine ddl Didanosine TDF Tenofovir ZDV Zidovudine, also abbreviated as AZT FTC Emtricitabine NVP Nevirapine DLV Delavirdine EFV Efavirenz RTV, r Ritonavir Pl/r Ritonavir boosted protease inhibitor SQV Saquinavir IDV Indinavir LPV Lopinavir NEV Nelfinavir APV Amprenavir ATV Atazanavir DRV Darunavir... 

A 36-year-old HIV-infected woman who had been receiving stavudine, saquinavir, ritonavir, and didanosine developed lactic acidosis (serum lactate 11.4 mmol/1) and hepatomegaly. She had acute pancreatitis and, despite ventilatory support for respiratory failure, died after 8 weeks. 

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. 

Zidovudine/lamivudine plus either Ritonavir 600 mg twice daily Didanosine/stavudine Saquinavir soft gel 1,200 mg three times daily... 

A 49-year-old HIV-positive Caucasian man had taken ritonavir (400 mg bd), saquinavir (400 mg bd), and stavudine (40 mg bd) for 4 months. His CD4 cell count was 617 x 106 cells/1 and HIV-1 RNA less than 400 copies/ml. He had previously taken zidovudine for 7 months. He self-injected twice with metamfetamine and sniffed amyl nitrite and was found dead a few hours later. At autopsy, there was no obvious cause of death. Metamfetamine was detected in the bile (0.5 mg/1) and cannabinoids and traces of benzodiazepines were detected in the blood. 

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. ... 

A 42-year-old HIV-positive man with a prior history of Pneumocystis jiroveci pneumonia who had been treated with zidovudine and dideoxycytidine started to take saquinavir 600 mg tds. His CD4 cell count rose from 28 X 10 /1 to 101 X 10 /1 and zidovudine and dideoxycytidine were replaced by stavudine and lamivudine, because of mild peripheral neuropathy. Saquinavir was continued unchanged. A few months later he developed left-sided loin pain and hematuria and a left renal calculus was seen on ultrasound. A month later the same signs and symptoms recurred and a few weeks later he passed a small black stone in the urine. Ultrasonic lithotripsy was performed, with a good result. Saquinavir was discontinued, after which he had no further renal problems. 

Eruptive angiolipomata occurred in a 49-year-old woman after she had taken stavudine 30 mg bd, lamivudine 150 mg bd, and saquinavir 600 mg 8-hourly for 3 months (11). This has also been reported with other protease inhibitors (12,13) and the mechanism is not known. In one case lipomata regressed after the introduction of indinavir (14). 

Gynecomastia has been reported in a series of men taking saquinavir (5). In these cases the association was clear (particularly since there was positive dechallenge), but this is a rare effect and has not previously been reported with either this or other protease inhibitors, although it has been associated with the nucleoside analogue reverse transcriptase inhibitor stavudine. 

Successful treatment of human immunodeficiency virus (HIV-1) infection has been achieved through successful implementation of highly active antiretroviral therapy, frequently referred to as HAART. This involves simultaneous administration of both nucleoside and nonnucleoside reverse transcriptase inhibitors and one or more protease inliibitors. The common nucleoside reverse transcriptase inhibitors are the thymidine analogs didanosine (ddl), lamivudine (3TC), and zalcitabine (ddC) and the non-thymidine analogs abacavir (Ziazen), stavudine (d4T), and zidovudine (AZT). The nonnucleoside reverse transcriptase inhibitors include delavirdine, efavirenz, and nevirapine. The protease inhibitors include indinavir, nelfinavir, ritonavir, and saquinavir. Response to therapy is monitored by quantification of HIV-RNA copies (viral load) and CD-4+ T-lymphocyte count. Successful therapy is indicated when viral load is reduced to <50 copies/mL and CD-4+ count >500 per mL. 

Nelfinavir plus lamivudine (or emtricitabine) plus zidovudine (or stavudine) Saquinavir-ritonavir plus lamivudine (or emtricitabine) plus zidovudine (or stavudine)... 

ABBREVIATIONS EFV, efavirenz 3TC, lamivudine AZT, zidovudine TDF, tenofovir disoproxil fumarate d4T, stavudine LPV/r, lopinavir/ritonavir coformulation FTC, emtricitabine NVP, nevirapine ddl, didanosine ATV, atazanavir fosAPV, fosamprenavir RTV, ritonavir IDV, indinavir NFV, nelfinavir SQV, saquinavir. 

An HIV-positive patient taking methadone 90 mg daily with indinavir, lamivudine and zidovudine, developed withdravral symptoms and was hospitalised within a week of stopping these HIV drugs and starting ritonavir 400 mg, saquinavir 400 mg and stavudine 40 mg twice daily. The patient was eventually re-stabilised taking methadone 130 mg daily. ... 

Saquinavir. A 73-year-old man who was HIV-positive and who had been taking warfarin, co-trimoxazole, nizatidine, stavudine and lamivudine for 7 months started taking saquinavir 600 mg three times daily. His ESTR, which had been stable at around 2 for five months, rose to about 2.5 after... 

A case of valproate-associated hepatotoxicity occurred in a 51-year-old man about 3 weeks after he started nevirapine 200 mg twice daily, saquinavir/ritonavir 400/400 mg twice daily, and stavudine. Serum valproic acid levels remained therapeutic. ... 

The protease inhibitors indinavir, ritonavir, and saquinavir had no effect on intracellular activation of various NRTIs (didanosine, lamivu-dine, stavudine, zalcitabine and zidovudine). No interaction would be expected by this mechanism. Other potential interactions are discussed below. 

A 32-year-old HIV-positive man was admitted with suspected fusidic acid toxicity after taking fusidic acid 500 mg three times daily for one week, with his usual treatment of ritonavir 400 mg twice daily, saquinavir 400 mg twice daily and stavudine 40 mg twice daily. His plasma fusidic acid level was found to be twice the expected level, and his ritonavir and saquinavir levels were also elevated. He improved spontaneously, but... 

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