Sustiva

Currently, Bristol-Myers Squibb is marketing Efavirenz under their brand name of Sustiva and Merck under the brand name of Stocrin . 

Figure 1. Chemical structures of representative ligands investigated A) biotin, B) 2-(4 -hydroxyazobenzene) benzoic acid (HABA), C) charged (X=CH2) and neutral (X=NH2+) carboxylate MMP inhibitors, D) TIBO scaffold, E) sustiva, and F) hydroxyethylamine scaffold. The biotin derivatives," MMP inhibitors,19 TIBO analogs,21 and cathepsin D inhibitors22 derived from structures A), C), D), and F), respectively, have been published elsewhere.

Shown below are snapshots of structures from our simulations of native RT with Sustiva and nevirapine. No crystal structure had been reported for RT with Sustiva when the calculations were performed however, confidence in the computed structure comes from the quantitative accord for the inhibition penalties and because Matador yielded docked structures for nevirapine, MKC-442, and 9-C1-TIBO that are virtually identical to the crystal structures.57 Sustiva hydrogen bonds with the backbone of K101, as do MKC-442 and 9-chloro-TIBO, and it has hydrophobic interactions in the Y181-Y188 pocket, also typical of NNRTIs. 

A crystal structure for the Sustiva/RT complex was subsequently reported and fully confirmed the correctness of the computed structure.58... 

Figure 3. Sustiva (left) and nevirapine (right) shown with select residues in the NNRTI binding site of H1V-RT. The initial structure of Sustiva/RT complex was obtained by docking.

Droperidol (Inapsine) Econazole (Spectazole) Efavirenz (Sustiva)... 

Abacavir (Ziagen) Amprenavir (Agenerase) Delavirdine (Rescriptor) Didanosine [ddl] (Videx) Efavirenz (Sustiva) Efavirenz/Emtricitabine/ Tenofovir (Atripla) Fosamprenavir (Lexiva)... 

Efavirenz (Sustiva) [Antiretroviral/NNRTI] Uses Hiv infxns Action Antiretroviral nonnucleoside RTI Dose Adults. 600 mg/d PO qhs Feds. See package insert avoid high-fat meals Caution [D, ] CDC recommends HIV-infected mothers not breast-feed Contra Component sensitivity Disp Caps SE Somnolence, vivid dreams, dizziness, rash, N/V/D Interactions T Effects W/ ritonavir T effects OF CNS depressants, ergot derivatives, midazolam, ritonavir, simvastatin, triazolam, warfarin X effects W/ carbamazepine, phenobarbital, rifabutin, rifampin, saquinavir, St. John s wort i effects OF amprenavir, carbamazepine, clarithromycin, indinavir, phenobarbital, saquinavir, warfarin may alter effectiveness OF OCPs EMS Concurrent EtOH usage can t CNS d ression OD May cause muscle contractions and adverse CNS effects activated charcoal may be effective... 

Bacheler, L., Weislow, O., Snyder, S., Hanna, G., D Aquila, R. and the SUSTIVA Resistance Study Team (1998). Abstract presented at the 12th World AIDS Conference. 

Efavirenz (Sustiva) is approved for the therapy of HIV infection of adults and children and is also used for postexposure prophylaxis. It is the only NNRTI approved for once-daUy dosing. Rash, although rarely severe, is a common adverse effect of efavirenz. Elevated liver enzymes and serum cholesterol also may occur. Central nervous system (CNS) effects in approximately half of patients may include dizziness, headache, insomnia, drowsiness, euphoria, agitation, impaired cognition, nightmares, vivid dreams, and hallucinations. These effects often subside after several weeks to months of therapy. 

Furtulon, Furzron Sustiva, Stocklin, Stocrin Emtriva Fludara... 

More recently, RTIs that are chemically distinct from zidovudine and other NRTIs have also been developed (see Table 34-3). These agents are known as nonnucleoside reverse transcriptase inhibitors (NNR-TIs), and include drugs such as delavirdine (Rescrip-tor), efavirenz (Sustiva), and nevirapine (Viramune).32 These drugs also inhibit the reverse transcriptase enzyme, but act at a different site on the enzyme than do their NRTI counterparts. 

The third strategy developed to inhibit HIV replication is the NNRTIs. These drugs include delavir-dine (Rescriptor), efavirenz (Sustiva), and nevirapine (Viramune). Fike their nucleoside counterparts, NNR-... 

Oral (Videx-EC) 125, 200, 250, 400 mg delayed release capsules Efavirenz(Sustiva)... 

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