Cloned from: HIV meds



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Atazanavir
1. Not associated with lipid abnormalities • May not be associated with lipodystrophy 2. May cause asymptomatic hyperbilirubinemia • Indirect • maybe associated with scleral icterus 3. May increase PR interval
Lamivudine (cytosine)
1. Very well tolerated 2. Active against HBV 3. Resistance can develop rapidly in nonadherent patient
Tenofovir (adenosine)
1. Only nucleotide analog (requires less phosphorylation) 2. Active against HBV 3. Some unique drug interaction (will ↓ atazanavir ↑ didanosine) 4. Associated with renal toxicity (most common if underlying kidney disease present; monitor creatinine, UA, electrolytes)
Abacavir (guanosine)
1. metabolized by alcohol dehydrogenase and glucuronyl transferase (alcohol increases ABC levels 41%) 2. may cause hypersensitivity reaction • occurs in 2-9% of patients (median onset 9 days, 90% occur in first eight weeks) • multisystem signs and symptoms (fever, skin rash, fatigue, nausea, vomiting, diarrhea, abdominal pain, pharyngitis, dyspnea, cough, myalgias, arthralgia) • increase in intensity as patient continues abacavir; improve within 24 hours of d/c of abacavir • has caused life threatening hypotension and death on rechallenge • genetic link (check for presence of HLA-B5701 and do not use abacavir if this allele is present) • management: discontinue 3. Recent data suggests abacavir linked with cardiac events
Zidovudine (thymidine)
1. May cause macrocytic anemia 2. May cause myopathy
Emtricitabine (cytosine)
Back1. Very similar to lamivudine 2. Well tolerated 3. Active against HBV 4. Resistance develops rapidly
Efavirenz
1. Food effect: avoid after high fat meal 2. Neuropsychiatric side effects common (dizziness, drowsiness, abnormal dreams); usually self limiting 3. Teratogenic 4. May cause false positive urine drug screen for marijuana 5 Combination product: Atriplaฎ efavirenz plus tenofovir plus emtricitabine. One tablet once daily. Good choice for most treatment na๏ve patients; treatment experienced patients likely will have resistance to emtricitabine and/or efavirenz 6. Resistance develops rapidly in nonadherent patient.
Etravirine
1. Food effect: take with food 2. Well tolerated 3. Likely effective when resistance present to efavirnez or nevirapine; as NNRTI mutations accumulate, etravirine susceptibility is reduced
Nevirapine
1. Higher incidence of hepatotoxocity; not recommended in patients with CD4 counts >250 for females and >400 for males; check serum transaminases at baseline, at 2 weeks, 4 weeks and then monthly for the first 18 weeks 2. Higher incidence of rash (rash present in 50% of hepatotoxicity cases) 3. Resistance develops rapidly in nonadherent patient
Ritonavir
1. Ritonavir is used as a pharmacologic enhancement of other protease inhibitors • will reduce pill burden • increases trough allowing for possible activity against moderately resistant strains f 2. Food effect: take with meals to improve bioavailability and t tolerance
Fosamprenavir
1. Prodrug to amprenavir 2. Contains sulfa moiety • little cross reactive with sulfa drugs 3. May cause rash
Darunavir
1. Non-peptidic structure • useful for HIV with resistance to other PIs 2. May cause rash, but generally well tolerated 3. Must use with ritonavir
Lopinavir/ ritonavir
1. Current gold standard for potency. 2. Take with food to increase tolerability and improve AUC
Nelfinavir
1. Food effect: levels increase 2-3 X with food, take with meals or light snack 2. Diarrhea common 3. Only protease inhibitor that does not benefit from boosting effects of ritonavir
Saquinavir
1. Food effect: take with food • Oral bioavailability only 4% • Levels increase 6 fold with food • Must be given with ritonavir
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