-
NRTI drugs
- Abacavir
- Didanosine
- Emtricitabine
- Lamivudine
- Stavudine
- Zidovudine
-
NNRTI
- Delavirdine
- Efavirenz
- Nevirapine
-
Protease inhibitors
- Atazanavir
- Indinavir
- Lopinavir
- Ritonavir
- Saquinavir
-
-
Integrase Inhibitors
Raltegravir
-
Nucleotide Reverse transcriptase inhibitors
MOA
CLINICAL
A/E
- competitive inhibition of HIV-1 reverse transcriptase
- Incorporation into viral DNA chain -> premature chain termination.
HIV 1/2
Mitochondrial toxicity
-
Abacavir
NRTI
- Guanosine analog
- Oral
- Resistance needs 2-3 mutations
A/E: hypersensitivity reactions
-
Didanosine
- NRTI
- Deoxyadenosine synthetic analog
- Oral (empty stomach)
A/E: Pancreatitis, neuropathy, cardiomyopathy, retinal changes***
CONTRA: with indinavir, delavirdane, atazanavir, dapsone, itraconazole, & fluoroquinolone
-
Emtricitabine
- NRTI
- Fluorinated analog of Lamivudine
- ORAL
- Spectrum: HIV & HBV
Contra: Kids, pregnancy, renal failure, hepatic failure, with metronidazole disulfira or lamivudine
-
Lamivudine
- NRTI
- Cytosine analog
- ORAL
- Spectrum: HIV-1, HBV
MOA: inhibits HIV reverse transcriptase and HBV DNA polymerase
CONTRA: with zalcitabine
-
Stavudine
- NRTI
- Thymidine analog
- ORAL
A/E: neuropathy, panreatitis, arthralgias.
- CONTRA: Advanced immunosuppression.
- With neuropathy-inducing drugs
-
Zidovudine
- NRTI
- Deoxythymidine analog
- CLINICAL:
- Prevent HIV vertical transmission
- Occupational HIV
-
NNRTI
MOA: Bind HIV-1 reverse transcriptase in an allosteric fashion.
A/E: Steven Johnsons syndrome
- CONTRA:
- Not with: Anti-arrhythmics
- antihistamines
- sedative hypnotics
- Neuroleptics
- Ergot alkaloid derivatives
- HMG COA reductase inhibitors
- Anticonvulsants
- Oral contraceptives
-
-
Efavirenz
ORAL (empty stomach)
- CONTRA:
- High fat meals
- Pregnancy
-
Nevirapine
Clincal: HIV vertical transmission
-
PI
MOA: prevent posttranslational cleavage of Gag-Pol polyprotein -> immature viral particles
- A/E: Cushing like fat redistribution
- inc LDL and trigylceride levels
-
Atazanavir
- Contra:
- with acid-reducing agents
- with indinavir, irinotecan, tenofovir, and efavirenz
-
Indinavir
- A/E: indirect hyperbilirubinemia and nephrolithiasis
- Thrombocytopenia
-
Lopinavir
- PI
- Oral with ritonavir (inhibits CYP3A metabolism of lopinavir)
-
Rotinavir
A/E: paresthesias, elevated aminotransferase levels
- Contra: impaired hepatic function
- with digoxin and theophylline
-
Saquinavir
- PI
- Oral(with ritonavir, 2 hours after fatty meal)
-
Enfuvirtide
Entry inhibitor
Spectrum: HIV 1
MOA: bind gp 41 (mutation)
A/E: hypersensitivity, inc risk of bacterial pneumonia
-
Maraviroc
Entry inhibitor
Oral
Spectrum: R5 HIV-1
- MOA: bind CCR5
- Mutation: in V3 loop of gp 120
Last drive drug
-
Raltegrvir
Spectrum: HIV1/2
MOA: binds integrase (mutation)
Clinical: treatment experienced patients as last resort
Contra: with rifampin and antacids
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