HIV Therapy Flashcards
Atazanavir
Protease inhibitor.
Assembly of virions depends on HIV-1 protease (pol gene), which cleaves polypeptide products of HIV mRNA into functional parts. Protease inhibitors prevent maturation of new viruses and inhibits assembly of new viruses.
Hyperglycemia, GI intolerance (nausea, diarrhea), lipodystrophy.
Darunavir
Protease inhibitor.
Assembly of virions depends on HIV-1 protease (pol gene), which cleaves polypeptide products of HIV mRNA into functional parts. Protease inhibitors prevent maturation of new viruses and inhibits assembly of new viruses.
Hyperglycemia, GI intolerance (nausea, diarrhea), lipodystrophy.
Fosamprenavir
Protease inhibitor.
Assembly of virions depends on HIV-1 protease (pol gene), which cleaves polypeptide products of HIV mRNA into functional parts. Protease inhibitors prevent maturation of new viruses and inhibits assembly of new viruses.
Hyperglycemia, GI intolerance (nausea, diarrhea), lipodystrophy.
Indinavir
Protease inhibitor.
Assembly of virions depends on HIV-1 protease (pol gene), which cleaves polypeptide products of HIV mRNA into functional parts. Protease inhibitors prevent maturation of new viruses and inhibits assembly of new viruses.
Hyperglycemia, GI intolerance (nausea, diarrhea), lipodystrophy, crystal-induced nephropathy (drug precipitates in urine), hematuria.
Lopinavir
Protease inhibitor.
Assembly of virions depends on HIV-1 protease (pol gene), which cleaves polypeptide products of HIV mRNA into functional parts. Protease inhibitors prevent maturation of new viruses and inhibits assembly of new viruses.
Hyperglycemia, GI intolerance (nausea, diarrhea), lipodystrophy.
Ritonavir
Protease inhibitor.
Assembly of virions depends on HIV-1 protease (pol gene), which cleaves polypeptide products of HIV mRNA into functional parts. Protease inhibitors prevent maturation of new viruses and inhibits assembly of new viruses.
Hyperglycemia, GI intolerance (nausea, diarrhea), lipodystrophy. Boosts other drug concentrations by inhibiting CYP450.
Saquinavir
Protease inhibitor.
Assembly of virions depends on HIV-1 protease (pol gene), which cleaves polypeptide products of HIV mRNA into functional parts. Protease inhibitors prevent maturation of new viruses and inhibits assembly of new viruses.
Hyperglycemia, GI intolerance (nausea, diarrhea), lipodystrophy.
Abacavir (ABC)
Nucleoside analog RTI
Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3’ OH group). Need phosphorylation for activation.
Bone marrow suppression (reversible with G-CSF and erythropoeitin), peripheral neuropathy, lactic acidosis.
Didanosine (ddI)
Nucleoside analog RTI
Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3’ OH group). Need phosphorylation for activation.
Bone marrow suppression (reversible with G-CSF and erythropoeitin), peripheral neuropathy, lactic acidosis, pancreatitis.
Emtricitabine (FTC)
Nucleoside analog RTI
Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3’ OH group). Need phosphorylation for activation.
Bone marrow suppression (reversible with G-CSF and erythropoeitin), peripheral neuropathy, lactic acidosis.
Lamivudine (3TC)
Nucleoside analog RTI
Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3’ OH group). Need phosphorylation for activation.
Bone marrow suppression (reversible with G-CSF and erythropoeitin), peripheral neuropathy, lactic acidosis.
Stavudine (d4T)
Nucleoside analog RTI
Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3’ OH group). Need phosphorylation for activation.
Bone marrow suppression (reversible with G-CSF and erythropoeitin), peripheral neuropathy, lactic acidosis.
Tenofovir (TDF)
Nucleotide analog RTI
Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3’ OH group). Does not need phosphorylation for activation.
Bone marrow suppression (reversible with G-CSF and erythropoeitin), peripheral neuropathy, rash.
Zidovudine (ZDV)
Nucleoside analog RTI
Competitively inhibit nucleotide binding to reverse transcriptase and terminate the DNA chain (lack 3’ OH group). Need phosphorylation for activation.
Bone marrow suppression (reversible with G-CSF and erythropoeitin), peripheral neuropathy, lactic acidosis, anemia.
Used for general prophylaxis and in pregnancy to decrease fetal transmission.
Efavirenz
NNRTI
Bind to reverse transcriptase at different site than NRTIs. Do not require phosphorylation for activation. Do not compete with nucleotides. Prevents incorporation of viral genome into host DNA.
Rash, hepatotoxicity, vivid dreams, CNS symptoms. Contraindicated in pregnancy.
