Antiretroviral Drugs Flashcards
What are the Nucleoside/tide Reverse Transcriptase Inhibitors (NRTIs) and MOA?
MOA: lack of 3’OH terminates DNA elongation, competitive inhibitors of RT with activity against HIV-2/1
- Abacavir
- Didanosine
- Emtricitabine
- Lamivudine
- Stavudine
- Tenofovir (only nucleotide)
- Zidovudine
Abacavir AE and DI
NRTI
AE: hypersensitivity reactions with fever, rash malaise, respiratory, and/or GI
DI: avoid alcohol
Didanosine AE, DI
NRTI
AE: pancreatitis, peripheral neuropathy, GI disturbances, insulin resistance, retinal changes, optic neuritis
DI: Tenofovir, avoid concurrent neuropathic drugs
Emtricitabine AE
NRTI
AE: well tolerated but can cause hyperpigmentation of the palms and soles (especially in dark skinned pts)
Lamivudine AE
NRTI
AE: well tolerated compared to other NRTIs
Stavudine AE, DI
NRTI
AE: hyperlipidemia, peripheral neuropathy, increased serum aminotransferase levels, diabetes, pancreatitis, fatal lactic acidosis
DI: avoid concurrent neuropathic drugs
Tenofovir AE, DI
NRTI
AE: generally well tolerated; renal toxicity, decreased bone density and osteomalacia can occur
DI: Tenofovir lowers serum concentrations of Atazanavir; combined use with didanosine has been associated with CD4+ decline
Zidovudine AE, DI
NRTI
AE: bone marrow suppression, nausea, vomiting, headache, fatigue, confusion, malaise, hepatitis, diabetes
DI: myelosuppression may increase with coadministration of Ganciclovir, interferon alpha, Ribavirin, and other bone marrow suppressive agents; Coadministration with Doxorubicin or Stavudine should be avoided
What are the Nonnucleoside Reverse Transcriptase Inhibitors (NNRTIs) and MOA?
MOA: highly selective, noncompetitive inhibitors of HIV-1 RT and do not require phosphorylation
- Efavirenz
- Nevirapine
- Rilpivirine
Efavirenz AE, DI
NNRTI
AE: difficulty concentrating, vivid dreams, nightmares, teratogenic in 1st trimester, rash diziness, HA, insomnia, reduction in vitamin D levels, and hyperlipidemia
DI: substrate of CYP3A4 and inducer of CYP3A4 and 2B6
Nevirapine AE, DI
NNRTI
AE: rash, fever, nausea, HA, severe, hepatotoxicity, hepative failure and death
DI: inducer of CYP3A4 and 2B6
Rilpivirine AE
NNRTI
AE: rash, insomnia, depression, increased liver enzymes
What are the Protease Inhibitors and MOA?
MOA: reversible inhibitors of HIV aspartyl protease (which cleaves viral polyprotein into RT, protease, integrase)
- Atazanavir
- Darunavir
- Indinavir
- Lopinavir
- Nelfinavir
Atazanavir AE, DI
PI
AE: benign hyperbilirubinemia, rash, PR interval prolongation, nephrolithiasis
DI: concurrent use of drugs that increase gastric pH, such as PPIs, H2 blockers, and antacids may decrease absoprtion of Atazanavir
Darunavir AE, DI
PI
AE: rash
DI: inhibits CYP3A4; avoid in pts with sulfur allergy
