C/6. Antiretroviral Agents Flashcards
Drugs need to know in this topic (11)
Zidovudine Lamivudine Emtricitabine Abacavir Tenofovir Etravirine Ritonavir Darunavir Lopinavir Elvitegravir Maraviroc
Nuceloside/nucleotide reverse transcriptase inhibitor (NRTI’s)
MOA
Prodrug
Comeptitively inhibit binding of natural neceotide to RTase
NRTI’s general SEs
GI distress Headache, fatigue Hepatotoxicity Lactic acidosis Mitochondrial toxicity
NRTI’s drug (5)
Zidovudine Lamivudine Emtricitabine Abacavir Tenofovir
Ziduvudine
Hepatic metabolism
Renal elemination
DOC during pregnancy and lactation
Most toxic
BM suppresion
Lamivudine
Least potent and least toxic agent
Tx of hepatitis B infection
Emtricitabine
Newer form of lamivudine
CI in pregnancy, children, renal or hepatic dysfunction
Abacavir
Guanosine analogue
Allergy
Tenofovir
Nucleotide analogue
Tx of hepatitis B infection
Nephrotoxicity
Non-NRTI’s
MOA
Bind to site of RT different from the binding site of NRTI’s
Not required via phosphorylation
Etravirine
The newest NNRTI approved for HIV tx
Rash, nausea, diarrhea
Inhibitor+inducer of CYP450 enzyme
Protease inhibitors(PI's) MOA
Inhibits aspartate protease which is important to form viral structure
Ritonavir
Most commonly used protease inhibitor
GI distress
Hepatotoxicity
Most potent inhibitor of P450 enzymes
Darunavir
Used in combination with ritonavir in pts restant to other PI’s
GI distress, skin rash
Lopinavir
Used in combination with a subtherapeutic dose of ritonavir
Well tolerated
