antivirals2: HIV Flashcards
Zidovudine (RetrovirR)
Nucleoside Reverse Transcriptase Inhibitor (NRTI)
- thymidine analog, contains a 3’-azido group rather than a 3’-hydroxyl group, results in chain termination
- good CSF penetration, plasma protein bound, excreted by kidneys
Zidovudine (RetrovirR) SEs
CNS: ha, malaise, confusion, dizziness.
short term: GI: N/V/D, hepatitis
long term: blood: Anemia, granulocytopenia, thrombocytopenia, bone
marrow toxicity.
CI: admin w. extreme caution to pts w. compromised BM function (anemia/neutropenia after 2-6 wks may occur)
Zidovudine (RetrovirR) uses
- drug of choice for reducing HIV transmission: used alone starting at 14-34 wks gestation and continued in infant for 1st 6 wks of life*
- alone and in fixed-dose combos with lamivudine as (CombivirR) and with lamivudine and abacavir as (TrizivirR); virtually any other NRTI except for stavudine
Didanosine (VidexR)
Nucleoside Reverse Transcriptase Inhibitor (NRTI)
Inhibits of RT by competing with the natural nucleotide triphosphate, dATP, for binding to active site of the enzyme.
-incorporation of ddATP into viral DNA leads to chain termination, and thus inhibition of viral replication, similar to Zidovudine
Didanosine (VidexR) SEs
peripheral neuropathy, potentially fatal pancreatitis and GI disturbances.
Lamivudine (EpivirR)
Nucleoside Reverse Transcriptase Inhibitor (NRTI)
- Hep B*
- does not cause peripheral neuropathy
- recommended for “naive” pts*
Abacavir (ZiagenR)
Nucleoside Reverse Transcriptase Inhibitor (NRTI)
recommended for “naive” pts
Abacavir (ZiagenR) SEs
severe hypersensitivity reaction, usually with rash, fever and malaise, and sometimes with respiratory or GI symptoms
Emtricitabine (EmtrivaR)
Nucleoside Reverse Transcriptase Inhibitor (NRTI)
5-fluorinated derivative of lamivudine
HepB
Emtricitabine (EmtrivaR) SEs
hyperpigmentation of the palms and soles
Tenofovir (VireadR)
NucleoTide Reverse Transcriptase Inhibitor
HepB
Available alone as VireadR and in fixed-dose combinations with emtricitabine (TruvadaR) and with emtricitabine and efavirenz (AtriplaR)
Tenofovir (VireadR) SEs
GI: N/V/D
renal toxicity
Nevirapine (ViramuneR) FYI
Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
how NNRTIs are different than NRTIs (KNOW!)
They bind DIRECTLY to reverse transcriptase
Efavirenz (SustivaR)
Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
substrate for cytP450 isoforms