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Flashcards in antivirals2: HIV Deck (30):
1

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

2

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)

3

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

4

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

5

Didanosine (VidexR) SEs

*peripheral neuropathy*, potentially fatal pancreatitis and GI disturbances.

6

Lamivudine (EpivirR)

Nucleoside Reverse Transcriptase Inhibitor (NRTI)
*Hep B*
-does not cause peripheral neuropathy
*recommended for "naive" pts*

7

Abacavir (ZiagenR)

Nucleoside Reverse Transcriptase Inhibitor (NRTI)
*recommended for "naive" pts*

8

Abacavir (ZiagenR) SEs

*severe hypersensitivity reaction*, usually with rash, fever and malaise, and sometimes with respiratory or GI symptoms

9

Emtricitabine (EmtrivaR)

Nucleoside Reverse Transcriptase Inhibitor (NRTI)
5-fluorinated derivative of lamivudine
*HepB*

10

Emtricitabine (EmtrivaR) SEs

hyperpigmentation of the palms and soles

11

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)

12

Tenofovir (VireadR) SEs

GI: N/V/D
renal toxicity

13

Nevirapine (ViramuneR) FYI

Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)

14

how NNRTIs are different than NRTIs (KNOW!)

*They bind DIRECTLY to reverse transcriptase*

15

Efavirenz (SustivaR)

Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
substrate for cytP450 isoforms

16

Efavirenz (SustivaR) SEs

dizziness, headache, insomnia, inability to concentrate and rash.
-Neural tube defects have been reported in women who took the drug during the first trimester of pregnancy

17

Ritonavir (NorvirR)

Protease Inhibitor (PI)
*precursor protein* (peptidomimetic)
metabolized by and inhibitor of cytP450 (all PIs)

18

Ritonavir (NorvirR) SEs

*Circumoral and peripheral paresthesia*
N/V/D
Elevated liver enzymes

19

Indinavir sulfate (CrixivanR)

Protease Inhibitor (PI)
cytP450

20

Indinavir sulfate (CrixivanR) SEs (KNOW)

*kidney stones* (nephrolithiasis)
also derm changes: alopecia, dry skin/mucous membranes

21

Nelfinavir mesylate(ViraceptR)

Protease Inhibitor (PI)
cytP450

22

Lopinavir/Ritonavir (KaletraR)

Protease Inhibitor (PI)
cytP450

23

Atazanavir sulfate

Protease Inhibitor (PI)
cytP450

24

Maraviroc (SelzentryR) (FYI, in sketchy)

Chemokine Receptor CCR5 Antagonist

25

Goals of antiretroviral (ART) therapy

-suppress the HIV viral load to less than 50 copies of the virus per mL
-restore the patient’s immune function( CD4+ count)
-prevent transmission of HIV
-prevent drug resistance
-preserve therapeutic function
-improve pt quality of life

26

HIV tx in ??
meanwhile, monitor the pts??

combo (3 or 4 drugs)
-HIV RNA levels, known as the “viral load” and the CD4 cell count.

27

lipid membrane plays an important role

helps virus attach to host cell

28

indications for ART

1. Presence of symptomatic HIV disease
2. CD4 count below 200 cells/microliter
3. CD4 count between 200-350 cell/microliter with high viral load or rapid CD4 decline
4. Pregnant women with HIV to reduce vertical transmission

29

case: Protease inhibitor SEs

abnormal fat distribution

30

HIV drugs that can be used for HepB as well

Lamivudine (EpivirR)
Emtricitabine (EmtrivaR)
Tenofovir (VireadR)