antivirals2: HIV Flashcards

1
Q

Zidovudine (RetrovirR)

A

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
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2
Q

Zidovudine (RetrovirR) SEs

A

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)

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3
Q

Zidovudine (RetrovirR) uses

A
  • 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
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4
Q

Didanosine (VidexR)

A

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

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5
Q

Didanosine (VidexR) SEs

A

peripheral neuropathy, potentially fatal pancreatitis and GI disturbances.

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6
Q

Lamivudine (EpivirR)

A

Nucleoside Reverse Transcriptase Inhibitor (NRTI)

  • Hep B*
  • does not cause peripheral neuropathy
  • recommended for “naive” pts*
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7
Q

Abacavir (ZiagenR)

A

Nucleoside Reverse Transcriptase Inhibitor (NRTI)

recommended for “naive” pts

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8
Q

Abacavir (ZiagenR) SEs

A

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

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9
Q

Emtricitabine (EmtrivaR)

A

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

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10
Q

Emtricitabine (EmtrivaR) SEs

A

hyperpigmentation of the palms and soles

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11
Q

Tenofovir (VireadR)

A

NucleoTide Reverse Transcriptase Inhibitor
HepB
Available alone as VireadR and in fixed-dose combinations with emtricitabine (TruvadaR) and with emtricitabine and efavirenz (AtriplaR)

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12
Q

Tenofovir (VireadR) SEs

A

GI: N/V/D

renal toxicity

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13
Q

Nevirapine (ViramuneR) FYI

A

Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)

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14
Q

how NNRTIs are different than NRTIs (KNOW!)

A

They bind DIRECTLY to reverse transcriptase

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15
Q

Efavirenz (SustivaR)

A

Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)

substrate for cytP450 isoforms

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16
Q

Efavirenz (SustivaR) SEs

A

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
Q

Ritonavir (NorvirR)

A
Protease Inhibitor (PI)
*precursor protein* (peptidomimetic)
metabolized by and inhibitor of cytP450 (all PIs)
18
Q

Ritonavir (NorvirR) SEs

A

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

19
Q

Indinavir sulfate (CrixivanR)

A
Protease Inhibitor (PI)
cytP450
20
Q

Indinavir sulfate (CrixivanR) SEs (KNOW)

A

kidney stones (nephrolithiasis)

also derm changes: alopecia, dry skin/mucous membranes

21
Q

Nelfinavir mesylate(ViraceptR)

A
Protease Inhibitor (PI)
cytP450
22
Q

Lopinavir/Ritonavir (KaletraR)

A
Protease Inhibitor (PI)
cytP450
23
Q

Atazanavir sulfate

A
Protease Inhibitor (PI)
cytP450
24
Q

Maraviroc (SelzentryR) (FYI, in sketchy)

A

Chemokine Receptor CCR5 Antagonist

25
Q

Goals of antiretroviral (ART) therapy

A
  • 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
Q

HIV tx in ??

meanwhile, monitor the pts??

A

combo (3 or 4 drugs)

-HIV RNA levels, known as the “viral load” and the CD4 cell count.

27
Q

lipid membrane plays an important role

A

helps virus attach to host cell

28
Q

indications for ART

A
  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
Q

case: Protease inhibitor SEs

A

abnormal fat distribution

30
Q

HIV drugs that can be used for HepB as well

A

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