HIV Pharm Flashcards

1
Q

zidovudine (AZT)

A
  • Nucleotide RT inhibitor
  • Blocks thymidine addition
  • Effective against HIV and HTLV
  • risk of lactic acidosis syndrome, bone marrow suppression, myopathy, hepatic steatosis
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2
Q

stavudine

A
  • Like AZT
  • Nucleotide RT inhibitor
  • Blocks thymidine addition
  • Only effective against HIV
  • risk of lactic acidosis syndrome, peripheral neuropathy, fat wasting, hepatic steatosis
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3
Q

emtricitabine

A
  • Nucleotide RT inhibitor
  • Blocks cytosine addition
  • Effective against HIV and HBV
  • long half life, and excreted unchanged in urine
  • leads to hyperpigmentation
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4
Q

lamivudine

A
  • Nucleotide RT inhibitor
  • Blocks cytodine addition
  • Effective against HIV and HBV
  • dual treatment with doltegravir is used for treatment naïve patients
  • long half life, and excreted unchanged in urine
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5
Q

abacavir

A
  • Nucleotide RT inhibitor
  • Blocks guanosine addition
  • patient can’t have HLA-B*5701 genotype due to toxicity
  • not a CYP substrate
  • risk of hyperlipidemia and cardiac events
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6
Q

didanosine

A
  • Nucleotide RT inhibitor
  • Blocks adenosine addition
  • can be toxic: peripheral neuropathy, pancreatitis, hepatic steatosis
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7
Q

tenofovir disoproxil fumarate

A
  • Nucleotide RT inhibitor
  • Blocks adenosine addition
  • Effective against HIV and HBV
  • can cause renal tubular necrosis and Fanconi syndrome, and decreased bone mineral density.
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8
Q

tenofavir alafenamide

A
  • -Nucleotide RT inhibitor
  • Blocks adenosine addition
  • Effective against HIV and HBV
  • distributes differently than TDF (lower [plasma], higher [IC])
  • less renal and bone toxicity
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9
Q

raltegravir

A
  • Integrase Strand Transfer Inhibitors
  • blocks covalent bond formation in viral & host DNA (strand transfer)
  • rare skin and immune hypersensitivity rxns
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10
Q

elvitegravir (/c or /r)

A
  • Integrase Strand Transfer Inhibitors
  • blocks covalent bond formation in viral & host DNA (strand transfer)
  • metabolozed by CYP3A4 so it needs to be boosted
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11
Q

dolutegravir

A
  • Integrase Strand Transfer Inhibitors
  • blocks covalent bond formation in viral & host DNA (strand transfer)
  • high genetic barrier to resistance
  • avoid in pregnancy due to neural tube defects
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12
Q

bictegravir

A
  • Integrase Strand Transfer Inhibitors
  • blocks covalent bond formation in viral & host DNA (strand transfer)
  • high genetic barrier to resistance
  • only available in tablet bictegravir/emtricitabine/TAF
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13
Q

enfuvirtide

A
  • 36 aa peptide derived from viral gp41 part that fuses with cell membrane
  • inhibits membrane fusion
  • ONLY effective against HIV-1
  • only parenteral administration
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14
Q

saquinavir

A
  • protease inhibitor, prevents maturation of HIV particle
  • not often used due to pill burden
  • GI distress and fat wasting
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15
Q

lopinavir /r

A
  • protease inhibitor, prevents maturation of HIV capsid
  • often works after other PIs fail
  • GI distress, hyperlipidemia
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16
Q

azatanavir /c

A
  • protease inhibitor, prevents maturation of HIV capsid
  • treatment-naïve patients
  • unconjugated hyperbilirubinemia not associated with hepatitis
  • GI distress, fat wasting
17
Q

darunavir /c

A
  • non-peptide protease inhibitor, prevents maturation of capsid
  • sulfa drug, can cause allergy
  • GI distress, fat wasting
18
Q

nevirapine

A
  • Non-Nucleoside Reverse Transcriptase Inhibitors
  • ONLY for HIV-1
  • induces CYP3A4, reduces level of birth control
  • rash/itching
19
Q

efavirenz

A
  • Non-Nucleoside Reverse Transcriptase Inhibitors
  • ONLY for HIV-1
  • given as efavirenz/emtricitabine/tenofovir
  • induces CYP3A4
  • psychiatric effects, potentially teratogenic
20
Q

etravirine

A
  • Non-Nucleoside Reverse Transcriptase Inhibitors
  • ONLY for HIV-1
  • Still works after mutations that disable other NNRTIs
  • induces CYP3A4
  • can cause fat redistribution and Stevens-Johnson Syndrome
21
Q

rilpivirine

A
  • Non-Nucleoside Reverse Transcriptase Inhibitors
  • ONLY for HIV-1
  • not affected by mutations that inhibit efavirenz and nevirapine
  • metabolized by CYP3A4
  • depression, decreased cortisol, fat redistribution, immune reconstitution syndrome
22
Q

doravirine

A
  • Non-Nucleoside Reverse Transcriptase Inhibitors
  • ONLY for treatment-naïve patients with HIV-1
  • novel resistance unlike others in class
  • metabolized by CYP3A4
  • immune reconstitution syndrome
23
Q

maraviroc

A
  • chemokine receptor antagonist, blocks binding of GP120 to CCR5 co-receptor
  • resistance develops by shift tot CXCR4 or mutation in V3 loop in GP120
  • expensive tropism test req’d before use
  • CYP3A4 substrate
  • minor rxn, and hepatic toxicity
24
Q

/r = ritonavir

A
  • protease inhibitor that blocks CYP3A4

- used to boost levels of protein inhibitors

25
Q

/c = cobicistat

A
  • CYP3A4 inhibitor

- used to boost levels of protein inhibitors

26
Q

indinavir

A
  • protease inhibitor, prevents maturation of HIV particle

- can cause crystaluria or renal stones