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Pharmacology > Antiretrovirals > Flashcards

Antiretrovirals Flashcards

1
Q

what are the six classes of antiretrovirals

A
  • nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs)
  • non nucleoside/nucleotide reverse transcriptase inhibitors (NNRTIs)
  • Protease Inhibitors (PIs)
  • Fusion Inhibitors (FIs)
  • CCR5 antagonists
  • Integrase Strand Transfer Inhibitors (INSTIs)
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2
Q

what drugs are used to improve the pharmacokinetic profiles of some antiretrovirals

A

pharmacokinetic enhancers

-ex: PIs and the INSTIs, elvitegravir

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3
Q

what does a typical antiretroviral regimen consist of

A
  • two NRTIs
  • usually abacavir + lamivudine
  • or tenofivir + emtricitabine
  • with a third antiretroviral from the classes NNRTIs, INSTIs, or PIs
  • with a pharmacokinetic enhancer
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4
Q

what are the NRTIs (nucleoside/nucleotide reverse transcriptase inhibitors)

A

TADELSZ

Tenofovir
Abacavir
Didanosine
Emtricitabine
Lamivudine
Stavudine
Zidovudine
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5
Q

mechanism of NRTIs

A

TADELSZ - tenofovir, abacavir, didanosine, emtricitabine, lamivudine, stavudine, zidovudine

  • enters the cells and undergoes phosphorylation to generate synthetic substrates for the HIV RNA dependent DNA polymerase enzyme aka reverse transcriptase
  • phosphorylated analogue competitively inhibits incorporation of native nucleotides and prevents elongation of nascent provirus because they lack a 3’ OH
  • essentially prevents formation of provirus from HIV RNA
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6
Q

what are most of the adverse effects of NRTIs associated with (name them)

A

TADELSZ - tenofovir, abacavir, didanosine, emtricitabine, lamivudine, stavudine, zidovudine

-some NRTIs have an affinity for human DNA polymerase-gamma, a mitochondrial enzyme –> anemia, granulocytopenia, myopathy, peripheral neuropathy, lipatrophy, lactic acidosis, and pancreatitis

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7
Q

adverse effects of abacavir and what drug should be avoided

A

hypersensitivity rash with fever, rash, malaise, respiratory and or GI symptoms

avoid alcohol

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8
Q

adverse effects of didanosine and what drug should be avoided

A

PANCREATITIS (insulin disturbance)
Peripheral Neuropahty
Retinal Changes

avoid Tenofovir because it increases the concentration of didanosine –> more likely cause side effects

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9
Q

of all the NRTIs which are nucleoside and which are nucleotide

A

Tenofovir is a nucleotide while the rest are nucleosides and hence need to be phosphorylated to be active

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10
Q

adverse effect of emtricitabine

A

hyperpigmentation of palms and soles especially in darker skinned people

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11
Q

adverse of Staduvine and what drug to avoid

A

FATAL LACTIC ACIDOSIS
Peripheral Neuropathy
Diabetes
Pancreatitis

avoid concurrent neuropathic drugs

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12
Q

drug interactions of Tenofovir

A
  • lowers serum conc of atazanavir
  • increases conc of didanosine
  • together with didanosine –> decreased CD4 T cells
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13
Q

adverse effects of Tenofovir

A

Renal Toxicity
Decreased bone density
Osteomalacia

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14
Q

adverse effects of Zidovudine and what drugs should be avoided

A

Myelosuppression (bone marrow suppression)

avoid co-administration with doxorubicin and stavudine; also avoid other myelosuppressive drugs

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15
Q

what are the NNRTIs (non nucleoside/nucleotide reverse transcriptase inhibitors)

A

REN

Rilpivirine
Efavirenz
Nevirapine

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16
Q

mechanism of NNRTIs (name them)

A

REN - Rilpivirine, Efavirenz, Nevirapine

they non-competitively bind to reverse transcriptase distant from the active site and cause conformational changes hence reducing its activity without the need for phosphorylation

17
Q

adverse effect of Efavirenz

A

DVN’T (DON’T

Difficulty concentrating
Vivid Dreams
Nightmares
Teratogenic (avoid in 1st trimester)

18
Q

adverse effects of Rilpivirine

A

Insomnia

Depression

19
Q

adverse effects of Nevirapine

A

Severe Hepatotoxicity

Hepatic Failure

20
Q

what are inducers of both CYP3A4 and CYP2B6

A

Nevirapine and Efavirenz

21
Q

what are the protease inhibitors

A

NAVIR tease a Protease LIDAN

Lopinavir
Indinavir
Darunavir
Atazanavir
Nelfinavir
22
Q

which protease inhibitor is not a substrate for CYP3A4

A

Nelfinavir

23
Q

mechanism of protease inhibitors (name them)

A

NAVIR tease a protease LIDAN - lopinavir, indinavir, darunavir, atazanavir, nelfinavir

competitively inhibits virus aspartyl protease hence inhibiting proteolytic cleavage of HIV gag and pol that includes enzymatic and structural component of HIV

24
Q

adverse effects of Lopinavir, Indinavir, and Darunavir

A

Lopinavir - Asthenia (lack of energy) and Pancreatitis

Indinavir - increased indirect bilirubin, nephrolithiasis, cholelithiasis, rash, blurred vision

Darunavir - Rash

25
Q

who should avoid darunavir

A

those with sulfa allergy

26
Q

adverse effects of Atazanavir and Nelfinavir

A

Atazanavir - Hyperbilirubinemia and PR elongation

Nelfinavir - nausea and flatulence

27
Q

in general what are adverse effects of protease inhibitors (name them)

A

NAVIR tease a protease LIDAN - lopinavir, indinavir, darunavir, atazanavir, and nelfinavir

disorders of fat and carb distribution - hyperglycemia, insulin resistance, hyperlipidemia, truncal obesity etc

28
Q

what are the integrase strand transfer inhibitors (INSTIs)

A

Integrase RED GRAVIR

Raltegravir
Elvitegravir
Dolutegravir

29
Q

how is raltegravir eliminated and what can increase its elimination hence decreasing its con

A

eliminated by glucuronidation mediated by UDP glucuronosyltransferase 1A1 aka UGT1A1

conc can be decreased by strong inducer of UGT1A1 for ex rifampin

30
Q

adverse of INSTIs (name them)

A

Integrase RED Gravir - Raltegravir, Elvitegravir, Dolutegravir

increase in creatinine phosphokinase, myopathy, rhabdomyolysis, and systemic hypersensitivity reactions

31
Q

what is the CCR5 antagonist and its mechanism

A

Maraviroc binds to CCR5 co receptor and prevents entry of CCR5 tropic viruses into CD4 T cells

32
Q

what is the fusion inhibitor and its mechanism

A

Enfuvirtide binds to gp41 and prevents conformational change that would allow HIV virus to fuse to host cell

33
Q

what are the pharmacokinetic enhancers

A

Cobicistat

Ritonavir

34
Q

mechanism of pharmacokinetic enhancers (name them)

A

Cobicistat and Ritonavir

both potent inhibitors of CYP3A4 hence increasing plasma conc of antiretroviral drugs that are broken down by CYP3A4 leading to higher efficacy and less frequent dosing

35
Q

difference between Cobicistat and Ritonavir

A
  • Ritonavir has its own antiretroviral activity although it is not used for that but rather for its pharmacokinetic enhancing ability while cobicistat has no antiretroviral activity
  • Ritonavir is mainly used with PIs while Cobicistat is used with INSTIs
36
Q

antiretroviral drugs that should be avoided during pregnancy

A
  • Efavirenz due to its teratogenic activity

- Nevirapine in those with CD4 greater than 250 due to its increased risk of hepatotoxicity

37
Q

preferred regimen for occupational post exposure prophylaxis of HIV

A

superficial: 2 NRTIs

Deep: 2 NRTIs and one from another group
Raltegravir + Tenofovir + Emtricitabine

38
Q

general recommended treatment for HIV patients (also be specific)

A

2 NRTIs and INSTI (highly effective with fewer side effects and no CYP3A4 drug interactions0
(Tenofovir + Emtricitabine + Raltegravir)
(Tenofovir + Emtricitabine + Daltegravir)

2 NRTIs and PI
(Tenofovir + Emtricitabine + Darunavir or Ritonavir)

39
Q

what are HIV prophylactic vaccines

A

Strep pneumonia
Hep A and B
Influenza

Pharmacology (79 decks)

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