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Systemic Pharm I > Antivirals Pt. 2 > Flashcards

Antivirals Pt. 2 Flashcards

1
Q

Nucleoside Reverse Transcriptase Inhibitors for HIV

A

abacavir, didanosine, emtricitabine, lamivudine, stavudine, tenofovir, zidovudine (adel sings to zebras)

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2
Q

Non-Nucleoside Reverse Transcriptase Inhibitors for HIV

A

efavirenz, etravirine, nevirapine, rilpivirine

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3
Q

Protease Inhibitors

A

atazanavir, darunavir, fosamprenavir, indinavir, nelfinavir, ritonavir, saquinavir, tipranavir (find star)

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4
Q

Fusion inhibitors

A

enfuvirtide

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5
Q

Entry inhibitors

A

maraviroc

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6
Q

Integrase Inhibitors

A

dolutegravir, elvitegravir, raltegravir (-gravir)

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7
Q

What percent of people do not know they are infected with AIDs?

A

15% –1.1 million are infected

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8
Q

What is the treatment for HIV (generally)?

A

combinations of drugs aimed at suppressing HIV replication and allowing for restoration of CD4 cells and immunocompetence, aka HAART highly active antiretroviral therapy

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9
Q

What are the six classes of drugs that treat HIV?

A

NRTIs, NNRTIs, protease inhibitors, fusion inhibitors, entry inhibitors, integrase inhibitors

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10
Q

What is the current recommendation for primary therapy of HIV?

A

2 NRTIs and either a protease inhibitor, NNRTI or integrase inhibitor

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11
Q

What do you need to avoid with drug combinations for HIV?

A

two agents of the same nucleoside analog, overlapping toxicities, impact of drug interactions etc

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12
Q

What is the MOA of NRTIs?

A

inhibit reverse transcriptase and incorporates into viral DNA resulting in DNA chain termination

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13
Q

What is true of NRTIs in relation to host cell and mitochondrial DNA?

A

affinity is much lower for host cell DNA reverse transcriptase but mitochondrial DNA is susceptible

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14
Q

How are NRTIs excreted?

A

renal excretion except abacavir!

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15
Q

What are the adverse effects of NRTIs?

A

decreased bone density, kidney disease, GI disturbance, fatty liver, abnormal distribution of body fat, anxiety/confusion/depression, lactic acidosis, pancreatitis

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16
Q

T/F there are many NRTI drug interactions

A

false (zidovudine and tenofovir have a few)

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17
Q

What resistance exists for NRTIs?

A

cross resistance between agents of the same analog class– do not combine them

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18
Q

How are NRTIs and ARMD related?

A

NRTIs block the activity of a biological inflammatory pathway

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19
Q

Which NRTI is associated with major hypersensitivity reactions?

A

abacavir 5%

20
Q

Which NRTI has a long half-life (1x/day)

A

tenofovir

21
Q

What was the first anti HIV NRTI?

A

zidovudine

22
Q

What is the MOA of NNRTIs?

A

highly selective inhibitors of HIV-1 reverse transcriptase causing a conformational change to the enzyme

23
Q

What are two advantages of NNRTIs?

A

do not require activation by cellular enzymes and do not have cross-resistance with NRTIs

24
Q

What are disadvantages of NNRTIs?

A

there is cross resistance between NNRTIs, many drug interactions, high incidence of hypersensitivity reactions

25
Q

What is the most effective NNRTI?

A

efavirenz, longest half life

26
Q

Which NNRTI is associated with CNS side effects including vivid dreams?

A

efavirenz

27
Q

Which NNRTI is reserved for advanced disease because of potential for severe liver toxicity?

A

nevirapine

28
Q

What is the MOA of HIV protease inhibitors?

A

inhibit aspartyl protease stopping formation of essential enzymes and proteins in order to prevent maturation of the viral particles (results in production of noninfectious virions?

29
Q

T/F treatment with a protease inhibitor and two NRTIs results in a decrease in viral load to undetectable levels in 60-95% of new patients

A

true

30
Q

What is HIV treatment failure most likely due to?

A

lack of patient adherence

31
Q

What is the pharmacokinetics of HIV protease inhibitors?

A

poor oral bioavailability, metabolized by CYP450, no dosage adjustments for patients with renal impairment, limited CNS penetration

32
Q

What are adverse effects of HIV protease inhibitors?

A

paresthesias (tingling), GI disturbances, changes in glucose and lipid metabolism, fat redistribution

33
Q

What are the glucose and lipid metabolism changes from HIV protease inhibitors?

A

diabetes, hypercholesterolemia, and hypertriglyceridemia

34
Q

What is the main drug interaction dilemma with HIV protease inhibitors?

A

drugs that rely on metabolism for their termination of action may accumulate to toxic levels… do not use and caution lists of drugs

35
Q

Which PI is used as an enhancer of other protease inhibitors?

A

ritonavir, increases bioavailability of second drug because CYP450 inhibitor

36
Q

What are the adverse effects of ritonavir?

A

GI disturbance, headache, paresthesias

37
Q

What is the MOA of maraviroc (entry inhibitor)?

A

blocks the binding of the viral membrane to the host cell by blocking host cell virus receptor

38
Q

Why does the dose of an entry inhibitor (maraviroc) need to be reduced when given with protease inhibitors?

A

because of liver metabolism

39
Q

What is the MOA of enfuvirtide (fusion inhibitor)?

A

binds viral transmembrane glycoprotein and prevents the conformational change that would allow viral entry into the cell

40
Q

What drug is approved for therapy of patients who have already been treated and that have evidence of continued viral replication?

A

enfuvirtide (fusion inhibitor)

41
Q

How is enfuvirtide administered?

A

must be given subcutaneously (peptide), adverse effects are related to the injection

42
Q

What is the MOA of the integrase inhibitors?

A

inhibits the final step in integration of viral DNA into the host DNA

43
Q

What are the pharmacokinetic considerations of raltegravir?

A

no CYP450 interactions because kidney metabolism, side effects: headache and GI disturbances

44
Q

What drug works well in new patients AND in patients who have been treated previously?

A

raltegravir

45
Q

What are the pharmacokinetic considerations of dolutegravir?

A

highly protein bound, extensive liver metabolism, once daily dosing (or twice daily if previous treatment with integrase inhibitors)

46
Q

When is elvitegravir used?

A

only when in combination with tenofovir/emtricitabine/elvitegravir/cobicistat

47
Q

What are the two new drug combinations approved as a single pill?

A

juluca and dovato

Systemic Pharm I (13 decks)

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