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Pharmacology > EXAM #4: ANTIRETROVIRALS > Flashcards

EXAM #4: ANTIRETROVIRALS Flashcards

1
Q

What does NRTI stand for?

A

Nucelotide Reverse Transcriptase Inhibitor

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2
Q

List the NRTIs.

A 
Zidovudine 
Lamivudine 
Abacavir 
Tenofovir disoproxil
Emtricitabine
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3
Q

What is the MOA of the NRTIs?

A

Analogs of nucleotides that inhibit nucleotide binding to REVERSE TRANSCRIPTASE and cause DNA chain termination

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4
Q

What is required for conversion of the NRTIs into their active form?

A

Cellular kinases

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5
Q

What infection aside from HIV can be treated with NRTIs?

A

HBV

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6
Q

What are the adverse effects common to the NRTIs?

A

1) Lactic acidosis
2) Fatty liver disease
3) Lipodystrophy

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7
Q

What is Abacavir?

A

Guanosine analog NRTI

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8
Q

What specific adverse effects are associated with Abacavir?

A

Allergic reaction

Think “A” for allergic reaction*

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9
Q

What is the allergic reaction in with Abacavir associated with?

A

HLA-B5707–must do genetic testing first!

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10
Q

What type of drug is Lamivudine?

A

Cytosine analog NRTI

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11
Q

What is unique about the toxicity associated with Lamivudine?

A

LEAST toxic of the antiretrovirals

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12
Q

What is the unique clinical utility associated with Lamivudine?

A

Safe in pregnancy

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13
Q

What type of drug is Emtricitabine?

A

Fluorinated analog of Lamivudine–NRTI

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14
Q

What specific adverse effect is associated with Emtricitabine?

A

Hyperpigmentation of the palms and soles

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15
Q

When is Emtricitabine contraindicated?

A

1) Young children
2) Pregnant women
3) Hepatic or renal failure

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16
Q

What type of drug is Tenofovir?

A

Nucleotide analog of adenosine–NRTI

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17
Q

How is Tenofovir administered?

A

Orally; however, not that is is normally given as “Tenofovir disoproxil” that has more oral bioavalibility

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18
Q

What adverse effects are associated with Tenofovir?

A

1) Bone marrow toxicity (Faconi anemia)

2) Decreased bone density and fetal growth

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19
Q

What type of drug is Zidovudine or AZT?

A

Deoxythymidine analog NRTI

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20
Q

What unique adverse effects are associated with Zidovudine?

A

Myelosuppression

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21
Q

What is the unique clinical indication for Zidovudine?

A

Post-exposure prophylaxis

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22
Q

What does NNRTI stand for?

A

Non-nucleoside Reverse Transcriptase Inhibitors

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23
Q

What is the MOA of the NNRTIs?

A

Binds to Reverse Transcriptase at a site OTHER THAN THE ACTIVE SITE and inhibits the enzyme

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24
Q

How do the NNRTIs compare to NRTIs?

A

NNRTIs do NOT require phosphorylation for activation

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25
Q

What strain of HIV are the NNRTIs NOT active against?

A

HIV-2

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26
Q

What adverse reactions are common to the NNRTIs?

A

1) Rash
2) Steven Johnson Syndrome
3) Hepatotoxicity
4) Major drug-drug interactions b/c of CYP450

27
Q

List the NNRTIs.

A

asdf

28
Q

What specific adverse effects are associated with Efavirnez?

A

1) Teratogenic
2) Adverse CNS effects
3) CYP 450 inducer

29
Q

When is Efavirnez contraindicated?

A

Pregnancy

30
Q

What specific toxicity is associated with Nevirapine?

A

Hepatitis

31
Q

What is unique about the clinical indications for Nevirapine?

A

Can be used to prevent VERTICAL transmission

32
Q

What is the MOA of the protease inhibitors in HIV therapy?

A

Block the protease necessary for maturation of virion proteins

33
Q

What adverse effects are associated with the Protease Inhibitors?

A

1) Hyperlipidemia
2) Iipodystrophy
3) Hepatotoxicity
4) GI intolerance
5) Increased bleeding risk
6) Drug-drug interactions via CYP p450

34
Q

List the Protease Inhibitors.

A

asdf

35
Q

What type of drug is contraindicated with Atazanavir?

A

PPIs–requires acid for absorption

36
Q

What major adverse effects are associated with Atazanavir?

A

1) Peripheral neuropathy
2) Hyperbilirubinemia
3) Adverse cardiac effects

37
Q

What effect does Atazanavir have on the CYP p450 enzymes?

A

Inhibition

38
Q

What is the effect of Ritonavir on liver metabolism?

A

Potent INHIBITOR or CYP p450 enzymes

39
Q

How is Ritonavir used clinically?

A

“Booster” to increase the half-life of co-administered drugs

40
Q

How is Darunavir administered?

A

Orally + pharmacokinetic enhancer e.g. Ritonavir

41
Q

What are the specific adverse effects seen with Darunavir?

A

1) Increased liver enzymes

2) Increased serum amylase

42
Q

What is Darunavir specifically good for treating?

A

Drug resistant HIV-1

43
Q

What is the MOA of the CCR5 Receptor Antagonists?

A

Blocks interaction of HIV (gp120) with the CCR5 co-receptor

44
Q

What drug is a CCR5 receptor antagonist?

A

Maraviroc

45
Q

What is the major toxicity associated with Maraviroc?

A

Increased cardiac events in those with underlying heart disease

46
Q

What is the mechanism of resistance to Maraviroc?

A

Change in HIV tropism i.e. switch from CCR5 to CXCR4 tropism

47
Q

What are the indications for Maraviroc?

A

HIV “experienced” patients with a tropsim for CCR5

48
Q

What is the mechanism of the Fusion Inhibitors?

A

Blockade of the gp41 fusion protein

49
Q

What is the Fusion inhibitor?

A

Enfurvirtide

50
Q

What is the only anti-viral that is given parenterally?

A

Enfurvirtide

*Given SubQ

51
Q

What are the adverse effects associated with Enfurvirtide?

A

1) Injection site reaction
2) Allergy to drug
3) Increased risk for bacterial pneumonia

52
Q

What is the clinical utility of Enfurvirtide?

A

HIV experienced patients with resistance

53
Q

What is the MOA of the Integrase Inhibitors?

A

Inhibit viral integration into the host genome

54
Q

List the Integrase Inhibitors.

A

Raltegravir
Elvitegravir
Dolutegravir

55
Q

What major toxicities are associated with Raltegravir?

A

1) Mypoathy

2) Rhabdomyolysis

56
Q

How is Elvitegravir administered?

A

Orally with a CYP p450 inhibitor e.g. ritonavir

57
Q

What specific adverse effect is associated with Elvitegravir ?

A

Elevated lipase enzymes

58
Q

What are the adverse effects associated with Dolutegravir?

A

1) Hypersensitivity reaction

2) Elevation of liver enzymes

59
Q

What is unique about Dolutegravir in terms of resistance?

A

Retains activity against strains that are resistant to other integrase inhibitors

60
Q

How much does a patient need to weigh to be given Dolutegravir?

A

At least 40 kg

61
Q

When do you initiate ARV therapy?

A

ALL HIV infected individuals

62
Q

At what point is there the strongest recommendation for ART initiation?

A

CD4+ T-cell count less than 350

63
Q

What is the standard of care for ART?

A

Combination of at LEAST 3 antiretroviral drugs/classes

64
Q

What is the preferred combination of ART for initial therapy?

A

1) Protease inhibitor (Ritonavir)
2) 2x NRTIs

OR

1) Integrase Inhibitor
2) 2x NRTIs

Pharmacology (64 decks)

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