EXAM #4: ANTIRETROVIRALS Flashcards Preview

Pharmacology > EXAM #4: ANTIRETROVIRALS > Flashcards

Flashcards in EXAM #4: ANTIRETROVIRALS Deck (64):
1

What does NRTI stand for?

Nucelotide Reverse Transcriptase Inhibitor

2

List the NRTIs.

Zidovudine
Lamivudine
Abacavir
Tenofovir disoproxil
Emtricitabine

3

What is the MOA of the NRTIs?

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

4

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

Cellular kinases

5

What infection aside from HIV can be treated with NRTIs?

HBV

6

What are the adverse effects common to the NRTIs?

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

7

What is Abacavir?

Guanosine analog NRTI

8

What specific adverse effects are associated with Abacavir?

Allergic reaction

****Think "A" for allergic reaction*****

9

What is the allergic reaction in with Abacavir associated with?

HLA-B5707--must do genetic testing first!

10

What type of drug is Lamivudine?

Cytosine analog NRTI

11

What is unique about the toxicity associated with Lamivudine?

LEAST toxic of the antiretrovirals

12

What is the unique clinical utility associated with Lamivudine?

Safe in pregnancy

13

What type of drug is Emtricitabine?

Fluorinated analog of Lamivudine--NRTI

14

What specific adverse effect is associated with Emtricitabine?

Hyperpigmentation of the palms and soles

15

When is Emtricitabine contraindicated?

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

16

What type of drug is Tenofovir?

Nucleotide analog of adenosine--NRTI

17

How is Tenofovir administered?

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

18

What adverse effects are associated with Tenofovir?

1) Bone marrow toxicity (Faconi anemia)
2) Decreased bone density and fetal growth

19

What type of drug is Zidovudine or AZT?

Deoxythymidine analog NRTI

20

What unique adverse effects are associated with Zidovudine?

Myelosuppression

21

What is the unique clinical indication for Zidovudine?

Post-exposure prophylaxis

22

What does NNRTI stand for?

Non-nucleoside Reverse Transcriptase Inhibitors

23

What is the MOA of the NNRTIs?

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

24

How do the NNRTIs compare to NRTIs?

NNRTIs do NOT require phosphorylation for activation

25

What strain of HIV are the NNRTIs NOT active against?

HIV-2

26

What adverse reactions are common to the NNRTIs?

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

27

List the NNRTIs.

asdf

28

What specific adverse effects are associated with Efavirnez?

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

29

When is Efavirnez contraindicated?

Pregnancy

30

What specific toxicity is associated with Nevirapine?

Hepatitis

31

What is unique about the clinical indications for Nevirapine?

Can be used to prevent VERTICAL transmission

32

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

Block the protease necessary for maturation of virion proteins

33

What adverse effects are associated with the Protease Inhibitors?

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

34

List the Protease Inhibitors.

asdf

35

What type of drug is contraindicated with Atazanavir?

PPIs--requires acid for absorption

36

What major adverse effects are associated with Atazanavir?

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

37

What effect does Atazanavir have on the CYP p450 enzymes?

Inhibition

38

What is the effect of Ritonavir on liver metabolism?

Potent INHIBITOR or CYP p450 enzymes

39

How is Ritonavir used clinically?

"Booster" to increase the half-life of co-administered drugs

40

How is Darunavir administered?

Orally + pharmacokinetic enhancer e.g. Ritonavir

41

What are the specific adverse effects seen with Darunavir?

1) Increased liver enzymes
2) Increased serum amylase

42

What is Darunavir specifically good for treating?

Drug resistant HIV-1

43

What is the MOA of the CCR5 Receptor Antagonists?

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

44

What drug is a CCR5 receptor antagonist?

Maraviroc

45

What is the major toxicity associated with Maraviroc?

Increased cardiac events in those with underlying heart disease

46

What is the mechanism of resistance to Maraviroc?

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

47

What are the indications for Maraviroc?

HIV "experienced" patients with a tropsim for CCR5

48

What is the mechanism of the Fusion Inhibitors?

Blockade of the gp41 fusion protein

49

What is the Fusion inhibitor?

Enfurvirtide

50

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

Enfurvirtide

*Given SubQ

51

What are the adverse effects associated with Enfurvirtide?

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

52

What is the clinical utility of Enfurvirtide?

HIV experienced patients with resistance

53

What is the MOA of the Integrase Inhibitors?

Inhibit viral integration into the host genome

54

List the Integrase Inhibitors.

Raltegravir
Elvitegravir
Dolutegravir

55

What major toxicities are associated with Raltegravir?

1) Mypoathy
2) Rhabdomyolysis

56

How is Elvitegravir administered?

Orally with a CYP p450 inhibitor e.g. ritonavir

57

What specific adverse effect is associated with Elvitegravir ?

Elevated lipase enzymes

58

What are the adverse effects associated with Dolutegravir?

1) Hypersensitivity reaction
2) Elevation of liver enzymes

59

What is unique about Dolutegravir in terms of resistance?

Retains activity against strains that are resistant to other integrase inhibitors

60

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

At least 40 kg

61

When do you initiate ARV therapy?

ALL HIV infected individuals

62

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

CD4+ T-cell count less than 350

63

What is the standard of care for ART?

Combination of at LEAST 3 antiretroviral drugs/classes

64

What is the preferred combination of ART for initial therapy?

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

OR

1) Integrase Inhibitor
2) 2x NRTIs

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