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Flashcards in Antiretrovirals Deck (67)
1

NRTI's

Zidovudine, Zalcitabine, Diadanosine, Stavudine, Abacavir, tenofovir, Lamivudien, emcitabine

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NRTI's MOA

substrate for RT, lack 3'OH group can't elongate RNA

3

NRTI's- what cells does it work in

Newly infected cells

4

NRTI- HIV1, 2 or both

Both

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What is given to mother to prevent spread of HIV during child birth

NRIT

6

NRTI- AE

Lactic Acidosis (mtDNA interference), hepatic steatosis, N/V/D, fatigue, insomnia drugs with a d cause reversible, dose dependent peripheral neuropath

7

Zidovudine- abrev

AZT

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Zidovudine- AE

Bone marrow suppression, malaise, myopathies, N/V, HA

9

Zidovudine- Contraindications

Don't give to people with Ganciclovir, used to tx CMV

10

Zalcitabine- abrev

ddC

11

Zalcitabine- AE

peripheral neuropathy, pancreatitis

12

Didanosine- Abrev

ddl

13

Didanosine- AE

Pancreatitis- deadly Peripheral neuritis is common

14

Didanosine- meals

Do not take with meals, acid will destroy the drug

15

Stavudine- Abrev

d4t

16

Stavudine- AE

lipodystrophy- prevrent with pravastatin and atrovastatin peripheral nueropathy

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Abacavir- abrev

ABC

18

Abacavir- AE

hypersensitivity rxn- deadly

19

Tenofovir- AE

nephrotoxic

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Lamivudine, emtricitabine- AE

minimal toxicity, GI, HA

21

Emtricitabine- abrev

FTC

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NRTI- MOR

3-4 AA mutations

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NNRTI's

Nevirapine, delavirdine, enfavirenz, etravirine, rilpirivine

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NNRTI- MOA

non competitive antagonist of RT

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NNRTI- new or old cells?

New

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NNRTI- HIV1, 2, or both

HIV 1

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NNRTI- AE

Rash, hepatotoxicity

28

NNRTI- MOR

1 codon change- very common

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NNRTI- T1/2

long

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NNRTI- protein binding

high

31

NNRTI- metabolism

in the liver and high

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Nevirapine- effect on CYP450

Inducer

33

Delvaridine- effect on CYP450

Inhibitor

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Efavirenz- AE

Abnormal CNS effects- vivid dreams, insomnia, dizziness

35

Effavirenz- Food

don't take with fatty meals

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Efavirenz- Contraindications

Pregnancy

37

Etravirine- - use

last line, NNRTI is have developed resistance to all the others

38

Riplirivine- AE

Severe rash, GI

39

Protease inhibitors

Indinavir, atazanavir, tipranavir, fosamprenavir, lopinavir, nelfinavir, ritonavir, saquinavir

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PI- MOA

binds to active site of protease --> cant cleave the polyprotein

41

PI- new, old, both

both

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PI- AE

hyperglycemia, dyslipidemia, lipodystrophy, osteoperosis, GI disturbances, redistribution of fat from face and extremities to waist

43

PI- resistance

4-5 Codon mutation

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PI- lymphodystrophy

redistribution of fat from face and extremities to waist, HIV lymphodystrophy syndrome. Tx atrovastatin, provastatin

45

PI- liver enzymes

inhibitors or CYP3A4 --> lots of drug interactions

46

PI- metabolism

hepatic

47

PI- protein binding

high

48

PI- excretion

renal

49

PI- order of CYP3A4 interactions

Ritonavir- greatest squinavir- least

50

Indinavir- AE

Kidney stones, hyperbillirubinemia, alopecia

51

Atazanavir- AE

prolonged PR- messes up atria hyperbiirubinemia

52

Tipranavir-AE

Intracranial hemorrhage

53

Ritonavir- AE

largest inhibitor of CYP3A4 enzyme --> inhibits metabolism of other HIV drugs, so saves $

54

Fusion inhibitor

Enfuviritide- Fuzeon

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Enfuviritide- MOA

binds to gp41 env protein and prevents fusion of HIV to cell

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Enfuviritide- resistance

1 codon change, low barrier

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Enfuviritide- HIV1,2, both

HIV1

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Enfuviritide- usees

last ditch when all other drugs have failed

59

Enfuviritide- AE

Injection site rxns, N/D, fatigue, Neutropenia

60

Enfuviritide- admin

subcutaneous injection

61

Enfuviritide- protein binding

92%

62

Enfuviritide- metabolism

Proteloytic degridation, not hepatic metabolism

63

Agents for MDR HIV

Maraviroc, Raltegavir, Etravirine

64

Maraviroc- MOA

binds to CCR5, CCR5 antagonists, HIV can't bind

65

Maraviroc- AE

Major hepatotoxicity

66

Raltegavir- MOA

integrase inhibitor

67

Etravirine- uses

really an NNRTI that is used when other drugs have failed