Antiretrovirals Flashcards

1
Q

NRTI’s

A

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

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2
Q

NRTI’s MOA

A

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

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3
Q

NRTI’s- what cells does it work in

A

Newly infected cells

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4
Q

NRTI- HIV1, 2 or both

A

Both

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5
Q

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

A

NRIT

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6
Q

NRTI- AE

A

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

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7
Q

Zidovudine- abrev

A

AZT

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8
Q

Zidovudine- AE

A

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

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9
Q

Zidovudine- Contraindications

A

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

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10
Q

Zalcitabine- abrev

A

ddC

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11
Q

Zalcitabine- AE

A

peripheral neuropathy, pancreatitis

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12
Q

Didanosine- Abrev

A

ddl

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13
Q

Didanosine- AE

A

Pancreatitis- deadly Peripheral neuritis is common

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14
Q

Didanosine- meals

A

Do not take with meals, acid will destroy the drug

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15
Q

Stavudine- Abrev

A

d4t

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16
Q

Stavudine- AE

A

lipodystrophy- prevrent with pravastatin and atrovastatin peripheral nueropathy

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17
Q

Abacavir- abrev

A

ABC

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18
Q

Abacavir- AE

A

hypersensitivity rxn- deadly

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19
Q

Tenofovir- AE

A

nephrotoxic

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20
Q

Lamivudine, emtricitabine- AE

A

minimal toxicity, GI, HA

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21
Q

Emtricitabine- abrev

A

FTC

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22
Q

NRTI- MOR

A

3-4 AA mutations

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23
Q

NNRTI’s

A

Nevirapine, delavirdine, enfavirenz, etravirine, rilpirivine

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24
Q

NNRTI- MOA

A

non competitive antagonist of RT

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25
Q

NNRTI- new or old cells?

A

New

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26
Q

NNRTI- HIV1, 2, or both

A

HIV 1

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27
Q

NNRTI- AE

A

Rash, hepatotoxicity

28
Q

NNRTI- MOR

A

1 codon change- very common

29
Q

NNRTI- T1/2

A

long

30
Q

NNRTI- protein binding

A

high

31
Q

NNRTI- metabolism

A

in the liver and high

32
Q

Nevirapine- effect on CYP450

A

Inducer

33
Q

Delvaridine- effect on CYP450

A

Inhibitor

34
Q

Efavirenz- AE

A

Abnormal CNS effects- vivid dreams, insomnia, dizziness

35
Q

Effavirenz- Food

A

don’t take with fatty meals

36
Q

Efavirenz- Contraindications

A

Pregnancy

37
Q

Etravirine- - use

A

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

38
Q

Riplirivine- AE

A

Severe rash, GI

39
Q

Protease inhibitors

A

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

40
Q

PI- MOA

A

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

41
Q

PI- new, old, both

A

both

42
Q

PI- AE

A

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

43
Q

PI- resistance

A

4-5 Codon mutation

44
Q

PI- lymphodystrophy

A

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

45
Q

PI- liver enzymes

A

inhibitors or CYP3A4 –> lots of drug interactions

46
Q

PI- metabolism

A

hepatic

47
Q

PI- protein binding

A

high

48
Q

PI- excretion

A

renal

49
Q

PI- order of CYP3A4 interactions

A

Ritonavir- greatest squinavir- least

50
Q

Indinavir- AE

A

Kidney stones, hyperbillirubinemia, alopecia

51
Q

Atazanavir- AE

A

prolonged PR- messes up atria hyperbiirubinemia

52
Q

Tipranavir-AE

A

Intracranial hemorrhage

53
Q

Ritonavir- AE

A

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

54
Q

Fusion inhibitor

A

Enfuviritide- Fuzeon

55
Q

Enfuviritide- MOA

A

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

56
Q

Enfuviritide- resistance

A

1 codon change, low barrier

57
Q

Enfuviritide- HIV1,2, both

A

HIV1

58
Q

Enfuviritide- usees

A

last ditch when all other drugs have failed

59
Q

Enfuviritide- AE

A

Injection site rxns, N/D, fatigue, Neutropenia

60
Q

Enfuviritide- admin

A

subcutaneous injection

61
Q

Enfuviritide- protein binding

A

92%

62
Q

Enfuviritide- metabolism

A

Proteloytic degridation, not hepatic metabolism

63
Q

Agents for MDR HIV

A

Maraviroc, Raltegavir, Etravirine

64
Q

Maraviroc- MOA

A

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

65
Q

Maraviroc- AE

A

Major hepatotoxicity

66
Q

Raltegavir- MOA

A

integrase inhibitor

67
Q

Etravirine- uses

A

really an NNRTI that is used when other drugs have failed