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Pharm Final > HIV > Flashcards

HIV Flashcards

1
Q

HIV process

A

free virus binds to CD4 molecule and one of two coreceptors (CCR5 or CXCR4) on cell surface, virus fuses with cell –> contents empty into cell –> RT converts RNA to DNA –> Integrate incorporates viral DNA into cell DNA –> Transcription –> assembly of proteins –> budding –> breaks free of infected cell –> Maturation: protease cuts HIV protein into functional proteins

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2
Q

NRTIS

A

Zidovudine
Tenofovir & emtricitabine
Lamivudine
Abacovir

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3
Q

NNRTI’s

A

Rilpivirine

Efavirenz

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4
Q

PI

A 
Ritonavir (booster)
Darunivir
Atezanivir
Saquinivir
Lopinavir/Ritonivir
Indinavir
Tipranovir
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5
Q

Fusion inhibitors

A

enfuvirtide

maraviroc

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6
Q

Integrage inhibitor

A

Dulutegravir

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7
Q

Only parenteral (SC) HIV drug

A

Enfuvirtide (Fuzeon)

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8
Q

Zidovudine MOA

A

thymidine analog - NRTIs

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9
Q

Tenovovir/emtricitabine MOA

A

T: adenosine
E: Cytosine

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10
Q

Abacavir MOA

A

guanisine analog

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11
Q

Non-peptide PI

A

Tipranovir

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12
Q

How do NNRTI’s work

A

bind directly to RT and inhibit - phosphorylation not needed

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13
Q

Phosphorylation of NRTI’s

A

done by the host - resistance is not due to enzyme mutation for phosphorylation

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14
Q

DOC for HIV dimentia

A

Zidovudine

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15
Q

DOC for HIV - 1st line

A

Tenofovir/Emtricitabine (don’t give with Lamivudine, same MOA)

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16
Q

DOC of NNRTIs

A

Efavirenz

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17
Q

Contra of efavirenz

A

pregnancy!!!! - teratogenic

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18
Q

When is rilpivirine used

A

substitutde for efavirenz in pregnant women

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19
Q

Abacavir contraindication

A

HLA-B-5701 (SCREEN!)

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20
Q

Sulfa HIV drugs

A

Darunivir, Tipranivir (Don’t Take)

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21
Q

first choice HIV therapy

A

Emtircitabine and tenofovir

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22
Q

Alternative HIV therapy

A

lamivudine

Abacavir

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23
Q

CNS penetration

A

Zidovudine

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24
Q

Toxicity of Zidovudine

A

CNS: H/A, Nausea, vomiting, insomnia, myalgia
Lactic acidosis and hepatotoxicity
Myelosuppression (treat w/ epogen, neupogen)

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25
Q

Caution of zidovudine use

A

other myelosuppressives: ganciclovir, ribavirin

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26
Q

Side effects of tenofovir/emtricitabine

A

Flatulence

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27
Q

Lamivudine use

A

good for HIV/HBV coinfected individuals

Monotherapy in HBV

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28
Q

Toxicity of Lamivudine

A

well tolerates: H/A, fatique, insomnia, GI; safe in pregnancy

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29
Q

Abacavir use

A

(+) lamivudine or zidovidine

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30
Q

Toxicity of abacavir

A

HYPERSENSITIVITY: test for HLA-B-5701 prior to tx.

Nausea, vomiting, diarrhea

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31
Q

Hypersensitivity reaction

A

fever, malaise, skin rash, chills, sore throat, dysnpea

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32
Q

Side effects of all NRTI’s

A

lactic acidosis & hepatotoxicity;

more likely if pt. is obese, previous liver disease or takes drugs for long time

33
Q

DOC for NNRTI’s

A

Efavirenz

34
Q

Toxicity of Efavrienz

A

induces CYP3A4: decrease effectiveness of BC or methadone

Teratogenic- DON”T USE IN PREGNANCY (substitute w/ rilpivirine)

35
Q

Potent CYP3A4

A

Rifampin- inducer
Ketoconazole - p450 inhibitor
Efavirenz- CYP3A4 inducer

36
Q

Rilpivirine use

A

replaces efavirenz in pregnant patients for NNRTIs

37
Q

Side effects of rilpivirin

A

depression, increased cholesterol, H/A

38
Q

Not recommended to use rilpivirin

A

hepatitis co-infection (may increase liver enzymes)

39
Q

PI’s

A 
Ritonavir (boost)
Darunavir
Atazanavir
Saquinavir
Lopinavir/ritonavir
Indinavir
Tipranavir
40
Q

-avir

A

Protease inhibitor (exceptions: abacavir (NRTI) and dulutegravir (integrase inhibitor))

41
Q

Common kinetics of PI

A

oral
combine with NRTI’s
metabolized by CYP3A4 -often given w/ ritonivir to inhibit CYP3A4 and increase PI levels

42
Q

Drug interactions of PI

A

Drugs which induce CYP3A$ will decrease PI levels (rifampin, rifabutin, phenytoin, carbamazepine, phenobarbitol)
St. John’s Work: increases metabolism of PIs

43
Q

Common toxicities of PI

A

altered body fat (buffalo hump and truncal obesity, facial and peripheral atroph)

Insulin resistance and hyperglycemia

Increase serum cholesterol: don’t combine with statins

Spontaneous bleeding in hemophilia A/B patient’s

44
Q

Ritonavir use

A

booster: inhibits CYP3A4 - allows less frequent dosing and greater antiviral activity

45
Q

Side effects of Ritonavir

A

GI
Burning, tingling and elevated liver enzymes, nausea
Contains ethanol: don’t combine with metronidazole or cephalosporins

46
Q

Don’t use ritonavir with

A

Saquinavir (QT)

47
Q

DOC for PI’s

A

Darunavir

48
Q

Side effects of darunavir

A

Rash, nausea, diarrhea, H/A, bad dreams

49
Q

Contra for darunavir

A

Sulfa allergy (use Atazenavir instead)

50
Q

2nd DOC for PI

A

atazenavir

51
Q

Dosing for Atazenavir

A

once/day

52
Q

Side effects of Atazenavir

A

less effect on body fat distribution
May increase bilirubin (inhibits UGT)
Diarrhea, rash and nausea is common (maybe hyperglycemia)

53
Q

Saquinavir use

A

alternate PI

54
Q

Side effects of saquinavir

A

QT (don’t use with ritonavir)

GI

55
Q

Saquinavir kinetics

A

low bioavailability- take with high-fat food or grapefruit juice to increase (inhibit P450)

56
Q

Lopinavir/ritonavir side effect

A

diarrhea with nausea; liver enzymes may be elevated if there is pre-existing hepatic disease

57
Q

Indinavir kinetics

A

cross-resistance with ritonavir

58
Q

Side effects of indinavir

A

nephrolithiasis and hyperbilirubinemia (HYDRATE!!!)

59
Q

Tipranavir use

A

tx-experienced resistant patients

60
Q

Side effects of tipranavir

A

Intracranial hemorrhage when used with ritonavir in head injury

Sulfa
GI
Liver toxicity - more common in HBV/HCV coinfected

61
Q

Fusion inhibitors

A

Enfuviritide

Maraviroc

62
Q

MOA of enfuviritide

A

binds gp41 on viral envelope and prevents conformational change required for fusion

63
Q

Use of enfuviritide

A

tx-experienced resistant patients

64
Q

Enfuviritide kinetics

A

SUBCUTANEOUS INJECTION
no cross-resistance w/ other antiretroviral agents
well tolerated
Increases likelihood of bacterial pneumonia

65
Q

Increased liklihood of bacterial pneumoniae

A

Enfuviritide

66
Q

Flatulence

A

Tenofovir/emtricatabine

67
Q

Depression

A

Rilpivirin

68
Q

Hypersensitivity

A

abacavir

69
Q

QT

A

saquinavir (+ ritonavir)

70
Q

Myelosuppression

A

Zidovudine

71
Q

Nephrolithiasis

A

Indinavir

72
Q

Maraviroc MOA

A

binds CCR5 receptor of the CD4 T-cell and inhibits fusion

73
Q

Side effect of maraviroc

A

rash

74
Q

Don’t use maraviron

A

CXCR4 or mixed tropism

75
Q

Integrase inhibitor

A

Dolutegravir

76
Q

Dolutegravir use

A

tx-experience resistance

77
Q

Side effects of dolutegravir

A

H/A and insomnia

78
Q

Used during tx-experience resistant individuals

A

Tipranovir (PI)
Enfuviritide (FI)
Maraviroc (FI)
Dolutegravir (II)

Pharm Final (6 decks)

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