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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
Caution of zidovudine use
other myelosuppressives: ganciclovir, ribavirin
26
Side effects of tenofovir/emtricitabine
Flatulence
27
Lamivudine use
good for HIV/HBV coinfected individuals Monotherapy in HBV
28
Toxicity of Lamivudine
well tolerates: H/A, fatique, insomnia, GI; safe in pregnancy
29
Abacavir use
(+) lamivudine or zidovidine
30
Toxicity of abacavir
HYPERSENSITIVITY: test for HLA-B-5701 prior to tx. Nausea, vomiting, diarrhea
31
Hypersensitivity reaction
fever, malaise, skin rash, chills, sore throat, dysnpea
32
Side effects of all NRTI's
lactic acidosis & hepatotoxicity; more likely if pt. is obese, previous liver disease or takes drugs for long time
33
DOC for NNRTI's
Efavirenz
34
Toxicity of Efavrienz
induces CYP3A4: decrease effectiveness of BC or methadone | Teratogenic- DON"T USE IN PREGNANCY (substitute w/ rilpivirine)
35
Potent CYP3A4
Rifampin- inducer Ketoconazole - p450 inhibitor Efavirenz- CYP3A4 inducer
36
Rilpivirine use
replaces efavirenz in pregnant patients for NNRTIs
37
Side effects of rilpivirin
depression, increased cholesterol, H/A
38
Not recommended to use rilpivirin
hepatitis co-infection (may increase liver enzymes)
39
PI's
``` Ritonavir (boost) Darunavir Atazanavir Saquinavir Lopinavir/ritonavir Indinavir Tipranavir ```
40
-avir
Protease inhibitor (exceptions: abacavir (NRTI) and dulutegravir (integrase inhibitor))
41
Common kinetics of PI
oral combine with NRTI's metabolized by CYP3A4 -often given w/ ritonivir to inhibit CYP3A4 and increase PI levels
42
Drug interactions of PI
Drugs which induce CYP3A$ will decrease PI levels (rifampin, rifabutin, phenytoin, carbamazepine, phenobarbitol) St. John's Work: increases metabolism of PIs
43
Common toxicities of PI
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
Ritonavir use
booster: inhibits CYP3A4 - allows less frequent dosing and greater antiviral activity
45
Side effects of Ritonavir
GI Burning, tingling and elevated liver enzymes, nausea Contains ethanol: don't combine with metronidazole or cephalosporins
46
Don't use ritonavir with
Saquinavir (QT)
47
DOC for PI's
Darunavir
48
Side effects of darunavir
Rash, nausea, diarrhea, H/A, bad dreams
49
Contra for darunavir
Sulfa allergy (use Atazenavir instead)
50
2nd DOC for PI
atazenavir
51
Dosing for Atazenavir
once/day
52
Side effects of Atazenavir
less effect on body fat distribution May increase bilirubin (inhibits UGT) Diarrhea, rash and nausea is common (maybe hyperglycemia)
53
Saquinavir use
alternate PI
54
Side effects of saquinavir
QT (don't use with ritonavir) | GI
55
Saquinavir kinetics
low bioavailability- take with high-fat food or grapefruit juice to increase (inhibit P450)
56
Lopinavir/ritonavir side effect
diarrhea with nausea; liver enzymes may be elevated if there is pre-existing hepatic disease
57
Indinavir kinetics
cross-resistance with ritonavir
58
Side effects of indinavir
nephrolithiasis and hyperbilirubinemia (HYDRATE!!!)
59
Tipranavir use
tx-experienced resistant patients
60
Side effects of tipranavir
Intracranial hemorrhage when used with ritonavir in head injury Sulfa GI Liver toxicity - more common in HBV/HCV coinfected
61
Fusion inhibitors
Enfuviritide | Maraviroc
62
MOA of enfuviritide
binds gp41 on viral envelope and prevents conformational change required for fusion
63
Use of enfuviritide
tx-experienced resistant patients
64
Enfuviritide kinetics
SUBCUTANEOUS INJECTION no cross-resistance w/ other antiretroviral agents well tolerated Increases likelihood of bacterial pneumonia
65
Increased liklihood of bacterial pneumoniae
Enfuviritide
66
Flatulence
Tenofovir/emtricatabine
67
Depression
Rilpivirin
68
Hypersensitivity
abacavir
69
QT
saquinavir (+ ritonavir)
70
Myelosuppression
Zidovudine
71
Nephrolithiasis
Indinavir
72
Maraviroc MOA
binds CCR5 receptor of the CD4 T-cell and inhibits fusion
73
Side effect of maraviroc
rash
74
Don't use maraviron
CXCR4 or mixed tropism
75
Integrase inhibitor
Dolutegravir
76
Dolutegravir use
tx-experience resistance
77
Side effects of dolutegravir
H/A and insomnia
78
Used during tx-experience resistant individuals
Tipranovir (PI) Enfuviritide (FI) Maraviroc (FI) Dolutegravir (II)

Pharm Final (6 decks)

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