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PHARM 2 > Anti-retrovirals > Flashcards

Anti-retrovirals Flashcards

1
Q

abacavir

A

NRTI

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2
Q

didanosine

A

NRTI

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3
Q

emtricitabine

A

NRTI

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4
Q

lamivudine

A

NRTI

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5
Q

stavudine

A

NRTI

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6
Q

tenofovir

A

NRTI

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7
Q

zidovudine

A

NRTI

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8
Q

efavirenz

A

NNRTI

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9
Q

nevirapine

A

NNRTI

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10
Q

rilpivirine

A

NNRTI

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11
Q

atazanavir

A

protease inhib

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12
Q

darunavir

A

protease inhib

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13
Q

indinavir

A

protease inhib

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14
Q

lopinavir

A

protease inhib

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15
Q

nelfinavir

A

protease inhib

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16
Q

enfuviritide

A

entry inhibitor

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17
Q

maraviroc

A

entry inhibitor

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18
Q

dolutegravir

A

integrase inhib

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19
Q

elvitegravir

A

integrase inhib

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20
Q

raltegravir

A

integrase inhib

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21
Q

cobicistat

A

pharmacokinetic enhancers

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22
Q

ritonavir

A

pharmacokinetic enhancer

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23
Q

NRTI MOA

A

riboside analog - lacking 3’ OH

phosphorylated by cell enzymes, incorp into viral DNA = terminates DNA elongation

COMPETITIVE INHIB of RT

active against HIV-1 and 2

(1 - western world. 2 - west africa)

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24
Q

NRTI resistance

A

rapidly emerges if used alone

most common mutation at viral codon 184 - lamivudine; can inc sensitivity to zidovudine and tenofovoir

cross resistance does occur

dose changes with renal insufficiency

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25
Q

NRTI AE

A

inhib mitochondrial DNA pol = periph neuropathy, myopathy, lipoatrophy, lactic acidosis

pancreatitis
myelosuppression
fatal liver toxicity - rare

zidovudine and stavudine = dyslipidemia, insulin resistance

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26
Q

NRTI interactions

A

didanosine and tenofovir: tenofovir inc didanosine levels (must reduce didanosine levels)

not metabolized by cytochrome enzymes

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27
Q

zidovudine

A

thymidine analog
(ZDV, AZT)

oral
crosses BBB
dosage adj in cirrhosis

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28
Q

zidovudine AE

A

BM suppression

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29
Q

ganciclovir + zidovudine

A

BOTH CAUSE BM SUPPRESSION - don’t give together

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30
Q

zidovudine contraindications

A

coadmin with acetaminophen, lorazepam, indomethacin, cimetidine

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31
Q

Stavudine

A

(d4T)

inhibitor of beta and gamma DNA polymerases (high aff for mitochondrial DNA pol)

thymidine analog

oral

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32
Q

stavudine AE

A

peripheral neuropathy
lactic acidosis
hyperlipidemia
NM weakness

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33
Q

Didanosine

A

adenosine analog

best if taken in fasting state - acid labile
penetrates CSF

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34
Q

Didanosine AE

A

PANCREATITIS

peripheral neuropathy, diarrhea, hepatic dysfunction, CNS effects

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35
Q

Tenofovoir

A

(TDF)

adenosine nucleotide analog

combos: tenofovir + emtricitabine AND tenofovir + emtricitabine + efavirenz

36
Q

tenofovir PK

A

take with food to inc bioavail

long t 1/2

37
Q

only NRTI with significant drug interaction

A

tenofovir + didanosine

Tenofovir decreases concentrations of atazanavir

Can boost atazanavir with ritonavir

38
Q

Lamivudine

A

(3TC)
no affect on mitochondrial DNA or BM

cytosine nucleoside analog

39
Q

emtricitabine

A

relative of lamivudine

cytosine nucleoside analg

40
Q

emtricitabine AE

A

hyperpigmentation - more frequently in darker skinned

41
Q

abacavir

A

guanosine nucleoside analog

42
Q

abacavir AE

A

GI, HA

5% hypersensitivity reaction - rash, GI, malaise, respiratory distress

CONTRAINDIC in HLA-B 5701 mutation

don’t ever rechallenge sensitized individuals

43
Q

NNRTI MOA

A

selectively, noncomp inhibitor of HIV-1 RT

don’t bind at active site

inhibit RNA and DNA dep DNA pol

NO phosphorylation by cellular enzymes

no activity against HIV-2

44
Q

NNRTI adv/disadv

A

no cross resistance, effect on host blood forming elements

cross ressistance within NNRTI’s. drug interactions. high incidence of hypersensitivty

45
Q

NNRTI’s AE

A

skin rash – stevens johnson syndrome

CYP3A4 substrates: can act as inducers, inhibitors, or both of CYP

46
Q

Nevirapine excretion

A

urine - CYP3A4, 2B6

47
Q

nevirapine AE

A

hepatotoxicity (severe)
- don’t use unless have to

rash

titration period for 14 days at 1/2 dose to dec risk of serious epidermal reactions

48
Q

nevirapine PK

A

CYP3A4 inducer

increases metab of PI’s , OCP, ketoconazole, methoadone, metronidazole, quinidne, theophylline, warfarin

49
Q

efavirenz

A

increases CD4+ counts, dec viral load

oral

40 hr half life

P450 inducer

50
Q

efavirenz AE

A

high rate of CNS toxicity

rash

inc TG, HDL, cholest (must monitor lipids)

contraindcated in pregnancy - but can be used after 1st trimerster

51
Q

Rilpivirine AE

A

**Rash

insomina, depression

LFTs increased

52
Q

Protease inhibitor MOA

A

reversible inhib of HIV aspartyl protease = prevents viral maturation and production of non-infectious virions

NO intracellualr activ required

active against HIV-1 and 2

53
Q

Protease inhib PK

A

poor oral bioavail -
high fat inc = nelfinavir
high fat dec = indinavir

substrate for CYP3A4
substrate for P glycoprotein pump

bound to plasma proteins = dec amt of free drug available to pt (alpha1-acid glycoprotein)

54
Q

protease inhib AE

A

parathesias, n/v/d

disturbances in lipid metab

fat redistribution and accum: central obesity, dorsocervical fat enlargement - buffalo hump, peripheral wasting; cushingoid appearance –> AE decreases compliance

55
Q

protease inhib contraindic

A

CYP inhibitors
- rhabdo (simvastain), excess sedation (midzolam), respiratory depression (fentanyl)

warfarin, sildenafil, phenytoin - require dosage adj

contraindic with rifampin and st john’s wort

56
Q

PI resistance

A

stepwise mutations of protease gene

57
Q

atazanavir AE

A

PR interval prolongation
benign hyperbilirubinemia
rash
nephrolithiasis

58
Q

Which protease inhib is NOT given with RTV

A

Nelfinavir

b/c metabolized by several CYPs

59
Q

Enfuviritide

A

(T-20)
inhibits viral fusion

“Tx-experienced pt with evidence of HIV replication”

No activity against HIV-2

60
Q

enfuviratide MOA

A

gp41 structural analog

binds gp41 - prevent ability of virion to fuse to cell membrane

61
Q

enfuvirataide contraindications

A

NO drug interactions with other retrovirals

62
Q

Maraviroc MOA

A

binds only CCR5 - blocking HIV entry

63
Q

maraviroc PK

A

CYP3A4 metabolized

64
Q

Integrase strand transfer inhibitor

A

approved for tx experienced and tx naive

65
Q

INSTI MOA

A

binds integrase

inhibits final step of integration of viral DNA into host cell DNA

66
Q

INSTI’s AE

A

rash, nausea, diarrhea, insomnia, HA

inc in creatine phosphokinases, myopathy, rhabdo, hypersensitivity

67
Q

Dolutegravir

A

eliminated via glucronidation via UGT1A1

68
Q

Elvitegravir

A

CYP3A4 metabolized - may require enhancer (Cobicistat)

69
Q

Raltegravir

A

eliminiated by glucoronidation by UGT1A1

70
Q

raltegravir AE

A

can cause increases in creatine phosphokinases

71
Q

raltegravir interactions

A

rifampin
tipranavir
efavirenz
= may dec raltegravir

PPI can increase raltegravir

72
Q

ritonavir

A

PK enhancer

73
Q

cobicistat

A

PK enhancer

74
Q

PK enhancer MOA

A

CYP3A4 inhibitor

Inc plasma concen of ARV = allows for lower and/or less frequent dosing

improves tolerability of ARV

75
Q

Ritonavir use

A

in combo with PI’s (not nelfinavir)

NEVER USED ALONE

76
Q

what drug is ritonavir never used with?

A

nelfinavir

77
Q

cobicistat use

A

combo with INSTI - elvitegravir, also with darunavir and atazanavir

78
Q

Initial Tx for Treatment-naive pt

A

2x NRTI + INSTI
OR

2x NRTI + PI

avoid use of 2 agents of same nucleotide analog, overlapping toxicity

79
Q

INSTI based regiments

A

1) Raltegravir + tenofovir + emtricitabine

2) Dolutegravir + tenofovir + emtricitabine

80
Q

PI based regiment

A

Ritonavir boosted with darunavir + tenofovir + emtricitabine

81
Q

HIV prophylaxis following needle stick

A

raltegravir + tenofovir + emtricitabine (x28 days)

82
Q

HIV prophylactic vaccines

A

S. pneumo
HAV
HBV
Influenza

83
Q

Vaccines contraindic in HIV pt with CD4 <200

A

LIVE VACCINES:
MMR
Varicella
Zoster

84
Q

darunavir

A

inhibits CYP3A4

avoid in pt with sulfur allergy

85
Q

indinavir

A

give with RTV
absorption dec with meals

nephrolithiasis
hyperbili
blurred vision

86
Q

lopinavir

A

give with RTV

contraindic with inducers (St. Johns wort)

Avoid with disulfiram or metronidazole - contains EtOH

87
Q

nelfinavir

A

lots of contraindications b/c CYP inhibition

PHARM 2 (18 decks)

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