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SBL > HIV Pharm > Flashcards

HIV Pharm Flashcards

1
Q

Maraviroc

A

MOA: inhibits viral entry via binding to CCR5
-oral administration
-CYP3A4
Resistance: mutations of V3 loop of gp120
Emergence of CXCR4 tropic virus
hepatotoxic

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2
Q

Enfuvirtide

A

MOA: inhibits viral fusion via binding to gp41 preventing conformational changes
*subQ injection
Resistance: mutations in Gp41
AE: HA, Dizziness, Nausea

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3
Q

NTRI (nucleotide/side reverse transcriptase inhibitor)

A

competitive inhibition on HIV reverse transcriptase
leads to premature chain termination due to inhibition of binding with incoming nucleotide

Resistance: mutations of HIV reverse transcriptase
Impaired kinase activity to prevent phosphorylation and activation

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4
Q

Nucleotide Reverse Transcriptase Inhibitor

A

Tenofovir

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5
Q

Nucleoside Reverse Transcriptase Inhibitor

A

Abacavir, Didanosine, Lamivudine, Emtricitabine, Stavudine, Zidovudine

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6
Q

Abacavir

A 
NsRTI
\+lamivudine
\+zidovudine
serum levels increased with ethanol ingestion due to metabolism via alcohol dehydrogenase
AE: HS and Skin Rash
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7
Q

Didanosine

A

NsRTI

  • *Dose dependent pancreatitis
  • *Retinal changes with optic neuritis
  • *Increased risk with lactic acidosis
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8
Q

Lamivudine

A

NsRTI

active against HIV and HBV

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9
Q

Emtricitabine

A

NsRTI
active against HIV and HBV
long intracellular half life
**hyperpigmentation of palms/soles esp in black people

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10
Q

Stavudine

A

NsRTI

  • *dose dependent peripheral sensory neuropathy
  • *Dyslipidemia
  • *Increased risk of lactic acidosis and hepatic steatosis with combined with didanosine
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11
Q

Zidovudine

A

NsRTI

  • **macrocytic anemia
  • **Neutropenia
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12
Q

Tenofovir

A

NtRTI
Active against HBV and HIV
AE: flatulance

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13
Q

NNRTIs

A

binds directly to HIV reverse transcriptase distant from active site

  • binding =conformational change in enzyme and reduced activity
  • non-competitive inhibitors

Resistance: HIV reverse transcriptase point mutations that alter NNRTI binding

CYP450: drug-drug interactions

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14
Q

Delavirdine

A

NNRTI
decreased potency compared to others
**skin rash
Increased aminotransferase levels

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15
Q

Efavirenz

A 
NNRTI
increased half life (once daily)
**CNS: dizziness, drowsiness, insomnia, nightmares, HA
**skin rash
\+tenofovir, emtricitabine,
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16
Q

Nevirapine

A

NNRTI

–> prevents transmission of HIV from mother to child

17
Q

Etravirine

A

NNRTI (2nd gen)

Rash, nausea, diarrhea

18
Q

Rilpivirine

A

NNRTI (2nd gen)

**high doses associated with QT prolongation

19
Q

INSTIS

A 
integrase strand transfer inhibitors
MOA: binds HIV integrase
inhibits strand transfer and prevents ligation of reverse transcribed DNA into chromosome of host cell
AE: headache and GI
(end in suffix-"gravir")
20
Q

INSTIs

A

Dolutegravir
Elvitegravir
Raltegravir

21
Q

Dolutegravir

A 
INSTI
treatment naive patients
\+ tenofovir, emtricitabine
\+abacavir, lamivudine
long half life
22
Q

Elvitegravir

A

INSTI
combination pill
requires boosting with cobicistat

23
Q

Raltegravir

A

INSTI

preferred for treatment naive patients

24
Q

Protease Inhibitors

A

blocks HIV protease and prevents maturation of final structural proteins to make viron core
-specifically inhibits HIV aspartyl protease

  • quick resistance if monotherapy
  • GI intolerance, Lipodystrophy (metabolic, morphologic)
  • **redistribution and accumulation of body fat
25
Q

CYP3A4 metabolism of Protease inhibitors

A

ritonavir has the most pronounced inhibitory effect

saquinavir has the least inhibitory effect

26
Q

Protease Inhibitors

A 
Atazanivir
Darunavir
Ritonavir (used as a booster)
Fosamprenavir
Indinavir
Lopinavir
Nelfinavir
Saquinavir
Tipranavir
27
Q

Atazanavir

A

PI
Once daily dosing
Skin rash

28
Q

Darunavir

A

PI
HS if sulfa allergy
+ritonavir
+cobicistat

29
Q

Fosamprenavir

A

PI
+ritonavir
HS if sulfa allergy

30
Q

Indinavir

A

PI
Unconjugated hperbillirubinemia, nephrolithiasis
drink lots of water

31
Q

Lopinavir

A

PI
+ritonavir
generally well tolerated

32
Q

Nelfinavir

A

PI

Diarrhea and flatulence

33
Q

Ritonavir

A

high rate GI side effects
CYP450 inhibitor
**primarily used as a booster

34
Q

Saquinavir

A

less GI effects if ritonavir used as a booster

35
Q

Tipranavir

A

indicated if resistant to other protease inhibitors
Urticarial or maculopapular rash**
HS rxn if sulfa allergy

36
Q

HAART

A

2 NTRI +

  • 1 protease inhibitor
  • 1 NNRTI
  • INSTI

MC: tenofovir+emtricitabine+others

SBL (1 decks)

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