Protease Inhibitors Flashcards

1
Q

What are the Protease Inhibitors

A
Ritonavir
Atazanavir
Indinavir
Nelfinavir
Fosamprenavir
Lopinavir
Saquinavir
Tirranavir
Darunavir
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2
Q

What does HIV aspartyl protease do

A

Cleaves HIV polyprotein into RT, protease and integrase

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3
Q

Do PIs need intracellular activation

A

No

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4
Q

What is the problem with the low protease bioavailability

A

Can be affected by high fat meals

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5
Q

What are Protease inhibitors substrates for

A

3A4

P-glycprotein

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6
Q

What are the general PI AE

A

Paresthesia

N/V/D

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7
Q

What are the main PI AE

A

Lipodystrophy - looks like cushings
Hyperglycemia and Insulin resistance
Crystal induced Nephropathy

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8
Q

Which PI has least AE

A

Atazanavir

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9
Q

PI interaction with statins

A

Rabdomyolysis

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10
Q

PI interaction with Midazolam

A

Excessive sedation

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11
Q

PI interaction with Fentanyl

A

Resp depression

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12
Q

What drugs are contraindicated with PI

A

Rifampin

St. John’s Wort

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13
Q

What is the main effect of Ritonavir

A

Enhancer of other PIs due to 3A4 inhibition

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14
Q

What are the only once-daily preferred PIs

A

Ritonavir + Atazanavir

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15
Q

What is a preferred PI that can causes insulin resistance

A

Lopinavir

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16
Q

Which PI can inhibit PPIs

A

Atazanavir

17
Q

What are the main Atazanavir AE

A

Jaundice

Increased PR interval

18
Q

Which PI cannot be boosted by Ritonavir

A

Nelfinavir

19
Q

Indinavir AE

A

Renal stones/Hematuria

Hyperbilirubinemia

20
Q

How do you control Nelfinavir diarrhea

A

Loperamide

21
Q

Major metabolite has equal anti-viral activity as parent

A

Nelfinavir

22
Q

Pro-drug with lots of contraindications

A

Fosamprenavir

23
Q

Oral solution contains EtOH

A

Lopinavir

24
Q

What should you avoid when on Lopinavir

A

Disulfiram
Metro
P450 inducers (St. John’s Wort)

25
Q

High fat meals enhance absorption

A

Saquinavir

26
Q

Saquinavir Contraindications

A

P450 inducers

27
Q

When is Tipranavir/Darunavir given

A

Resistant to other PIs

28
Q

Tipranavir AE

A

Fatal Hep

Intracranial Hemorrhages

29
Q

Effect of Tipranavir on P450

A

Inducer

30
Q

Inhibitor of 3A4

A

Darunavir

31
Q

Darunavir AE

A

Rash

32
Q

Can Darunavir be given with food

A

Yes