Anti-HIV Drugs Flashcards Preview

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Flashcards in Anti-HIV Drugs Deck (33):
1

Abacavir

- NRTI
- metabolized by alcohol dehydrogenase; alcoholics will occupy ADH with EtOH and drug will build up toxically
- "LAD ZEST"

2

Lamivudine

- NRTI
- "LAD ZEST"

3

Tenofovir-Disproxyl

- NRTI
- "LAD ZEST"

4

Emtricitabine

- NRTI
- "LAD ZEST"

5

Didanosine

- NRTI
- Neuropathy (2nd worst)
- "LAD ZEST"

6

Stavudine

- NRTI
- Neuropathy (worst)
- "LAD ZEST"

7

Efaviranez

- NNRTI
- CYP3A4/2B6 inducer: oral contraceptive failure
- OK to use it with rifampin/rifaburin, just adjust the dose
- don't use in pregnancy
- wacky, vivid dreams (will resolve)
- "efaviraNEZ NEVirapine"

8

Nevirapine

- NNRTI
- CYP3A4/2B6 inducer: oral contraceptive failure
- "efaviraNEZ NEVirapine"

9

Atazanavir

- Protease inhibitor
- "You'll NAVIR cleave your proteins!"

10

Ritonavir

- Protease inhibitor
- can be used in combination with other "NAVIRs" because of CYP inhibition
- "You'll NAVIR cleave your proteins!"

11

Darunavir

- Protease inhibitor
- used with ritonavir to boost
- "You'll NAVIR cleave your proteins!"

12

Fosamprenavir

- Protease inhibitor
- "You'll NAVIR cleave your proteins!"

13

Indinavir

- Protease inhibitor
- Kidney stones
- "You'll NAVIR cleave your proteins!"

14

Lopinavir

- Protease inhibitor
- used with ritonavir to boost
- "You'll NAVIR cleave your proteins!"

15

Saquinavir

- Protease inhibitor
- "You'll NAVIR cleave your proteins!"

16

Enfuviratide

- Fusion inhibitor
- pro-drug, needs to be activated in body; must be given subQ
- Gp41 analogue
- "-vir-"

17

Maraviroc

- Fusion inhibitor
- CCR5 inhibitor
- "-vir-" "maraviroC"

18

Raltegravir

- Integrase inhibitor
- "-tegra-"

19

Cobicistat

- CYP3A4 inhibitor
- No antiviral activity, increases serum concentrations of CYP3A4 substrate drugs

20

Atripla

- Tenofovir/Emtricitabine/Efaviranez

21

Stribild

-Tenofovir/Emtricitabine/Elivtigravir
*Cobicistat to enhance

22

Complera

-Tenofovir/Emtricitabine/Elitigravir
- Heavy viral loads (>100,000)

23

NRTI properties

- CYP3A4 neutral
- excreted in urine
- oral dosing

24

NNRTI properties

- CYP inducers/inhibitors
- Urine/stool excretion

25

Protease inhibitor properties

- TONS of Pgp/CYP interactions

26

NRTI Major BBWs

Hepatic disease – across the board a problem – obesity/women/prolonged exposure

Lactic acidosis – across the board a problem – obesity/women/prolonged exposure

Pancreatitis – enzyme elevation, abdominal pain (radiating to back), big problem

Neutropenia with AZT

Neuropathy – with all drugs (most likely with stavudine, then didanosine, then all the rest)

27

Zidovudine (AZT)

- NRTI
- BBW: Neutropenia
- "LAD ZEST"

28

NNRTI BBWs

- Women shouldn't take these if CD4+ is below 250
- Hepatic disease/Hepatitis
- Rash

29

Protease inhibitor BBWs

GI intolerance
Lipodystrophy - buffalo hump
diabetes - inhibit GLUT 4

30

What types of drugs would likely interact with HAART drugs?

Azoles – metabolism through CYP3A4 (anti-fungal) – voriconizole – so don’t use it

Tuberculosis (TB) that was latent and now with compromised immune system – rifampin

31

CMV infections

o Valganciclovir = prodrug of ganciclovir for oral dosing
- Mutation in viral kinase for resistance
- Renal clearance is in excess of blood flow (actively pumped out), so if you have diminished renal function then you can have toxic accumulation

o Foscarnate
- Doesn’t need viral kinase to be activated (only host kinases)
- Very insoluable – so we hydrate the patient before administing (saline hydration). We want the most volume possible for the drug to be dissolved
- Only by controlled infusion pump IV, if you gave it all at once, it precipitates
- Still nephrotoxic

32

EBV

o Vidarabine (topical)
- Applied to eye as ointment as a very small amount to limit toxicity

33

KS

o Cidofovir (IV)
- Renal clearance by active tubular secretion
- Renal toxicity