HIV drugs - Because I guess we should know these? Flashcards Preview

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Flashcards in HIV drugs - Because I guess we should know these? Deck (9)
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1
Q

Which drug is used to increase the serum dose of the other HIV drugs in its class?

A

Ritonavir

It is poorly tolerated at high doses, but it is used at low doses to increase the serum concentration of the other protease inhibitors (-navirs)

Navir! Swimming in the proteases!
(like nadar? get it?)
Potently inhibits CYP3A4

2
Q

What is maraviroc’s mechanism of action?

A

Prevents HIV from binding to host CCR5

3
Q

What is raltegravir’s mechanism of action?

A

Integrase inhibitor
-prevents integration of proviral DNA into host chromosome

rALTEGRAvir
hALT intEGRAse -vir…

4
Q

What is Darunavir’s mechanism of action?

A

Prevent protease action required to mature the virus
-cleavage events of env, gag, and pol

(just like the rest of the -navirs!)

5
Q

Which class of HIV antiretrovirals can cause lactic acidosis and hepatic steatosis (fatty liver)?

A

NRTIS

Zidovudine, lamivudine, emtricitabine, abacavir

6
Q

What is the mechanism of action of the NRTIs?

A
  • competitively inhibit reverse transcriptase and terminate DNA chain through incorporation.
  • Must by phosphorylated by cellular enzymes to be activated
7
Q

What is the mechanism difference between tenofovir and the other NRTIs?

Toxicity difference?

A

It is the same as the NRTIs, but is already phosphorylated so that it can skip that step in the body. NucleosideRTIs have to be phosphorylated by the host cell.

Can still cause lactic acidosis. Also renal failure

8
Q

What are the non-NRTIs mechanism of action?

What are the names of the non-NRTIs?

A

Bind directly to reverse transcriptase at a site distinct from NRTI

Etravirine
Efavirenz

9
Q

What HIV drug works as a fusion inhibitor?

How does it work?

A

Enfuvirtide

Binds to gp41 to prevent conformational change allowing fusion of viral and host membranes