Antiretroviral Drugs

Question 1

What are the different types/targets of HIV Drugs?

Answer 1

Copreceptor antagonists
Fusion Inhibitors, Integrase inhibitors, Protease inhibitors, Nucleoside and non-nucleoside reverse transcritase inhibitors

Question 2

Which Drugs are NRTIS?

Answer 2

Zidovudine
Lamivudine 
Abacavir 
Tenofovir 
Emtricitibine

Question 3

What is the MOA of NRTIs

Answer 3

Targets reverse transcriptase. prevents nucleotide binding to the catalytic site ==> Chain termination. Fits in the active site of Reverse Trasncriptase.

Question 4

What are the adverse effects of NRTIs?

Answer 4

Lactic Acidosis, fatty liver disease, and lipodystrophy

Question 5

Adverse effects of Abacavir?

Answer 5

Allergic reactions. increased risk of cardiac events, lower effectiveness of methadone.

Question 6

What is a benefit of Lamivudine?

Answer 6

One of the least toxic antiretroviral drugs .

Question 7

What is the benefit of using Emtricitabine?

Answer 7

Half life is longer (>24hrs) than others in its class.

Question 8

Unique adverse effects of Tenofovir?

Answer 8

Renal and bone toxicity. Drug crosses placenta and decreases bone density in fetus.

Question 9

unique adverse effects of Zidovudine?

Answer 9

Myelosupression, fatuige, malaise, nausea, headache, etc…

Question 10

MOA of NNRTIs.

Answer 10

Bind to a site other than the active site on Reverse Transcriptase.

Question 11

Common Adverse effects of NNRTIs?

Answer 11

Rash, Steven Johnson Syndrome, hepatotox, effects Cyt p450 enzymes.

Question 12

How does resistance develop to Efavirenz?

Answer 12

A sigle base change in gene for rev. Transcriptase.

Question 13

Adverse effects of Nevirapine?

Answer 13

Rash, Hepatitis(cqn be fulminant!

Question 14

How to Protease inhibitor drugs work?

Answer 14

Mimic Peptide targets of protease, blcock maturation of virion particles.

Question 15

Common Adverse effects of Protease inhibitors?

Answer 15

Cyt P450 Enzymes ==> Drug interactions, Hyperlipidemia, lipodystrophy, hapatotox.

Question 16

Unique Pharmkinetics of Atazanavir?

Answer 16

Food increases bioavailability. Acid Needed. PPIs contraindicated

Question 17

Adverse effects of Ritonavir?

Answer 17

POTENT inhbitor of CYP3A4 Cyt P450 enzyme. Increased half life of combined drugs.

Question 18

What drug is combined with Darunavir?

Answer 18

Ritonavir because it increases half life

Question 19

Adverse effects of Maraviroc?

Answer 19

Cough, URT infections, postural hypotension, arthralgia, myalgia.

Question 20

Indications for Maraviroc?

Answer 20

Good for CCR5 tropic virus. but not others. Screen for tropisms first!

Question 21

How do fusion inhibitors work on virally infected cell?

Answer 21

Prevent viruses from bringing membranes together in order to bud off from cell.

Question 22

What is unique about the administration of Enfuvirtide?

Answer 22

Only parenterally delivered antiretroviral agent.

Question 23

Adverse effects of Enfuvirtide?

Answer 23

Painful erythematous nodule at sote of injection, increased risk of bacterial pnumonia.

Question 24

How do integrase inhibiting drugs work?

Answer 24

Prevent virus from integrating its DNA into the host DNA! Only infefected til cells die!

Question 25

Adverse effects of Raltegravir?

Answer 25

Myopathy, rhabdomyolysis, creatine kinase elevation

Question 26

Pharmicokinetics of Elvitegravir?

Answer 26

Requires co-admin with cobicistat which inhibits CYP3A4

Question 27

Benefits of using Dolutegravir?

Answer 27

Can work on viruses that have developed resistance to other Integrase inhibitors.

Question 28

When is it reccomended to start antiretroviral treatment?

Answer 28

Good to start at any level of immunosupression! Reccomendations get stronger as CD4 counts go lower.

Question 29

Why is ARV treatment reccomended?

Answer 29

Prevents transmission of virus to others!

Question 30

What is the standard of care of ARV therapy?

Answer 30

3 drugs from 2 different classes. 1PI and 2 NRTIs or 1II and 2 NRTIs.