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Flashcards in Antiretroviral Agents Deck (44)
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1

This step of HIV replication involves binding of HIV to receptors on the surface of CD4 T cells.

ENTRY

2

This step in HIV replication involves the use of an enzyme to convert HIV RNA into DNA which then migrates to the host nucleus.

REVERSE TRANSCRIPTION

3

This step in HIV Replication involves the use of an enzyme to insert viral DNA into host DNA

INTEGRATION VIA INTEGRASE

4

This step in HIV replication involves creation of new viral rna

REPLICATION

5

This step in HIV replication involves transformation into immature, noninfectious HIV particle or bud

ASSEMBLY

6

This step in HIV replication involves cutting of the long HIV polyprotein chains into smaller functional HIV proteins to make mature infectious viral particle

BUDDING & MATURATION

7

This drug class blocks entry of CCR5-tropic viruses into the CD4 T cell. Give the only approved drug in this class.

CCR5 Antagonists
Maraviroc

8

Drugs in this class bind to envelope gp41 to prevent viral fusion to the CD4 T cell. Give the only approved drug of this class.

FUSION INHIBITORS
Enfuvirtide

9

This drug class is known as the backbone of the ART regimens

NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS

10

What is the MOA of NRTIs?

Undergoes intracellular phosphorylation
Active triphosphate bunds to reverse transcriptase
DNA elongation is terminated after incorporation of NRTI triphosphate

11

What 3 NRTIs should not be used as monotherapy for Hepatitis B? Why?

Lamivudine
Emtricitabine
Tenofovir

Risk of HBV resistance after prolonged use.
HBV flares after discontinuation

12

What are the 2 ADR of NRTIs?

Mitochondrial toxicity which may present as peripheral neuropathy, pancreatitis, lipoatrophy, and hepatic steatosis.

Lactic acidosis syndrome

13

NRTIs have drug to drug interactions with?

Rifampicin
It decreases the concentration of Tenofovir

14

This NRTI is commonly combined with Emtricitabine.
If combined with Emtricitabine, considered as superior to other NRTI combi

Tenofivir Disoproxil Fumarate (TDF)

15

This NRTI combi is effective in decreasing HIV transmission when administered as pre-exposure prophylaxis to HIV-uninfected patients

Tenofovir Disoproxil Fumarate + Emtricitabine (TDF/FTC)

16

What are the main toxicities of Tenofovir Disoproxil Fumarate (TDF)?

Kidney Injury and Bone Loss

*do not give in px with GFR <60mL/min

17

What is the NRTI approved for use in patients with GFR of less than/equal ti 30mL/min

Tenofovir Alafenamide (TAF)

18

What are the 2 drugs that if combined with TAF, increases TAF levels?

Cobicistat or Ritonavir

19

How do Cobicistat and Ritonavir increase TAF bioavailability?

They inhibit intestinal P-glycoprotein

20

This NRTI in combination with Lamivudine is considered as first line NRTI combination for HIV

Abacavir

21

Abacavir-lamivudine combination has the greatest efficacy if combined with?

Dolutegravir

22

This NRTI is not given to patients with CAD because it increases risk for hyperlipidemia and vascular events

Abacavir

23

These NRTIs should not be used in combination because they will compete for intracellular phosphorylation

Lamivudine & Emtricitabine

24

What is the adr of lamivudine?

Pancreatitis. More severe in children

25

What is the adr of Emtricitabine?

Skin changes: hyperpigmentation of palms and soles

26

NNRTIs for tx-naive patients are?

Efavirens and Rilpivirine

27

NNRTI for drug-resistant px is?

Etravirine

28

What is the MOA of NNRTIs?

Prevents HIV-1 Reverse Transcriptase from adding new nucleotides to the growing DNA chain. Blocks cDNA elongation

29

True or False: NNRTIs are active against both HIV-1 and HIV-2.

False. Only vs HIV-1

30

What happens when an NNRTI-containing regimen is discontinued?

A period if functional NNRTI monotherapy may occur

31

What happens in a Functional NNRTI Monotherapy?

This happens when an NNRTI-containing regimen is discontinued.

NNRTI concentrations decline slower than other retrovirals. Therefor increasing the risk for NNRTI resistance

32

What is the remedy for the Functional NNRTI Monotherapy?

Once an NNRTI-containing regimen is stopped, the concomitant nucleoside backbone should be continued for 3-7 days after the NNRTI is discontinued

33

What are the adr of efavirenz and rilpivirine?

Neurologic and Psychologic

34

This NNRTI is given at a dose of 600mg OD. High-fat/high-caloric meals increase absorption.

Efavirenz

35

Why shouldn't Efavirenz be initiated in women who are likely to become pregnant or are in the 1st 8 weeks of pregnancy?

Potential risk for NTDs, facial clefts, and anopthalmia. But it can be used later in gestation

36

What are the side effects of Efavirenz?

Cns toxicity, rash, hyperlipidemia, elevated hepatic transaminase

37

What are the advantages of efavirenz combined with TDF/FTC?

Excellent potency
Low pill burden
Durability

38

This NNRTI may be used in tx-naive px with a baseline viral load <100,000 copies/mL and a CD4 count of morethan or equal to 200 cells/microL.

Rilpivirine

39

What are the side effects of Rilpivirine?

QT prolongation
Depression
Insomnia
Headache
Rash

40

Rilpivirine must be administered with a meal and concimitant use of rilpivirine with ____________ & ___________ is contraindicated

PPI
H2 antagonists
Antacids

41

Drug to drug interactions of rilpivirine

Rifampin, phenytoin, phenobarb, azoles, macrolides

42

This is the most commonly used NNRTI for px with drug-resistant virus

Etravirine

43

This drug class is an attractive option for px with either abn lipid profiles or risk factors for CAD since they have neutral effects on cholesterol & triglycerides

INSTI

44

What is the MOA of Integrase Strand Transfer Inhibitors?

Target the strand transfer step of viral DNA integration
Prevent/inhibit the binding of the preintegration complex (PIC) to host cell DNA