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Flashcards in Antiretrovirals Deck (58):
1

What allows HIV to mutate so rapidly?

Really error prone reverse transcriptase

2

What is the enzyme that integrates HIV genetic material into host DNA?

integrase

3

What is the enzyme that is packaged with the HIV virus, and cleaves viral proteins to mature proteins?

Protease

4

What is the viral antigen of HIV that is measured in the serum to follow the early course of the disease?

p24

5

What is the antibody that is followed with HIV infections?

Anti-HIV ab (gp120)

6

What is the MOA of Nucleotide reverse transcriptase inhibitors?

Mimic nucleotides to inhibit nucleotide binding to the catalytic site, and cause chain termination

7

What are the adverse effects of Nucleoside reverse transcriptase inhibitors?

Lactic acidosis
Fatty liver disease
Lipodystrophy

8

Why can NRTIs be used in Hep B infections?

Has reverse transciptase

9

What type of drug is Abacavir? Route of administration? Adverse effects?

NRTI
PO
Increase chances of MI

10

What drug does Abacavir interfere with?

Methadone

11

How is resistance to abacavir brought about?

Multiple mutations in HIV reverse transcriptase

12

What type of drug is Lamivudine? Route of administration? Adverse effects?

NRTI
PO
CNS effects, but safer than most

13

How is resistance to Lamivudine brought about?

Single base change

14

Which HIV drugs are safe for use in pregnancy?

Lamivudine
Nevirapine
***

15

What type of drug is Emtricitabine? Route of administration? Adverse effects?

Fluorinated analog of lamivudine (NRTI)
PO
HA, n/v/d

16

How is resistance to Emtricitabine brought about?

single mutation in reverse transcriptase

17

What type of drug is Tenofovir? Route of administration? Adverse effects?

NRTI
PO
Renal and bone toxicity

18

How is resistance to Tenofovir brought about?

single mutation in reverse transcriptase

19

What type of drug is Zidovudine (AZT)? Route of administration? Adverse effects?

NRTI
PO
Myelosuppression

20

How is resistance to Zidovudine brought about?

Multiple mutations in HIV needed

21

What is the MOA of Non-nucleoside reverse transcriptase inhibitors? What is the major difference between these and NRTIs?

bind to a site on the enzyme distinct from the active site

Do NOT need to be phosphorylated to become activated

22

How is resistance to NNRTIs brought about?

Single amino acid change

23

What is the major adverse reaction that is common to the class of NNRTIs?

Drug-Drug interactions d/t p450 effects

Stven-Johnson syndrome

24

What type of drug is Efavirenz? Route of administration? Adverse effects?

NNRTI
PO
CNS effects

25

Resistance to Efavirenz will often mean resistance to what other NNRTI?

Nevirapine

26

What type of drug is Nevirapine? Route of administration? Adverse effects?

NNRTI
PO
Hepatitis

27

What is the MOA of the proteases used for treating HIV?

mimic peptides for the protease

28

Generally, how is resistance to protease inhibitors brought about?

Multiple mutations

29

What are the common adverse effects of protease inhibitors?

Drug-drug interactions high d/t p450

30

What is the major difference between mature and immature HIV viruses?

Well formed blob on EM with mature, whilst immature have poorly defined blob

31

What type of drug is Atazanavir? Route of administration? Adverse effects?

Protease inhibitor
PO
Peripheral neuropathy, cardiac effects

32

What class of drugs cannot be administered concurrently with Atazanavir? Why?

PPIs, since acid required for absorption

33

What type of drug is Ritonavir? Route of administration? Adverse effects?

Peptidomimetic protease inhibitor
PO
POTENT inhibitor of p450

34

What is the therapeutic indication for Ritonavir?

Booster to increase the half-life of coadministered ARV drugs d/t inhibiting p450 effects

35

What type of drug is Darunavir? Adverse effects?

Protease inhibitor
Increased serum amylase

36

What is different about the resistance with Darunavir?

90% of HIV-1 isolates that are resistant to multiple protease inhibitors are still susceptible to this

37

What is the MOA of CCR5 receptor antagonists?

Inhibits the coreceptor CCR5

38

What are the two coreceptors for HIV? Which causes a lower susceptibility to HIV infection?

CCR5
CXCR4--cause lower susceptibility***

39

What is the role of gp120 on HIV?

Envelope protein/anchor on cells

40

What is the role of gp41 protein on HIV?

Fusion protein

41

What type of drug is Maraviroc? Adverse effects?

Co-receptor antagonist
URT infections/increased cardiac events

42

What is the therapeutic indications for Maraviroc?

For HIV experience pts, who have a *predominantly CCR% tropic virus*

43

How is resistance brought about with Maraviroc?

Change in tropism or mutations in gp120

44

What is the MOA of fusion inhibitors?

Inhibits gp41 from fusing cell membranes of HIV

45

What is the only type of antiretroviral that is administered IV?

Fusion inhibitors

46

What type of drug is Enfuvirtide? Adverse effects?

Peptide fusion inhibitor
Injection pain, bacterial pneumonia

47

How is resistance to Enfuvirtide brought about?

Multiple mutations in gp41

48

What is the therapeutic index of enfuvirtide?

Treatment experienced patients with evidence of ARV resistance

49

What is the MOA of integrase inhibitors?

Inhibit HIV integrase, and prevents DNA strand transfer

50

What type of drug is Raltegravir? Adverse effects?

Integrase inhibitor
Myopathy/rhabdo

51

How is resistance to Raltegravir ad Elvitegravir brought about?

Single mutation in integrase gene

52

What type of drug is Elvitegravir? Adverse effects?

Integrase inhibitor
Usual side efects

53

What type of drug is Dolutegravir? Adverse effects?

Integrase inhibitor
Elevation of serum aminotransferases, fat redistribution syndrome

54

What is the therapeutic indications for Dolutegravir?

Need to weigh 40 kg and be over 12 yo

55

What is significant about the resistance profile of Dolutegravir?

Retains activity against some viruses resistant to both raltegravir and elvitegravir

56

What is the clinical definition of AIDS?

Less than 250 cells/mm3 of CD4 cells

57

True or false: all pts who have HIV are recommended to take antiretroviral agents

True

58

What is the standard of care for HIV?

Use at least 3 antiretroviral drugs, usually form at least two different classes.

1 PI + 2 NRTIs
1 II + 2 NRTIs