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Pharm > Antiretrovirals > Flashcards

Antiretrovirals Flashcards

1
Q

What allows HIV to mutate so rapidly?

A

Really error prone reverse transcriptase

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2
Q

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

A

integrase

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3
Q

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

A

Protease

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4
Q

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

A

p24

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5
Q

What is the antibody that is followed with HIV infections?

A

Anti-HIV ab (gp120)

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6
Q

What is the MOA of Nucleotide reverse transcriptase inhibitors?

A

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

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7
Q

What are the adverse effects of Nucleoside reverse transcriptase inhibitors?

A

Lactic acidosis
Fatty liver disease
Lipodystrophy

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8
Q

Why can NRTIs be used in Hep B infections?

A

Has reverse transciptase

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9
Q

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

A

NRTI
PO
Increase chances of MI

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10
Q

What drug does Abacavir interfere with?

A

Methadone

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11
Q

How is resistance to abacavir brought about?

A

Multiple mutations in HIV reverse transcriptase

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12
Q

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

A

NRTI
PO
CNS effects, but safer than most

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13
Q

How is resistance to Lamivudine brought about?

A

Single base change

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14
Q

Which HIV drugs are safe for use in pregnancy?

A

Lamivudine
Nevirapine
***

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15
Q

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

A

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

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16
Q

How is resistance to Emtricitabine brought about?

A

single mutation in reverse transcriptase

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17
Q

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

A

NRTI
PO
Renal and bone toxicity

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18
Q

How is resistance to Tenofovir brought about?

A

single mutation in reverse transcriptase

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19
Q

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

A

NRTI
PO
Myelosuppression

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20
Q

How is resistance to Zidovudine brought about?

A

Multiple mutations in HIV needed

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21
Q

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

A

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

Do NOT need to be phosphorylated to become activated

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22
Q

How is resistance to NNRTIs brought about?

A

Single amino acid change

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23
Q

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

A

Drug-Drug interactions d/t p450 effects

Stven-Johnson syndrome

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24
Q

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

A

NNRTI
PO
CNS effects

25
Q

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

A

Nevirapine

26
Q

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

A

NNRTI
PO
Hepatitis

27
Q

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

A

mimic peptides for the protease

28
Q

Generally, how is resistance to protease inhibitors brought about?

A

Multiple mutations

29
Q

What are the common adverse effects of protease inhibitors?

A

Drug-drug interactions high d/t p450

30
Q

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

A

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

31
Q

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

A

Protease inhibitor
PO
Peripheral neuropathy, cardiac effects

32
Q

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

A

PPIs, since acid required for absorption

33
Q

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

A

Peptidomimetic protease inhibitor
PO
POTENT inhibitor of p450

34
Q

What is the therapeutic indication for Ritonavir?

A

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

35
Q

What type of drug is Darunavir? Adverse effects?

A

Protease inhibitor

Increased serum amylase

36
Q

What is different about the resistance with Darunavir?

A

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

37
Q

What is the MOA of CCR5 receptor antagonists?

A

Inhibits the coreceptor CCR5

38
Q

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

A

CCR5

CXCR4–cause lower susceptibility***

39
Q

What is the role of gp120 on HIV?

A

Envelope protein/anchor on cells

40
Q

What is the role of gp41 protein on HIV?

A

Fusion protein

41
Q

What type of drug is Maraviroc? Adverse effects?

A

Co-receptor antagonist

URT infections/increased cardiac events

42
Q

What is the therapeutic indications for Maraviroc?

A

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

43
Q

How is resistance brought about with Maraviroc?

A

Change in tropism or mutations in gp120

44
Q

What is the MOA of fusion inhibitors?

A

Inhibits gp41 from fusing cell membranes of HIV

45
Q

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

A

Fusion inhibitors

46
Q

What type of drug is Enfuvirtide? Adverse effects?

A

Peptide fusion inhibitor

Injection pain, bacterial pneumonia

47
Q

How is resistance to Enfuvirtide brought about?

A

Multiple mutations in gp41

48
Q

What is the therapeutic index of enfuvirtide?

A

Treatment experienced patients with evidence of ARV resistance

49
Q

What is the MOA of integrase inhibitors?

A

Inhibit HIV integrase, and prevents DNA strand transfer

50
Q

What type of drug is Raltegravir? Adverse effects?

A

Integrase inhibitor

Myopathy/rhabdo

51
Q

How is resistance to Raltegravir ad Elvitegravir brought about?

A

Single mutation in integrase gene

52
Q

What type of drug is Elvitegravir? Adverse effects?

A

Integrase inhibitor

Usual side efects

53
Q

What type of drug is Dolutegravir? Adverse effects?

A

Integrase inhibitor

Elevation of serum aminotransferases, fat redistribution syndrome

54
Q

What is the therapeutic indications for Dolutegravir?

A

Need to weigh 40 kg and be over 12 yo

55
Q

What is significant about the resistance profile of Dolutegravir?

A

Retains activity against some viruses resistant to both raltegravir and elvitegravir

56
Q

What is the clinical definition of AIDS?

A

Less than 250 cells/mm3 of CD4 cells

57
Q

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

A

True

58
Q

What is the standard of care for HIV?

A

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

1 PI + 2 NRTIs
1 II + 2 NRTIs

Pharm (73 decks)

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