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Hematology-Oncology Exam 2 > Pharmacology: Anti-retroviral Agents > Flashcards

Pharmacology: Anti-retroviral Agents Flashcards

1
Q

What are 4 goals of chronic disease management for HIV patients?

A
  1. Achieve durable virologic suppression
  2. Stabilize or restore immune function
  3. Maintain or improve the patient’s quality of life
  4. Reduce HIV related mortality and morbidity
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2
Q

What leads to increases in the CD4 cell counts of over 100-200 cells/mm/year?

A

HAART therapy

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3
Q

Regimens of how many agents are used in HAART therapy?

A

3 or more

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4
Q

What are 4 examples of FDA approved agents for Drug Therapy for HIV?

A
  1. Nuceloside reverse transcriptase inhibitors (NRTIs)
  2. Nonnucleoside reverse transcriptase inhibitors (NNRTIs)
  3. Protease Inhibitors (PIs)
  4. Fusion Inhibitors (FIs)
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5
Q

What is the key viral enzyme that converts viral RNA to DNA?

A

Reverse transcriptase (catalyzes viral RNA to viral DNA)

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6
Q

What does reverse transcriptase allow for?

A

Selective toxicity

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7
Q

What does reverse trascriptase have to do before HIV can be inserted into the host cell’s genetic material?

A

Convert viral RNA into proviral DNA

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8
Q

What kind of cells do NRTIs protect?

A

Only newly infected cells

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9
Q

What is the MOA of NRTIs?

A

They target the early/essential step in HIV replication by acting as substrates for reverse transcriptase…
THEY INHIBIT REVERSE TRANSCRIPTASE BY INCORPORATING FALSE NUCLEIC ACIDS INTO THE NEWLY PRODUCED PROVIRAL DNA
-These agents lack a 3’ hydroxyl group, thus incorporation into DNA terminates chain elongation

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10
Q

How do NNRTIs work?

A

They inhibit reverse transcriptase activity by binding adjacent to the enzyme’s active site and inducing conformational changes

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11
Q

What kind of cells do NNRTIs protect?

A

Newly infecting cells

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12
Q

What strain of HIV are NNRTIs effective against?

A

Only HIV-1

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13
Q

What kind of metabolism do NNRTIs have?

A

Hepatic…many potential drug interactions

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14
Q

True or False: There is no need for phosphorylation in NNRTIs

A

TRUE

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15
Q

What stage of infection do NRTIs and NNRTIs work?

A

They only protect NEWLY INFECTED CELLS

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16
Q

What is an essential enzyme for viral survival and infectivity?

A

HIV PROTEASE

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17
Q

What does HIV protease do?

A

Cleaves viral polyprotein into active viral enzymes (reverse transcriptase, protease, and integrase)

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18
Q

Where do protease inhibitors bind?

A

Reversibly to the active site of the HIV protease

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19
Q

What happens to the viral particles with a protease inhibitor?

A

They become immature and non-infectious

20
Q

What cells do protease inhibitors inhibit viral replication in?

A

Any infected cells

21
Q

What is a unique indication for enfuvirtide (fusion inhibitor)?

A

Advanced HIV-1 infection patients

They have ongoing viral replication despite antiretroviral therapy

22
Q

What types of drugs are given in a PI-based HAART regimen?

A

Protease inhibitor and 2 NRTIs

Example: Iopinavir/ritonavir + (sidovudine or stavudine) + Lamivudine

23
Q

What are 3 advantages of PI-based HAART Regimen?

A
  1. Standard of care
  2. Longest data record including data on survival benefit
  3. Effective and durable
24
Q

What are 3 disadvantages of PI-based HAART Regimen?

A
  1. Metabolic complications
  2. CYP3A4 metabolizes all the PIs and PIs inhibit it
  3. Complex regimens
25
Q

What are 3 advantages of NNRTI-based regimens over PI-based regimens as HAART?

A
  1. Simple regimens
  2. Less fat maldisritbution dyslipidemia than PI-based regiments (well tolerated)
  3. Save PI options for future use
26
Q

What are 2 significant tests to be done to determine the severity of HIV infection?

A
  1. Plasma HIV RNA levels

2. CD4 T-cell counts

27
Q

What do Plasma HIV RNA levels show?

A

Indicates the magnitude of HIV replication and its associate rate of CD4 T-cell destruction

28
Q

What do CD4 T-cell counts show?

A

Indicated the extent of HIV-induced immune damage already suffered

29
Q

When do HIV RNA levels stabilize after diagnosis?

A

6-9 months

30
Q

True or False: HIV RNA level changes are predictable?

A

FALSE… they are unpredictable

31
Q

What is the best measure of the activity of antiretroviral therapy in HIV-infected persons?

A

HIV RNA levels

32
Q

What is the goal with antiretroviral therapy in HIV-infected persons?

A

To decrease HIV RNA levels to undetectable (this may take up to 16-24

33
Q

What is the most prominent AE to Zidovudine (AZT)?

A

BM suppression (myelosuppression)

34
Q

What is the most prominent AE to Stavudine (d4T)?

A

Peripheral neuropathy (20-30%)

35
Q

What is the most prominent AE to Didanosine (ddl)?

A

Pancreatitis, peripheral neuropathy

36
Q

What are 2 indications that drug failure has occurred with anti-retroviral agents?

A
  1. Inadequate viral suppression

2. Unsatisfactory increase in CD4 count

37
Q

What enzyme metabolizes all PIs?

A

CYP3A4- Metabolizes all PIs and PIs inhibit it

38
Q

What population shouldn’t receive efavirenz?

A

PREGGERS

39
Q

Which 2 NRTIs are preferred for treatment of HIV?

A
  1. Emtricitabine

2. Tenofovir

40
Q

What are 4 disadvantages of NNRTI-based regimens over PI-based regimens as HAART?

A
  1. Not all NNRTI are equipotent to PI
  2. Low genetic barrier to resistance
  3. Cross-resistance among NNRTIs
  4. Skin rash
41
Q

What can increase HIV RNA levels?

A

Immunizations or infections

42
Q

What AE are common to Zidovudine, Stavudine, and Didanosine?

A

Cause lactic acidosis with hepatic steatosis

43
Q

What AE can Abacavir cause?

A

HS (can be fatal, so stop drug), nausea, HA

44
Q

What AE can Zalcitabine cause?

A

Peripheral neuropathy or pancreatitis

45
Q

What is a major AE to anti-retrovirals (especially NNRTIs and PIs)?

A

Hepatotoxicity

46
Q

How do you monitor and define hepatotoxicity from anti-retrovirals?

A

Serum transaminases- The hepatotox is defined as a 3-5 fold increase

Hematology-Oncology Exam 2 (15 decks)

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