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Skin, Blood & Lymph Exam #2 > Pharmacology of HIV > Flashcards

Pharmacology of HIV Flashcards

1
Q

How does HIV attach and enter a host T-cell?

Describe the glycoproteins involved.

A

HIV’s gp120 receptor (on the end of gp41 - “fusion protein”) binds the CD4 receptor on T-cells. There is a co-receptors which also interact (CXCR4 or CCR5). The protease enzyme creates a pore in the host, which allows the virus to enter.

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2
Q

What drug is considered an HIV “entry inhibitor”?

A

Maraviroc

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3
Q

What is the specific MOA of Maraviroc?

What is the clinical indications of it?

How is it administered?

How does resistance occur? (2)

What are the side-effects?

A

It binds selectively to CCR5 and prevents viral entry into the host cell.

Used in combination with other anti-RV agents infected only with CCR5-tropic HIV.

Orally administered.

Mutations in V3 loop of gp120.
Emergence of CXCR4-tropic virus.

It is well-tolerated, but systemic allergic reactions followed by hepatotoxicity has been reported.

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4
Q

What drug is considered an HIV “fusion inhibitor”?

A

Enfurvitide

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5
Q

What is the MOA of Enfurvitide?

How is it administered?

How does resistance occur? (1)

What are the side-effects? (3)

A

Binds to gp41 and prevents the conformational and structural changes needed to allow fusion of the viral envelope with the host cell membrane.

Must be given subQ.

Mutations in gp41.

Local injections site reactions.
Insomnia, HA, dizziness, nausea.
Hpersensitivity - rare.

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6
Q

What HIV drug class is used in almost every anti-RV regimen?

A

Nucleoside and nucleotide reverse transcriptase inhibitors (NRTIs).

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7
Q

What is the MOA of NRTIs?

How does resistance occur? (2)

A

Competitive inhibition of HIV RT by incorporation into the growing viral DNA chain. This leads to premature chain termination.

Point mutations in HIV RT.
Impaired kinase activity to prevent phosphorylation/activation.

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8
Q

What drugs are nucleoSide RT inhibitors?

A 
Lamivudine
Emtricitabine
Abacavir
Didanosine
Stavudine
Zidovudine
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9
Q

What drugs are nucleoTide RT inhibitors?

A

Tenofovir

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10
Q

What is the most common side-effect of Abacavir?

What else might be seen?

What must be avoided when taking it?

A

Skin rash (50%).

Fever, N/V/D, pulmonary symptoms.

EtOH can increase serum concentration of Abacavir.

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11
Q

What are the most common side-effects of Didanosine? (3)

A

Dose-dependent pancreatitis.

Retinal changes with optic neuritis - must have periodic retinal exams.

Increased risk of lactic acidosis and hepatic steatosis when combined with Stavudine.

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12
Q

What are the indications for Lamivudine?

What side-effects are common?

A

HIV and HBV.

S/E are relatively rare.

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13
Q

What is the unique structure of Emtricitabine?

What are the indications for it?

What is unique about the PKs?

What side-effects might be seen? (2)

A

Fluorinated analog of Lamivudine.

HIV and HBV.

Its long intracellular half-life allows for once daily dosing.

HA, N/V, rashes.
*Hyperpigmentation of palms/soles(more common in AA patients).

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14
Q

What side-effects might be seen with Stavudine? (3)

A

Dose-dependent peripheral neuropathy.

Dyslipidemia.

Increased risk of lactic acidosis and hepatic steatosis when used with Didanosine.

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15
Q

What side-effects are seen in Zidovudine? (3)

A

Macrocytic anemia.

Neutropenia.

GI intolerance, HA and insomnia - tends to resolve during therapy.

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16
Q

What was the first anti-RV drug approved?

A

Zidovudine

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17
Q

What are the indications for Tenofovir?

What side-effects might be seen?

What tends to enhance oral absorption?

A

HIV and HBV.

Flatulence, but generally well-tolerated.

Concomitant use with Disoproxil or Alafenamide prodrugs.

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18
Q

Abacavir is often used in tandem with which 2 other drugs?

A

Abacavir + Lamivudine

Abacavir + Zidovudine

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19
Q

What are the following drugs analogs of?

Lamivudine
Abacavir
Didanosine
Stavudine
Zidovudine

Tenofovir

A

Lamivudine: cytosine.

Abacavir: guanosine.

Didanosine: deoxyadenosine.

Stavudine: thymidine.

Zidovudine: deoxythymidine

Tenofovir: acyclic nucleotide analog of adenosine.

20
Q

What is the general MOA of non-nucleoside reverse transcriptase inhibitors (NNRTIs)?

How does resistance develop?

A

They bind directly to HIV RT in a site distant from the active site. This causes a conformational change in the enzyme. They act as non-competitive inhibitors.

It develops rapidly with monotherapy due to HIV RT point mutations that alter NNRTI binding.

21
Q

What are the side-effects of NNRTI drugs? (3)

A

GI intolerance.

Skin rash.

CYP450 metabolism (CYP3A4 substrate).

22
Q

Which drugs are first-generation NNRTIs? (3)

Which drugs are second-generation NNRTIs? (2)

A

First-generation:
Delavirdine - not used.
Efavirenz
Nevirapine

Second-generation:
Etravirine
Rilpivirine

23
Q

How often is Efavirenz given?

What other drugs is it combined with? (2)

A

Once daily due to increased half-life.

Tenofovir and Emtricitabine.

24
Q

What is the indication for Nevirapine?

A

Prevention of transmission of HIV from mother to baby.

25
Q

What is the indication of Etravirine?

A

It is used to overcome HIV resistance to first-generation NNRTIs.

26
Q

What 2 drugs is Rilpivirine coformulated with?

What is its unique side-effect?

A

Emtricitabine and Tenofovir.

QT prolongation with high doses.

27
Q

What is the general MOA of integrase strand transfer inhibitors (INSTIs)?

A

Binds HIV integrase and inhibits strand transfer and prevents ligation of RT HIV DNA into the chromosomes of the host cell.

28
Q

What are the side-effects of INSTIs?

A

They are generally well-tolerate, but may cause HA and GI-related side-effects.

29
Q

What is the MOA of drugs ending in “-gravir”?

A

INSTIs

Dolutegravir
Elvitegravir
Raltegravir

30
Q

What is the indication of Dolutegravir?

A

It is the preferred agent for treatment of treatment-naive patients when combined with:

Tenofovir/Emtricitabine
Abacavir/Lamivudine

31
Q

What drug is Elvitegravir combined with?

A

Cobicistat; ELvitegravir is only used in combo with other meds.

32
Q

What is the indication for Raltegravir?

A

It is the preferred medicine for treatment-naive patients.

33
Q

What is the general MOA of protease inhibitors?

A

Blocks the HIV protease and prevens the maturation of the final structural proteins that make up the mature virus. It is a competitive inhibitor.

34
Q

What are the side-effects of protease inhibitors? (3)

A

GI intolerance.
Lipodystrophy - metabolic and morphologic.
Redistribution and accumulation of fat.

35
Q

Which protease inhibitor has the most pronounced CYP inhibitory effect?

Which one has the least?

A

Most: Ritonavir.

Least: Saquinavir.

36
Q

What is the general suffix of the protease inhibitors?

A

-navir

37
Q

What other drugs is commonly prescribed with Darunavir?

A

Ritonavir or Cobicistat.

38
Q

Fosamprenavir is a prodrug of which other drug?

What is it often given with?

A

Amprenavir.

Low dose Ritonavir.

39
Q

What are the unique side-effects associated with Indinavir? (2)

What other drug should it be “boosted” with?

A

Unconjugated hyperbilirubinemia and nephrolithiasis.
*recommend drinking >48 oz. water daily.

Boost with Ritonavir, but increases risk of kidney stones.

40
Q

Lopinavir is only used in association with which other drug?

A

Ritonavir

41
Q

What side-effects are typical for Nelfinavir?

A

Diarrhea and flatulence.

42
Q

What is the typical indication of Ritonavir?

What side-effects are most common?

A

It is used mainly as a booster.

High rate of GI side-effects.

43
Q

Squinavir is used in tandem with what drug?

A

Ritonavir

44
Q

What is the indication for Tipranovir?

What drug is it used with?

What side-effect is common with it?

A

Indicated in patients resistant to other protease inhibitors.

It is used with Ritonavir.

Urticaria or maculopapular rash.

45
Q

What is considered HAART therapy?

A

3 or 4 drugs total.

2 NRTIs plus either:

  • 1 protease inhibitor (sometimes 2).
  • 1 NNRTI
  • 1 INSTI

Skin, Blood & Lymph Exam #2 (7 decks)

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