C / 6 - antiretroviral agents Flashcards

1
Q

What does HAART stand for?

A

Highly active antiretroviral therapy

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2
Q

What is the goal of HAART?

A
  • suppress the replication of HIV
  • restore the number of CD4 cells
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3
Q

What are the 5 different classes of antiviral therapy?

A
  1. Nucleotide/side reverse transcriptase inhibitors (NRTIs)
  2. Non-nucleoside reverse transcriptase inhibitors (NNRTIs)
  3. Protease inhibitors
  4. Integrase inhibitors
  5. Entry inhibitors
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4
Q

What is the start combination for HAART?

A

2 NRTI + 1 NNRTI or PI or II

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4
Q

NRTIs used to treat HIV

A
  • Tenofovir
  • Abacavir
  • Zidovudine
  • Emtricitabine
  • Lamivudine

Ten Abandonned Zinc Emitting Lamps

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5
Q

NRTIs
- MOA
- Indication
- ROA
- Toxicity
- Pharmacodynamics

A
  • Terminate the growing DNA chain : inhibit binding of nucleotides to reverse transcriptase
  • HIV 1 + 2 infection
  • Oral
  • GI symptoms, headache, hepatotoxicity, lactic acidosis
  • All penetrate CNS, except for tenofovir + renal excretion
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6
Q

Etravirine (NNRTI)
- MOA
- Indication
- ROA
- Toxicity
- Pharmacodynamics

A
  • Bind to reverse transcriptase on a different site than NRTIs
  • HIV-1
  • Oral
  • Hepatotoxicity, rash, nausea, diarrhea
  • Hepatic metabolism
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7
Q

Protease inhibitors
- MOA
- ROA
- Toxicity
- Pharmacodynamics

A
  • Inhibition of HIV protease
  • Oral
  • Insulin resistance, hyperlipidemia, GI and neurological disorders
  • No CNS penetration
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8
Q

Name 2 protease inhibitors

A
  1. Ritonavir
  2. Darunavir
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9
Q

Dolutegravir
- MOA
- Indication
- Toxicity

A
  • Integrase inhibitor : binding to integrase inhibits the integration of proviral DNA to host chromosome
  • HIV-1
  • Severe hypersensitivity reaction
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10
Q

Maraviroc
- MOA
- Indication
- ROA
- Toxicity

A
  • Entry inhibitor : prevents interaction between CD4 and viral gp120
  • Used in combination with other antiretroviral agents
  • Oral
  • Headache, dizziness, diarrhea

(CCR5 co-receptor antagonist )

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