Integrase inhibitors & Fusion inhibitor Flashcards

1
Q

What are the agent drugs under integrase inhibitors??

A
  • Raltegravir
  • Dolutegravir

*rapid decrease in viral load

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2
Q

How are the integrase inhibitors administered?

A

Orally

*Well absorbed with food

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3
Q

CSF penetration?

A

Yeah, good levels in CSF

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4
Q

What’s the metabolic pathway of the integrase inhibitors?

A
  • Metabolized by the UGT 1A1 pathway in the liver.
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5
Q

What are the common side effects from using integrase inhibitors?

A
  • Diarrhea
  • nausea
  • headaches
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6
Q

What drug agent is found under fusion inhibitors?

A
  • Enfuvirtide
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7
Q

What’s the administration route of enfuvirtide?

A
  • Subcutaneous administration
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8
Q

Which antiretroviral therapy agent, is used as salvage therapy?

A
  • Enfuvirtide
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9
Q

What’s the metabolic pathway of fusion inhibitors?

A
  • Proteolytic hydrolysis, (not cytochrome P450)
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10
Q

What are the toxicities or side effects from enfuvirtide?

A
  • Injection site reaction
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11
Q

Raltegravir, an integrase interacts with Rifampicin. What outcome is seen from this?

A

Reduced Raltegravir plasma levels

Adverse effects: myopathy, rhabdomyolysis

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12
Q

What drugs does dolutegravir, interacts with? And what outcomes are seen with such?

A
  • Antacids & iron supplements  ↓ DTG plasma conc.  Dose spacing
  • Anticonvulsants (carbamazepine, phenobarbital, phenytoin)  ↓ DTG
    plasma conc.  Avoid co-admin if possible
  • Metformin  ↑Metformin plasma conc.  Limit metformin dose to max
    500 mg 12-hourly
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13
Q

When is the right weight and age to use Dolutegravir as an ART regimen?

A
  • Weight (>/= 3kg)
  • Age (>/=4 weeks) but less than 10 years
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14
Q

Why is dolutegravir’s use feared on infants younger than 4 weeks?

A
  • It increases the risk of neural tube tube defect
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15
Q

A drug to avoid at periconception and on first 6 weeks of pregnancy

A

Dolutegravir

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16
Q

What are the adverse effects of using dolutegravir?

A
  • Insomnia
  • Weight gain
  • neuropsychiatric effects