Integrase Inhibitor

Question 1

Integrase Inhibitor prototype

Answer 1

Raltegravir

Question 2

Raltegravir indications

Answer 2

In combination with other antiviral agents for the treatment of HIV-1 infection in treatment-experienced adult patients who have evidence of viral replication and HIV-1 strains resistant to multiple antiretroviral agents.

Question 3

Raltegravir actions

Answer 3

Inhibits the activity of the virus-specific enzyme integrase, an encoded enzyme needed for viral replication. Blocking this enzyme prevents the formation of the HIV-1 provirus and leads to a decrease in viral load and an increase in active CD4 cells.

Question 4

Raltegravir route, onset, peak

Answer 4

Oral, rapid, 3 h

Question 5

Ralegravir adverse effects

Answer 5

Headache, dizziness, nausea, vomiting, diarrhea, fever, rhabdomyolysis (the breakdown of muscle fibers that leads to the release of muscle fiber contents (myoglobin) into the bloodstream. Myoglobin is harmful to the kidney and often causes kidney damage) and myopathy (which can lead to kidney and cardiac disease).

Question 6

Raltegravir facts

Answer 6

• Contraindicated if known hypersensitivity to any component of drug, as initial treatment in adults, for use in children, and for nursing mothers.
• Use CAUTION with patients at risk for rhabdomyolysis or myopathy.
• Do not use St. John’s wort.
• Do not use with Rifampin (anti-tb drug) b/c it reduces serum Raltegravir levels.