Raltegravir

Mechanism :

Raltegravir inhibits the catalytic activity of integrase, thus preventing integration of the proviral gene into human DNA.

Indication :

Treatment of HIV-1 infection in combination with other antiretroviral agents

Contraindications :

Hypersensitivity to raltegravir or any other component of the formulation

Dosing :

3 to <20 kg: 6 mg/kg/dose PO twice daily; Maximum dose: 300 mg/dose.

Adverse Effect :

Increased serum AST, ALT & cholesterol, increased glucose, hyperbilirubinemia, fatigue, abdominal pain, cough, rash, dizziness, insomnia, vomiting, arthralgia, extremity pain, nausea, diarrhea, pyrexia.

Interaction :

Etravirine: May decrease the serum concentration of Raltegravir.
Fibric Acid Derivatives: Raltegravir may enhance the myopathic (rhabdomyolysis) effect.
HMG-CoA Reductase Inhibitors (Statins): Raltegravir may enhance the myopathic (rhabdomyolysis) effect of HMG-CoA Reductase Inhibitors.
Proton Pump Inhibitors: May increase the serum concentration of Raltegravir.
Rifampin, Rifabutin, Rifapentine: May decrease the serum concentration of Raltegravir.

Hepatic Dose :

Mild to moderate hepatic impairment: No adjustment of dosage recommended
Severe hepatic impairment: Dose reduction is reasonable.