Use of Raltegravir in Pediatric HIV-1 Infection

Marcia L. Buck, Pharm.D., FCCP, FPPAG; Kristi N. Hofer, Pharm.D; Michelle W. McCarthy, Pharm.D.; FASHP Susan B. Cogut, Pharm.D

Disclosures

Pediatr Pharm. 2012;18(1) 

In This Article

Drug Interactions

Rifampin, a strong inducer of UGT1A1, increases the rate of metabolism of raltegravir and reduces plasma concentrations. In adults taking raltegravir who require treatment with rifampin, the raltegravir dose should be increased to 800 mg twice daily. There have been no studies to determine the appropriate dosage adjustment in children requiring this combination.[2,3,11]

The effect of concomitant administration of other medications used for the treatment of HIV-1 infection has also been studied. Administration with antiretrovirals that induce UGT1A1 such as efavirenz, etravirine, or tipranavir/ritonavir reduce raltegravir concentrations, but the clinical significance of these interactions has not been assessed and no dosage adjustment is recommended. Although atazanavir is a strong inhibitor of UGT1A1 and has been shown to produce a 30–70% increase in plasma raltegravir concentrations, the interaction has not been found to result in increased toxicity.[2,3,12]

Medications that increase gastric pH, such as H2 blockers or proton pump inhibitors, may increase raltegravir absorption and result in higher plasma concentrations. Studies have demonstrated no significant difference in clinical response, so no dosage adjustment is recommended.[2,3]

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