No specific information is available on the treatment of overdosage with ISENTRESS. Multiple doses as high as 1800 mg (3 x 600 mg) q.d. for 28 days and 800 mg b.i.d. were studied in Phase I without evidence of toxicity. Occasional doses of 2400 mg per day were taken in Phase II/III studies without evidence of toxicity. Based upon available data, raltegravir appears to be well tolerated at doses up to 800 mg b.i.d. and when administered with drugs that increase exposure by 50-70% (such as tenofovir disoproxil fumarate and atazanavir). Raltegravir had a wide therapeutic margin; thus the potential for toxicity as a result of overdose is limited.
In the event of an overdose, it is reasonable to employ the standard supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring (including obtaining an electrocardiogram), and institute supportive therapy if required. The extent to which ISENTRESS may be dialyzable is unknown.