Preliminary Observations on a New Derivative of Isoniazid (Ro 2-4969)

Abstract

Summary

1. Ro 2-4969, a compound of low solubility, related to isoniazid, has been administered experimentally to human subjects to determine the rate and extent of absorption from the gastrointestinal tract. 2. The compound or its derivatives appeared in the plasma and, probably because of slow absorption, detectable and clinically significant amounts remained for a longer period than when the highly soluble isoniazid was administered. 3. The drug administered in a single daily dose of 10 mg/kg/day was found to maintain drug concentrations of one μg/ml of plasma without dangerous cumulative effect. 4. No toxic reactions have been observed in 26 patients treated for 2 months or more.