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Pharmacokinetic evaluation of ethionamide suppositories.

Author(s): Peloquin CA, James GT, McCarthy E, Goble M

Affiliation(s): Department of Medicine, National Jewish Center for Immunology and Respiratory Medicine, Denver, Colorado 80206.

Publication date & source: 1991, Pharmacotherapy., 11(5):359-63.

Publication type: Clinical Trial; Randomized Controlled Trial

The absorption and elimination of ethionamide (ETA) after oral tablets and rectal suppositories were determined in 12 healthy, adult male volunteers. A randomized, double-blind, double-dummy, crossover design was used. Treatments compared 250-mg ETA tablets and a placebo suppository to a 500-mg ETA suppository and two placebo tablets, given 7 days apart. Blood samples were collected at predetermined intervals for 12 hours after the dose. Serum concentrations of ETA were determined using high-performance liquid chromatography. The area under the serum concentration-time curve was used to compare the relative bioavailability of ETA from the two preparations. Relative bioavailability after rectal administration was 57.3% of that after oral administration. The maximum serum concentration after rectal administration was 33% of that after oral administration. Higher doses of ETA and serum concentration monitoring are recommended whenever the suppositories are used.

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