Pharmacokinetic evaluation of ethionamide suppositories.
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.
Peloquin
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Department of Medicine, National Jewish Center for Immunology and Respiratory Medicine, Denver, Colorado 80206.
James
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McCarthy
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Goble
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D000284:Administration, Oral; D000285:Administration, Rectal; D000293:Adolescent; D000328:Adult; D001682:Biological Availability; D002851:Chromatography, High Pressure Liquid; D004311:Double-Blind Method; D005000:Ethionamide / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D008875:Middle Aged; D013488:Suppositories; D013607:Tablets
D013488:Suppositories; D013607:Tablets; D005000:Ethionamide