Lidocaine shows pronounced first-pass metabolism upon peroral administration in man (about 30 per cent peroral bioavailability). Since the rectal bioavailability is about 65 per cent in man it is assumed that some drug is directly absorbed into systemic circulation by-passing the liver. In rats pero
First-pass elimination of salicylamide in man following oral and rectal administration
β Scribed by A. G. de Boer; D. D. Breimer; J. M. Gubbens-Stibbe; A. Bosma
- Publisher
- John Wiley and Sons
- Year
- 1983
- Tongue
- English
- Weight
- 474 KB
- Volume
- 4
- Category
- Article
- ISSN
- 0142-2782
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β¦ Synopsis
In order t o study the avoidance of hepatic first-pass elimination following rectal administration, 500 mg of salicylamide (SAM) were given orally and rectally to man. Plasma SAM concentrations were measurable following oral administration, but following rectal administration SAM concentrations were either very low or not detectable. The mean excretion of SAM sulphate (SAMS) and SAM glucuronide (SAMG) in the urine following oral and rectal administration was 71.3 per cent and 45.6 per cent respectively. Increasing the oral and rectal dose (1500mg of SAM, solution) showed that the mean AUC values were 911 and 144pgminml-', respectively. The mean urinary excretion of SAMS plus SAMG following oral and rectal administration was 82.0 and 75.6 per cent respectively; the mean plasma elimination -half-lives were 3 I and 40min, respectively, while the mean urinary elimination half-lives were 63 and 73 min, respectively.
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