Clinical pharmacokinetics of etintidine

✍ Scribed by Shiew-Mei Huang; Howard S. Weintraub; Robert Abels; William Harris; Thomas B. Marriott; John D. Arnold; Joseph Boccagno

• Book ID: 101758143
• Publisher: John Wiley and Sons
• Year: 1988
• Tongue: English
• Weight: 435 KB
• Volume: 9
• Category: Article
• ISSN: 0142-2782
• DOI: 10.1002/bod.2510090506

✦ Synopsis

The pharmacokinetics of etintidine (E), a potent HZ blocker, were studied in 12 normal, fasted subjects, The subjects received five ascending doses of E HCl in capsules at 72-h intervals. Blood and urine samples were collected and the plasma and urine levels of E were determined by HPLC. Following oral admininstration, plasma E levels showed double peaks in half of the subjects. Mean C,, (042, 2.1 1,3*82,4.50, and 7.15 pg ml-I), 4.94, 11.3, 17.5, and 24.5 h pg ml-I), and the amount of E excreted unchanged in 72 h (20, 54.8, 170, 320, and 371 mg) were determined. These parameters indicate the amount of E absorbed increased linearly with dose for each individual. Renal clearance was independent of the dose and the mean value (166 lh-') was about twice that of the creatinine clearance (which did not significantly change as a result of E treatment), indicating that E is actively secreted into the renal tubules. As E was eliminated rapidly from the body (ts<2 h), no substantial accumulation of E is expected after multiple dose treatment.