Beschreibung:
<jats:title>Abstract</jats:title><jats:p>The pharmacokinetics of etintidine (E), a potent H<jats:sub>2</jats:sub> blocker, were studied in 12 normal, fasted subjects. The subjects received five ascending doses of E HCI 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 administration, plasma E levels showed double peaks in half of the subjects. Mean C<jats:sub>max</jats:sub>., (0.42, 2.11, 3.82, 4.50, and 7.15 μg ml<jats:sup>−1</jats:sup>), AUC<jats:sub>0‐∞</jats:sub> (0.96, 4.94, 11.3, 17.5, and 24.5 h μg ml<jats:sup>−1</jats:sup>), 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 (16.6 lh<jats:sup>−1</jats:sup>) 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 (t<jats:sub>½</jats:sub><2 h), no substantial accumulation of E is expected after multiple dose treatment.</jats:p>