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Gastric and biliary excretion of meperidine in man
Author(s) -
Dunkerley R.,
Johnson R.,
Schenker S.,
Wilkinson G. R.
Publication year - 1976
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1002/cpt1976205546
Subject(s) - pharmacokinetics , basal (medicine) , chemistry , stimulation , medicine , stomach , endocrinology , anesthesia , insulin
The role and importance of enterogastric secretion in the disposition and elimination of the weak base, meperidine (pKa 8.63), was studied after intravenous administration (50 mg) of the drug to 6 normal volunteers. Continuous collection of the gastric fluid over a 4‐hr period demonstrated the establishment of high gastric fluid/plasma concentration ratios for meperidine (mean about 50, range, 10 to 200). However, the total amount of drug recovered, even after correction for incomplete collection, was only a small percentage of the administered dose. Under basal conditions a mean ± SE of 1.9 ± 0.3 mg, equivalent to 3.7% ofthe administered dose, wasfound in the total gastric aspirate. Stimulation of gastric secretion by subcutaneous injection of betazoie (1.5 mg/kg) increased this recovery to 3.6 ± 0.3 mg (7.2%) primarily due to the increase in gastric volume output. Aspiration of the gastric fluid in either the basal or stimulated situation had no observable effect upon the plasma concentration/time profile of meperidine whether assessed by the terminal half‐life, t ½ β or the plasma clearance; control values were 3.8 ± 0.5 hr and 1,190 ± 130 ml/min, respectively. In 2 subjects “bile fluid” was also collected for 2.5 hr and found to contain less than 0.2% of the administered dose. Enterosystemic recycling is therefore of minor importance in the disposition and elimination of meperidine in man.