PMID: 41039Oct 1, 1979

The effects of physiocochemical properties of pethidine and its basic metabolites on their buccal absorption and renal elimination

The Journal of Pharmacy and Pharmacology
K Chan

Abstract

The pKa values, RF values, partition coefficients between n-heptane and phosphate buffer (pH = 7.4), and buccal absorption tests of pethidine and its basic metabolites, norpethidine and pethidine N-oxide, have been determined. The amounts of these compounds recovered in the 48 h urine samples after intramuscular administration of pethidine (1.5 mg kg-1) to six healthy subjects varies with urinary pH values: the recovery from acidic urine (pH 5.0) is 15.2 to 52.0%, 6.7 to 12.9% and 0.2 to 2.3% of dose for pethidine, norpethidine and pethidine N-oxide respectively; in alkaline urine (pH 8.0) the values are 0.8 to 1.8%, 0.6 to 2.8% and 0.3 to 2.1% respectively. The physicochemical properties (pKa values, RF values, partition coefficients) and buccal absorption of pethidine, norpethidine and pethidine N-oxide are in good agreement with the pattern of their renal elimination in acidic and alkaline urine conditions. The contribution of the physiocochemical properties of pethidine and its metabolites to the drug's disposition in the body and the effect of urinary pH on its metabolism should be taken into account in pharmacokinetic studies and interpretation of intersubject variation in response to pethidine.

References

Apr 1, 1990·Pharmacology & Toxicology·L L ChristrupH Flachs
Sep 1, 1982·Journal of Clinical and Hospital Pharmacy·K ChanR G Sibeon
Sep 1, 1985·Journal of Clinical and Hospital Pharmacy·K Chan
Mar 18, 2005·The Journal of Pain : Official Journal of the American Pain Society·Vincent Launay-VacherGilbert Deray
Dec 1, 1981·British Journal of Clinical Pharmacology·G EdwardsS A Ward
Jul 1, 1987·Journal of Clinical Pharmacology·K ChanM L Orme
Mar 22, 2020·The Journal of Pharmacology and Experimental Therapeutics·Weize HuangNina Isoherranen

Citations

Apr 1, 1975·The Journal of Pharmacy and Pharmacology·K ChanM Mitchard
Aug 1, 1975·British Journal of Clinical Pharmacology·K ChanW D Wells
Nov 1, 1971·The Journal of Pharmacy and Pharmacology·M M Abdel-Monem, P S Portoghese
Apr 1, 1972·The Journal of Pharmacy and Pharmacology·M Mitchard
Nov 1, 1972·The Journal of Pharmacy and Pharmacology·M MitchardK Chan
Apr 1, 1963·British Journal of Pharmacology and Chemotherapy·A M ASATOORM L SIMENHOFF

Related Concepts

Metabolic Process, Cellular
Urine
Phosphate buffers
Buccal Surface
Meperidine
Meperidine Hydrochloride
Process of Absorption
Cheek Structure
Kidney
n-heptane

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