Presystemic metabolism of meperidine to normeperidine in normal and cirrhotic subjects

Susan M. Pond, Theodore Tong, Neal L. Bertowitz, Peyton Jacob, Jean Rigod

Research output: Contribution to journalArticlepeer-review

43 Scopus citations


Plasma concentrations and urinary excretion of meperidine and its metabolite normeperidine were determined after intravenous and oral administration to II men; five men had hepatic cirrohosis and six were normal. Systemic clearance of meperidine was smaller and bioavailability and half-life greater in the cirrhotic patients than in the normal subjects. Plasma concentrations and 24-hr urinary excretion of normeperidine was lower and persistence of normeperidine in plasma longer in the patients with cirrhosis. The route of administration did not alter the fraction of normeperidine generated from meperidine. The results suggest that in patients requiring repeated meperidine dosage the drug should be taken parenterally rather than orally to allow maximal analgesia and minimal formation of normeperidine. Patients with cirrhosis may be relatively protected from normeperidine toxicity because of impaired formation, but the risk of cumulative toxicity may be greater than in normal subjects because of slower elimination of the metabolite and greater sensitivity to the effects of narcotics on the central nervous system.

Original languageEnglish (US)
Pages (from-to)183-188
Number of pages6
JournalClinical Pharmacology and Therapeutics
Issue number2
StatePublished - Aug 1981

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)


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