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Journal of Pharmacology And Experimental Therapeutics, Vol. 96, Issue 4, 477-484, 1949
Copyright © 1949 by American Society for Pharmacology and Experimental Therapeutics


THE ABSORPTION, DISTRIBUTION AND EXCRETION OF ISONIPECAINE (DEMEROL)

E. Leong Way 1, Abraham I. Gimble 2, William P. McKelway 2, Helen Ross 2, Chen-Yu Sung 2, and Homer Ellsworth 2

1 University of California, College of Pharmacy and Division of Pharmacology, School of Medicine, San Francisco, Calfornia.
2 Department of Pharmacology and the Department of Obstetrics, The George Washington University, School of Medicine, Washington, D. C.

1. After administration of isonipecaine (Demerol) to rats the compound concentrates mainly in the kidneys, spleen, lungs and liver. Appreciable levels are attained in the brain and lower concentrations in heart and muscle.

2. After repeated administration of isonipecaine three times daily for several days virtually no isonipecaine could be recovered from the animals 24 hours later.

3. Isonipecaine is rapidly and almost totally absorbed after oral administration.

4. Isonipecaine or its metabolite(s) is excreted to some extent in saliva; but no isonipecaine was detected in the milk of individuals receiving the compound.

5. Less than 5 per cent of the total oral isonipecaine dosage was separated and characterized from urine by countercurrent techniques.

6. An even smaller amount of isonipecaine (less than one per cent) was found in the urine of newborns whose mothers had previously received isonipecaine during the first stage of delivery.

Submitted on May 31, 1949







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Copyright © 1949 by the American Society for Pharmacology and Experimental Therapeutics.