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Research ArticleArticle

METABOLISM AND DISPOSITION OF METHYLPHENIDATE-14C: STUDIES IN MAN AND ANIMALS

B. A. Faraj, Z. H. Israili, J. M. Perel, M. L. Jenkins, S. G. Holtzman, S. A. Cucinell and P. G. Dayton
Journal of Pharmacology and Experimental Therapeutics December 1974, 191 (3) 535-547;
B. A. Faraj
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Z. H. Israili
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J. M. Perel
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M. L. Jenkins
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S. G. Holtzman
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S. A. Cucinell
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P. G. Dayton
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Abstract

Threo-dl-methylphenidate-14C·HCl (MEPH-14C·HCl) was found to be extensively metabolized in man, dog, rat and mouse. Pronounced species differences in the metabolism of the drug were found. In human subjects, plasma levels of MEPH-14C were found always to be much higher after i.v. than after oral administration. After oral administration, 50 and 90% of the 14C was excreted in urine in 8 and 48 hours, respectively. This suggests essentially complete absorption of MEPH. The main urinary metabolite was the deesterified product, ritalinic acid (RA), accounting for 80% of the dose. Upon i.v. administration of MEPH-14C·HCl to dogs, 50 to 60% of the radioactivity was excreted in 7-hour urine. The major metabolites in dog urine were RA and threo-dl-2-phenyl-2-(2'-piperidyl-6'-one) acetic acid (oxo-RA). In rats, both after i.p. and oral administration of MEPH-14C·HCl, 50 to 60% of the 14C was eliminated in urine and 30 to 40% in feces within 48 hours. Significant biliary excretion of 14C (25-30% in 12 hours) was found in bile-cannulated rats. The major metabolites in rat urine besides RA were threo-dl-2-(p-hydroxyphenyl)-2-(2'-piperidyl) acetic acid (p-OH RA), its methyl ester (p-OH MEPH)and the glucuronide conjugate of p-OH RA. The locomotor activity of MEPH, certain metabolites and N-acetyl MEPH was studied in mice.

Footnotes

    • Received April 22, 1974.
    • Accepted July 26, 1974.
  • © 1974 by The Williams & Wilkins Co.

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Journal of Pharmacology and Experimental Therapeutics
Vol. 191, Issue 3
1 Dec 1974
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Research ArticleArticle

METABOLISM AND DISPOSITION OF METHYLPHENIDATE-14C: STUDIES IN MAN AND ANIMALS

B. A. Faraj, Z. H. Israili, J. M. Perel, M. L. Jenkins, S. G. Holtzman, S. A. Cucinell and P. G. Dayton
Journal of Pharmacology and Experimental Therapeutics December 1, 1974, 191 (3) 535-547;

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Research ArticleArticle

METABOLISM AND DISPOSITION OF METHYLPHENIDATE-14C: STUDIES IN MAN AND ANIMALS

B. A. Faraj, Z. H. Israili, J. M. Perel, M. L. Jenkins, S. G. Holtzman, S. A. Cucinell and P. G. Dayton
Journal of Pharmacology and Experimental Therapeutics December 1, 1974, 191 (3) 535-547;
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