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Disposition of parenteral butorphanol in man


Drug Metabolism and Disposition: the Biological Fate of Chemicals 8(4): 230-235
Disposition of parenteral butorphanol in man
The metabolism and elimination of the analgesic agent 3H-butorphanol (l-3,14-dihydroxy-N-(cyclobutylmethyl)[15-3H]morphinan) tartrate were determined in man after therapeutic i.m. (2 mg) and i.v. (1 mg) doses. As judged from urinary excretion of radioactivity, the i.m. dose was completely absorbed. Butorphanol was rapidly distributed to tissues, had a plasma half-life of .apprx. 3 h, and was extensively metabolized prior to elimination. The major route of elimination was renal, with fecal excretion being a minor route. Hydroxybutorphanol [3,14-dihydroxy-N-(trans-3'-hydroxycyclobutylmethyl)morphinan] was isolated and identified as a major urinary metabolite and was present in the plasma. The disposition of butorphanol is compared and contrasted to the disposition of morphine and pentazocine.

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Accession: 005170924

PMID: 6105056

DOI: 10.1097/00132586-198106000-00020



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