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The Pharmacokinetics of Butorphanol and its Metabolites at Steady State Following Nasal Administration in Humans by NIMISH N. VACHHARAJANI; WEN CHYI SHYU; DOUGLAS S. GREENE; RASHMI H. BARBHAIYA is a Medicine article available to read on EtoBox.

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The single-dose and steady state pharmacokinetics of butorphanol and its metabolites, hydroxybutorphanol (HO-B) and norbutorphanol (NOR-B), were studied in nine healthy male volunteers. Each subject received a single 1 mg dose of butorphanol on days 1 and 6, and a 1 mg dose every 6 h (q6h) on days 2-5, via nasal administration. Serial blood and urine samples were collected for 24 h after the first dose on day 1 and for 72 h at steady state on day 6. Plasma and urine samples were analyzed for free and conjugated butorphanol, HO-B, and NOR-B. The plasma samples were analyzed using validated gas chromatography-electron capture negative chemical ionization-mass spectrometric methods and the urine samples were analyzed using a validated HPLC procedure. In the plasma, conjugated metabolites were not detected and only trace amounts of NOR-B were present. Therefore, pharmacokinetic parameters could not be estimated for NOR-B and conjugated metabolites. AUC0-->infinity of butorphanol after the first dose and AUC0-->tau at steady state were not statistically different, indicating that the kinetics of butorphanol were not significantly altered after repeated dosing. Steady state levels of but

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Author

NIMISH N. VACHHARAJANI; WEN CHYI SHYU; DOUGLAS S. GREENE; RASHMI H. BARBHAIYA

Publisher

John Wiley and Sons; Wiley (John Wiley & Sons); John Wiley & Sons Inc.; Wiley (ISSN 0142-2782)

Published

1997

Language

EN

Field

Medicine (Health Sciences)