Transdermal fentanyl for cancer pain: Repeated dose pharmacokinetics Journal Article
| Authors: | Portenoy, R. K.; Southam, M. A.; Gupta, S. K.; Lapin, J.; Layman, M.; Inturrisi, C. E.; Foley, K. M. |
| Article Title: | Transdermal fentanyl for cancer pain: Repeated dose pharmacokinetics |
| Abstract: | Background: The transdermal therapeutic system (fentanyl), or TTS(fentanyl), continuously delivers fentanyl for up to 72 h. The transdermal therapeutic system (fentanyl)-100 delivers approximately 100 μg/h. The repeated dose pharmacokinetics of this drug using the recommended dosing interval have not been evaluated previously and were determined in the present study. Methods: Blood samples were obtained from ten opioid-tolerant cancer patients who received five applications of TTS(fentanyl) at 72-h intervals. A sample of venous blood was taken before each dose; multiple samples were taken during and after the fifth application. A gas chromatographic/mass spectrometry method was used to assay fentanyl (limit of detection 0.2 ng/ml). Results: For the fifth dose, the mean (SD) maximum concentration was 2.6 (1.3) ng/ml and the mean (SD) area under the serum fentanyl concentration-time curve (0-72 h) was 116.9 (59.9). Following removal of the system, the mean (SD) apparent half-life was 21.9 (8.9) h. There were no differences among the serum fentanyl concentrations measured before the second through fifth doses. Fentanyl absorption was 47% complete at 24 h, 88% complete at 48 h, and 94% complete at 72 h. The mean (SD) dose delivered during the 72-h period was 4.3 (1.1) mg. A first-dose trough concentration predicted from fifth-dose kinetics and the actual first-dose trough concentration were very similar. Adverse effects ascribed to the transdermal system were minimal. Conclusions: These results suggest that steady-state serum concentrations are approached by the second dose of TTS(fentanyl) and that the kinetics are stable with repeated dosing. The apparent half-life following system removal is relatively long, indicating ongoing absorption from a subcutaneous depot. |
| Keywords: | adult; clinical article; aged; area under the curve; dose response; anorexia; mass spectrometry; gastrointestinal symptom; cancer pain; hypotension; erythema; drug absorption; drug blood level; drug half life; lethargy; drug delivery system; fentanyl; gas chromatography; maximum permissible dose; human; male; female; priority journal; article; transdermal drug administration; analgesics, opioid: fentanyl; anesthetic techniques: transdermal; pain, chronic: cancer; pharmacokinetics: transdermal fentanyl |
| Journal Title: | Anesthesiology |
| Volume: | 78 |
| Issue: | 1 |
| ISSN: | 0003-3022 |
| Publisher: | Lippincott Williams & Wilkins |
| Date Published: | 1993-01-01 |
| Start Page: | 36 |
| End Page: | 43 |
| Language: | English |
| DOI: | 10.1097/00000542-199301000-00007 |
| PUBMED: | 8424569 |
| PROVIDER: | scopus |
| DOI/URL: | |
| Notes: | Source: Scopus |
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