Abstract
The pharmacokinetics of nalbuphine were studied in 10 healthy volunteers on two separate occasions following administration by either the intravenous (20 mg) or oral (60 mg) route. After administration, serum concentrations of nalbuphine were measured for 12 h using a high pressure liquid chromatography assay, and pharmacokinetic parameters were derived using a three compartment model. After i.v. administration, elimination half-life was 222 (111-460) min (mean and range) and total body clearance was 1.5 (0.8-2.3) 1 min-1.Cmax after oral administration was 21.4 (6.0-36.2) ng ml-1 and tmax was 46.6 (15.3-89.0) min. Bioavailability of the oral preparation was 11.8 (6.1-20.1)%.
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Selected References
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- Aungst B. J., Lam G., Shefter E. Oral and rectal nalbuphine bioavailability: first-pass metabolism in rats and dogs. Biopharm Drug Dispos. 1985 Oct-Dec;6(4):413–421. doi: 10.1002/bdd.2510060407. [DOI] [PubMed] [Google Scholar]
- Bahar M., Rosen M., Vickers M. D. Self-administered nalbuphine, morphine and pethidine. Comparison, by intravenous route, following cholecystectomy. Anaesthesia. 1985 Jun;40(6):529–532. [PubMed] [Google Scholar]
- Beaver W. T., Feise G. A. A comparison of the analgesic effect of intramuscular nalbuphine and morphine in patients with postoperative pain. J Pharmacol Exp Ther. 1978 Feb;204(2):487–496. [PubMed] [Google Scholar]
- Beaver W. T., Feise G. A., Robb D. Analgesic effect of intramuscular and oral nalbuphine in postoperative pain. Clin Pharmacol Ther. 1981 Feb;29(2):174–180. doi: 10.1038/clpt.1981.28. [DOI] [PubMed] [Google Scholar]
- DiFazio C. A., Moscicki J. C., Magruder M. R. Anesthetic potency of nalbuphine and interaction with morphine in rats. Anesth Analg. 1981 Sep;60(9):629–633. [PubMed] [Google Scholar]
- Hull C. J. Pharmacokinetics and pharmacodynamics. Br J Anaesth. 1979 Jul;51(7):579–594. doi: 10.1093/bja/51.7.579. [DOI] [PubMed] [Google Scholar]
- Jasinski D. R., Mansky P. A. Evaluation of nalbuphine for abuse potential. Clin Pharmacol Ther. 1972 Jan-Feb;13(1):78–90. doi: 10.1002/cpt197213178. [DOI] [PubMed] [Google Scholar]
- Keegan M., Kay B. Detection of nalbuphine in plasma: an improved high-performance liquid chromatographic assay. J Chromatogr. 1984 Nov 9;311(1):223–226. doi: 10.1016/s0378-4347(00)84714-3. [DOI] [PubMed] [Google Scholar]
- Klein D. S. Nalbuphine and droperidol combination for local standby sedation. Anesthesiology. 1983 Apr;58(4):397–397. doi: 10.1097/00000542-198304000-00034. [DOI] [PubMed] [Google Scholar]
- Lake C. L., DiFazio C. A., Duckworth E. N., Moscicki J. C., Engle J. S., Durbin C. G. High-performance liquid chromatographic analysis of plasma levels of nalbuphine in cardiac surgical patients. J Chromatogr. 1982 Dec 10;233:410–416. doi: 10.1016/s0378-4347(00)81777-6. [DOI] [PubMed] [Google Scholar]
- Lo M. W., Juergens G. P., Whitney C. C., Jr Determination of nalbuphine in human plasma by automated high-performance liquid chromatography with electrochemical detection. Res Commun Chem Pathol Pharmacol. 1984 Jan;43(1):159–168. [PubMed] [Google Scholar]
- Moldenhauer C. C., Roach G. W., Finlayson D. C., Hug C. C., Jr, Kopel M. E., Tobia V., Kelly S. Nalbuphine antagonism of ventilatory depression following high-dose fentanyl anesthesia. Anesthesiology. 1985 May;62(5):647–650. [PubMed] [Google Scholar]
- Murphy M. R., Hug C. C., Jr The enflurane sparing effect of morphine, butorphanol, and nalbuphine. Anesthesiology. 1982 Dec;57(6):489–492. doi: 10.1097/00000542-198212000-00010. [DOI] [PubMed] [Google Scholar]
- Pinnock C. A., Bell A., Smith G. A comparison of nalbuphine and morphine as premedication agents for minor gynaecological surgery. Anaesthesia. 1985 Nov;40(11):1078–1081. doi: 10.1111/j.1365-2044.1985.tb10605.x. [DOI] [PubMed] [Google Scholar]
- Ramsay J. G., Higgs B. D., Wynands J. E., Robbins R., Townsend G. E. Early extubation after high-dose fentanyl anaesthesia for aortocoronary bypass surgery: reversal of respiratory depression with low-dose nalbuphine. Can Anaesth Soc J. 1985 Nov;32(6):597–606. doi: 10.1007/BF03011405. [DOI] [PubMed] [Google Scholar]
- Romagnoli A., Keats A. S. Ceiling effect for respiratory depression by nalbuphine. Clin Pharmacol Ther. 1980 Apr;27(4):478–485. doi: 10.1038/clpt.1980.67. [DOI] [PubMed] [Google Scholar]