Use of the mixed agonist-antagonist nalbuphine in opioid based analgesia

Acute Pain

Volumn 6, Issue 1, 2004, Pages 29-39

  Gunion, Mark W ^a   Marchionne, Anna Maria ^a,b   Anderson, Corrie T M ^a,b  

^a UNIVERSITY OF WASHINGTON MEDICAL CENTER   (United States)

^b SEATTLE CHILDREN S RESEARCH INSTITUTE   (United States)

Author keywords

Kappa receptor; Mixed agonist antagonist; Mu receptor; Nalbuphine; Opioid side effects

Indexed keywords

3,4 DICHLORO N METHYL N [2 (1 PYRROLIDINYL)CYCLOHEXYL]BENZENEACETAMIDE METHANESULFONATE; ADL 10 0101; BETA ENDORPHIN; DELTA OPIATE RECEPTOR; DIPHENHYDRAMINE; DYNORPHIN A; DYNORPHIN B; ENDOMORPHIN 1; ENDOMORPHIN 2; FENTANYL; HISTAMINE H1 RECEPTOR ANTAGONIST; HYDROMORPHONE; KAPPA OPIATE RECEPTOR; LEUCINE ENKEPHALIN; LOCAL ANESTHETIC AGENT; METENKEPHALIN; METHADONE; MORPHINE; MU OPIATE RECEPTOR; MU OPIATE RECEPTOR AGONIST; NALBUPHINE; NALOXONE; OPIATE AGONIST; OPIATE ANTAGONIST; PETHIDINE; SIGMA OPIATE RECEPTOR;

ANALGESIA; BINDING AFFINITY; BRADYCARDIA; CONSTIPATION; CYANOSIS; DRUG ABSORPTION; DRUG ABUSE; DRUG ANTAGONISM; DRUG COST; DRUG DEPENDENCE; DRUG EFFECT; DRUG EFFICACY; DRUG ELIMINATION; DRUG FORMULATION; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG TOLERANCE; FETUS DISEASE; GASTROINTESTINAL SYMPTOM; HUMAN; LABOR PAIN; MUSCLE HYPOTONIA; NAUSEA; NEWBORN DISEASE; NONHUMAN; PAIN; PAIN ASSESSMENT; PRIORITY JOURNAL; PROTEIN LOCALIZATION; PRURITUS; RECEPTOR BINDING; RECEPTOR BLOCKING; RESPIRATION DEPRESSION; REVIEW; SEDATION; SIDE EFFECT; TOOTH PAIN; URINE RETENTION; VOMITING;

EID: 2342577496     PISSN: 13660071     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.acpain.2004.02.002     Document Type: Review

References (87)

1. Sechzer P.H. Patient-controlled anagesia (PCA): a retrospective. Anesthesiology. 72:1990;735-736
2. Ready L.B. Patient-controlled analgesia - does it provide more than comfort? Can. J. Anesth. 37:1990;719-721
3. Krechel S.W., Helikson M.A., Kittle D., Eggers G.W. Jr. Intrathecal morphine (ITM) for postoperative pain control in children: a comparison with nalbuphine patient controlled analgesia (PCA). Paed. Anaesth. 5:1995;177-183
4. Gaukroger PB, Patient-controlled analgesia in children. In: Schechter NL, Berde CB, Yaster M, editors. Pain in infants, children, and adolescents. Baltimore: Williams & Wilkins; 1993. p. 203-11.
5. Shin D., Kim S., Kim C.S., Kim H.-S. Postoperative pain management using intravenous patient-controlled analgesia for pediatric patients. J. Craniofac. Surg. 12:2001;129-133
6. Beyer J.E. Judging the effectiveness of analgesia for children and adolescents during vaso-occulsive events of sickle cell disease. J. Pain Sympt. Manage. 19:2000;63-72
7. Anderson C.T.M., Brill J.E. Advances in pediatric pain management. Sem. Anesth. 11:1992;158-171
8. Morton NS, Simple and systemic management of postoperative pain. In: Finley GA, McGrath PJ, editors. Progress in pain research and management: acute and procedure pain in infants and children. 20th ed. Seattle: IASP Press; 2001. p. 13-32.
9. Pasternak GW. The opiate receptors. Clifton, New Jersey: The Humana Press; 1988.
10. Gutstein H.B, Akil H, Opioid analgesics. In: Hardman JG, Limbird LE, editors. Goodman & Gilman's The pharmacological basis of therapeutics. 10th ed. New York: McGraw-Hill; 2001. p. 569-619.
11. Wilson A.M., Soignier R.D., Zadina J.E., Kastin A.J., Nores W.L., Olson R.D., et al. Dissociation of analgesic and rewarding effects of endomorphin-1 in rats. Peptides. 21:2000;1871-1874
12. Chen J.-C., Smith E.R., Cahill M., Cohen R., Fishman J.B. The opioid receptor binding of dezocine, morphine, fentanuyl, butorphanol, and nalbuphine. Life Sci. 52:1993;389-396
13. Pick C.G., Paul D., Pasternak G.W. Nalbuphine, a mixed kappa1 and kappa3 analgesic in mice. J. Pharmacol. Exp. Ther. 262:1992;1044-1050
14. Pasternak G.W. Opiate, enkephalin, and endorphin analgesia: relations to a single subpopulation of opiate receptors. Neurology. 31:1981;1311-1315
15. Zadina J.E., Martin-Schild S., Gerall A.A., Kastin A.J., Hackler L., Ge L.-J., et al. Endomorphins: novel endogenous mu-opiate receptor agonists in regions of high mu-opiate receptor density. Gastroenterology. 897:1999;136-144
16. Zukin RS, Zukin SR. The sigma receptor. In: Pasternak GW, editor. The opiate receptors. Clifton, New Jersey: The Humana Press; 1988. p. 143-63 [Chapter 5].
17. Schmidt W.K., Tam S.W., Shotzberger G.S., Smith D.W. Jr., Clark R., Vernier V.G. Nalbuphine. Drug Alcohol Dep. 14:1985;339-362
18. DeSouza E.B., Schmidt W.K., Kuhar M.J. Nalbuphine: an autoradiographic opioid receptor binding profile in the central nervous system of an agonist/antagonist analgesic. J. Pharmacol. Exp. Ther. 244:1988;391-402
19. Craft R.M., Bernal S.A. Sex differences in opioid antinociception: kappa and 'mixed action' agonists. Drug Alcohol. Dep. 63:2001;215-228
20. Gear R.W., Miaskowski C., Gordon N.C., Paul S.M., Heller P.H., Levine J.D. Kappa-opioid produce significantly greater analgesia in women than in men. Nat. Med. 2:1996;1248-1250
21. Wood PL, Iyengar S. Central actions of opiates and opioid peptides: in vivo evidence for opioid receptor multiplicity. In: Pasternak GW, editor. The opiate receptors. Clifton, New Jersey: The Humana Press; 1988. p. 307-56.
22. Schmauss C., Yaksh T.L. In vivo studies on spinal opiate receptor systems mediating antinociception. II. Pharmacological profiles suggesting a differential association of mu, delta and kappa receptors with visceral chemical and cutaneous thermal stimuli in the rat. J. Pharmacol. Exp. Ther. 228:1984;1-12
23. Schmauss C., Doherty C., Yaksh T.L. The analgetic effects of an intrathecally administered partial opiate agonist, nalbuphine hydrochloride. Eur. J. Pharmacol. 86:1983;1-7
24. Fioramonti J., Bueno L. Centrally acting agents and visceral sensitivity. Gut. 51(Suppl 1):2002;i91-i95
25. Wessendorf M.W., Dooyema J. Coexistence of kappa-and delta-opioid receptors in rat spinal cord axons. Neurosci. Lett. 298:2001;151-154
26. Eisenach J.C., Carpenter R., Curry R. Analgesia from a peripherally active κ-opioid receptor agonist in patients with chronic pancreatitis. Pain. 101:2003;89-95
27. Loomis C.W., Penning J., Milne B. A study of the analgesic interaction between intrathecal morphine and subcutaneous nalbuphine in the rat. Anesthesiology. 71:1989;704-710
28. Ho S.T., Wang J.J., Hu O.Y., Tzeng J.I., Liaw W.J. Comparison of PCA nalbuphine and morphine in Chinese gynecologic patients. Acta Anaesthesiol. Sin. 36:1998;65-70
29. Fournier R., VanGessel E., Macksay M., Gamulin Z. Onset and offset of intrathecal morphine versus nalbuphine for postoperative pain relief after total hip replacement. Acta Anaesthesiol. Scand. 44:2000;940-945
30. Culebras X., Gaggero G., Zatloukal J., Kern C., Marti R.-A. Advantages of intrathecal nalbuphine, compared with intrathecal morphine, after Cesarean delivery: an evaluation of postoperative analgesia and adverse effects. Anesth. Analg. 91:2000;601-605
31. Yamamoto T., Ohno M., Ueki S.A. selective k-opioid agonist, U-50, 488H, blocks the development of tolerance to morphine analgesia in rats. Eur. J. Pharmacol. 156:1988;173-176
32. Pchelintsev M.V., Gorbacheva E.N., Zvartau E.E. Simple methodology of assessment of analgesics' addictive potential in mice. Pharm. Biochem. Behav. 39:1991;873-876
33. Etches R.C., Sandler A.N., Lawson S.L. A comparison of the analgesic and respiratory effects of epidural nalbuphine or morphine in postthoracotomy patients. Anesthesiology. 75:1991;9-14
34. Jaffe R.S., Moldenhauer C.C., Hug C.C., Finlayson D.C., Tobia V., Kopel M.E. Nalbuphine antagonism of fentanyl-induced ventilatory depression: a randomized trial. Anesthesiology. 68:1988;254-260
35. Zsigmond E.K., Winnie A.P., Raza S.M.A., Wang X.Y., Barabas E. Nalbuphine as an analgesic component in balanced anesthesia for cardiac surgery. Anesth. Analg. 66:1987;1155-1164
36. Pugh G.C., Drummond G.B. A dose-response study with nalbuphine hydrochloride for pain in patients after upper abdominal surgery. Br. J. Anaesth. 59:1987;1356-1363
37. Gal T.J., DiFazio C.A., Moscicki J. Analgesic and respiratory depressant activity of nalbuphine: a comparison with morphine. Anesthesiology. 57:1982;367-374
38. Dan U., Rabinovici Y., Barkai G., Modan M., Etchin A., Mashiach S. Intravenous pethidine and nalbuphine during labor: a prospective double-blind comparative study. Gynecol. Obstet. Invest. 32:1991;39-43
39. Wahab S.A., Askalani A.H., Amar R.A., Ramadan M.E., Neweigy S.B., Saleh A.A. Effect of some recent analgesics on labor pain and maternal and fetal blood gases and pH. Int. J. Gynecol. Obstet. 26:1988;75-80
40. Wilson C.M., McClean E., Moore J., Dundee J.W. A double-blind comparison of intramuscular pethidine and nalbuphine in labor. Anaesthesia. 41:1986;1207-1213
41. Frank M., McAteer E.J., Cattermole R., Loughnan B., Stafford L.B., Hitchcock A.M. Nalbuphine for obstetric analgesia. A comparison of nalbuphine with pethidine for pain relief in labour when administered by patient-controlled analgesia (PCA). Anaesthesia. 42:1987;697-703
42. Podlas J., Breland B.B. Patient-controlled analgesia with nalbuphine during labor. Obstet. Gynecol. 70:1987;202-204
43. Morselli P.L., Rovei V. Placental transfer of pethidine and norpethidine and their pharmacokinetics in the newborn. Eur. J. Clin. Pharmacol. 18:1980;25-30
44. Giannina G., Guzman E.R., Lai Y.-L., Lake M.F., Cernadas M., Vintzileos A.M. Comparison of the effects of meperidine and nalbuphine on intrapartum fetal heart rate tracings. Obstet. Gynecol. 86:1995;441-445
45. Wilson S.J., Errick J.K., Balkon J. Pharmacokinetics of nalbuphine during parturition. Am. J. Obstet. Gynecol. 155:1986;340-344
46. Dadabhoy Z.P., Tapia D.P., Zsigmond E.K. Transplacental transfer of nalbuphine in patients undergoing Cesarean section. Anesth. Analg. 64:1985;205
47. Sgro C., Escousse A., Tennenbaum D., Gouyon J.B. Perinatal adverse effects of nalbuphine given during labour. Lancet. 336:1990;1070
48. Guillonneau M., Jacqz-Aigrain E., DeCrepy A., Zeggout H. Perinatal adverse effects of nalbuphine given during parturition. Lancet. 335:1990;1588
49. Sherer D.M., Cooper E.M., Spoor C., Serletti B.L., Woods J.R. Jr. Resolution of marked intrapartum fetal tachycardia following intravenous nalbuphine hydrochloride. Am. J. Perinatol. 11:1994;367-368
50. Poehlmann S., Pinette M., Stubblefield P. Effect of labor analgesia with nalbuphine hydrochloride of fetal response to vibroacoustic stimulation. J. Reprod. Med. 40:1995;707-710
51. Feinstein S.J., Lodeiro J.G., Vintzileos A.M., Campbell W.A., Montgomery J.T., Nochimson D.J. Sinusoidal fetal heart rate pattern after administration of nalbuphine hydrochloride: a case report. Am. J. Obstet. Gynecol. 154:1986;159-160
52. Rosow C. Agonist-antagonist opioids: theory and clinical practice. Can. J. Anaesth. 36:1989;S5-S8
53. Morselli P.L., Franco-Morselli R., Bossi L. Clinical pharmacokinetics in newborns and infants: age-related differences and therapeutic implications. Clin. Pharmacokinet. 5:1980;485-527
54. Nicolle E., Devillier P., Delanoy B., Durand C., Bessard G. Therapeutic monitoring of nalbuphine: transplacental transfer and estimated pharmacokinetics in the neonate. Eur. J. Clin. Pharmacol. 49:1996;485-489
55. Cox BM. Peripheral actions mediated by opiate receptors. In: Pasternak GW, editor. The opiate receptors. Clifton, New Jersey: The Humana Press; 1988. p. 357-422.
56. Muldoon S.M., Donlon M.A., Tood R., Helgeson E.A., Freas W. Plasma histamine and hemodynamic responses following administration of nalbuphine and morphine. Agents Actions. 15:1984;229-234
57. Wyatt EL, Sutter SH, Drake LA. Dermatological pharmacology. In: Hardman JG, Limbird LE, editors. The pharmacological basis of therapeutics. 10th ed. New York: McGraw-Hill; 2001. p. 1795-818.
58. Thomas D.A., Williams G.M., Iwata K., Kenshalo D.R. Jr., Dubner R. Effects of central administration of opioids on facial scratching in monkeys. Brain Res. 585:1992;315-317
59. Woods M.P., Rayburn W.F., McIntosh D.G., Scott J.C. Jr., Smith M.L., Anderson J.R. Nalbuphine after major gynecologic surgery. Comparison of patient-controlled analgesia and intramuscular injections. J. Reprod. Med. 36:1991;647-650
60. Somrat C., Oranuch K., Ketchada U., Siriprapa S., Thipawan R. Optimal dose of nalbuphine for treatment of intrathecal-morphine induced pruritus after Caesarean section. J. Obstet. Gynaecol. Res. 25:1999;209-213
61. Charuluxananan S., Kyokong O., Somboonviboon W., Lertmaharit S., Ngamprasertwong P., Nimcharoendee K. Nalbuphine versus propofol for treatment of intrathecal morphine-induced pruritus after cesarean delivery. Anesth. Analg. 93:2001;162-165
62. Cohen S.E., Ratner E.F., Kreitzman T.R., Archer J.H., Mignano L.R. Nalbuphine is better than naloxone for treatment of side effects after epidural morphine. Anesth. Analg. 75:1992;747-752
63. Davies G.G., From R. A blinded study using nalbuphine for prevention of pruritus induced by epidural fentanyl. Anesthesiology. 69:1988;763-765
64. Parker R.K., Holtmann B., White P.F. Patient-controlled epidural analgesia: interactions between nalbuphine and hydromorphone. Anesth. Analg. 84:1997;757-763
65. Teter K.A., Viellion G., Keating E.M. Patient controlled analgesia and GI dysfunction. Orthop. Nurs. 9:1990;51-56
66. Humphreys H.K., Fleming N.W. Opioid-induced spasm of the sphincter of Oddi apparently reversed by nalbuphine. Anesth. Analg. 74:1992;308-310
67. Murphy D.B., Sutton J.A., Prescott L.F., Murphy M.B. Opioid-induced delay in gastric emptying: a peripheral mechanism in humans. Anesthesiology. 87:1997;765-770
68. Shook J.E., Pelton J.T., Hruby V.J., Burks T.F. Peptide opioid antagonist separates peripheral and central opioid antitransit effects. J. Pharmacol. Exp. Ther. 243:1987;492-500
69. Riviere P.J.M., Pascaud X., Chevalier E., LeGallou B., Junien J.-L. Fedotozine reverses ileus induced by surgery or peritonitis: action at peripheral κ-opioid receptors. Gastroenterology. 104:1993;724-731
70. Malinovsky J.-M., Lepage J.-Y., Karam G., Pinaud M. Nalbuphine reverses urinary effects of epidural morphine: a case report. J. Clin. Anesth. 14:2002;535-538
71. Baxter A.D., Samson B., Penning J., Doran R., Dube L.M. Prevention of epidural morphine-induced respiratory depression with intravenous nalbuphine infusion in post-thoracotomy patients. Can. J. Anaesth. 36:1989;503-509
72. Penning J.P., Samson B., Baxter A.D. Reversal of epidural morphine-induced respiratory depression and pruritus with nalbuphine. Can. J. Anaesth. 35:1988;599-604
73. Bailey P.L., Clark N.J., Pace N.L., Stanley T.H., East K.A., van Vreeswijk H., et al. Antagonism of postoperative opioid-induced respiratory depression: nalbuphine versus naloxone. Anesth. Analg. 66:1987;1109-1114
74. Blaise G.A., McMichan J.C., Nugent M., Hollier L.H. Nalbuphine produces side-effects while reversing narcotic-induced respiratory depression. Anesth. Analg. 65:1986;S19
75. Romagnoli A., Keats A.S. Ceiling effect for respiratory depression by nalbuphine. Clin. Pharmacol. Ther. 27:1980;478-485
76. Lee S.-C., Wang J.-J., Ho S.-T., Tao P.-L. Nalbuphine coadministered with morphine prevents tolerance and dependence. Anesth. Analg. 84:1997;810-815
77. Fang J.Y., Sung K.C., Hu O.Y., Chen H.Y. Transdermal delivery of nalbuphine and nalbuphine pivalate from hydrogels by passive diffusion and iontophoresis. Arzneimittelforschung. 51:2001;408-413
78. Yen S.Y., Sung K.C., Wang J.J., Yoa-PuHu O. Controlled release of nalbuphine propionate from biodegradable microspheres: in vitro and in vivo studies. Int. J. Pharm. 220:2001;91-99
79. Rawal N., Nuutinen L., Raj P.P., Lovering S.L., Gobuty A.H., Hargardine J., et al. Behavioral and histopathologic effects following intrathecal administration of butorphanol, sufentanil, and nalbuphine in sheep. Anesthesiology. 75:1991;1025-1034
80. Clinical practice guideline for acute pain management: operative or medical procedures and trauma (publ. no. 92-0032). Agency for Health Care Policy and Research, USPHS, 1992.
81. Krenn H., Oczenski W., Jellinek H., Krumpl-Stroher M., Schweitzer E., Fitzgerald R.D. Nalbuphine by PCA-pump for analgesia following hysterectomy: bolus application versus continuous infusion with bolus application. Eur. J. Pain. 5:2001;219-226
82. Chalmers P.C., Lang C.M., Greenhouse B.B. The use of nalbuphine in association with epidural narcotics. Anesthesiol. Rev. 15:1988;21-27
83. Jaillon P., Gardin M.E., Lecocq B., Richard M.O., Meignan S., Blondel Y., et al. Pharmacokinetics of nalbuphine in infants, young healthy volunteers, and elderly patients. Clin. Pharmacol. Ther. 46:1989;226-233
84. Houlihan K.P.G., Mitchel R.G., Flapan A.D., Steedman D.J. Excessive morphine requirements after pre-hospital nalbuphine analgesia. J. Accid. Emerg. Med. 16:1999;29-31
85. Mills C.A., Flacke J.W., Flacke W.E., Bloor B.C., Liu M.D. Narcotic reversal in hypercapnic dogs: comparison of naloxone and nalbuphine. Can. J. Anaesth. 37:1990;238-244
86. DesMarteau J.K., Cassot A.L. Acute pulmonary edema resulting from nalbuphine reversal of fentanyl-induced respiratory depression. Anesthesiology. 65:1986;237
87. Prough D.S., Roy R., Bumgarner J., Shannon G. Acute pulmonary edema in healthy teenagers following conservative doses of intravenous naloxone. Anesthesiology. 60:1984;485-486