Les bases pharmacologiques de la rotation des opioïdes
Rev Med Suisse
2001; volume -3.
21285
Résumé
L'utilisation accrue de morphine dans le traitement de la douleur cancéreuse a entraîné l'émergence de phénomènes neurotoxiques méconnus jusqu'alors. La rotation des opioïdes, c'est-à-dire la substitution séquentielle d'opioïdes de même palier antalgique, s'est révélée une stratégie efficace dans cette situation. Les bases pharmacologiques sous-tendant le bénéfice observé ne sont pas bien élucidées et comprennent plusieurs mécanismes physiopathologiques dont l'activité de chaque molécule sur différents récepteurs, opioïdes ou non, la présence de métabolites actifs, l'efficacité intrinsèque de l'opioïde et la réponse individuelle à l'action analgésique.
Bibliographie
1 Twycross R. Opioids. Dans : Wall P, Melzack R, editors. Textbook of pain. 4th ed. Edinburgh : Churchill Livingstone, 1999 ; 1187-215.
2 Daeninck PJ, Bruera E. Opioid use in cancer pain. Is a more liberal approach enhancing toxicity ? Acta Anaesthesiol Scand 1999 ; 43 : 924-38.
3 Galer B, Coyle N, Pasternak G, Portenoy R. Individual variability in the response to different opioids : Report of five cases. Pain 1992 ; 49 : 87-91.
4 MacDonald N, Der L, Allan S, Champion P. Opioid hyperexcitability : The application of alternate opioid therapy. Pain 1993 ; 53 : 353-5.
5 Sjogren P, Jonsson T, Jensen NH, Drenck NE, Staehelin Jensen T. Hyperalgesia and myoclonus in terminal cancer patients treated with continuous intravenous morphine. Pain 1993 ; 55 : 93-7.
6 de Stoutz N, Bruera E, Suarez-Almazor M. Opioid rotation for toxicity reduction in terminal cancer patients. J Pain Symptom Manage 1995 ; 10 : 378-83.
7 Ashby M, Martin P, Jackson K. Opioid substitution to reduce adverse effects in cancer pain management. Med J Austr 1999 ; 170 : 68-71.
8 Reisine T, Pasternak G. Opioid analgesics and antagonists. Dans : Hardman J, Limbird L, Molinoff P, Ruddon R, Goodman Gilman A, editors. The pharmacological basis of therapeutics. 9th ed. New York : McGraw-Hill, 1996 ; 521-55.
9 Cox BM. Opioid receptor-G protein interactions : Acute and chronic effects of opioids. Dans : Herz A, editor. Opioids I. 1st ed. Berlin : Springer-
Verlag, 1993 ; 145-88.
10 Mogil J, Sternberg W, Marek P, et al. The genetics of pain and pain inhibition. Proc Natl Acad Sci 1996 ; 93 : 3048-55.
11 Ebert B, Thorkildsen C, Andersen S, Christrup L, Hjeds H. Opioid analgesics as noncompetitive N-methyl-D-aspartate antagonists. Biochem Pharmacol 1998 ; 56 : 553-9.
12 Mao J, Price D, Mayer D. Mechanisms of hyperalgesia and morphine tolerance : A current view of their possible interactions. Pain 1995 ; 62 : 259-74.
13 Davis A, Inturrisi C. d-Methadone blocks morphine tolerance and N-methyl--D-aspartate-induced hyperalgesia. J Pharmacol Exp Ther 1999 ; 289 : 1048-53.
14 Szeto H, Inturrisi C, Houde R, et al. Accumulation of normeperidine, an active metabolite of meperidine, in patients with renal failure or cancer. Ann Intern Med 1977 ; 86 : 738-41.
15 Kaiko R, Foley K, Grabinski P, et al. Central nervous system excitatory effects of meperidine in cancer patients. Ann Neurol 1983 ; 13 : 180-5.
16 Smith M, Watt J, Cramond T. Morphine-3-glucuronide a potent antagonist of morphine analgesia. Life Sci 1990 ; 47 : 579-85.
17 Gong QL, Hedner J, Björkman R, Hedner T. Morphine-3-glucuronide may functionally antagonize morphine-6-glucuronide induced antinociception and ventilatory depression in the rat. Pain 1992 ; 48 : 249-55.
18 Faura C, Olaso MJ, García Cabanes C, Horga J. Lack of morphine-6-glucuronide antinociception after morphine treatment. Is morphine-3-glucuronide involved ? Pain 1996 ; 65 : 25-30.
19 Bartlett S, Cramond T, Smith M. The excitatory effects of morphine-3-glucuronide are attenuated by LY274614, a competitive NMDA receptor antagonist, and by midazolam, an agonist at the benzodiazepine site on the GABAA receptor complex. Life Sci 1994 ; 54 : 687-94.
20 Osborne R, Joel S, Trew D, Slevin M. Morphine and metabolite behavior after different routes of morphine administration : Demonstration of the importance of the active metabolite morphine-6-glucuronide. Clin Pharmacol Ther 1990 ; 47 : 12-9.
21 Osborne R, Joel S, Grebenik K, Trew D, Slevin M. The pharmacokinetics of morphine and morphine glucuronides in kidney failure. Clin Pharmacol Ther 1993 ; 54 : 158-67.
22 Peterson GM, Randall CTC, Paterson J. Plasma levels of morphine and morphine glucuronides in the treatment of cancer pain : Relationship to renal function and route of administration. Eur J Clin Pharmacol 1990 ; 38 : 121-4.
23 Portenoy R, Foley K, Stulman J, et al. Plasma morphine and morphine-6-glucuronide during chronic morphine therapy for cancer pain : Plasma profiles, steady-state concentrations and the consequences of renal failure. Pain 1991 ; 47 : 13-9.
24 Hagen N, Foley K, Cerbone D, Portenoy R, Inturrisi C. Chronic nausea and morphine-6-glucuronide. J Pain Symptom Manag 1991 ; 6 : 125-8.
25 Wright A, Nocente ML, Smith M. Hydromorphone-3-glucuronide : Biochemical synthesis and preliminary pharmacological evaluation. Life Sci 1998 ; 63 : 401-11.
26 Samuelsson H, Hedner T, Venn R, Michalkiewicz A. CSF and plasma concentrations of morphine and morphine glucuronides in cancer patients receiving epidural morphine. Pain 1993 ; 52 : 179-85.
27 Goucke C, Hackett L, Ilett K. Concentrations of morphine, morphine-6-glucuronide and morphine-3-glucuronide in serum and cerebrospinal fluid following morphine administration to patients with morphine-resistant pain. Pain 1994 ; 56 : 145-9.
28 Wolff T, Samuelsson H, Hedner T. Morphine and morphine metabolite concentrations in cerebrospinal fluid and plasma in cancer pain patients after slow-release oral morphine administration. Pain 1995 ; 62 : 147-54.
29 Ivarsson M, Neil A. Differences in efficacies between morphine and methadone demonstrated in the guinea pig ileum : A possible explanation for previous observations on incomplete opioid cross-tolerance. Pharmacol Toxicol 1989 ; 65 : 368-71.
30 Sosnowski M, Yaksh T. Differential cross-tolerance between intrathecal morphine and sufentanil in the rat. Anesthesiology 1990 ; 73 : 1141-7.
31 Duttaroy A, Yoburn B. The effect of intrinsic efficacy on opioid tolerance. Anesthesiology 1995 ; 82 : 1226-36.
32 Dirig D, Yaksh T. Differential right shifts in the dose-response curve for intrathecal morphine and sufentanil as a function of stimulus intensity. Pain 1995 ; 62 : 321-
8.
33 Saeki S, Yaksh T. Suppression of nociceptive responses by spinal mu opioid agonists : Effects of stimulus intensity and agonist efficacy. Anesth Analg 1993 ; 77 : 265-74.
2 Daeninck PJ, Bruera E. Opioid use in cancer pain. Is a more liberal approach enhancing toxicity ? Acta Anaesthesiol Scand 1999 ; 43 : 924-38.
3 Galer B, Coyle N, Pasternak G, Portenoy R. Individual variability in the response to different opioids : Report of five cases. Pain 1992 ; 49 : 87-91.
4 MacDonald N, Der L, Allan S, Champion P. Opioid hyperexcitability : The application of alternate opioid therapy. Pain 1993 ; 53 : 353-5.
5 Sjogren P, Jonsson T, Jensen NH, Drenck NE, Staehelin Jensen T. Hyperalgesia and myoclonus in terminal cancer patients treated with continuous intravenous morphine. Pain 1993 ; 55 : 93-7.
6 de Stoutz N, Bruera E, Suarez-Almazor M. Opioid rotation for toxicity reduction in terminal cancer patients. J Pain Symptom Manage 1995 ; 10 : 378-83.
7 Ashby M, Martin P, Jackson K. Opioid substitution to reduce adverse effects in cancer pain management. Med J Austr 1999 ; 170 : 68-71.
8 Reisine T, Pasternak G. Opioid analgesics and antagonists. Dans : Hardman J, Limbird L, Molinoff P, Ruddon R, Goodman Gilman A, editors. The pharmacological basis of therapeutics. 9th ed. New York : McGraw-Hill, 1996 ; 521-55.
9 Cox BM. Opioid receptor-G protein interactions : Acute and chronic effects of opioids. Dans : Herz A, editor. Opioids I. 1st ed. Berlin : Springer-
Verlag, 1993 ; 145-88.
10 Mogil J, Sternberg W, Marek P, et al. The genetics of pain and pain inhibition. Proc Natl Acad Sci 1996 ; 93 : 3048-55.
11 Ebert B, Thorkildsen C, Andersen S, Christrup L, Hjeds H. Opioid analgesics as noncompetitive N-methyl-D-aspartate antagonists. Biochem Pharmacol 1998 ; 56 : 553-9.
12 Mao J, Price D, Mayer D. Mechanisms of hyperalgesia and morphine tolerance : A current view of their possible interactions. Pain 1995 ; 62 : 259-74.
13 Davis A, Inturrisi C. d-Methadone blocks morphine tolerance and N-methyl--D-aspartate-induced hyperalgesia. J Pharmacol Exp Ther 1999 ; 289 : 1048-53.
14 Szeto H, Inturrisi C, Houde R, et al. Accumulation of normeperidine, an active metabolite of meperidine, in patients with renal failure or cancer. Ann Intern Med 1977 ; 86 : 738-41.
15 Kaiko R, Foley K, Grabinski P, et al. Central nervous system excitatory effects of meperidine in cancer patients. Ann Neurol 1983 ; 13 : 180-5.
16 Smith M, Watt J, Cramond T. Morphine-3-glucuronide a potent antagonist of morphine analgesia. Life Sci 1990 ; 47 : 579-85.
17 Gong QL, Hedner J, Björkman R, Hedner T. Morphine-3-glucuronide may functionally antagonize morphine-6-glucuronide induced antinociception and ventilatory depression in the rat. Pain 1992 ; 48 : 249-55.
18 Faura C, Olaso MJ, García Cabanes C, Horga J. Lack of morphine-6-glucuronide antinociception after morphine treatment. Is morphine-3-glucuronide involved ? Pain 1996 ; 65 : 25-30.
19 Bartlett S, Cramond T, Smith M. The excitatory effects of morphine-3-glucuronide are attenuated by LY274614, a competitive NMDA receptor antagonist, and by midazolam, an agonist at the benzodiazepine site on the GABAA receptor complex. Life Sci 1994 ; 54 : 687-94.
20 Osborne R, Joel S, Trew D, Slevin M. Morphine and metabolite behavior after different routes of morphine administration : Demonstration of the importance of the active metabolite morphine-6-glucuronide. Clin Pharmacol Ther 1990 ; 47 : 12-9.
21 Osborne R, Joel S, Grebenik K, Trew D, Slevin M. The pharmacokinetics of morphine and morphine glucuronides in kidney failure. Clin Pharmacol Ther 1993 ; 54 : 158-67.
22 Peterson GM, Randall CTC, Paterson J. Plasma levels of morphine and morphine glucuronides in the treatment of cancer pain : Relationship to renal function and route of administration. Eur J Clin Pharmacol 1990 ; 38 : 121-4.
23 Portenoy R, Foley K, Stulman J, et al. Plasma morphine and morphine-6-glucuronide during chronic morphine therapy for cancer pain : Plasma profiles, steady-state concentrations and the consequences of renal failure. Pain 1991 ; 47 : 13-9.
24 Hagen N, Foley K, Cerbone D, Portenoy R, Inturrisi C. Chronic nausea and morphine-6-glucuronide. J Pain Symptom Manag 1991 ; 6 : 125-8.
25 Wright A, Nocente ML, Smith M. Hydromorphone-3-glucuronide : Biochemical synthesis and preliminary pharmacological evaluation. Life Sci 1998 ; 63 : 401-11.
26 Samuelsson H, Hedner T, Venn R, Michalkiewicz A. CSF and plasma concentrations of morphine and morphine glucuronides in cancer patients receiving epidural morphine. Pain 1993 ; 52 : 179-85.
27 Goucke C, Hackett L, Ilett K. Concentrations of morphine, morphine-6-glucuronide and morphine-3-glucuronide in serum and cerebrospinal fluid following morphine administration to patients with morphine-resistant pain. Pain 1994 ; 56 : 145-9.
28 Wolff T, Samuelsson H, Hedner T. Morphine and morphine metabolite concentrations in cerebrospinal fluid and plasma in cancer pain patients after slow-release oral morphine administration. Pain 1995 ; 62 : 147-54.
29 Ivarsson M, Neil A. Differences in efficacies between morphine and methadone demonstrated in the guinea pig ileum : A possible explanation for previous observations on incomplete opioid cross-tolerance. Pharmacol Toxicol 1989 ; 65 : 368-71.
30 Sosnowski M, Yaksh T. Differential cross-tolerance between intrathecal morphine and sufentanil in the rat. Anesthesiology 1990 ; 73 : 1141-7.
31 Duttaroy A, Yoburn B. The effect of intrinsic efficacy on opioid tolerance. Anesthesiology 1995 ; 82 : 1226-36.
32 Dirig D, Yaksh T. Differential right shifts in the dose-response curve for intrathecal morphine and sufentanil as a function of stimulus intensity. Pain 1995 ; 62 : 321-
8.
33 Saeki S, Yaksh T. Suppression of nociceptive responses by spinal mu opioid agonists : Effects of stimulus intensity and agonist efficacy. Anesth Analg 1993 ; 77 : 265-74.
