Antagonist treatment of opioid withdrawal: Translational low dose approach

Journal of Addictive Diseases

Volumn 25, Issue 2, 2006, Pages 1-8

  Mannelli, Paolo ^a   Gottheil, Edward ^b   Van Bockstaele, Elisabeth J ^c  

^a DUKE UNIVERSITY MEDICAL CENTER   (United States)

^b UNIVERSITY OF WASHINGTON SCHOOL OF MEDICINE   (United States)

^c THOMAS JEFFERSON UNIVERSITY   (United States)

Author keywords

Cellular messengers; Detoxification; Integrative research; Inverse agonist; Neural adaptation

Indexed keywords

DIAMORPHINE; ENKEPHALIN; METHADONE; MORPHINE; NALMEFENE; NALOXONE; NALTREXONE; OPIATE AGONIST; OPIATE ANTAGONIST; OPIATE RECEPTOR; PLACEBO;

ANALGESIA; ANALGESIC ACTIVITY; ANIMAL BEHAVIOR; ANTINOCICEPTION; BRAIN REGION; BRAIN STEM; DRUG DEPENDENCE; DRUG DETOXIFICATION; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG WITHDRAWAL; ELECTROPHYSIOLOGY; HUMAN; HYPERALGESIA; IN VITRO STUDY; INFLAMMATORY DISEASE; LOW DRUG DOSE; NERVE CELL; NEUROBIOLOGY; NONHUMAN; OPIATE ADDICTION; REVIEW; SPINAL GANGLION; THALAMUS; WITHDRAWAL SYNDROME;

ANIMALS; BRAIN; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; HUMANS; NALOXONE; NALTREXONE; NARCOTIC ANTAGONISTS; NARCOTICS; OPIOID-RELATED DISORDERS; SUBSTANCE WITHDRAWAL SYNDROME;

EID: 33746645569     PISSN: 10550887     EISSN: 15450848     Source Type: Journal    
DOI: 10.1300/J069v25n02_01     Document Type: Review

References (76)

1. Blachley P, Casey D, Marcel L. Rapid detoxification from heroin and methadone using naltrexone. A model for study of the treatment of the opiate abstinence syndrome. In: Senay E, Shorty L, Alkesne H, eds. Developments in the field of drug abuse. Cambridge, MA: Schenkman Publishing Co, 1975; 327-336.
2. Kurland AA, McCabe L. Rapid detoxification of the narcotic addict with naloxone hydrochloride. A preliminary report. J Clin Pharmacol. 1976; 16(1):66-74.
3. Scherbaum N, Klein S, Kaube H, Kienbaum P, Peters J, Gastpar M. Alternative strategies of opiate detoxification: evaluation of the so-called ultra-rapid detoxification. Pharmacopsychiatry. 1998; 31(6):205-209.
4. Golden SA, Sakhrani DL. Unexpected delirium during Rapid Opioid Detoxification (ROD). J Addict Dis. 2004; 23(1):65-75.
5. Tretter F, Burkhardt D, Bussello-Spieth B, Reiss J, Walcher S, Buchele W. Clinical experience with antagonist-induced opiate withdrawal under anaesthesia. Addiction. 1998; 93(2):269-275.
6. O'Connor PG, Kosten TR. Rapid and ultrarapid opioid detoxification techniques. JAMA. 1998; 279(3):229-234.
7. Kosten TA, Kosten TR. Pharmacological blocking agents for treating substance abuse. J Nerv Ment Dis. 1991 Oct; 179(10):583-592.
8. Wang Z, Bilsky EJ, Porreca F, Sadee W. Constitutive μ opioid receptor activation as a regulatory mechanism underlying narcotic tolerance and dependence. Life Sci. 1994; 54(20):PL339-350.
9. Spanagel R. Is there a pharmacological basis for therapy with rapid opioid detoxification? Lancet. 1999; 354(9195):2017-2018.
10. Spanagel R, Kirschke C, Tretter F, Holsboer F. Forced opiate withdrawal under anaesthesia augments and prolongs the occurrence of withdrawal signs in rats. Drug Alcohol Depend. 1998; 52(3):251-256.
11. Streel E, Dan B, Bredas P, Clement B, Pelc I, Verbanck P. Interference with withdrawal signs of naloxone-induced opiate withdrawal under anesthesia is anesthetic-specific in opiate-dependent rats. Life Sci. 2001; 70(5):517-522.
12. Gonzalez G, Oliveto A, Kosten TR. Combating opiate dependence: a comparison among the available pharmacological options. Expert Opin Pharmacother. 2004; 5(4):713-725.
13. Fontaine E, Godfroid IO, Guillaume R. Ultra-rapid detoxification of opiate dependent patients: review of the literature, critiques and proposition for an experimental protocol. Encephale. 2001; 27(2):187-193.
14. Gowing L, Ali R, White J. Opioid antagonists under heavy sedation or anaesthesia for opioid withdrawal. Cochrane Database Syst Rev. 2002; (2):CD002022.
15. Gowing L, Ali R, White J. Opioid antagonists with minimal sedation for opioid withdrawal. Cochrane Database Syst Rev. 2002; (2):CD002021.
16. Hamilton RJ, Olmedo RE, Shah S, Hung OL, Howland MA, Perrone J, Nelson LS, Lewin NL, Hoffman RS. Complications of ultrarapid opioid detoxification with subcutaneous naltrexone pellets. Acad Emerg Med. 2002; 9(1):63-68.
17. Pfab R, Hirtl C, Zilker T. Opiate detoxification under anesthesia: no apparent benefit but suppression of thyroid hormones and risk of pulmonary and renal failure. J Toxicol Clin Toxicol. 1999; 37(1):43-50.
18. Kirby KC, Stitzer ML, Heishman SJ. Acute opioid physical dependence in humans: effect of varying the morphine-naloxone interval II. J Pharmacol Exp Ther. 1990; 255(2):730-737.
19. Linseman MA. Naloxone-precipitated withdrawal as a function of the morphine-naloxone interval. Psychopharmacology (Berl). 1977; 54(2):159-164.
20. Gonzalez JP, Brogden RN. Naltrexone. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in the management of opioid dependence. Drugs. 1988; 35(3):192-213.
21. Crain SM, Shen KF. Ultra-low concentrations of naloxone selectively antagonize excitatory effects of morphine on sensory neurons, thereby increasing its antinociceptive potency and attenuating tolerance/dependence during chronic cotreatment. Proc Natl Acad Sci U S A. 1995; 92(23):10540-10544.
22. Mannelli P, De Risio S, Pozzi G, Janiri L, De Giacomo M. Serendipitous rapid detoxification from opiates: the importance of time-dependent processes. Addiction. 1999; 94(4):589-591.
23. Mannelli P, Gottheil E, Buonanno A, De Risio S. Use of very low-dose naltrexone during opiate detoxification. J Addict Dis. 2003; 22(2):63-70.
24. Kayser V, Guilbaud G. Dose-dependent analgesic and hyperalgesic effects of systemic naloxone in arthritic rats. Brain Res. 1981; 226:344-348.
25. Kayser V, Benoist JM, Neil A, Gautron M, Guilbaud G. Behavioural and electrophysiological studies on the paradoxical antinociceptive effects of an extremely low dose of naloxone in an animal model of acute and localized inflammation. Exp Brain Res.1988; 73:402-410.
26. Guilbaud G, Benoist JM, Gautron M, Kayser V. Effects of systemic naloxone upon ventrobasal thalamus neuronal responses in arthritic rats. Brain Res. 1982; 243:59-66.
27. Ueda H, Fukushima N, Kitao T, Ge M, Takagi H. Low doses of naloxone produce analgesia in the mouse brain by blocking presynaptic autoinhibition of enkephalin release. Neurosci Lett. 1986; 65:247-252.
28. Mudge AW, Leeman SE, Fischbach GD. Enkephalin inhibits release of substance P from sensory neurons in culture and decreases action potential duration. Proc Natl Acad Sci U S A. 1979 76:526-530.
29. Shen KF, Crain SM. Dual opioid modulation of the action potential duration of mouse dorsal root ganglion neurons in culture. Brain Res. 1989; 491:227-242.
30. Crain SM, Shen KF. Etorphine elicits unique inhibitory-agonist and excitatory-antagonist actions at opioid receptors on sensory neurons: new rationale for improved clinical analgesia and treatment of opiate addiction. NIDA Res Monogr. 1995; 147:234-268.
31. Shen KF, Crain SM. Ultra-low doses of naltrexone or etorphine increase morphine's antinociceptive potency and attenuate tolerance/dependence inmice. Brain Res. 1997; 757:176-190.
32. Crain SM, Shen KF. Acute thermal hyperalgesia elicited by low-dose morphine in normal mice is blocked by ultra-low-dose naltrexone, unmasking potent opioid analgesia. Brain Res. 2001; 888:75-82.
33. Powell KJ, Abul-Husn NS, Jhamandas A, Olmstead MC, Beninger RJ, Jhamandas K. Paradoxical effects of the opioid antagonist naltrexone on morphine analgesia, tolerance, and reward in rats. J Pharmacol Exp Ther. 2002; 300(2):588-596.
34. Lasagna L. Drug interaction in the field of analgesic drugs. Proc R Soc Med.1965; 58:978-983.
35. Buchsbaum MS, Davis GC, Bunney WE, Jr. Naloxone alters pain perception and somatosensory evoked potentials in normal subjects. Nature. 1977; 270:620-622.
36. Levine JD, Gordon NC, Fields HL. Naloxone dose dependently produces analgesia and hyperalgesia in postoperative pain. Nature. 1979; 278:740-741.
37. Levine JD, Gordon NC. Method of administration determines the effect of naloxone on pain. Brain Res. 1986; 365:377-378.
38. Bergman SA, Wynn RL, Myers DE, Rudo FG. Low dose naloxone enhances buprenorphine in a tooth pulp antinociceptive assay. Arch Int Pharmacodyn Ther. 1988; 291:229-237.
39. Levine JD, Gordon NC, Taiwo YO, Coderre TJ. Potentiation of pentazocine analgesia by low-dose naloxone. J Clin Invest. 1988; 82:1574-1577.
40. Gan TJ, Ginsberg B, Glass PS, Fortney J, Jhaveri R, Perno R. Opioid-sparing effects of a low-dose infusion of naloxone in patient-administered morphine sulfate. Anesthesiology. 1997; 87:1075-1081.
41. Joshi GP, Duffy L, Chehade J, Wesevich J,Gajraj N, Johnson ER. Effects of prophylactic nalmefene on the incidence of morphine-related side effects in patients receiving intravenous patient-controlled analgesia. Anesthesiology. 1999; 90:1007-1011.
42. Martin WR, Jasinski DR, Mansky PA. Naltrexone, an antagonist for the treatment of heroin dependence. Effects in man. Arch Gen Psychiatry. 1973; 28:784-791.
43. Volavka J, Mallya A, Bauman J. Hormonal and other effects of naltrexone in normal men. Adv Exp Med Biol. 1979; 116:291-305.
44. Wettstein JG, Martin WR. An analysis of naltrexone and naloxone's possible agonistic actions in the dog. Drug Alcohol Depend. 1985; 15(4):353-360.
45. Mello NK, Mendelson JH, Kuehnle JC, Sellers MS. Operant analysis of human heroin self-administration and the effects of naltrexone. J Pharmacol Exp Ther. 1981; 216:45-54.
46. Grunberger J, Linzmayer L, Fodor G, Presslich O, Praitner M, Loimer N. Static and dynamic pupillometry for determination of the course of gradual detoxification of opiate-addicted patients. Eur Arch Psychiatry Clin Neurosci. 1990; 240(2):109-112.
47. Charney DS, Redmond DE, Jr., Galloway MP. Naltrexone precipitated opiate withdrawal in methadone addicted human subjects: evidence for noradrenergic hyperactivity. Life Sci. 1984; 35:1263-1272.
48. Verebey K, Volavka J, Mule SJ, Resnick RB. Naltrexone: disposition, metabolism, and effects after acute and chronic dosing. Clin Pharmacol Ther 1976; 20:315-328.
49. Verebey K. The clinical pharmacology of naltrexone: pharmacology and pharmacodynamics. NIDA Res Monogr 1981; 28:147-158.
50. Quigley MA, Boyce SH. Unintentional rapid opioid detoxification. Emerg Med J. 2001;18(6):494-495.
51. Bristow K, Meek R, Clark N. Acute opioid withdrawal in the emergency department: inadvertent naltrexone abuse? Emerg Med. 2001;13(3):359-363.
52. Yeo M, Campbell V, Bonomo Y, Sawyer SM. Acute opioid withdrawal on accidental injection of naltrexone. J Paediatr Child Health. 2003; 39(4):315-317.
53. Lee MC, Wagner HN, Jr., Tanada S, Frost JJ, Bice AN, Dannals RF. Duration of occupancy of opiate receptors by naltrexone. J Nucl Med. 1988; 29:1207-1211.
54. Zimmerman DM, Leander JD. Opioid antagonists: structure activity relationships. NIDA Res Monogr. 1990; 96:50-60.
55. Amato L, Davoli M, Ferri M, Ali R. Methadone at tapered doses for the management of opioid withdrawal. Cochrane Database Syst Rev. 2004; 18(4):CD003409.
56. Bale RN, Van Stone WW, Kuldau JM, Engelsing TM, Elashoff RM, Zarcone VP Jr. Therapeutic communities vs methadone maintenance. A prospective controlled study of narcotic addiction treatment: design and one-year follow-up. Arch Gen Psychiatry. 1980; 37(2):179-193.
57. O'Connor PG, Carroll KM, Shi JM, Schottenfeld RS, Kosten TR, Rounsaville BJ. Three methods of opioid detoxification in a primary care setting. A randomized trial. Ann Intern Med. 1997; 127(7):526-530.
58. Rea F, Bell JR, Young MR, Mattick RP. A randomised, controlled trial of low dose naltrexone for the treatment of opioid dependence. Drug Alcohol Depend. 2004; 75(1):79-88.
59. Sevarino KA, Oliveto A, Kosten TR. Neurobiological adaptations to psychostimulants and opiates as a basis of treatment development. Ann N Y Acad Sci. 2000; 909:51-87.
60. Emmett-Oglesby MW, Mathis DA, Moon RT, Lal H. Animal models of drug withdrawal symptoms. Psychopharmacology. 1990; 101(3):292-309.
61. Pierce TL, Raper C. The effects of laboratory handling procedures on naloxone-precipitated withdrawal behavior in morphine-dependent rats. J Pharmacol Toxicol Methods. 1995; 34(3):149-155.
62. Koob GF, Sanna PP, Bloom FE. Neuroscience of addiction. Neuron. 1998; 21(3):467-476.
63. Nestler EJ. Molecular mechanisms of drug addiction. Neuropharmacology. 2004; 47 Suppl 1:24-32.
64. Johnston CA, Watts VJ. Sensitization of adenylate cyclase: a general mechanism of neuroadaptation to persistent activation of Galpha(i/o)-coupled receptors? Life Sci. 2003; 73(23):2913-2925.
65. Stornetta RL, Norton FE, Guyenet PG. Autonomic areas of rat brain exhibit increased Fos-like immunoreactivity during opiate withdrawal in rats. Brain Res. 1993; 624(1-2):19-28.
66. Koob GF. Circuits, drugs, and drug addiction. Adv Pharmacol. 1998; 42:978-982.
67. Mannelli P, Gottheil E, Peoples JF, Oropeza VC, Van Bockstaele EJ. Chronic very low dose naltrexone administration attenuates opioid withdrawal expression. Biol Psychiatry. 2004; 56(4):261-268.
68. Van Bockstaele EJ, Rudoy C, Mannelli P, Oropeza V, Qian Y. Elevated μ-opioid receptor expression in the nucleus of the solitary tract accompanies attenuated withdrawal signs following chronic very low naltrexone in opiate dependent rats. J Neurosci Res 2006; 83(3): 508-514.
69. Koob GF, Ahmed SH, Boutrel B, Chen SA, Kenny PJ, Markou A, O'Dell LE, Parsons LH, Sanna PP. Neurobiological mechanisms in the transition from drug use to drug dependence. Neurosci Biobehav Rev. 2004; 27(8):739-749.
70. Carroll KM, Rounsaville BJ. Bridging the gap: a hybrid model to link efficacy and effectiveness research in substance abuse treatment. Psychiatr Serv. 2003; 54(3):333-339.
71. Gowing L, Ali R, White J. Opioid antagonists and adrenergic agonists for the management of opioid withdrawal. Cochrane Database Syst Rev. 2000;(2):CD002021.
72. Update in: Cochrane Database Syst Rev. 2002;(2):CD002021.
73. Buntwal N, Bearn J, Gossop M, Strang J. Naltrexone and lofexidine combination treatment compared with conventional lofexidine treatment for in-patient opiate detoxification. Drug Alcohol Depend. 2000; 59(2):183-188.
74. Greenwald MK, Johanson CE, Moody DE, Woods JH, Kilbourn MR, Koeppe RA, Schuster CR, Zubieta JK. Effects of buprenorphine maintenance dose on mu-opioid receptor availability, plasma concentrations, and antagonist blockade in heroin-dependent volunteers. Neuropsychopharmacology. 2003; 28(11):2000-2009.
75. Koob GF, Le Moal M. Drug abuse: hedonic homeostatic dysregulation. Science. 1997; 278(5335):52-58.
76. Nestler EJ. Common molecular and cellular substrates of addiction and memory. Neurobiol Learn Mem. 2002; 78(3):637-647.