Longer occupancy of opioid receptors by nalmefene compared to naloxone as measured in vivo by a dual-detector system

Journal of Nuclear Medicine

Volumn 38, Issue 11, 1997, Pages 1726-1731

  Kim, Stanley ^b   Wagner Jr , Henry N ^a   Villemagne, Victor L ^b   Kao, Pan Fu ^b   Dannals, Robert F ^b   Ravert, Hayden T ^b   Joh, Tenshang ^b   Dixon, Rosina B ^b   Civelek, A Cahid ^b  

^a DEPARTMENT OF PATHOLOGY   (United States)

^b NONE

Author keywords

Carfentanil; Dual detector probe; Nalmefene; Naloxone; Positron emission

Indexed keywords

CARBON 11; CARFENTANIL; MU OPIATE RECEPTOR; NALMEFENE; NALOXONE; OPIATE ANTAGONIST; OPIATE RECEPTOR;

ADULT; ARTICLE; BRAIN; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DRUG CLEARANCE; FEMALE; HUMAN; INTRAVENOUS DRUG ADMINISTRATION; MALE; NORMAL HUMAN; PLASMA HALF LIFE; POSITRON EMISSION TOMOGRAPHY; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; RECEPTOR OCCUPANCY;

ADULT; ANALGESICS, OPIOID; BRAIN; CARBON RADIOISOTOPES; CROSS-OVER STUDIES; FEMALE; FENTANYL; HUMANS; MALE; NALOXONE; NALTREXONE; NARCOTIC ANTAGONISTS; RECEPTORS, OPIOID; TIME FACTORS; TOMOGRAPHY, EMISSION-COMPUTED;

EID: 0030659004     PISSN: 01615505     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (25)

1. Pasternak GW. The Opiate Receptors. New York, NY: Humana Press; 1988.
2. Kennedy SK, Longnecker DE. History and principles of anesthesiology. In: Goodman Gilman A, Rall TW, Nies AS, Taylor P, eds. The pharmacological basis of therapeutics. New York, NY: Pergamon Press; 1990:260-275.
3. Johnstone R, Jobes DR, Kennell EM, Behar MG, Smith TC. Reversal of morphine anesthesia with naloxone. Anesthesiology 1974;41:361-367.
4. Evans JM, Hogg MIJ, Lunn JN, Rosen M. Degree and duration of reversal by naloxone of effects of morphine in conscious subjects. Br Med J 1974;2:589-591.
5. Ngai SH, Berkowitz BA, Yang JC, Hempstead J, Spector S. Pharmacokinetics of naloxone in rats and in man. Anesthesiology 1976;44:398-401.
6. Jaffe JH, Martin WR. Opioid analgesics and antagonists. In: Goodman Gilman A, Rall TW, Nies AS, Taylor P, eds. The pharmacological basis of therapeutics. New York, NY: Pergamon Press: 1990:491-531.
7. Ling W, Wesson DR. Drugs of abuse: opiates. West J Meet 1990;152:565-572.
8. Foldes FF, Lunn JN, Moore J, Brown IMN. Allylnoroxymorphone. A new potent narcotic antagonist. Am J Med Sci 1963;245:23-30.
9. Sadove MS, Balagot RC, Hatano S, Jobgen EA. Study of a narcotic antagonist: N-allyl-noroxymorphone. J Am Med Assoc 1963;183:666-668.
10. Barsan WG, Seger D, Danzl DF, et al. Duration of antagonistic effects of nalmefene and naloxone in opiate-induced sedation for emergency department procedures. Am J Emerg Med 1989:7:155-161.
11. Kaplan JL, Marx JA. Effectiveness and safety of intravenous nalmefene for emergency department patients with suspected narcotic overdose: a pilot study. Ann Emerg Med 1991;22:187-190.
12. Van Vugt DA, Webb MY, Reid RL. Comparison of the duration of action of nalmefene and naloxone on the hypothalamic-pituitary axis of the rhesus monkey. Neuroendocrinology 1989;49:275-280.
13. Gal TJ, DiFazio CA. Prolonged antagonism of opioid action with intravenous nalmefene in man. Anesthesiology 1986;64:175-180.
14. Gal TJ, DiFazio CA, Dixon R. Prolonged blockade of opioid effect with oral nalmefene. Clin Pharmacol Ther 1986;40:537-542.
15. Frost JJ, Wagner HN Jr, Dannals RF, et al. Imaging opiate receptors in the human brain by positron tomography. J Comput Assist Tomogr 1985;9:231-236.
16. 11C]carfentanil binding to opiate receptors in humans by positron emission tomography. J Cereb Blood Flow Metab 1990;10:484-492.
17. Bice AN, Wagner HN Jr, Frost JJ, et al. A simplified detection system for neuroreceptor studies in the human brain. J Nucl Med 1986;27:184-191.
18. 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.
19. 11C-carfentanil in vivo binding to opiate receptors in man using a dual detector system. Eur J Pharmacol 1994;257:195-197.
20. 11C]carfentanil. Int J Appl Radiat Isot 1985;36:303-306.
21. Mayberg HS, Frost JJ. Opiate receptors. In: Frost JJ, Wagner HN Jr, eds. Quantitative imaging. New York, NY: Raven Press; 1990:81-95.
22. Aitkenhead AR, Derbyshire DR, Pinnock CA, Achola K, Smith G. Pharmacokinetics of intravenous naloxone in healthy volunteers [Abstract]. Anesthesiology 1984;61: A381.
23. Dixon R, Hsiao J, Taaffe W, Hahn E, Turtle R. Nalmefene. Radioimmunoassay for a new opioid antagonist. J Pharm Sci 1984;73:1645-1646.
24. Dixon R, Howes J, Gentile J, et al. Nalmefene. Intravenous safety and kinetics of a new opioid antagonist. Clin Pharmacol Ther 1986;39:49-53.
25. Michel ME, Bolger G, Weissman B. Binding of a new opiate antagonist, nalmefene, to rat brain membranes. Methods Find Exp Clin Pharmacol 1985;7:175-177.