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Titolo:
LONGER OCCUPANCY OF OPIOID RECEPTORS BY NALMEFENE COMPARED TO NALOXONE AS MEASURED IN-VIVO BY A DUAL-DETECTOR SYSTEM
Autore:
KIM S; WAGNER KN; VILLEMAGNE VL; KAO PF; DANNALS RF; RAVERT HT; JOB T; DIXON RB; CIVELEK AC;
Indirizzi:
JOHNS HOPKINS MED INST,DIV NUCL MED,615 N WOLFE ST BALTIMORE MD 21205 JOHNS HOPKINS MED INST,DIV NUCL MED BALTIMORE MD 21205 JOHNS HOPKINS MED INST,DIV RADIAT HLTH SCI BALTIMORE MD 21205 OHMEDA INC LIBERTY CORNER NJ 00000
Titolo Testata:
The Journal of nuclear medicine
fascicolo: 11, volume: 38, anno: 1997,
pagine: 1726 - 1731
SICI:
0161-5505(1997)38:11<1726:LOOORB>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
OPIATE RECEPTORS; C-11 DIPRENORPHINE; DURATION; BINDING; ANTAGONIST; REVERSAL; MORPHINE; BRAIN;
Keywords:
POSITRON EMISSION; CARFENTANIL; NALOXONE; NALMEFENE; DUAL-DETECTOR PROBE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
25
Recensione:
Indirizzi per estratti:
Citazione:
S. Kim et al., "LONGER OCCUPANCY OF OPIOID RECEPTORS BY NALMEFENE COMPARED TO NALOXONE AS MEASURED IN-VIVO BY A DUAL-DETECTOR SYSTEM", The Journal of nuclear medicine, 38(11), 1997, pp. 1726-1731

Abstract

Surgical procedures usually involve the administration of narcotic drugs as anesthetics or adjuvants. To reverse the effects of anesthesia,opioid antagonists such as naloxone are commonly used. Due to its short lasting effects, patients receiving naloxone must be monitored carefully. Nalmefene, a pure opiate antagonist with a longer duration of action than naloxone, has shown promise in the reversal of opioid anesthesia. Methods: A simple dual-detector positron radiation detector system and [C-11]carfentanil were used to compare the duration of blockade of cerebral mu opioid receptors by naloxone and nalmefene in eight normal volunteers. Carbon-11-carfentanil brain kinetics were monitored for 5 min and 2, 4, 8 and 24 hr after the administration of either nalmefene (1 mg or 1 mu g/kg) or naloxone (2 mg or 2 mu g/kg). Blood samples were obtained at the same times for plasma determinations. Results: Clearance half-times from opioid receptors were 28.7 +/- 5.9 hr for 1 mg of nalmefene and 2.0 +/- 1.6 hr for 2 mg of naloxone. Brain clearance times were about 21.1 and 3.4 times slower than plasma clearance times for nalmefene and naloxone, respectively. Conclusion: These findings suggest that the prolonged effects of nalmefene are related to the slow dissociation of nalmefene from opioid receptors, which are not reflected in the plasma curve. This longer blockade of opioid receptors by nalmefene represents an advantage in the clinical management of postsurgical reversal of narcotic anesthesia and opioid side effects aswell as the reversal of opioid overdose.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 21/10/20 alle ore 16:51:50