Document Detail


Preclinical pharmacology and opioid combinations.
MedLine Citation:
PMID:  22420604     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Although effective alone, opioids are often used in combination with other drugs for relief of moderate to severe pain. Guidelines for acute perioperative pain recommend the use of multimodal therapy for pain management, although combinations of opioids are not specifically recommended. Mu opioid drugs include morphine, heroin, fentanyl, methadone, and morphine 6β-glucuronide (M6G). Their mechanism of action is complex, resulting in subtle pharmacological differences among them and with unpredictable differences in their potency, effectiveness, and tolerability among patients. Highly selective mu opioids do not bind to a single receptor. Rather, they interact with a large number of mu receptor subtypes with different activation profiles for the various drugs. Thus, mu-receptor-based drugs are not all the same and it may be possible to utilize these differences for enhanced pain control in a clinical setting. These differences among the drugs raise the question of whether combinations might result in better pain relief with fewer side effects. This concept has already been demonstrated between two mu opioids in preclinical studies and clinical trials on other combinations are ongoing. This article reviews the current state of knowledge about mu opioid receptor pharmacology, summarizes preclinical evidence for synergy from opioid combinations, and highlights the complex nature of the mu opioid receptor pharmacology.
Authors:
Gavril W Pasternak
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Review    
Journal Detail:
Title:  Pain medicine (Malden, Mass.)     Volume:  13 Suppl 1     ISSN:  1526-4637     ISO Abbreviation:  Pain Med     Publication Date:  2012 Mar 
Date Detail:
Created Date:  2012-03-16     Completed Date:  2012-11-30     Revised Date:  2013-06-26    
Medline Journal Info:
Nlm Unique ID:  100894201     Medline TA:  Pain Med     Country:  United States    
Other Details:
Languages:  eng     Pagination:  S4-11     Citation Subset:  IM    
Copyright Information:
Wiley Periodicals, Inc.
Affiliation:
Laboratory of Molecular Neuropharmacology, Memorial Sloan-Kettering Cancer Center, New York, New York 10065, USA. pasterng@mskcc.org
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MeSH Terms
Descriptor/Qualifier:
Analgesics, Opioid / classification,  metabolism,  pharmacology*
Drug Synergism
Drug Therapy, Combination / methods,  standards,  trends*
Humans
Pain / drug therapy*,  metabolism,  physiopathology
Receptors, Opioid, mu / agonists*,  classification,  physiology*
Grant Support
ID/Acronym/Agency:
DA02615/DA/NIDA NIH HHS; DA06241/DA/NIDA NIH HHS; DA07242/DA/NIDA NIH HHS; R01 DA002615-31/DA/NIDA NIH HHS; R01 DA006241-23/DA/NIDA NIH HHS; R01 DA007242/DA/NIDA NIH HHS; R01 DA007242-22/DA/NIDA NIH HHS; R56 DA002615/DA/NIDA NIH HHS
Chemical
Reg. No./Substance:
0/Analgesics, Opioid; 0/Receptors, Opioid, mu
Comments/Corrections

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