Methadone's effect on nAChRs--a link between methadone use and smoking?
Article Details
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Talka R, Tuominen RK, Salminen O
Methadone's effect on nAChRs--a link between methadone use and smoking?
Biochem Pharmacol. 2015 Oct 15;97(4):542-549. doi: 10.1016/j.bcp.2015.07.031. Epub 2015 Jul 29.
- PubMed ID
- 26231941 [ View in PubMed]
- Abstract
Methadone is a long-acting opioid agonist that is frequently prescribed as a treatment for opioid addiction. Almost all methadone maintenance patients are smokers, and there is a correlation between smoking habit and use of methadone. Methadone administration increases tobacco smoking, and heavy smokers use higher doses of methadone. Nevertheless, methadone maintenance patients are willing to quit smoking although their quit rates are low. Studies on nicotine-methadone interactions provide an example of the bedside-to-bench approach, i.e., observations in clinical settings have been studied experimentally in vivo and in vitro. In vivo studies have revealed the interplay between nicotine and the endogenous opioid system. At the receptor level, methadone has been shown to be an agonist of human alpha7 nAChRs and a non-competitive antagonist of human alpha4beta2 and alpha3* nAChRs. These drugs do not have significant interactions at the level of drug metabolism, and thus the interaction is most likely pharmacodynamic. The net effect of the interaction may depend on individual characteristics because pharmacogenetic factors influence the disposition of both methadone and nicotine.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Methadone Neuronal acetylcholine receptor subunit alpha-3 Protein Humans UnknownAntagonistDetails Methadone Neuronal acetylcholine receptor subunit alpha-4 Protein Humans UnknownAntagonistDetails Methadone Neuronal acetylcholine receptor subunit alpha-7 Protein Humans YesAgonistDetails Methadone Neuronal acetylcholine receptor subunit beta-2 Protein Humans UnknownAntagonistDetails