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Serotonin‐norepinephrine reuptake inhibitors and the influence of binding affinity (Ki) on analgesia
Author(s) -
Raouf M.,
Glogowski A. J.,
Bettinger J. J.,
Fudin J.
Publication year - 2017
Publication title -
journal of clinical pharmacy and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.622
H-Index - 73
eISSN - 1365-2710
pISSN - 0269-4727
DOI - 10.1111/jcpt.12534
Subject(s) - reuptake inhibitor , monoamine neurotransmitter , reuptake , norepinephrine , norepinephrine transporter , serotonin , pharmacology , neuropathic pain , analgesic , medicine , receptor , dopamine
Summary What is known and objective Serotonin‐norepinephrine reuptake inhibitors ( SNRI s) are commonly used for various psychiatric conditions and neuropathic pain syndromes. SNRI s inhibit the reuptake of serotonin (5‐ HT ) and norepinephrine ( NE ); however, NE reuptake inhibition is thought to be the primary mediator for their analgesic effect. Comment Key differences in pharmacodynamics and receptor affinities exist between SNRI s. The selectivity for each monoamine differs among SNRI s based on the agent's affinity and activity at the monoamine reuptake transporter. We review differences in receptor affinities and monoamine selectivity among SNRI s and the corresponding clinical impact. What is new and conclusion The varying selectivity for 5‐ HT and NE among the SNRI s may help explain the therapeutic dosing required for neuropathic pain as well as dose‐related adverse effects. It is important to understand the pharmacologic differences among SNRI s, in addition to the data from clinical trials, to guide their safe and effective use.