Antidepressants as long-acting local anesthetics

Strümper, Danja; Durieux, Marcel E.

doi:10.1016/j.rapm.2004.03.001

Cited by 19 publications

(10 citation statements)

References 81 publications

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“…Antidepressants may elicit their analgesic effect acting as local anesthetics through peripheral mechanisms such as sodium channel and the blockade of 5-HT receptors (Sawynok et al, 2001;Strumper and Durieux, 2004;Groves, 2006). Because peripheral 5-HT is primarily pronociceptive (Sommer, 2004), it is less likely that it may contribute to the analgesic action of antidepressants.…”

Section: Differential Analgesic Effects Of Various Antidepressants Inmentioning

confidence: 99%

Mice Lacking Central Serotonergic Neurons Show Enhanced Inflammatory Pain and an Impaired Analgesic Response to Antidepressant Drugs

Zhao¹,

Chiechio²,

Sun³

et al. 2007

J. Neurosci.

124

101

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Section: Differential Analgesic Effects Of Various Antidepressants Inmentioning

confidence: 99%

Mice Lacking Central Serotonergic Neurons Show Enhanced Inflammatory Pain and an Impaired Analgesic Response to Antidepressant Drugs

Zhao¹,

Chiechio²,

Sun³

et al. 2007

J. Neurosci.

124

101

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“…It is often associated to abnormal pain messages like allodynia (a painful response to an innocuous stimulus) and is generally considered to respond poorly to standard analgesic treatments. In animals, tricyclic antidepressants (TCAs) exhibit long-lasting local analgesic properties in nociceptive, inflammatory and neuropathic pain [1][2][3]. In humans, given locally or even systemically, they are widely used for the treatment of various chronic and neuropathic pain conditions [4].…”

Section: Introductionmentioning

confidence: 99%

Tricyclic Antidepressants-loaded Biodegradable PLGA Nanoparticles: In Vitro Characterization and In Vivo Analgesic and Anti-Allodynic Effect

García¹,

Escribano²,

Colom³

et al. 2011

CNANO

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Tricyclic antidepressants (TCAs) have potent local pain blockade properties that could be of interest in relieving chronic pain states as neuropathic pain. The aim of this work was to reach a persistent control of nociceptive and neuropathic pain by means of an injectable controlled release system using lower than usual doses of TCAs. To address this issue, amitriptyline, doxepin and imipramine were encapsulated with poly (lactic-co-glycolic) acid (PLGA) as polymer. Nanoparticles were characterized. The in vitro drug release profile and mechanism was evaluated, and the in vivo analgesic and anti-allodynic activity in front of heat-induced nociceptive pain and sciatic nerve chronic constriction injury, respectively, was tested. The mean±SD particle size and drug loadings (%) of the nanoparticles obtained were 420±13, 480±73 and 373±25nm, and 40.46±4.11, 31.09±3.02 and 32.20±3.20 % for amitriptyline, doxepin and imipramine, respectively. According to the Korsmeyer-Peppas model, the release mechanism of doxepin was diffusion controlled, while a combination of Fickian diffusion and polymer relaxation/erosion of the PLGA matrix was involved for amitriptyline and imipramine. After local infiltration of nanoparticles in rats, the antinociceptive and anti-allodynic activity of the encapsulated drugs were long-lasting and higher than that observed from the solutions. Amitriptyline elicited the lower analgesic effect. Doxepin showed the most outstanding results and its encapsulation led to a 62% and 229% increase in antinociceptive and anti-allodynic activity, respectively. So, this drug could be considered as a therapeutical alternative in pain relieving treatments.

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“…These compounds indeed have chemical similarity to local anaesthetics: both antidepressants and local anaesthetics consist of a hydrophobic portion (usually a tricyclic structure in tricyclic antidepressants and a single ring structure in local anaesthetics), linked via a linear intermediate moiety (a hydrocarbon chain in tricyclic antidepressants and an amide or ester linkage in local anaesthetics) to an amine [51].…”

Section: Peripheral Mechanisms Of Analgesic Actionmentioning

confidence: 99%

Mechanism-Based Treatment in Chronic Neuropathic Pain: The Role of Antidepressants

Coluzzi

Mattia

2005

CPD

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Antidepressant drugs have been widely used for many years to treat neuropathic pain, despite the rationale for their use was still unclear. We review recent insights into their mechanism of action, focusing on central and peripheral analgesic actions. Beside the traditional monoaminergic hypothesis, other pharmacological actions have been studied: antidepressants interfere with the opioid system, interact with the NMDA receptors, and inhibit ion channel activity. Firm evidence from randomised controlled trials demonstrated that TCAs are the most effective drugs for treatment of different neuropathic pain conditions. They exhibit the lowest number needed to treat compare with all other drugs investigated. SSRIs failed to provide an adequate analgesia, due to their high selectivity. SSRIs are clearly less effective than TCAs (NNT: 6.7 vs 2.4) supporting the hypothesis that a balanced inhibition of noradrenaline and serotonin reuptake is more effective in relieving pain. On the basis of initial results Venlafaxine seems to be the most promising of the newer antidepressants as analgesic. Newer antidepressants show a better side effects profile, but further investigation are warranted to clarify their potential role in management of pain. Neuropathic pain remains a challenging condition to treat, as all currently available drugs fail to achieve adequate pain relief in a significant proportion of patients. TCAs should be currently considered the first choice in treatment of neuropathic pain and the gold standard against which to compare other potential new treatments.

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Antidepressants as long-acting local anesthetics

Cited by 19 publications

References 81 publications

Mice Lacking Central Serotonergic Neurons Show Enhanced Inflammatory Pain and an Impaired Analgesic Response to Antidepressant Drugs

Mice Lacking Central Serotonergic Neurons Show Enhanced Inflammatory Pain and an Impaired Analgesic Response to Antidepressant Drugs

Tricyclic Antidepressants-loaded Biodegradable PLGA Nanoparticles: In Vitro Characterization and In Vivo Analgesic and Anti-Allodynic Effect

Mechanism-Based Treatment in Chronic Neuropathic Pain: The Role of Antidepressants

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