Levomilnacipran - CAS 175131-60-9
Catalog number: 175131-60-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Levomilnacipran (brand name Fetzima) is an antidepressant approved for the treatment of major depressive disorder in the United States. It was developed by Forest Laboratories and Pierre Fabre Group, and was approved by the Food and Drug Administration in July 2013. Levomilnacipran is the levo- enantiomer of milnacipran, and has similar effects and pharmacology, acting as a serotonin-norepinephrine reuptake inhibitor (SNRI).
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1.Effect of spinal monoaminergic neuronal system dysfunction on pain threshold in rats, and the analgesic effect of serotonin and norepinephrine reuptake inhibitors.
Tamano R1, Ishida M2, Asaki T1, Hasegawa M1, Shinohara S3. Neurosci Lett. 2016 Feb 26;615:78-82. doi: 10.1016/j.neulet.2016.01.025. Epub 2016 Jan 19.
Dysfunction in the central serotonin (5-HT) and norepinephrine (NE) systems cause depression and pain. Descending spinal pain modulatory pathways are important in the analgesic mechanisms of antidepressants, particularly serotonin and norepinephrine reuptake inhibitors (SNRIs). While many non-clinical studies have demonstrated the roles of central monoaminergic systems in pain, there is little evidence to illuminate the direct contribution of spinal descending pain modulatory systems independently of depressive-like behavior. To examine the effects of dysfunction of spinal monoaminergic systems on pain sensitivity, we established a rat chronic pain model by administering lumbar-intrathecal reserpine to minimize its influence on brain. Lumbar-intrathecal reserpine evoked persistent mechanical hypersensitivity and corresponding reductions in spinal 5-HT and NE concentrations (from 767.2 to 241.6ng/g and from 455.9 to 41.7ng/g, respectively after reserpine 30nmol).
2.Electroacupuncture Enhances the Antiallodynic and Antihyperalgesic Effects of Milnacipran in Neuropathic Rats.
Li C1, Ji BU, Kim Y, Lee JE, Kim NK, Kim ST, Koo S. Anesth Analg. 2016 May;122(5):1654-62. doi: 10.1213/ANE.0000000000001212.
BACKGROUND: Milnacipran, a selective serotonin/norepinephrine-reuptake inhibitor, has been shown to elicit a beneficial effect in various models of neuropathic pain. Previously, we reported that repetitive electroacupuncture (EA) significantly ameliorates neuropathic pain induced by L5 spinal nerve ligation (SNL). In the present study, we sought to determine whether a single treatment with EA produces analgesia and whether EA in combination with a subeffective dosage of milnacipran exhibits an additive effect in SNL rats.
3.Comparative efficacy and tolerability of duloxetine, pregabalin, and milnacipran for the treatment of fibromyalgia: a Bayesian network meta-analysis of randomized controlled trials.
Lee YH1, Song GG2. Rheumatol Int. 2016 May;36(5):663-72. doi: 10.1007/s00296-016-3468-5. Epub 2016 Mar 21.
The aim of this study was to assess the relative efficacy and tolerability of duloxetine, pregabalin, and milnacipran at the recommended doses in patients with fibromyalgia. Randomized controlled trials (RCTs) examining the efficacy and safety of duloxetine 60 mg, pregabalin 300 mg, pregabalin 150 mg, milnacipran 200 mg, and milnacipran 100 mg compared to placebo in patients with fibromyalgia were included in this Bayesian network meta-analysis. Nine RCTs including 5140 patients met the inclusion criteria. The proportion of patients with >30 % improvement from baseline in pain was significantly higher in the duloxetine 60 mg, pregabalin 300 mg, milnacipran 100 mg, and milnacipran 200 mg groups than in the placebo group [pairwise odds ratio (OR) 2.33, 95 % credible interval (CrI) 1.50-3.67; OR 1.68, 95 % CrI 1.25-2.28; OR 1.62, 95 % CrI 1.16-2.25; and OR 1.61; 95 % CrI 1.15-2.24, respectively]. Ranking probability based on the surface under the cumulative ranking curve (SUCRA) indicated that duloxetine 60 mg had the highest probability of being the best treatment for achieving the response level (SUCRA = 0.
4.Evidence-Based Pharmacologic Approaches for Chronic Orofacial Pain.
Clark G. J Calif Dent Assoc. 2015 Nov;43(11):643-54.
For neuropathic pain, the three medications to use are gabapentinoids, tricyclic antidepressants and serotonin norepinephrine reuptake inhibitors plus topical anesthetics. Beta-blockers, tricyclic antidepressants and anti-epileptic drugs are effective preventive medications for daily migraine headaches. The three FDA-approved drugs for fibromyalgia, pregabalin, duloxetine and milnacipran, are not robust. For osteoarthritis, nonsteroidal anti-inflammatories have good efficacy, and when gastritis contraindicates them, corticosteroid injections are helpful.
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CAS 175131-60-9 Levomilnacipran

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