Milnacipran - CAS 92623-85-3
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Not Intended for Therapeutic Use. For research use only.
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Milnacipran is a serotonin-norepinephrine reuptake inhibitor (SNRI) used in the clinical treatment of fibromyalgia. It is not approved for the clinical treatment of major depressive disorder in the USA, but it is in other countries. It inhibits the reuptake of serotonin and norepinephrine in an approximately 1:3 ratio. It is well absorbed after oral dosing and has a bioavailability of 85%. It is conjugated to the inactive glucuronide and excreted in the urine as unchanged drug and conjugate. Only traces of active metabolites are found.
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Dalcipran; Ixel; Savella; Toledomin
1.Antidepressants modulate glycine action in rat hippocampus.
Chang HK1, Kim KH1, Kang KW2, Kang YJ2, Kim TW3, Park HK4, Kim SE4, Kim CJ4. J Exerc Rehabil. 2015 Dec 31;11(6):311-9. doi: 10.12965/jer.150263. eCollection 2015.
Antidepressants are drugs that relieve symptoms of depressive disorders. Fluoxetine, tianeptine, and milnacipran are different types of antidepressants, and they have widely been used for relieving of depression symptoms. In the present study, the effects of fluoxetine, tianeptine, and milnacipran on the glycine-induced ion current by nystatin-perforated patch clamp and on the amplitude of field potential in the hippocampal CA1 region by multichannel extracellular recording, MED64, system, were studied. In the present results, fluoxetine, tianeptine, and milnacipran reduced glycine-induced ion current in the hippocampal CA1 neurons in nystatin-perforated patch clamp method. These drugs enhanced the amplitude of the field potential in the hippocampal CA1 region in MED64 system. These results suggest that antidepressants may increase neuronal activity by enhancing field potential through inhibition on glycine-induced ion current.
2.Treatment Patterns Associated with ACR-Recommended Medications in the Management of Fibromyalgia in the United States.
Liu Y1, Qian C2, Yang M2. J Manag Care Spec Pharm. 2016 Mar;22(3):263-71. doi: 10.18553/jmcp.2016.22.3.263.
BACKGROUND: Fibromyalgia (FM) affects up to 6% of U.S. adults, resulting in a significant burden on the health care system and poor quality of life for patients. Duloxetine, pregabalin, and milnacipran are approved for management of FM; however, consensus is lacking regarding optimal therapy. Patients with FM taking approved medications often do not experience meaningful symptom relief, and many experience intolerable adverse events.
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 Mar 21. [Epub ahead of print]
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.Milnacipran treatment and potential biomarkers in depressed patients following an initial SSRI treatment failure: a prospective, open-label, 24-week study.
Hashimoto T1, Sakurai D2, Oda Y2, Hasegawa T3, Kanahara N4, Sasaki T3, Komatsu H5, Takahashi J6, Oiwa T7, Sekine Y8, Watanabe H2, Iyo M9. Neuropsychiatr Dis Treat. 2015 Dec 10;11:3031-40. doi: 10.2147/NDT.S95067. eCollection 2015.
BACKGROUND: We assessed the effect of switching patients with major depressive disorder to milnacipran following an initial selective serotonin reuptake inhibitor treatment failure, and explored potential biomarkers in their blood.
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CAS 92623-85-3 Milnacipran

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