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Hydrolytic Enzymes for the Synthesis of Pharmaceuticals
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Sergio González-Granda, Vicente Gotor-Fernández
Milnacipran is a selective serotonin re-uptake inhibitor applied as anti-depressant but also can be supplied to chronic pain patients associated with fibromyalgia. CAL-B has been found as an adequate enzyme for its KR through acylation (Scheme 9.37), finding moderate selectivities in the best studied conditions that include the use of a large excess of methyl iso-butyrate as acyl donor in TBME at 50°C for 4 h, yielding the (1R,2S)-amide and the unreacted (1S,2R)-amine in 55% and 98% ee, respectively, after a 65% conversion (Sanfilippo et al., 2014). KR of Milnacipran using CAL-B and methyl iso-butyrate through N-acylation.
Psychiatric Treatment Approaches for Pediatric Pain
Published in Andrea Kohn Maikovich-Fong, Handbook of Psychosocial Interventions for Chronic Pain, 2019
While milnacipran is approved for the treatment of adults with major depression in Europe, its approved use in the U.S. is limited to treatment of adult fibromyalgia. A small study of milnacipran for JFMS did find mild clinical improvements without significant side effects, but was an uncontrolled open trial (Arnold, Bateman, Palmer, & Lin, 2015).
Fibromyalgia
Published in Gary W. Jay, Practical Guide to Chronic Pain Syndromes, 2016
Milnacipran, a norepinephrine serotonin reuptake inhibitor (NSRI), has been shown to have better analgesic properties, reportedly, than the SSRIs (277). This medication became the third to receive FDA approval for its use in the treatment of FMS. It was also found that milnacipran can relieve not only pain but other symptoms of FMS, including fatigue, sleep, and depression (48, 278). A recently published RCT shows the drug is efficacious at both 100 and 200 mg/day. The most commonly reported adverse events included nausea, headache, and constipation (279).
The state-of-the-art pharmacotherapeutic options for the treatment of chronic non-cancer pain
Published in Expert Opinion on Pharmacotherapy, 2022
Ryan S. D’Souza, Brendan Langford, Rachel E. Wilson, Yeng F. Her, Justin Schappell, Jennifer S. Eller, Timothy C. Evans, Jonathan M. Hagedorn
The most widely used SNRI agents include duloxetine, venlafaxine, and milnacipran (Table 4). A review of 18 trials found that a duloxetine dose as low as 60 mg daily was effective in treating neuropathic pain including diabetic peripheral neuropathy, fibromyalgia, and painful physical symptoms in depression [60]. Duloxetine may also offer short-term pain reduction and improvement in physical function in patients with osteoarthritis and chronic low back pain as early as within 2 weeks of initiation [61]. A systematic review of 11 RCTs revealed that venlafaxine was efficacious for neuropathic pain, particularly when higher dosages were administered (150–225 mg) for longer durations. This strategy may lead to greater norepinephrine reuptake inhibition and greater activation of noradrenergic pathways involved in analgesia and descending inhibition of pain signal transmission [62]. Milnacipran is an FDA-approved agent for treatment of fibromyalgia with Level I evidence indicating that doses of 100–200 mg/day of milnacipran are superior to placebo (number needed to treat: 11) [63].
Duloxetine for pain in fibromyalgia in adults: a systematic review and a meta-analysis
Published in International Journal of Neuroscience, 2020
Yan-Na Lian, Yi Wang, Ying Zhang, Chun-Xiao Yang
This meta-analysis showed that DLX was more effective than placebo in relieving pain of FM patients. However, the potential analgesic benefit of DLX was counteracted by its adverse events. Importantly, its efficacy in pain reduction had been shown in FM patients with or without major depression [17,22]. In contrast, there were no data available to show whether other SNRIs were effective in FM patients with major depression [24]. Recently, it has been reported that milnacipran is likely to be a useful late stage antidepressant option in treatment-resistant patients as well as those with chronic pain [25]. Therefore, both DLX and milnacipran might be regarded as the first drug option for FM patients with major depression. Although DLX group was not better than the placebo group in PGIC or PGII, the result might show that DLX only focused on certain key symptom not all symptoms of FM.
Antidepressants with different mechanisms of action show different chronopharmacological profiles in the tail suspension test in mice
Published in Chronobiology International, 2019
Hiroshi Kawai, Reiko Iwadate, Takuya Ishibashi, Naomi Kudo, Yoichi Kawashima, Atsushi Mitsumoto
Antidepressant activity is influenced by circadian rhythm. Several antidepressants show diurnal activity in clinical settings and animal models. Lofepramine and clomipramine most effectively ameliorate depression when they are administered at midnight (00:00 h) and midday (12:20 h), respectively (Nagayama 1999; Nagayama et al. 1991; Philipp and Marneros 1978). The sedation and xerostomia caused by amitriptyline administration are more severe following morning than evening treatments (Nakano and Hollister 1983). On the other hand, the effects of fluoxetine do not differ between morning and evening administration (Usher et al. 1991). Timing for the maximal efficacy differs among the drugs. In animal studies, amitriptyline and fluvoxamine were most effective in the early dark phase (Ushijima et al. 2005), whereas nomifensine, milnacipran, and imipramine worked best in the light phase (Borsini et al. 1990; Kawai et al. 2018a, 2018b). A behavioral test suggested that the serotonergic and noradrenergic activities of milnacipran may contribute toward its overall antidepressant activity in the morning and evening, respectively (Kawai et al. 2018a). The dosing time-dependent antidepressant activity of these drugs could be explained by the circadian fluctuation of monoaminergic neuron activity (Kawai et al. 2018a; Ushijima et al. 2005). Earlier results suggested that the chronopharmacological profiles of antidepressants depend on their modes of action. To the best of our knowledge, however, no study to date has yet compared the chronopharmacological profiles of various antidepressants administered under the same experimental conditions.