Buy Levomilnacipran (Fetzima) Cas 96847-54-0

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Buy Levomilnacipran (Fetzima) Cas 96847-54-0

Levomilnacipran, sold under the brand name Fetzima, is an antidepressant, used for the treatment of major depressive disorder in adults.[4] It is the levorotatory enantiomer of milnacipran, and has similar effects and pharmacology, acting as a serotonin–norepinephrine reuptake inhibitor.[7][8]

Levomilnacipran was approved for medical use in the United States in July 2013.[9]

Medical uses

A bottle of Fetzima.

Levomilnacipran is indicated for the treatment of major depressive disorder in adults.[4]

Side effects

Side effects seen more often with levomilnacipran than with placebo in clinical trials included nauseadizzinesssweatingconstipationinsomnia, increased heart rate and blood pressureurinary hesitancyerectile dysfunction and delayed ejaculation in males, vomitingtachycardia, and palpitations.[10][11]

Pharmacology

Pharmacodynamics

Relative to other serotonin and norepinephrine reuptake inhibitors, levomilnacipran, as well as milnacipran, differ in that they are much more balanced reuptake inhibitors of serotonin and norepinephrine.[12][13][14] To demonstrate, the serotonin:norepinephrine ratios of SNRIs are as follows: venlafaxine = 30:1, duloxetine = 10:1, desvenlafaxine = 14:1, milnacipran = 1.6:1, and levomilnacipran = 1:2.[12] The clinical implications of more balanced elevations of serotonin and norepinephrine are unclear,[12] but may include improved effectiveness, though also increased side effects.[13][14][15]

Levomilnacipran is selective for the serotonin and norepinephrine transporters, lacking significant affinity for over 23 off-target sites.[16] However, it does show some affinity for the dizocilpine (MK-801/PCPTooltip phencyclidine) site of the NMDA receptor (Ki = 1.7 μM), and has been found to inhibit NR2A and NR2B subunit-containing NMDA receptors with respective IC50 values of 5.62 and 4.57 μM.[16] As such, levomilnacipran is an NMDA receptor antagonist at high concentrations.[16]

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