Levomilnacipran Hydrochloride

Cipran is a serotonin and norepinephrine reuptake inhibitor (SNRI) indicated for the treatment of Major Depressive Disorder (MDD) in adults. Limitation of Use: Cipran is not approved for the management of fibromyalgia. The efficacy and safety of Cipran for the management of fibromyalgia have not been established.

The exact mechanism of the antidepressant action of levomilnacipran is unknown, but is thought to be related to the potentiation of serotonin and norepinephrine in the central nervous system, through inhibition of reuptake at serotonin and norepinephrine transporters. Non-clinical studies have shown that levomilnacipran is a potent and selective serotonin and norepinephrine reuptake inhibitor (SNRI). Levomilnacipran binds with high affinity to the human serotonin (5-HT) and norepinephrine (NE) transporters (Ki = 11 and 91 nM, respectively) and potently inhibits 5-HT and NE reuptake (IC50 = 16-19 and 11 nM, respectively). Levomilnacipran lacks significant affinity for any other receptors, ion channels or transporters tested in vitro, including serotonergic (5HT1-7), α- and β-adrenergic, muscarinic, or histaminergic receptors and Ca 2+ , Na + , K + or Cl

channels. Levomilnacipran did not inhibit monoamine oxidase (MAO).

Recommended dose : 40 mg to 120 mg once daily with or without food. Initiate dose at 20 mg once daily for 2 days and then increase to 40 mg once daily. Based on efficacy and tolerability, increase dose in increments of 40 mg at intervals of 2 or more days. The maximum recommended dose is 120 mg once daily. Take capsules whole; do not open, chew or crush. Renal Impairment : Do not exceed 80 mg once daily for moderate impairment. Do not exceed 40 mg once daily for severe renal impairment. Discontinuation : Reduce dose gradually whenever possible.