indication

Milnacipran is used to treat moderate to severe clinical depression and chronic pain.

mechanism of action

Milnacipran inhibits norepinephrine and serotonin reuptake in a 3:1 ratio, in practical use this means a balanced (equal) action upon both transmitters. The serotonin reuptake inhibition is likely to improve depression, while the norepinephrine reuptake inihibition probably improves chronic pain. Milnacipran exerts no significant actions on postynaptic H1, alpha-1, D1, D2, and muscarinic receptors, as well as on benzodiazepine/opiate binding sites. [Wikipedia]

biotransformation

Only traces of active metabolites are found. Cytochrome P450 enzymes play no role in the metabolism of Milnacipran.

absorption

Milnacipran is well absorbed following oral administration with an absolute bioavailability of 85%. Meals have no effect on absorption.

half life

8 hours

route of elimination

It is excreted predominantly unchanged in urine (55%) and has a terminal elimination half-life of about 6 to 8 hours. The main route of elimination of bepotastine besilate is urinary excretion (with approximately 75-90% excreted unchanged in urine).

drug interactions

Desvenlafaxine: Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.

Tranylcypromine: Increased risk of serotonin syndrome. Concomitant therapy should be avoided. A significant washout period, dependent on the half-lives of the agents, should be employed between therapies.

Venlafaxine: Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.

Zolmitriptan: Use of two serotonin modulators, such as zolmitriptan and milnacipran, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.