Milnacipran

Products

In many countries, no medicines containing milnacipran are registered. In other countries, film-coated tablets and capsules are available, for example Savella in the United States.

Structure and properties

Milnacipran (C15H22N2O, Mr = 246.4 g/mol) is present in the drug as milnacipran hydrochloride, a white crystalline powder that is readily soluble in water. It is a racemate. The active 1S,2R enantiomer levomilnacipran is also commercially available, but as an antidepressant (Fetzima).

Effects

Milnacipran (ATC N06AX17) has analgesic and antidepressant properties. The effects are due to selective inhibition of the reuptake of norepinephrine and serotonin into presynaptic neurons in the central nervous system. It has a stronger effect on norepinephrine. Milnacipran has a half-life of 6 to 8 hours.

Indications

Dosage

According to the professional information. The tablets are taken twice daily. Therapy initiation is gradual, and discontinuation is gradual.

Contraindications

  • Hypersensitivity
  • Combination with MAO inhibitors
  • Breastfeeding
  • Cardiovascular disease (see FI).

Full precautions can be found in the drug label.

Interactions

Milnacipran is mainly glucuronidated and interacts poorly with CYP450 isozymes. Drug-drug interactions have been described with the following agents and others:

Adverse effects

The most common possible adverse effects include nausea, headache, constipation, dizziness, insomnia, flushing, sweating, vomiting, palpitations, increased heart rate, dry mouth, and hypertension. Milnacipran is serotonergic and therefore may cause serotonin syndrome.