Savella inhibits the reuptake of serotonin and norepinephrine. The preparation aligns depressive mood, which is pathologically altered, and normalizes the emotional sphere. Savella improves concentration, accelerates and enhances the thinking processes during depressions. The medication is characterized by no affinity for alpha1-adrenoceptors, m-cholinergic receptors, the dopamine D1 and D2-receptors, histamine H1 receptors, opioid receptors, and the benzodiazepine; it has no disastrous effect on cognitive function. Savella provides sedation, while naturally improves sleep. Savella makes no adverse impact on blood pressure and cardiac conduction system, which is essential for elderly patients on cardiotropic medications.
Savella indications for use
The medication is designed for treatment of depression of varying severity in adults.
Savella pharmacological action
When ingested Milnacipran is rapidly and almost completely absorbed; bioavailability equals approximately 85% and doesn’t differ depending on the nature of power, the maximum concentration is reached after 2 hours, plasma protein binding at approximately 13% level. The maximum concentration at a single dose of 50mg is approximately equal to 120mg/ml. The maximum concentration is directly proportional to the magnitude of the dose. The equilibrium state is reached after 2 - 3 days of regular use, while it is 70 - 100% more than when a single dose. The volume of distribution of milnacipran is about 5 l/kg.
Savella is metabolized primarily by conjugation with glucuronic acid. The metabolites have pharmacological activity. The half-life of the preparation equals approximately 7-8 hours. Milnacipran crosses the placenta and excreted in breast milk. With repeated use the medication is derived from the body entirely within 2-3 days after cancellation. The half-life in people with minor, moderate and severe impaired renal function increases to 38%, 41%, 122% respectively.
Milnacipran is prescribed for ingestion (preferably with meals), 2 times each 25 hours, 50 mg, for 1+ month (the duration of therapy is determined individually). In patients suffering from renal insufficiency, depending on creatinine clearance, reducing the dose may be required. Between the use of monoamine oxidase inhibitors and milnacipran is required two weeks interval. Between the use of Savella and monoamine oxidase inhibitors must be not less than 1 week.
Drinking alcohol during treatment must be avoided. When used together, drugs that affect serotonin reuptake with drugs that inhibit its metabolism may develop serotonin syndrome (neuroleptic malignant syndrome), which manifests the development of hallucinations, irritability, coma, labile blood pressure, tachycardia, hyperthermia, loss of coordination, hyperreflexia, nausea, vomiting, diarrhea and is a danger to the patient's life.
During the antidepressants course the patients should be supervised for suicidal behavior and inclinations. Savella may provoke excitation, variability of mood, fatigue, anxiety, paresthesia, headache, emotional lability, drowsiness, convulsions. The use of milnacipran in patients who have a history of hypomania and/or mania, must be done with caution as there is a risk of exacerbation of these conditions. Using milnacipran in those who drive vehicles and those whose profession is associated with increased concentration and speed of psychomotor reactions.