Composition
mirtazapine 45 mg
Pharmacological action
An antidepressant of tetracyclic structure. Increases central adrenergic and serotonergic transmission. It blocks serotonin 5-HT2-and 5-HT3-receptors; therefore, increased serotonergic transmission is realized only through serotonin 5-HT1-receptors.
Both spatial enantiomers are involved in the manifestation of antidepressant activity: the S (+) – enantiomer blocks α2-adrenergic receptors and serotonin 5-HT2-receptors. Moderately blocks histamine H1-receptors, has a sedative effect.
It has little effect on α1-adrenergic receptors and cholinergic receptors; in therapeutic doses, it does not significantly affect the cardiovascular system.
In clinical settings, an anxiolytic and hypnotic effect is also manifested, so mirtazapine is most effective in anxiety depressions of various origins. Due to its moderate sedative effect, it does not actualize suicidal thoughts during treatment.
Pharmacokinetics
Mirtazapine is rapidly absorbed from the gastrointestinal tract after oral use. Bioavailability is 50%. Cmax in blood plasma is reached after 2 hours
. Css in blood plasma is established after 3-4 days of continuous use. Binding to plasma proteins is 85%.
It is actively metabolized in the liver by demethylation and oxidation, followed by conjugation. Dimethyl-mirtazapine is just as pharmacologically active as the parent substance.
Mirtazapine is excreted by the kidneys and through the intestines. T1 / 2 is 20-40 hours.
With renal and hepatic insufficiency, mirtazapine clearance may decrease.
Indications
Depressive states (including anhedonia, psychomotor retardation, insomnia, early awakening, weight loss, loss of interest in life, suicidal thoughts, and mood lability).
Contraindications
Renal and hepatic insufficiency, pregnancy, lactation, hypersensitivity to mirtazapine.
Side effects
From the central nervous system and peripheral nervous system: Â sleepiness, lethargy, emotional lability, mental changes, agitation, anxiety, apathy, hallucinations, depersonalization, hostility, mania, epileptic seizures, dizziness, vertigo, hyperesthesia, convulsions, tremor, myoclonus, hyperkinesis, hypokinesia.
From the side of hematopoietic organs: Â hematopoietic depression – granulocytopenia, agranulocytosis, neutropenia, eosinophilia, aplastic anemia, thrombocytopenia.
From the side of metabolism: Â slight increase in appetite and weight gain; in isolated cases – edema.
From the cardiovascular system: Â rarely-orthostatic hypotension.
From the digestive system: Â nausea, vomiting, constipation, increased appetite, weight gain, dry mouth, thirst, abdominal pain; in some cases – increased activity of liver transaminases.
From the side of the reproductive system: Â decreased potency, dysmenorrhea.
Other services: Â skin rashes, urticaria, flu-like syndrome, suffocation, edematous syndrome, myalgia, back pain dysuria.
Interaction
When used concomitantly, mirtazapine enhances the sedative effect of benzodiazepine derivatives.
A case of developing a hypertensive crisis with simultaneous use with clonidine is described.
When used concomitantly with levodopa, a case of severe psychosis has been described; with sertraline, a case of hypomania has been described.
When used concomitantly with ethanol, it is possible to increase the depressing effect on the central nervous system of ethanol and ethanol-containing drugs.
How to take, course of use and dosage
When taken orally, the effective dose for adults is 15-45 mg / day, mainly 1 time / day before bedtime. The dose is gradually increased to 30-45 mg / day.
The antidepressant effect develops gradually, usually after 2-3 weeks from the start of treatment, but the reception should be continued for another 4-6 months. If no therapeutic effect is observed within 6-8 weeks of treatment, treatment should be discontinued.
Mirtazapine is discontinued gradually.
Special instructions
It is used with caution in patients with epilepsy and organic brain damage, with impaired liver and/or kidney function, acute cardiovascular diseases, with arterial hypotension, when urination is disturbed due to benign prostatic hyperplasia, with angle-closure glaucoma, with diabetes mellitus.
In patients with schizophrenia, mirtazapine may cause increased delusions and hallucinations. When treating the depressive phase of manic-depressive psychosis, this condition can go into the manic phase.
Sudden discontinuation of mirtazapine after prolonged treatment may cause nausea, headache, and poor health.
It should be borne in mind that if symptoms such as fever, sore throat, stomatitis appear during treatment, treatment should be stopped and a clinical blood test should be performed.
If jaundice occurs, mirtazapine should be discontinued.
Do not use concomitantly with MAO inhibitors and within 2 weeks after their withdrawal.
It is possible to develop drug dependence, withdrawal syndrome.
During treatment, patients should refrain from drinking alcohol.
Mirtazapine is not used in children due to the lack of data on the effectiveness and safety of its use in pediatric practice.
Influence on the ability to drive motor vehicles and manage mechanisms
Use with caution in patients whose activity is associated with the need for high concentration of attention and speed of psychomotor reactions.
Form of production
film-coated tablets
Storage conditions
Store in a dry place, protected from light, at a temperature not exceeding 25 °C. Keep out of reach of children.
Shelf
life is 2 years.
Active ingredient
Mirtazapine
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Description
For pregnant women as prescribed by a doctor, For adults as prescribed by a doctor
Indications
Depression
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