Mirtazapine Canon, 30 mg 30 pcs

A tetracycline antidepressant. Enhances central adrenergic and serotonergic transmission. It blocks serotonin 5-HT2- and 5-HT3-receptors, due to this the enhancement of serotonergic transmission is realized only through serotonin 5-HT1-receptors.

Both spatial enantiomers are involved in the antidepressant activity: S(+)-enantiomer blocks α2-adrenoceptors and serotonin 5-HT2-receptors. Moderately blocks histamine H1-receptors, has a sedative effect.

Little effect on α1-adrenoreceptors and cholinoreceptors; in therapeutic doses has no significant effect on the cardiovascular system.

In clinical conditions, anxiolytic and hypnotic effects are also seen, which is why mirtazapine is most effective for anxiety depressions of different genesis. Because of moderate sedative action during treatment it does not actualize suicidal thoughts.

Pharmacokinetics

Mirtazapine is rapidly absorbed from the gastrointestinal tract after oral administration. Bioavailability is 50%. Cmax in plasma is reached after 2 hours.

The Css in plasma is established after 3-4 days of continuous administration. Binding to plasma proteins is 85%.

It is actively metabolized in the liver by demethylation and oxidation followed by conjugation. Dimethyl-mirtazapine is as pharmacologically active as the parent substance.

Mirtazapine is excreted by the kidneys and through the intestine. The T1/2 is 20-40 hrs.

In renal and hepatic insufficiency, the clearance of mirtazapine may be decreased.

Indications

Depressive states (including anhedonia, psychomotor retardation, insomnia, early awakening, weight loss, loss of interest in life, suicidal thoughts and mood lability).

Pharmacological effect

Antidepressant with tetracyclic structure. Strengthens central adrenergic and serotonergic transmission. It blocks serotonin 5-HT2 and 5-HT3 receptors; therefore, the enhancement of 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 and has a sedative effect.

Has little effect on α1-adrenergic receptors and cholinergic receptors; in therapeutic doses does not have a significant effect on the cardiovascular system.

In clinical conditions, anxiolytic and hypnotic effects are also manifested, therefore mirtazapine is most effective for anxious depression of various origins. Due to the moderate sedative effect, it does not actualize suicidal thoughts during the treatment process.

Pharmacokinetics

Mirtazapine after oral administration is rapidly absorbed from the gastrointestinal tract. 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. Plasma protein binding is 85%.

Actively metabolized in the liver by demethylation and oxidation followed by conjugation. Dimethylmirtazapine is as pharmacologically active as the parent substance.

Mirtazapine is excreted by the kidneys and intestines. T1/2 is 20-40 hours.

In case of renal and hepatic failure, the clearance of mirtazapine may be reduced.

Special instructions

Use with caution in patients with epilepsy and organic brain damage, impaired liver and/or kidney function, acute cardiovascular diseases, arterial hypotension, urinary disorders caused by benign prostatic hyperplasia, angle-closure glaucoma, and 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 develop into a manic phase.

Sudden cessation of mirtazapine after long-term treatment may cause nausea, headache, and poor health.

It should be borne in mind that if symptoms such as fever, sore throat, or stomatitis appear during treatment, treatment should be stopped and a clinical blood test done.

If jaundice occurs, mirtazapine should be discontinued.

Should not be used simultaneously with MAO inhibitors and within 2 weeks after their discontinuation.

It is possible to develop drug dependence and 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.

Impact on the ability to drive vehicles and operate machinery

Use with caution in patients whose activities require a high concentration of attention and speed of psychomotor reactions.

Active ingredient

Mirtazapine

Composition

mirtazapine45 mg

Contraindications

Renal and liver failure, pregnancy, lactation, hypersensitivity to mirtazapine.

Side Effects

From the central nervous system and peripheral nervous system: drowsiness, lethargy, emotional lability, changes in mentality, agitation, anxiety, apathy, hallucinations, depersonalization, hostility, mania, epileptic seizures, dizziness, vertigo, hyperesthesia, convulsions, tremor, myoclonus, hyperkinesis, hypokinesia.

From the hematopoietic organs: inhibition of hematopoiesis – granulocytopenia, agranulocytosis, neutropenia, eosinophilia, aplastic anemia, thrombocytopenia.

Metabolism: slight increase in appetite and weight gain; in isolated cases – swelling.

From the cardiovascular system: rarely – orthostatic hypotension.

From the digestive system: nausea, vomiting, constipation, increased appetite, weight gain, dry mouth, thirst, abdominal pain; in isolated cases – increased activity of liver transaminases.

From the reproductive system: decreased potency, dysmenorrhea.

Other: skin rashes, urticaria, flu-like syndrome, shortness of breath, edema syndrome, myalgia, back pain, dysuria.

Interaction

With simultaneous use, mirtazapine enhances the sedative effect of benzodiazepine derivatives.

A case of the development of a hypertensive crisis with simultaneous use with clonidine has been described.

When used simultaneously with levodopa, a case of severe psychosis has been described; with sertraline – a case of hypomania.

When used simultaneously with ethanol, the inhibitory effect of ethanol and ethanol-containing drugs on the central nervous system may be enhanced.

Storage conditions

In a dry place, protected from light, at a temperature not exceeding 25 °C.

Shelf life

2 years.

Manufacturer

Kanonpharma production CJSC, Russia