Mirtazapine Canon, 45 mg 30 pcs

A tetracycline antidepressant. Enhances central adrenergic and serotonergic transmission. It blocks serotonin 5-HT2- and 5-HT3-receptors, in connection with this strengthening 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).

Active ingredient

Composition

mirtazapine – 45 mg.

How to take, the dosage

When administered orally, the effective dose for adults is 15-45 mg/day preferably once/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 use should be continued for another 4-6 months. If no therapeutic effect is noted during 6-8 weeks of treatment, treatment should be discontinued.

Withdrawal of mirtazapine should be done gradually.

Interaction

When used concomitantly, mirtazapine increases the sedative effect of benzodiazepine derivatives.

A case of hypertensive crisis has been described when used concomitantly with clonidine.

In concomitant use with levodopa a case of severe psychosis has been described; with sertraline a case of hypomania.

Concomitant use with ethanol may increase the CNS depressant effects of ethanol and ethanol-containing drugs.

Special Instructions

With caution, use in patients with epilepsy and organic brain lesions, hepatic and/or renal dysfunction, acute cardiovascular disease, arterial hypotension, urinary disorders due to benign prostatic hyperplasia, closed-angle glaucoma, diabetes mellitus.

In patients with schizophrenia, mirtazapine may cause increased delirium, hallucinations. When treating the depressive phase of manic-depressive psychosis, this condition may progress to the manic phase.

A sudden discontinuation of mirtazapine after long-term treatment may cause nausea, headache, and worsening of well-being.

Please note that if symptoms such as fever, sore throat, stomatitis occur during treatment, treatment should be stopped and a clinical blood test done.

Mirtazapine should be stopped if jaundice occurs.

Do not use concomitantly with MAO inhibitors and for 2 weeks after their withdrawal.

The development of drug dependence and withdrawal syndrome is possible.

Patients should refrain from drinking alcohol during treatment.

Mirtazapine is not used in children due to lack of data on the effectiveness and safety of its use in pediatric practice.

Impact on driving and operating ability

Perhaps with caution in patients whose activities require a high level of concentration and quick psychomotor reactions.

Contraindications

Hepatic and renal failure, pregnancy, lactation, hypersensitivity to mirtazapine.

Side effects

In controlled trials lasting 6 weeks, approximately 16% of 453 patients receiving mirtazapine discontinued treatment because of side effects, compared with 7% of 361 patients receiving placebo. Side effects observed in ≥1% of patients associated with treatment discontinuation and found to be due to mirtazapine (i.e., observed with mirtazapine at least twice as often as placebo) included the following: drowsiness 10.4% (2.2%), nausea 1.5% (0%).

The following are side effects that occurred in short-term (6-week) placebo-controlled trials 1% or more of the time and were more frequent than in the placebo group (the % occurrence in the placebo group is shown in parentheses). Note that these data cannot be used to predict the occurrence of side effects in routine medical practice, because patient conditions and other factors differ from those that prevailed in clinical trials. The figures given for the incidence of side effects may differ from those obtained by other clinical researchers, but they can give the physician information about the relative contribution of the substance itself and other factors (not related to the drug) in the development of side effects in the study population.

Nervous system and sense organs: drowsiness 54% (18%), asthenia 8% (5%), dizziness 7% (3%), unusual dreaming 4% (1%), impaired thought process 3% (1%), tremor 2% (1%), confusion 2% (0%).

Gastrointestinal organs: dry mouth 25% (15%), increased appetite 17% (2%), constipation 13% (7%).

Others: weight gain 12% (2%), flu-like syndrome 5% (3%), back pain 2% (1%), myalgia 2% (1%), urinary frequency 2% (1%), peripheral edema 2% (1%), dyspnea 1% (0%).

The adverse effects noted in these clinical trials in at least 1% of patients receiving mirtazapine and observed less frequently than in the placebo group were Headache, infection, chest pain, palpitations, tachycardia, orthostatic hypotension, nausea, dyspepsia, diarrhea, flatulence, decreased libido, hypertension, pharyngitis, rhinitis, sweating, amblyopia, tinnitus, perversion of taste.

Overdose

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

Store out of the reach of children.

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