Mirtazapine Canon pills 45mg, 30pcs

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

In a controlled trial lasting 6 weeks, approximately 16% of 453 patients treated with mirtazapine discontinued treatment due to side effects, compared to 7% of 361 patients treated with placebo. Side effects observed in ≥1% of patients, associated with discontinuation of treatment and recognized as due to mirtazapine (i. e., observed with mirtazapine treatment at least 2 times more often than placebo), include the following: drowsiness 10.4% (2.2%), nausea 1.5% (0%).

The following are side effects that were observed in short-term (6 weeks) placebo-controlled trials in 1% or more cases and were more frequent than in the placebo group (the% occurrence in the placebo group is indicated in parentheses). It should be borne in mind that these data cannot be used to predict the occurrence of side effects in normal medical practice, since the condition of patients and other factors differ from those that prevailed in clinical trials. The given figures for the frequency of side effects may differ from those obtained by other clinical researchers, but they can give the doctor information about the relative contribution of the substance itself and other factors (not related to the drug) to the development of side effects in the study population.

Nervous system and sensory disorders:  sleepiness 54% (18%), asthenia 8% (5%), dizziness 7% (3%), unusual dreams 4% (1%), impaired thinking 3% (1%), tremor 2% (1%), confusion 2% (0%).

From the digestive tract:  dry mouth 25% (15%), increased appetite 17% (2%), constipation 13% (7%).

Other services:  weight gain 12% (2%), flu-like syndrome 5% (3%), back pain 2% (1%), myalgia 2% (1%), increased urination 2% (1%), peripheral edema 2% (1%), dyspnoea 1% (0%).

Adverse effects reported in these clinical trials in at least 1% of patients treated with mirtazapine and observed less frequently than in the placebo group: headache, infection, chest pain, palpitations, tachycardia, orthostatic hypotension, nausea, dyspepsia, diarrhea, flatulence, decreased libido, hypertension, pharyngitis, rhinitis, sweating, amblyopia, tinnitus, taste distortion.

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.

Overdose

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

Keep out of reach of children.

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

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