Remeron, tablets 30 mg, 10 pcs.

Remeron has an antidepressant effect.

Blocks presynaptic alpha₂-adrenoceptors in CNS and increases noradrenergic transmission of nerve impulses. It also enhances serotonergic transmission (the effect is realized only through 5-NT₁ receptors, because 5-NT₂– and 5-NT₃-receptors are blocked.

Pharmacodynamics

The two spatial enantiomers of mirtazapine are involved in the antidepressant activity, with the S(+)-enantiomer blocking alpha₂– and 5-NT₂-receptors, and the R(-)-enantiomer blocks 5-NT₃-receptors.

Blocks H₁ receptors and has a sedative effect. In therapeutic doses has almost no anticholinergic effect and does not affect the function of the cardiovascular system.

Pharmacokinetics

After oral administration, it is rapidly absorbed, bioavailability is about 50%, C_max in blood is reached after about 2 hours. Binding to plasma proteins is about 86%. Equilibrium concentration in blood is established after 3-4 days of continuous use. Pharmacokinetic parameters in the recommended dose range have a linear dependence on the dose. It is actively metabolized in the liver by demethylation and oxidation with subsequent conjugation. Demethylmirtazapine is as pharmacologically active as the parent substance. It is excreted with urine and feces, T_1/2 is 20-40 h, sometimes up to 65 h (which allows the drug to be taken once daily), T_1/2 is shorter in young people than in the elderly. Clearance may decrease in renal or hepatic insufficiency.

Indications

Depressive states.

Pharmacological effect

Remeron has an antidepressant effect.

Blocks presynaptic alpha2-adrenergic receptors in the central nervous system and enhances noradrenergic transmission of nerve impulses. It also enhances serotonergic transmission (the effect is realized only through 5-HT1 receptors, since 5-HT2 and 5-HT3 receptors are blocked.

Pharmacodynamics

Both spatial enantiomers of mirtazapine are involved in the manifestation of antidepressant activity, with the S(+) enantiomer blocking alpha2 and 5-HT2 receptors, and the R(-) enantiomer blocking 5-HT3 receptors.

Blocks H1 receptors and has a sedative effect. In therapeutic doses, it has virtually no anticholinergic effect and does not affect the function of the cardiovascular system.

Pharmacokinetics

After oral administration, it is rapidly absorbed, bioavailability is about 50%, Cmax in the blood is reached in about 2 hours. Plasma protein binding is about 86%. Equilibrium concentration in the blood is established after 3–4 days of continuous use. In the recommended dose range, pharmacokinetic parameters have a linear relationship with dose. Actively metabolized in the liver by demethylation and oxidation followed by conjugation. Demethylmirtazapine is as pharmacologically active as the parent substance. It is excreted in urine and feces, T1/2 is 20–40 hours, sometimes up to 65 hours (which allows you to take the drug once a day), T1/2 is shorter in young people than in older people. Clearance may be reduced with renal or hepatic insufficiency.

Special instructions

Should not be prescribed simultaneously with MAO inhibitors and within 2 weeks after their discontinuation. It should be borne in mind that suppression of hematopoiesis (usually in the form of granulocytopenia or agranulocytosis) often appears after 4-6 weeks and usually disappears after cessation of treatment. If symptoms such as fever, sore throat, stomatitis and other signs of the development of an infectious disease appear, treatment must be stopped and a clinical blood test performed. If jaundice appears, treatment should also be stopped.

Use with caution in patients with epilepsy and organic brain damage (possible development of convulsive seizures), with liver or kidney failure, heart disease with conduction disorders, angina pectoris and acute myocardial infarction, arterial hypotension, in patients with urination disorders, incl. with prostatic hypertrophy, in patients with acute angle-closure glaucoma, patients with diabetes mellitus.

It should be taken into account that during therapy in patients with schizophrenia, psychotic symptoms may increase. When treating the depressive phase of bipolar affective psychosis, the development of mania is possible.

Abrupt withdrawal after long-term use can lead to nausea, headaches and a general deterioration in health.

During treatment, patients should refrain from drinking alcohol. During treatment it is necessary to use reliable methods of contraception.

During treatment, you should avoid performing potentially dangerous activities that require a high speed of psychomotor reactions, for example, driving a car and operating machinery (may impair concentration and level of wakefulness).

Active ingredient

Mirtazapine

Composition

Active ingredient:

mirtazapine

Pregnancy

During pregnancy, use is only possible if absolutely necessary (the safety of use in pregnant women has not been studied). During treatment, breastfeeding should be stopped (no data on penetration into breast milk).

Contraindications

Hypersensitivity

Side Effects

From the nervous system and sensory organs: drowsiness/lethargy (usually appear during the first weeks of treatment), rarely – mania, convulsions, tremor, myoclonus.

From the cardiovascular system and blood (hematopoiesis, hemostasis): rarely – orthostatic hypotension, eosinophilia, granulocytopenia, agranulocytosis, aplastic anemia, thrombocytopenia.

Other: increased appetite and weight gain, rarely – fluid retention and concomitant increase in body weight, increased plasma transaminase activity, skin reactions.

Interaction

Strengthens the sedative effect of benzodiazepines (care should be taken when taking them simultaneously), and the inhibitory effect of alcohol on the central nervous system. Incompatible with MAO inhibitors.

Overdose

Symptoms: pronounced sedative effect.

Treatment: gastric lavage, symptomatic treatment to maintain the function of vital organs and systems.

Storage conditions

In a dry place, protected from light, at a temperature of 2–30 °C

Shelf life

3 years

Manufacturer

N.V.Organon, Netherlands