Expiration date: 07/2025

Structure and Composition:

1 tablet coated liner contains mianserin hydrochloride 30 mg and auxiliary substances (potato starch, colloidal silicon dioxide, magnesium stearate, methyl cellulose, calcium hydrogen phosphate, methyl hydroxypropyl cellulose, polyethylene glycol, titanium oxide) in blisters of 10 pcs., In a cardboard bundle 2 packs.

Characteristic:

Tablets, film-coated, white, oblong, has a lenticular form with the code on the right side and marked «Organon» on the other, with a transverse line on the front surface.

Refers to a group piperazino-azepine derivatives and different from the tricyclic antidepressants (TCAs), lack of side chain characteristic of tricyclics.

Pharmachologic effect:

Blocks presynaptic alpha2-adrenergic receptors increases the release of neurotransmitter into the synaptic cleft, amplifies adrenergic transmission in the brain. It affects the alpha1-adrenergic receptors and H1 histamine receptors. It has a sedative effect.

Pharmacokinetics:

If ingestion is rapidly absorbed from the gastrointestinal tract, bioavailability is 20%. Cmax in the blood is reached after 3 hours Linking blood protein -. 95%. The equilibrium concentration in the blood reached after 6 days of admission. It is metabolized in the liver by demethylation and oxidation followed by conjugation of metabolites. Return with urine and faeces. T1 / 2 - 21-61 hours (allowing you to use the drug 1 time per day).

Clinical Pharmacology:

When used in therapeutic doses holinoliticheskoy shows no activity has no significant effect on the cardiovascular system.

It is effective for depression combined with anxiety, as well as sleep disorders on the background of depression.

Dosage:

Approved by the Pharmacological Committee of the Ministry of Health of the Russian Federation December 30, 1999 Minutes ?11 (b)

INSTRUCTION for medical use of the drug lerivon (LERIVON)

Description

White convex on both sides, oblong film-coated tablets, with a transverse line on the front surface. Each tablet inscriptions - on the front side code ST-7, on the back - the name of the manufacturer «Organon».

Composition

Each tablet contains as active ingredient 30 mg of mianserin hydrochloride.

Excipients: potato starch, colloidal silicon dioxide, magnesium stearate, methylcellulose, calcium phosphate, methylhydroxypropylcellulose, polyethylene glycol, titanium oxide.

pharmacological properties

pharmacodynamics

It has antidepressant action. It refers to a group piperazino-azepine derivatives and different from the tricyclic antidepressants (TCAs). The chemical structure of mianserin no side chain characteristic of tricyclics that is believed to determine their anticholinergic effects. Lerivon antidepressant efficacy comparable to other modern antidepressants. Lerivon also possesses anxiolytic activity, which is important in the treatment of patients whose depression is combined with anxiety. The presence of sedation associated with the effect of mianserin on the alpha1-adrenergic receptors and H1 histamine receptors, allows Lerivon for the treatment of sleep disorders that occur against a background of depression. Lerivon well tolerated, including the elderly and patients with cardiovascular disease. When used in therapeutic doses Lerivon has no anticholinergic effect and has no significant effect on the cardiovascular system. In case of overdose has lerivon significantly lower than the TCAs, cardiotonic effect. Lerivon not interact with sympathomimetics and antihypertensive drugs, the effect of which is associated with the effect on beta-adrenergic receptors (such as betanidin) or alpha-adrenoceptor (e.g., clonidine, methyldopa), and has no influence on the action of anticoagulants coumarin (e.g., phenprocoumon).

Pharmacokinetics

When taken orally lerivon, mianserin - the active ingredient is absorbed quickly. Its bioavailability is 20%. Mianserin Cmax plasma levels achieved after 3 h. Associated with the blood proteins 95%. T1 / 2 - 21-61 h (this explains the possibility of the drug 1 time per day). Stable mianserin blood concentrations reached after 6 days of its reception. Metabolized and excreted in the urine and feces within 7-9 days. The main pathways of biotransformation - demethylation and oxidation, followed by conjugation of metabolites.

Testimony

Depressions of different genesis.

Contraindications

• Mania,
  
• Severe hepatic dysfunction,
  
• The acute phase of myocardial infarction,
  
• Pregnancy,
  
• breast-feeding,
  
• Up to age 18 years.
  

Side effects

In the early days of admission may cause drowsiness, which later passes. Intensity sleepiness independent of dose. Dose reduction does not reduce drowsiness, but reduces the antidepressant effect, so to ensure optimal antidepressant effects lerivon dosage should not be reduced.

In rare cases, a violation of hematopoiesis, agranulocytosis, convulsions, hypomania, hypotension, arthralgia, peripheral edema, gynecomastia, abnormal liver function, hypokinesia, rash.

Interaction

Do dampening effect of alcohol on the central nervous system (should refrain from drinking alcohol during the course of treatment). Incompatible with MAO inhibitors (avoid the simultaneous application and for the following 2 weeks after completing the course of treatment of these funds).

Lerivon no effect on the action of drugs such as betanidin, clonidine, methyldopa, guanethidine or propranolol, including in combination with hydralazine. In the course of therapy with antihypertensive drugs necessary to control blood pressure.

Overdose

Symptoms usually prolonged sedation, unlikely - cardiac arrhythmia, convulsions, severe hypotension and respiratory depression. No specific antidote.

Treatment: gastric lavage, symptomatic therapy aimed at maintaining vital functions.

Dosing and Administration

The inside is not liquid, squeezed water or other liquid.

Adult dosage selected individually. The recommended initial daily dose - 30 mg. The dosage can be increased to achieve the optimal therapeutic effect. The average effective daily dose - 60-90 mg.

Older patients the dose selected individually, the initial dose - 30 mg, a further gradual increase. Supporting effective dose may be somewhat lower than for patients of mature age.

In the absence of clinical experience, doses are not developed for children.

The daily dose can be divided into several stages, but considering the beneficial effect on sleep drug, preferably in one step to take at night.

Treatment of adequate doses should lead to positive results within 2-4 weeks of therapy. In case of insufficient effectiveness of the daily dose increased. In the absence of positive dynamics over the next 2-4 weeks of treatment, therapy should be discontinued lerivon. After clinical improvement achieved, to maintain a positive effect, the treatment should be continued over the next 4-6 months. Stopping lerivon rarely causes withdrawal symptoms.

Special instructions

Lerivon can influence psychomotor reactions during the first few days of treatment. Therefore, the drug should not be used during the drivers of vehicles and people skills relate to the high concentration of attention.

Lerivon, like other antidepressants, may cause hypomania in bipolar disorder patients. In this case, treatment should be discontinued lerivon.

There are reports that the treatment lerivon may suppress bone marrow function (or pancytopenia agrunolitsitoz). This manifests itself, usually within 4-6 weeks after starting treatment, but bone marrow function is fully restored at the end of a course of therapy. In the event the patient fever, sore throat, stomatitis or other signs of infectious diseases, clinical blood test is necessary. Older people have such adverse reactions may occur more frequently than patients in other age groups.

When treating patients with diabetes, cardiac, hepatic or renal insufficiency should observe the usual precautions, and doses of concomitant treatments should be under constant medical supervision. Patients with narrow-angle glaucoma and in patients with suspected prostate hypertrophy must be under constant medical supervision, although usually not anticholinergic effects associated with taking lerivon.

When jaundice or seizures lerivon treatment should be discontinued.

Release Form

Tablets for oral use 30 mg mianserin hydrochloride, in blisters of 20 tab., In a cardboard bundle one package.

Storage conditions

At a temperature of 2-30 ° C in a dark, dry place inaccessible to children.

Shelf life

5 years from date of manufacture when stored.