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Active ingredients
Mianserin
Release form
Pills
Composition
Active ingredient: Mianserin Auxiliary substances: potato starch, anhydrous colloidal silicon dioxide, magnesium stearate, methylcellulose, calcium hydrogen phosphate, hypromellose, macrogol, titanium dioxide (E 171). Active ingredient concentration (mg): 30 mg
Pharmacological effect
Mianserin belongs to the group of piperazine-azepine compounds that are not chemically related to tricyclic antidepressants (TCAs). Lerivon enhances noradrenergic brain transmission by blocking alpha 2 receptors and inhibiting norepinephrine reuptake. In addition, interactions with serotonin receptors in the CNS were found. The activity of the drug Lerivon in relation to histamine H1 receptors and antagonism to α1-adrenoreceptors is responsible for its sedative properties, the drug also has an anxiolytic effect, which is important in the treatment of patients with anxiety disorders and sleep disorders associated with depressive disorders. Lerivon is well tolerated as older people and patients with cardiovascular diseases. In therapeutically effective doses, the drug Lerivon does not actually possess anticholinergic activity and has virtually no effect on the cardiovascular system. Compared with TCA, it causes less cardiotoxic effects in overdose. The drug Lerivon is not an antagonist of sympathomimetic and antihypertensive drugs.
Pharmacokinetics
Absorption and distribution After ingestion of the active substance of the drug Lerivon, mianserin, quickly and well absorbed, reaching Cmax in plasma after 3 hours. Bioavailability is about 20%. The binding of mianserin to plasma proteins is about 95%. Equilibrium plasma levels are reached after 6 days. Metabolism and excretion of T1 / 2 (21-61 hours) allows to justify a single daily dose. Mianserin is extensively metabolized and excreted in urine and feces in 7-9 days. The main pathways of biotransformation are demethylation and oxidation, followed by the formation of conjugates.
Indications
Depression of various etiologies.
Contraindications
Mania; Liver disease with severe dysfunction; Hypersensitivity to mianserin or to any component of the drug; The drug Lerivon should not be used in children and adolescents under the age of 18 years.
Precautionary measures
Do not exceed the recommended dose. With caution: Hepatic or renal failure, chronic heart failure, angle-closure glaucoma, prostatic hypertrophy, diabetes mellitus.
Use during pregnancy and lactation
Although animal experiments and limited data on humans indicate that mianserin does not cause prenatal or neonatal harm and that mianserin is excreted in human milk only in very small amounts, the use of Lerivon during pregnancy or lactation should be evaluate the possible risks to the fetus or newborn.
Dosage and administration
Tablets should be taken orally, when necessary with a glass of water, and swallowed without chewing. Adults: Dosing regimen is determined individually. An initial dose of 30 mg per day is recommended. This dose can be gradually increased every few days for optimal clinical response. The effective daily dose is usually 60-90 mg. Elderly: Dosing regimen is determined individually. The initial dose should be 30 mg. This dose can be gradually increased every few days. A satisfactory clinical response may require a lower dose than usual for adults. Children: The drug Lerivon should not be used in children and adolescents under the age of 18 years (see Sections Contraindications, Special Instructions). The daily dose can be divided into several doses or preferably (taking into account the favorable effect on sleep) in the form of a single dose for the night. Treatment with an appropriate dose should result in a positive response to treatment after 2-4 weeks. In case of insufficient response to treatment, the dose may be increased. If after this, after another 2-4 weeks, there is no response to treatment, then in this case, treatment with the drug should be stopped. It is recommended to conduct antidepressant treatment for 4-6 months after the onset of clinical improvement.Abrupt cessation of treatment with Lerivon in very rare cases causes withdrawal symptoms.
Side effects
Frequent undesirable manifestations of Lerivon's action are disorders of the central nervous system: hypomania, convulsive readiness with hyperkinetic syndrome, neuroleptic malignant syndrome. At the initial stage of taking the drug, it is possible that the addiction to bradycardia, various arrhythmias. Pharmacokinetic features of the drug cause the appearance of increased activity of liver enzymes and jaundice in some cases. Agranulocytosis and granulocytopenia are possible in the blood picture. In some patients, arthralgia and an allergic rash occurred as adverse reactions to taking Lerivon.
Overdose
Symptoms of acute overdose are usually limited to an increase in the duration of the sedative effect. Cardiac arrhythmias, convulsions, severe hypotension and respiratory depression are rare. There is no specific antidote. Treatment consists of gastric lavage combined with symptomatic and supportive therapy for vital functions.
Interaction with other drugs
Lerivon may increase the inhibitory effect of alcohol on the central nervous system, and patients should be advised to refrain from alcohol during treatment. Lerivon should not be consumed simultaneously with MAO inhibitors or for the next two weeks after the course of treatment with these agents. Lerivon does not interact with betanidin, clonidine , methyldopa, guanethidine and propranolol (both in combination with and without hydralazine). However, it is recommended to control blood pressure in patients who are simultaneously receiving treatment with antihypertensive drugs. As in the case of other antidepressants, Lerivon may interfere with the metabolism of coumarin derivatives, for example, warfarin, which requires monitoring.
special instructions
Use in children and adolescents under the age of 18 years. The drug Lerivon should not be used in children and adolescents under the age of 18 years. In clinical studies, suicidal behavior (suicidal attempts and suicidal thoughts) and hostility (mainly aggressiveness, oppositional behavior and anger) were more often observed among children and adolescents treated with antidepressants compared with those who received a placebo.If, on the basis of clinical need, a decision is made to conduct treatment, then the patient should be carefully monitored for the occurrence of suicidal symptoms. In addition, there are no data on long-term safety in children and adolescents concerning growth, maturation, and cognitive and behavioral development. Suicide / suicidal thoughts Depression is associated with an increased risk of suicidal thoughts, self-harm and suicide (suicidal gestures). This risk persists until significant remission occurs. Since there may be no improvement during the first few weeks, patients should remain under direct control until improvement occurs. Patients with a history of suicidal gestures, showing a high degree of suicidal imagination before starting treatment, and young adults are at greater risk of suicidal thoughts or suicidal attempts, and they should be carefully monitored during treatment. Patients (and caregivers) should be warned about the need to control Vat sudden emergence of suicidal ideation and immediate access to medical care in the event of such simptomov.Soobschalos that during treatment with Lerivon noted bone marrow suppression, which is usually expressed in the form of granulocytopenia or agranulocytosis. These reactions most often occurred after 4-6 weeks of treatment and were usually reversible upon discontinuation of treatment; they were observed in all age groups, but more often in elderly patients. If a patient has a fever, pharyngitis, stomatitis, or other signs of infection, then treatment should be stopped and the expanded blood formula should be checked. Lerivon preparation, like other antidepressants, in susceptible subjects suffering from bipolar depressive illness can cause hypomania. In this case, treatment with Lerivon should be discontinued. During treatment with Lerivon, it is recommended that very careful monitoring of patients with hepatic or renal failure, heart disease, and diabetes. Patients with angle-closure glaucoma or symptoms of prostatic hypertrophy should be monitored,due to the unpredictability of anticholinergic side effects with Lerivon. In case of jaundice, treatment with the drug should be discontinued. In case of seizures, treatment with the drug should be stopped. Impact on the ability to drive or work with mechanisms treatment. Patients undergoing treatment with Lerivon should avoid activities that pose a potential danger, such as driving a car or working with machinery.