Remeron coated pills 30mg N10
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Active ingredients
Mirtazapine
Release form
Pills
Composition
Mirtazapine 30 mg.
Pharmacological effect
The drug Remeron (mirtazapine) is a tetracyclic antidepressant with a predominantly sedative effect. The drug is most effective in depressive conditions with the presence in the clinical picture of symptoms such as inability to experience pleasure and joy, loss of interest (anhedonia), psychomotor retardation, sleep disorders (especially in the form of early awakenings) and weight loss, as well as other symptoms: suicidal thoughts and daily mood swings .; The antidepressant effect of the drug Remeron usually occurs after 1-2 weeks of treatment .; Mirtazapine is an antagonist of presynaptic 2-adrenoreceptors in the central nervous system and enhances central noradrenergic and serotonergic transmission of nerve impulses. At the same time, enhancement of serotonergic transmission is realized only through serotonin 5-HT1 receptors, since mirtazapine blocks serotonin 5-HT2 and 5-HT3 receptors. Both enantiomers of mirtazapine are believed to have antidepressant activity, S (+) enantiomer - blocking 2-adreno and serotonin 5-HT2 receptors, and R (-) enantiomer - blocking serotonin 5-HT3 receptors .; The sedative properties of mirtazapine are due to its antagonistic activity against H1-histamine receptors .; Mirtazapin is usually well tolerated. In therapeutic doses, it has almost no m-anticholinergic blocking effect and has virtually no effect on the cardiovascular system.
Pharmacokinetics
After oral administration, mirtazapine is rapidly absorbed (bioavailability of about 50%), reaching Cmax in blood plasma after approximately 2 hours. About 85% of mirtazapine is bound to plasma proteins. The average T1 / 2 ranges from 20 to 40 hours (rarely up to 65 hours). Shorter T1 / 2 is observed in young people. The equilibrium concentration of the substance is reached in 3-4 days and in the future it does not change. In the recommended dose range, the pharmacokinetic indicators of mirtazapine are linearly dependent on the administered dose of the drug. Eating does not affect the pharmacokinetics of the drug .; Mirtazapine is actively metabolized and excreted in the urine and feces for several days.The main pathways of its metabolism in the body are demethylation and oxidation, followed by conjugation. Cytochrome P450 isoenzymes (CYP2D6 and CYP1A2) are involved in the formation of 8-hydroxymetabolite mirtazapine, while CYP3A4 presumably determines the formation of N-demethylated and N-oxidized metabolites. Demetilmirtazapin is pharmacologically active .; The clearance of mirtazapine decreases with renal or hepatic insufficiency.
Indications
Depressive conditions requiring pharmacotherapy.
Contraindications
Hypersensitivity to mirtazapine.
Use during pregnancy and lactation
The safety of the use of Remeron during pregnancy in humans has not been established, however, no animal teratogenic effect has been identified, so it can be used during pregnancy only when the benefit to the mother outweighs the potential risk to the fetus .; The use of the drug Remeron during lactation is not recommended due to the lack of data on its excretion in human breast milk.
Dosage and administration
For adults, the effective daily dose is usually 15-45 mg. The standard daily dose is 30 mg. Appointed mainly 1 time / day before bedtime. Therapy should be continued after the complete disappearance of the clinical symptoms of depression for at least another 4-6 months. The drug should be discontinued gradually .; In elderly patients, the recommended dose is the same as in younger patients .; In children, clinical studies on the use of the drug were not conducted.
Side effects
Patients with depression have a number of symptoms due to the disease, so it is sometimes difficult to distinguish between the symptoms associated with the disease and the symptoms caused by the use of the drug. The following classification is used to indicate the frequency of side effects: very often (≥1 / 10), often (≥1 / 100 and ≤1 / 10), infrequently (> 1/1000 and ≤1/100), rarely (> 1/10000 and ≤1 / 1000), the frequency is not set (≤1 / 10,000) .; Blood and lymphatic system disorders: frequency not established - bone marrow suppression (granulocytopenia, agranulocytosis, aplastic anemia and thrombocytopenia), eosinophilia .; Nervous system disorders: very often, drowsiness (which can lead to impaired concentration), usually occurring during the first weeks of treatment. (N.B.dose reduction usually does not lead to less sedative effect, but may reduce the effectiveness of the antidepressant), sedation, headache; often - lethargy, dizziness, tremor; infrequently - paresthesia, restless legs syndrome, syncope; rarely - myoclonus, very rarely - convulsions (stroke), serotonin syndrome, paresthesia of the oral mucosa .; Violations of the gastrointestinal tract: very often - dry mouth; often - nausea, diarrhea, vomiting; infrequently - reduced sensitivity of the oral mucosa; frequency is not installed - swelling of the oral mucosa .; Violations of the skin and subcutaneous tissues: often - skin rash .; Disorders of the musculoskeletal and connective tissues: often - arthralgia, myalgia, back pain .; Endocrine disorders: frequency not established - violation of antidiuretic hormone secretion; ; Metabolic and nutritional disorders: very often - increased appetite .; Vascular disorders: often - orthostatic hypotension; infrequently - arterial hypotension .; General disorders and disorders at the injection site: often - local edema; infrequently - fatigue .; Disorders of the liver and biliary tract: rarely - increase the activity of serum transaminases .; Mental disorders: often - unusual dreams, confusion, anxiety, insomnia; infrequently - nightmares, mania, agitation, hallucinations, psychomotor agitation (including akatasia and hyperkinesia); frequency not established - suicidal ideation, suicidal behavior .; Laboratory and instrumental data (according to the results of post-registration studies): very often - an increase in body weight.
Overdose
Experience with an overdose of Remeron alone indicates that the symptoms are usually mild. Reported CNS depression, accompanied by disorientation and prolonged sedation combined with tachycardia and a weak increase or decrease in blood pressure. However, there is a possibility of more severe results (including death) at doses much higher than the therapeutic dose, especially when overdosing with several drugs taken at the same time.In case of overdose, symptomatic therapy should be carried out to maintain the vital functions of the body. Activate charcoal or flush the stomach.
Interaction with other drugs
Pharmacokinetic interaction; - Mirtazapine is intensively metabolized with participation of CYP2D6 and CYP3A4 isoenzymes, and to a lesser extent with participation of CYP1A2 isoenzyme. A study of the interaction in healthy volunteers showed that paroxetine, an inhibitor of the isoenzyme CYP2D6, does not affect the pharmacokinetics of mirtazapine in the equilibrium state. Introduction in combination with a potent inhibitor of the CYP3A4 isoenzyme, ketoconazole, increased the maximum plasma concentration and AUC of mirtazapine by approximately 40% and 50%, respectively. Care should be taken when using mirtazapine in combination with powerful inhibitors of the isoenzyme CYP3A4, HIV protease inhibitors, azole antifungal drugs, erythromycin or nefazodone .; - carbamazepine and phenytoin, inducers of the CYP3A4 isoenzyme, increased clearance of mirtazapine approximately two times, which resulted in a 45-60% decrease in plasma concentrations of mirtazapine. If carbamazepine or another inducer of hepatic metabolism (for example, rifampicin) is added to mirtazapine therapy, the dose of mirtazapine should be increased if necessary. If you stop treatment with this drug, it may be necessary to reduce the dose of mirtazapine .; - when used in combination with cimetidine, the bioavailability of mirtazapine may increase by more than 50%. The dose of mirtazapine, if necessary, should be reduced at the beginning of treatment in combination with cimetidine or increased when discontinuing treatment with cimetidine .; - in studies of in vivo interactions, mirtazapine did not affect the pharmacokinetics of risperidone or paroxetine (CYP2D6 isoenzyme substrate), carbamazepine (CYP3A4 isoenzyme substrate), amitriptyline, cymetidine or phenytoin .; - no significant clinical effects or changes in pharmacokinetics were observed in humans during treatment with mirtazapine in combination with lithium .; Pharmacodynamic interaction; - Mirtazapin should not be used in combination with MAO inhibitors or for two weeks after stopping treatment with an MAO inhibitor .; - Mirtazapin may enhance the sedative properties of benzodiazepines and other sedatives.Caution should be exercised when prescribing these medicines along with mirtazapine .; - Mirtazapin may enhance the depressive effect of alcohol on the central nervous system. Therefore, patients should be warned about the need to avoid alcohol consumption .; - in case of using other serotonergic drugs (for example, selective serotonin and venlafaxine reuptake inhibitors) in combination with mirtazapine, there is a risk of interaction, which can lead to the development of serotonin syndrome. Based on the post-registration experience of using the drug, it turned out that serotonin syndrome occurs very rarely in patients receiving treatment with mirtazapnn in combination with selective serotonin reuptake inhibitors or venlafaxine. If it is believed that such a combination is therapeutically necessary, then in this case, the dose should be carefully changed and the signs of the onset of sustained serotonergic overstimulation should be directly monitored .; - Mirtazapine at a dose of 30 mg once a day caused a small but statistically significant increase in MHO (international normalized ratio) in subjects treated with warfarin. A more pronounced effect at a higher dose of mirtazapine cannot be ruled out. It is recommended to control MHO in case of treatment with warfarin in combination with mirtazapine.
special instructions
When using the drug Remeron, it should be borne in mind that worsening of psychotic symptoms can occur when antidepressants are used to treat patients with schizophrenia or other psychotic disorders; paranoid ideas may increase; The depressive phase of a manic-depressive psychosis during treatment can be transformed into a manic phase .; In young people (under 24 years) with depression and other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing Remeron in young people (under 24 years), the risk of suicide should be correlated with the benefits of using the drug. In short-term studies, the risk of suicide was not increased in people over 24 years old, and in people over 65 years old - somewhat decreased. Any depressive disorder itself increases the risk of suicide.Therefore, during treatment, the patient should be monitored in order to identify violations or behavioral changes, as well as suicidal tendencies .; Although the drug Remeron is not addictive, based on post-registration experience, it turned out that abrupt cessation of treatment after prolonged use can sometimes cause withdrawal symptoms. Most undo reactions are weak and self-limiting. The most frequently reported withdrawal symptoms were dizziness, agitation, anxiety, headache, and nausea. Although they were reported as withdrawal symptoms, it should be understood that these symptoms may be associated with the underlying disease. It is recommended to stop treatment with mirtazapine gradually .; Elderly patients are usually more sensitive, especially with regard to side effects. In clinical studies of the drug Remeron, it was not noted that in elderly patients, side effects are more common than in other age groups, but they may be more pronounced; however, data is still limited .; If signs of jaundice appear, treatment should be interrupted .; Patients are advised to avoid the use of alcohol during treatment with Remeron .; Inhibition of bone marrow function, usually manifested in the form of granulocytopenia or agranulocytosis, is rarely observed when using the drug Remeron. Appears mostly after 4-6 weeks of treatment and is reversible after cessation of treatment. The physician should carefully consider (and inform the patient) symptoms such as fever, sore throat, stomatitis, and other signs of flu-like syndrome; If these symptoms appear, stop the treatment and have a blood test .; Based on the post-registration experience, it turned out that serotonin syndrome occurs very rarely in patients receiving treatment with Remeron only .; Influence on ability to drive and work with mechanisms. Drug Remeron; may reduce concentration. In the course of treatment with antidepressants, patients should avoid performing potentially hazardous activities that require high-speed psychomotor reactions, such as driving a car or controlling machinery.