Mirtalan - instructions for use, doses, side effects, contraindications

Excipients: lactose monohydrate 198.00 mg, corn starch 60.0 mg, giprolose 6.00 mg, silicon dioxide colloidal anhydrous 3.00 mg, magnesium stearate 3.0 mg;

Sheath: Opaprai II light brown: polyvinyl alcohol 2,640 mg, lecithin OD 10 mg, titanium dioxide 1,128 mg, macrogol 3350 0.741 mg, talc 1,200 mg, iron dye oxide yellow 0.0708 mg, ferric oxide red oxide 0.0066 mg, iron dye oxide black 0.0036 mg

Description:

Round, biconvex light brown colored tablets, film-coated, with a risk on one side

Pharmacotherapeutic group:Antidepressant

ATX: & nbsp

N.06.A.X.11 Mirtazapine

Pharmacodynamics:

Antidepressant tetracyclic structure. Antagonist of presynaptic α₂receptors in the central nervous system, strengthens the central adrenergic and serotonergic transmission. Blocks 5-HT₂ and 5-HT₃ receptors, in connection with which the enhancement of serotonergic transmission is realized through 5-HT₁-receptors. In the manifestation of antidepressant activity both spatial enantiomers participate: S(+)-the enantiomer blocks α₂-adrenoceptors and gray or new 5-HT₂-receptors, R(-)- enantiomer blocks 5-HT₃-receptors. It blocks histamine H₁receptors, has a sedative effect.

Mirtazapine is usually well tolerated. In therapeutic doses, it has almost no anticholinergic effect and practically no effect on the cardiovascular system.

In clinical conditions, anxiolytic and hypnotic properties also appear, so mirtazapine is most effective in anxiety depressions of different genesis. Thanks to a moderate sedative effect during the treatment, suicidal thoughts are not actualized.

Antidepressant effect is manifested after 1-2 weeks of treatment.

Pharmacokinetics:

After oral administration of the drug, mirtazaline is rapidly absorbed (bioavailability of about 50%), reaching a maximum concentration in the blood plasma after about 2 hours. About 85% of mirtazaline binds to plasma proteins. The average half-life is between 20 and 40 hours (rarely up to 65 hours). A shorter half-life is observed in young people. The equilibrium concentration is established after 3-5 days. AT The recommended dosage range of pharmacokinetic parameters of mirtazapine is linear depending on the administered dose of the drug. Eating does not affect the pharmacokinetics of the drug

Mirtazapine is actively metabolized and excreted in urine and feces for several days. The main ways of its metabolism in the body are demethylation and oxidation followed by conjugation. Cytochrome P450-dependent enzymes CYP2D6 and CYP1A2 participate in the formation of 8-hydroxy metabolite mirtazapine, while CYP3A4 presumably defines education N-demethylated (active) and N-oxidized metabolites.

The clearance of mirtazapine decreases with renal or hepatic insufficiency.

Indications:

Depressive states of various etiologies.

Contraindications:

Hypersensitivity to mirtazaline or other components of the drug.

Simultaneous reception with monoamine oxidase (MAO) inhibitors.

Lactose intolerance (lactase deficiency).

Glucose-galactose malabsorption.

Age to 18 years (effectiveness and safety not established).

Carefully:

- Epilepsy and organic lesions of the brain (against the background of mirtazapine therapy, in rare cases, the development of convulsive conditions);

- hepatic or renal insufficiency;

- heart disease (conduction disorder, angina pectoris, or recent myocardial infarction);

- cerebrovascular diseases (including ischemic attacks in the anamnesis);

- arterial hypotension and conditions predisposing to hypotension (including dehydration and hypovolemia);

- in patients who abuse drugs, with drug dependence, mania, hypomania;

- violation of urination, incl. with hyperplasia of the prostate;

- acute angle-closure glaucoma and increased intraocular pressure;

- diabetes.

Pregnancy and lactation:

The safety of using Mirtazapine during pregnancy is not established, so it can be used during pregnancy only if the benefit to the mother exceeds the potential risk to the fetus and under the supervision of the doctor.

The use of the drug during lactation and breast-feeding is not recommended (there is no data on excretion of the drug with breast milk).

Dosing and Administration:

Inside, not liquid, squeezed a little water.

Adults: the initial dose is 15 mg per day, after 4 days it can be increased to 30 mg / day, after 10 days, in the absence of effect - up to 45 mg per day.

Elderly patients: the recommended dose is the same as for adults.

To achieve a satisfactory effect and to ensure safety, an increase in the dose should be carried out under close medical supervision.

With renal and hepatic insufficiency: the daily dose should be reduced by approximately 1/3.

The daily dose should be taken at one time, at night. It is also possible to take fractional doses evenly distributed throughout the day.

The course of treatment - 4-6 months (until the disappearance of clinical symptoms).

Treatment is canceled gradually.If there is no effect of therapy during 6-8 weeks of treatment, treatment should be discontinued.

Side effects:

Frequency: very often (10% or more), often (from 1 to 10%), infrequently (from 0.1 to 1%), rarely (from 0.01 to 0.1%), very rarely (less than 0, 01%).

From the nervous system: often - drowsiness (with reduced concentration of attention) occurs more often in the first weeks of treatment (lowering the dose usually does not lead to a decrease in sedation, but may reduce the antidepressant effect); dizziness, headache; rarely - nightmares or bright dreams, mania, agitation, confusion, hallucinations, anxiety, sleep disturbance, psychomotor agitation (including akathisia, hyperkinesis), convulsions, tremor, myoclonus, paresthesia, restless legs syndrome, fainting; very rarely - serotonin syndrome, paresthesia of the oral mucosa.

On the part of the organs of hematopoiesis: rarely - oppression hemopoiesis (granulocytopenia, agranulocytosis, aplastic anemia and thrombocytopenia), eosinophilia.

From the digestive system: often - increased appetite; infrequently - nausea; rarely - dry mouth, diarrhea, vomiting, increased activity of "liver" transaminases; very rarely - paresthesia of the oral mucosa, edema of the oral mucosa.

From the genitourinary system: dysmenorrhea.

From the side of the cardiovascular system: orthostatic hypotension.

From the side of the musculoskeletal system: rarely - arthralgia, myalgia.

Allergic reactions: rarely - skin rash.

Other: often - edematic syndrome (generalized or local), weight gain; rarely - fatigue, withdrawal syndrome,

Overdose:

Oppression of the central nervous system, disorientation, pronounced sedation, hallucinations, tachycardia, increased or decreased blood pressure.

Treatment: gastric lavage, Activated carbon, oxygenation and ventilation of the lungs, symptomatic therapy.

Interaction:

Mirtazapine may enhance the sedative effects of benzodiazepines and other sedatives.

Mirtazapine can enhance the inhibitory effect of ethanol on the central nervous system.

Mirtazapine should not be used concurrently with MAO inhibitors or within 2 weeks after discontinuation of their use.

Caution is required in cases where powerful inhibitors CYP3A4, such as HIV protease inhibitors, antifungal agents of the azole group, erythromycin and nefazodone, are administered concomitantly with mirtazalin.

Inductors CYP3A4 (carbamazepine and phenytoin) increase the clearance of mirtazaline approximately 2-fold, which reduces its plasma concentrations by 45-60%. If it is necessary to combine mirtazalin with carbamazepine or other inducer of metabolism in the liver (incl. rifampicin), the dose of mirtazaline should be increased. After cessation of treatment with this combination, it may be necessary to reduce the dose of mirtazaline.

Cimetidine can significantly increase the bioavailability of mirtazaline, which may require a reduction in the dose of mirtazaline with the onset of concomitant cimetidine treatment or an increase in cimetidine discontinuation.

Simultaneous reception with other serotonergic drugs (including selective serotonin reuptake inhibitors, venlafaxine) - the risk of developing serotonin syndrome. If you need this combination, you should carefully change the dose of drugs and carefully monitor the signs of the onset of serotonergic hyperstimulation.

Mirtazapine at a dose of 30 mg 1 time per day caused a small but statistically significant increase in the International Normalized Ratio (MNO) with simultaneous use with warfarin.It is not possible to exclude a more pronounced effect with a higher dose of mirtazaline. It is recommended to monitor INR in case of treatment with warfarin in combination with mirtazapine.

Special instructions:

In patients with schizophrenia, psychotic symptoms may increase.

In the treatment of the depressive phase of bipolar affective psychosis, an affect inversion with the development of mania can be observed.

Given the possibility of suicidal tendencies, the patient should be given only a small number of tablets.

Women of reproductive age should be treated only if reliable contraception is used.

Abrupt cancellation after prolonged use is undesirable. A sharp cessation of treatment after prolonged use can cause the development of the "withdrawal" syndrome. Most of the symptoms of the "cancellation" syndrome are weak and pass on their own. The most frequently reported dizziness, agitation, anxiety, headache and nausea, although these symptoms may be related to the underlying disease. It is recommended to stop treatment with mirtazapine gradually.

When jaundice, symptoms of infectious diseases or a change in the blood picture, mirtazaline should be discontinued.

Elderly patients are usually more sensitive to the development of side effects.

During the treatment should refrain from taking ethanol.

Oppression of bone marrow functions, usually manifested in the form of granulocytopenia or agranulocytosis, is rarely observed with the use of the drug, usually after 4-6 weeks of treatment and, as a rule, is reversible after discontinuation of treatment. It is necessary to inform the patient about the need to consult a doctor if symptoms such as fever, sore throat, stomatitis, other symptoms of influenza-like syndrome occur; when such symptoms appear, the treatment is stopped and a general blood test is performed.

Effect on the ability to drive transp. cf. and fur:During treatment with Mirtalan, care must be taken when driving vehicles and engaging in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated, 30 mg.

Packaging:

For 10 tablets in blisters of PVC / PVDC film and aluminum foil.

For 1, 2 or 3 blisters in a cardboard box together with instructions for use

Storage conditions:

In a dry, sheltered place, at a temperature of no higher than 25 ° C,

Keep out of the reach of children.

Shelf life:

3 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:LSR-001052/10

Date of registration:16.02.2010 / 12.11.2013

Expiration Date:Unlimited

The owner of the registration certificate:VALEANT, LLC VALEANT, LLC Russia

Manufacturer: & nbsp

G.L.PHARMA, GmbH Austria

Representation: & nbspVALEANT LLC VALEANT LLC Russia

Information update date: & nbsp09.06.2018

Illustrated instructions

Instructions

Myrtlean (Mirtalan)