Mirtazapine Canon

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Mirtazapine Canon: instructions for use and reviews

1. Release form and composition
2. Pharmacological properties
3. Indications for use
4. Contraindications
5. Method of application and dosage
6. Side effects
7. Overdose
8. Special instructions
9. Application during pregnancy and lactation
10. Use in childhood
11. In case of impaired renal function
12. For violations of liver function
13. Use in the elderly
14. Drug interactions
15. Analogs
16. Terms and conditions of storage
17. Terms of dispensing from pharmacies
18. Reviews
19. Price in pharmacies

Latin name: Mirtazapine Canon

ATX code: N06AX11

Active ingredient: mirtazapine (Mirtazapine)

Producer: Kanonpharma production, CJSC (Russia)

Description and photo update: 2019-08-07

Prices in pharmacies: from 565 rubles.

Buy

Mirtazapine Canon is a drug used for depressive conditions.

Release form and composition

Dosage form - film-coated tablets: biconvex round, purple, the core in the cross section is almost white (dosage 15 and 30 mg: in a cardboard box of 1-3 or 6 blisters of 10 tablets or 1 or 2 contour cell packs of 30 tablets, dosage 45 mg: 1–3 or 6 blister packs of 10 tablets or 2 or 4 blister packs of 15 tablets each. Each pack also contains instructions for the use of Mirtazapine Canon).

Composition of 1 tablet:

active substance: mirtazapine - 15, 30 or 45 mg (mirtazapine hemihydrate 15.5; 31 or 46.5 mg, respectively);
auxiliary components (15/30/45 mg): corn starch - 40/80/120 mg; croscarmellose sodium - 6.5 / 13 / 19.5 mg; mannitol - 33/66/99 mg; magnesium stearate - 1/2/3 mg; povidone - 7/14/21 mg; microcrystalline cellulose - 37.5 / 75 / 112.5 mg;
film coating (15/30/45 mg): Opadry II violet (polyvinyl alcohol - 1.6 / 3.2 / 4.8 mg; macrogol - 0.808 / 1.616 / 2.424 mg; talc - 0.592 / 1.184 / 1.76 mg; dioxide titanium - 0.6 / 1.2 / 1.8 mg; indigo carmine dye - 0.24 / 0.48 / 0.72 mg; crimson dye Ponso 4R - 0.16 / 0.32 / 0.48 mg) - 4/8/12 mg.

Pharmacological properties

Pharmacodynamics

Mirtazapine - the active substance of Mirtazapine Canon, belongs to the number of tetracyclic antidepressants, which have a predominantly sedative effect. It is most effective in the treatment of depressive conditions, which are accompanied by an inability to experience joy and pleasure, psychomotor retardation, anhedonia (loss of interest), sleep disturbances (especially in the form of early awakenings), weight loss, as well as some other symptoms, including daily mood swings and suicidal thoughts.

Most often, the antidepressant effect of mirtazapine develops after 1–2 weeks of therapy.

Mirtazapine is an antagonist of presynaptic α ₂ -adrenergic receptors of the central nervous system, it enhances the central serotonergic and noradrenergic transmission of nerve impulses. In this case, the implementation of the enhancement of serotonergic transmission is carried out only through 5-HT ₁ receptors, since mirtazapine blocks 5-HT ₂ and 5-HT ₃ receptors. It is generally accepted that both enantiomers of a substance have antidepressant activity: S (+) - enantiomer blocks α ₂ - and 5-HT ₂ -receptors, R (-) - enantiomer - 5-HT ₃ -receptors.

The sedative effect of mirtazapine is due to its antagonistic activity against H ₁ -histamine receptors.

The therapy is usually well tolerated. Mirtazapine practically does not possess m-anticholinergic activity; when used in therapeutic doses, its effect on the cardiovascular system is limited.

Pharmacokinetics

Absorption of mirtazapine after oral administration is rapid. Bioavailability is approximately 50%. The time to reach C _max (maximum concentration of the substance) in blood plasma is about 2 hours.

Binds to plasma proteins about 85% of the dose. A stable concentration of mirtazapine is achieved within 3-4 days, and then it does not change. Pharmacokinetic parameters of a substance in the recommended dose range are linear in relation to the administered dose.

Mirtazapine is actively metabolized. The main metabolic pathways in the body: oxidation and demethylation followed by conjugation. Cytochrome P450-dependent isoenzymes CYP2D6 and CYP1A2 are involved in the formation of 8-hydroxymetabolite mirtazapine, while it is assumed that the formation of N-demethylated and N-oxidized metabolites is determined by the isoenzyme CYP3A4. Demethylmirtazapine exhibits pharmacological activity and is most likely pharmacokinetically similar to mirtazapine.

Mirtazapine is excreted through the intestines and kidneys for several days. T _1/2 (half-life) averages 20-40 hours (in rare cases - up to 65 hours). Young people have a shorter half-life.

In patients with renal or hepatic insufficiency, the clearance of mirtazapine decreases.

Indications for use

Mirtazapine Canon is prescribed for depressive conditions, including anhedonia, psychomotor retardation, insomnia, early awakening, weight loss, loss of interest in life, mood lability and suicidal thoughts.

Contraindications

Absolute:

combination therapy with monoamine oxidase inhibitors;
lactation period;
age up to 18 years;
individual intolerance to the components of the drug.

Relative (Mirtazapine Canon is prescribed under regular medical supervision):

hepatic or renal impairment;
epilepsy and organic lesions of the brain (in rare cases, convulsive states may develop while taking Mirtazapine Canon);
heart disease, including conduction disturbances, angina pectoris, or recent myocardial infarction;
arterial hypotension and conditions predisposing to its development (including dehydration and hypovolemia);
cerebrovascular diseases, including a burdened history of ischemic attacks;
drug abuse, drug dependence, mania, hypomania;
acute angle-closure glaucoma and increased intraocular pressure;
violations of urination, including against the background of prostatic hyperplasia;
hyponatremia;
diabetes;
pregnancy.

Mirtazapine Canon, instructions for use: method and dosage

Mirtazapine Canon is taken orally whole, without chewing, and washed down with a small amount of water. Food intake does not affect the pharmacokinetic parameters of the drug.

Since T1 _{/ 2 of} mirtazapine is long (20 to 40 hours), it can be used once a day, preferably before bedtime. If necessary, the daily dose can be divided into two doses (in the morning and in the evening).

The recommended duration of therapy is 4–6 months. After the symptoms have completely disappeared, the drug may be gradually withdrawn.

The onset of action of Mirtazapine Canon is on average 1–2 weeks. A positive response with an adequate dose is usually observed after 2-4 weeks of treatment.

At the beginning of therapy, the daily dose for adults, including elderly patients, is 15 or 30 mg. If the response is insufficient, the dose may be increased to the maximum (45 mg). If in this case there is no improvement in 2–4 weeks, the drug is discontinued.

In elderly patients, it is recommended to increase the dose under the direct supervision of a physician to achieve a safe and satisfactory response.

When determining the dose of Mirtazapine Canon for patients with renal / hepatic insufficiency, it should be borne in mind that the clearance of the substance may be reduced.

Side effects

With depression, there are a number of symptoms that are caused by the disease itself, so it is sometimes difficult to distinguish them from the side effects of Mirtazapine Canon.

Possible adverse reactions (> 10% - very common;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rare; with an unknown frequency - based on available data there is no way to establish the frequency of occurrence of adverse reactions):

endocrine system: with an unknown frequency - violation of the synthesis of antidiuretic hormone;
blood and lymphatic system: with an unknown frequency - eosinophilia, oppression of hematopoiesis (in the form of granulocytopenia, agranulocytosis, aplastic anemia and thrombocytopenia);
digestive system: very often - xerostomia; often - vomiting, nausea, diarrhea; infrequently - hypoesthesia of the oral mucosa; with an unknown frequency - increased salivation, edema of the oral mucosa;
psyche: often - confusion, unusual dreams, insomnia *, anxiety *; infrequently - hallucinations, nightmares, agitation, mania, psychomotor agitation (including akathisia, hyperkinesia); rarely - aggressiveness; with an unknown frequency - suicidal behavior, suicidal thoughts;
metabolism and nutrition: very often - weight gain, increased appetite; with an unknown frequency - hyponatremia;
nervous system: very often - drowsiness (can cause impaired concentration of attention; in most cases it is observed in the first weeks of treatment; with a decrease in dose, a decrease in the sedative effect usually does not occur, and a decrease in the effectiveness of therapy is observed), headache, sedation; often - dizziness, lethargy, tremor; infrequently - restless legs syndrome, paresthesia, fainting; rarely, myoclonus; with an unspecified frequency - articulation disorder, convulsions, paresthesia of the oral mucosa, serotonin syndrome;
skin and subcutaneous tissue: often - skin rash; with an unknown frequency - toxic epidermal necrolysis, Stevens-Johnson syndrome, erythema multiforme, bullous dermatitis;
musculoskeletal and connective tissue: often - arthralgia, back pain, myalgia;
liver and biliary tract: rarely - increased activity of liver enzymes;
vessels: often - orthostatic hypotension; infrequently - a decrease in blood pressure;
general disorders: often - local edema; infrequently - fatigue; with an unspecified frequency - local or generalized edema;
others: urticaria, withdrawal syndrome, thirst.

* When using antidepressants, symptoms such as insomnia and anxiety (refer to signs of depression) may occur or worsen. While taking Mirtazapine Canon, the development or worsening of anxiety was reported in rare cases.

When evaluating the information that was obtained in the course of clinical studies, there was a short increase in the level of transaminases and gamma-glutamyl transpeptidase. However, the development of any adverse reactions associated with taking mirtazapine, which were observed with a greater frequency than with placebo, were not reported.

Overdose

Based on toxicity studies, it can be argued that with an overdose of Mirtazapine Canon, there is no clinically significant cardiotoxic effect.

The main symptoms: depression of the central nervous system in combination with disorientation and prolonged sedation, tachycardia, hallucinations, change (decrease or increase) in blood pressure of moderate severity. There is a risk of developing more severe violations of the physiological functions of the body, which, when used in doses that are much higher than the therapeutic one, can cause a fatal outcome (especially against the background of mixed overdoses).

Therapy: symptomatic, measures should be aimed at maintaining the vital functions of the body. Gastric lavage and intake of activated charcoal are recommended.

special instructions

In patients under 24 years of age with depression and other mental disorders, the use of antidepressants increases the risk of suicidal behavior and suicidal thoughts when compared with placebo. In this regard, before prescribing Mirtazapine Canon, it is necessary to correlate the possible risk of suicide and the benefits of therapy. When conducting short-term studies, it was found that in patients over 24 years of age, the risk of suicide does not increase, and in patients over 65 years of age, it slightly decreases.

By itself, any depressive disorder is characterized by an increased risk of suicide, therefore, the patient should be monitored while taking Mirtazapine Canon to timely detect changes or violations of behavior, as well as suicidal tendencies. Given the possibility of suicide, especially at the beginning of therapy, the patient should be given the lowest dose, which reduces the likelihood of overdose.

Depression of bone marrow functions, which usually manifests itself as granulocytopenia or agranulocytosis, while taking Mirtazapine Canon occurs in rare cases, usually after 4-6 weeks of therapy. After the end of taking the drug, the symptoms of the disease disappear. The doctor and patient should be alert to signs of bone marrow suppression such as sore throat, fever, stomatitis, and other symptoms of flu-like syndrome. If they appear, you must stop taking the drug and do a blood test.

In case of signs of jaundice, therapy should be interrupted.

Careful and regular medical supervision when using Mirtazapine Canon is required in the following cases:

lowering blood pressure;
heart disease, including conduction disturbances, angina pectoris and recent myocardial infarction: these patients require the usual precautions when prescribing the drug;
epilepsy and organic lesions of the brain: despite the information that epileptic seizures during treatment with antidepressants, including mirtazapine, rarely occur, patients with a history of epileptic seizures should be prescribed Mirtazapine Canon with caution;
renal failure: in moderate and severe renal failure (in patients with creatinine clearance of 10-40 and <10 ml / min, respectively), the clearance of mirtazapine after taking the drug at a dose of 15 mg decreases by about 30 and 50%, and the average plasma concentration of mirtazapine in the blood increases by 55 and 115%, respectively, in comparison with healthy patients. In mild renal failure (in patients with creatinine clearance in the range of 40–80 ml / min), there were no significant differences compared with the control group;
hepatic impairment: in mild to moderate hepatic impairment, oral administration of 15 mg of mirtazapine decreases the clearance of the substance by about 35% in comparison with patients without liver dysfunction. The average plasma concentration of mirtazapine in the blood increases by about 55%;
diabetes mellitus: taking antidepressants in this group of patients can affect the blood glucose level, and therefore it may be necessary to adjust the dose of insulin and / or oral hypoglycemic drugs. In the case of the appointment of Mirtazapine Canon, careful monitoring of the patient's condition is required.

As during therapy with other antidepressants, the following conditions may develop with the use of mirtazapine:

transformation of the depressive phase of bipolar disorder into a manic one;
worsening of existing psychotic symptoms in patients with schizophrenia or other mental disorders; the appearance of paranoid ideas is possible;
the development of withdrawal symptoms. Antidepressants do not cause addiction, however, based on post-registration experience, it can be concluded that with a sharp cancellation of therapy after a long course, withdrawal symptoms may appear. In most cases, they are weak and self-limiting. The most commonly reported symptoms were dizziness, nausea, headache, malaise, agitation, anxiety. It must be borne in mind that these conditions can also be associated with an underlying disease. Cancellation of Mirtazapine Canon should be gradual.

Antidepressant therapy is associated with the occurrence of akathisia. It is characterized by subjectively unpleasant or anxious excitement in combination with increased motor activity. The appearance of such symptoms is most likely during the first few weeks of using Mirtazapine Canon. An increase in the dose may have a negative impact on the patient's health in such cases.

Serotonin syndrome can develop against the background of combined therapy of selective serotonin reuptake inhibitors with other serotonergic drugs. The main symptoms include: myoclonus, rigidity, fever, changes in mental state (including confusion, severe agitation, irritability, progressive disorder of consciousness, coma), disorder of the autonomic nervous system, possibly in combination with rapid fluctuations in vital indicators of the functional the state of the body. When prescribing this combination of drugs, caution should be exercised, therapy should be carried out under close clinical monitoring of the condition. With the development of these disorders, Mirtazapine Canon is canceled and symptomatic therapy is prescribed. Based on post-registration experience, it was establishedthat serotonin syndrome occurs very rarely in patients receiving mirtazapine monotherapy.

There are rare reports of the development of hyponatremia during therapy. Patients at risk (elderly patients or patients taking drugs that can lead to the development of hyponatremia), Mirtazapine Canon is prescribed with caution.

Patients with urination disorders (including against the background of prostatic hypertrophy), as well as patients with acute angle-closure glaucoma and increased intraocular pressure, Mirtazapine Canon is prescribed with caution, despite the fact that the anticholinergic activity of mirtazapine is very weak and the negative effect of the drug unlikely.

Elderly patients are usually more sensitive to the action of the drug, especially in relation to the development of adverse reactions. During clinical trials, it was not noted that in elderly patients, side effects occur more often than in other age groups, but they can be more pronounced (information is limited).

When prescribing Mirtazapine Canon simultaneously with benzodiazepines, care must be taken.

During the period of therapy, it is recommended to refrain from drinking alcohol.

Influence on the ability to drive vehicles and complex mechanisms

During the period of therapy with Mirtazapine Canon, driving should be abandoned.

Application during pregnancy and lactation

The safety of therapy with Mirtazapine Canon during pregnancy has not been established, therefore, the drug can be prescribed only in cases where the expected benefit is higher than the possible harm. Treatment should be carried out under medical supervision. When using the drug, especially in the later stages of pregnancy, the likelihood of persistent pulmonary hypertension in newborns may increase.

There is no information confirming or refuting the fact that mirtazapine is excreted in breast milk, therefore, taking Mirtazapine Canon for breastfeeding women is not recommended.

Pediatric use

The drug is not prescribed to patients under 18 years of age, since the experience of using Mirtazapine Canon in this age group of patients is limited.

With impaired renal function

For patients with renal failure, Mirtazapine Canon is prescribed with caution.

For violations of liver function

For patients with hepatic impairment, Mirtazapine Canon is prescribed with caution.

Use in the elderly

In elderly patients, in order to achieve a safe and satisfactory response, it is recommended to increase the dose of Mirtazapine Canon under the direct supervision of a physician.

Drug interactions

Pharmacokinetic interaction

When using mirtazapine, an intensive metabolism occurs with the participation of isoenzymes CYP2D6 and CYP3A4, the isoenzyme CYP1A2 is involved in the process to a lesser extent. When studying the interaction of mirtazapine and paroxetine in healthy volunteers, it was shown that paroxetine (an inhibitor of the isoenzyme CYP2D6) has no effect on the pharmacokinetics of mirtazapine at steady state.

Against the background of combination therapy with ketoconazole (a potent inhibitor of the isoenzyme CYP3A4), there is an increase in the maximum plasma concentration and the AUC (area under the concentration-time curve) of mirtazapine by about 40 and 50%, respectively. When prescribing Mirtazapine Canon with potent inhibitors of the isoenzyme CYP3A4 (inhibitors of HIV protease, azole antifungal drugs, erythromycin, nefazodone), care must be taken.

Inducers of the isoenzyme CYP3A4 (carbamazepine, phenytoin) lead to an approximately two-fold increase in the clearance of mirtazapine, which causes a decrease in its plasma concentration by 45-60%. When adding carbamazepine or another inducer of hepatic metabolism (for example, rifampicin) to therapy, an increase in the dose of mirtazapine may be required. After canceling such an inducer, the dose of Mirtazapine Canon can be reduced.

When combined with cimetidine, the bioavailability of mirtazapine can significantly increase, which requires a dose adjustment of Mirtazapine Canon.

Pharmacodynamic interaction

monoamine oxidase inhibitors: combined use, as well as the use of Mirtazapine Canon for 14 days after the end of their intake is contraindicated; treatment with these drugs can be started no earlier than 14 days after the end of taking mirtazapine;
benzodiazepines and other sedatives (in particular, most antagonists of H ₁ -histamine receptors, opioids, antipsychotics): their sedative properties can be enhanced;
alcohol: its depressing effect on the central nervous system increases, therefore, during the period of therapy, alcohol should be avoided;
serotonergic drugs (including tryptan, L-tryptophan, linezolid, tramadol, selective serotonin reuptake inhibitors, venlafaxine, lithium preparations, St. John's wort preparations): with combined use, the development of serotonin syndrome is possible;
warfarin (with 30 mg of mirtazapine per day): there is a small but statistically significant increase in the INR (International Normalized Ratio), therefore, a more pronounced effect with therapy with a higher dose of mirtazapine cannot be excluded; with combined therapy, it is recommended to monitor the INR value.

Analogs

Analogues of Mirtazapine Canon are: Mirzaten Ku-tab, Caliksta, Mirtalan, Remeron, Noxibel, Mirtazonal, Esprital.

Terms and conditions of storage

Store in a place protected from light and moisture at temperatures up to 25 ° C.

Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Mirtazapine Canon

Reviews of Mirtazapine Canon are different. It is considered by many to be an effective treatment for depression. It is noted that the drug improves mood and sleep, relieves anxiety, panic and depressive states. In other cases, they indicate the development of pronounced side effects, manifested mainly in the form of drowsiness and weight gain. The cost is assessed as high.

The price of Mirtazapine Canon in pharmacies

The approximate price for Mirtazapine Canon for a pack of 30 tablets is: dosage of 30 mg - 699-828 rubles; dosage 45 mg - 770-937 rubles.

Mirtazapine Canon: prices in online pharmacies

Drug name

Price

Pharmacy

Mirtazapine Canon 30 mg film-coated tablets 30 pcs.

RUB 565

Buy

Mirtazapine Canon 45 mg film-coated tablets 30 pcs.

575 RUB

Buy

Mirtazapine Canon tablets p.o. 45mg 30 Pcs.

598 r

Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!