Agomelatine

Agomelatine (agomelatine) - an antidepressant, is used for the effective treatment of adults with major depressive disorder.  Agomelatine in the package

Pharmacological action

Agomelatine (analogue agomelatine) antagonizes the melatonin MT 1 - And MT 2 receptor and serotonin 5-HT 2c receptors.

As a result, research has proven activity of agomelatine in the treatment of:

  • Meets the requirements model of depression, such as learned helplessness, despair, chronic stress moderate severity;
  • Simulate the depression caused by a violation of the cyclical fluctuations of intensity of biological processes associated with the change of day and night (circadian rhythms);
  • In situations experimentally provoked anxiety and stress.

It is proved that agomelatine has no effect on monoamine uptake and no effect on the work of α-, β-adrenergic, histamine receptors, cholinergic receptors, dopaminergic and benzodiazepine receptors.

Agomelatine enhances the release of norepinephrine and dopamine, particularly in the prefrontal cortex and has no influence on the concentration of serotonin is the cells.

The results showed that by stimulating melatonin receptors agomelatine promotes the release of melatonin. It restores the circadian rhythms, normalizes sleep pattern and reduces the temperature of the body, slowing down the physiological processes.

Even a short-term intake of agomelatine (6-8 weeks) 25-50 mg per day is effective in major depressive episodes are more severe forms of depression, while initially high level of anxiety and the combination of depressive and anxiety disorders. The study confirms the long-term, supportive and antidepressant agomelatine protivoretsedivnoe influence.

The daily intake of 25 mg of agomelatine in depressed patients has no effect on memory and attention. It contributes to the rapid fall asleep and improve sleep quality (long duration of the phase of sleep increases, the amount and duration of REM does not change). At night, reduced heart rate, and the day is not observed inhibition. Emerging trends reduce sexual dysfunction, there is a positive effect on sexual arousal and orgasm.

In the daytime, heart rate, pulse and blood pressure of patients receiving agomelatine does not change, body weight stable.

Withdrawal does not occur even if the discontinuation of sharp tools, agomelatine does not cause addiction syndrome.

Product form

The tablets are oblong, film-coated yellow-orange color, on one side of the logo of the manufacturer. Active ingredient - agomelatine: 25 mg 1 tablet.

Agomelatine analogues

Analogues of agomelatine - existing active substance agomelatine (Agomelatine *) - in today's pharmaceutical market does not exist.

Indications agomelatine

According to the instructions, agomelatine is used for the treatment of major depressive disorder in adults.

Contraindications

Agomelatine, according to instructions, is contraindicated in:

  • Children up to 18 years;
  • In severe hepatic insufficiency - various liver disease in the active phase;
  • If lactose intolerance - galactosemia, lactase deficiency, malabsorption syndrome glucose / galactose;
  • If you are sensitive to agomelatine and other auxiliary substances;
  • Simultaneous treatment with strong inhibitors of the CYP1A2 - ciprofloxacin, fluvoxamine;
  • Women during breastfeeding.

Agomelatine, according to the instructions, should be used with caution and mandatory supervision by a doctor in the following cases:

  • Elderly patients over 65 years old;
  • Patients with severe or moderate renal impairment at a major depressive episode;
  • When concomitantly with moderate inhibitors of the CYP1A2 - grepafloksatsin, propranolol, enoxacin;
  • In patients with manic or hypomanic episodes;
  • Patients with suicidal tendencies or suicide attempts before you start taking the drug;
  • When pregnancy;
  • Patients who abuse alcohol or consume drugs, provoking functional impairment of the liver.

Dosing agomelatine

Agomelatine, according to instructions, taken orally, swallowing the tablet whole (without chewing). From eating pills independent.

The daily dose of agomelatine recommended for receiving - one tablet (25 mg) before bedtime. If improvement is not observed within two weeks, the dose may be increased to two tablets (50 mg) overnight.

Monitoring of liver function is recommended during the first days of admission and periodically during the course of treatment - 3, 6, 12 and 24 weeks. The treatment of depression agomelatine at least 6 months, or until full recovery.

The gradual  Agomelatine tablets
 reducing the dose is not necessary, since the drug does not cause addiction.

Drug interaction agomelatine

Strong inhibitors of CYP1A2 isoenzyme significantly slow down the metabolism of agomelatine on the order of increasing its concentration in the body. Therefore, administration of drugs ciprofloxacin, fluvoxamine and their analogues with agomelatine simultaneously prohibited.

Moderate inhibitors isoenzyme CYP1A2 - estrogens increase the concentration of the agomelatine several times. Appoint propranol, enoxacin, grepafloksatsin and their analogues with agomelatine with caution.

Do not combine the receiving agomelatine with ethanol.

According to studies and reviews, agomelatine:

  • No effect on the concentration of drug in the body, which is associated with metabolism by cytochrome P450 isozymes;
  • No effect on the concentration of free drug binds to plasma proteins, and they do not affect the concentrations of agomelatine;
  • No pharmacodynamic and pharmacokinetic interaction agomelatine with drugs used in psychiatry - benzodiazepines, lithium, paroxetine, fluconazole and teofelin.

Data on the use of electroconvulsive therapy in conjunction with agomelatine to patients there. Animal studies indicate no adverse effects of the combined treatment.

Side effects of agomelatine

Acceptance of agomelatine, according to reviews, is moderate to minor side effects such as dizziness and nausea. They observed the first 2 weeks of treatment, then pass.

Also receiving agomelatine, reviews, can affect:

  • Integument - sweating, itching, eczema, rash;
  • View - defocus, blurred, blurred;
  • Musculoskeletal system - back pain;
  • It is - frequent fatigue.

In some cases, receiving agomelatine, reviews, causing side effects that are difficult to distinguish from the symptoms of a depressive disorder.

storage conditions

Special storage conditions of the drug is not required. Keep out of reach of children must be in place. Shelf life - three years from the date of manufacture. After the expiration date printed on the package does not apply.





Яндекс.Метрика