Valdoksan

Valdoksan (агомелатин) – antidepressant, is applied to effective treatment at adults of big depressive frustration.

Pharmacological action

Valdoksan (an analog агомелатин) counteracts work melatoninovy _MT1-and _{MT2-receptors} and serotoninovy _{5-Nt2s-retseptorov}.

As a result of scientific research Valdoksan's activity at treatment was proved:

• Conforming to the established requirements of models of depressions, such as the acquired helplessness, despair, chronic stresses of moderate expressiveness;
• The Modelirovanny depressions caused by disturbance of cyclic fluctuations of intensity of the biological processes connected with change of day and nights (circadian rhythms);
• In the situations which are experimentally provoked alarm and a stress.

It is proved that Valdoksan has no influence on capture of monoamines and does not exert impact on work α-, β-adrenoceptors, histamine receptors, holinoretseptor, dopamine and benzodiazepine receptors.

Valdoksan promotes strengthening of release of noradrenaline and dopamine, especially in prefrontal cortex of a brain, and does not exert impact on concentration of serotonin out of cells.

Results of researches showed that by stimulation of melatoninovy receptors Valdoksan promotes release of melatonin. It recovers circadian rhythms, normalizes structure of a dream and reduces body temperature, slowing down physiological processes.

Even short-term reception of Valdoksan (6-8 weeks) of 25-50 mg a day is effective at big depressive episodes, more severe forms of depressions, at initially high level of alarm and at a combination of depressive and alarming frustration. The long-term supporting antidepressive and protivoretsedivny influence of Valdoksan is confirmed by researches.

Daily reception of 25 mg of Valdoksan at patients with a depression does not influence memory and attention. Promotes bystry backfilling, improvement of quality of a dream (duration of a phase of a long dream increases, the quantity and duration of phases of a REM sleep do not change). At night heart rate decreases, and block is not observed in the afternoon. The tendency of reduction of sexual disturbances forms, positive influence on sexual excitement and an orgasm is noted.

In the afternoon the heart rate, pulse and arterial pressure of patients from Valdoksan's reception do not change, body weight is stable.

The withdrawal does not arise even at the sharp termination of reception of means, Valdoksan does not cause an accustoming syndrome.

Release form

Tablets are oblong, are covered with a film cover of yellow-orange color, on one of the parties the logo of manufacturing firm is represented. Active ingredient – агомелатин: 25 mg in 1 tablet.

Analogs

Valdoksan's analogs – the operating active agent агомелатин (Agomelatine *) – in the modern pharmaceutical market do not exist.

Indications to Valdoksan's use

According to the instruction, Valdoksan is applied to treatment of big depressive frustration at adults.

Contraindications

Valdoksan, according to the instruction, is contraindicated:

• To children up to 18 years;
• At a heavy liver failure – various diseases of a liver in an active phase;
• At a lactose intolerance – a galactosemia, a lactose intolerance, a glucose/galactose sprue;
• At hypersensitivity to an agomelatin and other excipients;
• Concomitant use with strong inhibitors of an isoenzyme CYP1A2 – ciprofloxacin, флувоксамин;
• To women during breastfeeding.

Valdoksan, according to the instruction, it is necessary to appoint with care and obligatory observation at the doctor in the following cases:

• To patients of advanced age 65 years are more senior;
• To patients with the expressed or moderate renal failure at big depressive episodes;
• At a concomitant use with moderate inhibitors of an isoenzyme CYP1A2 – грепафлоксацин, propranolol, эноксацин;
• To patients with hypomaniacal or maniacal attacks;
• To patients with suicide bents or attempts of a suicide prior to administration of drug;
• At pregnancy;
• To the patients abusing alcohol or using the drugs provoking functional disturbances of a liver.

Valdoksan route of administration

Valdoksan, according to the instruction, accept inside, swallowing a tablet entirely (without chewing). Reception of tablets does not depend on meal.

The daily dose of Valdoksan recommended for reception – one tablet (25 mg) before going to bed. If improvement is not observed within two weeks, it is possible to increase a dose to two tablets (50 mg) for the night.

Control of function of a liver in the first days of reception and periodically during all course of treatment – in 3, 6, 12 and 24 weeks is recommended. A depression course of treatment Valdoksan at least 6 months or before full treatment.

In a gradual dose decline there is no need as drug does not cause accustoming.

Medicinal interaction of Valdoksan

Strong inhibitors of an isoenzyme CYP1A2 considerably slow down metabolism of an agomelatin, much increasing its concentration in an organism. Therefore administration of drugs ciprofloxacin, флувоксамин and their analogs with Valdoksan is at the same time prohibited.

Moderate inhibitors of an isoenzyme CYP1A2 – estrogen, increase concentration of an agomelatin several times. To appoint пропранол, эноксацин, грепафлоксацин and their analogs with Valdoksan follows with care.

It is not necessary to combine Valdoksan's reception with ethanol.

By results of researches and to responses, Valdoksan:

• Does not influence concentration in an organism of drugs which metabolism is connected with P450 cytochrome isoenzymes;
• Does not influence free concentration of the medicines which are taking up with proteins of plasma, and they do not exert impact on concentration of an agomelatin;
• There is no pharmakodinamichesky and pharmacokinetic interaction of Valdoksan with the drugs which are used in psychiatry – benzodiazepines, lithium drugs, пароксетин, флуконазол and теофелин.

There are no data on use of electroconvulsive therapy along with Valdoksan to patients. Animal experiments show lack of undesirable effects of such joint treatment.

Side effects of Valdoksan

Valdoksan's reception, according to reviews, causes moderately expressed or insignificant side effects, such as dizziness and nausea. They are observed the first 2 weeks of treatment, then pass.

Also Valdoksan's reception, according to reviews, can be reflected on:

• Integuments – perspiration, an itch, eczema, rash;
• Sight – a defocusing, a zatumanennost, a vagueness;
• To musculoskeletal system – a dorsodynia;
• Health – frequent fatigue.

In certain cases Valdoksan's reception, according to reviews, causes side effects which are difficult for distinguishing from symptoms of depressive frustration.

Storage conditions

Drug does not demand special storage conditions. It is necessary to store in places unavailable to children. A period of validity – three years of date of production. Upon termination of the period of validity specified on packaging not to apply.