Expiration date: 11/2025

Structure and Composition:

The long-acting tablets. 1 tablet contains 150 mg of trazodone hydrochloride

Excipients: sucrose - 84.0 mg Carnauba wax - Povidone 24.0 mg - 24.0 mg Magnesium stearate - 6.0 mg

in blister PVC / aluminum foil 10 pcs. 2 in a pack or carton of blisters 6.

Description pharmaceutical form:

Biconvex tablets of white or white with a yellowish tint, oval-shaped with two parallel risks on both sides.

Pharmacokinetics:

The absorption of the drug from the gastrointestinal tract after oral administration is high. Trazodone during or immediately after a meal slows the rate of absorption, decreases in plasma Cmax of the drug and increases Tmax. Tmax drug attained within 1 / 2-2 hours after ingestion.

Gistogematicalkie drug penetrates through the barriers and into the tissues and fluids (bile, saliva, breast milk).

Binding to plasma proteins - 89-95%.

Trazodone is metabolised in the liver, an active metabolite - 1st-hlorofenilpiperazin. T1 / 2 in the first phase of 3-6 hours, in a second phase -. 9.5 hours, most of excretion of the drug metabolized via the kidneys, with urine (about 75%) and fully complete after 98 h after drug administration with bile output about 20%.

in vitro studies in human microsomes showed that trazodone is mainly metabolized by cytochrome P450 CYP3A4.

Description of the pharmacological actions:

Trazodone, triazolopyridine derivatives being, preferably has antidepressant action, with some sedative and anxiolytic effects. Trazodone has no effect on MAO, which distinguishes it from MAO inhibitors, tricyclic antidepressants.

Quickly affects the mental (affective tension, irritability, anxiety, insomnia) and somatic anxiety symptoms (palpitations, headache, muscle pain, frequent urination, sweating, hyperventilation).

Trazodone effective in sleep disorders in patients with depression, increases the depth and duration of sleep, restores its physiological structure and quality.

Trazodone stabilize the emotional state, it improves mood, reduces the craving for alcohol in patients with chronic alcoholism in the period of alcohol withdrawal syndrome, in remission. When withdrawal syndrome in patients addicted to benzodiazepines, trazodone is effective in the treatment of anxiety, depression and sleep disorders. In remission benzodiazepines can be completely replaced with trazodone.

The drug is not addictive.

Promotes restoration of libido and potency, as in patients with depression, and in persons not suffering from depression.

The mechanism of action of trazodone is associated with high affinity to certain drug serotonin receptor subtypes, trazodone which comes into interaction agonistic or antagonistic depending on the subtype, as well as the ability to cause a specific inhibition of serotonin reuptake.

On neutral seizure of norepinephrine and dopamine affects little.

The drug has no effect on body weight.

Testimony:

• anxiety and depression endogenous nature (including involutional depression)
  
• psychogenic depression (including reactive and neurotic depression)
  
• anxiety and depression on the background of organic CNS diseases (dementia, Alzheimer's disease, cerebral atherosclerosis)
  
• depression with long-term pain syndrome
  
• alcoholic depression
  
• benzodiazepine dependence
  
• libido and potency disorders (including erectile dysfunction in depressive states).
  

Contraindications:

• Hypersensitivity to the drug
  
• during pregnancy
  
• lactation
  
• Children up to age 6 years.
  

Precautions should be prescribed the drug in patients with AV block, myocardial infarction (early recovery period), hypertension (may require adjustment of doses of antihypertensive drugs), ventricular fibrillation, a history of priapism, renal and / or hepatic insufficiency. Patients under the age of 18 years, due to the possibility of risk of suicidality (suicidal plans, aggressiveness, propensity to contradiction, anger).

Application of pregnancy and breastfeeding:

The drug is not recommended for pregnant women.

The drug is not recommended for use during breastfeeding.

Side effect:

CNS: fatigue, drowsiness, irritability, headache, dizziness, weakness, myalgia, discoordination, paresthesia, disorientation, tremors.

From the CCC and the hematopoietic system: decrease in blood pressure, orthostatic hypotension due adrenoliticheskoe effect (especially in patients with vasomotor lability), arrhythmia, conduction disorders, bradycardia, leukopenia and neutropenia (usually minor) ..

On the part of the digestive tract: dry and bitter taste in the mouth, nausea, vomiting, diarrhea, decreased appetite.

Other: allergic reactions, eye irritation, priapism (should immediately stop taking the drug and seek medical advice).

Drug Interactions:

Trazodone may enhance the effect of certain antihypertensive drugs, and usually requires a reduction in their dose.

Co-administration with drugs depressing the central nervous system (including clonidine, metiodopa), enhances the action of the latter.

Antihistamines and drugs having holinoliticheskoy activity, enhance the anticholinergic effect of trazodone.

Trazodone intensifies and prolongs the sedative and anticholinergic effects of tricyclic antidepressants, haloperidol, loxapine, maprotiline, phenothiazines, and pimozidana thioxanthine.

When concomitant administration of tricyclic antidepressants and trazodone may cause cardiovascular side effects.

MAO inhibitors increase the risk of side effects.

In a joint application increases the concentration of digoxin and phenytoin in blood plasma.

In vitro drug metabolism studies suggest the possibility of pharmacological interactions of trazodone with inhibitors of cytochrome P450 CYP3A4, such as ketoconazole, ritonavir, indinavir, and fluoxetine. Inhibitors of CYP3A4 may lead to a significant increase in the plasma concentration of trazodone, thereby increasing the likelihood of adverse events. Therefore, in case of receiving in combination with potent inhibitors of CYP3A4 trazodone dose should be reduced.

When trazodone in combination with carbamazepine plasma trazodone concentration decreases. Therefore, patients simultaneously receiving trazodone and carbamazepine should be monitored carefully.

Dosage and administration:

Inside, 30 minutes before or 2-4 hours after a meal. Tablets should be taken whole, without chewing and drinking plenty of water.

Initial dose - 50-100 mg, once before bedtime. On the 4th day, may increase the dose to 150 mg. A further increase in dosage should be made at 50 mg / day every 3-4 days, until reaching the optimal dose. The daily dose of 150 mg should be divided into 2 doses, with a smaller dose taken in the afternoon, and the main - before going to bed.

The maximum daily dose for outpatients - 450 mg for inpatients - 600 mg.

Children 6-18 years: The initial daily dose of 1.5-2 mg / kg / day, divided into several stages. If necessary, the dose is gradually (3-4 day intervals) was increased to 6 mg / kg / day.

Elderly or debilitated patients: an initial dose of 100 mg / day in divided doses or a single dose before bedtime. If necessary, the dose may be increased (generally not more than 300 mg / day).

Treatment libido disorders: The recommended daily dose of 50 mg.

Treatment of erectile dysfunction: monotherapy - the recommended daily dose - 150-200 mg, combination therapy - 50 mg.

Treatment for benzodiazepine dependence: The recommended treatment regimen is based on a gradual, sometimes for several months, reduction of the dose of benzodiazepine. Each time reducing the dose benzodiazepine 1/4 or 1/2 Table. Simultaneously added 50 mg of trazodone. This ratio is left unchanged for 3 weeks, then proceed to a further gradual reduction of the dose of benzodiazepines until their complete abolition. Thereafter reduce the daily dose of trazodone of 50 mg every 3 weeks.

Overdose:

Symptoms include nausea, drowsiness, hypotension, increased weighting and side effects.

Treatment: symptomatic therapy (gastric lavage, forced diuresis). There is no specific antidote.

Special instructions:

Since the drug has some adrenoliticheskoy activity, possibly bradycardia development and reduce blood pressure. Therefore, caution should be exercised when administering the drug to patients with impaired cardiac conduction, AV block of various degrees of severity, recent myocardial infarction. When using trazodone may be some reduction in the number of white blood cells, which do not require specific treatment, except severe leukopenia. Therefore it is recommended to carry out studies of peripheral blood, especially in the presence of pain in the throat when swallowing, and fever appears.

The drug does not possess anticholinergic action, so it can be administered to elderly patients suffering from hypertrophy of the prostate, narrow-angle glaucoma, impaired cognitive function.

When prolonged and inadequate erection should consult a doctor.

Relevant studies on the effectiveness of the drug in pediatric patients have not been conducted, and the drug should be used with caution in individuals under 18 years of age. Doses for children under 6 years of age have not been established.

During treatment should refrain from drinking alcohol.

Effects on ability to drive vehicles, machinery. Since the drug has anxiolytic and sedative activity, may reduce attention and reaction speed. During treatment should refrain from activities potentially hazardous activities that require concentration and rapid psychomotor reactions.