An antidepressant derivative of thiazolopyridine. It also has timoleptic, anxiolytic, sedative and muscle relaxant effects. It has a high affinity for certain subtypes of serotonin receptors, inhibits the reuptake of serotonin; neuronal uptake of norepinephrine and dopamine is little affected.
It does not have an anticholinergic effect, does not inhibit MAO, does not change body weight. Eliminates both mental (affective tension, irritability, fear, insomnia), and somatic manifestations of anxiety (palpitations, headache, myalgia, rapid urination, increased sweating). Increases the depth and duration of sleep in patients in a state of depression, restores its physiological structure.
Reduces pathological craving for ethanol. Effective in withdrawal symptoms in patients with drug dependence on anxiolytic drugs benzodiazepine derivatives, eliminates anxiety-depressive state and sleep disorders (during remission, benzodiazepines can be completely replaced by trazodone). Not addictive. Helps to restore libido and potency.
The therapeutic effect in 50% of patients is observed after 3-7 days, in 25% - after 2-4 weeks.
fter oral administration, absorption from the gastrointestinal tract is high. The time to reach Cmax in blood plasma is 1-2 hours. The administration of trazodone during or immediately after a meal increases absorption, decreases Cmax, and increases the time to reach it.
Penetrates through histohematological barriers, including the BBB. Penetrates into tissues and fluids (bile, saliva, breast milk). Binding to plasma proteins - 89-95%.
Metabolized in the liver by hydroxylation. Isoenzymes CYP3A4, CYP3A5 and CYP3A7 are involved in the metabolism of the drug.
T1 / 2 in the α phase 3-6 hours, in the β phase 5-9 hours. It is excreted by the kidneys - 75% in the form of inactive metabolites within 98 hours after administration; 20% - with bile.
Ventricular arrhythmia, tachycardia, myocardial infarction (early recovery period), history of priapism, pregnancy, lactation, hypersensitivity to trazodone.
Pregnancy and lactation
Use during pregnancy and lactation is contraindicated.
From the side of the central nervous system and peripheral nervous system: drowsiness, increased fatigue, dizziness, insomnia, headache, agitation, myalgia, impaired coordination of movements, paresthesia, disorientation, dimming of consciousness, tremor.
From the cardiovascular system: arrhythmia, impaired conduction, bradycardia, ventricular fibrillation, decreased blood pressure, orthostatic hypotension, fainting.
From the digestive system: nausea, vomiting, diarrhea, dryness and bitterness in the mouth.
From the side of the organ of vision: visual impairment, eye irritation.
From the hemopoietic system: leukopenia, neutropenia (usually insignificant).
Other: nasal congestion, priapism followed by impotence, allergic reactions.
A case of the development of pirouette type arrhythmia with the simultaneous use of trazodone with amiodarone is described.
A case of a moderately pronounced decrease in the anticoagulant effect of warfarin with simultaneous use with trazodone is described.
With simultaneous use, it is possible to increase the concentration of digoxin in blood plasma and the development of symptoms of intoxication.
With simultaneous use with carbamazepine, a case of increasing the concentration of carbamazepine in blood plasma has been described.
With simultaneous use with lithium salts, tremors, reversible symptoms of a neurotoxic effect are possible.
When taking pseudoephedrine with trazodone therapy, a case of anxiety, panic state, dimming of consciousness, and depersonalization has been described.
With simultaneous use with thioridazine, an increase in the concentration of trazodone in blood plasma is possible; with tryptophan - a case of the development of anorexia, psychosis, hypomania is described; with phenytoin - a case of increased side effects of phenytoin has been described; with fluoxetine - an increase in side effects is possible; with chlorpromazine, trifluoperazin - the development of arterial hypotension is possible.
With simultaneous use with ethanol, the inhibitory effect on the central nervous system is enhanced.
Dosage and administration
The initial daily dose is 150-200 mg (in 3 divided doses). In mild forms of depression, the average maintenance dose is 150 mg / day; with moderate and severe forms - 300 mg / day. If necessary, the dose can be increased to 600 mg / day. The main part of the daily dose is recommended to be taken before bedtime.
Use with caution in diseases of the heart, arterial hypotension, arterial hypertension, renal and / or liver failure, in children and adolescents under the age of 18 years.
Do not use concomitantly with MAO inhibitors.