Trazodone (Trazodonum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Antidepressants

Included in the formulation
  • Trittico
    pills inwards 
    Aziande Kimike Riounite Angelini Francesco AKR.A.A. SpA     Italy
    • АТХ:

    N.06.A.X   Other antidepressants

    N.06.A.X.05   Trazodone

    Pharmacodynamics:

    Inhibition of reverse neuronal capture of serotonin in the central nervous system, a decrease in the sensitivity of β-adrenoreceptors, an increase in the affinity of ligands for certain subtypes of serotonin receptors.

    Pharmacokinetics:

    Absorption is high. The connection with plasma proteins is 89-95%. Biotransformation in the liver by hydroxylation. Half-life 5-9 hours. Maximum concentration 2 hours (with food), 1 hour (without food). Elimination by the kidneys - 75%, with faeces - 20%.

    Indications:
    • Anxious-depressive states of endogenous nature (including involutional depression).
    • Psychogenic depression (including reactive and neurotic depression).
    • Anxiety-depressive states against the background of organic diseases of the central nervous system (dementia, Alzheimer's disease, cerebral artery atherosclerosis).
    • Depressive states with prolonged pain syndrome.
    • Alcoholic depression.
    • Benzodiazepine dependence.
    • Disorders of libido and potency, including in depressed states.
    ICD-10

    V.F10-F19.F13   Mental and behavioral disorders caused by the use of sedatives or hypnotics

    V.F30-F39.F31   Bipolar affective disorder

    V.F30-F39.F32   Depressive episode

    V.F30-F39.F33   Recurrent depressive disorder

    V.F40-F48.F40   Phobic anxiety disorders

    V.F40-F48.F41.2   Mixed anxiety and depressive disorder

    V.F50-F59.F52.0   Absence or loss of sexual desire

    V.F50-F59.F52.2   Insufficiency of the genital reaction

    Contraindications:

    Hypersensitivity; pregnancy, breast-feeding; ventricular arrhythmia, tachycardia, myocardial infarction (early recovery period); priapism in the anamnesis.

    Carefully:

    Heart diseases, arterial hypertension (correction of doses of antihypertensive drugs is necessary because of possible hypotensive action), renal and / or hepatic insufficiency, age to 18 years.

    Pregnancy and lactation:

    The animals show embryotoxic and teratogenic effects in doses 50 times higher than the maximum therapeutic values ​​for humans. Penetrates into breast milk. Do not apply!

    Recommendations for FDA - Category C.

    Dosing and Administration:

    Adults are given an initial dose of 100 mg once a day after meals before bedtime. On the 4th day, you can increase the dose to 150 mg. Further in order to achieve the optimal therapeutic effect, the dose is increased by 50 mg per day every 3-4 days until the optimal dose is reached.The daily dose of more than 150 mg should be divided into 2 doses, with a smaller dose taken after lunch, and the main one - before bedtime.

    For elderly and debilitated patients, the initial dose is up to 100 mg per day in divided doses or once a day before bedtime. The dose may be increased under the supervision of a doctor, depending on the effectiveness and tolerability of the drug. Usually, a dose exceeding 300 mg per day is not required.

    Children aged 6-18 years: the initial daily dose of 1.5-2 mg / kg per day, divided into several receptions. If necessary, the dose is gradually increased to 6 mg / kg per day with an interval of 3-4 days.

    Side effects:

    From the side CNS and peripheral nervous system: increased fatigue, drowsiness, agitation, headache, dizziness, weakness, myalgia, discoordination, paresthesia, disorientation, tremor.

    From the side of cardio-vascular system: reduction of blood pressure, orthostatic hypotension (especially in individuals with vasomotor lability) is due to adrenolitic action of the drug, arrhythmia, conduction disorders, bradycardia, leukopenia and neutropenia (usually minor).

    From the side digestive system: dryness and bitterness in the mouth, nausea, vomiting, diarrhea, decreased appetite.

    Other: allergic reactions, eye irritation, priapism (patients who have this side effect should immediately stop taking the drug and consult a doctor).

    Overdose:

    Symptoms: drowsiness, epileptiform seizures, nausea, vomiting.

    Treatment symptomatic. There is no specific antidote.

    Interaction:

    Alcohol and other drugs that depress the central nervous system - increased oppression of the central nervous system.

    Hypotensive drugs - increased hypotensive effect.

    Special instructions:Compared to placebo, new generation antidepressants do not cause clinically significant improvement in patients with moderate or even severe depression, showing a clinically significant effect only in the most severe depressive patients. The effect in these patients is probably associated with a decrease in the response to placebo, and not with an increase in response to an antidepressant. Researchers conclude that there is no reason to prescribe antidepressants of a new generation to anyone other than the most severe depressive patients, and only after demonstrating the ineffectiveness of alternative treatment options.The fact that severely depressed patients respond less to placebo, than less severe patients, but demonstrate the same response to antidepressants, is very important for understanding the nature of the response of depressed patients to antidepressants and placebo, and this need to be investigated further (a meta-analysis of studies presented in FDA, - 35 RCTs: 5 - fluoxetine, 8 - nefazadone, 16 - paroxetine, uniting 5,133 patients, of whom 3,292 were randomized to receive an antidepressant and 1,841 to a placebo. 4 RCTs, 486 participants (sertraline) and 1 RCT, 274 participants (citalopram), which did not show a statistically significant positive effect of antidepressants, were not included because they did not provide information on the severity of depression on a scale
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