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Description of the active ingredient Trazodone / Trazodone.
Formula: C19H22ClN5O, chemical name: 2- [3- [4- (3-Chlorophenyl) -1-piperazinyl] propyl] -1,2,4-triazolo [4,3-a] pyridin-3 (2H) -one (in hydrochloride).Pharmacological group: neurotropic drugs / antidepressants.Pharmachologic effect: antidepressant.
The mechanism of action of trazodone is not fully understood. Trazodone is characterized by pronounced affinity for a portion of serotonin receptor subtypes. Trazodone selectively inhibits serotonin reuptake by the brain synapses, potentiates the effects of 5-hydroxytryptophan (a precursor of serotonin), decreases the sensitivity of beta-adrenergic receptors, and slightly affects neuronal uptake of dopamine and noradrenaline and alpha-adrenergic receptors, MAO does not inhibit. Trazodone has almost no cholinolytic action, but can suppress or reduce salivation (especially in elderly and middle-aged patients). The antidepressant effect of trazodone is combined with anxiolytic and sedative effects. Trazodone relieves anxiety, both mental (fear, affective tension, insomnia), and somatic (headache, palpitations, myalgia, sweating, and frequent urination). Trazodone increases the duration and depth of sleep in patients in a state of depression, restores the physiological structure of sleep. Trazodone reduces the pathological craving for alcohol. In abstinence syndrome in patients with benzodiazepine dependence, trazodone eliminates sleep disorders and anxiety-depressive state (benzodiazepines can be completely replaced by trazodone during remission). Trazodone helps restore potency and libido. Trazodone can be used for concomitant cognitive impairment, prostatic hypertrophy, glaucoma, as well as in elderly patients, but the latter are more likely to have hypotensive and sedative effects. Trazodone does not cause addiction. The therapeutic effects in some patients (according to clinical trials) were noted by the end of the first week of therapy, in 75% of patients at the end of the second week, in 25% in 2–4 weeks.
Trazodone is well absorbed in the gastrointestinal tract. After 1 hour, the maximum plasma concentration is reached. Taking the drug during or immediately after a meal increases its absorption, however, reduces the maximum concentration, extending the time to reach it to 2 hours. Trazodone binds to plasma proteins at 89 – 95%. Trazodone passes through tissue barriers (including the blood-brain barrier). Trazodone is metabolized in the liver to form the active metabolite, m-chlorophenylpiperazine. The half-life of trazodone has two phases: the duration of the early phase is 3–6 hours, the late – 5–9 hours; in some patients, trazodone may accumulate. The drug is removed within 98 hours after its admission with urine (75%, including 70% as inactive metabolites) and with bile (20%). There is information about the effectiveness of trazodone in kleptomania, bulimia, panic attacks, phobias (including agoraphobia), acute withdrawal syndrome in alcoholism, pain syndrome in diabetic neuropathy and other types of chronic pain and for the prevention of migraine.
Depressive states of various origins (psychotic, endogenous, somatogenic, neurotic, etc.) with marked tension, anxiety; agoraphobia, pain syndrome with neuralgia, benzodiazepine drug dependence, alcohol withdrawal condition, impotence, decreased libido.
Trazodone and dosage
Trazodone is taken by mouth. Adults: the initial dose is 50 – 100 mg once a day at bedtime, the dose is increased, if necessary, by 50 mg every 3 – 4 days until a therapeutic effect is achieved. The maximum daily dose on an outpatient basis is 450 mg, in inpatient it is 600 mg. For debilitated and elderly patients, the initial dose is up to 100 mg per day; it can be increased, if necessary, to 300 mg per day. Children 6 – 18 years: 1.5 – 2 mg / kg per day, the dose is increased, if necessary, to 6 mg / kg per day.
Violations of libido: 50 mg per day. Impotence: 200 mg per day with monotherapy, 50 mg per day as part of a comprehensive treatment. Benzodiazepine dependence: gradually reducing the dose of benzodiazepines by 0.25 or 0.5 tablets, together add 50 mg of trazodone for 3 weeks, then continue to reduce the dose of benzodiazepines until completely discontinued, then reduce the dose of trazodone by 50 mg per day every 3 weeks. With trazodone therapy, it is necessary to regularly conduct a complete blood count (for the timely detection of blood changes), ECG monitoring in patients with circulatory system diseases is desirable. Careful monitoring of patients with suicidal tendencies is necessary, especially in the first weeks of therapy. With the development of severe neutro – and leukopenia, priapism, treatment is immediately canceled; in other cases, the elimination of trazodone should be done gradually. When trezodone therapy should avoid alcohol. Use caution to use trazodone for vehicle drivers at work and for people whose activity is associated with increased concentration.
Hypersensitivity, ventricular arrhythmia, myocardial infarction (early recovery period), tachycardia, extrasystole, renal or / and liver failure, age up to 6 years.
Restrictions on the use of
Priapism in history, arterial hypertension (may require adjustment of doses of antihypertensive drugs), age up to 18 years. Etc
pregnancy and breastfeeding naming
Do not use trazodone in women during pregnancy. In animal studies, it has been established that trazodone in doses that are 30 to 50 times higher than the MRDCh increases the frequency of fetal resorption and causes congenital malformations. At the time of treatment with trazodone, you must stop breastfeeding. Trazodone with its metabolites is found in the milk of lactating rats. It is not known whether trazodone is excreted in breast milk of women.
Side effects of trazodone
Sense organs and nervous system: fatigue, headache, weakness, dizziness, drowsiness, insomnia, agitation, hypomania, psychosis, hallucinations, muscle twitching, tremor, aphasia, large convulsive seizures (grand mal), akathisia, ataxia, dyskinesia, confusion , paresthesias, syncopal states, diplopia, blurred vision, blood and circulatory system: arterial hypotension (including orthostatic), arrhythmias (including ectopic ventricular rhythms, tachi and bradycardia), atrial fibrillation, congestive dechnaya failure, leukopenia or leukocytosis, neutropenia (usually minor), methemoglobinemia, hemolytic anemia, digestive system: increased appetite, unpleasant taste and dry mouth, dental caries, hypersalivation, disease periodontal tissues, nausea, oral candidiasis, vomiting, diarrhea, flatulence , constipation, increased levels of amylase and bilirubin in the blood plasma, cholestasis, jaundice; urogenital system: urinary retention, hematuria, increased urination, premature menstruation, increased libido, hirsutism, priapism m, retrograde ejaculation, impotence, allergic reactions: urticaria, skin rash; others: chest pain, myalgia, alopecia, edema, psoriasis.
Trazodone interaction with other substances
Trazodone, unlike typical antidepressants, does not reduce depriming effects of reserpine, weakens the peripheral effect of norepinephrine and the central effect of amphetamine. Trazodone enhances the effects of drugs that inhibit the central nervous system (including tricyclic antidepressants, barbiturates, clonidine, antihistamines, alcohol), as well as muscle relaxants and anticholinergics. With the combined use of trazodone with antihypertensive drugs increases the possibility of the development of orthostatic hypotension. Trazodone weakens the effects of psychostimulants. Trazodone increases the content of phenytoin and digoxin in the blood plasma. Do not use trazodone with MAO inhibitors. When sharing ritonavir and trazodone, you may need to reduce the dose of the latter. Patients who take together trazodone and carbamazepine should be under close medical supervision. When trazodone is combined with potent CYP3A4 inhibitors, its dose must be reduced.
With an overdose of trazodone, nausea, drowsiness, vomiting, dizziness, incoordination, lowering blood pressure, priapism, epileptiform seizures, respiratory arrest, ECG changes, and weighting of adverse reactions develop. Necessary: gastric lavage, reception of activated carbon, forced diuresis, maintenance of vital functions, symptomatic treatment; specific antidote is absent.