Desyrel (Trazodone Hydrochloride)

Pharmacological action Trazodone 100 mg

Antidepressant derivative tiazolopiridina. Has also timolepticheskoe, anxiolytic, sedative and muscle relaxant effects. It has a high affinity for certain subtypes of serotonin receptors, inhibits the reuptake of serotonin at the neuronal uptake of norepinephrine and dopamine has little effect.

No anticholinergic action, does not inhibit monoamine oxidase, does not alter body weight. Eliminates a psychic (affective tension, irritability, fear, insomnia), and somatic manifestations of anxiety (palpitations, headache, myalgia, frequent urination, sweating). Increases the depth and duration of sleep in patients with depression, restores its physiological structure.

Reduces pathological attraction to ethanol. Effective with the withdrawal syndrome in patients with drug addiction to the anxiolytic benzodiazepine derivative tools, eliminates anxiety and depression and sleep disorders (in remission benzodiazepines can be completely replaced with trazodone). Not addictive. Helps restore libido and potency.

Therapeutic effect in 50% of patients after 3-7 days in 25% – after 2-4 weeks.

Pharmacokinetics Trazodone 100 mg

After oral absorption from the gastrointestinal tract is high. Time to Cmax in plasma – 1-2 pm Admission trazodone during or immediately after a meal increases the absorption and reduces Cmax and increases the time to achieve it.

Penetrates through histohematogenous barriers including the BBB. Penetrates the tissues and fluids (bile, saliva, breast milk). Binding to plasma proteins – 89-95%.

Metabolized in the liver by hydroxylation. In the metabolism of the drug involved isozymes CYP3A4, CYP3A5 and CYP3A7.

T1 / 2 in the α-phase of 3-6 h, the β-phase – 9.5 h. Write the kidneys – 75% as inactive metabolites within 98 hours after admission, 20% – in the bile.

Statement Trazodone 100 mg

Various forms of depression (endogenous, psychotic, neurotic, somatogenic) including with severe anxiety, including at least four of the following symptoms: sleep disturbance, appetite, psychomotor agitation or retardation, decreased interest in surroundings, decreased sexual activity, feelings of guilt, fatigue, slow thinking, decreased ability to concentrate, suicidal attempts / thoughts , bulimia, kleptomania, anxiety, and phobias. Benzodiazepine drug dependency, acute alcohol withdrawal syndrome. Decreased libido, impotence. Prophylaxis of migraine attacks.

Dosage and administration Trazodone 100 mg

The initial daily dose – 150-200 mg (3 doses). In milder forms of depression, the average maintenance dose – 150 mg / day, with moderate and severe forms – 300 mg / day. If necessary the dose may be increased to 600 mg / day. The main part of the daily dose is recommended to take at bedtime.

Side effect Trazodone 100 mg

From the central and peripheral nervous system: drowsiness, fatigue, dizziness, insomnia, headache, agitation, myalgia, impaired coordination, paresthesia, disorientation, blackout, tremor.

Cardio-vascular system: arrhythmia, conduction disturbances, bradycardia, ventricular fibrillation, lower blood pressure, orthostatic hypotension, syncope.

Part of the digestive system: nausea, vomiting, diarrhea, dry and bitter in the mouth.

On the part of the vision: blurred vision, eye irritation.

From hemopoiesis system: leukopenia, neutropenia (usually minor).

Others: nasal congestion, followed by priapism impotence, allergic reactions.

Contraindications Trazodone 100 mg

Ventricular fibrillation, tachycardia, myocardial infarction (early recovery period), a history of priapism, pregnancy, lactation, hypersensitivity to trazodone.

Pregnancy and breast feeding Trazodone 100 mg

Pregnancy and lactation is contraindicated.

Cautions

C wary of cardiac disease, hypotension, hypertension, renal and / or liver failure in children and adolescents under the age of 18 years.

Should not be used concurrently with MAO inhibitors.

Drug Interactions Trazodone 100 mg

A case of arrhythmias such as “pirouette”, while the use of trazodone with amiodarone.

A case of moderate anticoagulant effect of warfarin decrease while the use of trazodone.

With simultaneous application may increase the concentration of digoxin in the blood plasma and the development of symptoms of intoxication.

While the use of carbamazepine described a case raising the concentration of carbamazepine in plasma.

While the use of lithium salts may be tremor, reversible symptoms of neurotoxic effects.

When receiving pseudoephedrine during therapy with trazodone described a case of anxiety, panic, blackout, depersonalization.

While the use of thioridazine may increase the concentration of trazodone in plasma with tryptophan – described the case of anorexia nervosa, psychosis, hypomania, phenytoin – described the case to strengthen the side effects of phenytoin; with fluoxetine – may increase the side effects of chlorpromazine, trifluoperazine – may develop hypotension.

While the use of ethanol enhanced the inhibitory effect on the CNS.