Saturday, July 11, 2009

Trazodon (Trazodone)




Trade names

Azona. Trittiko. Trazodon.

Action

Pharmacological Effects - antidepressive, sedative. The therapeutic effect of half of the patients seen after 3-7 days, with 3 / 4 - at the end of the 2 nd week and 1 / 4 - 2-4 weeks. Antidepressive (timolepticheskoe) effect combined with anxiolytic and trankviliziruyuschim (effective for the expression of anxiety and severe insomnia).

Mechanism of Action

Selective serotonin inhibits seizure sinaptosomami brain potentiator and behavioral change, induced by serotonin precursor 5-gidroksitriptofanom, blocking alpha-adrenergic receptors.

Pharmacokinetics
Quickly and completely absorbed from the ZHKT. Time achieving Cmax is approximately 1 hour (increasing after meals). Passes through gistogematicheskie barriers, including GEB. Penetrates the tissue and ekzosekret (bile, saliva, milk, etc.). In livers subjected to transformations. Eliminations are diphasic nature. T1 / 2 of the first phase of 3-6 h, 5-9 h later; possible accumulation. Ekskretiruetsya (together with metabolites), mainly from urine.

Indications

Various forms of depression (endogenous, neurotic, somatogennye) with anxiety and tension, depression in elderly patients with organic diseases of the central nervous system.

Contraindications

Hypersensitivity, start-up period after myocardial infarction, disturbance of heart rhythm expressed disorders of liver and kidney function, pregnancy, breast-feeding (at the time of treatment excluded).

Limitations to the use of

With caution (when continuous monitoring of cardiac rhythm) designate, with heart disease, hypertension (because of the high-risk hypotensive reactions may require the reduction of doses of antihypertensive drugs).

Side Effects
Changes in vision, eye irritation, mortgaged nose, constipation, diarrhea, dry and bitter taste in the mouth, nausea, vomiting, dizziness, drowsiness, fatigue, headache, mialgii, discoordination, paresthesia, disorientation, blackout, tremor, a violation of heart rate and conductivity , bradycardia, atrial fibrillation, arterial hypotension with elements of orthostatic hypotension and sinkopalnymi conditions, leukopenia, neutropenia (usually small), priapizm, allergic edema, skin allergic reactions.

Interaction

Modifies the effect of warfarin (increases or decreases), potentiator effect of drugs, oppressive central nervous system, including barbiturates, alcohol. Antihypertensive funds increases the risk of orthostatic hypotension. Decreases hypotension caused by clonidine. Increases plasma concentrations of digoxin and phenytoin.

Dosing and Administration in Adults

Inside, after the meal. As antidepressant - 50 mg 3 times a day, then, depending on the type and severity of depression, the dose gradually (50 mg every 3-4 days) increased to 300-500 mg / day (less than 600 mg), maintenance dose also be selected individually. The main part of the daily dose is recommended to take before bedtime.

As - 25 mg 3 times a day. B / B and V / m - 50 mg for.

Pregnancy and lactation

Not recommended during pregnancy and lactation period.

Overdosage

Symptoms: nausea, drowsiness, priapizm, stop breathing, epileptiformnye seizures, changes in ECG, frequency and Enhancement of side reactions.

Treatment: gastric lavage and forced diuresis in order to accelerate the elimination of, the maintenance of vital functions.

Cautions

It should not be used concurrently with MAO inhibitors.

Do not combine with electric shocks. Patients should be warned men about the need for immediate treatment to the doctor (to stop taking trazodona) if there are lengthy and inadequate erection. Because until a remission may be maintained suicidal tendencies, the patient should prescribe the drug in the minimum required amounts.

Before the operation under general anesthesia is required early lifting trazodona. During the period of treatment is not recommended to receive alcoholic beverages (trazodon may increase the effects of alcohol). With carefully applied during the drivers of vehicles and people, a profession which is related to increased concentration.