Effexor
Effexor (Venlafaxine)Effexor is an antidepressant. A powerful inhibitor of return capture of a serotonin and Noradrenalinum. It is applied to treatment and preventive maintenance of depressions of a various aetiology: depressions at presence or absence of symptoms of alarm, preventive maintenance of relapses of depression. In the form of tablets with immediate liberation it is shown for depression treatment. In the form of capsules with the modified liberation it is shown for treatment of depression, generalised disturbing disorder and social phobias.
Pharmacokinetics
Effexor is well soaked up from GASTROINTESTINAL TRACT. After unitary reception of 25-150 mg Cmax of Effexor and its active metabolite are reached during 3-5 and 5-9 h accordingly. At Effexor reception during meal time of achievement Cmax in a blood plasma is enlarged on 20-30 mines, however sizes Cmax and absorptions do not change. Linkage Effexor with fibers of plasma and its metabolite makes 27 % and 30 % accordingly.
Indications
Effexor is applied to treatment and preventive maintenance of depressions of a various aetiology:
Depressions (at presence or absence of symptoms of alarm) both in out-patient conditions, and in a hospital;
Preventive maintenance of relapses of depression, including at recurrent depressive disorder (at positive therapeutic effect).
Effexor in the form of tablets with immediate liberation it is shown for depression treatment.
Effexor in the form of capsules with the modified liberation it is shown for treatment of depression, generalised disturbing disorder and social phobias.
Way of application and dose
Effexor prescribe inside; tablets and capsules are recommended to be accepted during meal; swallow entirely, washing down with a liquid; it is impossible to divide, crush, chew or dissolve in water.
Recommended initial Effexor dose makes 75 mg in 2 receptions daily (37,5 mg 2 times a day). If after several weeks of treatment it is not observed appreciable improvement, daily Effexor dose is possible to raise about 150 mg a day in two steps (on 75 mg 2 times a day). If, according to the doctor, higher dose (serious depressive disorder or other conditions demanding hospitalisation), it it is possible to prescribe 150 mg Effexor at once in 2 receptions (75 mg 2 times a day) is necessary. The interval between risings of daily Effexor doses before achievement of desirable therapeutic effect can make 2 weeks and more, but it is not less 4 days. Maximum daily Effexor dose makes 375 mg. After achievement of necessary therapeutic effect daily Effexor dose can be gradually lowered to the minimum effective level.
Overdosage
Cases of Effexor overdosage became perceptible mainly at simultaneous reception of alcohol and-or other medical products.
Symptoms: electrocardiogram changes (elongation of interval QT, blockade of a leg of a ventriculonector, expansion of complex QRS), a bradycardia, a hypotension, giddiness, convulsive conditions, disturbance of consciousness of various degree of expression (depression of level of wakefulness - from drowsiness to a coma). At Effexor overdosage at simultaneous reception with alcohol and-or other psychotropic preparations, it was informed on a lethal outcome.
Treatment. Careful observation and monitoring of a rhythm of heart and other vital functions, symptomatic and a maintenance therapy Is recommended. Appointment of the activated coal, a gastric lavage for depression of Effexor absorption. It is not recommended to cause vomiting in connection with danger of an aspiration. Maintenance of passableness of respiratory tracts for maintenance of adequate ventilation and oxygenation. Efficiency of such actions as an artificial diuresis, a dialysis, a hemoperfusion and a metabolic hemotransfusion is improbable. Specific antidotes are unknown.
Contraindications
Effexor contraindicative in following cases:
Hypersensitivity to Venlafaxine or to other components of a preparation;
Simultaneous reception of inhibitors MAO and the period till 14 days after their cancellation (therapy by Effexor is necessary for stopping not less than for 7 days prior to the beginning of application of inhibitors MAO);
Serious disturbances of function of kidneys (rate of a glomerular filtration <10 ml/mines) and-or a liver (a prothrombin time> 18);
Children's and teenage age till 18 years (safety and efficiency for this age group are not proved);
The established or prospective pregnancy, the lactemia period (there are no sufficient given controllable researches).
Effexor prescribe with care:
Diseases of a liver and kidneys;
Diseases of heart and vessels: recently transferred myocardial infarction, an astable stenocardia, an arterial hypertensia, a tachycardia;
Convulsive syndrome in the anamnesis;
Ophthalmotonus rising, angle-closure glaucoma;
Maniacal conditions in the anamnesis;
Predisposition to bleedings from integuments and mucosas;
Initially lowered mass of a body.
Application at pregnancy and feeding by a breast
Adequate and strictly controllable researches on safety of Effexor application at pregnancy it is not spent; safety is not proved. Effexor Application during pregnancy (or prospective pregnancy) is contraindicative; use is possible only in case of emergency.
Effexor is allocated in thoracal milk. Safety of these substances for newborn children is not proved. In need of Effexor reception in a lactemia it is necessary to solve a question on the termination of thoracal feeding.
If Effexor applied directly ahead of sorts, it is necessary to consider possibility of development of symptoms of cancellation of a preparation at the newborn.
Side effects
The majority listed below Side effects depends on Effexor dose. At long treatment gravity and frequency of the majority of these effects decrease, and there is no necessity of cancellation of Effexor therapy.
The general symptoms: delicacy, fatigability.
From the alimentary system: appetite depression, a constipation, a nausea, vomiting, dryness in a mouth; sometimes - a bruxism (gnashing by a teeth in a dream), change of gustatory sensations; change of indicators of functional hepatic assays, a hepatitis.
From a metabolism: rising of level of cholesterol of blood serum (especially at long Effexor application or at application in higher doses), depression of mass of a body; sometimes - a hyponatremia, rising of mass of a body.
From cardiovascular system: an arterial hypertensia, expansion of blood vessels (rushes of blood); sometimes - an orthostatic hypotension (syncopes), a tachycardia; very seldom - change of interval QT, fibrillation of ventricles, a ventricular tachycardia (including a ventricular fibrillation).
From party TSNS and peripheric nervous system: an asthenia, the delicacy, unusual dreamings, giddiness, a sleeplessness, nervous excitability, paresthesias, a stupor, the raised tonus of muscles, a tremor, a yawning; sometimes - apathy, hallucinations, a myoclonus (spastic strictures of muscles) ; seldom - epileptic attacks (cramps), maniacal reactions, and also the symptoms reminding a malignant antipsychotic syndrome.
From genitourinary system: ejaculation disturbances, erection disturbance, orgasm disturbance, dysuric disorders (basically difficulties in the emiction beginning); sometimes - a menorrhagia, an ischuria.
From sense organs: accommodation disturbances, a mydriasis, sight disturbance; sometimes - disturbance of gustatory sensations.
From hemopoiesis system: sometimes - hemorrhages in a skin (ecchymomas) and mucosas; seldom - a thrombocytopenia, bleeding time elongation. Unstated frequency there is an agranulocytosis, an aplastic anaemia, a neutropenia, a pancytopenia.
Dermatological reactions: a sweating; sometimes - reactions photosensitivities (photosensitization), an alopecia.
Allergic reactions: sometimes - a dermal eruption; seldom - anaphylactic reactions, Stevens-Johnson's syndrome.
After sharp cancellation of Effexor or dose declines are possible fatigability, drowsiness, a headache, a nausea, vomiting, an anorexia, dryness in a mouth, giddiness, diarrhoeia, a sleeplessness, anxiety, alarm, nervous irritability, a disorientation, a hypomania, paresthesias, a sweating. These symptoms are usually weakly expressed and pass without treatment. Because of probability of occurrence of these symptoms it is very important to reduce gradually Effexor dose (as well as any other antidepressant), especially after reception in high doses. Duration of the period necessary for Effexor dose decline, depends on size of a dose, duration of therapy, and also individual sensitivity of the patient.
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