Венлифт ODES

General characteristics. Structure:

Active ingredient: 42,43 mg, 84,85 mg or 169,7 mg of a venlafaksin of a hydrochloride that there correspond 37,5 mg, 75 mg or 150 mg of a venlafaksin in the form of pellets.

Pharmacological properties:

Pharmacodynamics. Antidepressant. On chemical structure венлафаксин it is impossible to carry to one known class of antidepressants (tricyclic, tetracyclic or others). It has two active enantiomeric racemic forms.

The antidepressive effect of a venlafaksin is connected with strengthening of neyrotransmitterny activity in TsNS. Venlafaksin and his main metabolite O-desmetilvenlafaksin (ODV) are powerful inhibitors of the return serotonin reuptake and noradrenaline and poorly suppress the return capture of a dopamine neurons. Venlafaksin and ODV equally effectively influence the return capture of neurotransmitters. Venlafaksin and ODV reduce beta and adrenergic reactions.

Venlafaksin has no affinity to m - and N-holinoretseptoram, histamine H1 receptors and α1-адренорецепторам a brain. Venlafaksin does not suppress activity of MAO. Has no affinity to opioid, benzodiazepine, fentsiklidinovy or to NMDA receptors.

Pharmacokinetics. After intake венлафаксин it is well soaked up from a GIT. After a single dose in doses of 25-150 mg of Cmax in a blood plasma it is reached during about 2.4 h and makes 33-172 ng/ml. Venlafaksin is exposed to intensive metabolism at "the first passing" through a liver. Cmax of ODV in a blood plasma is reached approximately in 4.3 h after reception and makes 61-325 ng/ml. In the range of daily doses of 75-450 mg венлафаксин and ODV have linear kinetics. After reception during food time of achievement of Cmax in a blood plasma increases for 20-30 min., however the size Cmax and absorption do not change.

Linkng of a venlafaksin and ODV with proteins of a blood plasma makes respectively 27% and 30%. At multiple dose of Css of a venlafaksin and ODV are reached within 3 days.

The main metabolite - ODV. T1/2 of a venlafaksin and ODV makes respectively 5 both 11 h ODV and other metabolites, and also not changed венлафаксин are removed by kidneys.

Patients with cirrhosis have concentration in a blood plasma of a venlafaksin and ODV are increased, and the speed of their removal is reduced. At a moderate or heavy renal failure the general clearance of a venlafaksin and ODV decreases, and T1/2 is extended. Decrease in the general clearance is generally observed at patients with KK less than 30 ml/min. The age and a sex of the patient do not influence pharmacokinetics of a venlafaksin.

Indications to use:

Depression of various etiology (treatment and prevention).

Route of administration and doses:

Accept inside. The recommended initial dose makes 75 mg in 2 receptions (on 37.5 mg of 2 times/days) daily. If after several weeks of treatment considerable improvement is not observed, it is possible to raise a daily dose to 150 mg (on 75 mg of 2 times/days). At a heavy depression or others of a state, demanding hospitalization it is possible to apply 150 mg in 2 receptions at once (on 75 mg of 2 times/days). After that it is possible to increase a daily dose by 75 mg each 2-3 days before achievement of desirable therapeutic effect. The maximum dose - 375 mg/days.

After achievement of necessary therapeutic effect the daily dose can be gradually lowered to the minimum effective level. Duration of the period necessary for a dose decline depends on the size of a dose, therapy duration, and also individual sensitivity of the patient.

For a maintenance therapy and prevention of a recurrence the minimal effective dose applied at treatment of a depressive episode is shown.

Patients with a renal failure at KK of 10-30 ml/min. should lower a dose by 25-50%. Due to the lengthening of T1/2 of a venlafaksin and its active metabolite (ODV) such patients should accept all dose of 1 times/days.

The patients who are on a hemodialysis can receive 50% of a usual daily dose of a venlafaksin after completion of a session of a hemodialysis.

At a moderate liver failure (the prothrombin time from 14 to 18 sec.) a dose should be lowered by 50%.

At patients of advanced age венлафаксин it is necessary to apply in the smallest effective dose. At increase in a dose the patient has to be under careful medical observation.

Upon termination of treatment it is recommended to reduce gradually a dose, at least, within a week and to watch a condition of the patient to minimize the risk connected with cancellation of a venlafaksin. Duration of the period necessary for a dose decline depends on the size of a dose, therapy duration, and also individual sensitivity of the patient.

Features of use:

Use at pregnancy and feeding by a breast. Use at pregnancy and in the period of a lactation (breastfeeding) is contraindicated.

Women of childbearing age have to apply reliable methods of contraception during treatment and see immediately a doctor in case of approach of pregnancy or planning of pregnancy.

Venlafaksin and metabolite of ODV are allocated with breast milk. Safety of these substances for newborn children is not proved therefore in need of reception of a venlafaksin in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination. If treatment of mother was complete shortly before childbirth, the newborn can have cancellation symptoms.

Use at abnormal liver functions. It is contraindicated at heavy abnormal liver functions.

At a moderate liver failure (the prothrombin time from 14 to 18 sec.) a dose should be lowered by 50%.

Use at renal failures. It is contraindicated at a renal failure of heavy degree (KK <10 ml/min.).

Patients with a renal failure at KK of 10-30 ml/min. should lower a dose by 25-50%. Due to the lengthening of T1/2 of a venlafaksin and its active metabolite (ODV) such patients should accept all dose of 1 times/days.

The patients who are on a hemodialysis can receive 50% of a usual daily dose of a venlafaksin after completion of a session of a hemodialysis.

Use for children. It is contraindicated at children's and teenage age up to 18 years.

Use for elderly patients. At patients of advanced age венлафаксин it is necessary to apply in the smallest effective dose. At increase in a dose the patient has to be under careful medical observation

Patients of advanced age should be warned about possibility of dizziness and disturbance of sense of equilibrium. During reception of a venlafaksin, especially in the conditions of dehydration or decrease in OTsK, at elderly patients the hyponatremia and/or a syndrome of insufficient secretion of ADG can be observed

Special instructions. With care it is necessary to apply венлафаксин after recently postponed myocardial infarction, at heart failure in a decompensation stage, at unstable stenocardia, arterial hypertension, tachycardia, a tachyarrhythmia, spasms in the anamnesis, intraocular hypertensia, closed-angle glaucoma, maniacal states in the anamnesis, predisposition to bleedings from integuments and mucous membranes, initially reduced body weight.

At patients with depressive frustration before any medicinal therapy it is necessary to consider probability of suicide attempts. Therefore in an initiation of treatment it is necessary to apply to decrease in risk of overdose whenever possible венлафаксин in a minimal effective dose, and the patient has to be under careful medical observation.

Patients with affective frustration at treatment by antidepressants (including venlafaksiny), can have hypomaniacal or maniacal states. As well as other antidepressants, венлафаксин patients should appoint with care with a mania in the anamnesis. Such patients need medical observation.

When developing epileptic seizures treatment should be interrupted.

The risk of tachycardia increases at use of a venlafaksin in high doses.

During treatment regular control of the ABP, especially during specification or increase in a dose is recommended.

Patients, especially advanced age, it is necessary to warn about possibility of dizziness and disturbance of sense of equilibrium.

During reception of a venlafaksin, especially in the conditions of dehydration or decrease in OTsK (including at the elderly patients and patients accepting diuretics), the hyponatremia and/or a syndrome of insufficient secretion of ADG can be observed.

During administration of drug the mydriasis in this connection control of intraocular pressure at the patients inclined to its increase or having closed-angle glaucoma is recommended can be observed.

As well as at treatment by other drugs operating on TsNS, the doctor has to establish careful observation of patients for identification of signs of abuse venlafaksiny. Careful control and observation are necessary for the patients having in the anamnesis of the instruction on such symptoms.

Against the background of reception of a venlafaksin it is necessary to observe extra care when performing electroconvulsive therapy since experience of use of a venlafaksin in these conditions is absent.

During treatment it is necessary to avoid alcohol intake.

Influence on ability to driving of motor transport and to control of mechanisms. In spite of the fact that венлафаксин does not influence psychomotor and cognitive functions, it is necessary to consider that any medicinal therapy by psychoactive drugs can worsen thought processes and reduce ability to performance of motive functions. It is necessary to warn the patient before an initiation of treatment about it. At emergence of such disturbances degree and duration of restrictions have to be established by the doctor.

Side effects:

The majority of side effects depends on a dose. At prolonged treatment weight and frequency of the majority of these effects decreases, and there is no need of cancellation of therapy.

From the alimentary system: a loss of appetite, a lock, nausea, vomiting, dryness in a mouth; seldom - hepatitis.

From a metabolism: increase in level of cholesterol of blood serum, decrease in body weight; sometimes - disturbance of functional trials of a liver, a hyponatremia, a syndrome of insufficient secretion of ADG.

From cardiovascular system: arterial hypertension, hyperemia of integuments; sometimes - postural hypotension, tachycardia.

From TsNS and peripheral nervous system: unusual dreams, dizziness, sleeplessness, nervous irritability, paresthesias, stupor, increase in a muscle tone, tremor, yawning; sometimes - apathy, hallucinations, spasms of muscles, a serotonergic syndrome; seldom - epileptic seizures, maniacal reactions, and also the symptoms reminding ZNS.

From an urinary system: a dysuria (generally - difficulties at the beginning of an urination); sometimes - an ischuria.

From a reproductive system: disturbances of an ejaculation, erection, anorgazmiya; sometimes - decrease in a libido, a menorrhagia.

From sense bodys: accommodation disturbances, mydriasis, vision disorders; sometimes - disturbance of flavoring feelings.

Dermatological reactions: perspiration; sometimes - a photosensitization.

From system of a hemopoiesis: sometimes - hemorrhages in skin (ecchymomas) and mucous membranes, thrombocytopenia; seldom - lengthening of a bleeding time.

Allergic reactions: sometimes - skin rash; seldom - a mnogoformny erythema, Stephens-Johnson's syndrome; very seldom - anaphylactic reactions.

Others: weakness, fatigue.

After sharp cancellation or a dose decline fatigue, drowsiness, a headache, nausea, vomiting, anorexia, dryness in a mouth, dizziness, diarrhea, sleeplessness, concern, alarm, nervous irritability, a disorientation, a hypomania, paresthesias, perspiration are possible. These symptoms are usually poorly expressed and pass without treatment.

Interaction with other medicines:

It is possible to begin reception of a venlafaksin not less than in 14 days after the end of therapy with MAO inhibitors. If the MAO reversible inhibitor was applied (моклобемид), this interval can be shorter (24 h). It is possible to begin therapy with MAO inhibitors not less than in 7 days after drug withdrawal of a venlafaksin.

Simultaneous use of a venlafaksin with lithium can increase concentration of the last in a blood plasma.

Strengthening of effects of a haloperidol because of increase in its concentration in blood at combined use is possible with venlafaksiny.

At simultaneous use with clozapine increase in its level in a blood plasma and development of side effects can be observed (for example, epileptic seizures).

The main way of removal of a venlafaksin includes metabolism with participation of CYP2D6 and CYP3A4 therefore it is necessary to observe extra care at purpose of a venlafaksin in combination with medicines which are inhibitors of these both enzymes. The nature of this interaction is not studied yet.

Cimetidinum suppresses metabolism of a venlafaksin at "the first passing" through a liver and does not exert impact on ODV pharmacokinetics. At most of patients only slight increase of the general pharmacological activity of a venlafaksin and ODV is expected (it is more expressed at elderly patients and at an abnormal liver function).

At a concomitant use with warfarin strengthening of anticoagulating effect of the last is possible.

Contraindications:

Renal failure of heavy degree (KK <10 ml/min.); heavy abnormal liver functions; concomitant use of MAO inhibitors; children's and teenage age up to 18 years; the established or alleged pregnancy; period of a lactation (breastfeeding); hypersensitivity to a venlafaksin.

Overdose:

Symptoms: changes of an ECG (lengthening of an interval of QT, blockade of legs of a ventriculonector, expansion of the QRS complex, etc.), sinus and ventricular tachycardia, bradycardia, hypotension, dizziness, disturbance of consciousness of various degree of manifestation (from drowsiness to a coma), spasms, up to a lethal outcome.

Treatment: use of absorbent carbon, induction of vomiting, a gastric lavage (for absorption reduction). Maintenance of passability of respiratory tracts for ensuring adequate ventilation and oxygenation. Careful observation and monitoring of a heart rhythm and other vital functions, a symptomatic and maintenance therapy is recommended. Efficiency of such actions as an artificial diuresis, dialysis, hemoperfusion and exchange hemotransfusion is improbable. There is no specific antidote.

In post-market researches cases of overdose of a venlafaksin were noted preferential at a concomitant use of alcohol and/or other medicines.

Storage conditions:

To store in the dark place, at a temperature not above 25 °C. A period of validity - 36 months.

Issue conditions:

According to the recipe

Packaging:

10 pieces - blisters from aluminum foil (3) - packs cardboard.
10 pieces - blisters from aluminum foil (10) - packs cardboard.