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medicalmeds.eu Medicines Antidepressants. Венлаксор®

Венлаксор®

Препарат Венлаксор®. AS Grindex (АО Гриндекс) Латвия


Producer: AS Grindex (JSC Grindeks) Latvia

Code of automatic telephone exchange: N06AX16

Release form: Firm dosage forms. Tablets.

Indications to use: Depression.


General characteristics. Structure:

Active ingredient: 37,5 mg and 70 mg of a venlafaksin.

Excipients: calcium hydrophosphate anhydrous, lactose anhydrous, carboxymethylstarch of sodium, magnesium stearate, silicon dioxide colloid anhydrous, dye ferrous oxide red (E172).

Means of antidepressive action.




Pharmacological properties:

Pharmacodynamics. Antidepressant. On chemical structure венлафаксин does not belong to one class of antidepressants (tricyclic, tetracyclic or others), is a racemate of two active enantomer.

The mechanism of antidepressive effect of drug is connected with its ability to potentsiirovat transfer of nervous impulse in TsNS. Venlafaksin and his main metabolite O-desmetilvenlafaksin (ODV) are strong inhibitors of the return serotonin reuptake and noradrenaline and weak inhibitors of the return capture of a dopamine. Besides, венлафаксин and ODV reduce beta and adrenergic reactivity both after single introduction, and at constant reception. Venlafaksin and ODV equally effectively influence the return capture of neurotransmitters.

Venlafaksin has no affinity to m-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. Venlafaksin is well soaked up from a GIT. After a single dose inside in doses of 25-150 mg of Cmax in a blood plasma makes 33-172 ng/ml and it is reached during approximately during 2.4 h. After administration of drug 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.

Is exposed to intensive metabolism at "the first passing" through a liver. Its main metabolite - O-desmetilvenlafaksin (ODV). Cmax of ODV in a blood plasma of 61-325 ng/ml is reached approximately in 4.3 h after introduction. Linkng of a venlafaksin and ODV with proteins of a blood plasma makes respectively 27% and 30%.

At repeated introduction of Css in plasma of a venlafaksin and ODV are reached within 3 days. In the range of daily doses of 75-450 mg, венлафаксин and ODV have linear kinetics.

The elimination half-life of a venlafaksin and ODV makes respectively 5 both 11 h ODV and other metabolites, and also not changed венлафаксин are removed by kidneys.

Pharmacokinetics in special clinical cases. 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 renal failure of average or heavy degree the general clearance of a venlafaksin and ODV decreases, and T1/2 increases. Decrease in the general clearance is generally observed at patients with KK lower than 30 ml/min.

The age and sex of the patient do not influence drug pharmacokinetics.


Indications to use:

Depressions of various etiology (treatment and prevention).


Route of administration and doses:

Inside, during food.

The recommended initial dose — 75 mg in 2 receptions (on 37,5 mg) daily. If after several weeks of treatment considerable improvement is not observed, it is possible to increase a daily dose to 150 mg (on 75 mg 2 times a day). If, according to the doctor, higher dose (the heavy depressive frustration or other states demanding hospitalization) is necessary, it is possible to appoint 150 mg in 2 receptions at once (on 75 mg 2 times in in day). 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 daily dose — 375 mg. After achievement of necessary therapeutic effect perhaps gradual reduction of a daily dose to the minimum effective level.

Maintenance therapy and prevention of a recurrence: the supporting treatment can continue 6 months and more. The minimal effective doses applied at treatment of a depressive episode are appointed.

Renal failure: at a slight renal failure (SKF —> 30 ml/min.) correction of the mode of dosing is not required. At a moderate renal failure (SKF — 10–30 ml/min.) should lower a dose by 25–50%. Due to the lengthening of an elimination half-life of a venlafaksin and its active metabolite of ODV, such patients should accept all dose once a day. It is not recommended to apply венлафаксин at a heavy renal failure (SKF — <10 ml/min.) as reliable data on such therapy are absent. Patients on a hemodialysis can receive 50% of a usual daily dose of a venlafaksin after end of a hemodialysis.

Liver failure: at a slight liver failure (PV — <14 c) correction of the mode of dosing is not required. At a moderate liver failure (PV — from 14 to 18 c) should reduce a dose by 50%. It is not recommended to apply венлафаксин at a heavy liver failure as reliable data on such therapy are absent.

To elderly patients: advanced age of the patient in itself does not demand change of a dose, however (as well as at purpose of other medicines) at treatment of elderly patients care, for example in connection with a possibility of a renal failure is required. It is necessary to apply the smallest effective dose. At increase in a dose the patient has to be under careful medical observation.

Termination of administration of drug of Venlaksor®: upon termination of administration of drug of Venlaksor® it is recommended to reduce gradually a drug dosage, at least within a week and to watch a condition of the patient to minimize the risk connected with drug withdrawal.

The period demanded for complete cessation of administration of drug depends on its dosage, duration of a course of treatment and specific features of the patient.


Features of use:

Drug withdrawal of Venlaksor®: as well as at treatment by other antidepressants, the sharp termination of therapy venlafaksiny — especially after high doses of drug — can cause cancellation symptoms in this connection it is recommended to reduce gradually before drug withdrawal its dose. 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.

At purpose of the tablets Venlaksor® patients with a lactose intolerance should consider the content of lactose in drug (30 mg in each tablet of 37,5 mg; 60 mg in each tablet of 75 mg).

At patients with depressive frustration before any medicinal therapy it is necessary to consider probability of suicide attempts. Therefore for decrease in risk of overdose the initial dose of drug has to be whenever possible low, 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 it has to be appointed with care the patient with a mania in the anamnesis. Such patients need medical observation.

As well as other antidepressants, венлафаксин it has to be appointed with care the patient with epileptic seizures in the anamnesis. Treatment venlafaksiny has to be interrupted when developing epileptic seizures.

Patients should be warned about need to see immediately a doctor when developing rash, urtikarny elements or other manifestations of allergic reactions.

At some patients during reception of a venlafaksin dozozavisimy increase in the ABP in this connection regular control of the ABP, especially during selection or increase in a dosage is recommended is noted.

There can be an increase in ChSS, especially during reception of high doses. Care at a tachyarrhythmia is recommended.

Patients, especially elderly, have to be warned about possibility of dizziness and disturbance of sense of equilibrium.

As well as other inhibitors of the return serotonin reuptake, венлафаксин the risk of hemorrhages in skin and mucous membranes can raise. At treatment of the patients predisposed to such states care is necessary.

During reception of a venlafaksin, especially in the conditions of dehydration or decrease in volume of blood (including at the elderly patients and patients accepting diuretics), the hyponatremia and/or a syndrome of insufficient secretion of antidiuretic hormone 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.

Venlafaksin is not investigated at the patients who recently had a myocardial infarction and having dekompensirovanny heart failure. Such patients should appoint drug with care.

It is necessary to establish observation of patients for identification of signs of abuse of drug, especially for the patients having such symptoms in the anamnesis.

Women of childbearing age have to apply the corresponding methods of contraception during reception of a venlafaksin.

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 reduce ability of removal of judgments, thinking or performance of motive functions. It is necessary to warn the patient before an initiation of treatment about it. At emergence of such effects degree and duration of restrictions have to be established by the doctor. Also alcohol intake is not recommended.

Safety of use of a venlafaksin at pregnancy is not proved therefore use during pregnancy (or alleged pregnancy) is possible only if the potential advantage for mother surpasses possible risk for a fruit. Women of childbearing age have to be warned about it prior to treatment and have to see immediately a doctor in case of approach of pregnancy or planning of pregnancy during treatment by drug.

Venlafaksin and his metabolite ODV are allocated in breast milk. Safety of these substances for newborn children is not proved therefore reception of a venlafaksin during breastfeeding is not recommended. In need of administration of drug 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 drug withdrawal symptoms.


Side effects:

The majority of the listed below side effects depend 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.

As decrease in frequency: often (≥1%), sometimes (≥0,1– <1%), it is rare (≥0,01– <0,1%), is very rare (<0,01%).

General symptoms: weakness, increased fatigue.

From a GIT: 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 — change of laboratory liver function tests, a hyponatremia, a syndrome of insufficient secretion of antidiuretic hormone.

From cardiovascular system: arterial hypertension; sometimes — postural hypotension, tachycardia.

From a nervous system: unusual dreams, dizziness, sleeplessness, hyperexcitability, paresthesias, stupor, increase in a muscle tone, tremor, yawning; sometimes — apathy, hallucinations, spasms of muscles, a serotoninovy syndrome; seldom — epileptic seizures, maniacal reactions, and also the symptoms reminding a malignant antipsychotic syndrome.

From urinogenital system: disturbances of an ejaculation, an erection, an anorgazmiya, dysuric frustration (generally — difficulties at the beginning of an urination); sometimes — decrease a libido, a menorrhagia, an ischuria.

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

From integuments: hyperemia of integuments; perspiration; sometimes — reactions of a photosensitivity; seldom — a mnogoformny erythema, Stephens-Johnson's syndrome.

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

Hypersensitivity reactions: sometimes — skin rash; very seldom — anaphylactic reactions.

After sharp cancellation of a venlafaksin or reduction of its dose can be observed: fatigue, drowsiness, a headache, nausea, vomiting, anorexia, dryness in a mouth, dizziness, diarrhea, sleeplessness, alarm, an acrimony, a disorientation, a hypomania, paresthesias, perspiration. These symptoms are usually poorly expressed and pass without treatment. Because of probability of emergence of these symptoms it is very important to reduce a drug dose gradually.


Interaction with other medicines:

Simultaneous use of MAO inhibitors and venlafaksin contraindicated. It is possible to begin administration of drug of Venlaksor® 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 Venlaksor®.

Venlafaksin does not influence lithium pharmacokinetics.

At simultaneous use with Imipraminum the pharmacokinetics of a venlafaksin and its metabolite of ODV does not change.

Haloperidol: the effect of the last can amplify because of increase in level of drug in blood at combined use.

At simultaneous use with diazepam the pharmacokinetics of drugs and their main metabolites significantly do not change. Also influence on psychomotor and psychometric effects of diazepam is not revealed.

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).

At simultaneous use with risperidony (despite increase in AUC of a risperidon) the pharmacokinetics of the sum of active components (a risperidon and its active metabolite) significantly did not change.

Strengthens influence of alcohol on psychomotor reactions.

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

Medicines, metaboliziruyemy P450 cytochrome isoenzymes: unlike many other antidepressants, the dose of a venlafaksin can be not reduced at simultaneous introduction with the drugs suppressing activity of CYP2D6 or patients with genetically caused decrease of the activity have CYP2D6 (CYP2D6 enzyme of system of P450 cytochrome will transform венлафаксин to an active metabolite of ODV) as total concentration of active agent and a metabolite (a venlafaksina and ODV) at the same time will not change.

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 the medicines oppressing both of these enzymes. Such medicinal interactions are not investigated yet.

Venlafaksin — rather weak CYP2D6 inhibitor also does not suppress activity of isoenzymes of CYP1A2, CYP2C9 and CYP3A4; therefore it is not necessary to expect it interaction with other drugs in which metabolism these liver enzymes participate.

Cimetidinum suppresses metabolism of "the first passing" of a venlafaksin 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).

Clinically significant interactions of a venlafaksin with anti-hypertensive (including beta adrenoblockers, APF inhibitors and diuretics) and antidiabetic drugs are not found.

The medicines connected with proteins of a blood plasma: linkng with proteins of plasma makes 27% for a venlafaksin and 30% — for ODV therefore influence on concentration in a blood plasma of the HP possessing high extent of linkng with proteins is not revealed.

At a concomitant use with warfarin the anticoagulating effect of the last can amplify.

At a concomitant use with indinaviry the pharmacokinetics of an indinavir changes (from 28% reduction of AUC and 36% decrease in Cmax), and the pharmacokinetics of a venlafaksin and ODV does not change. However clinical value of this effect is unknown.


Contraindications:

- hypersensitivity;

- a concomitant use of MAO inhibitors (see also section "Interaction");

- heavy renal failures and/or liver (glomerular filtration rate (GFR) <10 ml/min.);

- age up to 18 years (safety and efficiency for this age group are not proved);

- the established or suspected pregnancy;

- breastfeeding period.

With care:

- recently postponed myocardial infarction;

- unstable stenocardia;

- arterial hypertension;

- tachycardia;

- a convulsive syndrome in the anamnesis;

- increase in intraocular pressure;

- closed-angle glaucoma;

- maniacal states in the anamnesis;

- predisposition to bleedings from integuments and mucous membranes;

- initially reduced body weight.


Overdose:

Symptoms: changes of an ECG (lengthening of an interval of QT, blockade of a leg of a ventriculonector, expansion of the QRS complex), sinus or ventricular tachycardia, bradycardia, hypotension, convulsive states, consciousness change (decrease in level of wakefulness).

At overdose of a venlafaksin at a concomitant use with alcohol and/or other psychotropic drugs it was reported about death.

Treatment: symptomatic. Specific antidotes are unknown. Continuous control of the vital functions (breath and blood circulation) is recommended.

Purpose of absorbent carbon for decrease in absorption of drug. It is not recommended to cause vomiting in connection with danger of aspiration. Venlafaksin and ODV are not removed at dialysis.


Storage conditions:

In the dark place, at a temperature not above 25 °C. To store in the place, unavailable to children.


Issue conditions:

According to the recipe


Packaging:

On 10 tablets in the blister from PVC/Al, on 3 blisters in a cardboard pack.



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