Velaxin retard 150mg 28pills

1 prolonged-acting capsule contains:

active substance:

venlafaxine hydrochloride 169.68 mg (equivalent to 150 mg of venlafaxine, respectively)

    
auxiliary substances:

MCC;

sodium chloride;

ethyl cellulose;

talc;

dimethicon;

potassium chloride;

copovidone;

silicon dioxide colloidal anhydrous;

xanthan gum;

iron oxide yellow;

gelatin capsule:

titanium dioxide;

iron oxide is red;

iron oxide yellow;

gelatin

Pharmacodynamics

The mechanism of antidepressant effect of Velaxin is associated with its ability to potentiate the transmission of nerve impulse in the central nervous system. Venlafaxine and its main metabolite O-desmethylvenlafaxine (EFA) are strong serotonin and norepinephrine reuptake inhibitors and weak dopamine reuptake inhibitors. Venlafaxine does not have a remedy for muscarinic, cholinergic, histamine (H1) and 1-adrenergic brain receptors.

Venlafaxine does not inhibit the activity of monoamine oxidase (MAO). It has no affinity for opiate, benzodiazepine, phencyclidine or N-methyl-d-aspartate (NMDA) receptors.

Pharmacokinetics

After taking Velaxin, prolonged-acting capsules, Cmax of venlafaxine and EFA (the main metabolite) in plasma are achieved within (6.0±1.5) and (8.8±2.2) hours, respectively. The rate of absorption of venlafaxine from prolonged-acting capsules is lower than the rate of its elimination. Therefore, T1_/2 venlafaxine after prescribing Velaxin in the form of prolonged-acting capsules - (15±6) h - is actually T1_/2 absorption, not T1_/2 distribution - (5±2) h - which is noted after prescribing Velaxin in the form of tablets.

The binding of venlafaxine and EFA with blood plasma proteins is 27 and 30%, respectively. EFA and other metabolites, as well as non-metabolized venlafaxine, are excreted by the kidneys. With repeated administration of Css, venlafaxine and EFA are achieved within 3 days. In the range of daily doses of 75-450 mg, venlafaxine and EFA have linear kinetics. After taking the drug while eating, Tmax in blood plasma increases by 20-30 minutes, but the values of Cmax and absorption do not change.

In patients with liver cirrhosis, the plasma concentrations of venlafaxine and EFA are increased, and the rate of their excretion is reduced. In moderate or severe renal failure, the overall clearance of venlafaxine and EFA decreases, and T1_/2 increases. A decrease in overall clearance is mainly observed in patients with Cle creatinine below 30 ml/min.

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

Depression of various etiologies, treatment and prevention

The safety of the use of venlafaxine during pregnancy has not been proven, so the use during pregnancy (or suspected pregnancy) is possible only if the potential benefit to the mother exceeds the possible risk to the fetus. Women of childbearing age should be warned about this before treatment and should immediately consult a doctor in case of pregnancy or planning of pregnancy during treatment with the drug.

Venlafaxine and EFA are released in breast milk. The safety of these substances for newborns has not been proven, so taking venlafaxine during breastfeeding is not recommended. If it is necessary to take the drug during lactation, the issue of stopping breastfeeding should be resolved. If the mother's treatment was completed shortly before childbirth, the newborn may have symptoms of drug withdrawal.

• hypersensitivity to any component of Velaxin;
• simultaneous intake of MAO inhibitors;
• severe kidney and/or liver dysfunction (glomerular filtration rate (GFR) less than 10 ml/min, PV more than 18 s);
• age up to 18 years (safety and effectiveness for this age group have not been proven);
• pregnancy or suspected pregnancy;
• lactation period (there is not enough data from controlled studies).

With caution: recent myocardial infarction, unstable angina, heart failure, coronary artery diseases, ECG changes, including elongation of the QT interval, electrolyte balance disorders, arterial hypertension, tachycardia, history of seizures, intraocular hypertension, closed-angle glaucoma, manic conditions in history, predisposition to bleeding from the skin and mucous membranes, initially reduced body weight.

Most of the side effects listed below depend on the dose. With long-term treatment, the severity and frequency of most of these effects decreases, and there is no need to cancel therapy.

Common symptoms: weakness, fatigue.

From the gastrointestinal tract: decreased appetite, constipation, nausea, vomiting, dry mouth.

From the metabolic side: increase in serum cholesterol, decrease in body weight.

From the cardiovascular system: arterial hypertension. skin hyperemia.

From the nervous system: unusual dreams, dizziness, insomnia, increased excitability, paresthesia, stupor, increased muscle tone, tremor, yawning.

On the part of the genitourinary system: ejaculation disorders, erection, anorgasmia, dysuric disorders.

From the sensory organs: accommodation disorders, mydriasis, visual impairment.

From the skin: sweating.

After a sharp withdrawal of venlafaxine or a decrease in its dose, fatigue, drowsiness, headache, nausea, vomiting, anorexia, dry mouth, dizziness, diarrhea, insomnia, anxiety, increased irritability, sweating. These symptoms are usually mild and go away without treatment. Due to the likelihood of these symptoms, it is very important to gradually reduce the dose of the drug.

Simultaneous use of MAO and venlafaxine inhibitors is contraindicated. Velaxin can be started at least 14 days after the end of therapy with MAO inhibitors. If a reversible MAO inhibitor (moclobemide) was used, this interval may be shorter (24 hours). Therapy with MAO inhibitors can be started at least 7 days after the withdrawal of Velaxin.

Simultaneous use of venlafaxine with lithium can increase the level of the latter.

When used simultaneously with imipramine, the pharmacokinetics of venlafaxine and EFA do not change. At the same time, their simultaneous use enhances the effects of desipramine - the main metabolite of imipramine - and its other metabolite - 2-OH - imipramine, although the clinical significance of this phenomenon is unknown.

Haloperidol: joint use increases the level of haloperidol in the blood and enhances its effects.

When used simultaneously with diazepam, the pharmacokinetics of drugs and their main metabolites do not change significantly. There was also no effect on the psychomotor and psychometric effects of diazepam.

When used simultaneously with clozapine, there may be an increase in its plasma level and the development of side effects (e.g. seizures).

When used simultaneously with risperidone (despite the increase in AUC of risperidone), the pharmacokinetics of the sum of the active components (risperidone and its active metabolite) does not change significantly.

The decrease in mental and motor activity under the influence of alcohol did not increase after the prima of venlafaxine. Despite this, as with other drugs that affect the CNS, the use of alcoholic beverages is not recommended during venlafaxine therapy.

Against the background of taking venlafaxine, special care should be taken in electroconvulsive therapy, as there is no experience of using venlafaxine in these conditions.

Drugs metabolized by cytochrome P450 isoenzymes: CYP2D6 enzyme of the cytochrome P450 system converts venlafaxine into an active metabolite of EFI. Unlike many other antidepressants, the dose of venlafaxine can not be reduced when administered simultaneously with drugs that suppress the activity of CYP2D6, or in patients with a genetically determined decrease in CYP2D6 activity, since the total concentration of venlafaxine and EFA will not change.

The main way of excretion of venlafaxine includes metabolism involving CYP2D6 and CYP3A4; therefore, special care should be taken when prescribing venlafaxine in combination with drugs that inhibit both of these enzymes. Such drug interactions have not yet been investigated.

Venlafaxine is a relatively weak CYP2D6 inhibitor and does not inhibit the activity of CYP1A2, CYP2C9 and CYP3A4 isoenzymes; therefore, its interaction with other drugs in the metabolism of which these liver enzymes are involved should not be expected.

Cimetidine inhibits the metabolism of the first passage of venlafaxine and does not affect the pharmacokinetics of EFA. Most patients are expected to have only a slight increase in the overall pharmacological activity of venlafaxine and EFA (more pronounced in elderly patients and in liver dysfunction).

Clinical studies have not found clinically significant interactions of venlafaxine with antihypertensive (including beta-blockers, ACE inhibitors and diuretics) and antidiabetic drugs.

Drugs associated with blood plasma proteins: binding to plasma proteins is 27% for venlafaxine and 30% for EFA, so drug interactions due to protein binding should not be expected.

When taken simultaneously with warfarin, the anticoagulant effect of the latter can be enhanced, while the PV is lengthened and MHO is increased.

When taken simultaneously with indinavir, the pharmacokinetics of indinavir changes (with a 28% decrease in AUC and a 36% decrease in Cmax), and the pharmacokinetics of venlafaxine and EFA do not change. However, the clinical significance of this effect is unknown.

Inside, while eating. Each capsule should be swallowed whole and washed down with liquid. Capsules cannot be divided, crushed, chewed or placed in water. The daily dose should be taken at one time (morning or evening), each time at about the same time.

Depression. The recommended initial dose is 75 mg once a day.

If, in the opinion of the doctor, a higher dose is needed (severe depressive disorder or other conditions that require inpatient treatment), you can immediately prescribe 150 mg once a day. Subsequently, the daily dose can be increased by 75 mg at intervals of 2 weeks or more (but not more than 4 days), until the desired therapeutic effect is achieved. The maximum daily dose is 350 mg.

After achieving the necessary therapeutic effect, the daily dose can be gradually reduced to the minimum effective level.

Supportive therapy and prevention of relapses. Treatment of depression should last at least 6 months. In stabilizing therapy, as well as therapy to prevent relapses or new episodes of depression, doses that have proven to be effective are usually used. The doctor should regularly (at least once every 3 months) monitor the effectiveness of long-term therapy with Velaxin.

Transfer of patients with Velaxin tablets. Patients taking Velaxin in the form of tablets can be transferred to take the drug in the form of prolonged-acting capsules, with an equivalent dose 1 time per day. However, an individual dose adjustment may be required.

Renal failure. In case of mild renal failure (GFR more than 30 ml/min), correction of the dosing regimen is not required. In case of moderate renal failure (GFF 10-30 ml/min), the dose should be reduced by 50%. Due to the elongation of T1_/2 venlafaxine and EFA, such patients should take the entire dose once a day. It is not recommended to use venlafaxine for severe renal failure (GFF less than 10 ml/min), as there are no reliable data on such therapy. Patients on hemodialysis can receive 50% of the usual daily dose of venlafaxine after completion of hemodialysis.

Liver failure. In case of mild liver failure (PV less than 14 s), correction of the dosing regimen is not required. In case of moderate liver failure (PV from 14 to 18 s), the dose should be reduced by 50%. It is not recommended to use venlafaxine for severe liver failure, as there are no reliable data on such therapy.

Elderly patients. The patient's old age itself does not require a change in the dose, but (as with the prescription of other drugs) caution is required in the treatment of elderly patients, for example, in connection with the possibility of impaired kidney function. The lowest effective dose should be used. When increasing the dose, the patient should be under close medical supervision.

Children and adolescents (under the age of 18). The safety and efficacy of venlafaxine in children and adolescents under the age of 18 have not been established.

Cancellation of the drug Velaxin. As with other antidepressants, abrupt withdrawal of (especially high doses) of venlafaxine can cause withdrawal symptoms. Therefore, a gradual reduction in the dose is recommended before the complete cancellation of the drug. If high doses have been used for more than 6 weeks, it is recommended to reduce the doses for at least 2 weeks. The duration of the period required to reduce the dose depends on the dose, the duration of therapy, as well as the patient's reactions.

Symptoms: ECG changes (elongation of the QT interval, blockade of the Geese bundle leg, expansion of the QRS complex), sinus or ventricular tachycardia, bradycardia, arterial hypotension, convulsive conditions, depression of consciousness (reduction of wakefulness). In case of an overdose of venlafaxine when taken simultaneously with alcohol and/or other psychotropic drugs, a fatal outcome was reported.

Treatment: symptomatic. Specific antidotes are unknown. Continuous monitoring of vital functions (breathing and blood circulation) is recommended. Purpose of activated carbon to reduce the absorption of the drug. It is not recommended to cause vomiting due to the danger of aspiration. Venlafaxine and EFA are not excreted during dialysis.

Depression increases the risk of suicidal thoughts and suicide attempts. This risk persists until the onset of persistent remission. Therefore, patients should be under constant medical supervision, and they should be given only a small number of capsules of the drug to reduce the risk of possible abuse and/or overdose.

Velaxin should not be used in the treatment of children and adolescents under 18 years of age. An increase in the likelihood of suicidal behavior (suicide attempt and suicidal thoughts), as well as hostility in clinical trials, is more common among children and adolescents receiving antidepressants than in placebo groups.

Aggressive behavior was reported while taking venlafaxine (especially at the beginning of treatment and after withdrawal of the drug).

The use of venlafaxine can cause psychomotor arousal, which clinically resembles akathisia, characterized by anxiety with the need to move, often combined with the inability to sit or stand still. This is most often observed during the first few weeks of treatment. If these symptoms occur, an increase in the dose may have an adverse effect, and consideration should be given to the advisability of continuing to take the drug.

Like all antidepressants, venlafaxine should be prescribed with caution to patients with mania and/or hypomania in history, as the drug can cause an increase in their signs. In these cases, medical supervision is necessary.

Care should be taken when treating patients with a history of seizures. If seizures occur or their frequency increases, treatment with venlafaxine should be interrupted.

Like selective serotonin reuptake inhibitors, venlafaxine should be used with caution when used simultaneously with antipsychotic drugs, as symptoms resembling neuroleptic malignant syndrome may develop.

Patients should be warned to see a doctor immediately if a rash, urticaria or other allergic reactions occur.

Some patients have a dose-dependent increase in blood pressure while taking venlafaxine, and therefore regular monitoring of BP is recommended, especially at the beginning of treatment or when the dose is increased.

During venlafaxine, individual cases of orthostatic hypotension are described. Patients, especially the elderly, should be warned about the possibility of dizziness and imbalance.

Venlafaxine can cause an increase in heart rate, especially when taking high doses. Special care should be taken when prescribing the drug to patients with conditions that may increase with an increase in heart rate.

There have not been sufficient studies on the use of venlafaxine in patients who have recently had a myocardial infarction or suffer from decompensated heart failure, so these patients should be used with caution.

Like other serotonin reuptake inhibitors, venlafaxine can increase the risk of hemorrhages in the skin and mucous membranes, so caution is needed in the treatment of patients predisposed to bleeding.

When taking venlafaxine, especially in conditions of dehydration or decreased blood volume (including in elderly patients and patients taking diuretics), hyponatremia and/or insufficient ADH secretion syndrome may occur.

Cases of mydriasis have been noted while taking venlafaxine, so patients with a predisposition to increased intraocular pressure or at risk of closed-angle glaucoma need careful medical supervision.

In case of renal and liver failure, special care is needed. In some cases, a dose reduction is required.

The safety and efficacy of venlafaxine with weight-reducing agents, including phentermine, have not been established, so their simultaneous use (as well as the use of venlafaxine as monotherapy for weight loss) is not recommended. A clinically significant increase in serum cholesterol was observed in some patients receiving venlafaxine for at least 4 months. Therefore, with long-term use of the drug, it is advisable to monitor the level of serum cholesterol.

After stopping taking the drug, especially sudden, withdrawal symptoms often occur. The risk of withdrawal symptoms may depend on several factors, including the duration of the course and dose, as well as the rate of dose reduction. Symptoms of withdrawal, such as dizziness, sensory disorders (including paresthesia and a feeling of electric current), sleep disorders (including insomnia and unusual dreams), arousal or anxiety, nausea and/or vomiting, tremor, sweating, headache, diarrhea, increased and increased heartbeat and emotional instability, are usually mild or moderate, but in some patients they can be severe. They are usually observed in the first days after withdrawal of the drug, although there have been separate reports of such symptoms in patients who accidentally missed one dose. Usually these phenomena disappear on their own within 2 weeks; however, in some patients they may be longer (2-3 months or more). Therefore, before canceling venlafaxine, it is recommended to gradually reduce its dose within a few weeks or months, depending on the patient's condition.

Influence on the ability to drive a car or perform work that requires an increased speed of physical and mental reactions. It should be borne in mind that any drug therapy with psychoactive drugs can reduce the ability to judge, think or perform motor functions. The patient should be warned about this before starting treatment. If such effects occur, the degree and duration of the restrictions should be established by a doctor.