Venlaxor
Venlaxor: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Venlaxor
ATX code: N06AX16
Active ingredient: venlafaxine (venlafaxine)
Producer: Grindeks, AO (Latvia)
Description and photo update: 2019-26-08
Prices in pharmacies: from 535 rubles.
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Venlaxor is an antidepressant drug.
Release form and composition
Dosage form Venlaxor - tablets: flat-cylindrical, light pink with dark pink blotches, with a line and a bevel on one side (10 pcs. In blisters, 3 blisters in a cardboard box).
Active ingredient: venlafaxine (in the form of hydrochloride), 1 tablet - 37.5 or 75 mg.
Additional components: anhydrous colloidal silicon dioxide, anhydrous lactose, calcium hydrogen phosphate anhydrous, magnesium stearate, sodium carboxymethyl starch, iron dye red oxide (E172).
Pharmacological properties
Pharmacodynamics
Venlaxor is an antidepressant.
The active substance of the drug, venlafaxine, is a racemate of two active enantomers and, in terms of chemical structure, does not belong to any class of antidepressants (tetracyclic, tricyclic or others).
The mechanism of the antidepressant action of venlafaxine is due to the ability to potentiate the transmission of nerve impulses to the central nervous system. The substance and its main metabolite EFA (O-desmethylvenlafaxine) are strong inhibitors of the reuptake of serotonin and norepinephrine and weak inhibitors of dopamine reuptake. In addition, they reduce β-adrenergic reactivity both after a single use and during prolonged therapy, and are equally effective in influencing the reuptake of neurotransmitters.
Venlafaxine has no affinity for m-cholinergic receptors, histamine H 1 receptors and α 1 -adrenergic receptors, as well as benzodiazepine, opioid, phencyclidine or NMDA receptors. The substance does not inhibit the activity of monoamine oxidase.
Pharmacokinetics
Venlafaxine is well absorbed from the gastrointestinal tract. After a single oral administration in doses from 25 to 150 mg, the value of C max (maximum concentration of the substance) in the blood plasma is in the range of 33-172 ng / ml, the time to reach it is 2.4 hours. After taking venlafaxine with meals, the time to reach C max in blood plasma increases by 20-30 minutes, but the absorption and C max remain unchanged.
Venlafaxine, during the first passage through the liver, undergoes intensive metabolism with the formation of the main metabolite - EFA. C max EFA in blood plasma of 61-325 ng / ml, the time to reach the index - 4.3 hours.
Venlafaxine and EFA bind to plasma proteins at 27% and 30%, respectively.
With repeated use of venlafaxine and EFA, their C ss (equilibrium concentrations) in plasma are reached within 3 days. With therapy in the dose range of 75 to 450 mg per day, venlafaxine and the major metabolite have linear kinetics.
T 1/2 (half-life) of the substance and EFA is 5 and 11 hours, respectively. EFA and other metabolites, as well as venlafaxine, are excreted unchanged by the kidneys.
With cirrhosis of the liver, the concentrations of venlafaxine and EFA in the blood plasma are increased, and the rate of their excretion decreases.
With moderate or severe renal failure, the total clearance of the substance and the main metabolite decreases, and T 1/2 increases. A decrease in total clearance is mainly observed when creatinine clearance is below 30 ml / min.
Neither gender nor age of the patient influences the pharmacokinetics of the drug.
Indications for use
According to the instructions, Venlaxor is a drug for the treatment of depression of various etiologies and prevention of relapse.
Contraindications
Absolute:
- severe liver dysfunction;
- severe renal dysfunction (glomerular filtration rate less than 10 ml / minute);
- established or suspected pregnancy;
- period of breastfeeding;
- age up to 18 years;
- simultaneous use of MAO (monoamine oxidase) inhibitors;
- hypersensitivity to the components of Venlaxor.
Relative:
- initially reduced body weight;
- suicidal tendencies;
- a history of manic conditions;
- a history of convulsive syndrome;
- predisposition to bleeding from the skin and mucous membranes;
- angle-closure glaucoma;
- arterial hypertension;
- unstable angina;
- tachycardia;
- recent myocardial infarction;
- increased intraocular pressure;
- hypovolemia;
- hyponatremia;
- renal or hepatic impairment;
- simultaneous use of diuretics.
Instructions for use of Venlaxor: method and dosage
Venlaxor tablets should be taken orally, preferably with meals.
The initial recommended daily dose is 75 mg - 37.5 mg 2 times a day. If there is no significant improvement in the condition within several weeks, the daily dose is increased to 150 mg - 75 mg 2 times a day. In severe depressive disorders or other conditions requiring inpatient treatment, it is possible to prescribe the drug immediately in a dose of 150 mg / day in 2 divided doses. After that, if necessary, the dose is continued to increase by 75 mg every 2-3 days until the desired therapeutic effect is achieved.
The highest daily dose of Venlaxor is 375 mg.
After achieving the desired effect, you can gradually reduce the therapeutic dose to the minimum effective.
Supportive therapy (including for the prevention of relapse) can last for 6 months or more. In this case, the minimum effective dose is prescribed, which was used during the treatment of the depressive episode.
With mild renal failure [glomerular filtration rate (GFR) more than 30 ml / minute] and mild liver failure [prothrombin time (PT) less than 14 seconds], there is no need to adjust the dose. In case of moderate renal failure (GFR 10-30 ml / minute), the dose is reduced by 25-50%, while the daily dose should be taken in 1 dose, since in this category of patients the half-life of venlafaxine and its active metabolite increases. With moderate hepatic impairment (PV 14-18 seconds), the dose is reduced by 50%.
For patients on hemodialysis, Venlaxor is prescribed at a dose of 50% of the usual dose. It is necessary to take pills after completing a hemodialysis session.
There is no need to adjust the dose in the elderly, but the minimum effective dose is recommended due to the likelihood of impaired renal function. These patients should be under constant medical supervision.
At the end of the course of therapy, Venlaxor should be canceled gradually, reducing the dose for at least a week, under the control of the patient's condition.
Side effects
Most of the side effects that occur are dose dependent. With prolonged treatment, their frequency and severity decrease, while the need to cancel Venlaxor usually does not arise.
Classification of side effects: often (> 1%), infrequently (0.1-1%), rarely (0.01-0.1%), very rarely (<0.01%).
Possible adverse reactions:
- from the central nervous system: often - nightmares, insomnia, asthenia, sedation, paresthesia, increased nervous irritability, muscle hypertonicity, dizziness, tremor; infrequently - myoclonus, hallucinations, apathy, fainting; rarely - manic disorders, convulsions, neuroleptic malignant syndrome;
- from the reproductive system: often - menorrhagia, anorgasmia, erectile dysfunction and / or ejaculation, decreased libido; infrequently - violation of orgasm in women;
- from the urinary system: often - urinary disorders; infrequently - urinary retention;
- from the digestive system: often - nausea, loss of appetite, vomiting; infrequently - involuntary teeth grinding (bruxism), increased activity of hepatic transaminases; rarely - hepatitis;
- on the part of the cardiovascular system: often - hyperemia of the skin, increased blood pressure; infrequently - lowering blood pressure, tachycardia, postural hypotension; very rarely - ventricular fibrillation, changes in the QT interval, ventricular tachycardia (including ventricular fibrillation);
- from the hematopoietic system: the frequency is unknown - neutropenia, agranulocytosis, pancytopenia, aplastic anemia;
- laboratory parameters: infrequently - thrombocytopenia; rarely - hyponatremia, increased bleeding time; with prolonged use or in high doses - hypercholesterolemia;
- from the senses: often - visual impairment, mydriasis, violation of accommodation; infrequently - a violation of taste perception;
- allergic reactions: infrequently - photosensitivity, rash; very rarely - anaphylaxis, erythema multiforme exudative (including Stevens-Johnson syndrome);
- others: often - sweating (including nighttime), weight loss; infrequently - an increase in body weight, ecchymosis; rarely - syndrome of inadequate secretion of antidiuretic hormone, serotonin syndrome (depression of consciousness of varying severity, psychomotor agitation, sweating, hyperthermia, tachycardia, abdominal pain, flatulence, diarrhea, nausea, vomiting, muscle rigidity, myoclonus, convulsions).
Withdrawal symptoms: sleep disturbances (difficulty falling asleep, drowsiness or insomnia, changes in the nature of dreams), asthenia, headache, increased fatigue, dizziness, increased sweating, increased nervous irritability, anxiety, paresthesias, confusion, hypomania, decreased appetite, dryness in mouth, diarrhea, nausea, vomiting. Most of these reactions are mild and do not require specific therapy.
Overdose
The main symptoms: ECG changes (in the form of a bundle branch block, lengthening of the QT interval, expansion of the QRS complex), ventricular / sinus tachycardia, hypotension, bradycardia, convulsive states, altered consciousness (decreased wakefulness). A fatal outcome has been reported against the background of an overdose of venlafaxine while taking it with alcohol and / or other psychotropic drugs.
Therapy: symptomatic. There is no specific antidote. In order to reduce the absorption of venlafaxine, the intake of activated charcoal is indicated. Vomiting is not recommended due to the risk of aspiration. Shows continuous monitoring of vital functions (blood circulation and respiration). During dialysis, the active substance and its metabolite are not excreted.
special instructions
As with other antidepressants, abrupt withdrawal of Venlaxor, especially when used in high doses, can lead to withdrawal. To prevent it, you should gradually reduce the dose. The period required for the complete withdrawal of the drug depends on the prescribed dose, the duration of the course of therapy and the individual characteristics of the patient.
When prescribing Venlaxor to patients with lactose intolerance, one should take into account: 1 37.5 mg tablet contains 30 mg of lactose, 1 tablet 75 mg - 60 mg of lactose.
Before starting therapy in patients with depressive disorders, the likelihood of suicidal attempts should be considered. Due to the risk of overdose, the starting dose should be as low as possible. In this case, the patient must be under constant medical supervision.
In case of recurrence of epileptic seizures in patients with a history of epilepsy, Venlaxor should be discontinued.
If allergic reactions develop, patients should immediately consult a doctor.
Due to the risk of increased blood pressure during treatment, especially during the period of selection and dose increase, regular monitoring of pressure is recommended.
Venlaxor may increase the heart rate, which should be taken into account when prescribing it (especially in high doses) to patients with tachyarrhythmia.
During therapy, it is necessary to monitor intraocular pressure in patients at risk of its increase or angle-closure glaucoma.
There is no experience with Venlaxor in combination with electroconvulsive therapy.
All patients during treatment should be monitored in order to detect signs of possible drug abuse in time.
Women of childbearing age should use reliable methods of contraception.
It is recommended to refrain from drinking alcohol during therapy.
Influence on the ability to drive vehicles and complex mechanisms
Venlafaxine does not affect cognitive and psychomotor functions, however, it should be borne in mind that psychoactive drugs can reduce the ability to think and make judgments and the speed of reactions, which should be warned about each patient when prescribing Venlaxor. In the event of the development of such effects, the degree and duration of the restrictions is determined by the doctor.
Application during pregnancy and lactation
Venlaxor is not prescribed during pregnancy (established or suspected) and lactation.
Women of childbearing age should use appropriate methods of contraception during treatment, and in case of pregnancy, consult a doctor immediately.
If the mother has stopped taking Venlaxor shortly before delivery, the newborn may develop a withdrawal syndrome.
Pediatric use
Venlaxor therapy is contraindicated in patients under 18 years of age.
With impaired renal function
- severe renal dysfunction (at a glomerular filtration rate of less than 10 ml / min): therapy is contraindicated;
- renal impairment: Venlaxor should be used under medical supervision.
Patients with moderate renal insufficiency (at a glomerular filtration rate of 10-30 ml / min), the dose should be reduced by 25-50%, Venlaxor should be applied once a day. Patients on hemodialysis are prescribed 50% of the usual daily dose after the end of hemodialysis.
For violations of liver function
- severe liver dysfunction: therapy is contraindicated;
- liver dysfunction: Venlaxor should be used under medical supervision.
With moderate hepatic impairment, the dose should be reduced by 50%.
Use in the elderly
Elderly patients need to be careful, in particular, because of the likelihood of impaired renal function. Venlaxor should be used at the lowest effective dose. When the dose is increased, careful medical monitoring of the patient's condition is required.
Drug interactions
Venlaxor is contraindicated during the period of use of MAO inhibitors. After their cancellation, at least 14 days should elapse, with the exception of moclobemide, in which case 24 hours are sufficient. MAO inhibitors can be used 7 days after Venlaxor is discontinued.
Venlafaxine can increase the concentration of haloperidol, which may increase its effect.
Venlaxor alters the pharmacokinetics of indinavir (the total concentration decreases by 28%, the maximum - by 36%), enhances the effect of ethanol on psychomotor reactions and the anticoagulant effect of warfarin, can increase the concentration of clozapine in the blood plasma and enhance its side effects (including epileptic seizures).
Caution should be exercised with the simultaneous use of drugs that inhibit the isoenzyme CYP2D6 or CYP3A4.
Analogs
Venlaxor analogs are: Velaxin, Velafax, Venlafaxine, Dapfix.
Terms and conditions of storage
Keep out of reach of children, protected from light at temperatures up to 25 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Venlaxor
Reviews of Venlaxor are mostly positive. The effect is noted to develop rapidly. Also, the advantages include a short course of use and the absence of addiction. Some users point to the development of pronounced adverse reactions. The cost of the funds is assessed as high.
Price for Venlaxor in pharmacies
The approximate price for Venlaxor is 668 rubles (30 tablets of 37.5 mg) or 874 rubles (30 tablets of 75 mg).
Venlaxor: prices in online pharmacies
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Drug name Price Pharmacy |
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Venlaxor 37.5 mg tablets 30 pcs. 535 RUB Buy |
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Venlaxor 75 mg tablets 30 pcs. 683 r Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
