Velaxin
Velaxin: 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: Velaxin
ATX code: N06AX16
Active ingredient: venlafaxine (venlafaxine)
Producer: EGIS Pharmaceuticals PLC (Hungary)
Description and photo update: 2019-21-08
Prices in pharmacies: from 714 rubles.
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Velaxin is a drug used to treat depression.
Release form and composition
Velaxin is available in the following dosage forms:
- Tablets: almost white or white, round, flat, beveled, odorless or almost odorless; engraving on one side (25 / 37.5 / 50/75 mg, respectively) "E 744", "E 741", "E 742" or "E 743" (10 pcs. in blisters, 1-3 or 6 blisters in a cardboard box; 14 pcs. in blisters, 2 blisters in a cardboard box);
- Sustained-release capsules: gelatinous solid, self-closing, with a transparent colorless body and an orange-brown cap; the contents of the capsules are a mixture of yellow and white pellets, odorless or almost odorless (10 pcs. in blisters, 3 blisters in a cardboard box; 14 pcs. in blisters, 2 blisters in a cardboard box).
The composition of 1 tablet includes:
- Active ingredient: venlafaxine (as venlafaxine hydrochloride) - 25, 37.5, 50 or 75 mg;
- Auxiliary components (25 / 37.5 / 50/75 mg, respectively): lactose monohydrate - 56.62 / 84.93 / 113.24 / 169.86 mg, microcrystalline cellulose - 24/36/48/72 mg, glycolate sodium starch (type A) - 8.4 / 12.6 / 16.8 / 25.2 mg, anhydrous colloidal silicon dioxide - 0.9 / 1.35 / 1.8 / 2.7 mg, magnesium stearate - 1, 8 / 2.7 / 3.6 / 5.4 mg.
1 capsule contains:
- Active ingredient: venlafaxine (as hydrochloride) - 75 or 150 mg;
- Auxiliary components: microcrystalline cellulose, ethyl cellulose, sodium chloride, dimethicone, talc, copovidone, potassium chloride, xanthan gum, anhydrous colloidal silicon dioxide, yellow iron oxide.
Composition of gelatin capsules: iron oxide yellow and red, titanium dioxide, gelatin.
Pharmacological properties
Pharmacodynamics
The active substance of Velaxin is venlafaxine. It is an antidepressant that is a racemate of two active enantiomers and does not chemically belong to any class of antidepressants (tetracyclic, tricyclic, or otherwise).
The mechanism of the antidepressant action of venlafaxine is based on its ability to potentiate the transmission of nerve impulses in the central nervous system. Venlafaxine and its main metabolite, O-desmethylvenlafaxine (EFA), are strong serotonin and norepinephrine reuptake inhibitors (SNRI) and weak dopamine reuptake inhibitors.
The substance and EFA equally effectively affect the reuptake of neurotransmitters and contribute to a decrease in beta-adrenergic reactivity both after a single use and during a course of therapy.
Venlafaxine has no affinity for cholinergic, muscarinic, α 1 -adrenergic and histamine (H 1) receptors in the brain, and does not inhibit the activity of monoamine oxidase. Also, the substance has no affinity for benzodiazepine, opiate, N-methyl-d-aspartate (NMDA) or phencyclidine receptors.
Pharmacokinetics
Venlafaxine is well absorbed from the gastrointestinal tract.
After a single dose of 25–150 mg of venlafaxine in the form of tablets, C max (maximum concentration of the substance) in blood plasma reaches 33–172 ng / ml in about 2.4 hours.
The substance undergoes intensive metabolism during the first passage through the liver with the formation of EFA. The half-lives of venlafaxine and EFA are approximately 5 and 11 hours, respectively. The maximum concentration of EFA in blood plasma is 61–325 ng / ml, the time to reach it is approximately 4.3 hours.
After taking Velaxin in the form of prolonged-release capsules, peak plasma concentrations of venlafaxine and EFA in the blood are reached within 6 ± 1.5 and 8.8 ± 2.2 hours, respectively. The rate of absorption of a substance from capsules of prolonged action is lower than the rate of its elimination. In this regard, the half-life of venlafaxine after using the drug in this dosage form is 15 ± 6 hours and is actually the absorption period, rather than the distribution period (5 ± 2 hours), which is observed after the administration of Velaxin in the form of tablets.
Venlafaxine and EFA bind to plasma proteins at 27% and 30%, respectively. The elimination of EFA and other metabolites, as well as unmetabolized venlafaxine, is carried out by the kidneys. Equilibrium concentrations of venlafaxine and EFA after repeated use are reached within 3 days.
Venlafaxine and EFA have linear kinetics over the 75–450 mg daily dose range. After taking Velaxin with meals, the time to reach C max in blood plasma increases by 20-30 minutes, while the values of absorption and maximum concentration do not change.
With cirrhosis of the liver, plasma concentrations of venlafaxine and EFA increase, and the rate of their excretion decreases.
The total clearance of venlafaxine and EFA in patients with moderate / severe renal impairment decreases and the elimination half-life increases. A decrease in total clearance is observed mainly when creatinine clearance is below 30 ml / min.
The effect of gender and age on the pharmacokinetics of the drug has not been recorded.
Indications for use
According to the instructions, Velaxin is prescribed for depressions of various etiologies, including anxiety (treatment and prevention).
Contraindications
Absolute:
- Severe functional disorders of the kidneys (at a glomerular filtration rate <10 ml per minute);
- Severe liver dysfunction;
- Simultaneous use with monoamine oxidase inhibitors;
- Age up to 18 years (the safety and efficacy of Velaxin for this category of patients has not been studied);
- Pregnancy (established or suspected) and lactation;
- Hypersensitivity to drug components.
Relative (Velaxin should be taken with caution in the presence of the following diseases / conditions):
- A history of seizures;
- Recently suffered myocardial infarction;
- Arterial hypertension;
- Unstable angina;
- Tachycardia;
- Closed-angle glaucoma;
- Increased intraocular pressure;
- Predisposition to bleeding from mucous membranes and skin;
- History of manic conditions;
- Initially low body weight.
Women of childbearing age should use reliable methods of contraception during the period of use of Velaxin. When planning or getting pregnant, you need to see your doctor.
Instructions for the use of Velaksin: method and dosage
Pills
Velaxin tablets are taken orally, preferably with meals.
The drug is recommended to be taken daily at 75 mg per day in 2 divided doses. If, after several weeks of therapy, significant improvement is not observed, a single dose can be increased to 75 mg, without changing the frequency of administration. In severe depressive disorders or other conditions requiring inpatient treatment, at the beginning of therapy, the doctor can immediately prescribe a daily dose of 150 mg in 2 divided doses, after which it can be increased every 2-3 days by 75 mg until the desired therapeutic effect is achieved.
The maximum dose of Velaxin is 375 mg per day. After achieving the desired therapeutic effect, the daily dose should be gradually reduced to the lowest effective level.
Supportive treatment can last 6 months or more. Velaxin is prescribed in the lowest effective dose used to treat depressive episodes.
In case of renal failure, depending on its severity, the following dosage regimens for Velaxin are used:
- Mild (at a glomerular filtration rate> 30 ml per minute): no dosage adjustment is required;
- Medium degree (at a glomerular filtration rate of 10-30 ml per minute): a dose reduction of 25-50% is required, while the daily dose should be taken once a day;
- Severe degree (at a glomerular filtration rate <10 ml per minute): Velaxin should not be used.
Patients on hemodialysis can receive 50% of the average daily dose of venlafaxine after the session ends.
In liver failure, depending on its severity, the following dosage regimens are used:
- Mild (with prothrombin time less than 14 seconds): no dosage adjustment is required;
- Moderate degree (with a prothrombin time of 14-18 seconds): a dose reduction of 50% is required;
- Severe degree: Velaxin should not be used.
Elderly patients should be treated with caution, which is associated with the likelihood of functional renal impairment. The lowest effective dose is usually prescribed. When the dose is increased, the patient should be under close medical supervision.
After the end of treatment, the dose of Velaxin must be reduced gradually, at least over 7 days. At this time, it is necessary to monitor the patient's condition in order to minimize the risk associated with drug withdrawal.
The period that is necessary to completely stop taking Velaxin is determined by the size of the dose taken, the duration of the course of therapy and the individual characteristics of the patient.
Sustained-release capsules
Velaxin capsules are taken orally, whole (they cannot be crushed, divided, placed in water or chewed), washed down with a liquid, preferably during meals.
The daily dose should be taken in 1 dose, preferably at the same time of the day (morning or evening).
The recommended starting dose for Velaxin is 75 mg per day. For severe depressive disorders or other conditions requiring hospital treatment, the doctor may immediately prescribe 150 mg per day, after which the dose can be increased at intervals of 14 days or more (but not more often than after 4 days) by 75 mg until the required therapeutic effect.
The maximum dose of Velaxin is 350 mg per day. After achieving the desired therapeutic effect, the daily dose can be gradually reduced to the minimum effective level.
For the treatment of depression, the drug should be used for at least 6 months. With stabilizing therapy and for the prevention of relapses or new episodes of depression, Velaxin is prescribed in doses that have demonstrated their effectiveness. The doctor should regularly, at least once every 3 months, monitor the effectiveness of the treatment.
Patients taking Velaxin in the form of tablets can be transferred to taking the drug in the form of prolonged-release capsules with the appointment of an equivalent dose once a day. However, in some cases, individual dose adjustment may be required.
The dosage regimen of the drug in the form of prolonged-release capsules for renal or hepatic insufficiency, as well as the recommendations regarding the use of Velaxin by elderly patients and the cancellation of therapy, correspond to those when prescribing the tablet form of the drug.
Side effects
Most of the side effects during the use of Velaxin depend on the dose. With prolonged therapy, the frequency and severity of most of them decreases, while the need to cancel therapy does not arise.
During treatment, the following disorders can be observed (1/100 - often, 1/1000 - infrequently, 1/10 000 - rarely, <1/10 000 - very rarely):
- Cardiovascular system: dilated blood vessels (hot flushes), arterial hypertension, heart palpitations; infrequently - fainting, orthostatic hypotension, tachycardia; very rarely - lengthening of the QT interval, arrhythmia of the "pirouette" type, ventricular fibrillation, ventricular tachycardia;
- Central and peripheral nervous system: often - dizziness, headache, agitation, insomnia, drowsiness, anxiety, unusual dreams, confusion, increased muscle tone, paresthesia, tremor; infrequently - hallucinations, apathy, myoclonus; rarely - speech disorders, ataxia, hypomania or mania, serotonergic syndrome, symptoms resembling neuroleptic malignant syndrome, seizures; very rarely - delirium, extrapyramidal disorders (including dystonia, dyskinesia, tardive dyskinesia), akathisia / psychomotor agitation;
- Hematopoietic system: infrequently - hemorrhages in the skin (ecchymosis) and mucous membranes; rarely - prolongation of bleeding time, thrombocytopenia; very rarely - aplastic anemia, agranulocytosis, pancytopenia, neutropenia;
- Urinary system: infrequently - urinary retention;
- Digestive system: decreased appetite, dry mouth, constipation, vomiting, nausea, abdominal pain; infrequently - a reversible increase in the activity of liver enzymes, bruxism; rarely - gastrointestinal bleeding; very rarely - hepatitis;
- Musculoskeletal system: myalgia, arthralgia; infrequently - muscle spasm; very rarely - rhabdomyolysis;
- Reproductive system: erectile dysfunction, ejaculation, anorgasmia; infrequently - menorrhagia, menstrual irregularities, decreased libido; rarely galactorrhea;
- Metabolism: weight loss, increased serum cholesterol levels; infrequently - impaired liver function tests, hyponatremia, syndrome of insufficient secretion of antidiuretic hormone; very rarely - an increase in the level of prolactin;
- Sense organs: mydriasis, accommodation disturbances, tinnitus, visual disturbances; infrequently - a violation of taste;
- Allergic reactions: rash, itchy skin; infrequently - maculopapular rash, angioedema, urticaria; rarely - erythema multiforme, Stevens-Johnson syndrome;
- Dermatological reactions: increased sweating; infrequently - photosensitivity; rarely - alopecia;
- The body as a whole: fever, fatigue, weakness, chills.
The following side effects were noted in children during therapy: ecchymosis, refusal to eat, abdominal pain, chest pain, tachycardia, weight loss, nausea, constipation, epistaxis, mydriasis, dizziness, myalgia, emotional lability, hostility, tremor, suicidal thoughts.
After reducing the dose or abruptly canceling Velaxin, fatigue, drowsiness, headache, vomiting, nausea, anorexia, dry mouth, dizziness, diarrhea, anxiety, insomnia, nervous irritability, anxiety, disorientation, hypomania, paresthesias, sweating may develop. As a rule, these symptoms are mild and go away on their own. Because of the likelihood of these disorders, it is very important to reduce the dose of Velaxin gradually, especially after high-dose treatment.
Overdose
The main symptoms: ventricular or sinus tachycardia, ECG changes (bundle branch block, lengthening of the QT interval, expansion of the QRS complex), bradycardia, convulsive states, arterial hypotension, depression of consciousness (in the form of a decrease in the level of wakefulness). There is information about a fatal outcome due to an overdose of venlafaxine in combination with alcohol and / or other psychotropic drugs.
Therapy: symptomatic. Recommended continuous monitoring of vital functions (blood circulation and respiration), taking activated charcoal (in order to reduce the absorption of Velaxin). Due to the danger of aspiration, vomiting should not be induced.
With dialysis, venlafaxine and EFA are not excreted. No specific antidotes are known.
special instructions
Before starting therapy in patients with depressive disorders, the likelihood of suicidal attempts must be considered. To reduce the risk of overdose and / or abuse, only a small number of capsules or tablets should be given at the beginning of treatment, and the patient should be under close medical supervision.
There have been reports of aggressive behavior while taking Velaxin (especially at the beginning of treatment and after stopping therapy).
The use of Velaxin can cause psychomotor agitation, clinically resembling akathisia (anxiety with the need to move, often combined with an inability to stand or sit still). Most often, the violation is observed during the first few weeks of therapy. With the development of these symptoms, increasing the dose may not have a beneficial effect. In addition, it is necessary to consider the appropriateness of continuing treatment.
Patients with mood disorders during the use of Velaxin may experience manic or hypomanic states. Such patients should be prescribed the drug with caution, and in the course of treatment they need medical supervision. Also, caution is required by the appointment of Velaxin to patients with a history of epileptic seizures, with an increase in the frequency of epileptic seizures or their occurrence, therapy should be interrupted.
With simultaneous use with antipsychotics, symptoms that resemble neuroleptic malignant syndrome may develop (the combination requires caution).
If you develop a rash, urticaria, or other allergic reactions, see your doctor.
When carrying out electroconvulsive therapy while taking Velaxin, special care must be taken (due to the lack of experience with its use in these conditions).
In some cases, during the use of Velaxin, a dose-dependent increase in blood pressure was noted, and therefore it is recommended to regularly monitor blood pressure, especially during the period of specification or increase in the dose.
During therapy, especially in elderly patients, it is necessary to take into account the possibility of dizziness and disturbances in the sense of balance.
While taking Velaxin, orthostatic hypotension may develop.
The drug may increase the risk of bleeding into the skin and mucous membranes. During treatment, patients with a predisposition to such conditions need to be careful.
The safety and efficacy of Velaxin with drugs that reduce body weight, including phentermine, have not been established, therefore their combined use (as well as the use of venlafaxine for weight loss as monotherapy) is not recommended.
With prolonged therapy, it is advisable to control serum cholesterol levels.
After stopping treatment, especially abruptly, withdrawal symptoms may occur. The risk of their development depends on several factors, including the duration of the course and the dose, as well as the rate of dose reduction. Withdrawal symptoms include dizziness, sensory disturbances (including paresthesia), sleep disturbances (including insomnia and unusual dreams), agitation or anxiety, nausea and / or vomiting, tremors, sweating, headache, diarrhea, rapid and rapid heart rate, and emotional lability … These symptoms are usually mild to mild, but in some people they can be severe. As a rule, they are observed in the first days after the discontinuation of Velaxin, although in some cases they develop even if the dose is accidentally skipped. Most often, these phenomena go away on their own within 14 days,but in some patients they may be longer (2-3 months or longer).
Influence on the ability to drive vehicles and complex mechanisms
During therapy, care must be taken when driving vehicles and performing work that requires increased attention and fast psychomotor reactions, this is due to the likelihood of a deterioration in thought processes and a decrease in the ability to perform motor functions. With the development of such violations, the duration and degree of restrictions are established by the doctor.
Application during pregnancy and lactation
Velaxin is not prescribed during pregnancy / lactation.
Carrying out therapy during the period of established or suspected pregnancy is possible only if the potential benefit is assessed above the possible harm. If the mother stopped taking Velaxin shortly before delivery, the newborn may experience withdrawal symptoms.
Pediatric use
Velaxin therapy is contraindicated in patients under 18 years of age.
With impaired renal function
Velaxin is contraindicated for severe renal impairment.
With a mild severity, the dosage regimen is not adjusted, with a moderate severity, the dose is reduced by 25-50%, taking Velaxin 1 time per day.
For violations of liver function
Velaxin is contraindicated in severe hepatic impairment.
With mild severity, the dosage regimen is not adjusted, with moderate severity, the dose is reduced by 50%.
Use in the elderly
Elderly patients need to be careful during drug therapy, as they have an increased likelihood of impaired renal function.
Drug interactions
The combined use of Velaxin with monoamine oxidase (MAO) inhibitors is contraindicated. You can start drug therapy no earlier than 14 days after the end of the use of MAO inhibitors. If moclobemide (a reversible MAO inhibitor) was used, this break may be shorter (24 hours). Treatment with MAO inhibitors can be started no earlier than 7 days after discontinuation of Velaxin.
Drinking alcohol during therapy is not recommended.
When combined with drugs that are inhibitors of CYP2D6 and CYP3A4 enzymes, care must be taken.
With the simultaneous use of Velaxin with some drugs, the following effects may occur:
- Lithium: increasing its level;
- Haloperidol: an increase in its effects, which is associated with an increase in its concentration in the blood;
- Clozapine: the development of side effects (for example, epileptic seizures) and an increase in its level in blood plasma;
- Anticoagulants: enhancing their effect.
Analogs
Analogues of Velaxin are: Alventa, Velafax, Velafax MV, Venlafaxine, Venlaxor, Venlift OD, Newvelong, Efektin depot.
Terms and conditions of storage
Store in a dry place out of reach of children at temperatures up to 30 ° C.
Shelf life:
- Tablets - 5 years;
- Sustained-release capsules - 4 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Velaxin
Many reviews of Velaxin testify to its high effectiveness. The development of side effects is often indicated. It is also noted that the drug has a high cost and can be addictive with prolonged use.
The price of Velaksin in pharmacies
The approximate price for Velaksin is: tablets (28 pcs. 37.5 or 75 mg each) - 701–798 rubles. or 885–1149 rubles, capsules (28 pieces, 75 or 150 mg each) - 1065–1206 rubles. or 1460-1888 rubles.
Velaxin: prices in online pharmacies
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Drug name Price Pharmacy |
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Velaxin 75 mg sustained release capsules 28 pcs. 1105 RUB Buy |
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Velaxin capsules prolong 75mg 28 pcs. 1289 RUB Buy |
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Velaxin 150 mg sustained release capsules 28 pcs. 1760 RUB Buy |
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Velaxin capsules prolong 150mg 28 pcs. 1812 RUB Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, 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!
