- done All payments are SSL encrypted
- done Full Refund if you haven't received your order
- done International shipping to the USA, UK and Europe
Venlafaxine - an antidepressant chemically not related to any class of antidepressants (tricyclic, tetracyclic, or others), is the racemate of two active enantiomers. Venlafaxine and its main metabolite, O-desmethylvenlafaxine (EFA), are potent inhibitors of serotonin reuptake and norepinephrine (abbreviated IOSPN or SSRI) and are weak dopamine reuptake inhibitors.
The mechanism of antidepressant action is associated with the ability of the drug to enhance the activity of neurotransmitters during the transmission of nerve impulses in the central nervous system (CNS). Venlafaxine and EFA equally effectively affect the reuptake of the above-mentioned neurotransmitters, and they do not have affinity (studied in vitro) with cholinergic (muscarinic), histamine (H1alpha1-adrenergic, opioid and benzodiazepine receptors, do not inhibit the activity of monoamine oxidase (MAO). By inhibition of serotonin reuptake, venlafaxine is inferior to selective serotonin reuptake inhibitors (SSRIs).
Depression. Prevention and treatment.
One tablet contains:
Active ingredient: venlafaxine hydrochloride - 84.84 mg, which corresponds to 75 mg of venlafaxine;
Excipients: microcrystalline cellulose 134.62 mg, pregelatinized starch 99.00 mg, colloidal silicon dioxide (aerosil) 1.64 mg, talc 6.60 mg, magnesium stearate 3.30 mg.
Venlafaxine is marketed under different brands and generic names, and comes in different dosage forms:
|Brand name||Manufacturer||Country||Dosage form|
No customer reviews for the moment.
Dosage and Administration
Velafax pills are recommended to be taken orally, during a meal, preferably at the same time, without chewing and squeezing fluid.
For treatment of depressions, the recommended initial dose is 37.5 mg 2 times / day, daily. If after several weeks of treatment there is no significant improvement, the dose can be increased to 150 mg / day - 75 mg 2 times / day.
If necessary, the use of the drug in a higher dose in severe depressive disorder or other conditions requiring inpatient treatment, you can immediately appoint 75 mg 2 times / day. After that, the daily dose can be increased by 75 mg every 2-3 days until the desired therapeutic effect is achieved. The maximum daily dose of the drug Velafax is 375 mg. After achieving the desired therapeutic effect, the daily dose can be gradually reduced to the minimum effective level. Supportive therapy and prevention of relapse continues for 6 months or more. The drug is prescribed in the minimum effective dose used in the treatment of a depressive episode.
Most of the side effects listed below are dose dependent. With prolonged treatment, the severity and frequency of most of these effects is reduced, and there is no need to cancel therapy.
Frequency of side effects: very often (≥10%), often (≥1%, but
On the part of the digestive system: often - loss of appetite, constipation, nausea, vomiting, dry mouth, dyspepsia, abdominal pain; infrequently - bruxism, increased activity of hepatic transaminases; rarely, hepatitis; in some cases, pancreatitis.
On the part of the metabolism: often - an increase in serum cholesterol level (especially after long-term intake or administration of the drug in high doses), a decrease or increase in body weight; infrequently - hyponatremia, syndrome of insufficient secretion of antidiuretic hormone (ADH); in some cases - an increase in the level of prolactin in blood plasma.
Since the cardiovascular system: often - increased blood pressure, redness of the skin; infrequently - decrease in blood pressure, postural hypotension, syncope, arrhythmia, tachycardia; very rarely - pirouette-type arrhythmia, prolongation of the QT interval, ventricular tachycardia, ventricular fibrillation.
On the part of the central nervous system and peripheral nervous system: often - dizziness, asthenia, nightmares, weakness, dizziness, insomnia, drowsiness, increased nervous irritability, paresthesias, stupor, muscle hypertonia, tremor, yawning, sedation; infrequently - apathy, hallucinations, myoclonus, syncope; seldom - convulsions, ataxia with impaired balance and coordination of movement, impaired speech, mania or hypomania, serotonin syndrome, symptoms resembling malignant neuroleptic syndrome, epileptic seizures; in some cases - delirium, extrapyramidal disorders, incl. dyskinesia and dystonia, tardive dyskinesia, psychomotor anxiety / akathisia.
From the side of mental status: frequency not established - depression, the appearance of suicidal thoughts and suicidal behavior during therapy and after discontinuation of the drug.
On the part of the hematopoietic system and the lymphatic system: infrequently - hemorrhages into the skin (ecchymosis) and mucous membranes, thrombocytopenia, prolonged bleeding time, hemorrhagic syndrome; in some cases - agranulocytosis, aplastic anemia, neutropenia and pancytopenia.
From the urinary system: often - urination disorders; infrequently - urinary retention.
On the part of the reproductive system: often - decreased libido, erectile dysfunction and / or ejaculation, anorgasmia in men, menorrhagia; infrequently - violation of the menstrual cycle, anorgasmia in women.
On the part of the senses: often - accommodation disturbances, mydriasis, visual disturbances, noise or tinnitus; infrequently - violations of taste sensations.
On the part of the skin and its appendages: often - excessive sweating (including night); infrequently - alopecia.
On the part of the respiratory system: infrequently - shortness of breath; in some cases - pulmonary eosinophilia.
On the part of the endocrine system: rarely - galactorrhea; in some cases - increased levels of prolactin.
Allergic reactions: infrequently - skin rash (including maculo-papular), pruritus, photosensitization, angioedema, urticaria; rarely erythema multiforme exudative, Stevens-Johnson syndrome; in some cases - anaphylactic reactions.
From the musculoskeletal system: often - arthralgia, myalgia; infrequently - muscle spasms; in some cases - rhabdomyolysis.
After abrupt cancellation of venlafaxine or dose reduction, increased fatigue, drowsiness, asthenia, headache, nausea, vomiting, anorexia, dry mouth, dizziness, diarrhea, insomnia, unusual dreams, difficulty falling asleep, anxiety, anxiety, irritability and emotional lability, anatomy, difficulty in falling asleep, anxiety, anxiety, irritability and emotional lability, anesthesia, difficulty falling asleep, anxiety, anxiety, irritability and emotional lability, math , confusion, disorientation, hypomania, tremor, paresthesias, excessive sweating, tachycardia, convulsions, ringing or tinnitus, refusal of food. To prevent the development of symptoms of withdrawal syndrome, it is very important to gradually reduce the dose of the drug, especially after taking it in high doses.
- pronounced impaired renal function (CC less than 10 ml / min) and / or liver;
- children's and teenage age up to 18 years;
- lactation period (breastfeeding);
- simultaneous administration of MAO inhibitors;
- individual intolerance to venlafaxine and other components of the drug.
Precautions to apply in case of recent myocardial infarction, unstable angina, hypertension, tachycardia, convulsive syndrome history, elevated intraocular pressure, angle-closure glaucoma, manic state history, hyponatremia, hypovolemia, dehydration, simultaneous administration of diuretics, suicidal tendencies, predisposition to bleeding (on the part of the skin and mucous membranes), with initially reduced body weight.
The simultaneous use of MAO inhibitors and venlafaxine contraindicated. Reception venlafaksina can begin no earlier than 14 days after the end of therapy with MAO inhibitors. If a reversible MAO inhibitor (moccobemide) was used, this interval may be shorter (24 hours). Therapy with MAO inhibitors can be started no earlier than 7 days after the abolition of venlafaxine.
With simultaneous use of venlafaxine with lithium preparations may increase the level of lithium in the blood.
When applied simultaneously with imipramine, the pharmacokinetics of venlafaxine and its EFA metabolite do not change. Venlafaxine does not affect the metabolism of imipramine and its metabolite 2-hydroxyimipramine, however, it increases the value of AUC and Cmax in the plasma of desipramine (the main metabolite of imipramine), and also reduces the renal clearance of 2-hydroxydesipramine. The clinical significance of this phenomenon is unknown.
With simultaneous use with neuroleptics, the appearance of symptoms resembling a malignant neuroleptic syndrome may occur.
Venlafaxine reduces the renal clearance of haloperidol by 42%, while the AUC and Cmax values increase by 70% and 88%, respectively. Haloperidol effects may be enhanced.
With simultaneous use with diazepam pharmacokinetics of drugs and their major metabolites are not significantly changed.
With simultaneous use with clozapine, an increase in its blood plasma level and the development of side effects (for example, epileptic seizures) can be observed.
With simultaneous use with risperidone, despite an increase in the AUC of the drug, the pharmacokinetics of the sum of the active components (risperidone and its active metabolite) did not change significantly.
The simultaneous use of ethanol and venlafaxine was not accompanied by a decrease in mental and physical activity. Despite this (as in the case of taking other drugs that affect the central nervous system), ethanol use is not recommended during venlafaxine therapy.
Cimetidine inhibits venlafaxine metabolism during the "first pass" through the liver and has no effect on the pharmacokinetics of EFA. In the majority of patients, only a slight increase in the total pharmacological activity of venlafaxine and EFA is expected (more pronounced in elderly patients and in impaired liver function). In elderly patients and in patients with impaired liver function, simultaneous use of cimetidine and venlafaxine should be carried out under medical supervision.
No clinically significant interaction of venlafaxine with antihypertensive drugs (including beta-blockers, ACE inhibitors and diuretics) and hypoglycemic drugs was detected.
Since the binding of plasma proteins venlafaxine and EFA is respectively 27% and 30%, drug interactions due to the competitive release of other drugs from plasma proteins are not expected.
Venlafaxine metabolism occurs with the participation of the cytochrome P450 system, CYP2D6 and CYP3A4 isoenzymes. Taking the drug with CYP2D6 isoenzyme inhibitors or patients with a genetically determined decrease in the activity of the CYP2D6 isoenzyme was not accompanied by significant changes in the concentration of the active substance and metabolite (venlafaxine and EFA), which allows not to reduce the dose of antidepressant. However, simultaneous administration with CYP3A4 isoenzyme inhibitors is accompanied by an increase in plasma venlafaxine concentration. Therefore, special care should be taken when prescribing venlafaxine with drugs that are inhibitors of the CYP3A4 isoenzyme (ketoconazole, erythromycin) or both isoenzymes (CYP2D6 and CYP3A4).
Venlafaxine is a relatively weak inhibitor of the isoenzyme CYP2D6 and does not inhibit the activity of the isoenzymes CYP1A2, CYP2C9 and CYP3A4. In vivo studies did not reveal the effect of venlafaxine on the metabolism of alprazolam (CYP3A4 isoenzyme), caffeine (CYP1A2 isoenzyme), carbamazepine (CYP3A4 isoenzyme) and diazepam (CYP3A4 and CYP2C19 isoenzymes).
With simultaneous use with warfarin, it is possible to enhance the anticoagulant effect of the latter, while the prothrombin time, expressed through MHO, is prolonged.
When taken simultaneously with indinavir, there is a decrease in the AUC value of indinavir by 28% and a decrease in its plasma Cmax by 36%, while the pharmacokinetic parameters of venlafaxine and EFA do not change. The clinical significance of this effect is unknown.
Venlafaxine can affect the pharmacodynamics of other drugs acting at the level of the serotonergic neurotransmitter system, so care should be taken when it is given simultaneously with triptans, other selective serotonin reuptake inhibitors and lithium drugs.
Pregnancy and Lactation
During pregnancy (including before childbirth), venlafaxine is contraindicated, because the safety of its use during this period is not defined.
Venlafaxine and the EFA metabolite are excreted in breast milk. The safety of these substances for newborns is not proven, so if you need to take the drug during lactation should stop breastfeeding for the duration of treatment.
When depression increases the risk of suicidal thoughts and suicidal attempts. This risk persists until the onset of persistent remission. Because improvement may not occur within the first few weeks of treatment or more, patients should be kept under constant medical supervision for this entire period until a lasting improvement occurs.The risk of suicidal attempts is highest immediately after the start of the drug, but also increases again in the early stages of recovery. Velafax should not be used in the treatment of children and adolescents under 18 years of age. In patients with a history of suicidal behavior, or a tendency to the occurrence of suicidal thoughts before the start of treatment, as well as in young adult patients, the risk of suicidal thoughts or suicide attempts is highest. In placebo-controlled clinical trials of antidepressants in adult patients with mental disorders, an increased likelihood of suicidal behavior (suicide attempt and suicidal thoughts) in people under 25 years of age who receive antidepressants, including venlafaxine, is shown.
Patients and people caring for patients should be warned about the need to monitor the occurrence of suicidal thoughts and immediately seek medical attention in case of symptoms.
As with other antidepressants, abrupt cessation of venlafaxine therapy — especially after high doses of the drug — can cause symptoms of withdrawal syndrome, and therefore it is recommended to gradually reduce the dose of the drug before discontinuing the drug. The risk of withdrawal symptoms depends on the dose, the duration of therapy, as well as the patient's individual sensitivity. Patients with affective disorders in the treatment of antidepressants (including venlafaxine) may experience hypomania or manic states. Velafax (as well as other antidepressants) should be prescribed with caution to patients with a history of mania (such patients need medical supervision).
Like other antidepressants, venlafaxine should be administered with caution to patients with a history of epileptic seizures. Treatment with venlafaxine should be interrupted when epileptic seizures occur. The drug should not be prescribed to patients with uncontrolled epilepsy, and patients with controlled epilepsy need careful observation.
The use of venlafaxine may be associated with the development of psychomotor anxiety, which clinically resembles akathisia and is characterized by subjectively unpleasant and distressing anxiety with the need to move, often in combination with the inability to sit or stand still. This condition is most often observed during the first few weeks of treatment. If such symptoms occur, increasing the dose may have an adverse effect, and consider the appropriateness of continuing to take venlafaxine.
Patients should be warned of the need to immediately consult a doctor if a rash, urticaria or other allergic reactions occur.
In some patients, while taking venlafaxine, a dose-dependent increase in blood pressure has been noted, therefore, regular monitoring of blood pressure is recommended, especially during the selection or dose increase period.
On the background of drug treatment, an increase in heart rate is possible, especially while taking in high doses. Caution must be exercised when using the drug in patients with a tendency to tachycardia.
Patients, especially the elderly, should be warned about the possibility of dizziness and imbalance (orthostatic hypotension).
In patients taking venlafaxine, changes in ECG parameters were rarely observed (prolongation of the PR interval, expansion of the QRS complex, prolongation of the QT interval).
Caution should be given to venlafaxine in patients who have recently had a myocardial infarction and with unstable angina, since the safety of the drug in this category of patients has not been studied.
Like other serotonin reuptake inhibitors, venlafaxine may increase the risk of hemorrhages in the skin and mucous membranes.At treatment of the patients predisposed to such states care is necessary.
While taking venlafaxine, especially in conditions of dehydration or reduction in circulating blood volume (including in elderly patients and patients taking diuretics), hyponatremia and / or syndrome of insufficient secretion of antidiuretic hormone can be observed.
While taking the drug, mydriasis can be observed, and therefore it is recommended that intraocular pressure be monitored in patients prone to elevation or with angle-closure glaucoma.
It is not recommended to combine venlafaxine with weight-reducing agents (including phentermine), due to the lack of data on efficacy and safety.
Conducted to date, clinical studies have not revealed tolerance to venlafaxine or dependence on it. Despite this, the physician should establish careful monitoring of patients to identify signs of drug abuse (as with other drugs acting on the central nervous system). Patients with a history of indications of drug dependence need special monitoring.
When venlafaxine is used for a long period of time, control of serum cholesterol level is required.
Precautions should be prescribed the drug in violation of the liver or kidneys. Sometimes it may require a dose reduction.
When taking venlafaxine, special care should be taken when conducting electroconvulsive therapy, since experience with venlafaxine in these conditions is missing.
During treatment, alcohol is not recommended.
Influence on ability to drive motor transport and control mechanisms
Venlafaxine has virtually no effect on psychomotor and cognitive functions. However, given the possibility of significant side effects from the CNS, during the period of treatment with venlafaxine, care must be taken when driving vehicles and engaging in potentially hazardous activities that require increased concentration and psychomotor speed.
Symptoms (often occur while taking ethanol): dizziness, decrease in blood pressure, ECG changes (prolongation of the QT interval, blockade of the bundle of the His bundle, expansion of the QRS complex), sinus and ventricular tachycardia or bradycardia, disturbances of consciousness (from drowsiness to coma), convulsions death
Treatment: conduct symptomatic therapy, under continuous monitoring of the ECG and functions of vital organs. Do not induce vomiting due to the risk of aspiration. It is recommended to provide airway patency, adequate pulmonary ventilation and oxygenation. Hemodialysis is ineffective because venlafaxine and EFA are not displayed during dialysis. Specific antidotes are unknown.
- Brand name: Venlafaxine
- Active ingredient: Venlafaxine
- Dosage form: Pills
- Manufacturer: Alsi Pharma
- Country of Origin: Russia
Studies and clinical trials of Venlafaxine (Click to expand)
- Venlafaxine: Discrepancy between in vivo 5-HT and NE reuptake blockade and affinity for reuptake sites
- Is There an Advantage to Venlafaxine in Comparison with Other Antidepressants?
- Urinary retention with venlafaxine-fluoxetine combination
- Venlafaxine. Pharmacology and therapeutic potential in the treatment of depression
- Effects of venlafaxine given repeatedly on α1-adrenergic, dopaminergic and serotonergic receptors in rat brain
- The synthesis of [o-methyl-11C]venlafaxine: A non-classical, fast-acting antidepressant
- New antidepressants and the cytochrome P450 system: Focus on venlafaxine, nefazodone, and mirtazapine
- Use of bupropion with SRIs and venlafaxine
- Relationship between clinical effects, serum drug concentration, and concurrent drug interactions in depressed patients treated with citalopram, fluoxetine, clomipramine, paroxetine or venlafaxine
- More than one-half of a decade of experience with venlafaxine dual serotonin-norepinephrine reuptake inhibitor
- Pharmacoeconomic studies of antidepressants: Focus on venlafaxine
- Neuropharmacology of venlafaxine
- Review of the pharmacokinetics, pharmacogenetics, and drug interaction potential of antidepressants: Focus on venlafaxine
- Antidepressant efficacy of venlafaxine
- Efficacy of venlafaxine in the treatment of severe depression
- Venlafaxine and treatment-resistant depression
- Efficacy of venlafaxine in geriatric depression
- Efficacy of venlafaxine in mixed depression-anxiety states
- Efficacy, safety, and tolerability of venlafaxine XR in generalized anxiety disorder
- Use of venlafaxine in children and adolescents: A review of current literature
- Use of venlafaxine other psychiatric disorders
- Nonaqueous capillary electrophoresis-mass spectrometry for separation of venlafaxine and its phase I metabolites
- Preparation and characterization of venlafaxine hydrochloride-loaded chitosan nanoparticles and in vitro release of drug
- Induction of drug efflux protein expression by venlafaxine but not desvenlafaxine