Velafax

Velafax is an antidepressant drug.

Indications Velafax

It is used to eliminate depressions of various origins, as well as anxiety disorders of a generalized and social nature.

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Release form

The release occurs in capsules, 10 pieces inside a blister pack. In a pack - 3 such blisters. Also in a blister plate there can be 14 capsules - in this case there will be 2 blister packs in the box.

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Pharmacodynamics

The chemical basis of this drug cannot be classified into any of the currently known categories of antidepressants.

The drug's effect is due to the potentiation of neurotransmitter activity within the nervous system. The substance is a powerful SSRI/SNRI.

Venlafaxine and its metabolite weakly block dopamine reuptake. These elements have similar efficacy in influencing the processes of neurotransmitter reuptake, and also suppress β-adrenergic manifestations.

Pharmacokinetics

The absorption rate of the active ingredient when using a single dose of the drug is 92%. The bioavailability level is 45%.

When administered orally, peak plasma levels of the active ingredient and its metabolite are observed after approximately 6 and 8 hours, respectively. The absorption rate is slower than the elimination rate. The half-life of the active ingredient is approximately 15 hours.

The level of plasma synthesis of venlafaxine with proteins is 27%, and its metabolic product is 30%. Taking the drug with food does not change the Cmax level and absorption indices.

The active element with its decay products is excreted mainly by the kidneys. A small insoluble particle of the capsular microspheres is excreted with the feces.

In case of kidney/liver failure the half-life is prolonged.

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Dosing and administration

The drug must be taken with food, washing down the capsules with plain water. It is forbidden to chew, crush or dissolve the medicine. The entire daily dose is taken at one time, in the morning or in the evening. The intake should be done daily at the same time of day.

To eliminate depression, you need to take 75 mg of the drug per day.

If higher doses are required, start with a 150 mg dose. The daily dose is increased by 37.5-75 mg at intervals of at least 2 weeks. Doctors recommend taking a maximum of 225 mg of the drug for moderate depression. If depression is severe, 350 mg of Velafax should be taken. Once the desired result is achieved, the dose should be gradually reduced to the minimum effective dose in any case. It should be taken into account that the higher the dose, the higher the risk of side effects.

Acute depressive episodes require treatment for at least 6 months.

The doses used to prevent relapse are similar to those used to treat patients with primary attacks. The patient must be examined at least once every 3 months to assess the effectiveness of the therapy.

If there are anxiety disorders of a social or generalized nature, it is necessary to use 75 mg of the substance once a day. After a maximum of 2 weeks, an improvement in the condition should be observed. If there is no effect, it is necessary to increase the portion to 150 mg.

For people with renal insufficiency with a glomerular filtration rate of 10-30 ml/minute, the dose should be reduced by half. If the glomerular filtration rate is less than 10 ml/minute, it is not advisable to take the drug, because there is not enough information on the treatment of this group of patients.

In case of moderate liver failure, it is recommended to reduce the dose of the drug by half. If the doses taken are increased, it is necessary for the patient to remain under constant medical supervision.

The drug is prescribed to elderly people with caution. The portion size should remain within the minimum effective limits. If the dose is increased, the patient's condition must be constantly monitored by doctors.

When using the drug in large portions for 1.5 months, it is recommended to reduce the dosage gradually, doing this over a period of at least 2 weeks. The total duration of the period during which the portion is reduced is selected individually.

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Use Velafax during pregnancy

It is prohibited to prescribe Velafax to pregnant women.

Contraindications

Among the contraindications:

• severe liver/kidney dysfunction;
• lactation period;
• the presence of intolerance to the components of the drug;
• age under 18 years.

Caution is required when using:

• people who have recently suffered a myocardial infarction;
• persons with high blood pressure;
• patients with a history of seizures;
• people with closed-angle glaucoma;
• people with a predisposition to the development of bleeding in the mucous membranes and skin;
• patients with unstable tachycardia or angina;
• patients with increased IOP levels;
• persons with a history of manic states;
• patients with low weight.

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Side effects Velafax

For the most part, the side effects of the drug are determined by the dosage. In the case of a long-term therapeutic course, the frequency and severity of most of them decreases. There is no need to cancel the therapy.

The use of Velafax may provoke the appearance of such negative consequences:

• feeling of weakness, chills, headaches, increased fatigue, abdominal pain and increased temperature;
• CNS symptoms: a feeling of intense excitement, as well as anxiety, confusion and drowsiness. Dizziness, apathy, paresthesia, insomnia, strange dreams, hallucinations and myoclonus also occur. Increased muscle tone may be observed;
• disturbances in the functioning of the sense organs: visual and taste disturbances, sensation of tinnitus, accommodation disorder, and mydriasis;
• skin symptoms: rashes, photosensitivity, hyperhidrosis, itching, angioedema, maculopapular rash and urticaria;
• metabolic disorders: increased serum cholesterol levels, development of hyponatremia, weight loss, problems with laboratory tests regarding liver function, and also the syndrome of insufficient secretion of the ADH element;
• problems with the gastrointestinal tract: nausea, constipation, dulling of the feeling of hunger, vomiting, treatable increase in the activity of liver enzymes, and in addition, bruxism;
• dysfunction of the cardiovascular system: increased heart rate, tachycardia, increased blood pressure, dilation of blood vessels, fainting, and orthostatic collapse;
• disorders in the functioning of the hematopoietic system: the appearance of hemorrhages in the mucous membranes and skin;
• lesions of the urogenital system: development of anorgasmia, ejaculation or erectile dysfunction, as well as menorrhagia, as well as decreased libido, urinary retention and menstrual irregularities;
• problems with the function of the musculoskeletal system: the occurrence of muscle spasms, the development of myalgia or arthralgia.

The following symptoms are occasionally observed:

• development of hypomania, pancreatitis, speech disorders, mania, ataxia, bleeding in the gastrointestinal tract, and also seizures;
• reactions similar to neuroleptic syndrome of malignant nature;
• development of extrapyramidal disorders, serotonergic syndrome, delirium, late-stage dyskinesia, and also akathisia or psychomotor agitation;
• prolongation of the QT interval, arrhythmia, and, in addition, cardiac fibrillation are possible;
• an extension of the bleeding period, the development of neutro-, thrombocyto- or pancytopenia, as well as aplastic anemia and agranulocytosis are noted;
• the appearance of erythema multiforme, Stevens-Johnson syndrome, and alopecia;
• hepatitis, rhabdomyolysis or galactorrhea may develop, and in addition, prolactin levels may increase.

If the drug is stopped too abruptly or the dose is reduced abruptly, vomiting, a feeling of intense anxiety or extreme fatigue, headaches, diarrhea, dry mouth, a feeling of drowsiness or disorientation may occur. Dizziness, paresthesia, anorexia, hyperhidrosis, nausea, hypomania, insomnia, and a feeling of anxiety may occur.

Due to the risk of such complications, it is necessary to reduce the dose of the drug gradually. The duration of the period during which the dosage is reduced is determined by individual characteristics: the characteristics of the pathology, the dose size of the drug, and also the duration of the course of treatment.

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Overdose

Possible signs of intoxication include: development of bradycardia and changes in consciousness or ECG readings, occurrence of ventricular or sinus tachycardia and seizures, and also a decrease in blood pressure. There is also evidence of a fatal outcome.

Symptomatic measures are taken. The drug has no specific antidote. It is necessary to constantly monitor and support vital body functions. Sometimes activated carbon may be prescribed to slow down the absorption of the drug. Vomiting should not be induced. Dialysis will be ineffective.

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Interactions with other drugs

It is prohibited to combine the medication with MAOIs. After completing the course of their use, a break of at least 14 days is required. If reversible MAOIs were used, this period may be shortened to 1 day. At the same time, after completing therapy with Velafax, you can start using MAOIs after at least 7 days have passed.

Combination with lithium leads to an increase in its indicators.

The combination with imipramine causes potentiation of the properties of its main metabolic products – desipramine with 2-OH-imipramine.

Simultaneous administration with haloperidol increases its levels in the blood and, in addition, potentiates its effect.

Use together with clozapine may cause an increase in its plasma values and the development of negative side effects.

During therapy with Velafax, it is forbidden to drink alcoholic beverages. There is information about fatal outcomes in case of using the drug in combination with alcohol or other psychotropic drugs.

Caution is required when combining with drugs that inhibit the activity of CYP2D6 and CYP3A4 enzymes.

Concomitant use with warfarin may enhance its anticoagulant properties.

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Storage conditions

Velafax should be kept in a place closed to children and moisture penetration. The temperature level should not exceed 30°C.

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Shelf life

Velafax is approved for use for 5 years from the date of manufacture of the drug.

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Reviews

Velafax is now quite often discussed on medical forums. Many patients indicate in their reviews the development of side effects after using the drug. In particular, there are many complaints about the development of withdrawal syndrome, as well as addiction. Almost all comments indicate that it is extremely difficult to reduce the dose of the drug.

Complications such as seizures, drowsiness, weakness, confusion, insomnia, depression and mental disorder are often reported. Some reviews indicate that negative symptoms persisted after the end of the course.

But the reviews of doctors about the drug are mostly positive. Some doctors still claim that the drug is completely safe, and getting into psychological and physical dependence is possible only in case of abuse.

Most patients disagree with this statement. They insist that the medication was taken in full compliance with the instructions, but side effects still occurred. More than 2,000 patients even signed a petition addressed to the manufacturer. Its text indicates that the use of the drug causes the development of severe side effects, including at the stage of drug withdrawal.

People who have taken the drug and become addicted to it or have experienced complications say that the risk of using the drug is much higher than is claimed in the medical community.