Venlaksor user's manual
Venlaxor is an antidepressant.
Form of issue and composition
Venlaxor is available in tablets, in dosages of 37.5 mg and 75 mg. Tablets in blisters with instructions are placed in cardboard packaging (30 tablets per pack).
The main active ingredient is venlafaxine hydrochloride.
Auxiliary components: anhydrous calcium hydrogen phosphate, anhydrous lactose, sodium carboxymethyl starch, magnesium stearate, colloidal anhydrous silica, red iron oxide dye.
Pharmacodynamics. Venlafaxine is an antidepressant. The chemical structure of the compound can not be attributed to any other group of antidepressants (tricyclic, tetracyclic, etc.).
The mechanism of action of venlafaxine is based on the ability to potentiate the transmission of a nerve impulse. Venlafaxine and its active metabolite have a pronounced inhibitory effect on the reuptake of serotonin and norepinephrine and a weak inhibitory effect on the mechanism of dopamine reuptake. Also, the active substance and active metabolite reduce the activity of β-adrenergic receptors (both after a single dose and after prolonged therapy).
Venlafaxine has no affinity for M-cholinergic receptors, H-1 histamine and α-1 adrenergic receptors. The drug does not inhibit MAO activity. Does not interact with opioid, phencyclidine, benzodiazepine and NMDA receptors.
Pharmacokinetics. Venlafaxine is well absorbed from the digestive tract. In the liver, the drug undergoes active metabolism: it is split into active metabolite (EFA) and inactive compounds.
2.4 hours after taking the tablets, the maximum concentration of venlafaxine in the blood plasma is reached. The maximum plasma concentration of the active metabolite (O-desmethylvenlafaxine or EFA) is noted 4.3 hours after the application of the tablets. If the drug is taken with food, then the maximum plasma concentration is set for 20-30 minutes faster. The maximum concentration and absorption are not affected.
With repeated use of the drug, a stable concentration of the active substance and EFA is achieved within 3 days. With blood plasma proteins, 27% of venlafaxine and 30% of the active metabolite are bound.
Venlafaxine with metabolites is excreted by the kidneys. The half-life is 5 hours (for venlafaxine) and 11 hours (for EFA). When dialysis, the active substance and metabolite are not withdrawn.
Indications for use
Venlaxor is prescribed for the treatment and prevention of depressive disorders of various origins.
Contraindications to the use of Venlaxor are:
- Severe functional impairment of kidney function;
- Severe functional impairment of liver function;
- Simultaneous treatment with MAO inhibitors;
- Age to 18 years;
- Pregnancy and the period of breastfeeding;
- Individual intolerance or hypersensitivity to the main, or one of the auxiliary components of the drug.
Dosing and Administration
Tablets should be taken with food.
The recommended initial daily dose is 75 mg of venlaxor (37, 5 mg in two divided doses). In the absence of the desired therapeutic effect after several days of the use of tablets, the dosage can be increased to 150 mg (75 mg per day).
In severe depressive disorders and conditions requiring treatment in a hospital , an initial daily dosage of 150 mg (75 mg in two divided doses) is prescribed, after which every 2-3 days the dose is increased by 75 mg until a positive therapeutic effect is achieved. The maximum permissible daily dosage of Venlaxor is 375 mg. After reaching the therapeutic effect, the doses gradually decrease to a minimum effective level.
For maintenance therapy and prevention of relapses, Venlaxor is used for a long time (6 months or more), at the lowest effective doses used during the acute stage of the disorder.
When taking Venlaxor, undesirable side effects can be noted:
- – астения, бессонница, нервная возбудимость, кошмары во сне, гипертонус мышц, парестезии, тремор, нечасто развивается апатия, галлюцинации, обморок, редко возникают маниакальные реакции, судороги ; From the side of the nervous system - asthenia, insomnia, nervous excitability, nightmares in a dream, hypertonus of muscles, paresthesia, tremor, apathy, hallucinations, fainting rarely, manic reactions, convulsions occur rarely;
- – нарушение аккомодации, мидриаз (расширение зрачка), нарушение восприятия вкуса; From the sense organs - a violation of accommodation, mydriasis (dilated pupil), a violation of the perception of taste;
- – гипертензия, гиперемия кожного покрова, понижение артериального давления и постуральная гипотензия, тахикардия , желудочковая тахикардия, фибрилляция желудочков; From the cardiovascular system - hypertension, flushing of the skin, lowering of blood pressure and postural hypotension, tachycardia , ventricular tachycardia, ventricular fibrillation;
- – апластическая анемия, агранулоцитоз, панцитопения, нейтропения; From the hematopoietic system - aplastic anemia, agranulocytosis, pancytopenia, neutropenia;
- – ухудшение аппетита, тошнота и рвота, непроизвольное скрежетание зубами (бруксизм), повышение активности ферментов печени, гепатит; On the part of the digestive system - deterioration of appetite, nausea and vomiting, involuntary gnashing of teeth (bruxism), increased activity of liver enzymes, hepatitis;
- – нарушение мочеиспускания, задержка мочи; On the part of the excretory system - violation of urination, urinary retention;
- – нарушение эрекции, снижение либидо, меноррагия, аноргазмия; From the genital system - erectile dysfunction, decreased libido, menorrhagia, anorgasmia;
- – сыпь, фотосенсибилизация, многоформная экссудативная эритема, анафилаксия. Allergic reactions - rash, photosensitivity, exudative erythema multiforme, anaphylaxis.
On the part of other body systems, a sharp decrease in weight, an increase in sweating, is possible. Rarely weight gain, ecchymosis, impaired production of antidiuretic hormone. Serotonin syndrome may occur, accompanied by pain in the stomach, nausea and vomiting, diarrhea, hyperthermia and muscle rigidity, depression of consciousness of varying severity.
With the development of withdrawal syndrome, the patient is noted asthenia, dizziness and headache, fatigue, sleep disorders (drowsiness or insomnia, difficult falling asleep, dreaming). Anxiety develops, marked nervous excitability, confusion of consciousness. Increases sweating, worse appetite, there is a constant dryness in the mouth. Nausea, vomiting, and diarrhea may occur. Such undesirable phenomena are usually weakly expressed, do not require special treatment, and after some time pass independently.
When an overdose of Venlaxor is observed: a change in the parameters of the electrocardiogram, ventricular / sinus tachycardia, hypotension, bradycardia, decreased wakefulness, convulsive conditions. If excessive doses are exceeded, the use of alcohol is likely to be fatal.
Treatment of an overdose is symptomatic. To reduce the absorption of venlafaxine, activated charcoal is prescribed. The control of vital functions (blood circulation, respiration) is carried out. Vomiting can not be caused, because the risk of aspiration is high. The specific venlafaxine antidotes are unknown.
During the appointment and use of Venlaxor it is important to consider:
- At the initial stages of treatment, the likelihood of suicide attempts is not ruled out, so the patient must be under constant supervision;
- In patients with affective disorders, the likelihood of developing manic conditions is possible (patients with a history of mania must be under constant medical supervision);
- During treatment, constant monitoring of blood pressure is necessary (especially when selecting / increasing doses);
- During treatment in elderly patients, dizziness, disturbance of balance may occur;
- When prescribing the drug to patients with lactose intolerance, it is important to take into account the lactose content of tablets;
- During therapy, you can not drink alcohol;
- Since the drug affects the central nervous system, during treatment it is better not to commit potentially dangerous activities that require reaction speed and concentration of attention (driving, handling mechanisms, etc.);
- In patients with cirrhosis of the liver, the concentration of venlafaxine and EFA in the blood plasma increases, and the rate of excretion decreases;
- With mild hepatic insufficiency, dose adjustment is not required;
- With moderate hepatic insufficiency the therapeutic dose is reduced by 50%;
- In severe hepatic impairment Venlaxor is not recommended;
- With mild renal failure, dose adjustments are not required;
- With moderate renal failure, the half-life of venlafaxine increases, so the therapeutic dose should be reduced by 25-50%, while the whole daily dose is taken once;
- In severe renal failure, Venlaxor is not recommended;
- Elderly patients the drug is administered with caution, at the lowest effective dosages because of the high probability of disrupting the kidneys;
- At the final stage of treatment the dosage of Venlaxor should decrease gradually for at least 7 days to avoid withdrawal syndrome;
- The period necessary for the complete cessation of venlaxor intake is established individually for each patient based on the doses used, the duration of the therapeutic course and the individual characteristics of the patient.
Venlaxor is administered with caution in the presence of certain concomitant diseases. It:
- Recently suffered myocardial infarction;
- Unstable angina ;
- Kidney failure;
- liver failure;
- A history of convulsive syndrome;
- Manic conditions in the anamnesis;
- Propensity to suicide;
- Angle-closure glaucoma;
- Increased intraocular pressure;
- Tendency to bleeding from the skin and mucous membranes;
- Simultaneous reception of diuretics;
- Initially low body weight.
- Simultaneous reception of Venlaxor with MAO inhibitors is contraindicated;
- Venlaxor is prescribed at least 14 days after administration of MAO inhibitors (the exception is the reversible MAO inhibitor moclobemide - in this case, the interval between doses should be 24 hours);
- MAO inhibitors are prescribed at least 7 days after the last administration of Venlaxor;
- In combination with haloperidol, its concentration in the blood increases and the therapeutic effect is enhanced;
- Combination with diazepam, risperidone does not cause a change in the therapeutic effect of these drugs and venlafaxine;
- When combined with clozapine, its plasma concentration increases, and side effects develop (including epileptic seizures);
- Venlafaxine enhances the effect of ethanol on psychomotor reactions;
- While concurrent administration of cimetidine suppresses the metabolism of venlafaxine and does not affect the pharmacokinetics of the active metabolite;
- Venlafaxine does not interact with hypoglycemic drugs and antihypertensive agents (diuretics, β-adrenoblockers, ACE inhibitors);
- Venlafaxine does not affect the concentration of drugs that have a high degree of binding to plasma proteins;
- Venlaxor strengthens the anticoagulant effect of warfarin;
- With simultaneous administration with indinavir reduces its concentration in the blood plasma.
Pregnancy and lactemia
There is no evidence regarding the safety of venlafaxine in pregnant women, so the drug is contraindicated during pregnancy.
If the drug is still administered to a pregnant woman shortly before the birth, the newborn can develop withdrawal syndrome.
Active metabolite and venlafaxine are excreted in breast milk, therefore Venlaxor is not used during lactation. If you need to take the drug, you need to stop breastfeeding.
The complete structural analogues of Venlaksor (with the same active substance in the composition) are preparations: Efektin, Velaxin, Ephevelone, Velafax.
Terms and conditions of storage
Venlaxor tablets are stored out of reach of children, dry, protected from sunlight at a temperature of up to 25 ° C. Shelf life is 3 years. Do not take the pill after the expiration date indicated on the package.
Venlaxor tablets 75mg, 30 pcs. - 815-930 rubles.