Venlaksor instructions for use
Venlaksor - an antidepressant.
Release form and composition
Venlaksor is available in tablets, in dosages of 37.5 mg and 75 mg. Tablets in blisters with the instruction placed in a carton (30 tablets per pack).
The main active ingredient is venlafaxine hydrochloride.
Auxiliary components: anhydrous calcium phosphate, anhydrous lactose, sodium carboxymethyl starch, magnesium stearate, colloidal anhydrous silica, dye iron oxide red.
Pharmacodynamics. Venlafaxine is an antidepressant. The chemical structure of the compound can not be attributed to any other group of antidepressants (tricyclic, tetracyclic, and so on.).
The basis of the mechanism of action of venlafaxine is the ability to potentiate the transmission of nerve impulses. Venlafaxine and its active metabolite have a pronounced inhibitory effect on the reuptake of serotonin and norepinephrine and a weak inhibitory effect on the reuptake mechanism of dopamine. Also, the active ingredient and the 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 the activity of MAO. 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: splits into an 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 observed 4.3 hours after the use of tablets. If the drug is taken with food, the maximum plasma concentration is set at 20-30 minutes faster. The value of the maximum concentration and absorption does not change.
With repeated use of the drug a steady concentration of the active substance and EFA is achieved within 3 days. 27% of venlafaxine and 30% of the active metabolite bind to plasma proteins.
Venlafaxine with metabolites excreted by the kidneys. The half-life is 5 hours (for venlafaxine) and 11 hours (for EFA). During dialysis, the active substance and metabolite are not excreted.
Indications for use
Venlaksor is prescribed for the treatment and prevention of depressive disorders of various origins.
Contraindications to the use of Venlaksora are:
- severe functional disorders of the kidneys;
- severe functional disorders of the liver;
- simultaneous treatment with MAO inhibitors;
- age up to 18 years;
- pregnancy and 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 meals.
The recommended initial daily dose is 75 mg of Venlaksor (37.5 mg in two doses). In the absence of the desired therapeutic effect, after several days of 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 to achieve a positive therapeutic effect. The maximum allowable daily dosage of Venlaksora is 375 mg. After reaching the therapeutic effect of the dose is gradually reduced to the minimum effective level.
Venlaksor is used for maintenance therapy and prevention of relapses for a long time (6 months or more), in the minimum effective doses used during the acute stage of the disorder.
When taking Venlaksora may experience undesirable side effects:
- – астения, бессонница, нервная возбудимость, кошмары во сне, гипертонус мышц, парестезии, тремор, нечасто развивается апатия, галлюцинации, обморок, редко возникают маниакальные реакции, судороги ; on the part of the nervous system - asthenia, insomnia, nervous irritability, nightmares in sleep, muscle hypertonia, paresthesia, tremor, apathy rarely develops, hallucinations, fainting, manic reactions, seizures rarely occur;
- – нарушение аккомодации, мидриаз (расширение зрачка), нарушение восприятия вкуса; on the part of the senses - disturbance of accommodation, mydriasis (dilated pupil), disturbance of taste perception;
- – гипертензия, гиперемия кожного покрова, понижение артериального давления и постуральная гипотензия, тахикардия , желудочковая тахикардия, фибрилляция желудочков; on the part of the cardiovascular system - hypertension, skin hyperemia, lowering blood pressure and postural hypotension, tachycardia , ventricular tachycardia, ventricular fibrillation;
- – апластическая анемия, агранулоцитоз, панцитопения, нейтропения; on the part of 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 - loss 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 - a violation of urination, urinary retention;
- – нарушение эрекции, снижение либидо, меноррагия, аноргазмия; on the part of the reproductive system - erectile dysfunction, decreased libido, menorrhagia, anorgasmia;
- – сыпь, фотосенсибилизация, многоформная экссудативная эритема, анафилаксия. allergic reactions - rash, photosensitization, erythema multiforme exudative, anaphylaxis.
On the part of other body systems, a sharp decrease in weight, increased sweating is possible. Rarely observed 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 the withdrawal syndrome, the patient has asthenia, dizziness and headache, fatigue, sleep disorders (drowsiness or insomnia, difficult falling asleep, dreams). Anxiety, marked nervous irritability, confusion develops. Sweating increases, appetite worsens, there is a constant dry mouth. Nausea, vomiting, diarrhea may occur. Such adverse events are usually mild, do not require special treatment, and after a while pass on their own.
In case of an overdose of Venlaksor, a change in the electrocardiogram indices, ventricular / sinus tachycardia, hypotension, bradycardia, decreased wakefulness, and convulsive states are noted. Excessive excess of doses due to alcohol consumption is fatal.
Symptomatic overdose treatment. To reduce the absorption of venlafaxine, activated carbon is prescribed. Vital functions are monitored (blood circulation, respiration). Vomiting can not be caused because the risk of aspiration is high. The specific antidotes for venlafaxine are unknown.
During the appointment and application of Venlaksora it is important to consider:
- in the initial stages of treatment, the likelihood of suicidal attempts is not excluded, therefore the patient should be under constant supervision;
- patients with affective disorders do not exclude the likelihood of developing manic states (patients with a history of mania should be under the constant supervision of physicians);
- during treatment, constant monitoring of blood pressure is necessary (especially when selecting / increasing doses);
- dizziness and imbalance may occur during treatment in elderly patients;
- when prescribing the drug to patients with lactose intolerance, it is important to take into account the lactose content of the tablets;
- during therapy should not consume alcohol;
- since the drug affects the central nervous system, during treatment it is better not to perform potentially hazardous activities that require speed of reaction and concentration of attention (driving vehicles, controlling mechanisms, etc.);
- in patients with liver cirrhosis, the concentration of venlafaxine and EFA in the blood plasma increases, and the elimination rate 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, Venlaksor is not recommended;
- with mild renal insufficiency, dosage adjustment is not required;
- in moderate renal failure, the half-life of venlafaxine increases, so the therapeutic dose should be reduced by 25–50%, with the entire daily dose taken once;
- in severe renal failure, Venlaksor is not recommended;
- Elderly patients are prescribed with caution, in the minimum effective dosage due to the high probability of renal impairment;
- at the final stage of treatment, the dosage of Venlaksora should be reduced gradually for at least 7 days to avoid drug withdrawal;
- the period required for the complete cessation of taking Venlaksora is set individually for each patient based on the doses of the drug used, the duration of the therapeutic course and the individual characteristics of the patient.
Venlaksor appointed with caution in the presence of some associated diseases. It:
- recent myocardial infarction;
- unstable angina ;
- renal failure;
- liver failure;
- history of convulsions;
- history of manic;
- suicidal tendency;
- angle-closure glaucoma;
- increased intraocular pressure;
- tendency to bleeding from the skin and mucous membranes;
- concomitant use of diuretics;
- initially low body weight.
- simultaneous reception of Venlaksor with MAO inhibitors is contraindicated;
- Venlaksor is appointed at least 14 days after administration of MAO inhibitors (an exception is the reversible MAO inhibitor, moccobemide - in this case, the interval between taking the drugs should be 24 hours);
- MAO inhibitors are appointed at least 7 days after the last dose of Venlaksor;
- in combination with haloperidol, its concentration in the blood increases and the therapeutic effect is enhanced;
- combination with diazepam, risperidone does not cause changes in the therapeutic effect of these drugs and venlafaxine;
- when combined with clozapine, its plasma concentration increases, and side effects (including epileptic seizures) develop;
- venlafaxine enhances the effect of ethanol on psychomotor reactions;
- while taking cimetidine inhibits venlafaxine metabolism and does not affect the pharmacokinetics of the active metabolite;
- venlafaxine does not interact with hypoglycemic drugs and antihypertensive drugs (diuretics, β-blockers, ACE inhibitors);
- venlafaxine does not affect the concentration of drugs with a high degree of binding to plasma proteins;
- Venlaksor enhances the anticoagulant action of warfarin;
- while taking it with indinavir, it decreases its concentration in the blood plasma.
Pregnancy and lactation
There is no evidence regarding the safety of venlafaxine in pregnant women, so the drug is contraindicated during pregnancy.
If the drug is still prescribed to a pregnant woman shortly before delivery, then a withdrawal may develop in the newborn.
The active metabolite and venlafaxine are excreted in breast milk, so Venlaksor is not used during lactation. If necessary, taking the drug is required to stop breastfeeding.
The complete structural analogs of Venlaksor (with the same active ingredient in the composition) are the preparations: Efectin, Velaksin, Efevelon, Velafax.
Terms and conditions of storage
Venlaksor tablets are stored out of reach of children, dry, protected from sunlight at a temperature up to 25 ° C. Shelf life is 3 years. Do not take pills after the expiration date indicated on the package.
Venlaksor tablets 75mg, 30 pcs. - 815-930 rub.