Velaxin capsules of prolonged action 75mg N28
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Active ingredients
Venlafaxine
Release form
Capsules
Composition
Venlafaxine hydrochloride 84.84 mg, which corresponds to the content Venlafaxine 75 mg Excipients:. Microcrystalline cellulose, sodium chloride, ethyl cellulose, talc, dimethicone, potassium chloride, copovidone, silica colloidal anhydrous, xanthan gum, yellow iron oxide; Composition gelatine capsules.: titanium dioxide, iron oxide yellow, iron oxide red, gelatin.
Pharmacological effect
Antidepressant. The chemical structure of venlafaxine cannot be attributed to any known class of antidepressants (tricyclic, tetracyclic, or others). It has two active enantiomeric racemic forms.; The antidepressant effect of venlafaxine is associated with increased neurotransmitter activity in the CNS. Venlafaxine and its main metabolite O-desmethylvenlafaxine (EFA) are potent inhibitors of serotonin and norepinephrine reuptake and weakly inhibit the reuptake of dopamine by neurons. Venlafaxine and EFA equally effectively affect the reuptake of neurotransmitters. Venlafaxine and EFA reduce beta-adrenergic reactions. Venlafaxine does not have affinity for the m- and n-cholinergic receptors, histamine H1 receptors and 1-adrenergic receptors of the brain. Venlafaxine does not inhibit the activity of MAO. It has no affinity for opioid, benzodiazepine, phencyclidine or NMDA receptors.
Pharmacokinetics
Absorption; After oral administration, Cmax of venlafaxine and EFA (the main metabolite) in the blood plasma is achieved within 6.0 ± 1.5 and 8.8 ± 2.2 h, respectively. The rate of absorption of venlafaxine from the capsules of prolonged action is lower than the rate of its elimination. Therefore, T1 / 2 venlafaxine after administration of capsules of prolonged action (15 ± 6 h) is actually T1 / 2 absorption, rather than T1 / 2 distribution (5 ± 2 h), which is observed after the administration of the drug in the form of pills. In the range of daily doses 75-450 mg venlafaxine and EFA have linear kinetics. After taking the drug while eating, the time to reach Cmax in the blood plasma is increased by 20-30 minutes, but the values of Cmax and absorption do not change.; Distribution; The binding of venlafaxine and EFA to plasma proteins is 27% and 30%, respectively. Css venlafaxine and EFA are achieved within 3 days.; Metabolism and excretion; The main metabolite is EFA.; EFA and other metabolites,as well as unchanged venlafaxine excreted by the kidneys.; Pharmacokinetics in special clinical cases; In patients with liver cirrhosis, plasma plasma concentrations of venlafaxine and EFA are increased, and their rate of excretion is reduced. With moderate or severe renal failure, the total clearance of venlafaxine and EFA decreases, and T1 / 2 is prolonged. A decrease in total clearance is mainly observed in patients with CC less than 30 ml / min. The age and sex of the patient do not affect the pharmacokinetics of the drug.
Indications
Depression (with or without anxiety symptoms) in both outpatient and inpatient settings; Prevention of relapse of depression (with a positive therapeutic effect).
Contraindications
Hypersensitivity, simultaneous use of MAO inhibitors, severe impairment of renal function (glomerular filtration rate 18 s), age up to 18 years (safety and efficacy for this age group are not proven), pregnancy or suspected pregnancy, lactation period (there are not enough data from controlled studies).
Use during pregnancy and lactation
The safety of using Velaxin in pregnancy is not proven. Therefore, use during pregnancy (or anticipated pregnancy) is possible only if the intended benefit to the mother outweighs the possible risk to the fetus. Women of childbearing age should use reliable methods of contraception during the period of drug treatment and immediately consult a doctor if pregnancy occurs or planning pregnancy. Venlafaxine and 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, you should decide on the termination of breastfeeding. If the mother’s treatment was completed shortly before delivery, the newborn may experience withdrawal symptoms.
Dosage and administration
Velaxin is taken orally, during meals. The recommended starting dose is 75 mg daily.
Side effects
Common symptoms: weakness, fatigue .; On the part of the gastrointestinal tract: decreased appetite, constipation, nausea, vomiting, dry mouth, rarely - hepatitis .; On the part of metabolism: an increase in cholesterol in the blood serum, a decrease in body weight,sometimes - changes in the results of laboratory tests of liver function, hyponatremia, syndrome of insufficient secretion of antidiuretic hormone .; Since the cardiovascular system: arterial hypertension, skin hyperemia, postural hypotension, tachycardia .; From the side of the central nervous system: unusual dreams, dizziness, insomnia, irritability, paresthesia, stupor, increased muscle tone, tremor, yawning; sometimes apathy, hallucinations, muscle spasms, serotonin syndrome, rarely epileptic seizures, manic reactions, as well as symptoms resembling a neuroleptic malignant syndrome .; On the part of the urogenital system: disturbances of ejaculation, erection, anorgasmia, dysuric disorders (mainly - difficulty at the beginning of urination); sometimes - decreased libido, menorrhagia, urinary retention .; From the sense organs: accommodation disturbances, mydriasis, visual disturbances; Infrequently - a violation of taste sensations .; On the part of the skin: sweating; sometimes - photosensitivity reactions; rarely, erythema multiforme, Stevens-Johnson syndrome; From the hemopoietic system: sometimes - hemorrhages into the skin (ecchymosis) and mucous membranes, thrombocytopenia; rarely, prolonged bleeding time.
Overdose
Symptoms: ECG changes (lengthening of the QT interval, blockade of the bundle of the His, extension of the QRS complex), sinus or ventricular tachycardia, bradycardia, hypotension, convulsive states, change of consciousness (decreased wakefulness). With an overdose of venlafaxine, while taking it with alcohol and / or other psychotropic drugs, fatalities were reported. Treatment: symptomatic therapy. Specific antidotes are unknown. Continuous monitoring of vital functions (respiration and circulation) is recommended. The appointment of activated carbon to reduce the absorption of the drug. Do not induce vomiting due to the risk of aspiration. Venlafaxine and EFA are not displayed during dialysis.
Interaction with other drugs
The simultaneous use of Velaxin with MAO inhibitors is contraindicated. Reception Velaksina can begin no less 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 begin no less than 7 days after discontinuation of the drug Velaxin.;; Simultaneous use of venlafaxine with lithium can increase the level of the latter.; When used simultaneously with imipramine, the pharmacokinetics of venlafaxine and its EFA metabolite do not change. At the same time, their simultaneous use enhances the effects of desipramine - the main metabolite of imipramine - and its other metabolite 2-OH-imipramine, although the clinical significance of this phenomenon is unknown.; It is possible to enhance the effects of haloperidol due to its increased blood concentration when used together Velaksinom.; With simultaneous use with diazepam pharmacokinetics of drugs and their major metabolites is not significantly changed. Also, there was no effect on the psychomotor and psychometric effects of diazepam. When used simultaneously with clozapine, there may be an increase in its plasma level and side effects (for example, epileptic seizures); With simultaneous use of risperidone (despite an increase in AUC of risperidone) the sum of the active components (risperidone and its active metabolite) did not change significantly. With the simultaneous use of venlafaxine with ethanol, there was no decrease in psychomotor reactions d. However, it is not recommended to use alcohol during venlafaxine therapy. Venlafaxine metabolism with the formation of the active metabolite EFA occurs with the participation of the CYP2D6 isoenzyme. Unlike many other antidepressants, the dose of venlafaxine can not be reduced while used with CYP2D6 inhibitors, or in patients with a genetically determined decrease in CYP2D6 activity, since the total concentration of the active substance and metabolite (venlafaxine and EFA) does not change. The main route of elimination venlafaxine includes a metabolism involving CYP2D6 and CYP3A4, therefore special care should be taken when prescribing venlafaxine in combination with drugs that are inhibitors of these drugs. enzymes. The nature of this interaction has not yet been studied.; Venlafaxine is a relatively weak inhibitor of CYP2D6 and does not inhibit the activity of CYP1A2 isoenzymes,CYP2C9 and CYP3A4; therefore, one should not expect its interaction with other drugs whose metabolism involves these liver enzymes. Cimetidine inhibits venlafaxine metabolism during the “first pass” through the liver and does not affect the EFA pharmacokinetics. In the majority of patients, only a slight increase in the overall pharmacological activity of venlafaxine and EFA is expected (more pronounced in elderly patients and in liver dysfunction). ) and hypoglycemic drugs. Since the binding of plasma proteins venlafaxine and EFA is respectively 27% and 30%, drug interactions due to impairment are not expected m binding to plasma proteins.; If taken simultaneously with warfarin, the anticoagulant effect of the latter can be enhanced, while the prothrombin time is prolonged and MHO is increased. pharmacokinetic parameters of venlafaxine and EFA do not change. The clinical significance of this effect is unknown.
special instructions
In patients with depressive disorders, the likelihood of suicidal attempts should be considered before starting any drug therapy. Therefore, to reduce the risk of abuse and / or overdose, only a small amount of capsules should be given out at the beginning of treatment, and the patient should be under close medical supervision. Aggressive behavior was reported during venlafaxine (especially at the start of treatment and after discontinuation of the drug) .; venlafaxine may cause psychomotor agitation, which is clinically reminiscent of akathisia, characterized by anxiety with the need to move, often in combination with an inability to sit or stand on m ste. This is most often observed during the first few weeks of treatment. If these symptoms occur, increasing the dose may have an adverse effect and the question should be considered about whether to continue taking the drug. In patients with affective disorders, treatment with antidepressants (includingvenlafaxine), hypomania or manic states may occur. Like other antidepressants, venlafaxine should be administered with caution to patients with a history of mania and / or hypomania. Such patients need medical supervision.; Velaxin; (like other antidepressants) should be prescribed with caution in patients with a history of epileptic seizures. Treatment with venlafaxine should be interrupted when epileptic seizures occur or their frequency increases. With caution it is necessary to prescribe the drug along with antipsychotic drugs, since possible development of symptoms resembling a malignant neuroleptic syndrome.; Patients should be warned about the need to immediately consult a doctor if a rash, urticarial elements or other allergic reactions occur.; In some patients a dose-dependent increase in blood pressure has been observed, and therefore regular monitoring is recommended HELL, especially during the period of clarifying or increasing the dose.; Patients, especially the elderly, should be warned about the possibility of dizziness and sheniya sense of balance;. Precautions should be prescribed venlafaxine in patients with recent myocardial infarction, suffering from decompensated heart failure, because the safety of the drug in these patients has not been studied;. The caution is recommended to use the drug in patients with tachyarrhythmias. Against the background of drug treatment, an increase in heart rate is possible, especially while taking high doses.; On the background of taking the drug, orthostatic hypotension may develop. When treating patients predisposed to such conditions, caution is needed.; During the intake of venlafaxine, especially in conditions of dehydration or reduction of BCC (including in elderly patients and patients taking diuretics), hyponatremia and / or insufficient secretion syndrome may occur ADH.; Mydriasis may be observed while taking the drug, and therefore it is recommended that intraocular pressure be monitored in patients prone to it or suffering from angle-closure glaucoma. buoy caution during electroconvulsive therapy, becausethere is no experience with venlafaxine in these conditions.; The drug is prescribed with caution in case of renal and hepatic insufficiency. The safety and efficacy of venlafaxine with weight-reducing agents, incl. Phentermine has not been established, so their simultaneous use (as well as the use of venlafaxine as a monotherapy for weight loss) is not recommended. A clinically significant increase in serum cholesterol level was observed in some patients receiving venlafaxine for at least 4 months. Therefore, with long-term use of the drug, it is advisable to monitor the level of serum cholesterol.; After stopping the drug, especially sudden, you may experience withdrawal symptoms. The risk of withdrawal symptoms may depend on several factors, including course duration and dose, as well as the rate of dose reduction. Symptoms of withdrawal (dizziness, sensory disturbances / including paresthesias /, sleep disturbances / including insomnia and unusual dreams /, agitation or anxiety, nausea and / or vomiting, tremor, sweating, headache, diarrhea, rapid and increased heart rate and emotional lability) usually have little or moderate severity, however, in some patients they can be severe. Usually observed in the first days after discontinuation of the drug, although there were separate reports of the occurrence of such symptoms in patients who accidentally missed a single dose. Usually these phenomena disappear on their own within 2 weeks. However, in some patients they may be longer (2-3 months or more). Therefore, before discontinuation of venlafaxine, it is recommended to gradually reduce its dose over several weeks or months depending on the patient's condition; Use in pediatrics; Safety and efficacy of using the drug in children and adolescents under the age of 18 years have not been studied. Increased likelihood of suicidal behavior, as well as hostility, in clinical trials is more common among children and adolescents receiving antidepressants, and compared with groups receiving placebo; Effect on ability to drive motor vehicles and control mechanisms; It should be noted that any drug therapy is psychoactive drugs can impair mental processes and reduce the ability to perform motor functions. This should alert the patient before starting treatment. When such violations occur, the degree and duration of the restrictions must be established by the doctor.