Newvelong film-coated pills prol, dI 75mg N30
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Active ingredients
Venlafaxine
Release form
Pills
Composition
Tablets of the prolonged action, film coated 1 tab. venlafaxine (in the form of hydrochloride) 75 mg.
Pharmacological effect
Venlafaxine is a structurally new antidepressant that is a racemate with two active enantiomers. The mechanism of antidepressant action of venlafaxine is associated with its potentiating effect on neurotransmitter activity in the central nervous system. Venlafaxine and its main metabolite, O-desmethylvenlafaxine (EFA) are strong inhibitors of serotonin reuptake and noradrenaline and weak dopamine reuptake inhibitors. By inhibition of serotonin reuptake, venlafaxine is inferior to selective serotonin reuptake inhibitors.
Pharmacokinetics
Absorption - not less than 92% of the dose of venlafaxine, once taken orally. The absolute bioavailability of venlafaxine is about 45%. After a single dose of venlafaxine Cmax pills, venlafaxine and EFA in plasma is achieved within 6.0 ± 1.5 and 8.8 ± 2.2 h, respectively. T1 / 2 drug prolonged action is 15 ± 6 h and is limited by the rate of absorption. Venlafaxine and EFA by 27% and 30%, respectively, are bound to plasma proteins. Venlafaxine undergoes a pronounced first pass metabolism in the liver with the participation of cytochrome P450 (CYP2D6 isoenzyme) with the formation of the active metabolite O-desmethylvenlafaxine. Venlafaxine is also metabolized by isoenzymes of CYP3A3 / 4 to N-desmethylvenlafaxine and other metabolites. In patients with reduced activity of the CYP2D6 isoenzyme, there is a 2-3 times greater exposure to venlafaxine and a 2-3 times lower exposure to the active metabolite EFA. Plasma clearance of venlafaxine is 1.3 l / h / kg, and 0.4 l / h / kg for the active metabolite EFA. T1 / 2 venlafaxine is 15 hours and EFA -11h. Specific patient groups Gender and age do not significantly affect venlafaxine pharmacokinetics. There was no accumulation of venlafaxine or EFA during prolonged administration in healthy subjects. In moderate to severe hepatic and renal failure, there was a decrease in the metabolism of venlafaxine and the elimination of EFA, which led to an increase in Cmax, a decrease in clearance and a prolongation of T1 / 2. The decrease in the total clearance of the drug is most pronounced in patients with creatinine clearance (CC) below 30 ml / min. The intake of venlafaxine with food does not affect either the absorption of venlafaxine or the subsequent formation of EFA.
Indications
- depression (treatment, prevention of recurrence).
Contraindications
- simultaneous administration with MAO inhibitors - lactase deficiency - lactose intolerance - glucose-galactose malabsorption - pregnancy - lactation period - age up to 18 years - hypersensitivity to venlafaxine or another component of the drug. With caution: recent myocardial infarction, unstable angina, arterial hypertension, arthritis. , history of convulsions, intraocular hypertension, angle-closure glaucoma, history of manic states, hyponatremia, hypovolemia, dehydration, one Belt diuretics, suicidal predisposition to bleeding from the skin and mucous membranes, renal / hepatic failure.
Use during pregnancy and lactation
Contraindicated in pregnancy and lactation.
Dosage and administration
Venlafaxine should be taken orally with food, not chewed and squeezed with a liquid 1 time / day, preferably at the same time, in the morning or in the evening. An effective dose for treating depression usually lies between 75 mg and 225 mg. Treatment should begin with 75 mg 1 time / day. A noticeable effect will appear after 2-4 weeks of treatment with a standard adequate dose. If the clinical outcome is not satisfactory, the dose may be increased to 150 mg, then to 225 mg. The maximum permissible daily dose is 375 mg, but it should be borne in mind that the use of high doses is not well understood. In all cases, high doses should be administered under close medical supervision. Doses may be increased with an interval of about 2 weeks or more, at least 4 days between each increase. If after 2-4 weeks of positive dynamics is not observed, treatment should be discontinued. Supportive treatment It is generally accepted that acute bouts of deep depression require 4-6 months of therapy. Some patients may require longer treatment. The physician should periodically overestimate the usefulness of long-term treatment with venlafaxine for each patient individually. Cancellation of the drug should be carried out gradually in order to avoid withdrawal syndrome: with 1 course of treatment for 6 weeks or more, the period of gradual withdrawal of the drug should be at least 2 weeks and depends on the dose, duration of therapy and individual characteristics of the patient.In case of impaired renal function (glomerular filtration rate - 10-70 ml / min), the daily dose should be reduced by 25-50%. In hemodialysis, the daily dose should be reduced by 50%, the drug should be taken after the end of the hemodialysis session. In patients with moderately severe liver failure, the daily dose should be reduced by 50% or more.
Side effects
It is often difficult to distinguish undesirable effects from the symptoms of depression. The degree of most side effects is dose dependent. Frequency rating: Very often:> 1/10; Often:> 1/100 is less than 1/10; Infrequently:> 1/1000 less than 1/100; Seldom:> 1/10 000 is less than 1/1000; Very rarely: less than 1/10 000 including individual messages; From the hemopoietic system: rarely - thrombocytopenia; very rarely, blood formation disorder (including agranulocytosis, aplastic anemia, neutropenia and pancytopenia). On the part of the immune system: infrequently - photosensitivity; very rarely - anaphylaxis. On the part of the endocrine system: very rarely - hyperprolactinemia. Metabolic and nutritional disorders: often - hypercholesterolemia (especially associated with long-term treatment and, possibly, with the use of large doses), weight loss; infrequently - hyponatremia, weight gain; rarely - syndrome of inadequate secretion of antidiuretic hormone. Nervous system: often - dizziness, headache, increased muscle tone, paresthesia, sedation, tremor, insomnia, drowsiness, nervousness, aggression, abnormal dreams, orgasm disorders (men), yawning, loss of appetite, anorexia, weakness, fatigue, asthenia; infrequently - myoclonia, apathy, hallucinations, arousal, orgasm disorders (women); rarely - serotonergic syndrome, neuroleptic malignant syndrome, convulsions, akathisia, mania or hypomania; very rarely, extrapyramidal reactions (including dystopia and dyskinesia), tardive dyskinesias, delirium. From the sensory organs: often - accommodation disturbances, mydriasis, anomalies of perception; infrequently - tinnitus From the side of the cardiovascular system: often - increase in blood pressure, vasodilation (very often a feeling of tide heat), ecchymosis, bleeding from mucous membranes; infrequently - arrhythmias (including tachycardia), lowering blood pressure, postural hypotension,fainting; rarely, hemorrhage (including cerebral hemorrhage), gastrointestinal bleeding; very rarely - prolongation of the QT interval and expansion of the QRS complex, ventricular fibrillation, ventricular tachycardia (including torsade des pointes), decompensation of heart failure, heart failure. On the part of the respiratory system: very rarely - pulmonary eosinophilia with respiratory failure, chest pain. On the part of the digestive system: often - constipation, loss of appetite, nausea, vomiting, dry mouth, dyspepsia; infrequently - bruxism, change in taste, diarrhea; impaired hepatic function tests; rarely, hepatitis; very rarely - pancreatitis. On the part of the skin: often - excessive sweating (including nighttime profuse sweating); infrequently - dermatitis, alopecia, photosensitization, rash; very rarely - erythema multiforme exudative, Stevens-Johnson syndrome, pruritus, pruritus, urticaria. On the part of the musculoskeletal system: very rarely - rhabdomyolysis. From the genitourinary system: often - a violation of urination (most often - intermittent urination), ejaculation disorders, erectile dysfunction, decreased libido; infrequently - urinary retention. menorrhagia, impaired orgasm in women. Changes in laboratory parameters: rarely - increased bleeding time. If withdrawal occurs: dizziness, headache, asthenia, fatigue, sleep disturbances (changing the nature of dreams, drowsiness or insomnia, difficulty falling asleep), hypomania, anxiety, increased nervous irritability, confusion, paresthesia, increased sweating, dry mouth, loss of appetite, nausea, vomiting, diarrhea (most of these reactions are mild and do not require treatment).
Overdose
Symptoms: (often occur while taking ethanol): impaired consciousness (from drowsiness to coma), as well as agitation, gastrointestinal disorders such as vomiting, diarrhea; tremor, change of electrocardiogram (ECG) (prolongation of the QT interval, blockade of the bundle of the bundle of His, expansion of the QRS complex), sinus and ventricular tachycardia or bradycardia, decrease or (weak) increase in blood pressure, seizures, rhabdomyolysis, mydriasis. Treatment: symptomatic; control of ECG and functions of vital organs; at risk of aspiration, vomiting is not recommended; gastric lavage (if overdose occurred recently, or overdose symptoms persist); Activated carbon.Forced diuresis, dialysis, hemoperfusion or exchange transfusion is not effective. There is no specific antidote.
Interaction with other drugs
The simultaneous use of venlafaxine with monoamine oxidase inhibitors (MAO) is unacceptable. The use of venlafaxine is possible not earlier than 14 days from the moment of termination of therapy with MAO inhibitors and should be stopped no less than 7 days before the start of taking any MAO inhibitor due to the risk of increasing side effects. Enhances the effect of ethanol on psychomotor reactions. When taken orally, it reduces the total clearance of haloperidol by 42%, increases its AUC by 70% and Cmax by 88%. Venlafaxine does not affect the metabolism of imipramine and its metabolite 2-hydroxy-imipramine, although the total renal clearance of 2-hydroxydesipramine is reduced, and AUC and Cmax increase by about 35%. Cimetidine inhibits the first-pass metabolism of venlafaxine, but does not affect the pharmacokinetics of O-desmethylvenlafaxine (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). With simultaneous use of venlafaxine with antidepressants (selective serotoninia reuptake inhibitors) (SSRIs), prolonged seizures have been noted. The risk of increased side effects, including seizures, with the simultaneous use of venlafaxine with clozalin, is increased due to an increase in the concentration of clozapine in the blood. Venlafaxine should be used with caution in patients taking medicines that increase the risk of bleeding, such as anticoagulants, salicylic acid derivatives and NSAIDs. With simultaneous use with warfarin, an increase in prothrombin time, partial thromboplastin time, or an international normalized ratio was observed. Caution is required when venlafaxine is used simultaneously with CYP2D6 isoenzyme inhibitors (for example, quinidine, paroxetine, fluoxetine, perphenazine, haloperidol, quinidine, paroxetine, fluoxetine, perphenazine, haloperidol, quinidine, paroxetine, fluoxetine, periphenazine, haloperidol, quinidine, paroxetine, fluoxetine, lopomethromisin, haloperidol, quinidine, paroxetine, fluoxetine, periphenazine, haloperidol, quinidine) CYP2D6 isoenzyme, increasing their plasma concentration. High concentrations of venlafaxine can be observed in patients with low activity of the CYP2D6 isoenzyme With simultaneous use of drugs - inhibitors of the CYP3A3 / 4 isoenzyme (ketoconazole, itraconazole, ritonavir), the concentration of venlafaxine in the blood plasma can be increased.It does not interact with lithium preparations, as well as with drugs that are metabolized by CYP3A4, CYP1A2 and CYP2C9 isoenzymes (including alprazolam, caffeine, carbamazepine, diazepam, tolbutamide). Does not affect the concentration of drugs in plasma, with a high degree of binding to proteins.
special instructions
In patients (under 24 years) with depression or other mental disorders, antidepressants, compared with placebo, increase the risk of suicidal thoughts and suicidal behavior. Therefore, when prescribing venlafaxine, patients under 24 years of age should correlate the risk of suicide with the benefits of their use. In short-term studies, the risk of suicide was not increased in people over 24 years of age, while in people over 65 years of age it was somewhat reduced. Any depressive disorder itself increases the risk of suicide. Therefore, during treatment with antidepressants, all patients should be monitored for the purpose of early detection of abnormalities or behavioral changes, as well as suicidal tendencies. For patients with diabetes mellitus, the treatment of SSRIs / SSRIs (selective norepinephrine reuptake inhibitors) may affect glucose levels. The dose of insulin and / or oral antidiabetic agents should be adjusted. During treatment, patients with hypovolemia or dehydrated patients (including elderly patients and receiving diuretics) may develop hyponatremia and / or syndrome of inadequate secretion of antidiuretic hormone. Careful dosing and regular monitoring are used in the following cases: - narrow-angle glaucoma, increased intraocular pressure (because venlafaxine has a weak m-anticholinergic effect), - diseases of the cardiovascular system (conduction disturbance, angina, recent myocardial infarction, ventricular arrhythmia , hypertension or hypotension). During long-term treatment with venlafaxine, it is necessary to control the concentration of serum cholesterol. With the occurrence of hypercholesterolemia, consideration should be given to switching to another antidepressant. Patients taking venlafaxine may have an increased risk of skin or mucous bleeding. During treatment with the drug is recommended to refrain from taking alcohol.Impact on the ability to drive and control mechanisms During the period of treatment with venlafaxine, care must be taken when driving vehicles or performing work that require increased concentration of attention and speed of psychomotor reactions.