PHARMACOLOGICAL PROPERTIES durabolin 100 – antidepressant chemically not related to any class of antidepressants (tricyclic, tetracyclic, or other), is a racemate of two active enantiomers. The mechanism of antidepressant effects of the drug associated with its ability to potentiate transmission of nerve impulses in the central nervous system (CNS). durabolin 100 and its main metabolite O-desmetilvenlafaksin (EFA) are potent inhibitors of the reuptake of serotonin and norepinephrine and weak inhibitors of dopamine reuptake. Furthermore, durabolin 100 and O-desmetilvenlafaksin reduce beta-adrenergic responsiveness after a single administration, or at a constant reception. durabolin 100 and EFA equally effectively affect the reuptake of neurotransmitters.durabolin 100 has no affinity for muscarinic, cholinergic, histamine (H1) and α 1 -adrenergic receptors of the brain. durabolin 100 does not inhibit the activity of monoamine oxidase (MAO). No affinity for opiate, benzodiazepine, fentsiklidinovym or N-methyl-d-aspartate (NMDA) receptors.
durabolin 100 is well absorbed from the gastrointestinal tract. After a single dose of 25-150 mg, the maximum plasma concentration is reached 33-172 ng / ml for approximately 2.4 hours. Subjected to intensive metabolism in the first passage through the liver. Its main metabolite – O-desmetilvenlafaksin (EFA). The half-life -venlafaksina and EFA are respectively 5 and 11 hours. Max EFA concentration in the blood plasma of 61-325 ng / ml is reached after about 4.3 hours after administration.
The binding of durabolin 100 and EFA to plasma proteins is respectively 27% and 30%. EFA and other metabolites and unmetabolized durabolin 100, excreted by the kidneys. Repeated administration of the equilibrium concentrations of durabolin 100 and EFA achieved within 3 days. In the range of 75-450 mg daily doses, durabolin 100 and EFA have linear kinetics. After taking the drug at meal time to maximum plasma concentration is increased to 20-30 minutes, but the maximum concentration values and removals are not changed.
In patients with liver cirrhosis the concentration of durabolin 100 blood plasma and increased EFA and their reduced rate of excretion. In moderate or severe renal insufficiency the overall clearance of durabolin 100 and EFA is reduced, and the half-life is prolonged. Reducing the total clearance generally occurs in patients with a creatinine clearance less than 30 mL / min. Age and sex of the patient did not affect the pharmacokinetics of the drug.
Depression different etiology, treatment and prevention.
Одновременный MAO inhibitors (see. also section “Interactions”).
Severe renal and / or hepatic impairment (glomerular filtration rate less than (GFR) of 10 mL / min).
Age 18 years (safety and efficacy in this age group have not been proved .)
Known or suspected pregnancy.
lactation. Precautions : recent myocardial infarction, unstable angina, hypertension, tachycardia, convulsions in history, increased intraocular pressure, angle-closure glaucoma, manic state in history, predisposition to bleeding from the skin and mucous membranes, initially weight loss, hyponatremia, hypovolemia, concomitant use of diuretics, suicidal tendencies, renal / hepatic failure.
Pregnancy and lactation
The safety of durabolin 100 during pregnancy has not been proven, so the use of the drug during pregnancy (or suspected pregnancy) is contraindicated.
Childbearing age women should be warned about this prior to the start of treatment and should seek medical attention immediately in the event of pregnancy or pregnancy planning period of drug treatment.
If the treatment of the mother had been completed shortly before delivery, the newborn drug withdrawal symptoms may occur.
durabolin 100 and its metabolite (EFA) are allocated into breast milk. The safety of these substances for newborn children is not proven, so taking durabolin 100 during breastfeeding is not recommended. If you want to receive the drug during lactation should decide the issue of termination of breastfeeding.
Dosing and Administration
Venlaksora recommended to take tablets during the meal.
The recommended starting dose is 75 mg in two divided doses (37.5 mg) daily. When – after several weeks of treatment, no significant improvement is observed, the daily dose can be increased to 150 mg (2×75 mg per day). If, in the opinion of the physician, requires a higher dose (major depression or other conditions that require hospital treatment), you can immediately assign 150 mg in two divided doses (2×75 mg per day). Thereafter, the daily dose may be increased to 75 mg every 2-3 days until the desired therapeutic effect. The maximum daily dose Venlaksor drug is 375 mg. After reaching the desired therapeutic effect, the daily dose can be gradually reduced to the lowest effective level. Supportive therapy and relapse prevention : Maintenance treatment may last for 6 months or more. Appointed by the minimum effective dose used in the treatment of depressive episodes. Renal impairment : in mild renal insufficiency (glomerular filtration rate (GFR) was 30 mL / min) correction mode is not required. At moderate renal failure (GFR 10-30 ml / min), the dose should be reduced by 25-50%. In connection with the elongation of the half-life of durabolin 100 and its active metabolite (EFA), such patients should take the entire dose once a day. Not recommended for durabolin 100 in severe renal impairment (GFR less than 10 mL / min), since reliable data on such therapy available. Patients on hemodialysis may receive 50% of the usual daily dose of durabolin 100 after the completion of hemodialysis. Hepatic impairment : in mild hepatic insufficiency (prothrombin time (PT) of less than 14 seconds) correction mode is not required. In moderate hepatic insufficiency (PV from 14 to 18 seconds), the dose should be reduced by 50%. Not recommended for durabolin 100 in severe hepatic insufficiency, since reliable data on such therapy available. Elderly patients : in itself an elderly patient’s age does not require changing the dose, however (as in the appointment of other drugs) for the treatment of elderly patients need to be careful, for example, in connection with renal dysfunction. Use the smallest effective dose. When the dose the patient should be under close medical supervision. Stopping Venlaksor preparation : After receiving Venlaksor drug is recommended to gradually reduce the dosage of the drug, at least for a week and observe the patient’s condition in order to minimize the risk associated with the abolition of the drug (see. below). The period required for the complete cessation of the drug depends on its dosage, duration of treatment and individual patient characteristics.
Most of the following side effects depend on the dose. With long-term treatment of the severity and frequency of most of these effects is reduced, and there is no need for treatment discontinuation.
Depending on the frequency of occurrence of the group are the following side effects: frequent – more than 1%, infrequent – 0.1-1%, rare – 0.01 0.1%, very rare – less than 0.01%. From the nervous system : often – dizziness, asthenia, insomnia, “nightmarish” dream, increased nervous irritability, paresthesia, muscle hypertonicity, tremors, sedation; infrequently – apathy, hallucinations, myoclonus, fainting; rarely – seizures, manic disorder, neuroleptic malignant syndrome. Since the cardiovascular system : often – increased blood pressure, flushing of the skin; infrequently – decreased blood pressure, postural hypotension, tachycardia; very rarely – change of the interval QT, ventricular fibrillation, ventricular tachycardia (including ventricular flickering). From the digestive system : often – loss of appetite, nausea, vomiting; infrequently – bruxism (involuntary teeth grinding), increased activity of “liver” transaminases; rarely – hepatitis. With the genitourinary system : often – decreased libido, erectile dysfunction and / or ejaculation, anorgasmia, menorrhagia, violation of urination; Infrequent – urinary retention, disturbance of orgasm in women. From the senses : common – disturbance of accommodation, mydriasis, visual disturbances; rarely – a violation of taste perception. From the side of hematopoiesis: frequency unknown – agranulocytosis, aplastic anemia, neutropenia, pancytopenia. Allergic reactions : seldom – rash, photosensitivity; very rarely – exudative erythema multiforme (including Sind Stevens – Johnson), anaphylaxis. Laboratory findings : rarely – thrombocytopenia; rarely – increased bleeding time, hyponatremia;with long-term appointment and the use of high doses – hypercholesterolemia. Other : often – weight loss, sweating (including night); infrequently – ecchymosis, increased body mass index; seldom – a syndrome of inappropriate secretion of antidiuretic hormone, serotonin syndrome (nausea, vomiting, abdominal pain, diarrhea, flatulence, agitation, tachycardia, hyperthermia, muscle rigidity, seizures, myoclonus, sweating, depression of consciousness of varying severity). In the event of a syndrome ” cancellation “: dizziness, headache, asthenia, fatigue, sleep disturbances (change in the nature of dreams, drowsiness or insomnia, difficulty falling asleep), hypomania, anxiety, increased nervous irritability, confusion, paraesthesia, increased sweating, dry mouth, decreased appetite , nausea, vomiting, diarrhea (most of these reactions are slightly pronounced and do not require treatment).
Overdose Symptoms : ECG changes (prolongation of the interval QT, bundle branch block feet blockade, expansion of the QRS complex), sinus and ventricular tachycardia, bradycardia, hypotension, apnea condition, the change of consciousness (decreased level of consciousness). With an overdose of durabolin 100 while taking alcohol and / or other psychotropic drugs, reported fatal. Treatment : symptomatic.Specific antidotes are not known. Recommended continuous monitoring of vital functions (respiration and circulation). Appointment of activated charcoal to reduce absorption of the drug. Do not induce vomiting due to aspiration hazard. durabolin 100 and EFA are not displayed during dialysis.
Interaction with other medicinal products
Concomitant use of monoamine oxidase inhibitors (MAOIs) is contraindicated and durabolin 100. Admission Venlaksor drug can be started at least 14 days after the end of therapy MAO inhibitors. If you used a reversible MAO inhibitor (moclobemide), this interval may be shorter (24 hours). MAO inhibitor therapy can begin at least 7 days after the cancellation Venlaksor drug. durabolin 100 did not affect the pharmacokinetics of lithium .
In an application with imipramine pharmacokinetics of durabolin 100 and its metabolite EFA does not change. Haloperidol : last effect can be enhanced due to increased levels of drug in the blood in a joint application. While the use of diazepam pharmacokinetics of drugs and their main metabolites are not significantly changed. Also, it is not revealed effects on psychomotor and psychometric effects of diazepam. While the use of clozapine may experience an increase in its level in the blood plasma and the development of side effects (eg, seizures). While the use of risperidone (despite the increase in AUC of risperidone), the pharmacokinetics of the amount of active components (risperidone and its active metabolite) did not change significantly. Enhances the effects of alcohol on psychomotor reactions. be particularly careful when on patients receiving durabolin 100 electroconvulsive therapy , as the experience with durabolin 100 in these conditions is missing. drugs metabolized by cytochrome P-450 : CYP2D6 enzyme cytochrome P-450 converts to the active metabolite of durabolin 100 EFA. Unlike many other antidepressants, durabolin 100 dose can not reduce, while administered with drugs that inhibit the activity of CYP2D6, or in patients with a genetically determined reduction in CYP2D6 activity, as the total concentration of the active substance and metabolite (durabolin 100 and EFA) will not change. The main path includes the elimination of durabolin 100 metabolism by CYP2D6 and CYP3A4; so you should be very careful in the appointment of durabolin 100 in combination with drugs, depressing both the enzyme. Such drug interactions have not been investigated. durabolin 100 – a relatively weak inhibitor of CYP2D6 and does not inhibit the activity of isozymes CYP1A2, CYP2C9, and CYP3A4; so do not expect its interaction with other drugs in the metabolism involving the liver enzymes. Cimetidine inhibits metabolism “first pass” of durabolin 100 and has no effect on the pharmacokinetics of EFA. The majority of patients are expected only a slight increase in the overall pharmacological activity of durabolin 100 and EFA (more pronounced in older patients and in liver dysfunction). Clinically relevant interaction of durabolin 100 with antihypertensive (including beta-blockers, ACE inhibitors and diuretics) and hypoglycemic agents are not found . medications associated with blood plasma proteins : plasma protein binding is 27% for durabolin 100 and 30% for EFA. Therefore, it does not affect the concentration of drug in blood plasma, a high degree of protein binding. When concomitantly with warfarin may intensify the anticoagulant effect of the latter. When concomitantly with indinavir alter the pharmacokinetics of indinavir (28% -s’ decrease in area under the curve AUC and 36% reduction in the maximum concentration C max) and the pharmacokinetics of durabolin 100 and EFA is not changed. However, the clinical significance of this is unknown effect.
Cancel Venlaksor preparation : as with treatment with other antidepressants, durabolin 100 abrupt cessation of therapy – especially after high doses – may cause withdrawal symptoms in connection with what is recommended to gradually reduce the dose before discontinuing the drug. The length of time required to reduce the dose depends on the dose, duration of therapy, and individual sensitivity of the patient.
In appointing Venlaksor tablets to patients with lactose intolerance should take into account the content of lactose (30 mg in each tablet 37.5 mg, 60 mg in each tablet 75 mg).
patients with depressive disorders before starting any drug therapy should consider the likelihood of suicide attempts. Therefore, to reduce the risk of overdosing the initial dose should be as low as possible, and the patient must remain under close medical supervision.
In patients with affective disorders in the treatment of antidepressants, including durabolin 100 may occur hypomanic or manic states. As with other antidepressants, durabolin 100 should be administered with caution to patients with mania in history. Such patients need medical supervision.
As with other antidepressants, durabolin 100 should be administered with caution to patients with a history of seizures. durabolin 100 treatment should be interrupted in the event of seizures.
Patients should be warned of the need to consult a doctor immediately in case of rash, urticaria, or other allergic reactions.
Some patients while receiving durabolin 100 observed a dose-dependent increase in blood pressure, and therefore recommended that regular monitoring of blood pressure, especially during the selection or dose escalation.
It may happen increase heart rate, especially when high doses. Caution is advised when tachyarrhythmia.
Patients, especially the elderly, should be alerted to the possibility of dizziness and impaired sense of balance.
As with other serotonin reuptake inhibitors, durabolin 100 may increase the risk of bleeding into the skin and mucous membranes. When treating patients predisposed to these conditions, caution is required.While receiving durabolin 100, especially under conditions of dehydration or reduction of blood volume (including elderly patients and in patients receiving diuretics), hyponatremia can be observed and / or syndrome of inadequate secretion of antidiuretic hormone. During dosing mydriasis can be observed, and therefore recommended that the control of intraocular pressure in patients who are prone to increase his suffering or narrow-angle glaucoma.
durabolin 100 has not been studied in patients with recent myocardial infarction, and suffering from decompensated heart failure. Such patients the drug should be used with caution.
It is necessary to establish monitoring of patients for signs of abuse of the drug, particularly for patients who have symptoms such history.
Women of childbearing potential must use appropriate contraceptive methods while taking durabolin 100. Despite the fact that durabolin 100 does not affect on psychomotor and cognitive function, please note that any medication psychoactive drugs can reduce the ability to make judgments, thinking, or motor function performance. this should warn the patient before treatment. In the event of such effects the extent and duration of the restrictions should be set by your doctor. It is also not recommended alcohol reception.
Form release tablets 37.5 mg : 10 tablets in a blister made of PVC film and aluminum foil. 3 blisters with instruction placed in a stack of cardboard. Tablets 75 mg : 10 tablets in a blister made of PVC film and aluminum foil. 3 blisters with instruction placed into cardboard pack. buy legal anabolic steroids online
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