mechanism of antidepressant effects of the drug associated with its ability to potentiate transmission of nerve impulses in the central nervous system (CNS).
winstrol steroid and its main metabolite O-desmetilvenlafaksin (EFA) are potent inhibitors of the reuptake of serotonin and norepinephrine (SNRI) and weak inhibitors of dopamine reuptake. Furthermore, winstrol steroid and O-desmetilvenlafaksin reduce beta-adrenergic responsiveness after a single administration, or at a constant reception. winstrol steroid and EFA equally effectively affect the reuptake of neurotransmitters.
winstrol steroid has no affinity for muscarinic, cholinergic, winstrol steroid and α 1 -adrenergic receptors of the brain. winstrol steroid does not inhibit the activity of monoamine oxidase (MAO). No affinity for opiate, benzodiazepine, fentsiklidinovym or N-methyl-d-aspartate (NMDA) receptors.
winstrol steroid is well absorbed from the gastrointestinal tract. After a single dose 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-desmethyl winstrol steroid (EFA)
The half-life of winstrol steroid and EFA is respectively 5 and 11 hours.
Maximum EFA concentration in the blood plasma of 61-325 ng / ml is achieved after about 4.3 hours after administration. The binding of winstrol steroid and EFA to plasma proteins is respectively 27% and 30%. EFA and other metabolites and unmetabolized winstrol steroid, excreted by the kidneys. Repeated administration of the equilibrium concentrations of winstrol steroid and EFA achieved within 3 days, daily doses in the range 75-450 mg, winstrol steroid 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 winstrol steroid blood plasma and increased EFA and their reduced rate of excretion. In moderate or severe renal insufficiency the overall clearance of winstrol steroid and EFA is reduced; and elimination half-life is prolonged. Reduction in total clearance is mainly seen in patients with creatinine clearance below 30 ml / min. Age and sex of the patient did not affect the pharmacokinetics of the drug.
Depression different etiology, treatment and prevention.
- Simultaneous treatment with MAO inhibitors (see. As “Interaction” section).
- Severe renal and / or hepatic impairment (glomerular filtration rate (GFR) of less than 10 ml / min).
- Age 18 years (safety and efficacy in this age group have not been proved).
- Known or suspected pregnancy.
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, weight loss initially.
Pregnancy and lactation
The safety of winstrol steroid during pregnancy has not been proven, so use during pregnancy (or suspected pregnancy) is possible only if the potential benefit to the mother outweighs the potential risk to the fetus. Women of childbearing age should be warned about this prior to the start of treatment and should seek medical attention immediately in the event of pregnancy or planning pregnancy during drug treatment. winstrol steroid and its metabolite (EFA) are allocated into breast milk. The safety of these substances for newborn children is not proven, so taking winstrol steroid during breastfeeding is not recommended. If you want to receive the drug during lactation should decide the issue of termination of breastfeeding. If maternal treatment was completed shortly before the birth, the newborn drug withdrawal symptoms may occur.
Dosing and Administration
Velafaksa recommended to take tablets during the meal.
The recommended starting dose is 75 mg in two divided doses (37.5 mg) daily.
If 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 × x 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, the drug Velafaks is 375 mg. After achieving the desired therapeutic effect, the daily dose can be gradually reduced to the minimum effective level. Supportive therapy and relapse prevention: Maintenance treatment may last for months or more b. Appointed by the minimum effective dose used in the treatment of depressive episodes.Renal insufficiency: the light renal failure (glomerular filtration rate (GFR) of more than 30 ml / min), a correction mode is not required. In moderate renal insufficiency. (GFR 10-30 ml / min), the dose should be reduced by 25-50%. In connection with the elongation of the half-life of winstrol steroid and its active metabolite (EFA), such patients should take the entire dose once a day. Not recommended for winstrol steroid 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 winstrol steroid 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 winstrol steroid 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 Velafaks preparation:
After receiving Velafaks 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 a complete cessation of the drug depends on the 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.
In decreasing order of frequency: Frequent> 1%, infrequent> 0.1% – <1%, Rare> 0.01% – <0.1 %, very rare <0.01%. Common symptoms: weakness, fatigue, the part of the gastrointestinal tract: loss of appetite, constipation, nausea, vomiting, dry mouth, rarely hepatitis. on the part of metabolism: increase in serum cholesterol levels blood, decrease in body weight; Uncommon: changes in liver function laboratory samples, hyponatremia, syndrome of inadequate secretion of antidiuretic hormone. On the part of the cardiovascular system: hypertension, flushing of the skin; Uncommon: postural hypotension, tachycardia, From the nervous system: abnormal dreams, dizziness, insomnia, irritability, paresthesias, stupor, increased muscle tone, tremor, yawning; unclean: apathy, hallucinations, muscle spasms, serotonin syndrome; Rare: seizures, manic reaction, and symptoms resembling neuroleptic malignant syndrome (NMS). From the urogenital system: ejaculation disorders, erectile dysfunction, anorgasmia, dizuricheskie disorders (mainly – difficulties at the beginning of urination); Uncommon: decreased libido, menorrhagia, urinary retention. From the senses: accommodation disturbances, mydriasis, blurred vision; . Uncommon: dysgeusia For the skin: Sweating; Infrequent: photosensitivity reactions; rare: erythema multiforme, Stevens-Johnson syndrome. From the hematopoietic system: Uncommon: bleeding in the skin (ecchymosis) and mucous membranes, thrombocytopenia; rare; . prolonged bleeding Hypersensitivity reactions: Uncommon: rash; very rare:. anaphylactic reactions after abrupt withdrawal of winstrol steroid or reducing the dose can be observed: fatigue, drowsiness, headache, nausea, vomiting, anorexia, dry mouth, dizziness, diarrhea, insomnia, anxiety, irritability, disorientation, hypomania, paresthesia sweating. These symptoms are usually mild and go away without treatment. Because of the likelihood of these symptoms it is important to gradually reduce the dose.
Symptoms: ECG changes (prolongation of the interval QT, bundle branch block, the 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 winstrol steroid while taking alcohol and / or other psychotropic drugs, it reported deaths.
Treatment: symptomatic. Specific antidotes are not known. Recommended continuous monitoring of vital functions (respiration and circulation).
The appointment of activated charcoal to reduce absorption of the drug. Do not induce vomiting because of risk of aspiration, winstrol steroid and EFA are not displayed during dialysis.
Interaction with other drugs
Concomitant use of monoamine oxidase inhibitors (MAOIs) and winstrol steroid contraindicated. Admission Velafaks 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 in no less than 7 days after discontinuation of the drug Velafaks.
winstrol steroid did not affect the pharmacokinetics of lithium .
In an application with imipramine pharmacokinetics of winstrol steroid and its metabolite O-dezmetilvenlafaksina (EFA) is not changed. Haloperidol: last effect can be amplified iz the increased level of drug in the blood in a joint application. while the use of diazepam pharmacokinetics of drugs and their main metabolites does not change significantly. Also 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 winstrol steroid electroconvulsive therapy , as the experience with winstrol steroid in these conditions is missing. drugs metabolized by cytochrome P-450: CYP2D6 enzyme cytochrome P 450 converts the winstrol steroid active metabolite O-desmethyl winstrol steroid (OD B). Unlike many other antidepressants, winstrol steroid 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 (winstrol steroid and EFA) will not change. The main path includes the elimination of winstrol steroid metabolism by CYP2D6 and CYP3A4; so you should be very careful in the appointment of winstrol steroid in combination with drugs, depressing both the enzyme. Such drug interactions have not been investigated. winstrol steroid – 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 winstrol steroid and has no effect on the pharmacokinetics of O-dezmetilvenlafaksina. The majority of patients are expected only a slight increase in the overall pharmacological activity of winstrol steroid and O-dezmetilvenlafaksina (more pronounced in older patients and in violation of the liver). Clinically relevant interaction of winstrol steroid with antihypertensive (including beta-blockers, ACE inhibitors and diuretics) and antidiabetic agents are not detected. medications associated with blood plasma proteins: plasma protein binding is 27% for winstrol steroid 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. In simultaneous reception with indinavir alter the pharmacokinetics of indinavir (28% -s’ decrease in area under the curve AUC and 36% reduction in the maximum concentration Cmax) and the pharmacokinetics of winstrol steroid and EFA is not changed. However, the clinical significance of this is unknown effect.
Cancel Velafaks preparation: As with treatment with other antidepressants, winstrol steroid 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, as well as individual patient sensitivity.
When assigning tablets Velafaks patients with lactose intolerance to consider the content of lactose (56.62 mg in each tablet 25 mg 84.93 mg in each tablet 37.5 mg 113.24 mg in each tablet 50 mg 169.86 mg each tablet of 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 winstrol steroid may occur hypomanic and manic states.
Like other antidepressant drugs, winstrol steroid should be administered with caution to patients with mania in history. Such patients need medical supervision.
As with other antidepressants, winstrol steroid should be administered with caution to patients with a history of seizures. Treatment with winstrol steroid 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 elements or other allergic reactions.
Some patients while receiving winstrol steroid and observed a dose-dependent increase in blood pressure, and therefore the It recommends regular monitoring of blood pressure, especially in the period specification or increase the dosage.
It may happen increasing 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, winstrol steroid may increase the risk of bleeding into the skin and mucous membranes, in the treatment of patients predisposed to these conditions, caution.
while receiving winstrol steroid. particularly under conditions of dehydration or reduction of blood volume (including elderly patients and in patients receiving diuretics) may occur hyponatremia and / or syndrome of inadequate secretion of antidiuretic hormone.
During reception mydriasis may be a drug, therefore recommended to control intraocular pressure in patients who are prone to increase his suffering or narrow-angle glaucoma.
winstrol steroid 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.
The carried out to date in clinical trials showed no tolerance to winstrol steroid or depending on him. Despite this, as in the treatment of other drugs acting on the central nervous system, the physician must establish careful monitoring of patients for signs of drug abuse. Careful monitoring and observation are needed for patients who have symptoms such history.
Women of childbearing potential should use appropriate contraceptive methods while taking winstrol steroid.
Despite the fact that winstrol steroid does not affect the psychomotor and cognitive function, please note that any medication misuse drugs can reduce the ability to make judgments, thinking, or motor function performance. This should warn the patient before Nachet treatment.
If you experience such effects, the extent and duration of the restrictions should be set by your doctor. Also not recommended alcohol reception. geneza pharmaceuticals anabole steroide shop was sind steroide steroide kaufen online bodybuilding you tube vilafinil modafinil teen bodybuilder posing bodybuilding protein shake aqua test steroid high protein snacks bodybuilding