Pharmacodynamics sustanon 250 is a racemic mixture of a non-steroidal antiandrogenic activity of predominantly (R) -enantiomer, has no other endocrine activity. sustanon 250 binds to free or normal androgen receptors and without activating gene expression, inhibits the stimulatory effect of androgens. This results in a regression of prostate tumors.
In some patients receiving sustanon 250 cessation may lead to the development of clinical “anti-androgen withdrawal syndrome”.
Pharmacokinetics sustanon 250 is well absorbed from the gastrointestinal tract after oral administration. Food intake has no effect on its bioavailability.
(S) -enantiomer excreted faster (R) -enantiomer of the last half-life of the plasma is about 1 week.
At a daily intake of 50 mg of the equilibrium concentration of sustanon 250 (R) enantiomer in the plasma of about 9 mg / ml.
at a daily intake of 150 mg of the equilibrium concentration of sustanon 250 (R) -enantiomer in the plasma is increased by about 10 times because of the long half-life.
The daily reception sustanon 250 150 mg / day equilibrium concentration of (R) -enantiomer in plasma is approximately 22 ug / ml. In the equilibrium state, about 99% of total circulating enantiomers of the active (R) enantiomer.
Pharmacokinetics (R) enantiomer is independent of age, renal function, mild or medium human liver. In patients with severely impaired liver function slows elimination (11) enantiomer from plasma.sustanon 250 has a high ability to bind to proteins (for a racemic mixture of 96% for (R) enantiomer> 99%) and extensively metabolised (by oxidation and formation of conjugates with glucuronic acid). The metabolites are excreted in the urine and bile in approximately equal proportions.
A common prostate cancer in combination with LHRH analogue (releasing hormone luteinizing hormone) or surgical castration. sustanon 250 is indicated for the treatment of localized prostate cancer in patients who have not have been subjected to radical prostatectomy or radiotherapy. Patients with locally advanced prostate cancer sustanon 250 indicated as monotherapy or as adjunctive therapy in combination with radical prostatectomy or radiotherapy.
sustanon 250 also indicated for the treatment of locally advanced, nonmetastatic prostate cancer in cases where surgical castration or other medical intervention is not suitable or not acceptable .
: Hypersensitivity to sustanon 250 or any other auxiliary components within the drug.
Co-administration of sustanon 250 with drugs such as terfenadine, astemizole, and cisapride.
sustanon 250 is contraindicated in women and children.
sustanon 250 should be used with caution in patients with hepatic impairment.
Dosage and administration
for widespread treatment of prostate cancer in combination with LHRH analogue or surgical castration sustanon 250 taking 50 mg once a day. Treatment sustanon 250 should be started simultaneously with the start of reception LHRH analogue or surgical castration.
For the treatment of locally advanced, non-metastatic prostate cancer, adults and elderly men taking 150 mg / day (three tablets of 50 mg in one step) as monotherapy. sustanon 250 should be taken continuously, for at least 2 years or until disease progression. Renal function: You do not need dose adjustment in patients with impaired renal function. Disturbances of liver function: No need for dose adjustment in patients with mild hepatic impairment. In patients with moderate and severe hepatic impairment may experience increased accumulation of sustanon 250.
sustanon 250 generally well tolerated.
The pharmacological action of sustanon 250 can lead to the following undesirable effects: Very often (> 10%) . Gynecomastia, pain thoracic gland Gynecomastia can be maintained even after cessation of therapy, especially in the case of taking the drug for a long time. Often (> 1%): hot flushes, pruritus, asthenia, alopecia, hair growth reduction, skin dryness, decreased libido, nausea, sexual dysfunction and weight gain. rare (> 0.1% – <1%): pain abdominal pain, depression, dyspepsia and haematuria. Changes in liver function tests, rarely severe (increase in transaminases, cholestasis and jaundice) have been observed with the use of sustanon 250. Changes in the majority of cases were transient in nature, completely disappeared or decreased with continued therapy or after drug discontinuation. Very rarely during treatment with sustanon 250 developing liver failure, a causal relationship between the development of liver failure and treatment bikalumidom not reliably established. Given the possibility of such changes, it is advisable to periodically assess liver function.
Cases of overdose have not been described in humans. There is no specific antidote, therefore symptomatic treatment should wear character. Dialysis is not effective, since sustanon 250 is closely associated with proteins and excreted in the urine in unchanged form. Shown general supportive therapy, and monitoring of vital functions of the body.
Interaction with other medicinal products
No information of any kind was a pharmacodynamic or pharmacokinetic interactions between sustanon 250 and LHRH analogues. In in vitro studies have shown that the (R) -enantiomer is sustanon 250 ZA4 CYP inhibitor, to a lesser extent affect the activity of CYP 2C9, 2C19 and 2D6. In clinical studies using antipyrine as a marker of activity of the cytochrome P450 (CYP) has not detected a potential sustanon 250 ability to interact with other drugs. However, with sustanon 250 for 28 days to patients receiving midazolam AUC midazolam AUC increased by 80%. This increase can be important for drugs with a narrow therapeutic window.
Therefore, concurrent use of sustanon 250 is contraindicated with drugs such as terfenadine, astemizole, and cisapride. Caution must be exercised in the appointment of sustanon 250 together with cyclosporine or calcium channel blockers. You may need to decrease the dose of these drugs, particularly in the case or the potentiation of adverse reactions. After the start of the use or withdrawal of sustanon 250 recommend close monitoring of cyclosporine plasma concentrations and clinical condition of the patient. Caution must be exercised with concomitant administration of sustanon 250, and drugs that suppress the oxidation process of drugs, such as cimetidine or ketoconazole. Theoretically, such a combination may lead to an increase in plasma concentrations of sustanon 250, and possibly an increase in the incidence of adverse events.
sustanon 250 can displace coumarin anticoagulant – warfarin plots of protein binding. Therefore, the appointment of sustanon 250 in patients receiving coumarin anticoagulants, should regularly monitor the prothrombin time.
Effects on ability to drive and other moving machinery
sustanon 250 does not affect the patients’ ability to drive vehicles or to engage in other hazardous activities that require high speed of psychomotor reactions.
sustanon 250 is extensively metabolized in the liver. There is reason to believe that the elimination of the drug from the body may be delayed in patients with severely impaired liver function, which can lead to increased accumulation of sustanon 250. It is advisable to periodically assess liver function. Most of the changes of liver function occur in the first six months of treatment bikalutami house.
Severe hepatic changes when using sustanon 250 are rare. In case of severe changes, you must stop taking the drug. Patients with progressive disease on the background of increasing prostate-specific antigen level need to consider discontinuing treatment bikalutami house.
It is shown that sustanon 250 inhibits the activity of cytochrome P450 (CYP ZA4). This should be considered while appointing sustanon 250 with drugs that are primarily metabolized by CYP ZA4. buy anabolic steroids online bruce lee’s workout anabolic steroids online uk