Dianabol dosage is a selective, non-steroidal anti-androgen without having other types of endocrine activity. It is a racemic mixture of a non-steroidal antiandrogenic activity predominantly (R) -enantiomer. dianabol dosage binds to the androgen receptor and not activate gene expression, suppresses the stimulatory effect of androgens. The result is a regression of prostate tumors. In some patients receiving dianabol dosage cessation may lead to the development of the syndrome of “cancellation” anti-androgens. Dianabol dosage After intake of rapidly and completely absorbed from the gastrointestinal tract. Food intake does not affect absorption. (S) -enantiomer excreted faster (R) -enantiomer of the last half-life – about 7 days. With daily administration of dianabol dosage concentration of (R) -enantiomer in the plasma is increased by about 10 times because of the long half-life, which enables the drug once a day. The daily dose of dianabol dosage receiving 50 mg equilibrium concentration of the (R) enantiomer in the plasma of about 9 mg / ml. When administered 150 mg dianabol dosage daily equilibrium concentration of (R) enantiomer is approximately 22 mcg / mL. In the equilibrium state, about 99% of total circulating enantiomers of the active (R) -enantiomer. The connection to plasma proteins is high (for a racemic mixture of 96% for the (R) enantiomer 99.6%). The intensity and stereospecifically metabolized in the liver (by oxidation and glucuronic acid conjugates). The metabolites are not active, the kidneys and intestines in approximately equal proportions. In the pharmacokinetics (R) -enantiomer does not affect the age, renal impairment, mild to moderate hepatic dysfunction. There is evidence that patients with severely impaired liver function slows down the elimination of (R) enantiomer from plasma.
- Common prostate cancer in combination with an analogue of gonadotropin-releasing hormone (GnRH) or surgical castration.
- Locally common prostate cancer (TK-T4, any N, MO; T1-T2, N +, MO) as monotherapy or adjuvant therapy in combination with radiotherapy or radical prostatectomy.
- Locally advanced non-metastatic prostate cancer in cases where surgical castration or other medical intervention are not applicable or acceptable.
: Hypersensitivity to any component of the drug, simultaneous reception with terfenadine, astemizole, cisapride, lactase deficiency, lactose intolerance, glucose-galactose malabsorption (product contains lactose); childhood. Should not be administered to patients females. With caution Abnormal liver function.
Dosing and Administration
Adult males (including the elderly..): When the prevalence of prostate cancer in combination with a GnRH analogue or surgical castration: 50 mg once daily. Treatment dianabol dosage should be started simultaneously with the start of reception of GnRH analogue or surgical castration. In locally advanced prostate cancer: 150 mg once a day. dianabol dosage should take a long time, for at least 2 years. If signs of progression of the disease taking the drug should be discontinued. Violations nochek function: Dosage adjustment is not required. Violations of the liver: in mild disturbance of function of the liver dose adjustment is required. In patients with moderate and severe hepatic impairment increased accumulation of dianabol dosage can be observed.
The pharmacological action of dianabol dosage may condition the following side effects:
- very common (> 10%): gynecomastia (may persist even after the cessation of therapy, particularly in the case of taking the drug for a long time), thoracic pain glands, “tides” of blood to the face;
- frequent (> 1% and <10%): diarrhea, nausea, transient increase in activity of “liver” transaminases, cholestasis and jaundice (described liver function changes are rarely rated as serious, they were transient in nature, completely disappeared or decreased with continued therapy or after cancellation drug), pruritus, asthenia; when use of the drug in a daily dose of 150 mg – alopecia or hair regrowth, decreased libido, sexual dysfunction, weight gain.
- rare (> 0.1% – <1%): hypersensitivity reactions, including angioedema and urticaria, interstitial lung disease; angina pectoris, prolongation of the interval QT, cardiac arrhythmias; when use of the drug in a daily dose of 150 mg – abdominal pain, depression, dyspepsia, hematuria.
- very rarely (> 0.01% – <0.1%): vomiting, dry skin (when using the drug in a daily dose of 150 mg of dry skin occurs often), liver failure (causal connection with taking dianabol dosage significantly is not installed) thrombocytopenia.
With simultaneous use of dianabol dosage and GnRH analogues can also experience the following adverse events with a frequency of> 1% (causal connection with taking the drug is not installed, some of the noted side effects occurred in elderly patients): Since the cardiovascular system: heart failure. From the digestive system: anorexia, dry mouth, dyspepsia, dysphagia, constipation, flatulence. From the nervous system: dizziness, headache, insomnia, somnolence. respiratory system: shortness of breath. From the urinary system: nocturia, urinary infections tract, dysuria, urinary retention, urinary frequency, polyuria, hydronephrosis. From the hematopoietic system: anemia, leukopenia. On the part of the skin and its appendages: alopecia, rash, sweating, hirsutism. From the laboratory parameters: hyperglycemia, increased activity of “liver” transaminases. Other: abdominal pain, chest pain, pelvic pain, back pain, decreased or increased body weight, edema, diabetes, fever.
Cases of overdose have not been described in humans. There is no specific antidote. Treatment is symptomatic. Dialysis is not effective, since dianabol dosage is closely associated with proteins and excreted by the kidneys unchanged. Shown general supportive treatment and monitoring of vital body functions.
Interaction with other medicinal products
There are no data on the pharmacokinetic or pharmacodynamic interactions between dianabol dosage and GnRH analogues.
In in vitro studies have shown that (11) enantiomer of dianabol dosage inhibit CYP ZA4, to a lesser extent affecting the activity of CYP 2C9, 2C19 and 2D6. Potential to dianabol dosage for interaction with other drugs has been detected, but using dianabol dosage for 28 days to patients receiving midazolam, area under the curve “concentration-time» (AUC) midazolam is increased by 80%.
Incompatible with terfenadine, astemizole, cisapride.
caution must be exercised in the appointment of dianabol dosage together with cyclosporine or calcium channel blockers. You may need to decrease the dose of these drugs, particularly in the case or potentiation of side effects. After the start of the use or withdrawal of dianabol dosage is preferably carried out careful monitoring of cyclosporin plasma concentrations and the clinical condition of the patient.
The simultaneous use of dianabol dosage and drugs that inhibit microsomal oxidation of drugs, such as cimetidine or ketoconazole may increase dianabol dosage concentration in blood plasma and possibly to increase the incidence of adverse effects. It enhances the effect of coumarin anticoagulants, including warfarin (competition for protein binding).
Given the possibility of slowing down excretion of dianabol dosage in patients with impaired hepatic function it is advisable to periodically assess liver function. Most of the changes of liver function occur in the first six months of treatment with dianabol dosage.
In the case of pronounced changes in hepatic function receiving the drug should be discontinued. In patients with disease progression on higher levels of prostate-specific antigen (PSA) should consider stopping treatment dianabol dosage.
In the appointment of dianabol dosage in patients receiving coumarin anticoagulants should regularly monitor the prothrombin time. Given the possibility of dianabol dosage inhibiting the activity of cytochrome P450 (CYP ZA4), caution should be exercised with concomitant administration of dianabol dosage with drugs primarily metabolized by the CYP ZA4.
Effects on ability to drive vehicles and management mechanisms
In the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and psychomotor speed reactions.
tablets covered with a foil cover, 50 mg and 150 mg. On 14 tablets in blisters of PVC film and aluminum foil. On 2 blisters with instruction on use are placed in a pile of cardboard.
on blister indicate the number of production licenses and a trademark of the manufacturer, in Russian indicate the name of the drug, dosage form, dosage, lot number, production date, shelf life «in bulk».
The label on the box and the boxes indicate the number of production licenses and trade the manufacturer’s mark on the Russian and English languages indicate the manufacturer, address, country, name of the drug, dosage form, dosage, name and content of active substances in one tablet, storage conditions, batch number, production date, shelf life, ” just for packaging “, the number of tablets in a blister, the number of blisters. When packing at CJSC “Skopinsky pharmaceutical plant” and CJSC “MAKIZ PHARMA”, Russian.
On the pack and the label for packaging in Russian indicate pre-acceptance of the manufacturer, his trademark, country, name of the company in charge of the packaging, its trade sign, address, phone / fax, the owner of the registration certificate, his trademark, address, phone / fax number, drug name, dosage form, dosage, name and content of active substances in one tablet, the number of tablets in the package, the storage conditions, “Apply for doctor’s prescription “,” Keep out of the reach of children “, the batch number, manufacturing date (corresponding to« in bulk »the date of manufacture of the drug), the expiry date. On the bundle further indicate dispensing conditions, method of application, registration number, pharmacotherapy-matic group, a bar code, “Contains lactose monohydrate.” In the group the package label indicates the number of additional packages.