Androkur Depot
Androkur Depot: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Use in childhood
- 10. In case of impaired renal function
- 11. For violations of liver function
- 12. Use in the elderly
- 13. Drug interactions
- 14. Analogs
- 15. Terms and conditions of storage
- 16. Terms of dispensing from pharmacies
- 17. Reviews
- 18. Price in pharmacies
Latin name: Androcur Depot
ATX code: G03HA01
Active ingredient: cyproterone (Cyproterone)
Producer: Bayer AG (Germany)
Description and photo update: 2019-10-07
Androkur Depo is an antiandrogenic hormonal drug.
Release form and composition
The drug is produced in the form of an oily solution for intramuscular (i / m) administration: clear liquid from colorless to yellowish color (3 ml each in glass ampoules made of dark glass, 3 ampoules in a cardboard pallet, in a cardboard box 1 pallet and instructions for the use of Androkur Depot).
1 ml of solution contains:
- active substance: cyproterone acetate - 100 mg;
- auxiliary components: benzyl benzoate, castor oil.
Pharmacological properties
Pharmacodynamics
Androkur Depo is an antiandrogenic hormonal drug that has a gestagenic and antigonadotropic effect. Its active substance - cyproterone - competitively inhibits the influence of androgens on their target organs, suppressing androgenic stimulation of prostate tissue. Possessing a central antigonadotropic effect, it helps to reduce the synthesis of testosterone in the testes and its concentration in the blood serum.
The use of cyproterone in men causes effects such as inhibition of potency, libido and testicular function, which are reversible and completely disappear after stopping treatment.
The results of standard preclinical studies of cyproterone toxicity indicate the absence of any specific risk to the human body when Androkur Depo is administered for a long period.
Pharmacokinetics
After intramuscular (i / m) administration, cyproterone is released slowly and completely, its absolute bioavailability is considered complete. The maximum plasma concentration is reached after 2–3 days and is 180 ± 54 ng / ml. The half-life (T 1/2) is approximately 3 to 5 days. The total clearance of cyproterone from serum is 1.4 to 4.2 ml / min / kg.
Binding to proteins (albumin) of blood plasma is up to 96%, in a free form in the blood is only 3.5-4% of the administered dose. The change in the level of SHBG (globulin that binds sex hormones) as a result of the nonspecific connection of cyproterone with plasma proteins does not affect the pharmacokinetics of the drug.
Due to the fact that in the final phase of the distribution of T 1/2 of cyproterone from blood plasma is long, we can assume its cumulation against the background of the introduction of repeated doses. The equilibrium concentration is reached approximately 35 days after the administration of the first dose of Androkur Depot.
Cyproterone is metabolized by hydroxylation and conjugation. In blood plasma, the main metabolite is 15β-hydroxy derivative. The catalyst of the first phase of metabolism is mainly the cytochrome P 450 CYP3A4 isoenzyme.
With urine and bile, the main part of the administered dose is excreted in the form of metabolites, only small amounts are excreted in the bile unchanged.
Indications for use
- inoperable prostate cancer;
- increased sex drive in men with sexual deviations.
Contraindications
Absolute:
- liver disease (including Rotor syndrome, Dubin-Johnson syndrome);
- a history of neoplasms in the liver or at present (except for metastases of prostate cancer to the liver);
- cachexia (except for cachexia in prostate cancer);
- severe chronic depression;
- meningioma, including history;
- thromboembolism and thrombosis;
- age up to 18 years;
- hypersensitivity to the components of Androkur Depot.
In addition, it is contraindicated to use the drug for the treatment of increased sex drive in men with sexual abnormalities with functional disorders of the liver, severe diabetes mellitus with angiopathy, sickle cell anemia, thromboembolism and a history of thrombosis.
It is recommended to use Androkur Depo with caution in patients with diabetes mellitus, with glucose-galactose malabsorption syndrome, milk sugar intolerance, lactase deficiency.
In the treatment of inoperable prostate cancer, be careful and prescribe Androkur Depot only after an individual assessment of the benefit-risk ratio should be in patients with a history of thrombosis and thromboembolism, sickle cell anemia, severe diabetes mellitus with angiopathy.
Androkur Depot, instructions for use: method and dosage
The oil solution is intended exclusively for intramuscular administration. Androkura Depot injections should be done deeply and very slowly. This is due to the fact that as a result of pulmonary embolism with an oil solution, in some cases, cough, shortness of breath, chest pain and other symptoms may occur, including vasovagal reactions in the form of malaise, dizziness, increased sweating, paresthesia, or fainting. These reactions are reversible, their development is possible both during the injection and immediately after it. Oxygen inhalation is commonly used as maintenance therapy.
Do not allow intravascular administration of the drug.
Recommended dosage:
- inoperable prostate cancer: 300 mg 1 time in 7 days. The doctor determines the duration of treatment individually. It is not recommended to interrupt the course of treatment or reduce the dose of Androkur Depo after improvement of the condition or achievement of remission;
- reduction of increased sex drive in men with sexual deviations: 300 mg 1 time in 10-14 days. In exceptional cases, when the desired clinical effect is absent against the background of the usual dose, it is possible to use a dose of 600 mg 1 time in 10-14 days, which is preferable to inject 300 mg into each buttock. After achieving a satisfactory response to therapy, an attempt should be made to reduce the dose of the drug by gradually increasing the interval between injections. A stable effect is achieved when Androkur Depot is used for a long time against the background of simultaneous psychotherapy.
In renal failure and in elderly patients, dose adjustment is not required.
In patients with hepatic insufficiency, the use of Androkur Depo is possible only after the normalization of liver parameters.
Side effects
When using Androkur Depo, the following adverse reactions were recorded (criteria for assessing the incidence: very often - ≥ 10%; often - from ≥ 1% to <10%; infrequently - from ≥ 0.1% to <1%; rarely - from ≥ 0, 01% to <0.1%; very rarely - <0.01%; frequency not established - according to the reports, it is not possible to establish the frequency of occurrence of adverse reactions):
- from the hematopoietic system: frequency not established - anemia;
- from the side of the vessels: the frequency is not established - vasovagal reactions, oily microembolism of the pulmonary artery, thrombosis, thromboembolism;
- from the respiratory system: often - shortness of breath;
- from the immune system: rarely - hypersensitivity reactions;
- on the part of the genitals and mammary glands: very often - a reversible decrease in libido, suppression of spermatogenesis, impotence; often - gynecomastia;
- from the gastrointestinal tract: frequency unknown - intra-abdominal bleeding;
- on the part of the hepatobiliary system: often - liver failure, jaundice, hepatitis;
- on the part of the musculoskeletal system: frequency not established - osteoporosis;
- mental disorders: often - depressed mood, temporary feeling of anxiety, depression;
- dermatological reactions: infrequently - skin rash;
- others: often - increased fatigue, increased sweating, increase or decrease in body weight, hot flashes; very rarely - the development of benign or malignant neoplasms in the liver; frequency not established - meningioma.
Overdose
Overdose symptoms have not been established. The results of the acute toxicity study allow us to conclude that after a single use of a high dose of the drug, several times higher than the therapeutic dose, the risk of acute intoxication is unlikely.
When revealing the facts of Androkur Depot overdose, it is recommended to provide the patient with careful observation, if necessary, prescribe symptomatic therapy. There is no specific antidote.
special instructions
Treatment with Androkur Depot should be accompanied by a regular assessment of the functional state of the liver and adrenal cortex, and peripheral blood tests.
In men, the most frequently observed side effects during treatment with the drug include a decrease in sex drive and potency, suppression of the function of the gonads. In addition, the development of gynecomastia, accompanied by high tactile sensitivity and soreness of the nipples, is possible. These phenomena are reversible and, after discontinuation of therapy, pass on their own, including a gradual restoration of spermatogenesis.
Against the background of the use of cyproterone acetate at a dose of 100 mg and above, there were cases of hepatotoxicity in the form of the development of jaundice, liver failure, hepatitis, including fatal ones. More often, death was observed in men with advanced stage prostate cancer. The likelihood of developing toxicity depends on the dose of the drug; after the start of therapy, symptoms of toxicity may occur within a few months. If any symptoms of hepatotoxicity appear, a liver function test should be performed. If the suspicion is confirmed, then therapy is recommended to be canceled. If pathological processes in the liver are caused by metastases or other reasons not related to taking the drug, then after assessing the ratio of the expected effect and potential risk, treatment can be continued.
Along with hepatotoxicity, the most serious side effects include the development of benign and, less often, malignant liver tumors that can cause intra-abdominal bleeding and the appearance of thromboembolic processes. In this regard, the differential diagnosis of acute upper abdominal pain, liver enlargement, or signs of acute intra-abdominal bleeding should take into account possible liver tumor.
During the period of application of Androkur Depot, the risk of thromboembolic complications in patients with advanced stages of malignant diseases, with a history of cerebrovascular accidents, deep vein thrombosis, pulmonary embolism, myocardial infarction and other previous thrombotic or thromboembolic pathologies of arteries or veins increases.
Due to the fact that high doses of Androkur Depo have a corticoid-like effect and can suppress the function of the adrenal glands, during the period of treatment it is necessary to regularly monitor the function of the adrenal cortex.
It is recommended to avoid drinking alcohol during the treatment of increased sex drive in sexual dysfunctions, since the effect of the drug may decrease.
Influence on the ability to drive vehicles and complex mechanisms
During the treatment with Androkur Depot, caution is required when engaging in potentially hazardous activities, the implementation of which requires a high concentration of attention and quick psychomotor reactions, including driving.
Pediatric use
Information about the efficacy and safety of Androkur Depo in children and adolescents is insufficient, therefore, the drug should not be prescribed to a patient under 18 years of age.
It should be borne in mind that the use of cyproterone acetate before the end of puberty is associated with a high risk of its adverse effects on growth and the unstable endocrine system of the child.
With impaired renal function
In renal failure, dose adjustment of Androkur Depot is not required.
For violations of liver function
The appointment of Androkur Depo is contraindicated in liver diseases (including Rotor syndrome, Dubin-Johnson syndrome) and the presence of neoplasms in the liver in history or at the present time (with the exception of metastases of prostate cancer to the liver).
Use in the elderly
In elderly patients, dose adjustment of Androkura Depot injections is not required.
Drug interactions
- clotrimazole, ketoconazole, itraconazole, ritonavir and other drugs that are strong inhibitors of the CYP3A4 isoenzyme: inhibit the metabolism of cyproterone acetate;
- rifampicin, phenytoin, St. John's wort preparations and other inducers of the isoenzyme CYP3A4: can reduce the concentration of cyproterone acetate in plasma;
- statins: taking HMG-CoA reductase inhibitors (3-hydroxy-3-methylglutaryl coenzyme A reductase) increases the risk of myopathy and rhabdomyolysis;
- oral hypoglycemic agents, insulin: in patients with diabetes mellitus, dose adjustment of antidiabetic agents may be required.
The results of in vitro studies indicate a possible inhibition of the following isoenzymes of the cytochrome P 450 system during treatment with high therapeutic doses of cyproterone acetate (300 mg per day): CYP3A4, 2C8, 2C9, 2C19 and 2D6.
Analogs
Androkur Depot analogs are Androkur, Cyproteron-Teva.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
The shelf life is 5 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Androkur Depot
The few reviews about Androkur Depo are controversial. There are reports that long-term use of the drug for inoperable prostate cancer is well tolerated and allows maintaining normal levels of prostate specific antigen. Other patients prefer the tablet form of cyproterone.
Price for Androkur Depot in pharmacies
The price for Androkur Depot for a package containing 3 ampoules of solution can be 1863-1946 rubles.
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
