Androfarm (cyproterone) 100 mg/ml. 3 ml. ampoules N3

Androfarm (cyproterone) 100 mg/ml. 3 ml. ampoules N3

$152.00

Manufacturer: Ukraine

Hormones of the gonads and drugs used in the pathology of the genital area. Antiandrogens.

Code ATX G03H A01.

Androfarm is intended for use only by men.

Applicable:

  • to reduce sexual desire for sexual deviations;
  • for the palliative treatment of metastatic or locally advanced unresectable prostate cancer, if treatment with luteinizing releasing hormone (LRH) analogues or surgery is insufficient or contraindicated;
  • initially to reduce hot flashes, which may be caused by an increase in serum testosterone levels at the beginning of treatment with LHR agonists.

 

Category:

Description

Ingredients

active ingredient: cyproterone;

1 ml of the preparation contains cyproterone acetate 100 mg, calculated as 100% substance;

excipients: benzyl benzoate, castor oil.

Dosage form

Injection.

Basic physical and chemical properties: yellow or yellow-green oily liquid with a specific odor.

Pharmacotherapeutic group

Hormones of the gonads and drugs used in the pathology of the genital area. Antiandrogens.

Code ATX G03H A01.

Pharmacodynamics

Cyproterone acetate has antiandrogenic, gestagenic and antigonadotropic effects, confirmed in animal studies and the participation of volunteers.

Preclinical studies

Antiandrogenic action

Cyproterone acetate competitively inhibits the effect of androgens, which are formed endogenously and enter exogenously, on target organs. This leads to blockade of the translocation of the DHT receptor complex in the cell nucleus. The results of in vitro cell culture experiments conducted to test the effect of cyproterone acetate on androgen receptor function indicate a high antiandrogenic efficacy of cyproterone acetate. In addition, some in vitro test systems have shown a slight partial agonistic effect of cyproterone acetate on androgen receptors. Cyproterone acetate weakens or stops the stimulating effect of male sex hormones on androgen-dependent structures and functions: depending on the dose of cyproterone acetate in animals, it causes atrophy of the secondary sex glands. Affects testicular function: spermatogenesis is inhibited in a dose-dependent manner. As in humans, libido is inhibited in dogs, rabbits, pigs and monkeys due to the use of cyproterone acetate.

In rats, an obstruction or delay in the onset of puberty may occur. Cyproterone acetate inhibits the physiological closure of the bone growth zone and bone maturation.

The function of the sebaceous glands is disrupted, the thickness of the epidermis decreases.

Treatment of pregnant animals with cyproterone acetate results in impaired development of the male fetus. Affects testosterone-dependent differentiation processes, which leads to more or less pronounced feminization phenomena.

Gestagennoe action

The results of the Clauberg test (rabbits) showed that the effectiveness of cyproterone acetate after subcutaneous administration is 100 times greater than the effectiveness of progesterone. In rat progestogen tests, cyproterone acetate after subcutaneous administration is about as effective as progesterone.

Antigonadotropic action

Like all potent progestogens, cyproterone acetate has antigonadotropic properties, manifested in males by inhibition of testicular growth, and in females by inhibition of ovulation.

Clinical researches

Antiandrogenic action

Cyproterone acetate competitively inhibits the effect of androgens on target organs. In humans, the following interrelated conditions have been described:

inhibition of sexual desire, decreased activity of the sebaceous glands, effect on hair growth, delay in androgenic growth impulses in the prostate tissue, inhibition of premature pubertal development processes, as well as in bone tissue.

Gestagennoe action

Cyproterone acetate is a potent progestogen. According to the results of the Kaufman test, a total dose of 20-30 mg of the drug already leads to the transformation of the endometrium.

Antigonadotropic action

As a potent progestogen, cyproterone acetate has a depressant effect on the central nervous system. Due to this antigonadotropic action, there is no increase in the secretion of the reverse regulation of luteinizing hormone, although as a result of the antiandrogenic action of cyproterone acetate, androgens are displaced by the hypothalamic receptors, with which they have a negative feedback. Even more, the secretion of luteinizing and follicle-stimulating hormones is inhibited by the progestogenic effect of cyproterone acetate. As a result, the level of testosterone and estrogen in the blood serum decreases. This antigonadotropic effect in men is weakened, since the inhibitory effect of androgens is reduced due to the antiandrogenic components of the active substance that affect the hypothalamus.

Other effects on endocrine function

With the use of cyproterone acetate, the concentration of testosterone and estrogen decreases.

There was no significant effect on 17-ketosteroids and 17-ketogenic steroids. Cortisol secretion remains unchanged or decreased. The function of the hypothalamic-pituitary-adrenal axis in adults remains predominantly unchanged. Evaluation of all the results leads to the conclusion that the reactivity of the system, as a rule, is not damaged.

Indications

Androfarm is intended for use only by men.

Applicable:

  • to reduce sexual desire for sexual deviations;
  • for the palliative treatment of metastatic or locally advanced unresectable prostate cancer, if treatment with luteinizing releasing hormone (LRH) analogues or surgery is insufficient or contraindicated;
  • initially to reduce hot flashes, which may be caused by an increase in serum testosterone levels at the beginning of treatment with LHR agonists.

Contraindications

When used as a palliative therapy for advanced prostate cancer and initially to reduce heat influxes:

  • liver disease;
  • Dubin-Johnson syndrome, Rotor syndrome;
  • liver tumors, including a history (only in the case when the tumor is not caused by metastases of prostate cancer);
  • meningioma, including history;
  • established malignant diseases or suspicion of their presence (with the exception of progressive prostate cancer);
  • severe chronic depression;
  • thromboembolic events, including history;
  • hypersensitivity to the active substance or to any of the components of the drug;
  • children and adolescence until the end of puberty (see method of administration and dose).

When used to reduce sexual desire for pathological abnormalities in the genital area in men:

  • liver disease;
  • Dubin-Johnson syndrome, Rotor syndrome;
  • liver tumors, including or in history;
  • meningioma, including history;
  • established malignant diseases or suspicion of their presence;
  • severe chronic depression;
  • thromboembolic conditions, including history;
  • severe forms of diabetes mellitus with vascular complications;
  • sickle cell anemia;
  • hypersensitivity to the active substance or to any of the components of the drug;
  • children and adolescence until the end of puberty (see method of administration and dose).

Dosage and administration

Injections should be given very slowly. The drug is intended for intramuscular injection only. Care must be taken to ensure that the injected substance does not enter the vessel.

  • To reduce sexual desire for pathological abnormalities in the genital area in men.

Deviations in sexual behavior require treatment only in case of significant severity of the symptoms of this disease. A prerequisite for treatment is the desire of the patient to be treated.

The contents of one ampoule of the drug (3 ml) should be administered every 10-14 days as a deep intramuscular injection. In exceptional cases, if the effect of the treatment is insufficient, you can enter 2 ampoules every 10-14 days, preferably 3 ml (the contents of one ampoule) into the right and left gluteal muscle (M. glutaeus maximus).

To stabilize the therapeutic effect, it is necessary to use Androfarm for a long time and, if possible, simultaneously with psychotherapeutic measures.

After achieving a satisfactory therapeutic result, it is advisable to reduce the dose by gradually increasing the interval between injections. Dose reduction or discontinuation of the drug should occur gradually.

  • For the treatment of inoperable prostate cancer.

The contents of one ampoule of the drug (3 ml) should be administered weekly as a deep intramuscular injection.

With the improvement of the condition or remission of the disease, you should not change the prescribed dose or stop treatment.

  • Initially to reduce hot flashes.

The contents of one ampoule of Androfarm (300 mg) should be administered as a single deep intramuscular injection.

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