Primary Information
Clinical-pharmacological group
15.052 (progestin - depot form. Anticancer drug)
In the beginning of
Form of production, composition and packaging
Suspension for injection of white color.
1 fl.
medroxyprogesterone acetate 500 mg
Excipients: polyethylene glycol 3350, polysorbate 80, sodium chloride, methylparaben, propylparaben, water d / and.
3.3 ml vials (1) - packs cardboard.
Suspension for injection of white color.
1 fl.
medroxyprogesterone acetate 1 g
Excipients: polyethylene glycol 3350, polysorbate 80, sodium chloride, methylparaben, propylparaben, water d / and.
6.7 ml vials (1) - packs cardboard.
In the beginning of
Pharmacological action
Anticancer drug. Depo-Provera is gestagenom, do not possess estrogenic activity, its androgenic activity is considered to be minimal.
In appropriate doses suppresses the secretion of pituitary gonadotropins, which in turn prevents the maturing follicles, causing anovulation in women of childbearing age.
In addition, the drug in the relevant doses suppress the function of cells of Leydig in men, ie endogenous formation of testosterone.
In high doses has antitumor effect in hormone-malignant neoplasms. This effect of the drug due to its effects on the hypothalamic-pituitary-gonadal system, the receptors progestins and estrogen and metabolism steroids on the cellular level.
The drug has pyrogenic action, in very high doses of corticosteroid has activity.
In the beginning of
The Pharmacokinetics Of
Absorption
After the / m introduction of the drug is absorbed slowly, with the result that the long-term is in constant concentrations of medroxyprogesterone acetate. Cmax in blood plasma is achieved through 4-20 days after the / m introduction.
The Distribution Of
Binding to plasma proteins is 90-95%. Medroxyprogesterone acetate penetrates through hematoencephalic barrier, excreted in breast milk. Accumulate in the body, residual concentrations of medroxyprogesterone acetate is found in the plasma through 7-9 months.
Metabolism
Medroxyprogesterone acetate is metabolized in the liver. Currently described many metabolites medroxyprogesterone acetate.
Excretion
The most part of medroxyprogesterone acetate is displayed by biliary secretion with faeces. Approximately 44% of the drug is excreted in unchanged form in the urine. T1 / 2 is 6 weeks.
In the beginning of
Dosage
If endometrial cancer and cancer of the kidney initial dose of 400-1000 mg per week / m. If in the course of several weeks or months of improvement and achieved stabilization of the process, the prescribed maintenance therapy in the dose of 400 mg per month.
In breast cancer, the drug is prescribed in the / m in a dose of 500 mg / day for 28 days. Then apply the supporting dose of 500 mg two times a week. Treatment should continue until the appearance of signs of disease progression.
Directly before using bottle should stir well to the input of the drug has become the type of a homogeneous suspension.
In the beginning of
Overdose
Symptoms: increased body mass (with some delay fluid), increased fatigue, and in some cases are observed effects characteristic of glucocorticoids.
Discontinue use of the drug. Specific treatment is not required.
In the beginning of
Drug interaction
Drug interactions drug Depo-Provera is not described.
In a joint application aminoglutethimide can significantly reduce the bioavailability of medroxyprogesterone acetate.
In the beginning of
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation.
In the beginning of
Side effects of the
Allergic reactions: anaphylaxis and anaphylactoid reactions, urticaria.
From the blood coagulation system: thromboembolism, thrombophlebitis.
Central nervous system: increased nervous anxiety, insomnia, drowsiness, fatigue, depression, dizziness, headache.
Dermatological reactions: itching, rash, acne, girsutizm, alopecia.
On the part of the reproductive system: dysfunctional uterine bleeding, bleeding from the genital tract, amenorrhea, decrease of libido or anorgasmia, vaginitis, beli, hot flashes, pain in the lower abdomen, pain mammary glands, galactorrhea.
From the digestive system: pain or discomfort in the abdomen, nausea, flatulence.
From the musculoskeletal system: convulsions gastrocnemius muscles, pain in the back and joints.
Other: asthenia, pyrexia, the change in mass of body and moon face.
In the beginning of
Terms and conditions of storage
The preparation should be stored at room temperature (20-25 degrees C), in the places inaccessible to children. Shelf life - 5 years.
In the beginning of
Indications
- Recurrent and / or metastatic endometrial cancer;
- Hormone-dependent form of recurrent breast cancer for women in menopause;
- Recurrent and / or metastatic kidney cancer.
In the beginning of
Contraindications
- Pregnancy;
- The period of lactation;
- Increased sensitivity to components of the preparation.
In the beginning of
Special instructions
Before the appointment of the drug Depo-Provera, a thorough examination of the patient.
If you experience signs and / or symptoms of thromboembolism in front of the continuation of the application of the preparation it is necessary to weigh the risks and benefits.
When the background of the reception of the drug in high doses symptom complex Itsenko-Kushinga (moon face, fluid retention, reduced tolerance to glukoze, the AD) measures should be taken to reduce the dose of exercise and careful monitoring of the patient's condition.
The use of the drug in high doses may cause an increase in body weight and fluid retention. In connection with this, caution should be exercised in the treatment of patients, the condition of which could adversely affect body weight gain or fluid retention.
You should carefully observe patients in history where there are instructions on the treatment of the depressive state. During therapy with Depo-Provera some patients complain of depression, similar premenstrual.
In carrying out cytological or histological endometrial or cervical should warn the histology of the conducted therapy.
The drug should be used with caution in the postpartum period in connection with an increased risk of heavy and prolonged uterine bleeding.
It is believed that use of the drug Depo-Provera may increase the risk of developing osteoporosis.
Should discontinue use of the drug in a sudden partial or complete loss of vision, or if the development of exophthalmus, ghost in the eyes, migraines. If during an examination revealed damage of vessels fiber or swelling of the nipple of the optic nerve, also do not use the drug Depo-Provera.
With the development of jaundice should discontinue use of the drug.
Use of the drug can have an influence on the results of the laboratory research: determining the levels of gonadotropins (downward); determination of the levels in the blood plasma progesterone, cortisol, estrogens (downward); determination of the level of pregnandiola in the urine (in the direction of reducing); determination of the level of testosterone in the plasma of blood (downward); determination of the level of specific binding globulin sex hormones (downward); carrying out the test with sugar load (tolerance test to glukoze ) metapironovy test; may change the test results for prothrombin (factor II) and the factors of blood clotting (VII, VIII, IX, X (upward); increases the importance of the functions of the liver.
In the beginning of
The application in violation of the liver
With the development of jaundice should discontinue use of the drug.
In the beginning of
Dispensing conditions
The drug is sold by prescription.
In the beginning of
Registration numbers
* Susp. d / in / m of 1 g/6.7 ml: limit. 1 pcs. P # 013671/01 (2029-12-06 - 2029-12-11)
* Susp. d / in / m injection of 500 mg/3.3 ml: limit. 1 pcs. P # 013671/01 (2029-12-06 - 2029-12-11)
15.052 (progestin - depot form. Anticancer drug)
In the beginning of
Form of production, composition and packaging
Suspension for injection of white color.
1 fl.
medroxyprogesterone acetate 500 mg
Excipients: polyethylene glycol 3350, polysorbate 80, sodium chloride, methylparaben, propylparaben, water d / and.
3.3 ml vials (1) - packs cardboard.
Suspension for injection of white color.
1 fl.
medroxyprogesterone acetate 1 g
Excipients: polyethylene glycol 3350, polysorbate 80, sodium chloride, methylparaben, propylparaben, water d / and.
6.7 ml vials (1) - packs cardboard.
In the beginning of
Pharmacological action
Anticancer drug. Depo-Provera is gestagenom, do not possess estrogenic activity, its androgenic activity is considered to be minimal.
In appropriate doses suppresses the secretion of pituitary gonadotropins, which in turn prevents the maturing follicles, causing anovulation in women of childbearing age.
In addition, the drug in the relevant doses suppress the function of cells of Leydig in men, ie endogenous formation of testosterone.
In high doses has antitumor effect in hormone-malignant neoplasms. This effect of the drug due to its effects on the hypothalamic-pituitary-gonadal system, the receptors progestins and estrogen and metabolism steroids on the cellular level.
The drug has pyrogenic action, in very high doses of corticosteroid has activity.
In the beginning of
The Pharmacokinetics Of
Absorption
After the / m introduction of the drug is absorbed slowly, with the result that the long-term is in constant concentrations of medroxyprogesterone acetate. Cmax in blood plasma is achieved through 4-20 days after the / m introduction.
The Distribution Of
Binding to plasma proteins is 90-95%. Medroxyprogesterone acetate penetrates through hematoencephalic barrier, excreted in breast milk. Accumulate in the body, residual concentrations of medroxyprogesterone acetate is found in the plasma through 7-9 months.
Metabolism
Medroxyprogesterone acetate is metabolized in the liver. Currently described many metabolites medroxyprogesterone acetate.
Excretion
The most part of medroxyprogesterone acetate is displayed by biliary secretion with faeces. Approximately 44% of the drug is excreted in unchanged form in the urine. T1 / 2 is 6 weeks.
In the beginning of
Dosage
If endometrial cancer and cancer of the kidney initial dose of 400-1000 mg per week / m. If in the course of several weeks or months of improvement and achieved stabilization of the process, the prescribed maintenance therapy in the dose of 400 mg per month.
In breast cancer, the drug is prescribed in the / m in a dose of 500 mg / day for 28 days. Then apply the supporting dose of 500 mg two times a week. Treatment should continue until the appearance of signs of disease progression.
Directly before using bottle should stir well to the input of the drug has become the type of a homogeneous suspension.
In the beginning of
Overdose
Symptoms: increased body mass (with some delay fluid), increased fatigue, and in some cases are observed effects characteristic of glucocorticoids.
Discontinue use of the drug. Specific treatment is not required.
In the beginning of
Drug interaction
Drug interactions drug Depo-Provera is not described.
In a joint application aminoglutethimide can significantly reduce the bioavailability of medroxyprogesterone acetate.
In the beginning of
Pregnancy and lactation
The drug is contraindicated during pregnancy and lactation.
In the beginning of
Side effects of the
Allergic reactions: anaphylaxis and anaphylactoid reactions, urticaria.
From the blood coagulation system: thromboembolism, thrombophlebitis.
Central nervous system: increased nervous anxiety, insomnia, drowsiness, fatigue, depression, dizziness, headache.
Dermatological reactions: itching, rash, acne, girsutizm, alopecia.
On the part of the reproductive system: dysfunctional uterine bleeding, bleeding from the genital tract, amenorrhea, decrease of libido or anorgasmia, vaginitis, beli, hot flashes, pain in the lower abdomen, pain mammary glands, galactorrhea.
From the digestive system: pain or discomfort in the abdomen, nausea, flatulence.
From the musculoskeletal system: convulsions gastrocnemius muscles, pain in the back and joints.
Other: asthenia, pyrexia, the change in mass of body and moon face.
In the beginning of
Terms and conditions of storage
The preparation should be stored at room temperature (20-25 degrees C), in the places inaccessible to children. Shelf life - 5 years.
In the beginning of
Indications
- Recurrent and / or metastatic endometrial cancer;
- Hormone-dependent form of recurrent breast cancer for women in menopause;
- Recurrent and / or metastatic kidney cancer.
In the beginning of
Contraindications
- Pregnancy;
- The period of lactation;
- Increased sensitivity to components of the preparation.
In the beginning of
Special instructions
Before the appointment of the drug Depo-Provera, a thorough examination of the patient.
If you experience signs and / or symptoms of thromboembolism in front of the continuation of the application of the preparation it is necessary to weigh the risks and benefits.
When the background of the reception of the drug in high doses symptom complex Itsenko-Kushinga (moon face, fluid retention, reduced tolerance to glukoze, the AD) measures should be taken to reduce the dose of exercise and careful monitoring of the patient's condition.
The use of the drug in high doses may cause an increase in body weight and fluid retention. In connection with this, caution should be exercised in the treatment of patients, the condition of which could adversely affect body weight gain or fluid retention.
You should carefully observe patients in history where there are instructions on the treatment of the depressive state. During therapy with Depo-Provera some patients complain of depression, similar premenstrual.
In carrying out cytological or histological endometrial or cervical should warn the histology of the conducted therapy.
The drug should be used with caution in the postpartum period in connection with an increased risk of heavy and prolonged uterine bleeding.
It is believed that use of the drug Depo-Provera may increase the risk of developing osteoporosis.
Should discontinue use of the drug in a sudden partial or complete loss of vision, or if the development of exophthalmus, ghost in the eyes, migraines. If during an examination revealed damage of vessels fiber or swelling of the nipple of the optic nerve, also do not use the drug Depo-Provera.
With the development of jaundice should discontinue use of the drug.
Use of the drug can have an influence on the results of the laboratory research: determining the levels of gonadotropins (downward); determination of the levels in the blood plasma progesterone, cortisol, estrogens (downward); determination of the level of pregnandiola in the urine (in the direction of reducing); determination of the level of testosterone in the plasma of blood (downward); determination of the level of specific binding globulin sex hormones (downward); carrying out the test with sugar load (tolerance test to glukoze ) metapironovy test; may change the test results for prothrombin (factor II) and the factors of blood clotting (VII, VIII, IX, X (upward); increases the importance of the functions of the liver.
In the beginning of
The application in violation of the liver
With the development of jaundice should discontinue use of the drug.
In the beginning of
Dispensing conditions
The drug is sold by prescription.
In the beginning of
Registration numbers
* Susp. d / in / m of 1 g/6.7 ml: limit. 1 pcs. P # 013671/01 (2029-12-06 - 2029-12-11)
* Susp. d / in / m injection of 500 mg/3.3 ml: limit. 1 pcs. P # 013671/01 (2029-12-06 - 2029-12-11)
