The antitumor effect of the drug at therapeutic doses in treatment of hormone-dependent malignancies may be associated with its effects on hypothalamic-pituitary-gonadal system estrogen and progestin receptors and steroid metabolism at the cellular level.
Proviron buy as progesterone exerts pyrogenic effect. At very high doses used for the treatment of certain cancers (500 mg per day and above), corticosteroid activity can be observed.
After oral administration of MPA is rapidly absorbed from the gastrointestinal tract, maximum values of plasma concentration observed after about 2-4 hours. When taking the drug every day 1 time per day a constant concentration in the blood plasma is reached after about 10 days. After oral administration of medroxyprogesterone excretion is characterized by bi- or tri-exponential pharmacokinetics. Terminal half-life of about 30-60 hours.
With simultaneous food intake is increased bioavailability, while the half-life remains unchanged.
90% IPA is a blood protein-bound state (mainly albumin). IPA is not bound to a specific globulin, sex hormone binding. Unbound IPA also has pharmacological activity. MPA is excreted in the faeces by biliary secretion, as well as largely metabolized with participation of cytochrome P450 in the liver microsomes ZA4 by hydroxylation followed by conjugation. Currently at least 16 known metabolites of MPA. Most of the metabolites excreted in the urine as glucuronides and only a small part – in the form of sulphates.
The volume of distribution of 20 l + 3. IPA penetrates the blood-brain barrier and into breast milk.
- Relapses and / or metastatic endometrial cancer.
- Relapses and / or metastatic hormone-dependent forms of breast cancer.
- Relapses and / or metastatic renal cell carcinoma.
- Metastatic prostate cancer.
- The syndrome of anorexia and cachexia.
- Increased sensitivity to MPA or any other component of the formulation.
- Bleeding from the genital tract of unknown origin.
- Severe liver dysfunction.
- Pregnancy and lactation.
Dosing and Administration
Inside. Tablets should proviron buy be taken during or immediately after a meal, not liquid, squeezed water. If necessary, tablets can crush.
- breast cancer in postmenopausal women: at 400-1500 mg / day.
- Endometrial cancer and kidney cancer: at 100-600 mg / day.
- Metastatic Prostate Cancer: 100-500 mg / day.
- Anorexia and cachexia syndrome: 1000 mg / day.
With the genitourinary system: dysfunctional uterine bleeding (irregular, copious, scanty), amenorrhea, changes in cervical secretions, cervical erosion, prolonged anovulation, libido changes.
On the part of the central nervous system: confusion, depression, dizziness, euphoria, increased fatigue, headache, insomnia, decreased ability to concentrate, increased nervous irritability, drowsiness, visual disturbances.
From the digestive system: constipation, diarrhea, dry mouth, abnormal liver function, jaundice, nausea, vomiting, changes in appetite.
From endocrine system: galactorrhea, mammalgia, breast, or breast, the effects inherent corticosteroids (such as Cushing’s syndrome), impaired glucose tolerance, diabetic cataract, exacerbation of diabetes mellitus, glycosuria.
Cardio-vascular system: stroke, myocardial infarction, chronic heart failure, high blood pressure, feeling of palpitations, pulmonary embolism, thrombosis of the retinal vessels, tachycardia, thromboembolic disorders, thrombophlebitis.
From hemopoiesis system: an increase in the number of white blood cells and platelets in the blood.
Skin and skin appendages: Acne, alopecia, hirsutism, pruritus, rash, urticaria. Immune system: Hypersensitivity reactions (anaphylaxis and anaphylactoid reactions, angioedema).
Other: edema / fluid retention, hypercalcemia, pyrexia, weight change, malaise, adrenergic effects (such as tremor, sweating, leg cramps at night).
application is very high doses may cause a variety of symptoms including weight gain (with some fluid retention), fatigue, and in some cases effects inherent corticosteroids.
In cases of overdose should stop using the product. No specific treatment is required.
Interaction with other medicinal products
In a joint application aminoglutethimide can significantly reduce the bioavailability of the drug Provera and thus reduce its efficiency.
The drug is used strictly for its intended purpose and under medical supervision.
- In the event of dysfunctional uterine bleeding, and the patient should be evaluated to find out their etiology.
- In the treatment of patients, the state of which can adversely affect the fluid retention in the body need to be cautious.
- When drug therapy is necessary to closely monitor the status of patients who have previously been treated for depression.
- In the treatment of patients with diabetes, should take into account the ability of the IPA to reduce glucose tolerance.
- If during treatment proviron buy with the drug is carried out cytological or histological examination of endometrial or cervical cancer, the pathologist must notify about the therapy.
- With the sudden partial or complete loss of vision, or the sudden development of exophthalmos, diplopia, migraine attacks should immediately stop taking the drug. In identifying the vascular tissue damage or edema of the optic nerve treatment with Provera should be abolished.
- Despite the fact that the causal relationship between the use of IPA and the development of thromboembolic disorders have been identified in patients with these disorders in history or in the event of them on the background of treatment should carefully assess the potential risks and benefits of the appointment, or deciding whether to continue treatment with Provera.
- It is shown that the use as a contraceptive IPA intramuscularly with 150 mg of 1 every 3 months in adult women of childbearing age and adolescent girls leads to a decrease in bone density (FCT) loin bones for 5 years, on average 5.4% and 4 and 2%, respectively, while for the first 2 years after the drug is partially restored bone. The largest decrease of PCT observed in the first 2 years of the drug.Reduction of estrogen concentrations in blood serum caused by the use of the drug leads to a decrease of PCT in women before menopause and may increase the risk of osteoporosis later in life.
- All patients treated with the drug Provera, are advised to take calcium supplements and vitamin D, and in some cases, long-term use – periodically measure.
- Some patients receiving revealed suppression of adrenocortical function (decrease and hydrocortisone in the blood).
- In laboratory studies should take into account that the use of may decrease the levels of the following endocrine biomarkers: a) Under the blood plasma and urine steroid (cortisol, estrogen, pregnandiol, progesterone, testosterone); b) gonadotropins in plasma and in urine; c) a specific binding globulin sex hormones;
- During the test metapironovogo neobhoimosti bear in mind that high doses of used in oncology, can cause partial adrenal insufficiency (decrease in the response of the pituitary-adrenal axis), so that before the introduction of metapyron necessary to test the ability of adrenal cortex to respond .