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Medroxyprogesterone Review


Medroxyprogesterone is a progestin, a female hormone that helps regulate ovulation and menstrual periods.

Contents:

Indications for use

  • Hormone-dependent forms of recurrent breast cancer in females in menopause (the second phase of menopause) as a palliative (not directed to the treatment of the underlying disease but relieving the patient’s condition);
  • Recurrent and/or metastatic (accompanied by the appearance of new tumors in other organs and tissues that develop due to the transfer of cancer cells to blood or lymph from the primary tumor);
  • Endometrial cancer (the inner shell of the uterus) as an additional and/or palliative treatment recurrent and/or metastatic kidney cancer as an additional and/or palliative treatment.

Mechanism of action

Medroxyprogesterone has a progestin action (similar to the action of the female sex hormone progesterone) and is deprived of androgenic (similar to the action of male sex hormones) and estrogenic (similar to the action of female sex hormones – estrogens) activity. In high doses, te medicine has antitumor effect with hormone-sensitive malignancies. It exerts pyrogenic (body temperature-enhancing) action, in large doses it has a corticosteroid (similar action of hormones of the adrenal cortex) activity.

Dosage and mode of application

Medroxyprogesterone dose is determined individually. It depends on the indications, the dosage form of the drug, the treatment regimen used for the particular patient. It is necessary to strictly observe the compliance of a certain drug form with indications for use.

The drug is used orally or intramuscularly.

  • Medroxyprogesterone pills are administered orally with endometrial cancer and kidneys from 200 to 600 mg per day, with breast cancer – from 400 to 1200 mg per day. The effect is usually observed in 8-10 weeks;
  • The medicine is used intramuscularly with endometrial cancer and kidney cancer, the initial dose is 500-1000 mg per week. If the patient’s condition improves in a few weeks or a month and the condition stabilizes, then a maintenance therapy of 500 mg per week is prescribed;
  • In breast cancer, the medicine is prescribed in an initial dose of 500 mg per day for 28 days. Then use maintenance doses of 500 mg twice a week. Treatment continues until the patient responds to treatment. The results of therapy with a hormonal form of breast cancer can be observed even after 8-10 weeks from the beginning of treatment. If the disease progresses, medroxyprogesterone therapy should be stopped.

Overdose:

The use of very high doses of medroxyprogesterone can cause a number of symptoms, including an increase in body weight (with some fluid retention), increased fatigue. In cases of overdose, discontinue using the drug. Specific treatment is not required.

Contraindications

Do not use medroxyprogesterone pills or suspension in the following cases:

  • hypersensitivity to the drug components;
  • pregnancy;
  • thrombophlebitis;
  • thromboembolic disease or stroke in history;
  • liver disease;
  • vaginal bleeding;
  • breast-feeding.

With caution:

  • thrombophlebitis,
  • thromboembolic complications,
  • severe violations of the liver,
  • hypercalcemia.

Before using the drug for the treatment of gynecological diseases and contraception, it is necessary to exclude the presence of a tumor of genital organs or mammary glands in the patient. If you undergo a pathohistological examination of certain organs and tissues, it is necessary to warn the histologist about the previous treatment with progestins.

Side effects

  • Genitourinary system: dysfunctional uterine bleeding (irregular, abundant, poor), amenorrhea, changes in cervical secretion, erosion of the cervix, prolonged anovulation, changes in libido;
  • Nervous system: confusion, depression, dizziness, euphoria, fatigue, headache, insomnia, decreased ability to concentrate, increased nervous excitability, drowsiness, visual disturbances;
  • Digestive system: constipation, diarrhea, dry mouth, abnormal liver function, jaundice, nausea, vomiting, changes in appetite;
  • Endocrine system: galactorrhea, mastodynia, tenderness of the breast or mammary glands, effects characteristic of corticosteroids (such as Cushing’s syndrome), decreased glucose tolerance, diabetic cataracts, exacerbation of diabetes mellitus, glucosuria;
  • Cardiovascular system: stroke, myocardial infarction, chronic heart failure, increased blood pressure, a feeling of a strong heartbeat, pulmonary embolism, retinal vascular thrombosis, tachycardia, thromboembolic disorders, thrombophlebitis;
  • Hematopoiesis system: an increase in the number of leukocytes and platelets in the blood;
  • Skin and skin appendages: acne, alopecia, hirsutism, itching, rash, urticaria. Immune system: hypersensitivity reactions (anaphylaxis and anaphylactoid reactions, angioneurotic edema);
  • Local reactions: pain, residual compaction, discoloration of the skin at the injection site;
  • Other: swelling/fluid retention in the body, hypercalcemia, hyperthermia, weight change, adrenergic effects (such as hand tremor, sweating, muscle cramps at night), decreased bone density (PCT).

Interactions

Aminoglutethimide reduces the plasma concentration of medroxyprogesterone acetate, which can lead to a decrease in its effectiveness.

What if I miss a dose?

Take the missed dose of medroxyprogesterone as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take additional medication to make up for the missed dose.

Medroxyprogesterone and pregnancy

Medroxyprogesterone is contraindicated in pregnancy and breastfeeding (it is necessary to stop). In some cases, there is a connection between the developmental disorders of the genitals in the fetus and the intrauterine exposure of progestogens in the first trimester of pregnancy. Newborns, with an unplanned pregnancy that occurred within 1 to 2 months after the administration of medroxyprogesterone, have a high risk of developing hypotrophy, which increases the possibility of neonatal and intrapartum mortality. If pregnancy occurred in the background of using medroxyprogesterone, the patient should be warned about the possible risk to the fetus.

Special instructions

The drug is used strictly according to prescription and under the supervision of a doctor.

With dysfunctional uterine bleeding, it is necessary to exclude uterine cancer and other organic lesions.

Care should be taken in the treatment of patients whose condition may be adversely affected by fluid retention in the body.

A doctor should carefully monitor the condition of patients who were previously treated for depression and are currently taking medroxyprogesterone.

When treating patients with diabetes mellitus, medroxyprogesterone is able to reduce glucose tolerance should be considered.

If the cytological or histological examination of the endometrium or cervix is performed against the background of the treatment, the pathologist should be warned about the therapy.

With sudden partial or complete loss of vision, or with the sudden development of exophthalmos, double vision, migraine attacks, the drug should be stopped immediately.

Although there has been no causal relationship between the use of medroxyprogesterone and the development of thromboembolic disorders in patients with these abnormalities in the history or when they occur against the background of treatment, the possible risk and benefit should be carefully assessed when initiating or deciding whether to continue treatment.

The use of medroxyprogesterone as a contraceptive intramuscularly at a dose of 150 mg once in 3 months in adult women of childbearing age and in adolescent girls leads to a decrease in PCT of the lumbar bones for 5 years on average by 5.4% and 4.2%, respectively. During the first 2 years after the cancellation of the drug, bone tissue is partially restored. The greatest decrease in PCT is observed in the first 2 years of using the hormonal preparation.

All patients who use medroxyprogesterone are recommended to take calcium and vitamin D preparations.

When conducting laboratory studies, it should be noted that the use of medroxyprogesterone can reduce the levels of the following endocrine biomarkers: steroids in blood plasma and urine (cortisol, estrogens, pregnanediol, progesterone, testosterone); gonadotropins in blood plasma and in urine (LH and FSH); specific globulin that binds sex hormones.

When conducting the metapyrone test, bear in mind that high doses of medroxyprogesterone used in oncology can cause partial adrenal insufficiency (a decrease in the response of the pituitary-adrenal system), so before the introduction of the metapyron, it is necessary to check the ability of the adrenal cortex to respond to ACTH.

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