Medroxyprogesterone has these effects on the human body

Medroxyprogesterone is a type of drug. Taking medroxyprogesterone will promote the body's progesterone and control the body's cells. Long-term use of medroxyprogesterone can have a contraceptive effect on women, and can also effectively improve and treat some female ovarian and uterine diseases, and can prevent cancer and other effects.

Medroxyprogesterone is a white or off-white crystalline powder, odorless. Insoluble in water, easily soluble in chloroform, slightly soluble in anhydrous ethanol. Melting point 202～208℃. The plasma concentration rises rapidly after either oral or intramuscular injection. The peak blood concentration after intramuscular injection is lower than that after oral administration, but the duration is longer, more than 1 week. It is mainly used to treat kidney cancer, breast cancer, endometrial cancer, prostate cancer, and to enhance the appetite, improve general condition and increase weight of patients with advanced cancer.

Pharmacological Action

Medroxyprogesterone is a strong progestin with no estrogenic activity. After oral or injection, based on the appropriate amount of endogenous estrogen in the body, the proliferative endometrium can be transformed into secretory endometrium, preparing for the implantation of the fertilized egg. Its progestin activity is 20 to 30 times that of progesterone when injected subcutaneously and 10 to 15 times that of ethinyl progesterone when taken orally. Its main function is to promote the proliferation and secretion of the endometrium, complete the preparation for conception, and protect the safe growth of the fetus; it also has the effects of changing the menstrual cycle, enhancing the consistency of cervical mucus, and inhibiting ovulation. Large doses of medroxyprogesterone have anti-tumor effects and can also significantly increase patients' appetite and relieve pain. Medroxyprogesterone has an effect against estrogen, but does not oppose the beneficial effects of estrogen on lipoproteins, nor does it have a significant androgenic effect, making it the closest to natural progesterone. It mainly increases the viscosity of cervical mucus. Large doses can inhibit pituitary gonadotropin and thus inhibit ovulation, and have a long-lasting anti-fertility effect. When medroxyprogesterone is used as an anti-tumor hormone, years of experimental and clinical studies have shown that this type of preparation can have a dual effect, which is related to the dose.

1. Inhibit the anterior pituitary through negative feedback, thereby inhibiting the production of luteinizing hormone (LH), adrenocorticotropic hormone (ACTH) and other growth factors.

2. High-dose irradiation has a direct cytotoxic effect on sensitive cells. Medroxyprogesterone mainly counteracts the effect of estrogen in promoting tumor cell growth by preventing the renewal of estrogen receptors (ER) in cells, but has no such effect on drug-resistant cells. Pathological examination of endometrial cancer can reveal chromosomal damage. Medroxyprogesterone can also reduce the level of intracellular estrogen by enhancing the activity of E2-deoxygenase, inducing liver 5α-reductase to prevent androgens from being converted into estrogen, etc.

Pharmacokinetics

The average oral absorption rate is 5.7%, the bioavailability of intraperitoneal injection is better than that of oral and intramuscular injection, and it is well tolerated. The plasma half-life is 4 to 5 hours. After intramuscular injection, it is stored in local tissues and slowly released, producing a long-lasting effect that can last for more than 2 to 4 weeks, and up to 3 months at higher doses. After oral administration, it is metabolized by the liver and excreted mainly in the urine in the form of sulfate and glucuronide within 1 to 2 days. It is secreted in breast milk. Drug metabolism varies greatly from person to person.

Indications

1. Large doses can be used as long-term contraception. It is commonly used clinically for dysmenorrhea, functional amenorrhea, dysfunctional uterine bleeding, threatened abortion or habitual abortion, endometriosis, etc.

2. Large doses can also be used to treat renal cell carcinoma, breast cancer, endometrial cancer, prostate cancer, and to enhance appetite, improve general condition and increase weight in patients with advanced cancer.

Contraindications

Medroxyprogesterone is contraindicated in patients with thrombophlebitis, thromboembolism, stroke, severe hepatic or renal insufficiency, known or suspected breast or genital malignancy, hypercalcemia, missed abortion, uterine bleeding, pregnancy, coagulopathy, or hypersensitivity to medroxyprogesterone [2].

Precautions

1. Use with caution in patients with depression.

2. A comprehensive physical examination (especially breast and pelvic examination) should be performed before treatment. Long-term medication requires liver function checks, with special attention to breast examinations.

3. Progesterone can cause a certain degree of fluid retention, and epilepsy, migraine, asthma, etc. should be closely observed.

4. If there are signs of thrombosis during the use process, such as sudden visual impairment, diplopia, and migraine, you should be checked immediately. If optic disc edema or retinal vascular disease occurs, the drug should be discontinued immediately.

5. For long-term administration of medroxyprogesterone, the date of use should be calculated according to a 28-day cycle.

6. Women who use medroxyprogesterone for a long time should not smoke.

7. When taking large doses (more than 500 mg), you should sit or stand and drink plenty of water. If necessary, the tablet can be split in half.

8. The injection must not be mixed with other medicines and should be shaken well before use.

9. For women who use estrogen replacement therapy after menopause, adding progestin for more than 7 days can reduce the incidence of endometrial hyperplasia. Using progestins for 12 to 14 days provides optimal endometrial maturation and eliminates proliferative changes.

10. Store at room temperature.

11. For intramuscular injection, a long and thick needle should be used for deep injection, which can reduce local sterile abscesses or inflammatory infiltration. When used in cancer patients, it must be used under the guidance of an experienced cancer chemotherapy physician and should be discontinued if thromboembolism, migraine or eye disease occurs. Long-term use of large doses of the drug will produce adrenal cortex hormone reactions, and special attention should be paid to patients with diabetes and high blood pressure. Medroxyprogesterone may cause vaginal bleeding, but care should be taken to exclude more serious causes. Medroxyprogesterone use in early pregnancy can cause congenital heart dysplasia in the fetus. Long-term use of the drug in animals (beagles) has resulted in the development of mammary nodules that are malignant, but there have been no similar reports in humans.

Adverse Reactions

1. Breakthrough bleeding, spotting, changes in menstrual volume, amenorrhea, edema, weight change (increase or decrease), cholestatic jaundice, allergic reactions, rash, depression, insomnia, and nausea may occur. If breakthrough bleeding occurs, a detailed examination should be conducted to rule out organic diseases. Depending on the amount of bleeding, 0.05-0.1 mg of ethinyl estradiol can be added for 3 consecutive days to stop the bleeding.

2. Large doses used for tumors can cause progesterone-like reactions such as breast pain, galactorrhea, vaginal bleeding, amenorrhea, irregular menstruation, abnormal cervical secretion, uterine erosion, etc.; long-term use can also cause symptoms of hyperfunction of the adrenal cortex such as moon face, Cushing's syndrome, weight gain, etc. It can also produce effects similar to corticosteroids, such as weight gain, abdominal pain, headache, mood changes, hand tremors, sweating, calf cramps at night, and other adrenaline-like reactions. There have also been reports of it causing obstructive jaundice.

3. Medroxyprogesterone can cause abnormal coagulation function.

Dosage

1. Long-acting medroxyprogesterone powder injection is prepared into a water suspension for injection, 150 mg is injected intramuscularly every 3 months, and is administered on the 2nd to 7th day of menstruation. Cyproterone acetate oil injection is given once a month. Mothers should start using it 4 weeks after delivery. The medroxyprogesterone vaginal ring is a sustained-release system of medroxyprogesterone. It is removed during menstruation and can be used continuously for 3 to 6 months.

2. Threatened abortion: take orally 4-8 mg each time, 2-3 times a day.

3. Habitual abortion: Take 10 mg per day for the first 3 months, 20 mg per day for the 4th to 4.5th months, and finally reduce the dosage and stop taking the drug.

4. Dysmenorrhea: Starting from the 6th day of the menstrual cycle, 2-4 mg per day for 20 consecutive days; or starting from the 1st day of menstruation, 3 times a day for 3 consecutive days.

5. Functional amenorrhea: 4-8 mg per day, for 5-10 days.

6. Endometriosis: Start with 6-8 mg per day, gradually increase to a total of 20-30 mg per day, and use for 6-8 weeks.

7. For tumors: oral administration, 500-1 000 mg per day. Take once or in 2 doses for 10 consecutive days. Later, depending on the condition, the dosage can be changed to 250-500 mg per day, and it can be taken for a long time. Start with intramuscular injection of 500 mg once a day for a maximum of 4 weeks, then change to 3 times a week.

8. For endometrial cancer and prostate cancer: 0.2-0.5g per day;

9. For renal adenocarcinoma: 0.2-0.5g per day.