Medroxyprogesterone


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular
Contraception
Adult: 150 mg given during the 1st 5 days of normal menstrual cycle or within the 1st 5 days following childbirth (delay until 6 weeks after childbirth if breastfeeding). Further doses must be given at 12- or 13-week intervals. Initial administration schedule may vary when switching from another method of contraception to ensure continuous contraceptive coverage (refer to detailed product guideline).

Intramuscular
Hormone-dependent recurrent breast cancer in postmenopausal women
Adult: Initially, 500 mg daily for 4 weeks. Maintenance: 500 mg twice weekly according to patient response.

Intramuscular
Endometrial carcinoma, Renal cell carcinoma
Adult: As adjunctive and/or palliative therapy in advanced inoperable cases including those with metastatic and/or recurrent disease: Initially, 400-1,000 mg weekly. If there is improvement within a few weeks or months and the disease is stabilised, may maintain dose at the lowest recommended dose every month. Dosing recommendations may vary among countries and individual products (refer to specific product guideline).

Intramuscular
Endometriosis
Adult: 50 mg weekly or 100 mg every 2 weeks for at least 6 months.

Oral
Endometrial carcinoma, Renal cell carcinoma
Adult: 200-600 mg daily.

Oral
Endometriosis
Adult: In mild to moderate cases: 10 mg tid for 90 consecutive days, started on the 1st day of menstrual cycle.

Oral
Prophylaxis of endometrial hyperplasia
Adult: In non-hysterectomised postmenopausal women receiving oral conjugated estrogens: 5 or 10 mg daily for 12-14 consecutive days each month, started on the 1st or 16th day of the cycle. Use for the shortest duration possible at the lowest effective dose consistent with the treatment goals. Re-evaluate patients periodically as clinically appropriate.

Oral
Secondary amenorrhoea
Adult: 2.5-10 mg daily for 5-10 days, initiated on the assumed or calculated 16th-21st day of the cycle. Alternatively, treatment may be started at any time. Repeat for 3 consecutive cycles. In cases associated with a poorly developed proliferative endometrium: 5-10 mg for 10 days in conjunction with conventional estrogen therapy.

Oral
Dysfunctional uterine bleeding
Adult: 2.5-10 mg daily for 5-10 days, initiated on the assumed or calculated 16th-21st day of the cycle. Given for 2 consecutive cycles. In case of bleeding from a poorly developed proliferative endometrium: 5-10 mg for 10 days in conjunction with conventional estrogen therapy.

Oral
Breast carcinoma
Adult: In postmenopausal women: 400-1,500 mg daily.

Subcutaneous
Endometriosis
Adult: In cases when other options are considered inadequate: 104 mg every 12-14 weeks.

Subcutaneous
Contraception
Adult: 104 mg during the 1st 5 days of normal menstrual cycle or within the 1st 5 days following childbirth (delay until 6 weeks after childbirth if breastfeeding). Further doses must be given at 12-14 week intervals. Initial administration schedule may vary when switching from another method of contraception to ensure continuous contraceptive coverage (refer to detailed product guideline).
Cách dùng
May be taken with or without food. Incidence of minor indigestion may increase as dose increases. Take w/ meals if necessary.
Chống chỉ định
Undiagnosed vaginal bleeding, previous idiopathic or current venous thromboembolism (e.g. DVT, pulmonary embolism); active or recent arterial thromboembolic disease (e.g. angina, MI) or cerebrovascular disease; missed abortion. Gynaecological/contraceptive use: Known, history or suspected breast cancer; porphyria; metabolic bone disease (SC). Hepatic impairment. Pregnancy.
Thận trọng
Patient with risk factors for estrogen-dependent tumours; history of or risk factors for thromboembolic disorders; hypertension, liver disorders (e.g. liver adenoma), cholelithiasis, history of liver disease, diabetes mellitus (with or without vascular involvement), migraine or severe headache, SLE, epilepsy, asthma, otosclerosis, cardiac dysfunction, history of acute visual disturbances or mental depression, hypercholesterolaemia; hypoparathyroidism (in combination with estrogen). Obesity. Risk factors for osteoporosis (e.g. chronic alcohol or tobacco use, low BMI, eating disorder, previous low trauma fracture, family history of osteoporosis). Renal impairment. Lactation. Discontinue combination therapy with estrogens at least 4-6 weeks prior to surgery associated with an increased risk of thromboembolism or within periods of prolonged immobilisation.
Tác dụng không mong muốn
Significant: Decreased glucose tolerance, jaundice, increased blood pressure, new onset of migraine-type headache, weight gain, fluid retention; vaginal bleeding, depression, menstrual irregularities (e.g. amenorrhoea, unpredictable bleeding or spotting), Cushingoid symptoms, suppressed adrenal function, increased triglycerides (in women with pre-existing hypertriglyceridaemia), visual abnormalities, thromboembolic disorders, loss of bone mineral density, delayed return to ovulation and fertility (upon discontinuation), anaphylaxis or anaphylactoid reaction, severe abdominal pain (IM/SC).
Gastrointestinal disorders: Nausea, vomiting, constipation; abdominal pain, distension, or discomfort.
General disorders and administration site conditions: Pyrexia, fatigue; asthenia, inj site reaction (SC).
Investigations: Weight decreased; abnormal smear cervix (SC).
Metabolism and nutrition disorders: Hypercalcaemia (in treatment of breast carcinoma), increased appetite.
Musculoskeletal and connective tissue disorders: Back pain, pain in extremity.
Nervous system disorders: Headache, dizziness, tremors.
Psychiatric disorders: Insomnia, nervousness, libido decreased.
Reproductive system and breast disorders: Cervical discharge, breast pain or tenderness, erectile dysfunction, dysmenorrhea, genitourinary tract infection.
Skin and subcutaneous tissue disorders: Urticaria, alopecia, acne, pruritus, hyperhidrosis.
Vascular disorders: Hot flush.
IM/Parenteral/PO/SC: X
Chỉ số theo dõi
Obtain bone mineral density (prolonged use). Monitor blood pressure and glucose (in diabetic patients). Evaluate for vision loss, migraines, signs of thromboembolic disorders or depression. Contraceptive use: Verify pregnancy status prior to use. Monitor weight and assess potential health status changes.
Tương tác
Bioavailability may be decreased when used concomitantly with aminoglutethimide. May decrease plasma concentration with enzyme inducers including CYP3A4 (e.g. phenytoin, phenobarbital, carbamazepine, rifampicin, nevirapine). Concomitant use with ciclosporin may result in increased plasma levels of ciclosporin and/or decreased plasma levels of medroxyprogesterone. May decrease the haematological toxicity of cytotoxic agents. Increased risk of invasive breast cancer, dementia, and CV disease (e.g. DVT, pulmonary emboli, stroke) in postmenopausal women when used concomitantly with conjugated estrogens.
Tương tác với thức ăn
May decrease plasma concentration with St. John’s wort. Increased bioavailability with food.
Ảnh hưởng đến kết quả xét nghiệm
May alter results of glucose tolerance test, metyrapone test, thyroid function tests (e.g. protein bound iodine levels may increase and T3 uptake levels may decrease), prothrombin and platelet aggregation time.
Tác dụng
Description:
Mechanism of Action: Medroxyprogesterone is a progestogen derivative that inhibits the release of gonadotrophins which prevents follicular maturation and ovulation and causes thickening of cervical mucus, thereby inhibiting sperm entry into the uterus. It transforms a proliferative endometrium into a secretory endometrium. Its effect on endometriosis may be due to the suppression of serum estradiol concentrations, resulting in atrophy of the endometrial tissue and decreases the associated pain. Additionally, when given in high doses, medroxyprogesterone demonstrates antitumour activity.
Onset: Ovulation (after last inj): 10 months (range: 6-12 months).
Pharmacokinetics:
Absorption: Rapidly absorbed from the gastrointestinal tract (oral). Slowly absorbed after IM inj. Increased bioavailability with food. Bioavailability: 0.6-10%. Time to peak plasma concentration: 2-4 hours (oral); approx 3 weeks (IM); approx 1 week (SC).
Distribution: Enters breast milk. Plasma protein binding: 86-90%, mainly to albumin.
Metabolism: Metabolised in the liver by CYP450 enzymes via hydroxylation and conjugation into metabolites.
Excretion: Via urine (mainly as glucuronide conjugate). Elimination half-life: Approx 12-17 hours (oral); approx 50 days (IM); approx 43 days (SC).
Đặc tính

Chemical Structure Image
Medroxyprogesterone acetate

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 6279, Medroxyprogesterone acetate. https://pubchem.ncbi.nlm.nih.gov/compound/Medroxyprogesterone-acetate. Accessed May 27, 2021.

Bảo quản
Store between 20-25°C. Storage recommendations may vary among countries or individual products. Refer to detailed product guideline.
Phân loại MIMS
Liệu pháp nội tiết trong điều trị ung thư / Thuốc ngừa thai tác dụng chậm / Estrogen, progesteron & các thuốc tổng hợp có liên quan
Phân loại ATC
G03DA02 - medroxyprogesterone ; Belongs to the class of pregnen (4) derivative progestogens.
G03AC06 - medroxyprogesterone ; Belongs to the class of progestogens. Used as systemic contraceptives.
L02AB02 - medroxyprogesterone ; Belongs to the class of progestogens.
Tài liệu tham khảo
Anon. Medroxyprogesterone. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/03/2021.

Buckingham R (ed). Medroxyprogesterone Acetate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/03/2021.

Depo-Provera 150 mg/mL Sterile Suspension for Injection (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 04/03/2021.

Depo-Provera Injection, Suspension (Pharmacia and Upjohn Company LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/03/2021.

Depo-Provera Suspension for Injection (Pfizer [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/03/2021.

Depo-Subq Provera Injection, Suspension (Pharmacia and Upjohn Company LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/03/2021.

Joint Formulary Committee. Medroxyprogesterone Acetate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/03/2021.

Pfizer New Zealand Ltd. Depo-Provera 150 mg/mL Injection data sheet 27 February 2020. Medsafe. http://www.medsafe.govt.nz. Accessed 04/03/2021.

Provera 400 mg Tablets (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 04/03/2021.

Provera 5 mg Tablets (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 04/03/2021.

Provera Tablet (Pharmacia and Upjohn Company LLC). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 04/03/2021.

Provera Tablets (Pfizer [Malaysia] Sdn. Bhd.). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/03/2021.

Sayanaject 104 mg Suspension for Injection (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 04/03/2021.

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