Medroxyprogesterone

Oral:
Contraindicated.

Intramuscular/Subcutaneous:
Significant or severe: Contraindicated.

Medroxyprogesterone May be taken with or without food.

Active thrombophlebitis, current or history of thromboembolic disorders, or cerebrovascular disease; undiagnosed vaginal bleeding; known or suspected breast cancer (unless being treated for this disease). When used for contraception: Current or history of meningioma; known or suspected malignancy of genital organs. Hepatic impairment (oral); significant or severe hepatic impairment (IM/SC). Pregnancy. Contraindications may vary among countries or between individual products (refer to local or specific product guidelines).

Patient with cardiac dysfunction; history of mental depression; hypertension, diabetes mellitus, hyperlipidaemia, SLE; risk factors for thromboembolic disorders; risk factors for osteoporosis (e.g. low body mass index, eating disorder, previous low trauma fracture, family history of osteoporosis, alcohol abuse, tobacco use, chronic use of drugs that may reduce bone mass); family history of breast cancer; condition that may be aggravated by fluid retention (e.g. migraine, seizure disorders, asthma). Ensure adequate intake or supplementation of calcium and vitamin D. Not recommended as a long-term (>2 years) contraception or treatment for endometriosis-associated pain unless other options are considered insufficient. Renal impairment. Lactation.

Significant: Single and multiple meningiomas (mainly after prolonged use); significant loss of BMD; menstrual bleeding irregularities (e.g. amenorrhoea, irregular bleeding and spotting, prolonged bleeding episodes, heavy bleeding), weight gain, fluid retention; decreased glucose tolerance; depression or mood disorders, retinal thrombosis; may reduce ACTH and hydrocortisone blood levels; may increase plasma triglycerides, which may lead to pancreatitis (when used with estrogen in women with pre-existing hypertriglyceridaemia); increased risk of pulmonary embolism, DVT, stroke, MI, invasive breast cancer and probable dementia (in combination with estrogen); Cushingoid symptoms, jaundice, new onset of migraine-type headache. IM/SC: Possible ectopic pregnancy, anaphylaxis or anaphylactoid reactions; delayed return to full fertility (following discontinuation).
Gastrointestinal disorders: Nausea, vomiting, constipation, abdominal pain, discomfort or distension.
General disorders and administration site conditions: Fatigue, asthenia; inj site reactions (e.g. atrophy, indentation, dimpling, nodule or lump, pain, tenderness).
Metabolism and nutrition disorders: Increased appetite; hypercalcaemia (particularly in treatment of breast carcinoma).
Musculoskeletal and connective tissue disorders: Back pain.
Nervous system disorders: Dizziness, tremors.
Psychiatric disorders: Insomnia, nervousness.
Reproductive system and breast disorders: Breast pain or tenderness, cervical discharge, erectile dysfunction, decreased libido, dysmenorrhoea, genitourinary tract infection, vaginitis.
Skin and subcutaneous tissue disorders: Acne, alopecia, pruritus, urticaria, hyperhidrosis.

IM/Parenteral/PO/SC: X

Ensure adequate intake of calcium and vitamin D.

Obtain medical and family history and perform physical examination that includes special reference to the breasts and pelvic, and a Papanicolaou test (Pap smear), before initiating treatment and annually thereafter during continued use. Monitor blood glucose (in patients at risk of decreased glucose tolerance); blood pressure (regularly when used with estrogen). Evaluate persistent or severe abnormal bleeding. Assess for signs and symptoms of thromboembolic and thrombotic disorders (e.g. thrombophlebitis, pulmonary embolism, retinal thrombosis), liver dysfunction (e.g. jaundice, liver function deterioration), and depression (particularly in patients with history of depression). When used for endometrial cancer: Monitor for breast cancer in patients with strong family history of breast cancer. Consider evaluation of BMD in patients receiving high doses for prolonged periods. When used as contraceptive: Verify pregnancy status before initiation. Monitor for potential health status changes (regularly); BMD (for long-term use); weight (optional).

May decrease plasma concentration with enzyme inducers, including CYP3A4 (e.g. phenytoin, phenobarbital, carbamazepine, rifampicin). May significantly reduce bioavailability with aminoglutethimide.

May decrease plasma concentration with St. John's wort. Increased bioavailability with food.

May reduce the levels of plasma or urinary steroids (e.g. estrogen, cortisol, pregnanediol, progesterone, testosterone), plasma or urinary gonadotrophins (e.g. LH, FSH) and sex hormone-binding globulin. May cause partial decrease in pituitary-adrenal axis response during metyrapone testing. May increase coagulation test values for prothrombin and factors VII, VIII, IX and X. May alter the results of glucose tolerance test and thyroid function tests (e.g. protein-bound iodine levels may increase and T₃ uptake levels may decrease).

Description:
Overview: Medroxyprogesterone is a synthetic progestin that has anti-estrogenic, antigonadotrophic and anti-androgenic properties.
Mechanism of Action: As a contraceptive, medroxyprogesterone inhibits the secretion of pituitary gonadotrophins (suppression of midcycle surge of luteinising hormone [LH]) by binding to progesterone receptor in the target cells, which slows the frequency of gonadotrophin-releasing hormone (GnRH) release and blunts the pre-ovulatory LH surge. In endometriosis-associated pain, suppression of serum estradiol concentrations and a direct action on endometrial lesions are likely responsible for the therapeutic effect. Medroxyprogesterone also induces the transformation of the endometrium from the proliferative to the secretory phase in women with adequate endogenous estrogen. Additionally, it has antineoplastic activity against certain cancers (e.g. endometrial and renal carcinoma); however, its mechanism of action in these cancers has not been determined.
Pharmacodynamics: Medroxyprogesterone exhibits contraceptive actions, including the prevention of follicular maturation and ovulation, alterations of the endometrium that may impair implantation, and an increase in cervical mucus viscosity which blocks sperm entry into the uterus. In menopausal and postmenopausal women with an intact uterus receiving estrogen therapy, it reduces endometrial growth, thereby exerting a protective effect against endometrial hyperplasia. Medroxyprogesterone may also help to re-establish normal menstrual cycles by restoring adequate progesterone levels in pre-menopausal women with secondary amenorrhoea or dysfunctional uterine bleeding.
Onset: Ovulation (following 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: Extensively metabolised in the liver via hydroxylation and conjugation into metabolites.
Excretion: Via urine (mainly as glucuronide conjugate). Elimination half-life: 12-17 hours (oral); approx 50 days (IM); approx 43 days (SC).

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 10631, Medroxyprogesterone. https://pubchem.ncbi.nlm.nih.gov/compound/Medroxyprogesterone. Accessed Nov. 28, 2025.

Oral:
Tab: Store below 30°C.

Intramuscular:
Susp for inj (vial or pre-filled syringe): Store between 20-25°C. Store the vial upright. Do not refrigerate or freeze.

Subcutaneous:
Susp for inj (pre-filled syringe): Store between 20-25°C. Do not refrigerate or freeze.

Follow applicable procedures for receiving, handling, administration, and disposal. Storage recommendations may vary between individual products (refer to specific product guidelines).

Cancer Hormone Therapy / Depot Contraceptives / Oestrogens, Progesterones & Related Synthetic Drugs

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.

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Sayana 104 mg/0.65 mL Suspension for Injection (Pfizer Limited). MHRA. https://products.mhra.gov.uk. Accessed 07/10/2025.