Pronunciation: meh-DROX-ee-pro-JESS-tuh-rone ASS-uh-TATE
Class: Progestin, Contraceptive hormone

Trade Names

Amen
- Tablets 10 mg

Curretab
- Tablets 10 mg

Cycrin
- Tablets 2.5 mg
- Tablets 5 mg
- Tablets 10 mg

Depo-Provera
- Injection 150 mg/mL
- Injection 400 mg/mL

Provera
- Tablets 2.5 mg
- Tablets 5 mg
- Tablets 10 mg

Apo-Medroxy (Canada)
Gen-Medroxy (Canada)
Provera-Pak (Canada)
ratio-MPA (Canada)

Pharmacology

Inhibits secretion of pituitary gonadotropins, thereby preventing follicular maturation and ovulation (contraceptive effect); inhibits spontaneous uterine contraction; transforms proliferative endometrium into secretory endometrium; produces antineoplastic effect in advanced endometrial or renal carcinoma.

Slideshow: Top 10 Ways to Save on Your Medication Costs

Pharmacokinetics

Absorption

T _max is 2 to 4 h. Food increases the bioavailability of medroxyprogesterone acetate.

Distribution

Medroxyprogesterone protein binding is approximately 90%.

Metabolism

Medroxyprogesterone is extensively metabolized in the liver by hydroxylation with subsequent conjugation. At least 16 metabolites have been identified.

Elimination

Most of the metabolites are excreted in urine. The t _½ is approximately 12 h.

Special Populations

Hepatic Function Impairment

Metabolism and Cl are decreased in patients with hepatic function impairment. Lower doses or less frequent administration is recommended in patients with mild to moderate hepatic function impairment and is contraindicated in patients with severe hepatic function impairment.

Indications and Usage

PO

Treatment of secondary amenorrhea and abnormal uterine bleeding caused by hormonal imbalance; reduction of incidence of endometrial hyperplasia in nonhysterectomized postmenopausal women receiving conjugated estrogen 0.625 mg.

Parenteral

Prevention of pregnancy; adjunctive and palliative treatment of inoperable, recurrent, and metastatic endometrial or renal carcinoma.

Contraindications

Hypersensitivity to progestins; current or history of thrombophlebitis, thromboembolic disorders, cerebrovascular disease, or cerebral hemorrhage; impaired liver function; breast or genital organ cancer; undiagnosed vaginal bleeding; missed abortion; diagnostic test for pregnancy; known or suspected pregnancy.

Dosage and Administration

Abnormal Uterine Bleeding
Adults

PO 5 to 10 mg/day for 5 to 10 days beginning on 16th or 21st day of menstrual cycle.

Contraceptive
Adults

IM 150 mg every 3 mo.

Endometrial or Renal Carcinoma
Adults Initial

IM 400 to 1,000 mg/wk.

Maintenance

IM 400 mg/mo.

Reduction of Endometrial Hyperplasia
Adults

PO 5 to 10 mg daily for 12 to 14 consecutive days per month, beginning on the 1st or 16th day of cycle.

Secondary Amenorrhea
Adults

PO 5 to 10 mg/day for 5 to 10 days.

General Advice

• Injection
• For IM injection only. Not for intradermal, subcutaneous, or intra-arterial administration.
• Shake vial vigorously just before use to ensure that dose is being administered as a uniform suspension.
• Do not administer if particulate matter, cloudiness, or discoloration is noted.
• Administer by deep IM injection into gluteal or deltoid muscle. Rotate injection sites.
• When using as contraceptive, administer prescribed dose during first 5 days after the onset of a normal menstrual period, within 5 days postpartum if not breast-feeding, or if breast-feeding, at 6 wk postpartum.

Storage/Stability

Store tablets and injection at controlled room temperature (68° to 77°F).

Drug Interactions

Aminoglutethimide

May increase metabolism and decrease effect of medroxyprogesterone.

Laboratory Test Interactions

Endocrine, coagulation (increased amounts of some clotting factors), thyroid, and LFT results may be affected by progestins; may decrease glucose tolerance; decreased plasma and urinary steroid levels; decreased gonadotropin levels; decreased sex-hormone-binding-globulin concentrations.

Adverse Reactions

Cardiovascular

Thrombophlebitis; edema.

CNS

Depression; headache; nervousness; dizziness; insomnia; fatigue; somnolence.

Dermatologic

Rash; acne; melasma; chloasma; alopecia; hirsutism; photosensitivity; pruritus; urticaria.

GI

Abdominal pain or discomfort; nausea.

Genitourinary

Breakthrough bleeding; spotting; change in menstrual flow; amenorrhea; decrease in libido; changes in cervical erosion and secretions.

Hepatic

Cholestatic jaundice.

Respiratory

Pulmonary embolism.

Miscellaneous

Breast tenderness; masculinization of female fetus; edema; weight changes, especially weight gain; anaphylactoid reactions; bone mineral density changes, increasing risk of osteoporosis; hyperglycemia; pyrexia; galactorrhea.

Precautions

Pregnancy

Category X .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Conception

May prolong contraceptive effect, which may delay time to potential conception once therapy is discontinued.

Contraception

If period between injections is longer than 14 days, determine that patient is not pregnant before administering drug.

Fluid retention

Use with careful observation when conditions that might be affected by this factor are present (eg, asthma, cardiac or renal dysfunction, epilepsy).

Mental depression

Carefully observe patients with history of depression.

Ophthalmic effects

Discontinue medication if there are any sudden changes in vision, sudden onset of proptosis, diplopia, migraine, papilledema, or retinal vascular lesions.

Prolonged use

Effect of prolonged use on pituitary, ovarian, adrenal, hepatic, and uterine function not known.

Thromboembolic

Discontinue if occurring or suspected.

Vaginal bleeding

With irregular vaginal bleeding, including breakthrough bleeding, nonfunctional causes should be considered and adequate diagnostic measures undertaken.

Patient Information

• Advise patient to read patient information leaflet before using the first time and with each refill.
• Instruct diabetic patient taking estrogen and medroxyprogesterone to monitor blood glucose more frequently when therapy is started and to inform health care provider of significant changes in readings.
• Teach patient proper method of breast self-examination, and remind patient to perform monthly.
• Instruct patient to immediately report any of the following symptoms to health care provider: pain in groin or calves; sharp chest pain, coughing blood, or sudden shortness of breath; crushing chest pain or heaviness in chest; abnormal vaginal bleeding; breast lumps; sudden severe headache; dizziness or fainting; tremors or seizure; vision or speech problems; weakness or numbness of arms or legs; severe abdominal pain; depression; yellowing of the skin or eyes; persistent pain, pus, or bleeding at injection site.
• Advise patient that follow-up visits and examinations, including Pap smear, at least once a year, will be required to monitor therapy and to keep appointments.

• Tablets
• Advise patient to take each dose without regard to meals but to take with food if stomach upset occurs.

• Injection
• Advise patient that injection will be prepared and administered by a health care provider in a medical setting.
• Advise patient that menstrual cycle may be disrupted (eg, irregular or unpredictable bleeding, or spotting) but that this usually decreases over several months to the point of no menstrual flow. Advise patient to notify health care provider if abnormal bleeding persists or is severe.
• Advise patient that contraceptive injection does not protect against HIV infection and other sexually transmitted diseases.

Copyright © 2009 Wolters Kluwer Health.