medroxyprogesterone

Contraindicated in:

Hypersensitivity;
Hypersensitivity to parabens (IM suspension only);
Missed abortion;
Thromboembolic disease (e.g., deep vein thrombosis [DVT], pulmonary embolism [PE], MI, stroke)
;
Cerebrovascular disease;
Severe hepatic impairment;
History of breast cancer
;
Protein C, protein S, or antithrombin deficiency or other thrombophilic disorder
;
Porphyria;
OB: Pregnancy;
Lactation: Lactation.

Use Cautiously in:

Long-term use (>4–5 yr); may ↑ risk of MI, stroke, invasive breast cancer, DVT, PE, and dementia in postmenopausal women
;
Renal impairment;
Hepatic impairment;
Cardiovascular disease
;
Seizure disorders;
Depression.

Adv. Reactions/Side Effects ⬆ ⬇

CV: DVT, edema, MI, thrombophlebitis

Derm: chloasma, melasma, rash

EENT: retinal thrombosis

Endo: breast tenderness, galactorrhea, hyperglycemia

GI: drug-induced hepatitis, gingival bleeding

GU: amenorrhea, breakthrough bleeding, cervical erosions, changes in menstrual flow, dysmenorrhea

Local: injection site reactions

Metab: weight gain, weight loss

MS:

bone loss

Neuro:

dementia

, depression, STROKE

Resp: PE

Misc: HYPERSENSITIVITY REACTIONS (INCLUDING ANAPHYLAXIS OR ANGIOEDEMA), MALIGNANCY (BREAST, ENDOMETRIAL, OVARIAN)

Interactions ⬆ ⬇

Drug-drug:

Strong CYP3A4 inhibitors, including ketoconazole, itraconazole, clarithromycin, atazanavir, nefazodone, nelfinavir, ritonavir, and voriconazole, may ↑ levels and risk of toxicity; avoid concurrent use.
Strong CYP3A4 inducers, including phenytoin, phenobarbital, carbamazepine, rifampin, rifabutin, rifapentin, and phenobarbital, may ↓ levels and effectiveness; avoid concurrent use.
May ↓ effectiveness of bromocriptine when used concurrently for galactorrhea/amenorrhea.

Drug-Natural Products:

St. John's wort may ↓ levels and effectiveness; avoid concurrent use

Availability ⬆ ⬇

(Generic available)

Tablets: 2.5 mg; 5 mg; 10 mg; 100 mg
Suspension for intramuscular injection: 50 mg/mL; 150 mg/mL
Suspension for SUBQ injection (Depo-SubQ Provera 104): 104 mg/0.65 mL
In combination with: conjugated estrogens as Prempro (single combination tablet of 0.626 mg conjugated estrogens plus 2.5 or 5 mg medroxyprogesterone) or Premphase (0.625 mg conjugated estrogens tablet for 14 days followed by combination tablet of 0.625 mg conjugated estrogens plus 5 mg medroxyprogesterone for days 15–28) in convenience packages. See Appendix [not included in this PDA edition].

Route/Dosage ⬆ ⬇

Postmenopausal Women Receiving Concurrent Estrogen

PO (Adults ): 2.5–5 mg daily concurrently with 0.625 mg conjugated estrogens (monophasic regimen) or 5 mg daily on Days 15–28 of the cycle with 0.625 mg conjugated estrogens taken daily throughout cycle (biphasic regimen).

Secondary Amenorrhea

PO (Adults ): 5–10 mg/day for 5–10 days; start at any time in cycle.

Dysfunctional Uterine Bleeding/Induction of Menses

PO (Adults ): 5–10 mg/day for 5–10 days, starting on Day 16 or Day 21 of menstrual cycle.

Renal or Endometrial Carcinoma

IM (Adults ): 400–1000 mg; may be repeated weekly; if improvement occurs, attempt to ↓ dose to 400 mg monthly.

Endometriosis-Associated Pain

SC (Adults ): 104 mg every 12–14 wk (3 mo), beginning on Day 5 of normal menses (not recommended for more than 2 yr).

Prevention of Pregnancy

IM (Adults ): 150 mg within 1st 5 days of menses or within 5 days postpartum, if not breastfeeding. If breastfeeding, give 6 wk postpartum; repeat every 3 mo.
SC (Adults ): 104 mg within 1st 5 days of menses or within 5 days postpartum, if not breastfeeding. If breastfeeding, give 6 wk postpartum; repeat every 12–14 wk.

US Brand Names ⬆ ⬇

Depo-Provera, Depo-SubQ Provera 104, Provera

Action ⬆ ⬇

A synthetic form of progesterone; actions include secretory changes in the endometrium, increases in basal body temperature, histologic changes in vaginal epithelium, relaxation of uterine smooth muscle, mammary alveolar tissue growth, pituitary inhibition, and withdrawal bleeding in the presence of estrogen.

Therapeutic effects:

Decreased endometrial hyperplasia in postmenopausal women receiving concurrent estrogen (combination with estrogen decreases vasomotor symptoms and prevents osteoporosis).
Restoration of hormonal balance with control of uterine bleeding.
Management of endometrial or renal cancer.
Prevention of pregnancy.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics, contraceptive hormones

Pharmacologic Classification: hormones, progestins

Pharmacokinetics ⬆ ⬇

Absorption: 0.6–10% absorbed after oral administration.

Distribution: Unknown.

Metabolism/Excretion: Metabolized by the liver. Primarily excreted in the urine as metabolites.

Half-Life: 1st phase: 52 min; 2nd phase: 230 min; biological: 14.5 hr.

Time/Action Profile ⬆ ⬇

(IM = antineoplastic effects)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	unknown	unknown
IM	wk–mos	mo	unknown‡
SC	unknown	1 wk	3 mo

‡Contraceptive effect lasts 3 mo.

Patient/Family Teaching ⬆ ⬇

Explain purpose and side effects of medication to patient. Advise patient to read Patient Information before starting therapy and with each Rx refill or injection. Take missed doses as soon as remembered; do not double doses.
Advise patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult health care provider before taking other medications.
- Inform postmenopausal women that long-term use may ↑ risk of MI, stroke, invasive breast cancer, PE, DVT, and dementia.
- Explain the importance of adhering to every 3-mo schedule to patients using medroxyprogesterone for contraception.
- Advise patients receiving medroxyprogesterone for menstrual dysfunction to anticipate withdrawal bleeding 3–7 days after discontinuing medication.
- Advise patient to report signs and symptoms of thromboembolic disorders (pain, swelling, tenderness in extremities, headache, chest pain, blurred vision).
- Advise patient to keep a 1-mo supply of medroxyprogesterone available at all times.
- Instruct patient in correct method of monthly breast self-examination. ↑ breast tenderness may occur.
- Advise patient that gingival bleeding may occur. Instruct patient to use good oral hygiene and to receive regular dental care and examinations.
- Inform patient that medroxyprogesterone does not protect against HIV infection and other sexually transmitted infections.
- Medroxyprogesterone may cause melasma (brown patches of discoloration) on face when patient is exposed to sunlight. Advise patient to avoid sun exposure and to wear sunscreen or protective clothing when outdoors.
- Emphasize the importance of routine follow-up physical exams, including BP check; breast, abdomen, and pelvic examinations; Papanicolaou smears every 6–12 mo; and mammogram every 12 mo or as directed. Health care provider will evaluate possibility of discontinuing medication every 3–6 mo. If on continuous (not cyclical) therapy or without concurrent estrogens, endometrial biopsy may be recommended, if uterus is intact.
- Advise women of reproductive potential to notify health care provider if menstrual period is missed or if pregnancy is suspected or if breastfeeding. Patient should not attempt conception for 3 mo after discontinuing medication in order to ↓ risk to fetus. Once discontinued, may delay conception for ≥10 mo.
IM: SC: Advise patient to maintain adequate amounts of dietary calcium and vitamin D to help prevent bone loss.

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Indications ⬇

Contraind./Precautions ⬆ ⬇