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medroxyprogesterone actetate; acetoxymethylprogesterone (Provera, Cycrin, Amen)

Tradenames: Provera, Depo-Provera, Cycrin, Amen. Indications: - Contraceptive (Depo-Provera) - hormone replacement therapy - hot flash - relief of uterine vasomotor symptoms - amenorrhea - abnormal uterine bleeding - endometriosis [7] - hormonal imbalance - precocious puberty [7] - palliative therapy for advanced breast carcinoma & endometrial carcinoma (by similarity to megestrol) - endometrial dysplasia - polycystic ovary disease [7] - progesterone challenge test [7] Contraindications: 1) thrombophlebitis 2) cerebral hemorrhage 3) undiagnosed vaginal bleeding 4) liver dysfunction Dosage: 1) hormone replacement therapy: 2.5-5 mg PO QD 2) abnormal uterine bleeding: 5-10 mg PO X 5-10 days 3) relief of uterine vasomotor symptoms: 20 mg/day 4) amenorrhea: 5-10 mg/day for 5-10 days 5) contraception: 150 mg IM every 3 months - Sayana Press: a 104 mg SQ injection [8] Tabs: 2.5, 5, 10 mg. Injection (suspension): 150 mg/mL (1 mL); 400 mg/mL (2.5 & 10 mL). Pharmacokinetics: 1) withdrawal bleeding in estrogen-primed individuals occurs within 3-7 days of last dose 2) onset of relief from hot flashes occurs within 4-7 days 3) maximum effect on hot flashes after 1 month Adverse effects: 1) common (> 10%) - breakthrough bleeding, spotting, changes in menstrual flow, amenorrhea, pain at site of injection, anorexia, edema, weakness 2) less common (1-10%) - depression, fever, melasma, chloasma, allergic rash with or without pruritus, cholestatic jaundice, changes in cervical secretions, weight gain or loss, insomnia, breast tenderness, thrombophlebitis, thromboembolism 3) other - adverse lipid effects - bloating - headache - mood changes - accelerates HIV progression [6] Adverse effects of abrupt discontinuation: [5] 1) adrenal insufficiency may occur after long-term use 2) thromboembolism 3) breakthrough vaginal bleeding 4) peripheral edema 5) hyperglycemia 6) hypertension 7) Cushing's syndrome 8) osteoporosis [4] 9) alopecia Drug interactions: - aminoglutethimide may decrease effects Test interactions: -> altered thyroid & liver function tests Mechanism of action: 1) progestin (progestational agent) - prevents ovulation [4] 2) 17-alpha-acetoxyprogestational agent with more potent progestational effects & better bioavailability than progesterone Notes: - Deprecated Reference lists as antineoplastic agent

General

antineoplastic endocrine agent progestational agent

Properties

MISC-INFO: elimination route LIVER pregnancy-category X D safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Medical Knowledge Self Assessment Program (MKSAP) 11, 16. American College of Physicians, Philadelphia 1998, 2012
  5. Bruera & Neumann Canadian Medical Assoc. J (CAMJ):158:1717, 1998
  6. Stringer EM et al HIV disease progression by hormonal contraceptive method: Secondary analysis of a randomized trial. AIDS 2009 Jul 17; 23:1377. PMID: 19448528
  7. Deprecated Reference
  8. Bonny AE et al. A pilot study of depot medroxyprogesterone acetate pharmacokinetics and weight gain in adolescent females. Contraception 2014 May; 89:357. PMID: 24582292 - Beasley A et al. Randomized clinical trial of self versus clinical administration of subcutaneous depot medroxyprogesterone acetate. Contraception 2014 May; 89:352. PMID: 24656555 - Burke HM et al. Observational study of the acceptability of Sayana® Press among intramuscular DMPA users in Uganda and Senegal. Contraception 2014 May; 89:361. PMID: 24631328 - Burke HM et al. Provider acceptability of Sayana® Press: Results from community health workers and clinic-based providers in Uganda and Senegal. Contraception 2014 May; 89:368. PMID: 24576792

Component-of

conjugated estrogens/medroxyprogesterone (Prempro, Premphase) Depo-Provera flavocoxid (Limbrel) Lunelle