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progesterone (Progestasert, Prometrium, Pro-Gest, Prochieve)

Prepares the uterine endometrium for implantation & for maintenance of pregnancy. Synthesized endogenously from pregnenolone. Pharmacology: Tradenames: Progestasert, Prometrium. Indications: - endometrial carcinoma - renal carcinoma - secondary amenorrhea or abnormal uterine bleeding due to hormonal imbalance - ovarian failure - progesterone insufficiency - Progestasert: intrauterine contraceptive in women who - have had at least one child - are in a stable, mutually monogamous relationship - have no history of pelvic inflammatory disease - oral capsule may be used vaginally for infertility [4] - premature labor [6] - hot flashes - endometrial dysplasia - progesterone challenge test [6] Contraindications: - does not prevent preterm birth or intrauterine death in twin pregnancy Dosage: 1) amenorrhea: 5-10 mg IM QD for 6-8 consecutive days 2) dysfunctional uterine bleeding: 5-10 mg IM QD for 6 days 3) contraception: intrauterine device: insert single system into uterine cavity; contraception is effective for 1 year 4) menopause: in conjunction with estrogen 200 mg PO QHS* Injection: (in oil) 50 mg/mL (10 mL). Intrauterine system: reservoir: 38 mg in silicone fluid. * Prometrium: micronized progesterone capsule, 100, 200 mg (contains peanut oil) (safer alternative for menopause) [7] Crinone: progesterone vaginal cream [2] (contains palm oil) 1) can prevent endometrial hyperplasia 2) alternative to oral progesterone for use in conjunction with estrogen therapy in postmenopausal women Pro-Gest: topical progesterone used for hot flashes (OTC) [3] 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%) - edema, depression, fever, melasma, chloasma, allergic rash with or without pruritus, cholestatic jaundice, changes in cervical erosions & secretions, weight gain or loss, insomnia, increased breast tenderness, thrombophlebitis, central thrombosis & embolism

Interactions

molecular events

Related

progesterone in serum Progesterone receptor; PR; nuclear receptor subfamily 3 group C member 3 (PGR, NR3C3) steroid biosynthesis

Specific

17-hydroxyprogesterone (Duralutin, Makena, Prodrox) methoxyprogesterone

General

adrenal cortex hormone; corticosteroid pregnenedione progestational hormone

Properties

MISC-INFO: pregnancy-category X

Database Correlations

PUBCHEM correlations

References

  1. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  2. Prescriber's Letter 8(7):41 2001
  3. Prescriber's Letter 9(9):52 2002
  4. Prescriber's Letter 13(10): 2006 Alternative or 'Off-label' Routes of Drug Administration Detail-Document#: 221012 (subscription needed) http://www.prescribersletter.com
  5. Norman JE et al Progesterone for the prevention of preterm birth in twin pregnancy (STOPPIT): a randomised, double-blind, placebo- controlled study and meta-analysis Lancet, Early Online Publication, 11 June 2009 PMID: 19523680 doi:10.1016/S0140-6736(09)60947-8
  6. Deprecated Reference
  7. Anello J, Feinberg B, Heinegg J et al Medscape: New Guidelines and Recommendations, August 2017. http://reference.medscape.com/viewarticle/884517

Substructure-of

cortisone (Cortone)

Component-of

estradiol/progesterone