Estrone

What is Estrone

NOTE: These products are discontinued in the U.S.

Estrone is a naturally occurring steroidal estrogen that is one-third less active at the cellular level than estradiol, the principal premenopausal human estrogen.

Estrone is obtained from pregnant equine urine or prepared synthetically. Most commercially available estrone products are synthesized.

There is no evidence that ‘natural’ estrogens are more or less efficacious or safe than ‘synthetic’ estrogens.

Estrone is used primarily to treat vasomotor and urogenital symptoms associated with menopause, and for the prevention of osteoporosis. Estrone has also been used for conditions related to gonadotropin hormone dysfunction.

While many estrogen products were marketed as early as 1938, estrone injections were first FDA-approved in 1979 but have not been commercially marketed in the U.S. for decades.

Estrone is available in bulk products that are sometimes used for compounding estrogen products for specific patient needs.

The North American Menopause Society (NAMS) notes that compounded hormonal therapy can present safety concerns such as minimal government regulation and monitoring, dosing issues, the presence of impurities or lack of sterility, lack of scientific efficacy and safety data, and lack of a label outlining risks.

Prescribers using compounded products are encouraged to document the medical choice of compounded hormones over commercially available FDA-approved therapies

Indications

  1. atrophic vaginitis
  2. breast cancer
  3. dysfunctional uterine bleeding
  4. hot flashes
  5. hypogonadism
  6. menopause
  7. oophorectomy
  8. ovarian failure
  9. prostate cancer

For treatment of moderate to severe vasomotor symptoms (hot flashes) of menopause and/or related genitourinary symptoms including atrophic vaginitis, vulvar atrophy (kraurosis vulvae), whether menopause is natural or surgical (e.g., due to oophorectomy)

Side Effects

  1. abdominal pain
  2. acne vulgaris
  3. alopecia
  4. amenorrhea
  5. anorexia
  6. anxiety
  7. biliary obstruction
  8. breakthrough bleeding
  9. breast discharge
  10. breast enlargement
  11. candidiasis
  12. cervical dysplasia
  13. cervicitis
  14. cholecystitis
  15. cholelithiasis
  16. cholestasis
  17. depression
  18. diarrhea
  19. diplopia
  20. dizziness
  21. dysmenorrhea
  22. edema
  23. elevated hepatic enzymes
  24. emotional lability
  25. endometrial hyperplasia
  26. erythema
  27. erythema nodosum
  28. fatigue
  29. fluid retention
  30. galactorrhea
  31. gingivitis
  32. gynecomastia
  33. headache
  34. hepatitis
  35. hepatoma
  36. hyperglycemia
  37. hypertension
  38. hypocalcemia
  39. impaired cognition
  40. injection site reaction
  41. insomnia
  42. jaundice
  43. keratoconus
  44. libido decrease
  45. libido increase
  46. maculopapular rash
  47. mastalgia
  48. melasma
  49. menorrhagia
  50. migraine
  51. myocardial infarction
  52. nausea
  53. optic neuritis
  54. pancreatitis
  55. peliosis hepatis
  56. pruritus
  57. pulmonary embolism
  58. retinal thrombosis
  59. secondary malignancy
  60. stroke
  61. teratogenesis
  62. thromboembolism
  63. thrombosis
  64. urinary incontinence
  65. urticaria
  66. vaginal bleeding
  67. vaginitis
  68. vomiting
  69. weight gain

Monitoring Parameters

  • pap smear
  • pelvic exam

Contraindications

  • asthma
  • benzyl alcohol hypersensitivity
  • breast cancer
  • breast-feeding
  • cardiac disease
  • cerebrovascular disease
  • cervical cancer
  • children
  • contact lenses
  • coronary artery disease
  • dementia
  • depression
  • diabetes mellitus
  • endometrial cancer
  • endometrial hyperplasia
  • endometriosis
  • gallbladder disease
  • geriatric
  • hepatic disease
  • hepatocellular cancer
  • hypercalcemia
  • hypercholesterolemia
  • hyperlipoproteinemia
  • hypertension
  • hypocalcemia
  • hypoparathyroidism
  • hypothyroidism
  • intravenous administration
  • jaundice
  • migraine
  • myocardial infarction
  • neonates
  • new primary malignancy
  • obesity
  • ovarian cancer
  • pancreatitis
  • paraben hypersensitivity
  • porphyria
  • pregnancy
  • protein C deficiency
  • protein S deficiency
  • renal disease
  • seizure disorder
  • stroke
  • surgery
  • systemic lupus erythematosus (SLE)
  • thromboembolic disease
  • thromboembolism
  • thrombophlebitis
  • thyroid disease
  • tobacco smoking
  • uterine cancer
  • uterine leiomyomata
  • vaginal bleeding
  • vaginal cancer
  • visual disturbance

Interactions

No information is available regarding drug interactions associated with Estrone

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