Ethinyl Estradiol

Ethinyl Estradiol Brand Name– Estinyl

What is Ethinyl Estradiol

NOTE: This drug is discontinued in the US. Ethinyl estradiol is still available as an ingredient in many combination drug products, particularly those for use as combination oral contraceptives (see combination drug monographs).

Ethinyl estradiol is one of the most potent synthetic estrogens.

The presence of the ethinyl group at carbon 17 of ring D of the steroid nucleus greatly slows the hepatic and enzymatic degradation of the molecule and thereby makes oral ethinyl estradiol 15—20 times more active than oral estradiol.

Ethinyl estradiol can be used to prevent osteoporosis and relieve symptoms associated with menopause as well as treat female hypogonadism and other abnormalities of female gonadotropin dysfunction (see Indications). In selected circumstances, estrogens have been used to treat advanced inoperable breast carcinoma in both sexes or prostatic carcinoma.

Ethinyl estradiol is not commonly used as a single agent in clinical practice; the drug is most commonly found in combination oral contraceptive products.

Although ethinyl estradiol by itself is an excellent postcoital contraceptive, it produces a high incidence of nausea/vomiting.

Ethinyl estradiol was FDA approved in 1943.

The manufacture of Estinyl® ceased by Schering Plough in 2000.

Indications

1. atrophic vaginitis
2. hot flashes
3. hypogonadism
4. menopause
5. oophorectomy
6. osteoporosis prophylaxis
7. ovarian failure
8. palliative treatment of breast cancer
9. postcoital contraception
10. prostate cancer

For the treatment of symptoms associated with menopause, such as hot flashes, atrophic vaginitis, and/or vulvar atrophy (kraurosis vulvae)

Side Effects

1. abdominal pain
2. acne vulgaris
3. alopecia
4. amenorrhea
5. anaphylactoid reactions
6. angioedema
7. anorexia
8. anxiety
9. biliary obstruction
10. bowel ischemia
11. breakthrough bleeding
12. breast cancer
13. breast discharge
14. breast enlargement
15. candidiasis
16. cervical dysplasia
17. cervicitis
18. cholecystitis
19. cholelithiasis
20. cholestasis
21. colitis
22. dementia
23. depression
24. diarrhea
25. diplopia
26. dysmenorrhea
27. ectopic pregnancy
28. edema
29. elevated hepatic enzymes
30. emotional lability
31. endometrial cancer
32. endometrial hyperplasia
33. erythema multiforme
34. erythema nodosum
35. fatigue
36. fluid retention
37. galactorrhea
38. gingivitis
39. gynecomastia
40. headache
41. hepatitis
42. hirsutism
43. hypercalcemia
44. hyperglycemia
45. hypertension
46. hypocalcemia
47. impaired cognition
48. insomnia
49. irritability
50. jaundice
51. libido decrease
52. libido increase
53. maculopapular rash
54. mastalgia
55. melasma
56. menorrhagia
57. migraine
58. myocardial infarction
59. nausea
60. new primary malignancy
61. optic neuritis
62. ovarian cancer
63. pancreatitis
64. papilledema
65. peliosis hepatis
66. photosensitivity
67. pruritus
68. pulmonary embolism
69. retinal thrombosis
70. stroke
71. teratogenesis
72. thromboembolism
73. thrombosis
74. urinary incontinence
75. urticaria
76. vaginal bleeding
77. vaginitis
78. visual impairment
79. vomiting
80. weight gain

Monitoring Parameters

• LFTs
• pap smear
• serum lipid profile

Contraindications

• asthma
• 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
• hereditary angioedema
• history of angioedema
• hypercalcemia
• hypercholesterolemia
• hypertension
• hypertriglyceridemia
• hypocalcemia
• hypoparathyroidism
• hypothyroidism
• jaundice
• migraine
• myocardial infarction
• new primary malignancy
• obesity
• ovarian cancer
• pancreatitis
• porphyria
• pregnancy
• protein C deficiency
• protein S deficiency
• renal disease
• salicylate hypersensitivity
• seizure disorder
• stroke
• surgery
• systemic lupus erythematosus (SLE)
• tartrazine dye hypersensitivity
• thromboembolic disease
• thromboembolism
• thrombophlebitis
• thyroid disease
• tobacco smoking
• uterine cancer
• uterine leiomyomata
• vaginal bleeding
• vaginal cancer

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