Raloxifene

What is Raloxifene

Raloxifene is a selective estrogen receptor modulator (SERM) of the benzothiophene class.

Similar to tamoxifen, raloxifene produces estrogen-like effects on bone and lipid metabolism, while antagonizing the effects of estrogen on mammary tissue. However, unlike estrogen or tamoxifen, it does not stimulate uterine tissue and behaves as an estrogen antagonist in the uterus.

Raloxifene’s pharmacologic effects make it a useful agent for the prevention of postmenopausal osteoporosis; although it is not useful for postmenopausal hot flashes.

The effect of 60 mg/day on total-body bone mineral density is similar to that of estrogen/progestin HRT or alendronate 5 mg/day, but, the effect on bone mineral density of the lumbar spine may be less.

Raloxifene has been shown to significantly decrease the incidence of vertebral fractures, but not other fractures, in clinical trials.

According to the North American Menopause Society (NAMS), it is often considered for women who are at increased risk of vertebral fracture versus hip fracture (see Indications/Dosage for the patient populations for which NAMS recommends pharmacological treatment).

Brand Name

Evista

Indications & Dosage

  • breast cancer prophylaxis
  • osteoporosis
  • osteoporosis prophylaxis
  • uterine leiomyomata

For the treatment of osteoporosis or for osteoporosis prophylaxis in postmenopausal women

Side Effects

  1. abdominal pain
  2. arthralgia
  3. chest pain (unspecified)
  4. cholelithiasis
  5. conjunctivitis
  6. cough
  7. cystitis
  8. depression
  9. diarrhea
  10. dyspepsia
  11. fever
  12. flatulence
  13. headache
  14. hot flashes
  15. hyperhidrosis
  16. hypoesthesia
  17. infection
  18. influenza
  19. insomnia
  20. laryngitis
  21. leukorrhea
  22. mastalgia
  23. migraine
  24. muscle cramps
  25. myalgia
  26. nausea
  27. neuropathic pain
  28. peripheral edema
  29. pharyngitis
  30. phlebitis
  31. pulmonary embolism
  32. rash
  33. retinal thrombosis
  34. rhinitis
  35. sinusitis
  36. stroke
  37. syncope
  38. thromboembolism
  39. thrombosis
  40. vaginal bleeding
  41. vaginitis
  42. vertigo
  43. vomiting
  44. weight gain

Monitoring Parameters

  • LFTs

Contraindications

  • atrial fibrillation
  • breast cancer
  • breast-feeding
  • cardiac disease
  • cerebrovascular disease
  • children
  • coronary artery disease
  • heart failure
  • hepatic disease
  • hypertension
  • hypertriglyceridemia
  • infants
  • infertility
  • mortality
  • neoplastic disease
  • pregnancy
  • renal failure
  • renal impairment
  • reproductive risk
  • stroke
  • surgery
  • thromboembolic disease
  • thromboembolism
  • thrombophlebitis
  • tobacco smoking
  • vaginal bleeding

Interactions

  • Cholestyramine
  • Conjugated Estrogens
  • Conjugated Estrogens; Bazedoxifene
  • Conjugated Estrogens; Medroxyprogesterone
  • Dienogest; Estradiol valerate
  • Diethylstilbestrol, DES
  • Drospirenone; Estradiol
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Elagolix; Estradiol; Norethindrone acetate
  • Esterified Estrogens
  • Esterified Estrogens; Methyltestosterone
  • Estradiol
  • Estradiol Cypionate; Medroxyprogesterone
  • Estradiol; Levonorgestrel
  • Estradiol; Norethindrone
  • Estradiol; Norgestimate
  • Estradiol; Progesterone
  • Estrogens
  • Estropipate
  • Ethinyl Estradiol
  • Ethinyl Estradiol; Desogestrel
  • Ethinyl Estradiol; Ethynodiol Diacetate
  • Ethinyl Estradiol; Etonogestrel
  • Ethinyl Estradiol; Levonorgestrel
  • Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Fluoroestradiol F 18
  • Levothyroxine
  • Levothyroxine; Liothyronine (Porcine)
  • Levothyroxine; Liothyronine (Synthetic)
  • Liothyronine
  • Mestranol; Norethindrone
  • Ospemifene
  • Segesterone Acetate; Ethinyl Estradiol
  • Thyroid hormones
  • Warfarin