Anastrozole

Anastrozole Brand Name– Arimidex

What is Anastrozole

Anastrozole is a nonsteroidal aromatase inhibitor.

Anastrozole is highly potent and specific for aromatase, and represents the fourth generation of aromatase inhibitors.

Anastrozole significantly suppresses serum estradiol levels, and it offers an alternative to tamoxifen in postmenopausal women with breast cancer. Unlike aminoglutethimide, an early aromatase inhibitor, anastrozole does not inhibit adrenal steroid synthesis.

Patients taking anastrozole, therefore, do not require glucocorticoid or mineralocorticoid replacement therapy.

Anastrozole causes less weight gain than megestrol and may offer a survival advantage over megestrol in women with advanced breast cancer.

Aromatase inhibitors are considered to be a standard of therapy and drug class of choice for the treatment of early breast cancer in postmenopausal women with hormone-receptor positive disease.

The American Society of Clinical Oncology recommends that all postmenopausal women with hormone receptor-positive early breast cancer receive adjuvant aromatase inhibitor therapy.

Options include 5 years of an aromatase inhibitor or sequential therapy with 2—3 years or 5 years of tamoxifen followed by 2—3 years or 5 years of an aromatase inhibitor.

The results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial, which compared treatment with anastrozole to tamoxifen for 5 years in women with breast cancer, indicate that anastrozole confers improved disease-free survival compared to tamoxifen.

Long-term data indicate that the improvements in disease-free survival persist for the 5 years during treatment and after drug discontinuation (see Dosage).

Although not FDA-approved, several studies have shown that anastrozole further improves disease-free survival when used sequentially after 2—3 years of tamoxifen when compared to patients taking tamoxifen for 5 years.

Anastrozole was initially FDA-approved for the treatment of advanced breast cancer in postmenopausal women whose disease has progressed during tamoxifen therapy in December 1995.

In September 2000, the FDA approved anastrozole for the first-line treatment of postmenopausal women with advanced or metastatic breast cancer.

Approval for the adjuvant treatment of early breast cancer in postmenopausal women with hormone receptor positive disease was received in September 2002.

Indications

  1. breast cancer
  2. endometriosis
  3. uterine leiomyomata

Side Effects

  1. abdominal pain
  2. alopecia
  3. anemia
  4. angina
  5. angioedema
  6. anorexia
  7. anxiety
  8. arthralgia
  9. asthenia
  10. back pain
  11. bone fractures
  12. bone pain
  13. carpal tunnel syndrome
  14. cataracts
  15. chest pain (unspecified)
  16. confusion
  17. constipation
  18. cough
  19. depression
  20. diaphoresis
  21. diarrhea
  22. dizziness
  23. drowsiness
  24. dyspepsia
  25. dyspnea
  26. edema
  27. elevated hepatic enzymes
  28. erythema multiforme
  29. fatigue
  30. fever
  31. headache
  32. hepatitis
  33. hot flashes
  34. hyperbilirubinemia
  35. hypercalcemia
  36. hypercholesterolemia
  37. hypertension
  38. hypertonia
  39. infection
  40. influenza
  41. jaundice
  42. lethargy
  43. leukopenia
  44. leukorrhea
  45. malaise
  46. myalgia
  47. myocardial infarction
  48. nausea
  49. osteoporosis
  50. paresthesias
  51. pelvic pain
  52. peripheral vasodilation
  53. pharyngitis
  54. phlebitis
  55. pruritus
  56. pulmonary embolism
  57. rash
  58. retinal thrombosis
  59. rhinitis
  60. sinusitis
  61. skin ulcer
  62. spontaneous fetal abortion
  63. Stevens-Johnson syndrome
  64. stroke
  65. teratogenesis
  66. thromboembolism
  67. thrombosis
  68. urticaria
  69. vaginal bleeding
  70. vaginal discharge
  71. vaginal irritation
  72. vaginitis
  73. vomiting
  74. weight gain
  75. weight loss
  76. xerostomia

Monitoring Parameters

  • laboratory monitoring not necessary

Contraindications

  • breast-feeding
  • cardiac disease
  • children
  • hepatic disease
  • osteoporosis
  • pregnancy

Interactions

  • Estrogens
  • Prasterone, Dehydroepiandrosterone, DHEA (Dietary Supplements)
  • Prasterone, Dehydroepiandrosterone, DHEA (FDA-approved)
  • Tamoxifen
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