Megestrol

Megestrol Brand Names- Megace | Megace ES

What is Megestrol

Megestrol is a synthetic oral progestin. The drug has slight glucocorticoid and mineralocorticoid activity, but is not estrogenic, androgenic, or anabolic.

Megestrol acetate suspension is used for the treatment of anorexia, cachexia, or an unexplained, significant weight loss in patients with a diagnosis of acquired immunodeficiency syndrome (AIDS).

Megestrol acetate tablets are indicated for the palliative treatment of advanced breast cancer or endometrial cancer and have been used off-label for advanced prostate cancer; megestrol not be used in lieu of currently accepted procedures such as surgery, radiation, or chemotherapy.

Megestrol is considered second- or third-line therapy in the treatment of breast cancer; it is less effective than tamoxifen but as effective as aminoglutethimide.

Megestrol is also used for treating endometriosis and has some utility in treating hot flashes that occur from androgen-deprivation therapy for hormonally-dependent cancers.

Megestrol acetate was first approved by the FDA in 1971. A concentrated suspension of megestrol acetate (Megace ES) was approved in 2005 for the treatment of anorexia, cachexia, or unexplained weight loss in patients with AIDS; the concentrated 625 mg/5 mL suspension of megestrol acetate provides effect similar to 800 mg/20 mL of the regular suspension

Indications

  1. anorexia
  2. breast cancer
  3. cachexia
  4. endometrial cancer
  5. endometriosis
  6. hot flashes
  7. prostate cancer
  8. renal cell cancer

For the treatment of anorexia, cachexia, or unexplained weight loss in patients with acquired immunodeficiency syndrome (AIDS)

Side Effects

  1. abdominal pain
  2. adrenocortical insufficiency
  3. alopecia
  4. amblyopia
  5. anemia
  6. appetite stimulation
  7. asthenia
  8. breakthrough bleeding
  9. candidiasis
  10. cardiomyopathy
  11. carpal tunnel syndrome
  12. chest pain (unspecified)
  13. confusion
  14. constipation
  15. cough
  16. Cushing’s syndrome
  17. depression
  18. diabetes mellitus
  19. diaphoresis
  20. diarrhea
  21. dizziness
  22. dyspepsia
  23. dyspnea
  24. edema
  25. fever
  26. flatulence
  27. gynecomastia
  28. headache
  29. heart failure
  30. hepatomegaly
  31. hot flashes
  32. hypercalcemia
  33. hyperglycemia
  34. hypersalivation
  35. hypertension
  36. hypoesthesia
  37. hypotension
  38. hypothalamic-pituitary-adrenal (HPA) suppression
  39. impaired cognition
  40. impotence (erectile dysfunction)
  41. increased urinary frequency
  42. infection
  43. insomnia
  44. insulin resistance
  45. lethargy
  46. leukopenia
  47. libido decrease
  48. malaise
  49. menstrual irregularity
  50. nausea
  51. palpitations
  52. paresthesias
  53. peripheral edema
  54. peripheral neuropathy
  55. pharyngitis
  56. phlebitis
  57. pruritus
  58. rash
  59. seizures
  60. thromboembolism
  61. thrombosis
  62. urinary incontinence
  63. vesicular rash
  64. vomiting
  65. weakness
  66. weight gain
  67. xerostomia

Monitoring Parameters

  • blood glucose
  • LFTs
  • serum calcium
  • weight

Contraindications

  • adrenal insufficiency
  • breast cancer
  • breast-feeding
  • contraception requirements
  • Cushing’s syndrome
  • diabetes mellitus
  • dysfunctional uterine bleeding
  • females
  • geriatric
  • hepatic disease
  • hyperglycemia
  • hypotension
  • hypothalamic-pituitary-adrenal (HPA) suppression
  • infants
  • infection
  • neoplastic disease
  • pregnancy
  • pregnancy testing
  • renal failure
  • renal impairment
  • reproductive risk
  • surgery
  • thromboembolic disease
  • thrombophlebitis
  • vaginal bleeding
  • vomiting

Megestrol is contraindicated in those patients with a history of hypersensitivity to megestrol acetate or any component of the formulation.

Interactions

  • Dofetilide
  • Entecavir
  • Indinavir
  • Rifamycins
  • Trospium
  • Warfarin
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