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