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Home / Hormones / Progestin Hormone / APEIN
Hormones

APEIN

Megestrol acetate is a synthetic progestin medication used primarily as an appetite stimulant to treat anorexia, cachexia, or unexplained significant weight loss in patients with cancer or AIDS. It is also used in high doses for the palliative treatment of advanced hormone-sensitive breast and endometrial cancers.

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General Info

Category:

Antineoplastics, Hormone, Appetite Stimulant

Product information:

Generic name: MEGESTROL ACETATE
Composition: Each film coated tablet contains Megestrol Acetate 40 mg / 160 mg
Pharmacological Category: Progestin (Synthetic Progesterone)
Pregnancy Category: X
Lactation: Not recommended
Presentation: 5 x 10’s blister pack

INDICATIONS:
  • Advanced breast cancer (especially hormone receptor-positive types)
  • Endometrial carcinoma
  • Anorexia, cachexia, or unexplained significant weight loss in patients with AIDS or cancer
MECHANISM OF ACTION:

Megestrol Acetate works primarily as a synthetic progestin, but it also exhibits anti-gonadotropic and glucocorticoid-like activity. It helps:
For Cancer-related Cachexia & Anorexia:

  • Binds to progesterone receptors
  • Enhances appetite via central mechanism
  • Leads to increased calorie intake and weight gain

 

For Hormone-sensitive Cancers:

  • Suppresses luteinizing hormone (LH) and follicle-stimulating hormone (FSH)
  • Inhibits estrogen-dependent tumor growth in breast/endometrial cancer

 

↓ Hypothalamic-Pituitary-Gonadal Axis suppression
↓ Estrogen production
↓ Tumor stimulation
↓
Tumor regression or slowed progression

 

Pharmacokinetics:

Absorption: Well absorbed orally
Bioavailability: High
Onset of action: Within days to weeks (for weight gain)
Metabolism: Hepatic (liver)
Excretion: Primarily via urine and feces

Dosage Information:

Adults: 160 mg/day (divided or once daily) for cancer-related anorexia or cachexia. 40–320 mg/day depending on indication and response for cancer therapy

Note: Dosage must be individualized and supervised by a physician, especially for cancer therapy.

Side Effects:
  • Weight gain (desired in some indications)
  • Edema (fluid retention)
  • Increased blood sugar levels
  • Thromboembolic events (DVT, pulmonary embolism)
  • Hypertension
  • Menstrual irregularities
  • Mood changes
Contraindications:
  • Pregnancy (Category X – contraindicated)
  • Known hypersensitivity to Megestrol Acetate
  • Active or recent history of thrombosis or embolism
Precautions :

Use with caution in patients with:

    • History of thromboembolism
    • Diabetes mellitus
    • Hypertension
      • Monitor weight and blood pressure
      • Long-term use can cause adrenal suppression

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