megestrol acetate
Megace

Pharmacologic classification: progestin
Therapeutic classification: antineoplastic
Pregnancy risk category X


Available forms
Available by prescription only
Suspension: 200 mg/5 ml
Tablets: 20 mg, 40 mg

Indications and dosages
Dosage and indications may vary. Check current literature for recommended protocol.
 Palliative treatment of breast carcinoma. Adults: 40 mg (tablets) P.O. q.i.d.
 Palliative treatment of endometrial carcinoma. Adults: 10 to 80 mg (tablets) P.O. q.i.d.
 Anorexia, cachexia, or weight loss in patients with AIDS. Adults: 800 mg (suspension) P.O. daily; 100 to 400 mg for AIDS-related cachexia.
 Anorexia or cachexia in patients with neoplastic disease ◇. Adults: 480 to 600 mg P.O. daily.

Pharmacodynamics
Antineoplastic action: Megestrol inhibits growth and causes regression of progestin-sensitive breast and endometrial cancer tissue by an unknown mechanism.
Weight-raising action: Mechanism for weight gain is unknown. Drug may stimulate appetite by interfering with the production of mediators such as cachectin.

Pharmacokinetics
Absorption: Well absorbed across the GI tract.
Distribution: Appears to be stored in fatty tissue and is highly bound to plasma proteins.
Metabolism: Completely metabolized in the liver.
Excretion: Metabolites are eliminated primarily through the kidneys.

Route Onset Peak Duration
P.O. Unknown Unknown Unknown


Contraindications and precautions
Contraindicated in patients hypersensitive to drug and in pregnant women (especially during first 4 months). Use cautiously in patients with history of thrombophlebitis.

Interactions
None reported.

Adverse reactions
CV: thrombophlebitis, hypertension, edema, chest pain.
EENT: pharyngitis.
GI: increased appetite, nausea, vomiting, diarrhea, flatulence.
GU: breakthrough menstrual bleeding, impotence.
Hepatic: hepatomegaly.
Metabolic: weight gain, hyperglycemia.
Musculoskeletal: carpal tunnel syndrome.
Respiratory: pulmonary embolism, dyspnea, pneumonia, cough.
Skin: alopecia, rash, pruritus, candidiasis.
Other: decreased libido.

Effects on lab test results
• May increase glucose levels.

Overdose and treatment
No information available.

Special considerations
• Investigational uses include prevention of pregnancy, treatment of prostatic hypertrophy, endometriosis, and endometrial hyperplasias.
• Glucose levels may increase in diabetic patients.
• Drug is relatively nontoxic with a low risk of adverse effects.
• For patients with cancer, 2 months is an adequate trial period.
• Monitor hematopoietic function and liver function.
• Store tablets at 59° to 86° F (15° to 30° C) and oral suspension at 77° F (25° C) or less.

Patient education
• Inform patient that therapeutic response isn’t immediate.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use