Indications
Megestrol Oral Suspension is indicated for the treatment of anorexia, cachexia, or an
unexplained, significant weight loss in patients with a diagnosis of Acquired Immunodeficiency
Syndrome (AIDS) & cancer.
Pharmacology
Several investigators have reported on the appetite-enhancing property of Megestrol Acetate
and its possible use in anorexia, and cachexia. The precise mechanism by which Megestrol Acetate
produces effects in anorexia and cachexia is unknown at the present time but some studies
indicate there is a statistically significant negative correlation between the level of proinflammatory cytokines such as IL1 IL6, and TNF with various nutritional parameters and
improvement in quality of life and weight gain.
Plasma concentrations of Megestrol Acetate are dependent, not only on the method used, but
also on intestinal and hepatic inactivation of the drug, which may be affected by factors such as
intestinal tract motility, intestinal bacteria, antibiotics administered, body weight, diet, and liver
function. The effect of food on the bioavailability of Megestrol Acetate Oral Suspension has not
been evaluated. The major route of drug elimination in humans is urine. The mean elimination
half-life ranged from 20 to 50 hours in healthy subjects.
Dosage & Administration
The recommended adult initial dosage of Megestrol Oral Suspension is 800 mg/day (20 ml/day).
Interaction
Pharmacokinetic studies show that there are no significant alterations in pharmacokinetic
parameters of Zidovudine or Rifabutin to warrant dosage adjustment when Megestrol Acetate
is administered with these drugs. The effects of Zidovudine or Rifabutin on the
pharmacokinetics of Megestrol Acetate were not studied.
Contraindications
History of hypersensitivity to Megestrol Acetate or any component of the formulation. Known
or suspected pregnancy
Side Effects
Adverse events which occurred in at least 5% of patients in any arm of the two clinical efficacy
trials and the open trial are listed below by treatment group. These adverse events should be
considered by the physician when prescribing Megestrol Acetate. Those are- diarrhea,
impotence, rash, flatulence, hypertension, asthenia, insomnia, nausea, anemia, fever, libido
decreased, dyspepsia, hyperglycemia, headache, vomiting, pneumonia & urinary frequency.
Adverse events occurred in 1% to 3% of all patients enrolled in the two clinical efficacy
trials with at least one follow-up visit during the first 12 weeks of the study are listed below by
body system.
▪ Body as a Whole: abdominal pain, chest pain, infection, candidiasis, and sarcoma
▪ Cardiovascular System: cardiomyopathy and palpitation
▪ Digestive System: constipation, dry mouth, hepatomegaly & increased salivation
▪ Hemic and Lymphatic System: leukopenia
▪ Metabolic and Nutritional: LDH increased, edema and peripheral edema
▪ Nervous System: paresthesia, confusion, convulsion, depression, neuropathy,
hypesthesia and abnormal thinking
▪ Respiratory System: dyspnea, cough, and lung disorder
▪ Skin and Appendages: alopecia, herpes, pruritus, vesiculobullous rash, sweating and
skin disorder
▪ Urogenital System: albuminuria, urinary incontinence, urinary tract infection and
gynecomastia
Pregnancy & Lactation
Pregnancy Category X. There are no adequate and well-controlled studies in pregnant women.
If this drug is used during pregnancy, or if the patient becomes pregnant while taking this drug,
the patient should be apprised of the potential hazard to the fetus. Women of childbearing
potential should be advised to avoid becoming pregnant. Because of the potential for adverse
effects on the newborn, nursing should be discontinued if Megestrol Acetate is required.
Precautions & Warnings
General therapy with Megestrol Acetate for weight loss should only be instituted after treatable
causes of weight loss are required and addressed. These treatable causes include possible
malignancies, systemic infections, gastrointestinal disorders affecting absorption, endocrine
disease, and renal or psychiatric diseases. Effects on HIV viral replication have not been
determined. Use with caution in patients with a history of thromboembolic disease. Use in
Diabetics: Exacerbation of pre-existing diabetes with increased insulin requirements has been
reported in association with the use of Megestrol Acetate.
Use in Special Populations
Pediatric Use: Safety and effectiveness in pediatric patients have not been established.
Geriatric Use: In general, dose selection for an elderly patient should be cautious, usually
starting at the low end of the dosing range, reflecting the greater frequency of decreased
hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
Overdose Effects
No serious unexpected side effects have resulted from studies involving Megestrol Acetate
administered in dosages as high as 1200 mg/day.
Therapeutic Class
Hormonal Chemotherapy
Storage Conditions
Store at 20° to 25°C. Protect from heat. Shake well immediately before use.