Apetiz 160

Generic

Megestrol Acetate

 

Indications

Megestrol acetate is suitable for the palliative treatment of advanced breast cancer or endometrial cancer (ie, recurrent, inoperable or metastatic disease). It should not replace the currently accepted surgery, such as surgery, radiotherapy or chemotherapy.

 

Pharmacology

Megestrol acetate is a synthetic antitumor drug and progesterone. Although the exact mechanism of the antitumor effect of megestrol acetate on endometrial cancer is not yet clear, inhibition of pituitary gonadotropin production and the resulting decrease in estrogen secretion may be factors. The antitumor effect of megestrol acetate on breast cancer is achieved by changing the effects of other steroid hormones and producing direct cytotoxic effects on tumor cells. In metastatic cancer, hormone receptors may be present in some tissues but not others. The receptor mechanism is a cyclical process: estrogen produced by the ovary enters the target cell, forms a complex with the cytoplasmic receptor, and is transported to the nucleus. There it induces gene transcription and causes changes in normal cell function. Pharmacological doses of megestrol acetate can not only reduce the number of hormone-dependent human breast cancer cells, but also change and eliminate the stimulating effect of estrogen on these cells.

The estimated value of the plasma level of megestrol acetate depends on the measurement method used. The peak plasma concentration appears 2 to 3 hours after a single oral 160 mg tablet. The plasma half-life of megestrol acetate is 33 to 38 hours. Approximately 66% of the administered dose is excreted in the urine and approximately 20% is excreted in the faeces.

 

Dosage & Administration

• Breast cancer: 160 mg/day
• Endometrial carcinoma: 40-320 mg/day in divided doses.
• At least 2 months of continuous treatment is considered an adequate period for determining the efficacy of Megestrol.

 

Interaction

Pharmacokinetic studies have shown that when megestrol acetate is administered with these drugs, the pharmacokinetic parameters of zidovudine or rifabutin do not change significantly, and the dosage needs to be adjusted. The effect of zidovudine or rifabutin on the pharmacokinetics of megestrol acetate has not been studied.

 

Contraindications

History of allergy to megestrol acetate or any component of the preparation. Known or suspected pregnancy.

 

Side Effects

Weight gain: Weight gain is a common side effect of megestrol acetate. This increase is related to an increase in appetite, not necessarily fluid retention.

Thromboembolism: Thromboembolism has been reported, including thrombophlebitis and pulmonary embolism (which is fatal in some cases).

Glucocorticoid effect: The glucocorticoid activity of megestrol acetate has not been fully evaluated. Long-term use of megestrol acetate can reportedly lead to new-onset diabetes, exacerbation of existing diabetes, and obvious clinical cases of Cushing's syndrome. In addition, clinical cases of adrenal insufficiency have been observed in patients who received or stopped long-term megestrol acetate treatment under stress and non-stress conditions.

Others: nausea, dyspnea, tumor deterioration, high blood sugar, glucose intolerance, hair loss, high blood pressure, carpal tunnel syndrome, mood swings, hot flashes, malaise, weakness, lethargy, sweating, and rash.

 

Pregnancy & Lactation

The use of category D is not recommended. The use of the Progester medication during the first four months of pregnancy. Very small amounts (around 0.1%) are excreted to the milk of mothers. However, it is not known if these amounts have a detrimental effect on newborns. A newborn nurse should be canceled during treatment with a magnetrol acetate. 

 

Precautions & Warnings

General: Any patient receiving treatment for recurrent or metastatic cancer needs close monitoring. Use with caution in patients with a history of thromboembolism.

 Use in diabetic patients: It has been reported that the use of megestrol acetate may worsen pre-existing diabetes and be accompanied by an increase in insulin demand.

 

Therapeutic Class

Hormonal Chemotherapy.

 

Storage Conditions

Store at or below 25°C. Protect from heat, light & moisture.

 

Pharmaceutical Name

Aristopharma Ltd.