Megaplex (Tablets) Instructions for Use

ATC Code

G03DB02 (Megestrol)

Active Substance

Megestrol (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Gestagen. Antineoplastic drug

Pharmacotherapeutic Group

Antineoplastic agent – progestogen

Pharmacological Action

Progestogen. It has an antineoplastic effect, which is associated with an antiluteinizing effect realized through the pituitary gland and an action on steroid hormone receptors.

Pharmacokinetics

The plasma concentrations of megestrol depend on the degree of inactivation in the gastrointestinal tract and in the liver, which can be influenced by intestinal tract motility, intestinal microflora, concomitant use of antibiotics, body weight, diet, and the functional state of the liver.

Approximately 5-8% of the administered dose of megestrol accounts for metabolites. The main routes of megestrol excretion are renal (on average approximately 66%) and intestinal (on average approximately 20% of the administered dose). The part of the administered dose that is not detected in urine and feces may be excreted through the respiratory system and accumulate in adipose tissue.

Indications

Palliative treatment of advanced breast cancer or endometrial cancer.

Treatment of anorexia or weight loss in malignant neoplasms or acquired immunodeficiency syndrome.

ICD codes

Dosage Regimen

Establish the dosage individually based on the specific indication, disease stage, and overall antineoplastic therapy plan.

For the palliative treatment of advanced breast cancer, administer 160 mg orally per day as a single dose or in divided doses.

For the palliative treatment of advanced endometrial cancer, administer 40-320 mg orally per day in divided doses.

For the management of anorexia, cachexia, or significant weight loss in patients with AIDS, administer 800 mg orally per day as a single dose.

For the management of anorexia, cachexia, or significant weight loss in patients with cancer, the recommended dosage is 400-800 mg orally per day.

Divide total daily doses exceeding 400 mg into multiple administrations, typically two to four times daily.

Take tablets with or without food; administer with food if gastrointestinal upset occurs.

Continue therapy for as long as a clinical benefit is observed, as determined by the treating physician.

Monitor patients for signs of adrenal insufficiency, particularly during stress or after discontinuation following long-term use.

Do not use in pregnancy, lactation, or in patients under 18 years of age.

Adverse Reactions

Frequently increase in body weight (when used in patients with breast cancer or endometrial cancer – is a consequence of increased appetite).

Rarely thromboembolism, including thrombophlebitis and pulmonary embolism; nausea, vomiting, edema and uterine bleeding not associated with menstruation; dyspnea, pain, heart failure, arterial hypertension, hot flashes, mood changes, cushingoid signs on the face, temporary activation of tumor development (in the absence or presence of hypercalcemia), hyperglycemia, alopecia, carpal tunnel syndrome, diarrhea, lethargy, skin rashes; development of pathological conditions associated with impaired functioning of the pituitary-adrenal system: glucose intolerance, occurrence of diabetes mellitus and exacerbation of existing diabetes mellitus with decreased glucose tolerance and Cushing’s syndrome. In rare cases, patients shortly after discontinuation of megestrol therapy showed clinical signs of adrenal insufficiency. The possibility of suppression of adrenal function should be considered in all patients taking Megestrol for a long time, as well as after its withdrawal.

Contraindications

Hypersensitivity to megestrol; use as a diagnostic test for pregnancy; pregnancy, breastfeeding period; age under 18 years (efficacy and safety not established).

With caution in patients with a history of thrombophlebitis.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and during lactation (breastfeeding).

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Can be used in elderly patients according to indications, no dose adjustment is required.

Special Precautions

Megestrol is not a substitute for surgical treatment, chemotherapy or radiation therapy.

Treatment with megestrol should be carried out under the supervision of a specialist experienced in the use of chemotherapeutic treatment.

During therapy with megestrol and for at least 3 months after the end of therapy, reliable methods of contraception must be used.

Drug Interactions

With simultaneous use with aminoglutethimide, a decrease in the plasma concentration of megestrol is possible, apparently due to the induction of liver microsomal enzymes.

Carbamazepine, griseofulvin, phenobarbital, phenytoin, rifampicin may increase the clearance of progestogens.

Under the influence of progestogens, a change in the effectiveness of hypoglycemic drugs is possible.

Progestogens may inhibit the metabolism of cyclosporine, leading to an increase in its plasma concentration and an increased risk of toxicity.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.