Mamomit (Tablets) Instructions for Use

Marketing Authorization Holder

Pliva Hrvatska, d.o.o. (Croatia)

ATC Code

L02BG01 (Aminoglutethimide)

Active Substance

Aminoglutethimide (Rec.INN registered by WHO)

Dosage Form

Mamomit

Tablets 250 mg: 100 pcs.

Dosage Form, Packaging, and Composition

100 pcs. – dark glass bottles (1) – cardboard packs.

Clinical-Pharmacological Group

Adrenal cortex hormone synthesis inhibitor

Pharmacotherapeutic Group

Antineoplastic agent, steroid synthesis inhibitor

Pharmacological Action

Antineoplastic agent. Inhibitor of the aromatase enzyme involved in the biosynthesis of steroid hormones. It effectively suppresses the synthesis of cortisol and, to a lesser extent, the synthesis of other steroids (including testosterone, dihydrotestosterone, androstenedione).

It also has a pronounced inhibitory effect on the process of converting androgens into estrogens in various organs and tissues.

Pharmacokinetics

When taken orally, it is rapidly absorbed from the gastrointestinal tract. C_max in plasma is reached within 1.5 hours. Protein binding is 20-25%. It is metabolized in the liver to form N-acetylaminoglutethimide.

T_1/2 is 12.5 hours; after prolonged use, it decreases to 7 hours because Aminoglutethimide is an inducer of liver microsomal enzymes, which increases the rate of its own metabolism. It is excreted by the kidneys – 34-54% unchanged.

Indications

Metastatic breast cancer in the postmenopausal period or after oophorectomy (especially in patients with estrogen-dependent tumors), prostate cancer.

Cushing’s syndrome caused by adrenal cortex hyperplasia, adrenal cortex adenoma or carcinoma (including in the pre- and postoperative period, in inoperable cases), as well as ectopic ACTH production. Hyperaldosteronism.

ICD codes

Dosage Regimen

Determine the dosage individually based on the treated condition, disease stage, and clinical response.

For metastatic breast cancer or prostate cancer, initiate therapy with 250 mg administered orally two to three times daily.

For Cushing’s syndrome, initiate therapy with 250 mg administered orally two to three times daily.

After several weeks of treatment, titrate the dose upwards in increments of 250 mg daily at intervals of one to two weeks, if necessary and if tolerated.

The maximum total daily dose should not exceed 2 grams.

For long-term management of Cushing’s syndrome, adjust the maintenance dose to the lowest effective level based on regular monitoring of plasma cortisol levels.

Administer tablets in divided doses at regular intervals throughout the day, preferably with food or milk.

Concomitantly administer a glucocorticoid replacement (e.g., hydrocortisone) to prevent adrenal insufficiency, typically starting at 20-30 mg hydrocortisone in the morning and 10-20 mg in the evening.

Monitor plasma cortisol levels regularly to guide dosage adjustments of both aminoglutethimide and glucocorticoid replacement therapy.

In the event of severe skin rash or other significant adverse reactions, discontinue treatment immediately.

Adverse Reactions

From the central nervous system rarely – confusion, drowsiness, lethargy (these phenomena usually disappear after 6-8 weeks of treatment), headache, dizziness, depression; with the use of high doses – ataxia.

From the digestive system nausea, diarrhea, cholestasis.

From the endocrine system adrenal cortex insufficiency, suppression of thyroid function (with prolonged use), masculinization and hirsutism.

From the hematopoietic system leukopenia, thrombocytopenia, anemia.

Allergic reactions skin rash, fever; in some cases – exfoliative dermatitis, Stevens-Johnson syndrome, Lyell’s syndrome.

Other arterial hypotension (associated with suppression of aldosterone production); myalgia.

Contraindications

Inducible porphyria, liver dysfunction, pregnancy, hypersensitivity to aminoglutethimide or glutethimide.

Use in Pregnancy and Lactation

Aminoglutethimide is contraindicated during pregnancy. If it is necessary to use during lactation, the issue of discontinuing breastfeeding should be decided.

Women of childbearing age should use non-hormonal contraceptives during treatment.

In experimental studies, the mutagenic and teratogenic effects of aminoglutethimide have been established.

Use in Hepatic Impairment

Contraindication: liver dysfunction.

Use in Renal Impairment

Use with caution in patients with renal impairment.

Geriatric Use

Use with caution in elderly patients due to an increased risk of toxic effects (primarily concerning the central nervous system).

Special Precautions

Use with caution in patients with chickenpox (including recently recovered and after contact with sick individuals), herpes zoster, other acute infectious diseases, hypothyroidism, and renal impairment.

Use with caution in elderly patients due to an increased risk of toxic effects (primarily concerning the central nervous system).

The condition of patients using Aminoglutethimide should be carefully monitored during surgical interventions, injuries, and stressful conditions. In case of severe trauma or shock, Aminoglutethimide should be temporarily discontinued.

During treatment, blood pressure, thyroid function, peripheral blood picture, liver transaminase activity, alkaline phosphatase, and plasma bilirubin levels should be regularly monitored.

In Cushing’s syndrome, regular monitoring of plasma cortisol levels is necessary to correct the doses of aminoglutethimide.

If hypothyroidism develops, replacement therapy with thyroxine should be prescribed.

Effect on the ability to drive vehicles and operate machinery

At the beginning of treatment, the patient should avoid driving vehicles and other potentially hazardous activities.

Drug Interactions

With simultaneous use, Aminoglutethimide reduces the effectiveness of digoxin and theophylline.

With simultaneous use, Aminoglutethimide, being an inducer of cytochrome P450 microsomal enzymes, increases the rate of metabolism of indirect anticoagulants, oral hypoglycemic drugs, glucocorticosteroids, and mineralocorticoids.

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.