Lysodren

— THERAPEUTIC CATEGORIES —
  • Pancreatic, thyroid, and other endocrine cancers

Lysodren Generic Name & Formulations

General Description

Mitotane 500mg; scored tabs.

Pharmacological Class

Adrenal cytotoxic agent.

How Supplied

Tabs—100

Storage

Store bottles at 25°C (77°F); excursions permitted between 15°C and 30°C (59–86°F).

Manufacturer

Generic Availability

NO

Mechanism of Action

Mitotane is an adrenal cytotoxic agent with an unknown mechanism of action. Mitotane modifies the peripheral metabolism of steroids and directly suppresses the adrenal cortex.

Lysodren Indications

Indications

Inoperable adrenocortical carcinoma.

Lysodren Dosage and Administration

Adult

Swallow whole. Take with food. 2–6g/day in divided doses (3–4 times/day). Doses may be increased incrementally to achieve a blood concentration of 14–20mg/L, or as tolerated. Dose modifications: see full labeling.

Children

Not established.

Lysodren Contraindications

Not Applicable

Lysodren Boxed Warnings

Boxed Warning

Adrenal crisis in the setting of shock, severe trauma, or infection.

Lysodren Warnings/Precautions

Warnings/Precautions

Risk for adrenal insufficiency and adrenal crisis. Temporarily withhold and give exogenous steroids until recovery during shock, trauma, infection, or adrenal suppression. Withhold treatment prior to planned surgeries. CNS toxicity (esp. mitotane levels >20mg/L). Monitor closely for infections, behavioral and neurologic assessments. Monitor mitotane plasma levels periodically (eg, monthly); consider monitoring levels every 2 weeks after starting treatment, dose adjustments, and regularly (every 2 months) after discontinuation. Evaluate thyroid function if cognitive dysfunction occurs. Ovarian macrocysts in premenopausal women. Perform pelvic ultrasound in premenopausal women at baseline and in regular intervals. Hepatotoxicity. Hematologic toxicity. Monitor LFTs, CBCs including neutrophils prior to initiation, at dose titration, and periodically during treatment. Platelet function disorders. Prolonged bleeding time. Perform ADP-inducted platelet aggregometry testing prior to surgery or dental procedures. Overweight or recent weight loss; monitor mitotane levels closely. Hepatic or renal impairment (mild or moderate): monitor closely and adjust dose; (severe): not recommended. Elderly. Embryo-fetal toxicity. Advise females of reproductive potential to use effective nonhormonal contraception during and after discontinuation until mitotane levels are undetectable. Pregnancy: exclude status prior to initiation. Nursing mothers: not recommended.

Lysodren Pharmacokinetics

Metabolism

Hepatic.

Elimination

Renal, fecal. Half-life: 18–159 days.

Lysodren Interactions

Interactions

Avoid concomitant certain CYP3A4 substrates; if unavoidable, adjust substrate dosage. Avoid concomitant warfarin; if unavoidable, monitor INR frequently and adjust dose. Avoid concomitant hormonal contraceptives. May interfere with hormonal assays by increased plasma levels of hormone binding proteins (eg, sex hormone-binding globulin, corticosteroid-binding globulin).

Lysodren Adverse Reactions

Adverse Reactions

Anorexia, epigastric discomfort, nausea, vomiting, diarrhea, depression, dizziness, vertigo, rash, hypercholesterolemia, hypertriglyceridemia, hypothyroidism, decreased blood free testosterone in males.

Lysodren Clinical Trials

See Literature

Lysodren Note

Not Applicable

Lysodren Patient Counseling

See Literature