Mitotane

Mitotane is a prescription medication used to treat cancer of the adrenal gland (adrenal cortical carcinoma). 

• Mitotane is available under the following different brand names: Lysodren 

Common side effects of Mitotane include:

• Dizziness,
• Spinning sensation (vertigo),
• Drowsiness,
• Tiredness,
• Nausea,
• Vomiting,
• Diarrhea,
• Loss of appetite,
• Headache,
• Unusual weakness,
• Depression, or
• Skin rash.

Serious side effects of Mitotane include:

• Severe dizziness,
• Flushing,
• Fast or pounding heartbeat,
• Shakiness (tremors),
• Unusual or rapid weight loss,
• Change in skin color or thickness,
• Easy bleeding or bruising,
• Breast tenderness or enlargement (males),
• Unwanted facial or body hair (females),
• Mental/mood changes (e.g., depression, irritability, difficulty concentrating, confusion),
• Speech problems,
• Numbness or tingling of hands or feet,
• Unsteadiness,
• Pink urine, or
• Vision problems.

Rare side effects of Mitotane include:

• none 

Seek medical care or call 911 at once if you have the following serious side effects:

• Severe headache, confusion, slurred speech, arm or leg weakness, trouble walking, loss of coordination, feeling unsteady, very stiff muscles, high fever, profuse sweating, or tremors;
• Serious eye symptoms such as sudden vision loss, blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
• Serious heart symptoms include fast, irregular, or pounding heartbeats; fluttering in the chest; shortness of breath; sudden dizziness, lightheadedness, or passing out

This is not a complete list of side effects and other serious side effects or health problems that may occur because of the use of this drug. Call your doctor for medical advice about serious side effects or adverse reactions. You may report side effects or health problems to FDA at 1-800-FDA-1088.

Adult and pediatric dosage

Tablet

• 500 mg

Adrenal Carcinoma

Adult dosage

• Initial: 2-6 g/day orally divided every 6-8hours, THEN
• Increase incrementally to 9-10 g/day divided every 6-8 hours
• The maximum tolerated dose varies from 2-16 g/day, usually 9-10 g/day
• The highest doses used in clinical trials were 18-19 g/day

Dosage Considerations – Should be Given as Follows: 

• See “Dosages”

If your medical doctor is using this medicine to treat your pain, your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with your doctor, health care provider, or pharmacist first.

• Mitotane has severe interactions with the following drugs:
  • Cariprazine
  • Cobimetinib
  • Doravirine
  • Elbasvir/grazoprevir
  • Fostemsavir
  • Isavuconazonium sulfate
  • Lonafarnib
  • Lorlatinib
  • Lumacaftor/ivacaftor
  • Mavacamten
  • Naloxegol
  • Nirmatrelvir
  • Nirmatrelvir/ritonavir
  • Ombitasvir/paritaprevir/ritonavir & dasabuvir (dsc)
  • Panobinostat
  • Praziquantel
• Mitotane has serious interactions with at least 88 other drugs.
• Mitotane has moderate interactions with at least 262 other drugs.
• Mitotane has minor interactions with the following drug:
  • Omeprazole

This information does not contain all possible interactions or adverse effects. Visit the RxList Drug Interaction Checker for any drug interactions. Therefore, before using this product, tell your doctor or pharmacist about all your products. Keep a list of all your medications with you and share this information with your doctor and pharmacist. Check with your healthcare professional or doctor for additional medical advice, or if you have health questions or concerns.

Contraindications

• Hypersensitivity 

Effects of drug abuse

• None

Short-Term Effects

• See “What Are Side Effects Associated with Using Mitotane?”

Long-Term Effects

• See “What Are Side Effects Associated with Using Mitotane?”

Cautions

• Discontinue immediately following shock or severe trauma; exogenous steroid should be administered in such circumstances
• Adrenal insufficiency may develop requiring adrenal steroid replacement
• Patients with liver disease in addition to a metastatic lesion of the adrenal cortex
• Long-term administration of high doses may lead to brain damage
• Mitotane plasma concentrations above 20 mcg/mL are associated with a greater incidence of high-grade CNS toxicity
• Increases hormone binding proteins and measurement of free cortisol and corticotropin (ACTH) levels may be useful in achieving optimal steroid replacement
• Prolonged bleeding time reported; consider this possibility before any surgical intervention or if coadministered with anticoagulants
• Reduces tumor mass but no evidence of cure
• Advise women of the reproductive potential of risks to a fetus; use effective contraception
• Ovarian macrocysts, often bilateral and multiple, were reported in premenopausal patients; complications from cysts, including adnexal torsion and hemorrhagic cyst rupture, were reported; in some cases, improvement after mitotane discontinuation was reported; advise female patients to seek medical care if they experience gynecological symptoms such as vaginal bleeding and/or pelvic pain
• Decreased blood androstenedione and decreased blood testosterone were reported in females; increased sex hormone binding globulin in females and males, decreased blood-free testosterone in males
• Drug interaction overview
  • Mitotane is a potent CYP3A inducer; concomitant use of mitotane may decrease concentrations of CYP3A substrates, which may reduce e efficacy of these substrates
  • Avoid concomitant use of mitotane with certain CYP3A4 substrates where minimal concentration changes may lead to therapeutic failure; if concomitant use cannot be avoided, increase CYP3A substrate dosage by approved product labeling

Pregnancy and Lactation

• Use in LIFE-THREATENING emergencies when no safer drug is available.
• Lactation
  • Detected in breast milk; because of the potential for serious adverse reactions in nursing infants from mitotane, advise women to discontinue nursing during therapy and after treatment discontinuation for as long as mitotane plasma levels are detectable.