mitotane

Contraindicated in:

Hypersensitivity
OB: Pregnancy
Lactation: Lactation.

Use Cautiously in:

Obesity (↑ risk of adverse reactions)
Premenopausal women (↑ risk of ovarian macrocysts)
Rep: Women of reproductive potential
Pedi: Safety and effectiveness not established in children.

Exercise Extreme Caution in:

Shock, severe trauma, or infection (↑ risk of adrenal crisis).

Adv. Reactions/Side Effects ⬆ ⬇

CV: hypertension, hypotension.

Derm: maculopapular rash, flushing.

EENT: ↓hearing, blurred vision, diplopia, lens opacities, optic neuritis, toxic retinopathy.

Endo: adrenal suppression, ADRENAL CRISIS, gynecomastia, hypothyroidism.

GI: anorexia, diarrhea, nausea, vomiting, HEPATOTOXICITY, ↑ liver enzymes, ↑ salivation.

GU: albuminuria, hematuria, hemorrhagic cystitis, ovarian macrocysts.

Hemat: anemia, ↑bleeding time, leukopenia, thrombocytopenia.

Metab: hypercholesterolemia, hypouricemia.

MS: arthralgia, myalgia.

Neuro: lethargy, somnolence, brain damage, dizziness, fatigue, functional impairment (high-dose, long-term therapy), headache, irritability, mental depression, tremors, vertigo, weakness.

Resp: dyspnea, wheezing.

Misc: fever.

Interactions ⬆ ⬇

Drug-Drug:

May ↓ levels and effectiveness of CYP3A4 substrates; avoid concomitant use with narrow therapeutic index substrates; if concurrent use is unavoidable, ↑ dose of CYP3A4 substrate.
May ↓ levels and effectiveness of warfarin.
Additive CNS depression with other CNS depressants, including alcohol, antihistamines, antidepressants, opioid analgesics, or sedative/hypnotics.

Availability ⬆ ⬇

Tablets: 500 mg;

Route/Dosage ⬆ ⬇

Adrenocortical Carcinoma

PO (Adults): 2–6 g/day in 3–4 divided doses; may be ↑ as tolerated (range 2–16 g/day).

Cushing’s Syndrome

PO (Adults): 3–6 g/day in 3–4 divided doses initially; ↓ to maintenance dose of 500 mg twice weekly to 2 g/day.

US Brand Names ⬆ ⬇

Action ⬆ ⬇

Suppresses adrenal function.
Has a direct cytotoxic effect on adrenal tumors.
Structurally related to DDT (an insecticide).

Therapeutic Effects:

Regression of adrenal cortical tumors.

Classifications ⬆ ⬇

Therapeutic Classification: antineoplastics

Pharmacokinetics ⬆ ⬇

Absorption: 30–40% absorbed following oral administration.

Distribution: Widely distributed to all body tissues; accumulates in fatty tissue.

Metabolism/Excretion: Slowly released from fatty tissue. Mostly metabolized by the liver; 10% excreted by the kidneys; 15% excreted in bile.

Half-life: 18–159 days.

Time/Action Profile ⬆ ⬇

(clinical effects†)

ROUTE	ONSET	PEAK	DURATION
PO	2–4 wk	6 wk	unknown

†Onset = inhibition of adrenocortical function; peak = tumor response.

Patient/Family Teaching ⬆ ⬇

Instruct patient to take medication exactly as directed. Take missed doses as soon as remembered unless almost time for next dose. Notify health care provider of missed doses.
Teach patient that taking the medication regularly with fatty food aids absorption. Advise to not crush or chew the tablets; tablets should be swallowed whole.
Caregivers and family that assist in medication administration should be advised to wear disposable gloves. Medication should be kept away from children.
Explain to patient that this drug suppresses the adrenal glands and therefore impairs the body’s ability to cope with stress. Concurrent corticosteroid and mineralocorticoid therapy may be ordered to ensure that adequate amounts of adrenal hormones are present. Health care provider should be notified if an infection, illness, or injury occurs; supplemental steroids may be necessary or mitotane may need to be discontinued in the event of severe trauma or shock.
May cause drowsiness. Caution patient to avoid driving or other activities requiring alertness until response to medication is known.
Instruct patient to notify health care provider if vaginal bleeding, pelvic pain, abdominal pain or bloating, depression, dizziness/vertigo, nausea, vomiting, anorexia, diarrhea, skin rash, or darkening of skin or urine occurs or if muscle aches, fever, flushing, or muscle twitching become pronounced.
Instruct patient to notify health care provider of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care provider before taking other medications. Avoid taking alcohol or other CNS depressants with this medication.
Rep: May cause fetal harm. Advise females of reproductive potential to use an effective nonhormonal form of contraception during and following therapy for as long as instructed by health care provider. Advise patient to notify health care provider if pregnancy is planned or suspected and to avoid breastfeeding during therapy.
Advise patient to carry identification describing medication regimen in the event of an emergency in which patient cannot relate medical history.
Explain need for continued medical follow-up, including neurologic exam to assess effectiveness and possible side effects of medication.

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Indications ⬇

Contraind./Precautions ⬆ ⬇