Mitotane

Oral
Inoperable adrenocortical tumours

Oral
Cushing's syndrome

Dose reduction may be required.

Should be taken with food.

Adrenocortical insufficiency may develop; corticosteroid therapy is often required. Temporarily discontinue treatment and administer systemic corticosteroids in cases of trauma, infection or shock. Renal or hepatic impairment. Surgically remove all possible tumour tissue from large metastases prior to therapy. Perform regular behavioural and neurological assessments in patients receiving treatment for ≥2 yr. Monitor plasma levels (therapeutic window: 14-20 mcg/l). Monitor hepatic function. May affect ability to drive or operate machinery. Pregnancy and lactation.

CNS depression, somnolence, dizziness/vertigo, headache, confusion; skin rash; anorexia, nausea, vomiting, diarrhoea; weakness, muscle tremor; albuminuria, blurred vision, diplopia, flushing, haematuria, haemorrhagic cystitis, hypertension, hyperpyrexia, lens opacity, myalgia, orthostatic hypotension, decreased protein-bound iodine, toxic retinopathy.
Potentially Fatal: Possible permanent brain damage.

PO: D

Symptoms: Diarrhoea, vomiting, numbness of limbs, weakness. Management: Symptomatic and supportive.

May reduce the effects of coumarin anticoagulants, barbiturates, phenytoin. Reduced effects with spironolactone. CNS depression may occur with alcohol.

Absorption increases with food.

Urinary tetrahydrocortisol and tetrahydrocortisone glucuronides (measurable 17-OHCS) may be reduced in the 1st several wk of mitotane therapy. May interfere with certain thyroid function tests since it competitively binds to thyroxine-binding globulin and decreases serum protein-bound iodine.

Description:
Mechanism of Action: Mitotane is an antineoplastic with a selective inhibitory action on adrenal cortex activity causing tissue necrosis and atrophy. It can also modify peripheral metabolism of steroids.
Pharmacokinetics:
Absorption: 35-40% of a dose absorbed from the GI tract; absorption increases with food.
Distribution: Widely distributed and appears to be stored mainly in fatty tissues.
Metabolism: Metabolised in the liver and other tissues.
Excretion: Via urine and bile as metabolites. Elimination half-life: 18-159 days.

Store at room temperature.

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