Trilostane

(BAN, USAN, pINN)
Trilostane Chemical formula
Synonyms: Trilostaani; Trilostan; Trilostano; Trilostanum; Win-24540. 4α,5αEpoxy-17
Cyrillic synonym: Трилостан.

💊 Chemical information

Chemical formula: C20H27NO3 = 329.4.
CAS — 13647-35-3.
ATC — H02C A01.
ATC Vet — QH02CA01.

💊 Adverse Effects

Adverse effects associated with trilostane have included flushing, nausea, vomiting, diarrhoea, rhinorrhoea, and tingling and swelling of the mouth. Skin rashes may occur and, rarely, granulocytopenia in immunocompromised patients.

💊 Precautions

Trilostane is contra-indicated in pregnancy and should be used with caution in patients with renal or hepatic impairment. Circulating corticosteroids and blood electrolytes should be monitored. In some patients, supplementation with corticosteroids may be necessary.

💊 Interactions

Trilostane may interfere with the activity of oral contraceptives. Hyperkalaemia may occur if trilostane is given with potassiumsparing diuretics or aldosterone antagonists.

💊 Uses and Administration

Trilostane is an adrenocortical suppressant that inhibits the enzyme system essential for the production of glucocorticoids and mineralocorticoids. It is used for the treatment of adrenal cortical hyperfunction such as Cushing’s syndrome and primary hyperaldosteronism. It is also used in postmenopausal breast cancer that has relapsed after oestrogen antagonist therapy. The usual daily dose in adrenal cortical hyperfunction is 240 mg orally in divided doses for at least 3 days and then adjusted, according to response, within the range of 120 to 480 mg daily. Doses of 960 mg daily have been given. In postmenopausal breast cancer an initial daily dose of 240 mg is given in divided doses, with glucocorticoid replacement therapy. This is increased in steps of 240 mg every 3 days up to a maintenance dose of 960 mg daily; this may be reduced to 720 mg daily if adverse effects are intolerable.

💊 Preparations

Proprietary Preparations

Jpn: Desopan; UK: Modrenal.
Published May 08, 2019.