Aminoglutethimide
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(British Approved Name, rINN)
Drug Nomenclature
International Nonproprietary Names (INNs) in main languages (French, Latin, Russian, and Spanish):
Pharmacopoeias. In China, Europe, and US.
European Pharmacopoeia, 6th ed., 2008 and Supplements 6.1 and 6.2 (Aminoglutethimide). A white or slightly yellow, crystalline powder. Practically insoluble in water; freely soluble in acetone; soluble in methyl alcohol.
The United States Pharmacopeia 31, 2008 (Aminoglutethimide). A white or creamy-white, fine, crystalline powder. Very slightly soluble in water; readily soluble in most organic solvents. It forms water-soluble salts with strong acids. The pH of a 0.1% solution in dilute methyl alcohol (1 in 20) is between 6.2 and 7.3.
Adverse Effects
The most frequent adverse effects reported with aminoglutethimide include drowsiness, lethargy, and skin rashes (sometimes with fever); these generally diminish after the first 6 weeks of therapy. Dizziness and nausea occasionally occur. Leucopenia, thrombocytopenia, agranulocytosis, or severe pancytopenia have occurred rarely. Adrenal insufficiency may rarely occur, and there have been reports of other endocrine disturbances including hypothyroidism, and virilisation. Other rare effects include ataxia, headache, depression, gastrointestinal disturbances, hy-percholesterolaemia, and orthostatic hypotension. Overdosage may lead to CNS depression and impairment of consciousness, electrolyte disturbances, and respiratory depression.
Effects on the liver. Aminoglutethimide has been associated with reports of cholestatic jaundice, accompanied by rash and fever, and probably due to an idiosyncratic hypersensitivity reaction. It has been suggested that liver function tests should be carried out in patients receiving aminoglutethimide who develop fever and eruptions.
Effects on the lungs. Pulmonary infiltrates in a patient who developed progressive dyspnoea on starting therapy with aminoglutethimide were found to be due to diffuse alveolar damage and haemorrhage; thrombocytopenia was present but prothrombin and bleeding times were normal. The patient’s gas exchange and chest radiographs improved on stopping aminoglutethimide and giving corticosteroids. Blood and pulmonary eosinophilia, which resolved on stopping aminoglutethimide therapy, has also been reported.
Lupus. SLE occurred in a patient who received aminoglutethimide, and resolved when the drug was withdrawn. In another report, however, a patient with a lupus-like syndrome had a reduction in disease activity when tamoxifen therapy was changed to aminoglutethimide.
Precautions
Aminoglutethimide inhibits adrenal steroid production so supplementary glucocorticoid therapy with hydro cortisone must normally be given, although supplementation may not be necessary in patients with Cushing’s syndrome. Some patients also require a mineralocorticoid. It has been suggested that aminoglutethimide should be temporarily withdrawn in patients who undergo shock or trauma, or develop intercurrent infection. Blood pressure, blood counts, and serum electrolytes should be regularly monitored during aminoglutethimide therapy and periodic monitoring of liver and thyroid function is recommended. Aminoglutethimide should not be given during pregnancy as pseudohermaphroditism may occur in the fetus.
Aminoglutethimide frequently causes drowsiness: patients so affected should not drive or operate machinery.
Porphyria. Aminoglutethimide has been associated with acute attacks of porphyria and is considered unsafe in porphyric patients.
Interactions
The rate of metabolism of some drugs is increased by aminoglutethimide; patients also taking warfarin or other coumarin anticoagulants, theophylline, tamoxifen, medroxyprogesterone, or oral hypoglycaemics, may require increased dosages of these drugs. The metabolism of dexamethasone is also accelerated, which limits its value for corticosteroid supplementation in patients receiving aminoglutethimide. Use with diuretics may lead to hyponatraemia, while alcohol may potentiate the central effects of aminoglutethimide.
Pharmacokinetics
Aminoglutethimide is well absorbed after oral doses, with peak plasma concentrations occurring after 1 to 4 hours. It is metabolised in the liver, primarily to N-hydroxylaminoglutethimide and N-acetylaminoglutethimide, and appears to induce its own metabolism. The half-life, which is reported to be about 13 hours after a single dose, is decreased to around 9 hours after about 2 weeks of continuous therapy. Aminoglutethimide is excreted in urine, about half a dose being excreted unchanged and the remainder as metabolites. Only about 20 to 25% of a dose is bound to plasma protein.
Half-life. A study in 17 patients showed that the plasma half-life of aminoglutethimide had a mean value of 15.5 hours after single doses but fell to 8.9 hours during multiple-dose therapy. This marked reduction could largely be attributed to a decrease in the volume of distribution; auto-induction of metabolism might be of less importance in decreasing half-life than had been previously suggested.
Uses and Administration
Aminoglutethimide is an analogue of glutethimide and was formerly used for its weak anticonvulsant properties. Aminoglutethimide blocks the production of adrenal steroids and acts as an aromatase inhibitor to block the conversion of androgens to oestrogens (the major source of oestrogens in women without ovarian function). It was used in the treatment of meta-static breast cancer in postmenopausal or oophorect-omised women and as palliative treatment in men with advanced prostatic cancer.
Aminoglutethimide has also been used in the treatment of Cushing’s syndrome. Usual oral doses range from 1 to 2 g daily, in divided doses.
The dextroisomer of aminoglutethimide, dexaminoglutethimide has been investigated.
Preparations
British Pharmacopoeia 2008: Aminoglutethimide Tablets
The United States Pharmacopeia 31, 2008: Aminoglutethimide Tablets
Single-ingredient Preparations
The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed
Argentina: Orimeten¤; Australia: Cytadren; Austria: Orimeten¤; Belgium: Orimeten¤; Brazil: Orimeten¤; Canada: Cytadren¤; Chile: Orimeten¤; Czech Republic: Orimeten¤; France: Orimetene¤; Germany: Orimeten¤; Rodazol¤; Hong Kong: Orimetene; Ireland: Orimeten¤; Israel: Orimetene¤; Italy: Orimeten¤; Malaysia: Orimetene¤; Netherlands: Orimeten¤; Norway: Orimeten¤; New Zealand: Cytadren¤; Russia: Mamomit (Мамомит); Orimeten (Ориметен)¤; South Africa: Aminoblastin¤; Orimeten¤; Spain: Orimeten¤; Sweden: Orimeten¤; Switzerland: Orimetene¤; United Kingdom: Orimeten¤; United States: Cytadren
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