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Cytadren: Full Drug Profile

Medically reviewed by Min Clinic Staff | Updated: January 2026

Cytadren - General Information

An aromatase inhibitor that produces a state of "medical" adrenalectomy by blocking the production of adrenal steroids. It also blocks the conversion of androgens to estrogens. Cytadren has been used in the treatment of advanced breast and prostate cancer. It was formerly used for its weak anticonvulsant properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p454)

 

Pharmacology of Cytadren

Cytadren inhibits the enzymatic conversion of cholesterol to D5-pregnenolone, resulting in a decrease in the production of adrenal glucocorticoids, mineralocorticoids, estrogens, and androgens.

 

Cytadren for patients

Patients should be warned that drowsiness may occur and that they should not drive, operate potentially dangerous machinery, or engage in other activities that may become hazardous because of decreased alertness.

Patients should also be warned of the possibility of hypotension and its symptoms.

 

Cytadren Interactions

Cytadren accelerates the metabolism of dexamethasone; therefore, if glucocorticoid replacement is needed, hydrocortisone should be prescribed.

Aminoglutethimide diminishes the effect of coumarin and warfarin.

 

Cytadren Contraindications

Cytadren is contraindicated in those patients with serious forms, and/or more severe manifestations, of hypersensitivity to glutethimide or aminoglutethimide.

 

Additional information about Cytadren

Cytadren Indication

For the suppression of adrenal function in selected patients with Cushing's syndrome, malignant neoplasm of the female breast, and carcinoma in situ of the breast.

Mechanism Of Action
Cytadren reduces the production of D5-pregnenolone and blocks several other steps in steroid synthesis, including the C-11, C-18, and C-21 hydroxylations and the hydroxylations required for the aromatization of androgens to estrogens, mediated through the binding of aminoglutethimide to cytochrome P-450 complexes. A decrease in adrenal secretion of cortisol is followed by an increased secretion of pituitary adrenocorticotropic hormone (ACTH), which will overcome the blockade of adrenocortical steroid synthesis by aminoglutethimide. The compensatory increase in ACTH secretion can be suppressed by the simultaneous administration of hydrocortisone. Since aminoglutethimide increases the rate of metabolism of dexamethasone but not that of hydrocortisone, the latter is preferred as the adrenal glucocorticoid replacement. Although aminoglutethimide inhibits the synthesis of thyroxine by the thyroid gland, the compensatory increase in thyroid-stimulating hormone (TSH) is frequently of sufficient magnitude to overcome the inhibition of thyroid synthesis due to aminoglutethimide. In spite of an increase in TSH, aminoglutethimide has not been associated with increased prolactin secretion.
Drug Interactions
Anisindione The agent decreases the anticoagulant effect
Food Interactions
Take without regard to meals.
Generic Name
Aminoglutethimide
Synonyms
Dl-Aminoglutethimide; P-Aminoglutethimide
Drug Category
Antineoplastic Agents; Adrenergic Agents
Drug Type
Small Molecule; Approved
Other Brand Names containing Aminoglutethimide
Cytadren; Elipten; Orimeten;
Absorption
Rapidly and completely absorbed from gastrointestinal tract. The bioavailability of tablets is equivalent to equal doses given as a solution.
Toxicity (Overdose)
Oral LD50s (mg/kg): rats, 1800; dogs, >100. Intravenous LD50s (mg/kg): rats, 156; dogs, >100. Symptoms of overdose include respiratory depression, hypoventilation, hypotension, hypovolemic shock due to dehydration, somnolence, lethargy, coma, ataxia, dizziness, fatigue, nausea, and vomiting.
Protein Binding
21-25%
Biotransformation
Hepatic. 34-54% of the administered dose is excreted in the urine as unchanged drug during the first 48 hours, and an additional fraction as an N-acetyl derivative.
Half Life
12.5 ± 1.6 hours
Dosage Forms of Cytadren
Tablet Oral
Chemical IUPAC Name
3-(4-aminophenyl)-3-ethylpiperidine-2,6-dione
Chemical Formula
C13H16N2O2
Organisms Affected
Humans and other mammals