Aminoglutethimide
Pronouncation: (ah-MEE-no-glue-TETH-ih-mide)Class: Adrenal steroid inhibitor
Trade Names:
Cytadren
- Tablets 250 mg
Pharmacology
Feedback for Aminoglutethimide
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Aminoglutethimide inhibits the enzymatic conversion of cholesterol to Δ 5 -pregnenolone, thereby reducing the synthesis of adrenal glucocorticoids, mineralocorticoids, estrogens, and androgens.
Pharmacokinetics
Absorption
Rapidly and completely absorbed. C max is about 5.9 mcg/mL; T max is about 1.5 h.
Distribution
Minimally bound to proteins.
Elimination
T ½ is about 12.5 h. 34.54% is excreted in urine as unchanged drug.
Indications and Usage
Suppression of adrenal function in patients with Cushing syndrome.
Unlabeled Uses
Suppression of adrenal function in advanced breast carcinoma or metastatic prostate carcinoma.
Contraindications
Standard considerations.
Dosage and Administration
Cushing SyndromeAdults
PO 250 mg every 6 h. Titrate to adrenal response in increments of 250 mg/day every 1 to 2 wk. Max daily dose is 2,000 mg.
Dosage AdjustmentAdults
PO Dosage reduction may be required for a Ccr less than 10 mL/min; specific guidelines are not established.
Discontinue therapy if patient develops severe rash or rash that lasts more than 5 to 8 days. Therapy may be continued at a lower dose after resolution of mild to moderate skin rashes.
Storage/Stability
Store at room temperature. Protect from light.
Drug Interactions
CNS depressantsConcurrent use with CNS depressants (eg, narcotics, analgesics, alcohol, antiemetics, benzodiazepines, sedatives, tranquilizers) may potentiate CNS effects.
Dexamethasone, digitoxin, medroxyprogesterone, tamoxifen, theophylline, warfarinAminoglutethimide increases oxidative metabolism of these drugs. Higher doses of these agents may be required to achieve therapeutic response during concomitant therapy.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Orthostatic or persistent hypotension; tachycardia.
CNS
Headache; dizziness; drowsiness; lethargy.
Dermatologic
Morbilliform rash; pruritus.
Endocrine
Adrenocortical insufficiency; hypothyroidism; masculinization and hirsutism in females.
GI
Low potential for nausea and vomiting; elevated LFTs; cholestatic jaundice.
Genitourinary
Aminoglutethimide crosses the placenta and has caused pseudohermaphroditism in female infants whose mothers took this agent and anticonvulsants during pregnancy.
Musculoskeletal
Myalgia.
Precautions
MonitorAdrenal functionMonitor plasma cortisol to assess response to therapy for suppression of adrenal function. Thyroid functionThyroid function may decrease during therapy. Monitor at baseline and throughout therapy. Some patients may require thyroid supplements. |
Pregnancy
Category D .
Lactation
Undetermined.
Children
Safety and efficacy not established.
Cortical hypofunction
May cause adrenal cortical hypofunction, especially under conditions of stress.
Hypotension
Aminoglutethimide may suppress aldosterone production by the adrenal cortex and may cause orthostatic or persistent hypotension. Monitor BP.
Overdosage
Symptoms
Ataxia, somnolence, lethargy, dizziness, fatigue, coma, hyperventilation, respiratory depression, nausea and vomiting, loss of sodium and water, hyponatremia, hypochloremia, hyperkalemia, hypoglycemia, hypovolemic shock caused by dehydration, hypotension.
Patient Information
- May produce drowsiness or dizziness; use caution while driving or performing other tasks requiring alertness, coordination, or physical dexterity.
- May cause rash, fainting, weakness, or headache; notify health care provider if pronounced.
- Nausea and loss of appetite may occur during the first 2 wk of therapy; notify health care provider if these persist or become pronounced.
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More Aminoglutethimide resources:
Aminoglutethimide - Includes detailed dosage instructions.
Aminoglutethimide Drug Interactions
Prostate Cancer, Breast Cancer, Cushing's Syndrome
