Aminoglutethimide
Aminoglutethimide is an oral steroidogenesis inhibitor that blocks the synthesis of cortisol and other steroid hormones by inhibiting cytochrome P450 enzymes. It is primarily used in the management of Cushing's syndrome, adrenal carcinoma, and metastatic breast cancer.
Aminoglutethimide is a steroid synthesis inhibitor used to treat conditions involving excess hormone production and certain cancers.
Key facts at a glance
- ATC
- L02BG01
- RxNorm
- 677
- Generic
- Aminoglutethimide
- Class
- atc-l02
- Brands
- —
- Availability
- rx
- Lactation
- unknown
- Routes
- oral
- Forms
- tablet
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 500mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 250mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 400mg daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
10 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks
regular fetal monitoring and ultrasound
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
third trimesteravoid if possible
avoid use during pregnancy due to risk of fetal harm and potential preterm labor
regular fetal monitoring and uterine activity
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
breastfeedingdiscontinue breastfeeding
do not breastfeed during treatment with aminoglutethimide
not applicable
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
elderlystart at lower end of dosing range
use with caution in elderly patients, monitor renal and hepatic function
regular monitoring of renal function, hepatic function, and adrenal function
Use with caution and monitor for adverse effects.
pediatric_age
childrenuse with extreme caution
limited safety and efficacy data in pediatric patients; use only if benefits outweigh risks
close monitoring of growth, development, and adrenal function
Use with caution and monitor for adverse effects.
renal_impairment
mildno initial adjustment needed
monitor renal function regularly, adjust dose based on response
regular renal function monitoring
Use with caution and monitor for adverse effects.
renal_impairment
moderate to severereduce dose
reduce dose in patients with moderate to severe renal impairment, monitor closely
frequent renal function monitoring and drug level monitoring if available
Use with caution and monitor for adverse effects.
hepatic_impairment
mildno initial adjustment needed
use with caution, monitor liver function tests
regular hepatic function monitoring
Use with caution and monitor for adverse effects.
hepatic_impairment
moderate to severereduce dose
reduce dose in patients with moderate to severe hepatic impairment, use with extreme caution
frequent hepatic function monitoring and clinical assessment
Use with caution and monitor for adverse effects.
Statistics and clinical data
Drug class
Drug class classification for Aminoglutethimide
Primary mechanism
Primary pharmacological mechanism of action
Therapeutic uses
Approved and off-label therapeutic applications
Clinical availability
Current prescribing status
Treatment of Cushing's syndrome (hypercortisolism), adrenal carcinoma, and metastatic breast cancer. Historically used as second-line therapy when other treatments are inadequate or not tolerated.
Inhibits cytochrome P450 enzymes involved in steroid hormone biosynthesis, particularly blocking the conversion of cholesterol to pregnenolone (the rate-limiting step) and inhibiting C11β-hydroxylase, thereby reducing production of cortisol, aldosterone, and adrenal androgens.
Requires corticosteroid replacement therapy in most patients. May cause adrenal insufficiency, drowsiness, dizziness, and skin rash. Has been largely superseded by ketoconazole and metyrapone for Cushing's syndrome due to its side effect profile. Drug interactions with tamoxifen and certain sedatives should be monitored.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed August 24, 2026. · Read our editorial policy