Drug reference

aminoglutethimide

Adrenocortical steroidogenesis inhibitor (historical) · Antineoplastic

START

250 mg PO twice daily (with hydrocortisone replacement in Cushing's)

TYPICAL MAX

~2 g/day (toxicity-limited)

STOP IF

Adrenal crisis, severe rash (SJS), blood dyscrasias, or hepatitis

WATCH

Cortisol / electrolytes, CBC, LFTs, TSH, rash; cover stress with hydrocortisone

CDSCO approvedATC L02BG01

Dose laddermg/d

Renal dose adjustmenteGFR mL/min/1.73m²

KDIGO 2024 + manufacturer label

Pharmacokineticsplasma · t hours

ONSET: 45min · absorption
PEAK: 1.5h · Tmax
t½: 10h · t½ (steady)
DURATION: 12h · BID

EXCRETION

Renal — metabolites

route + CYP

INTERACTIONS

10 major

SEVERE in our sources

PREGNANCY

Contraindicated — virilisation of female fetus.

FDA category + note

Top interactionssee all 12 →

BenzhydrocodoneSevereDatabaseDDInter
ButorphanolSevereDatabaseDDInter
FentanylSevereDatabaseDDInter
HydrocodoneSevereDatabaseDDInter

Mechanism

Inhibits cholesterol side-chain cleavage (CYP11A1) and aromatase (CYP19), suppressing adrenal steroid (cortisol, aldosterone) and peripheral oestrogen synthesis; historical 'medical adrenalectomy' role in Cushing's and metastatic breast cancer.

Indications

Cushing syndrome (medical adrenalectomy — largely superseded by ketoconazole/metyrapone/levoketoconazole)Metastatic hormone-dependent breast cancer (historical; replaced by selective aromatase inhibitors)

Dosing

Adult: Start 250 mg PO twice daily; titrate every 1–2 weeks by 250 mg/day to 1 g/day in divided doses (with hydrocortisone replacement for adrenal blockade).
Pediatric: Not established.
Renal adjustment: Caution; no fixed adjustment.
Hepatic adjustment: Avoid in significant impairment.
Geriatric: Lower doses; AE risk.
Max dose: 2 g/day (rarely; toxicity-limited)

Pharmacokinetics

Onset

Cortisol suppression over days

Peak effect

~1.5 h (Tmax)

Duration

~12 h (divided dosing)

Half-life

~12 h (initially; auto-induction shortens to ~7 h)

Bioavailability

Well absorbed orally

Protein binding

Moderate

Metabolism

Hepatic (acetylation, hydroxylation; auto-induces own metabolism)

Excretion

Renal (metabolites)

Contraindications

Severe hepatic impairment
Hypersensitivity
Pregnancy

Side effects

Common

Drowsiness / lethargy (often severe, dose-limiting)Rash (often early — usually self-limited)Nausea/anorexiaHeadache

Serious

Adrenal insufficiency / Addisonian crisis
Severe blood dyscrasias (pancytopenia)
Hepatotoxicity
Stevens-Johnson syndrome
Hypothyroidism

Pregnancy & lactation

Pregnancy

Contraindicated — virilisation of female fetus.

Lactation

Avoid.

Drug interactions

Benzhydrocodone

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Butorphanol

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Fentanyl

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Hydrocodone

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Lumateperone

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Methadone

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Oliceridine

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Oxycodone

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Progesterone

Severe

Database

Decreased progesterone plasma concentrations, leading to reduced efficacy.

Avoid co-administration. If unavoidable, consider increasing progesterone dose or using an alternative progestin. Monitor for signs of reduced progesterone effect.

Source: DDInter

Ranolazine

Severe

Database

Drug interaction classified as: metabolism

Source: DDInter

Dexamethasone

Moderate

Database

Aminoglutethimide induces dexamethasone metabolism

Use hydrocortisone for replacement instead

Source: Kimi deep-research + Cla