Danazol

DANOCRINE

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What it isWeak androgen suppressing gonadotropin release; endometriosis and hereditary angioedema.

Why this oneIn hereditary angioedema it increases C1-inhibitor production rather than blocking bradykinin during an attack.

What limits itVirilization can be irreversible; monitor for liver injury and thrombosis, and avoid pregnancy.

FDA-approved for

endometriosis
hereditary angioedema, fibrocystic breast disease

Off-label

telomere disease and aplastic anemia
immune thrombocytopenia

FDA label

Read the full label on DailyMed ↗

BOXED WARNING Contraindicated in pregnancy (androgenic effects on the female fetus). Thromboembolic, thrombotic and thrombophlebitic events including sagittal sinus thrombosis and fatal strokes reported. Peliosis hepatis and hepatic adenoma (may be silent until fatal intra-abdominal hemorrhage) with long-term use. Benign intracranial hypertension (pseudotumor cerebri) reported.

FDA dosing	Population	Start	Target
Endometriosis — moderate/severe or infertility	Adult women	800 mg/day in 2 divided doses	titrate down to lowest dose maintaining amenorrhea
Endometriosis — mild	Adult women	200–400 mg/day divided BID
Hereditary angioedema	Adults	200 mg BID–TID	decrease by ≤50% at 1–3 mo intervals after response

Renal Contraindicated in markedly impaired renal function

Hepatic Contraindicated in markedly impaired hepatic function

Instructions

Endometriosis: begin therapy during menstruation; ensure patient is not pregnant; continue uninterrupted 3–6 months (may extend to 9)
Hereditary angioedema: after favorable response, decrease dose by ≤50% at 1–3 month intervals; if an attack occurs, may increase daily dose by up to 200 mg

Contraindications

Undiagnosed abnormal genital bleeding
Markedly impaired hepatic, renal, or cardiac function
Pregnancy
Breastfeeding
Porphyria
Androgen-dependent tumor
Active thrombosis/thromboembolic disease or history of such events

Cautions

Thromboembolism, including life-threatening/fatal stroke
Hepatic effects: peliosis hepatis, hepatic adenoma, hepatocellular injury/failure
Benign intracranial hypertension (pseudotumor cerebri)
Androgenic effects (voice change may be irreversible)

Adverse reactions

Weight gain, acne, seborrhea
Hirsutism, voice change/hoarseness
Menstrual disturbances, amenorrhea
Flushing, sweating, vaginal dryness
Hepatic dysfunction (elevated enzymes/jaundice)
Nervousness, emotional lability

Pregnancy Contraindicated — in-utero exposure may cause androgenic effects on the female fetus

Lactation Contraindicated (breastfeeding)

⚠ BOXED WARNINGS

Embryo-fetal toxicity
Thromboembolism
Peliosis hepatis

Cost, est. cash$10–$300/month

Generic entry1987

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4

Overdose danger2 / 4

Weight-gain liability0 / 4

Sedation liability0 / 4

QT / Torsades0 / 4

Direct muscarinic antagonism0 / 4

Embryofetal risk4 / 4

Legacy pregnancy categoryX

Defining liabilityErythrocytosis, infertility, hepatic/lipid effects and mood or misuse concerns.

Mechanism of action: Danazol ballicule

Danazol ballicule: receptor binding, kinetics and half-life diagram

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