Danazol is an orally active and ethisterone derivative having weak androgenic, anabolic, and progestational activities. Danazol is metabolized in the liver and has a t½ of 12–18 hours.
Mechanism of action.
- It suppresses the pituitary-ovarian axis by inhibiting pituitary gonadotropin output.
- This inhibits testicular function in males and ovarian functions in females.
- It also suppresses gonadal function directly by inhibiting steroidogenic enzymes in the body.
Clinical uses.
- Management of endometriosis. It causes improvement in 75% of cases by inhibiting ovarian function.
- Patients with hereditary angioedema.
- Menorrhagia by reducing menstrual blood loss.
- Fibrocystic breast disease.
Adverse effects.
- Complete amenorrhoea occurs with higher doses.
- Androgenic side effects include; acne, hirsutism, decreased breast size, deepening of the voice, edema, and weight gain.
- Loss of libido in men, night sweats, and hot flashes in females.
- Muscle cramping.
- GIT upset and elevation of hepatic enzymes.
Contraindication.
· Pregnancy and breastfeeding.
· Undiagnosed abnormal genital bleeding.
· Severe liver/renal/cardiac disease.
· androgen-dependent tumor.
· Active thrombosis or thromboembolic disease.
· Porphyria.
· Hypersensitivity to the drug.
Dosage.
- Dose: 200–600 mg/day; DANAZOL, LADOGAL,
DANOGEN, GONABLOK 50, 100, 200 mg capsule.
