Danazolum

Danazolum Uses, Dosage, Side Effects, Food Interaction and all others data.

As a gonadotropin inhibitor, danazol suppresses the pituitary-ovarian axis possibly by inhibiting the output of pituitary gonadotropins. Danazolum also depresses the preovulatory surge in output of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), thereby reducing ovarian estrogen production. Danazolum may also directly inhibits ovarian steroidogenesis; bind to androgen, progesterone, and glucocorticoid receptors; bind to sex-hormone-binding globulin and corticosteroid-binding globulin; and increases the metabolic clearance rate of progesterone. Another mechanism of action by which danazol may use to facilitate regression of endometriosis is by decreasing IgG, IgM, and IgA concentrations, as well as phospholipid and IgG isotope autoantibodies. In the treatment of endometriosis, as a consequence of suppression of ovarian function, danazol causes both normal and ectopic endometrial tissues to become inactive and atrophic. This leads to anovulation and associated amenorrhea. In fibrocystic breast disease, the exact mechanism of action of danazol is unknown, but may be related to suppressed estrogenic stimulation as a result of decreased ovarian production of estrogen. A direct effect on steroid receptor sites in breast tissue is also possible. This leads to a disappearance of nodularity, relief of pain and tenderness, and possibly changes in the menstrual pattern. In terms of hereditary angioedema, danazol corrects the underlying biochemical deficiency by increasing serum concentrations of the deficient C1 esterase inhibitor, resulting in increased serum concentrations of the C4 component of the complement system.

Danazolum is a derivative of the synthetic steroid ethisterone, a modified testosterone. It was approved by the U.S. Food and Drug Administration (FDA) as the first drug to specifically treat endometriosis, but its role as a treatment for endometriosis has been largely replaced by the gonadotropin-releasing hormone (GnRH) agonists. Danazolum has antigonadotropic and anti-estrogenic activities. Danazolum acts as an anterior pituitary suppressant by inhibiting the pituitary output of gonadotropins. It possesses some androgenic properties.

Trade Name Danazolum
Availability Prescription only
Generic Danazol
Danazol Other Names Danazol, Danazolum
Related Drugs norethindrone, medroxyprogesterone, Provera, leuprolide, Sprintec, Orilissa, stanozolol, Danocrine
Type
Formula C22H27NO2
Weight Average: 337.4553
Monoisotopic: 337.204179113
Groups Approved
Therapeutic Class Drugs affecting (inhibiting) gonadotrophin
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Danazolum
Danazolum

Uses

Danazolum is used for the following treatment-

  • Endometriosis
  • Benign breast disease
  • Menorrhagia
  • Gynecomastia
  • Preoperative thinning of the endometrium before hysteroscopic endometrial ablation.

Danazolum is also used to associated treatment for these conditions: Endometriosis, Fibrocystic Disease of Breast, Hereditary Angioedema, Refractory immune thrombocytopenia

How Danazolum works

As a gonadotropin inhibitor, danazol suppresses the pituitary-ovarian axis possibly by inhibiting the output of pituitary gonadotropins. Danazolum also depresses the preovulatory surge in output of follicle-stimulating hormone (FSH) and luteinizing hormone (LH), thereby reducing ovarian estrogen production. Danazolum may also directly inhibits ovarian steroidogenesis; bind to androgen, progesterone, and glucocorticoid receptors; bind to sex-hormone-binding globulin and corticosteroid-binding globulin; and increases the metabolic clearance rate of progesterone. Another mechanism of action by which danazol may use to facilitate regression of endometriosis is by decreasing IgG, IgM, and IgA concentrations, as well as phospholipid and IgG isotope autoantibodies. In the treatment of endometriosis, as a consequence of suppression of ovarian function, danazol causes both normal and ectopic endometrial tissues to become inactive and atrophic. This leads to anovulation and associated amenorrhea. In fibrocystic breast disease, the exact mechanism of action of danazol is unknown, but may be related to suppressed estrogenic stimulation as a result of decreased ovarian production of estrogen. A direct effect on steroid receptor sites in breast tissue is also possible. This leads to a disappearance of nodularity, relief of pain and tenderness, and possibly changes in the menstrual pattern. In terms of hereditary angioedema, danazol corrects the underlying biochemical deficiency by increasing serum concentrations of the deficient C1 esterase inhibitor, resulting in increased serum concentrations of the C4 component of the complement system. (Source: PharmGKB)

Dosage

Danazolum dosage

Preoperative thinning of the endometrium:

  • Adult: 400-800 mg daily, in up to 4 divided doses for 3-6 week.

Benign breast disorders:

  • Adult: Initially, 100-400 mg daily in 2 divided doses adjusted according to response and continued for 3-6 month.

Hereditary angioedema:

  • Adult: Initially, 200 mg bid-tid reduced thereafter according to patient's response.

Endometriosis:

  • Adult: 200-800 mg daily in 2 divided doses adjusted according to response, for 3-6 month or if necessary, up to 9 month.

Menorrhagia:

  • Adult: 200 mg once daily. Review treatment 3 month later.

Gynaecomastia:

  • Adult: Male adolescents: Initially, 200 mg daily, may increase to 400 mg daily after 2 month if no response occurs; adult men: Initial: 400 mg daily in up to 4 divided doses. Usual treatment duration: 6 month.
  • Child: Male adolescents: Initially, 200 mg daily increased to 400 mg after 2 month if no response occurs. Treatment usually up to 6 months.

Side Effects

Oedema, weight gain, sweating, acne, hirsutism, flushing, oily skin or hair, deepening of the voice, clitoral hypertrophy, amenorrhoea, hepatic dysfunction, CNS or GI disturbances, benign intracranial hypertension, reduction in breast size, visual disturbances, elevated LFT values.

Precaution

Epilepsy, migraine; cardiac, hepatic, renal disorders. Severe hypertension, diabetes, polycythaemia, history of thrombosis; children.

Interaction

Insulin: Patients taking danazol may show increased insulin resistance. The significance of this is not known but such patients should be carefully monitored.

Estrogens and progestogens: Theoretically danazol may interact with exogenous estrogens and/or progestogens. It has been suggested that danazol acts by binding to estrogen, progesterone or androgen receptors at various levels in the hypothalamic pituitary-ovarian axis. Therefore, women of child bearing age should use effective, non hormonal methods of contraception.

Anticonvulsant therapy: Danazolum may affect the plasma concentration of carbamazepin and possibly the patient's response to this agent and to phenytoin. A similar interaction is possible for phenobarbital.

Antihypertensive therapy: Danazolum can oppose the action of antihypertensive agents, possibly through effects on fluid retention.

Cyclosporine: Danazolum can increase the plasma concentration of cyclosporine.

Migraine therapy: Danazolum itself may provoke migraine and it may possibly reduce the effectiveness of medication to prevent the condition.

Food Interaction

  • Take with or without food. The absorption is unaffected by food.

Danazolum Hypertension interaction

[Major] Danazolum possess androgenic activity that can result in salt and water retention.

Danazolum is eliminated by the kidney, and its use is contraindicated in patients with severe renal dysfunction.

It should also be administered cautiously in patients adversely affected by volume overload, such as patients suffering from epilepsy, diabetes mellitus, migraine, cardiac or renal dysfunction, polycythemia and hypertension.

These patients will require careful observation.

Half Life

Approximately 24 hours.

Pregnancy & Breastfeeding use

Category X: Studies in animals or human beings have demonstrated fetal abnormalities or there is evidence of fetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Contraindication

  • Pregnancy and breast-feeding
  • Impaired hepatic, renal, or cardiac function
  • Porphyria
  • Thromboembolic disease
  • Androgen-dependent tumor
  • Abnormal vaginal bleeding that has not been fully investigated.
  • Hypersensitivity to danazol.

Acute Overdose

There have been no incidents of acute overdosage with Danazolum and it is unlikely that any immediate serious reaction will be seen from a single excessive dose. In case of the acute overdosage, the drug should be removed by gastric lavage and the patient should be kept under observation.

Storage Condition

Store at 15-30°C.

Innovators Monograph

You find simplified version here Danazolum

Danazolum contains Danazol see full prescribing information from innovator Danazolum Monograph, Danazolum MSDS, Danazolum FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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