Danazole

It has been demonstrated that Danazol [17230-88-5] C22H2yN02, is highly effective in post-coital regimens, and has a very low incidence of side effects. Danazol is marketed in many countries for the treatment of endometriosis and its availabiUty is unrestricted. It does not appear that there is a significant difference in effectiveness when doses of 800 to 1200 mg have been utilized daily for three days (64,65). When utilized in the post-coital mode, the precise mechanism of action of Danazol is not weU-understood. 

C3H9O2 109-94-4) see Danazol Drostanolone Fluorouracil Formeboloue, Metapramine Oxymetholone Perhexiline Stanozolol Tetroxoprim Trilostane Trimethoprim ethyl formylacetate... 

Prophylactic treatment of Cl INH deficiency consists of Cl INH replacement infusions, androgens (danazol, stanozolol, oxymethalone) or antifibrinolytic agents. Acute treatment employs Cl INH replacement (where available), fresh-frozen plasma, and placement of an airway when significant airway obstruction is evident. Abdominal attacks require IV fluid, analgesics, and watchful waiting . 

Cohen S, Koethe S, Kozin F, Rodey G, Arkins J, Fink J Acquired angioedema associated with rectal carcinoma and its response to danazol therapy. Acquired angioedema treated with danazol. J Allergy Clin Immunol 1978 62 217-221. 

Abciximab, aminophylline, amiodarone, amrinone, aspirin, carbamazepine, chlorpromazine, danazol, diltiazem, eptifi-batide, heparin, histamine2-receptor antagonists, low molecular weight heparins, methyldopa, milrinone, procainamide, quinidine, quinine, NSAIDs, thiazide diuretics, ticlopidine, tirofiban, and valproic acid... 

Chloral hydrate Chloramphenicol Cimetidine Ciprofloxacin Clofibrate Danazol Disulfiram Doxycycline Erythromycin Fenofibrate Fluconazole Fluorouracil Fluoxetine Fluvoxamine Gemfibrozil Influenza vaccine Isoniazid Itraconazole Fovastatin Metronidazole Miconazole Moxalactam Neomycin Norfloxacin Ofloxacin Omeprazole Phenylbutazone Piroxicam Propafenone Propoyxphene Quinidine Sertraline Sulfamethoxazole Sulfinpyrazone Tamoxifen Testosterone Vitamin E Zafirlukast... 

Cyclosporine alone fewer remissions than combination with ATG Androgens (such as Danazol—see dosing in ITP section)—can take 3 or more months to show effect... 

A 47-year-old premenopausal female with endometriosis is treated with danazol. Which of the following adverse effects is associated with danazol ... 

Fernandez L, Chirino R, Boada LD, Navarro D, Cabrera N, Del Rfo I, Dfaz-Chico BN (1994) Stanozolol and danazol, unlike natural androgens, interact with the low affinity glucocorticoid binding sites from male rat liver microsomes. Endocrinology 134 1401... 

Luzardo OP, Machln RP, Dlaz-Chico BN, Fernandez L (2000) Photoaffinity labeling identification of a specific binding protein for the anabolic steroids stanozolol and danazol an oligomeric protein regulated by age, pituitary hormones, and ethinyl estradiol. Endocrinology 141 3377... 

Danazol Good Weight gain, Os mild hyperandrogenism Long term Not expensive... 

Like the medical treatment of uterine leiomyomas, danazol, gestrinone, mifepristone, and GnRH-a, with or without add-back therapy, have been proposed for the treatment of endometriosis as well (Olive et al. 2001 Stones et al. 2004), but unlike leiomyomas, oral contraceptive pills, in cyclic or continuous administration, and medroxyprogesterone acetate also seem to be effective (Olive et al. 2001 Stones et al. 2004). A significant benefit in terms of pelvic pain relief also is obtained with the use of nonsteroidal anti-inflammatory drugs (Olive et al. 2001 Stones et al. 2004). 

Recently, a Japanese research group published preclinical safety and efficacy data of an oral antiestrogen (TZE-5323) (Saito et al. 2003). This drug has been shown to have a strong affinity for human ERa and ER/i and a dose-dependent capacity to inhibit estradiol-stimulated transcriptional activation (Saito et al. 2003). In the experimental endometriosis model in rats, TZE-5323 dose-dependently reduced the volume of the endometrial implant with an effectiveness similar to that of danazol and leuprorelin acetate without causing significant changes in bone mineral density and in serum estradiol levels (Saito et al. 2003). 

De Leo V, La Marca A, Morgante G (1999) Short-term treatment of uterine fibromyomas with danazol. Gynecol Obstet Invest 47 258-262... 

Figure 5 Bioavailability of danazol in the fasted and fed state. Open circles represent fasted state administration and closed circles fed state administration. Source From Ref. 16.

Charman W, Rogge M, Boddy A, Barr W, Berger B. Absorption of danazol after administration to different sites of the gastrointestinal tract and the relationship to single- and double-peak phenomena in the plasma profiles. J Clin Pharmacol 1994 33 1207-1212. 

The synthesis of Lp(a) can be influenced by hormones, as is reported by Albers et al. (A7), who observed a reduction of Lp(a) concentrations in nor-molipidemic postmenopausal women treated during 6 weeks with the anabolic steroid stanazolol. The same effect was reported for norethisterone (FI) and danazol (Cl2). Exogenous estrogens, as used in treatment of postmenopausal complaints and in oral contraceptives, induce a decrease of Lp(a) (D9, H27, K13, KAO, L21, S37). This effect is dose-related and dependent on Lp(a) levels before treatment (F2). Watanabe (W9) investigated the influence of progestogen (alone) and detected a decrease of Lp(a) during treatment. 

Lomstein Pedersen B, Mullertz A, Brondstedt H, Gjelstrup Kristensen H (2000) A comparison of the solubility of danazol in human and simulated gastrointestinal fluids. Pharm. Res. 17 891-894. 

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