Īlso, since this drug is a synthetic steroid, elevated blood pressure can occur and remains an area that merits further investigation, along with its effects on adrenal activity. Other than these, gynecologic side effects such as intermenstrual bleeding, breast atrophy, flushes, and androgenic side effects such as hirsutism, decreased breast size, acne, hair loss, oily skin, oily hair, menstrual irregularities and hoarseness, side effects due to weak mineralocorticoid activity such as swelling and edema have also been reported. Īs a synthetic steroid, danazol has many adverse effects in line with other androgens, making its adverse effects broad and systemic in nature. The most commonly reported side effects of danazol include weight gain, gastrointestinal symptoms including bloating, nausea, vomiting, gastroenteritis, elevated liver function tests, joint pain, muscle spasm, lethargy, headache, and depression.
MERK MANUALS FIBROCYSTIC BREAST CHANGES FREE
This effectively increases the free to plasma bound concentrations of sex hormones and steroids, which increases their effect.Īpart from the androgenic mode of action, danazol has also been shown to induce apoptosis and cytotoxicity and affect the expression of apoptosis regulating proteins in leukemic cells, where it has shown results in inducing apoptosis in chronic lymphocytic leukemia. Danazol is also known for its affinity to bind with sex hormone-binding globulin and corticosteroid-binding globulin. This phenomenon in the ovary suggests that danazol directly inhibits steroidogenesis in the ovary, independent of its inhibition of gonadotropin secretion. In the porcine ovary, danazol has been shown to inhibit the aromatization of the basal and luteinizing hormone-mediated progesterone secretion by the granulosa cells and luteal cells of the ovary.
There is evidence that danazol inhibits steroidogenesis in the adrenal glands, ovaries, and the testis In Vitro. Therefore, some of the biological effects of danazol are related to and in line with other androgens. It is a synthetic steroid and possesses some structural similarities with testosterone. The half-life of danazol has been reported to be at a mean of 9.7 hours, while in patients with endometriosis, six months treatment with 200 mg tablets of danazol three times daily reported the half-life of danazol to be 23.7 hours.ĭanazol has multiple mechanisms of action by which it exerts its effect. It has both urinary and fecal excretion, with urinary excretion accounting for the primary mode of excretion of the primary metabolites, while almost ten different products have been identified in feces. Danazol appears to be metabolized into two primary metabolites these are 2-hydroxymethyl danazol and ethisterone. It is mainly excreted in the urine, and a small amount is excreted in the feces. Metabolism and Excretion: Danazol is extensively metabolized in the liver to 2-hydroxymethyl ethisterone. Peak plasma concentration of danazol is reached within 2 to 8 hours post oral administration of 400 mg tablet, with a median Tmax value of 4 hours. Steady-state concentrations require twice-daily dosing of danazol for six days.ĭistribution: Danazol is lipophilic and hence has the potential to penetrate deep tissue compartments. Absorption: Danazol, like other steroids, is well absorbed from the gastrointestinal system.
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