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Zoladex
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GOSERELIN (Zoladex® 3.6 mg Implant, Zoladex® 3-month Implant) is a man-made protein that is like a hormone in the body called gonadotropin-releasing hormone (GnRH). Regular injections of goserelin decrease the levels of testosterone in men and estrogen in women. Goserelin can be used for the relief of endometriosis, or for the treatment of prostate cancer and breast cancer. Women receive the Zoladex® 3.6 mg implant only, and injections are given every 4 weeks. Men may receive the Zoladex® 3.6 mg implant every 4 weeks, or may receive a Zoladex® 3-month implant instead. Generic goserelin implants are not yet available.
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Zoladex (D-Ser(But)6 Azgly10 LHRH) is a synthetic analogue of naturally occurring LHRH. On chronic administration Zoladex results in inhibition of pituitary LH secretion leading to a fall in serum testosterone concentrations in males and serum estradiol concentrations in females. This effect is reversible on discontinuation of therapy. Initially, Zoladex, like other LHRH agonists, may transiently increase serum testosterone concentration in men and serum estradiol concentration in women.
When evaluated again at 36 months the Zoladex alone group had a change from baseline TBBM of 101.5%. This indicated that the patients on Zoladex alone had remineralized their bones after a one year cessation of the drug.
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Zoladex, a sustained-release luteinizing hormone--releasing hormone (LHRH) analogue administered by subcutaneous injection every 28 days, was evaluated at three dose levels in 46 men with untreated advanced prostate cancer. All three Zoladex doses yielded similar endocrinologic effects. After initial transient increases in serum luteinizing hormone, follicle-stimulating hormone, and testosterone concentrations, serum testosterone was suppressed uniformly to castration levels within 22 days. At a median follow-up of 41 weeks, Zoladex had maintained persistent suppression of serum testosterone. Measurements of serum Zoladex levels indicated that release of the drug from the injected depot was sustained over a period of 1 month and that there was no drug accumulation as evaluated over an initial 3-month period. No antibodies to Zoladex were detected.
Abstract: A new longer-acting depot formulation containing 10.8 mg Zoladex was administered subcutaneously without anesthetic to 35 patients with advanced carcinoma of the prostate. Pharmacodynamic and pharmacokinetic data show that following a transient elevation in serum LH and testosterone, the levels of both hormones decrease. Serum testosterone reaches the castrate range in all patients by week 4 and remains at this level for at least 12 weeks. The serum Zoladex profile shows that castrate serum testosterone values can be sustained by very low serum concentrations of the drug of around 0.05 ng/ml. In this preliminary report, the efficacy and safety of this new longer-acting 3-month depot formulation of 10.8 mg Zoladex has been shown to be comparable to the 1-month depot formulation of 3.6 mg Zoladex, in patients with advanced carcinoma of the prostate.
Do not take Zoladex if you are pregnant or could become pregnant during treatment. Zoladex is known to be harmful to an unborn baby. A nonhormonal method of birth control must be used during treatment with Zoladex to ensure prevention of pregnancy. Although Zoladex may stop ovulation and menstruation, a nonhormonal method of birth control must ... be used. If a dose of Zoladex is missed or delayed, ovulation and/or breakthrough bleeding may occur. A nonhormonal method of birth control must also be used until the return of menstruation or for at least 12 weeks following treatment with Zoladex.
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