Estrogens leuprolide

Bicalutamide may increase the effect of oral anticoagulants. Flutamide enhances the action of leuprolide. Additive antineoplastic effects may occur when leuprolide is administered with megestrol or flutamide. Estrogens decrease the effectiveness of tamoxifen. 

Several randomized trials have demonstrated that leuprolide and goserelin are effective agents when used alone in patients with advanced prostate cancer.19 Response rates around 80% have been reported, with a lower incidence of adverse effects compared with estrogens.19 There are no direct comparative trials of the currently available LHRH agonists or the dosage formulations, but a recent meta-analysis reported that there is no difference in efficacy or toxicity between leuprolide and goserelin. Therefore, the choice between the two usually is made based on cost and patient and physician preference for a dosing schedule. 

The nonapeptide leuprolide is a synthetic analog of the decapeptide, gonadotropin releasing hormone, and it exceeds the activity of the natural hormone and significantly elevates the level of testosterone and dihydrotestosterone in men, and estrogen in women. It also inhibits foUicle-stimulating hormone and leutenizing hormone. 

Leuprolide is used for prostate cancer, when orchiectomy or estrogen therapy is counterproductive to the patient. A synonym of this drug is lupron. 

Buserelin (Suprefact) and leuprolide (Lupron) are peptide analogues of the hypothalamic hormone LH-RH (luteinizing hormone-releasing hormone). Chronic exposure of the pituitary to these agents abolishes gonadotropin release and results in markedly decreased estrogen and testosterone production by the gonads. Their major clinical use is in the palliative hormonal therapy of cancer of the prostate. 

Uterine leiomyomata are benign, estrogen-sensitive, fibrous growths in the uterus that can cause menorrhagia, with associated anemia and pelvic pain. Treatment for 3-6 months with a GnRH agonist reduces fibroid size and, when combined with supplemental iron, improves anemia. Leuprolide, goserelin, and nafarelin are approved for this indication. The doses and routes of administration are similar to those described for treatment of endometriosis. 

Add-back estrogen replacement reduces the frequency and severity of these symptoms without apparently compromising the effectiveness of gonadorelin in women with endometriosis (19,27). In a randomized, multicenter, double-blind comparison of intranasal nafarelin twice daily and depot leuprolide acetate monthly for 6 months in 192 young women with endometriosis, nafarelin caused fewer hypoestrogenic symptoms, although the... 

Gonadotropin-releasing hormone agonists (buserehn, nafarelin, and leuprolide), available as injectable drugs or nasal spray, suppress the production of ovarian androgens and are efficacious in acne. By reducing estrogen, they can produce menopausal symptoms (headache and bone loss). They have not been approved for treatment of acne. ... 

Prostate carcinoma Leuprolide with or without fiutamide additonal drugs include estrogens and ketoconazole... 

Triptorelin pamoate is another superagonist of GnRH, which like nafarelin acetate contains only a single amino acid substitution (D-Trp for Gly ) when compared to the natural hormone (Fig. 7.12). In the treatment of advanced prostate cancer, it is important to reduce serum testosterone levels to very low levels, which can be achieved surgically by orchiectomy. When this surgical method Is unacceptable to the patient, an alternative approach Is chemical castration, which can be achieved by use of estrogen therapy, leuprolide. 

In an uncontrolled study in 13 patients aged 30-42 years with endometriosis or menorrhagia, who took the aromatase inhibitor letrozole 2.5 mg/day for the first 5 days after receiving leuprolide acetate 3.75 mg intramuscularly, the initial increase in estrogen concentrations was not apparent [6. In a randomized study in healthy subjects, mean age 30 years, who received triptorelin 3.75 mg (two injections 4 weeks apart), with or without oral exemestane 25 mg/day for 56 days, there was no effect on the initial flare of FSH, LH, and estrogen, although there was subsequent increased suppression of estrogen [7. Of the 14 women who received placebo with triptorelin, 11 had hot flushes compared with nine of the 15 who took exemestane. 

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