Estradiol | Health and Prostate

Posts Tagged ‘Estradiol’

Triptorelin Pamoate

Posted by admin on June 24th, 2011 No Comments

C64H82N18O13 • Triptorelin pamoate, a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin), is an antineoplastic agent. Uses • Prostate Cancer Triptorelin pamoate is used for the palliative treatment of advanced prostate cancer. The drug currently is considered alternative therapy when orchiectomy or estrogen therapy is not appropriate or is unacceptable to the patient. In a randomized, active-control trial in men with advanced prostate cancer who received triptorelin pamoate as a 1-month formulation or another GnRH agonist monthly for 9 months, castration levels of serum testosterone were achieved in 91.2% of triptorelin pamoate patients at day 29 and 97.7% of patients at day 57. Maintenance of castration levels of serum testosterone from day 57 through day 253 was found in 96.% of triptorelin-treated patients. In addition, on day 85 of the study, serum LH concentrations were less than 1 IU/L in 98.% of evaluable patients when measured 2 hours after triptorelin pamoate administration on day 85, indicating desensitization Read more [...]

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Leuprolide Acetate

Posted by admin on June 24th, 2011 No Comments

C59H84N16O12•C2H4O2 • Leuprolide acetate, a synthetic nonapeptide analog of naturally occurring porcine or ovine gonadotropin releasing hormone (GnRH, luteinizing hormone releasing hormone, gonadorelin), may be used as an antineoplastic agent and for its endocrine effects. Drug Interactions The manufacturer states there are no reports to date of drug interactions with leuprolide. The manufacturer also states that because leuprolide is a peptide that is mainly degraded by peptidase and not by cytochrome P-450 microsomal enzymes and because of the drug's low degree of protein binding, drug interactions would not be expected to occur with leuprolide. There is some evidence from studies in mice to suggest that the inhibitory effect of leuprolide on spermatogenesis may be used to therapeutic advantage in the prevention of azoospermia or severe oligospermia that frequently results from therapy with cytotoxic agents. In mice receiving combined therapy with leuprolide and cyclophosphamide, testicular damage was less than that observed in animals receiving cyclophosphamide alone. It has been Read more [...]

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Goserelin Acetate

Posted by admin on June 24th, 2011 No Comments

C 59H 84N 18O 14 • Goserelin acetate, a synthetic decapeptide analog of gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, gonadorelin), may be used as an antineoplastic agent and for its endocrine effects. Uses • Prostate Cancer Goserelin acetate is used for the palliative treatment of advanced prostate cancer. Therapy with a GnRH agonist (e.g., goserelin) currently is considered one of several first-line options for hormonal therapy in patients with prostate cancer; other options include orchiectomy, estrogens, and antiandrogens. In controlled clinical studies in patients with advanced prostate cancer, goserelin (3.6 mg administered subcutaneously every 4 weeks) was as effective as orchiectomy as determined by the degree of testosterone suppression, duration of response and survival, and/or objective response rate. Results of several dose-response studies in patients with advanced prostate cancer indicate that pharmacodynamic effects (i.e., reductions in serum testosterone and prostate specific antigen [PSA] concentrations) associated with administration Read more [...]

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Goserelin Acetate: Dosage and Administration

Posted by admin on June 24th, 2011 No Comments

• General Goserelin acetate is administered as a biodegradable implant subcutaneously into the upper abdominal wall, under the supervision of a clinician. Implants containing 3.6 mg of goserelin are administered every 4 weeks. When indicated, implants containing 10. mg of goserelin are administered every 12 weeks. 2 6 Although a delay of a few days is permitted, the manufacturer states that every effort should be made to adhere to the recommended schedule. A local anesthetic may be given prior to implantation of goserelin. In the event that the implant needs to be removed, it may be located by ultrasound. The manufacturer's labeling should be consulted for proper methods of administration and associated precautions. Dosage of goserelin acetate is expressed in terms of goserelin. • Prostate Cancer For the palliative treatment of advanced prostate cancer, the usual dosage of goserelin in men is 3.6 or 10.8 mg implanted subcutaneously every 4 or 12 weeks, respectively. For this indication, goserelin is intended for long-term administration unless it is clinically inappropriate. When Read more [...]

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Estramustine Phosphate Sodium

Posted by admin on June 24th, 2011 No Comments

C23H30ClNNaO6P • Estramustine phosphate sodium, a complex of 17 ?-estradiol and nornitrogen mustard, is an antimicrotubule antineoplastic agent. Uses • Prostate Cancer Estramustine phosphate sodium is used for the palliative treatment of metastatic and/or progressive prostate cancer. The drug, alone or in combination with other antineoplastic agents, currently is considered by many clinicians to be an alternative to conventional measures (e.g., orchiectomy, hormonal therapy) and generally is used in the treatment of hormone-refractory prostate cancer. Safety and efficacy of estramustine have been evaluated in controlled and uncontrolled studies in patients with advanced metastatic prostate cancer refractory to conventional measures (e.g., hormonal therapy) as well as in those with previously untreated disease. Most studies were conducted before the realization that administration of estramustine with milk or calcium-containing products substantially impairs absorption of the drug; therefore, overall clinical efficacy (i.e., objective response) of estramustine may have been underestimated. Read more [...]

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Prostatitis: Advanced Therapy

Posted by admin on June 21st, 2011 No Comments

Prostatitis is one of the most perplexing disease entities with which the practicing urologist must contend. Also, the treatment of this disease is the least gratifying in that the patients often are labeled as "crazy" and have a poor response. In many ways, there are some significant similarities with interstitial cystitis, and perhaps some of the patients with complaints of prostatitis actually have interstitial cystitis, as has been suggested. Indeed, many of the symptoms and physical findings are similar and are outlined in Table 71-1. As in the case of interstitial cystitis, prostatitis has also been difficult to study, being a disease that lacked a formal and specific definition. Therefore, the National Institute for Diabetes, Digestive, and Kidney Diseases (NIDDKD) convened a consensus group to define prostatitis, expressly for the purpose of describing the different prostatitis syndromes in such a way that they could be investigated, and ultimately treated, in a more efficacious fashion. These new definitions, while not being radically different from the old criteria, serve the purpose of Read more [...]

Posted in Prostatitis

Hormonal Mechanisms

Posted by admin on June 21st, 2011 No Comments

Role of Androgens The importance of the testis in benign prostatic hyperplasia has been well known since the 1890s when it was found that castration produced dramatic relief of obstructive benign prostatic hyperplasia in approximately 80% of patients. Scott later noted that benign prostatic hyperplasia development is uncommon if the patient is castrated prior to age 30 years. In murine models, the overall decrease in prostatic size after castration is approximately 80%, with a 93% decrease in the epithelial component and a 22% decrease in the stromal component. The development of benign prostatic hyperplasia also appears to be dependent on the timing of hormonal exposure. A recent study by Jie-Ping and Fang-Liu with follow-up periods of up to 65 years demonstrated that most patients castrated before age 26 years rarely develop a palpable prostate. Interestingly, 85% of these patients with very small prostates had voiding symptoms, including nocturia of two to ten times per night, demonstrating that an enlarged prostate is not necessary for the development of voiding symptoms. Isaacs found that Read more [...]

Posted in Benign Prostatic Hyperplasia

Opportunities for Chemoprevention

Posted by admin on June 21st, 2011 No Comments

Vitamin E The term "vitamin E" is used to refer to a group of naturally occurring substances that have vitamin E activity including a-, β-, δ-, and y-tocopherols (that have saturated side chains) and tocotrienols (that have unsaturated side chains). These agents have some degree of difference in biopotency with the naturally occurring d-a-tocopherol approximately 30% more potent than the synthetic forms — d- or d, l-a-tocopherol alone, acetate, or succinate. The principal food sources of vitamin E are vegetable and seed oils as well as alfalfa and lettuce. A primary function of vitamin E is as an antioxidant, interacting with free radicals (e.g., singlet oxygen, superoxide anion, organic peroxide radicals, hydrogen peroxide, and others) that are generated as a normal part of cellular metabolism. These free radicals can interact with cellular structures, primarily membranes, and lead to cellular damage, generally through lipid peroxidation. Over time, the oxidative stress in humans increases and, similarly, with aging, the endogenous antioxidant capability (from glutathione, vitamins A, C, Read more [...]

Posted in Prostate Cancer

Results of Hormonal Therapy for Localized Prostate Cancer

Posted by admin on June 21st, 2011 No Comments

Since the androgen dependence of prostate cancer was demonstrated by Huggins and Hodges, androgen withdrawal therapy has been used in treating advanced prostate cancer. In 1997, the Medical Research Council Prostate Cancer Working Party Investigators Group reported on the results of a trial randomizing 938 patients with locally advanced (clinical stage T2 to T4) or asymptomatic metastatic prostate cancer. Patients were treated with either immediate hormonal therapy with orchiectomy, a luteinizing hormone-releasing hormone analogue, or with deferred therapy Randomization was performed with stratification for age, clinical stage, and metastatic status. Comparison of the patients with nonmetastatic disease (256 patients randomized to immediate therapy and 247 randomized to deferred therapy), revealed a greater freedom from distant progression or death due to prostate cancer in patients receiving immediate therapy (96 events in 256 patients) versus deferred therapy (144 events in 244 patients) (p < .001, log rank test). These patients had both an improved crude survival (p = .02, log rank test) and Read more [...]

Posted in Hormonal Therapy

Benign Prostatic Hyperplasia: Etiology

Posted by admin on May 10th, 2011 No Comments

The exact mechanisms that cause benign prostatic hyperplasia are unknown. Extensive research indicates that hormonal changes and increasing age are clear risk factors for benign prostatic hyperplasia development. Cell culture studies have determined that the androgen dihydrotestosterone has an important role in prostatic growth. These studies also suggest other effects of this hormone on benign prostatic hyperplasia etiology, such as disruption of the equilibrium between serum testosterone and estrogen levels and changes in cell proliferation and/or apoptosis rates. The activity of growth factors is also suspected of contributing to prostate hyperplasia; deficiency or overexpression of certain growth factors significantly changes the rate of cell multiplication and cell death. Cellular senescence also affects apoptosis; as a result of this process, prostate cells do not respond to signals that initiate apoptosis. Dihydrotestosterone The presence of androgens evidently influences the development of benign prostatic hyperplasia. Men who are incapable of androgen activity (because of genetic mutations) Read more [...]

Posted in Benign Prostatic Hyperplasia

Posts Tagged ‘Estradiol’

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