Bicalutamide

Posts Tagged ‘Bicalutamide’

Pharmacotherapy in the Management of Prostate Cancer

Posted by admin on October 28th, 2011 No Comments

Prostate cancer is now the second leading cause of death due to cancer in men. Prostate cancer is usually classified as being early/localized (organ confined), locally advanced, metastatic or hormone-relapsed. The management of prostate cancer depends largely upon the stage and the Gleason grade of the tumour, as well as the patient's general medical condition and treatment preference. Surgical intervention is usually reserved for (early) localized prostate cancer, which is deemed to be confined to the prostate capsule. In the more advanced cases surgery is only used for performing channel transurethral resection of prostateto relieve severe lower urinary tract symptoms. The management of prostate cancer is sometimes controversial, not least as the diagnosis of localized or locally advanced prostate cancer is often difficult to establish precisely. Current modalities for diagnosing prostate cancer include prostate-specific antigen (PSA), digital rectal examination, trans-rectal rectal ultrasound scan and computerized tomography / magnetic resonance imaging. Often tumours thought to be localized Read more [...]

Posted in Urological Oncology

Management of locally advanced prostate cancer

Posted by admin on October 28th, 2011 No Comments

Hormone therapy alone is generally employed for unfit patients with localized prostate cancer, a life expectancy of < 10 years and a Gleason score of > 4, or for large, locally advanced disease in patients with a life expectancy of < 10 years and a PSA level of > 25 ng/ml. Hormone therapy in the treatment of locally advanced prostate cancer BICALUTAMIDE Bicalutamide is a nonsteroidal pure antiandrogen usually given at a dosage of 150 mg once daily as monotherapy for the treatment of early (localized or locally advanced) nonmetastatic prostate cancer. It is also used at a dosage of 50 mg once daily in combination with a luteinizing hormone-releasing hormone analogue or surgical castration for the treatment of advanced prostate cancer. Bicalutamide is slowly absorbed after oral administration, but absorption is unaffected by food. It has a long plasma elimination half-life (1 week) and accumulates about tenfold in plasma during daily administration. Daily administration of bicalutamide increases circulating levels of gon-adotrophins and sex hormones; although testosterone Read more [...]

Posted in Urological Oncology

Benign Prostatic Hyperplasia

Posted by admin on July 11th, 2011 No Comments

Definition Benign prostatic hyperplasia, a nearly ubiquitous condition, is the most common benign neoplasm of American men and occurs as a result of hormone-driven prostate growth. Pathophysiology The prostate gland comprises three types of tissue: epithelial or glandular, stromal or smooth muscle, and capsule. Both stromal tissue and capsule are embedded with О±1-adrenergic receptors. The precise pathophysiologic mechanisms that cause Benign prostatic hyperplasia are not clear. However, both intraprostatic dihydrotestosterone and type II 5 О±-reductase are thought to be involved. Benign prostatic hyperplasia commonly results from both static (gradual enlargement of the prostate) and dynamic (agents or situations that increase О±-adrenergic tone and constrict the gland's smooth muscle) factors. Examples of drugs that can exacerbate symptoms include testosterone, О±-adrenergic agonists (e.g., decongestants), anticholinergics (e.g., antihistamines, phenothiazines, tricyclic antidepressants, anticholinergic antispasmodics, Read more [...]

Posted in Benign Prostatic Hyperplasia

Nilutamide

Posted by admin on June 24th, 2011 No Comments

C12H10F3N3O4 • Nilutamide is a nonsteroidal antiandrogen. Uses • Prostate Cancer Nilutamide is used in combination with orchiectomy in the treatment of metastatic prostate cancer that involves distant lymph nodes, bone, or visceral organs (stage D2). Results of controlled clinical studies in patients with metastatic prostate cancer indicate that nilutamide in combination with orchiectomy slows progression of the disease, relieve bone pain associated with metastatic disease, and improve overall survival rate after long-term therapy (8.5 years). Prostate specific antigen (PSA) concentrations should be determined periodically during nilutamide therapy to monitor therapeutic response, including successful remission or possible progression of cancer. If PSA concentrations increase substantially and consistently during nilutamide therapy, the possibility of clinical progression should be evaluated. Progression noted after gonadal ablation (e.g., orchiectomy) and antiandrogen therapy may represent growth that is not androgen dependent. For patients receiving orchiectomy and nilutamide who Read more [...]

Posted in Drugs

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 [...]

Posted in Drugs

Flutamide

Posted by admin on June 24th, 2011 No Comments

C11H11F3N2O3 • Flutamide, a nonsteroidal antiandrogen, is an antineoplastic agent. Uses • Prostate Cancer Flutamide is used in combination with a gonadotropin-releasing hormone (GnRH) analog (e.g., goserelin, leuprolide acetate) in the treatment of prostate cancer that is clinically localized, such as that confined to the prostate but with extensive involvement of one lobe or with involvement of both lobes (stage B2) and that localized to the periprostatic area but extending beyond the capsule and possibly affecting seminal vesicles (stage C). Flutamide also is used in combination with a GnRH analog in the treatment of metastatic prostate cancer that involves distant lymph nodes, bone, or visceral organs (stage D2). For additional information on combined antiandrogenic and GnRH analog therapy. Prostate specific antigen (PSA) concentrations should be determined periodically during combined flutamide and GnRH analog therapy to monitor therapeutic response, including successful remission or possible progression of cancer. If PSA concentrations increase substantially and consistently Read more [...]

Posted in Drugs

Posted by admin on June 24th, 2011 No Comments

C18H14F4N2O4S • Bicalutamide, a nonsteroidal antiandrogen, is an antineoplastic agent. Uses • Prostate Cancer Bicalutamide is used in combination with a gonadotropin-releasing hormone (GnRH) luteinizing hormone-releasing hormone analog (e.g., goserelin or leuprolide acetate) for the palliative treatment of metastatic (stage D2) prostate cancer. In a double-blind, multicenter, randomized study in 813 patients with previously untreated advanced prostate cancer, similar survival rate, time to progression, and quality-of-life measurements were reported for bicalutamide (50 mg daily) and flutamide (250 mg 3 times daily) combined with a GnRH analog (goserelin acetate implant or leuprolide acetate depot). For additional information on combined antiandrogenic and GnRH analog therapy. Prostate specific antigen (PSA) concentrations should be determined periodically during bicalutamide therapy to monitor therapeutic response, including successful remission or possible progression of cancer. If PSA concentrations increase substantially and consistently during bicalutamide therapy, the possibility Read more [...]

Posted in Drugs

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

Secondary Hormonal Therapy

Posted by admin on June 21st, 2011 No Comments

Metastatic prostate cancer that progresses after initial androgen deprivation is most commonly referred to as hormone-refractory prostate cancer or androgen-independent prostate cancer. Both these labels are misleading, as Fowler and Whitmore et al. and Manni et al. proved in their findings that the disease flares when exogenous testosterone is given. Likewise, it becomes quiescent again on discontinuation of the exogenous androgen. These clinical observations strongly suggest that the disease is not refractory to or independent of growth stimulation by exogenous testosterone. Thus, there is debate about the role of low levels of endogenous adrenal androgens and that of continued suppression of testicular androgen production by means of luteinizing hormone-releasing hormone agonists. In two retrospective analyses, the question was asked whether androgen deprivation should be continued or maintained when the "hormone-refractory" state was reached. The hormone-refractory state was defined clinically as the need for chemotherapy. In a 341 patient cohort studied by the Eastern Cooperative Oncology Read more [...]

Posted in Hormonal Therapy

Second-Line Antiandrogens

Posted by admin on June 21st, 2011 No Comments

The addition of flutamide at the time of progressive metastatic disease is associated with an objective response in 15% and disease stabilization in 20% of patients (Table Secondary Hormonal Manipulation: Addition of Flutamide ). Patients treated on the placebo arm of the National Cancer Institute's Intergroup protocol 0036 comparing leuprolide and flutamide versus leuprolide and placebo, however, showed no survival benefit when flutamide was added at the time of disease progression. TABLE. Secondary Hormonal Manipulation: Addition of Flutamide Inhibits uptake and binding of androgen to the androgen receptor 230 patients, five trials: 15% objective response, 20% stable disease No obvious survival benefit in one phase III trial Toxicities: diarrhea, gynecomastia, abnormal liverfunction tests Recently, Fowler et al. reported an 80% prostate-specific antigen response rate in the same population. The role of flutamide in men progressing after treatment with another antiandrogen or its withdrawal has not been studied but is expected by many authorities to have some Read more [...]

Posted in Hormonal Therapy

Posts Tagged ‘Bicalutamide’

Symptoms and Treatment

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