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Topic: Antiandrogen

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	Antiandrogen - Wikipedia, the free encyclopedia
		An antiandrogen, or androgen antagonist, is any of a group of hormone antagonist compounds that are capable of preventing or inhibiting the biologic effects of androgens, male sex hormones, on normally responsive tissues in the body (see androgen insensitivity syndrome).
		Antiandrogens are often indicated to treat severe male sexual disorders, such as hypersexuality (excessive sexual desire) and sexual deviation, specifically paraphilias, as well as use as a antineoplastic agent and palliative, adjuvant or neoadjuvant hormonal therapy in prostate cancer.
		Antiandrogens can also be used for treatment of benign prostatic hyperplasia (prostate enlargement), acne, androgenetic alopecia (male pattern baldness), and hirsutism (excessive hairiness).
	en.wikipedia.org /wiki/Antiandrogen (454 words)

	[No title] (Site not responding. Last check: 2007-11-06)
		Antiandrogens are a class of drugs that specifically block the entry of testosterone into cells of the body, thus preventing its biological effects.
		Cyproterone (Androcur) is another antiandrogen that is not available in the U.S. In approximately 50% of patients whose cancer has started to grow again despite treatment that includes an antiandrogen, the cancer has been noted to regress by simply stopping the antiandrogen.
		While clonal differences among prostate cancer cells may be partially responsible for the timelimited response to antiandrogens observed in some prostate cancers, it has been shown that during or as a consequence of progression to an androgen independent state upward of 20% to 30% of tumors develop mutations in the androgen receptor.
	www.prostatepointers.org /library/aawr.txt (1343 words)

	[No title] (Site not responding. Last check: 2007-11-06)
		Antiandrogens are a class of drugs that specifically block the entry of androgenic hormones into cells of the body, thus preventing its biological effects.
		It is thought that antiandrogens competitively inhibit the action of androgenic hormones, such as DHT, by binding to cytosol androgen receptors, and preventing DHT from binding to the receptors and entering the cell nucleus.
		In an embodiment of the invention, the antiandrogen comprises an
	www.wipo.int /cgi-pct/guest/getbykey5?KEY=03/05889.030123&ELEMENT_SET=DECL (9083 words)

	Prostate Cancer Resources and Information \| OncoLink
		An antiandrogen is a drug that blocks the action of male hormones.
		Antiandrogens are used in prostate cancer as part of combined androgen blockade (CAB) therapy.
		Since antiandrogens are used in combination with LHRH analogs or just after an orchiectomy, it may be difficult to determine which component of the treatment is responsible for side effects.
	www.oncolink.upenn.edu /types/article.cfm?c=16&s=57&ss=449&id=5988 (1563 words)

	Antiandrogen withdrawal in treatment of hormone-refractory PCa, from the Prostate Cancer InfoLink site (preserved at ... (Site not responding. Last check: 2007-11-06)
		The antiandrogen withdrawal effect was first noted in patients who had received the nonsteroidal antiandrogen flutamide (Eulexin) as part of their combined hormonal therapy.
		However, it may be that this effect is exclusive to the nonsteroidal antiandrogens and will not be seen on withdrawal of any of the steroidal antiandrogens such as cyproterone acetate (Andocur).
		The possibility exists that the nonsteroidal antiandrogens -- while blocking the effects of dihydrotestosterone-receptor complexes on the synthesis of new protein in prostate cancer cells -- may also have a stimulatory effect on mutated androgen receptors in prostate cancer cells.
	www.phoenix5.org /Infolink/refractory/antiandrogenwithdrawal.html (729 words)

	How Do You Treat Prostate Cancer That Has Progressed On Primary Androgen Deprivation Therapy? - Prostate Cancer ...
		Interestingly, the time until PSA begins to decline after antiandrogen withdrawal appears to be shorter with flutamide than with bicalutamide, perhaps reflecting the longer half-life of elimination from the body with bicalutamide (1 week) vs flutamide (5.2 hours).
		In 51 patients, antiandrogen withdrawal was undertaken, and in 14 (31%) patients an AAWR occurred 8 weeks after stopping flutamide.
		Antiandrogen withdrawal is the first step to identify patients who may have had disease progression due to an androgen receptor gene mutation.
	www.prostate-cancer.org /education/andind/treatpc2.html (5977 words)

	REVIEW ARTICLE (Site not responding. Last check: 2007-11-06)
		Antiandrogen withdrawal is efficacious in approximately 20% of patients and can be observed with a variety of antiandrogens, including flutamide, bicalutamide, and megestrol acetate.
		The use of a second antiandrogen is predicated on the possibility that despite their functional similarities, different antiandrogens interact differently with the androgen receptor.
		For these receptors, an antiandrogen may act as a partial agonist, and antiandrogen withdrawal would be predicted to result in an improvement in PSA and possibly a reduction in tumor burden.
	www.prostatepointers.org /prostate/esmall/es2.html (4241 words)

	Environmental Health Perspectives: Perinatal exposure to low levels of the environmental antiandrogen vinclozolin ...
		In this study we examined the effects of exposure to the antiandrogenic fungicide vindozolin (Vz) on the development of two sex-differentiated behaviors that are organized by the perinatal actions of androgens.
		Investigations of the functional effects of low-level environmental antiandrogen exposure are needed to complement the high-dose studies and place organ deficits into the larger context of male reproductive health.
		Antiandrogens could therefore affect the reproductive success of a wide range of animal species by altering male copulatory behavior.
	www.findarticles.com /p/articles/mi_m0CYP/is_6_113/ai_n14816421 (1247 words)

	PCAW - Prostate Cancer Awareness Week - Tolerability of Nonsteroidal Antiandrogens in the Treatment of Advanced ...
		One of the first antiandrogens to be used in clinical practice as a component of CAB was the steroidal antiandrogen cyproterone acetate.
		The non-pharmacologic adverse events of the non-steroidal antiandrogens are generally specific to the individual compounds and, unlike the pharmacologic adverse events, their incidences are not influenced by castration per se.
		In one study of antiandrogen plus medical or surgical castration in patients with advanced prostate cancer, 20 of the patients were originally randomized to nilutamide, but the occurrence of visual side effects in 70% led to an early change to flutamide and the use of flutamide as the antiandrogen in all subsequent patients
	www.pcaw.com /info_articles/articles/archives/tolerability.asp (5880 words)

	Journal of Drugs in Dermatology: Antiandrogen oligonucleotides: active principles in hair- and skin-derived culture ...
		These could be a new class of antiandrogen oligonucleotides pharmacologically active in hair and skin derived cells, suitable for the treatment of dermatological disorders.
		There is, therefore, a need for a new generation of antiandrogens for better therapeutic results.
		In this article we describe potent antiandrogen antisense oligonucleotides as proper active principles for the inhibition of the androgen receptor expression in skin- and hair-derived cells and thereby suitable for treatment of dermatological disorders.
	www.findarticles.com /p/articles/mi_m0PDG/is_3_3/ai_n6056504 (1295 words)

	Prostate Cancer (Chemotherapy) Page 2
		Simultaneous antiandrogen withdrawal and treatment with ketoconazole and hydrocortisone in patients with advanced prostate carcinoma.
		The relationship between antiandrogen withdrawal and a change in PSA may be a general phenomenon, not unique to flutamide.
		BACKGROUND: Although antiandrogen withdrawal has moderate efficacy in patients with hormone refractory prostate carcinoma (HRPC), the effect of the simultaneous suppression of adrenal androgens with ketoconazole at the time of antiandrogen withdrawal is not known.
	www.lef.org /protocols/abstracts/abstr-136a.html (6800 words)

	Postgraduate Medicine: Hirsutism in Women
		In women of reproductive age, birth control is imperative because antiandrogen therapy is teratogenic to fetuses and has the potential to feminize male fetuses.
		Antiandrogen agents include drugs that block androgen cytochrome P-450 receptors, resulting in decreased testosterone, dihydrotestosterone, and DHEAS levels, and drugs that inhibit 5-alpha-reductase, which hinders conversion of testosterone to dihydrotestosterone and results in increased testosterone and estradiol levels.
		However, antiandrogen comparative studies have not been reported, and use of ketoconazole is considered an alternative antiandrogen therapy.
	www.postgradmed.com /issues/2000/06_00/bergfeld.htm (2863 words)

	British Journal of Pharmacology - Interactions of androgens, green tea catechins and the antiandrogen flutamide with ... (Site not responding. Last check: 2007-11-06)
		Flutamide is a nonsteroidal antiandrogen, known to antagonise testosterone binding to the androgen receptor (Benten et al., 1999; McDonald et al., 2000; Poujol et al., 2000).
		A standard antiandrogen response was obtained by observing the decrease in a half-maximal response to DHT with flutamide.
		Screening for androgenic and antiandrogenic effects of green tea catechins shows that in comparison with a standard androgen, dihydrotestosterone (DHT) and a standard antiandrogen, flutamide, the green tea catechins are virtually inactive (Figure 4).
	www.nature.com /bjp/journal/v140/n3/full/0705460a.html (7726 words)

	Comparison of flutamide and spironolactone in the treatment of hirsutism: a randomized controlled trial
		Conclusion: The present data obtained in a randomized prospective study clearly demonstrate that the pure antiandrogen flutamide is superior to spironolactone in the treatment of female hirsutism and its related androgen-dependent symptoms and signs in women.
		The first group (28 patients) received the antiandrogen flutamide at a dose of 250 mg twice daily; the second group (27 patients) received spironolactone at a dose of 50 mg twice daily from days 5 to 25 of their cycle in women having cycles.
		Flutamide is a pure antiandrogen with no intrinsic androgenic activity demonstrable in any of the in vitro (6) and in vivo tests used (4-6, 8, 12).
	www.fernand.labrie.crchul.ulaval.ca /flabrie/pub/241.htm (3154 words)

	Androgenetic Alopecia - Biopsy-proven cases respond to oral antiandrogen; regrowth possible - DermatologyTimes
		After a minimum of 12 months of treatment, the vast majority of women, approximately 90 percent, were determined to have some benefit from oral antiandrogen use based on blinded rater assessments of standardized photographs.
		In addition, we believe this is the first study to objectively demonstrate oral antiandrogen treatment can improve hair density in women with androgenetic alopecia rather than merely halt further loss.
		Sinclair noted his research is based on the assumptions that androgenetic alopecia and chronic telogen effluvium are distinct diseases and that the former can be differentiated from the latter by biopsy.
	www.dermatologytimes.com /dermatologytimes/article/articleDetail.jsp?id=45681 (789 words)

	[No title] (Site not responding. Last check: 2007-11-06)
		Bicalutamide is a newer nonsteroidal antiandrogen originally thought to have a pure antiandrogen activity without agonist activity.
		Although antiandrogen hormone therapy has been widely used for the treatment for prostate cancer, some antiandrogens may act as AR agonists which may result in"antiandrogen withdrawal syndrome."Miyamoto et al., Proc.
		"Antiandrogen withdrawal syndrome"as used herein refers to a phenomenon characterized by either no change or an increase in serum prostate-specific antigen (PSA) concentration upon administration of antiandrogen therapy, and a subsequent decreased PSA concentration observed after withdrawal of antiandrogen therapy.
	www.wipo.int /cgi-pct/guest/getbykey5?KEY=03/88927.031030&ELEMENT_SET=DECL (5695 words)

	Effect of Androgen Deficiency on the Human Meibomian Gland and Ocular Surface -- Krenzer et al. 85 (12): 4874 -- ...
		Effect of antiandrogen therapy on the degrees of corneal fluorescein and rose bengal staining.
		Secretions (n = 2 samples/individual) were obtained from the left and right eyes of patients (n = 5) taking antiandrogen therapy and their age-related controls (n = 6) and analyzed (n = 10–12 samples/group) on the same column for the content of cholesterol, cholesterol esters, wax esters, diglycerides, triglycerides, and squalene.
		Influence of antiandrogen treatment on the m/z ratios of fatty acids in the diglyceride fraction of meibomian gland secretions.
	jcem.endojournals.org /cgi/content/full/85/12/4874 (4746 words)

	Clinical Trial: Antiandrogen Withdrawal in Treating Patients With Hormone-Refractory Prostate Cancer
		PURPOSE: Randomized phase III trial to study the effectiveness of ketoconazole and hydrocortisone for antiandrogen withdrawal in treating men with prostate cancer that is refractory to hormone therapy.
		Compare the response rate and duration of response to antiandrogen withdrawal alone vs. antiandrogen withdrawal plus ketoconazole/hydrocortisone in patients with advanced hormone-refractory prostate cancer.
		Antiandrogen withdrawal alone or in combination with ketoconazole in androgen-independent prostate cancer patients: a phase III trial (CALGB 9583).
	www.clinicaltrials.gov /ct/show/NCT00002760 (565 words)

	Indications for Antiandrogen Use : BC Cancer Agency
		Maximal androgen blockade utilizing continuous antiandrogen therapy with medical or surgical castration does not significantly prolong survival and is therefore no longer indicated [Crawford et al with SWOG, ASCO proceedings, 1997].
		Monotherapy with nonsteroidal antiandrogens is not indicated or approved.
		During neoadjuvant therapy prior to radical radiation therapy, an antiandrogen will be added if there is a PSA rise, or if an inadequate PSA response is observed (defined as failure to achieve a PSA of <1 ng/ml after 4 months of adequate therapy as defined by castrate testosterone levels).
	www.bccancer.bc.ca /HPI/CancerManagementGuidelines/Genitourinary/Prostate/Management/SystemicManagementofProstateCancer/IndicationsforAntiandrogenUse.htm (349 words)

	PCAW - Prostate Cancer Awareness Week - Long-Term Follow-Up of Four Patients with Advanced Prostate Cancer Treated With ...
		This withdrawal response is seen in up to 20% of cases.5 Antiandrogens stimulate, rather than block, the development of mutant nuclear receptors in prostate cancer cells during hormonal treatment, effecting the withdrawal response.
		Due to different mechanisms of action, one antiandrogen may be effective in the treatment of patients in whom another antiandrogen or antiandrogen withdrawal has failed.
		Mild antiandrogenic effects and nausea, reversible interstitial pneumonitis in one patient and supraclavicular lymph node enlargement in another patient were the only side effects.
	www.pcaw.com /info_articles/articles/follow-up.asp (1518 words)

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