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5a-Reductase Inhibitor

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1. 5a-Reductase Inhibitor

Inhibitor Aka: 5a-Reductase Inhibitor , Finasteride , Proscar , Propecia , Dutasteride , Duagen , Avodart II. Indications BPH-Associated Large size >40 ml (see PSA to estimate size) in males (Finasteride) Adjunct to hair transplantation III. Mechanism Inhibits Testosterone to Dihydrotestosterone conversion Competitive inhibition of enzyme 5a-reductase Finasteride inhibits Type II 5a reductase Dutasteride inhibits both Type I and II 5a reductase Reduces volume of Improves urine blood flow IV (...) 5a-Reductase Inhibitor 5a-Reductase Inhibitor Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 5a-Reductase Inhibitor 5a-Reductase

2018 FP Notebook

2. 5a-Reductase Inhibitor

Inhibitor Aka: 5a-Reductase Inhibitor , Finasteride , Proscar , Propecia , Dutasteride , Duagen , Avodart II. Indications BPH-Associated Large size >40 ml (see PSA to estimate size) in males (Finasteride) Adjunct to hair transplantation III. Mechanism Inhibits Testosterone to Dihydrotestosterone conversion Competitive inhibition of enzyme 5a-reductase Finasteride inhibits Type II 5a reductase Dutasteride inhibits both Type I and II 5a reductase Reduces volume of Improves urine blood flow IV (...) 5a-Reductase Inhibitor 5a-Reductase Inhibitor Toggle navigation Brain Head & Neck Chest Endocrine Abdomen Musculoskeletal Skin Infectious Disease Hematology & Oncology Cohorts Diagnostics Emergency Findings Procedures Prevention & Management Pharmacy Resuscitation Trauma Emergency Procedures Ultrasound Cardiovascular Emergencies Lung Emergencies Infectious Disease Pediatrics Neurologic Emergencies Skin Exposure Miscellaneous Abuse Cancer Administration 4 5a-Reductase Inhibitor 5a-Reductase

2015 FP Notebook

3. Effects of aromatase inhibition and androgen activity on serotonin and behavior in male macaques. Full Text available with Trip Pro

for 5-7 months and then treated for 3 months with (a) placebo; (b) testosterone (T); (c) T + Dutasteride (5a reductase inhibitor; AvodartTM); (d) T + Letrozole (nonsteroidal aromatase inhibitor; FemeraTM); (e) Flutamide + ATD (androgen antagonist plus steroidal aromatase inhibitor); or (f) dihydrotestosterone (DHT) + ATD (n = 5/group). Behavioral observations were made during treatments. At the end of the treatment period, each animal was sedated with propofol and administered a bolus (...) response and Letrozole partially blocked the effect of T. Complete inhibition of aromatase with ATD, a noncompetitive inhibitor, significantly and similarly reduced the fenfluramine-induced serotonin/prolactin response in the presence or absence of DHT. Neither aggressive behavior nor yawning (indicators of androgen activity) correlated with serotonin/prolactin, but posited aromatase activity correlated significantly with prolactin (p < .0008; r² = 0.95). In summary, androgens induced aggressive

2013 Behavioral neuroscience Controlled trial quality: uncertain

5. Abiraterone acetate (prostate cancer) - Benefit assessment according to §35a Social Code Book V

pain e ? bisphosphonates and denosumab for the treatment of bone metastasis ? eplerenone for the treatment of mineralocorticoid side effects ? systemic glucocorticoids if clinically indicated in potentially fatal medical circumstances ? transfusions and haematopoietic growth factors Non-permitted concomitant treatment: ? any test medication except abiraterone ? other antineoplastic agents ? radiotherapy ? 5a reductase inhibitors ? chemotherapy ? immunotherapy (continued) Extract of dossier

2019 Institute for Quality and Efficiency in Healthcare (IQWiG)

6. Androgenetic Alopecia

follicle in predisposed men and women. Its aetiology is multifactorial and polygenic (13). Men Androgenetic alopecia in men is an androgen-dependent trait (14). Evidence from genetic disorders and from clinical trials of 5a-reductase inhibitors has shown that dihydrotestosterone (DHT) is the androgen chiefly responsible for the follicular pathology although the molecular and cellular events are only partially understood. DHT probably acts primarily on dermal papilla, the predominant site of androgen (...) receptor and Type II 5a-reductase expression within the hair follicle. A number of signaling molecules have been implicated in the inhibition of hair growth in AGA including TGF-ß1 and TGF-ß2(14), dickopf 1 (a member of the WNT-signaling family)(15) and IL-6(16). There is also evidence for involvement of prostaglandins in AGA. The enzyme PGD(2)-synthase and its product PGD(2) are elevated in balding scalp skin; PGD(2) has an inhibitory effect on hair growth in animal and in in vitro experiments (17). 6

2017 European Dermatology Forum

7. Male Hypogonadism

during the foetal period [7]. In addition, testosterone is needed for development of the prostate, penis and scrotum. However, in these organs testosterone is converted into the more potent metabolite 5a-dihydrotestosterone (DHT) by the enzyme 5a-reductase. Testosterone and DHT are required for penile growth, both activating the androgen receptor [8]. Intratesticular testosterone is needed to maintain the spermatogenic process and to inhibit germ cell apoptosis [9]. The seminiferous tubules (...) of the testes are exposed to concentrations of testosterone 25-100 times greater than circulating levels. Suppression of gonadotrophins (e.g. through excessive testosterone abuse) results in a reduced number of spermatozoa in the ejaculate and hypospermatogenesis [10]. Complete inhibition of intratesticular testosterone results in full cessation of meiosis up to the level of round spermatids [11, 12]. Testosterone does not appear to act directly on the germ cells, but functions through the Sertoli cells

2015 European Association of Urology

8. Treatment of Non-neurogenic Male LUTS

considerations 14 3C.2 Pharmacological management 14 3C.2.1 a 1 -Adrenoceptor antagonists (a 1 -blockers) 14 3C.2.2 5a-Reductase inhibitors 17 3C.2.3 Muscarinic receptor antagonists 18 3C.2.4 Phosphodiesterase 5 inhibitors 21 3C.2.5 Plant extracts - phytotherapy 23 3C.2.6 Vasopressin analogue - desmopressin 25 3C.2.7 Emerging therapies 26 3C.2.7.1 Beta-3 agonists 26 3C.2.8 Combination therapies 27 3C.2.8.1 a 1 -blockers + 5a-reductase inhibitors 27 3C.2.8.2 a 1 -blockers + muscarinic receptor antagonists 29 (...) aged > 80 years. 3 C When considering surgery in men with bothersome, predominantly voiding LUTS, PFS should be performed in men aged 30 mL and increased risk for disease progression showed that dutasteride reduced LUTS at least as much as, or even more effectively than, the a 1 -blocker tamsulosin [124, 157, 164]. The greater the baseline prostate volume (or serum PSA concentration), the faster and more pronounced the symptomatic benefit of dutasteride. 5a-reductase inhibitors, but not a 1

2015 European Association of Urology

9. GreenLight Laser for the Treatment of Benign Prostatic Hypertrophy

includes watchful waiting, medications (a 1 -adrenergic receptor antagonists, 5a-reductase inhibitors), minimally invasive treatments (transurethral microwave therapy, transurethral needle ablation), surgery (transurethral resection of the prostate [TURP], open prostatectomy), and laser treatment. 1 TURP involves removing part of the prostate gland through the urethra. Clinical trials have shown that TURP is effective in reducing BPH symptoms. 2 Complication rate following TURP is up to 20%, and up

2013 Canadian Agency for Drugs and Technologies in Health - Rapid Review

10. Mitochondrial dysfunction in an animal model of diabetic neuropathy is associated with a reduction of neurosteroid synthesis. Full Text available with Trip Pro

neuropathy ( ob/ob) and WT controls aged 60-80 days. Results: There was a key difference in the response of the WT and ob/ob cortical neurons to simultaneous incubation with diazepam and flumazenil. In contrast, diazepam and the 5a-reductase inhibitor finasteride, individually or in combination, produced the same response in both strains. Conclusions: The exaggerated effect of diazepam on GABAergic inhibitory tone in the ob/ob, despite the presence of the GABA AR benzodiazepine antagonist flumazenil

2018 F1000Research

11. BCL-2 and BCL-XL expression are down-regulated in benign prostate hyperplasia nodules and not affected by finasteride and/or celecoxib Full Text available with Trip Pro

the expression of B-cell lymphoma 2 (BCL-2) and B-cell lymphoma-extra large (BCL-XL), two important anti-apoptosis factors that are also capable of inhibiting cell proliferation via accelerated G1 arrest or delayed G1/S transition, using immunostaining in simple prostatectomy BPH specimens from patients naïve to androgen manipulation. Since androgens and inflammation are thought to play important roles in BPH pathogenesis, we tested the effect of inhibiting 5a-reductase and/or COX-2 on the expression of BCL (...) -2 and BCL-XL in BPH specimens from prostate cancer patients with BPH. These patients had no prior use of chronic NSAIDs and/or 5a-reductase inhibitors and were treated with celecoxib, finasteride, celecoxib plus finasteride or no treatment for 28 consecutive days prior to surgery. In all specimens, BCL-2 and BCL-XL staining was evident in both luminal and basal epithelial cells, with more intense staining in basal cells. Both luminal and basal cells exhibited decreased BCL-2 and BCL-XL staining

2018 American journal of clinical and experimental urology

12. Position Statement: Prostate Artery Embolization for Treatment of Benign Disease of the Prostate

to LUTS, ranging from 0 (delighted) to 6 (terrible). EXISTING THERAPIES PatientswithmildLUTSaregenerallytreatedwithwatchfulwaitingor lifestyle modi?cation. Medical treatment is usually the ?rst-line treat- ment option, and is indicated for patients with moderate LUTS. The two main categories of medications for management of BPH are a-blockers and 5a-reductase inhibitors. Patients who cannot tolerate these drugs, whose disease is refractory to treatment, or who develop complications of BPH while

2014 Society of Interventional Radiology

13. Consensus on women?s health aspects of polycystic ovary syndrome (PCOS): the Amsterdam ESHRE/ASRM-Sponsored 3rd PCOS Consensus Workshop Group

–binding globulin(SHBG),which,inturn,resultsinadecreaseincircu- lating free T levels. The progestin in the pill can compete for 5a-reductase at the level of the androgen receptor. Oral con- traception also decreases adrenal androgen production by a mechanism yet unclear, possibly due to a decrease in adre- nocorticotropin hormone (ACTH) production. There are few randomized double-blind studies compar- ing the metabolic effects of a combination of two OCPs, or combined with an insulin sensitizer (21 (...) - ual responses vary. It is not effective for hirsutism and occa- sionallymayleadtoalopecia.Physicalapproachestoremove unwanted hair, including electrolysis and laser treatments, may be acceptable to many patients. Topical treatment with e?ornithine hydrochloride, an inhibitor of ornithine decar- boxylase,limitscelldivisionandhasbeenshowntobeeffec- tive for decreasing the development of new unwanted facial hair (15). No effective pharmacologic treatment for alopecia exists. Conclusions(Agreement

2012 Society for Assisted Reproductive Technology

14. Saw Palmetto

Palmetto Scientific names: Serenoa repens, Sabal serrulata Dwarf palm tree grows in southeast U.S. Active ingredient: s Extract compositions are not standardized Some preparations contain almost no active ingredient VI. Pharmacokinetics: Saw Palmetto berry In vitro activity Anti-androgen Anti- Anti-Inflammatory Inhibits Testosterone-5a-reductase (High dose) Less Testosterone to Dihydrotestosterone conversion Inhibits binding of androgen to receptor (High dose) In vivo activity No anti-androgen effects

2018 FP Notebook

15. Bicalutamide With or Without Metformin for Biochemical Recurrence in Overweight or Obese Prostate Cancer Patients

free for ≥ 2 years. Subjects currently treated with metformin and/or bicalutamide or who have been treated with metformin and/or bicalutamide in the past 6 months. Subjects who have taken 5a-reductase inhibitors (finasteride or dutasteride), saw palmetto, or PC-SPES within the last 6 weeks are ineligible. Subjects will be eligible for the study after the wash out period of 6 weeks. Contacts and Locations Go to Information from the National Library of Medicine To learn more about this study, you

2015 Clinical Trials

16. A Randomized, Double-blind Clinical Trial to Evaluate the Safety and Efficacy of the X5 HairLaser for the Treatment of Androgenetic Alopecia in Males

area or scarring in the target area. Has photosensitivity to laser light. Has used Accutane in the previous year. Has a history of poor wound healing. Has a history of keloid formation. Has a known history of anticoagulant or antiplatelet use. Has used or currently takes any of the following medications during the six months prior to screening: finasteride (or any other 5a-reductase inhibitor medications), medications with anti-androgenic properties, topical estrogen, progesterone, tamoxifen

2014 Clinical Trials

17. Randomized Salvage Radiation Therapy Plus Enzalutamide Post Prostatectomy

woman. Exclusion Criteria: Currently active second malignancy Primary treatment with radiation therapy. Radiographic or clinical evidence of local-regional tumor recurrence, Concurrent use of other antiandrogens, estrogen-like agents, or 5a-reductase inhibitors. Use of systemic corticosteroids equivalent to prednisone (inhaled corticosteroids are permitted). Concurrent use of other anti-cancer agents or treatments. Serious concurrent medical illnesses (including uncontrolled major cardiac, pulmonary (...) Description: Enzalutamide is a second-generation androgen receptor signaling inhibitor that significantly prolongs survival in patients with metastatic castration-resistant prostate cancer who have received prior docetaxel chemotherapy 35,36. Enzalutamide has demonstrated activity in cells that overexpress the androgen receptor. Unlike previous androgen receptor blocker (ARB) agents, Enzalutamide does not display any agonist properties and blocks translocation of the ligand-receptor complex

2014 Clinical Trials

18. 5-Alpha-Reductase Deficiency (Treatment)

. Molecular genetics of steroid 5 alpha-reductase 2 deficiency. J Clin Invest . 1992 Sep. 90(3):799-809. . Azzouni F, Godoy A, Li Y, Mohler J. The 5 alpha-reductase isozyme family: a review of basic biology and their role in human diseases. Adv Urol . 2012. 2012:530121. . . Maimoun L, Philibert P, Bouchard P, Ocal G, Leheup B, Fenichel P. Primary amenorrhea in four adolescents revealed 5a-reductase deficiency confirmed by molecular analysis. Fertil Steril . 2011 Feb. 95(2):804.e1-5. . Costa EM, Domenice S (...) , Sircili MH, Inacio M, Mendonca BB. DSD due to 5a-reductase 2 deficiency - from diagnosis to long term outcome. Semin Reprod Med . 2012 Oct. 30(5):427-31. . Medonca BB, Domenice S, Arnhold, JP, and Costa EMF. 46, XY disorders of sex development (DSD). Clinical Endocrinology . 2009. 70:173-187. Allen L. Disorders of Sexual Development. Obstet Gynecol Clin N Am . 2009. 36:25-45. Bertelloni S, Scaramuzzo RT, Parrini D, Baldinotti F, Tumini S, Ghirri P. Early diagnosis of 5alpha-reductase deficiency

2014 eMedicine Pediatrics

19. 5-Alpha-Reductase Deficiency (Overview)

. Molecular genetics of steroid 5 alpha-reductase 2 deficiency. J Clin Invest . 1992 Sep. 90(3):799-809. . Azzouni F, Godoy A, Li Y, Mohler J. The 5 alpha-reductase isozyme family: a review of basic biology and their role in human diseases. Adv Urol . 2012. 2012:530121. . . Maimoun L, Philibert P, Bouchard P, Ocal G, Leheup B, Fenichel P. Primary amenorrhea in four adolescents revealed 5a-reductase deficiency confirmed by molecular analysis. Fertil Steril . 2011 Feb. 95(2):804.e1-5. . Costa EM, Domenice S (...) , Sircili MH, Inacio M, Mendonca BB. DSD due to 5a-reductase 2 deficiency - from diagnosis to long term outcome. Semin Reprod Med . 2012 Oct. 30(5):427-31. . Medonca BB, Domenice S, Arnhold, JP, and Costa EMF. 46, XY disorders of sex development (DSD). Clinical Endocrinology . 2009. 70:173-187. Allen L. Disorders of Sexual Development. Obstet Gynecol Clin N Am . 2009. 36:25-45. Bertelloni S, Scaramuzzo RT, Parrini D, Baldinotti F, Tumini S, Ghirri P. Early diagnosis of 5alpha-reductase deficiency

2014 eMedicine Pediatrics

20. 5-Alpha-Reductase Deficiency (Diagnosis)

. Molecular genetics of steroid 5 alpha-reductase 2 deficiency. J Clin Invest . 1992 Sep. 90(3):799-809. . Azzouni F, Godoy A, Li Y, Mohler J. The 5 alpha-reductase isozyme family: a review of basic biology and their role in human diseases. Adv Urol . 2012. 2012:530121. . . Maimoun L, Philibert P, Bouchard P, Ocal G, Leheup B, Fenichel P. Primary amenorrhea in four adolescents revealed 5a-reductase deficiency confirmed by molecular analysis. Fertil Steril . 2011 Feb. 95(2):804.e1-5. . Costa EM, Domenice S (...) , Sircili MH, Inacio M, Mendonca BB. DSD due to 5a-reductase 2 deficiency - from diagnosis to long term outcome. Semin Reprod Med . 2012 Oct. 30(5):427-31. . Medonca BB, Domenice S, Arnhold, JP, and Costa EMF. 46, XY disorders of sex development (DSD). Clinical Endocrinology . 2009. 70:173-187. Allen L. Disorders of Sexual Development. Obstet Gynecol Clin N Am . 2009. 36:25-45. Bertelloni S, Scaramuzzo RT, Parrini D, Baldinotti F, Tumini S, Ghirri P. Early diagnosis of 5alpha-reductase deficiency

2014 eMedicine Pediatrics

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