CURRENT ISSUES IN ALPHA1-ADRENERGIC BLOCKER THERAPY: INTEGRATION OF PHARMACOLOGICAL APPROACH AND CLINICAL EXPERIENCE


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Four successive stages in the action of the alpha1-adrenergic blocker (a1-AB) are discussed in the article. When describing the pharmaceutical and pharmacokinetic stages, the features of absorption, bioavailability and distribution of three a1-AB are discussed: alfuzosin, tamsulosin and silodosin. From a practical point of view, it is important that the bioavailability of alfuzosin and tamsulosin will increase during transit through the gastrointestinal tract, which means that extended-release dosage form (Alfuprost MR) has advantages compared to conventional immediate-release tablets. Alfuzosin has the highest volume of distribution among a1-AB (2.5 l/ kg), which indicates its maximum prostatotropic index compared to other a1-AB. The clinical uro selectivity of a1-AB directly depends on their pharmacological profile, in accordance with the chemical structure and pharmacological properties. The clinical uroselectivity of alfuzosin is provided mainly by unique pharmacokinetic/functional properties (volume of distribution, prostatotropism), while tamsulosin and silodosin are dominated by the receptor/pharmacodynamic component. Controlled studies have shown that a1-AB reduce I-PSS by about 30-40% and increase Qmax by about 20-25%. Evaluation of the safety of a1-AB includes monitoring for side effects, including asthenia, dizziness, and (orthostatic) hypotension. According to a meta-analysis, the vasodilatory effect is most pronounced with doxazosin and terazosin, but is much less common and with comparable alfuzosin and tamsulosin. For personalized approach in choosing an a1-AB for the drug therapy of LUTS in BPH one should takes into account, on the one hand, the individual characteristics of the patient (the presence of concomitant pathologies: arterial hypertension, coronary heart disease, diabetes mellitus), and on the other hand, the individual pharmacological profile of a1-AB, the risk of developing drug interactions. Based on the results of extensive clinical experience, including data from recent clinical trials, Alfuprost® MR (alfuzosin 10 mg in the form of extended-release tablets) demonstrated a pronounced clinical uroselectivity, high efficiency in the relief of LUTS and cardiovascular safety in comorbid patients, including those with cardiovascular diseases.

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Sobre autores

A. Martov

A.I. Burnazyan SRC FMBC, FMBA of Russia; City clinical hospital named after D.D. Pletnev of the Health Department c. Moscow”

Email: martovalex@mail.ru
corr. member of RAS, Ph.D., MD, professor, head of the Department of urology and Andrology of Federal Medical and Biological Center named after A.I. Burnazyan FMBA RF; Head of the Urology Department of City clinical hospital named after D.D. Pletnev of the Health Department c. Moscow” Moscow, Russia

A. Dukhanin

Pirogov Russian National Research Medical University

Email: das03@rambler.ru
Ph.D., MD, professor of the Department of the Molecular Pharmacology Moscow, Russia

A. Bernikov

A.I. Evdokimov Moscow State University of Medicine and Dentistry of Minzdrav of Russia

Email: bernikov@mac.com
Ph.D. Moscow, Russia

Bibliografia

  1. Грэхам-Смит Д.Г., Аронсон Д.К. Оксфордский справочник по клинической фармакологии и фармакотерапии. М.: Медицина, 2000. 744 с.
  2. Trame, Mirjam N., Biliouris, Konstantinos, Lesko, Lawrence J., Mettetal, Jerome T., Systems pharmacology to predict drug safety in drug development. 2016, doi: 10.1016/j.ejps.2016.05.027
  3. Dugger, S., Platt, A. & Goldstein, D. Drug development in the era of precision medicine. Nat Rev Drug Discov 2P18;17:183-196.
  4. Kiriiri, G.K., Njogu, P.M. & Mwangi, A.N. Exploring different approaches to improve the success of drug discovery and development projects: a review. Futur J Pharm Sci. 2020;6:27. https://doi.org/10.1186/s43094-020-00047-9
  5. Sinisa Vukovic, David J. Huggins. Quantitative metrics for drug-target ligandability. Drug Discovery Today. 2018; 23(6):1258-1266.
  6. Lepor H. Medical treatment of benign prostatic hyperplasia. Rev Urol. 2011;13(1):20-33.
  7. Andersson K.-E. The Concept of Uroselectivity. Eur Urol. 1998;33(2):7-11.
  8. Roehrborn C.G. Alfuzosin: overview of pharmacokinetics, safety, and efficacy of a clinically uroselective alfa-blocker. Urology. 2001; 58 (Suppl 6A):55-64.
  9. Spring S.K. Silodosin is a new drug of the group of selective a1-blockers. Experimental and clinical urology. 2012.Russian (Яровой СК. Силодозин - новый препарат группы селективных а1-адреноблокаторов. Экспериментальная и клиническая урология. 2012; 3).
  10. Электронный ресурс: https://go.drugbank.com/.Russian (Электронный ресурс: https://go.drugbank.com/)
  11. Sanki U.K., Mandal B.K. In vitro-in vivo correlation evaluation of generic alfuzosin modified release tablets. ISRN Toxicol. 2012; 2012:813-836.
  12. Vinarov Z., Abdallah M., Agundez J.A.G. et. al. Impact of gastrointestinal tract variability on oral drug absorption and pharmacokinetics: An UNGAP review. European Journal of Pharmaceutical Sciences. 2021; 162 https://doi.org/10.1016/j.ejps.2021.105812
  13. Alhayali A., Vuddanda P.R., Velaga S. Silodosin oral films: Development, physico-mechanical properties and in vitro dissolution studies in simulated saliva. J Drug Deliv Sci Technol. 2019;53:101122.
  14. White C.W., da Silva Junior E.D., Lim L., Ventura S. What makes the a(1A) -adrenoceptor gene product assume an a(1L) -adrenoceptor phenotype? Br J Pharmacol. 2019;176(14):2358-2365.
  15. Roehrborn С., Rosen R. Medical therapy options for aging men with benign prostatic hyperplasia: focus on alfuzosin 10 mg once daily. Clinical interventions in aging. 2008;3(3):511-524.
  16. Martin D.J., Lluel P., Pouyet T., Rauch-Desanti C., Angel I. Relationship between the effects of alfuzosin on rat urethral and blood pressures and its tissue concentrations. Life Sci. 1998;63(3):169-176.
  17. Eckert R.E. Prostate selectivity of alpha-1-adrenoreceptor blockers. J Urol. 1999;161(4):233.
  18. Пушкарь Д.Ю., Раснер П.И. Терапия а-адреноблокаторами у больных ДГПЖ. Лечащий врач. 2007;4:4-10.
  19. Yoo T.K., Cho H.J. Benign prostatic hyperplasia: from bench to clinic. Korean J Urol. 2012;53(3):139-148.
  20. Yuan.J, Liu Y., Yang Z., Qin X., Yang K., Mao C. The efficacy and safety of alpha-1 blockers for benign prostatic hyperplasia: an overview of 15 systematic reviews. Curr Med Res Opin. 2013;29(3):279-287.
  21. Chapple C.R. Alpha adrenoceptor antagonists in the year 2000: is there anything new? Curr Opin Urol 2001; 11:9-16.
  22. Archer M., Dogra N., Dovey Z. et al. Role of a- and ß-adrenergic signaling in phenotypic targeting: significance in benign and malignant urologic disease. Cell Commun Signal. 2021;19(78). https://doi.org/10.1186/s12964-021-00755-6
  23. Wade C.A., Goodwin J., Preston D, Kyprianou N. Impact of a-adrenoceptor antagonists on prostate cancer development, progression and prevention. Am J Clin Exp Urol. 2019;7(1):46-60.
  24. Michel M.C. The forefront for novel therapeutic agents based on the pathophysiology of lower urinary tract dysfunction: alpha-blockers in the treatment of male voiding dysfunction-how do they work and why do they differ in tolerability? J Pharmacol Sci. 2010;112(2):151-157.
  25. Patent WO 2004/037228 A1.Russian (патент WO 2004/037228 A1). https://patentimages.storage.googleapis.com/86/bc/a3/11f640bd555ea8/WO2004037228A1.pdf
  26. Calogero A.E. et al. Epidemiology and risk factors of lower urinary tract symptoms/benign prostatic hyperplasia and erectile dysfunction. The Aging Male. 2019;22(1):12-19.
  27. Аполихин О.И., Сивков А.В., Бешлиев Д.А. Анализ урологической заболеваемости в Российской Федерации в 2002-2009 гг. по данным официальной статистики/ Экспериментальная и клиническая урология. 2011;1:4-10.
  28. Просянников М.Ю., Цой А.А., Мадыкин Ю.Ю. Организация трёхуровневой системы медицинской помощи в урологии. М.: Издательство «Уромедиа», 2017. 122 c.
  29. Шпиленя Е.С., Бурлака О.О., Пешехонов К.С., Шабулдов К.В. Оказание неотложной помощи при острой задержке мочеиспускания у мужчин. Современная лечебная тактика, противоречия и перспективы. Скорая медицинская помощь. 2019;20(1):69-79.
  30. Наумов А.В., Алексеев И.Д., Будылев С.А. Болезни стареющих мужчин: в фокусе предстательная железа. Врач скорой помощи. 2011;6:31-39.
  31. Jacobsen S.J., Jacobson D.J., Girman C.J., Roberts R.O., Rhodes T., Guess H.A., Lieber M.M. Natural History of Prostatism: Risk Factors for Acute Urinary Retention. The Journal of Urology. 1997; 158(2):481-487. doi: 10.1016/s0022-5347(01)64508-7.
  32. EAU Guidelines on Management of Non-Neurogenic Male Lower Urinary Tract Symptoms (LUTS), 2022. https://uroweb.org/guidelines/management-of-non-neurogenic-male-luts entry date 20.04.2022.
  33. Djavan B. et al. State of the art on the efficacy and tolerability of alpha1-adrenoceptor antagonists in patients with lower urinary tract symptoms suggestive of benign prostatic hyperplasia. Urology. 2004. 64:1081. https://www.ncbi.nlm.nih.gov/pubmed/15596173
  34. Barendrecht M.M., et al. Do alpha1-adrenoceptor antagonists improve lower urinary tract symptoms by reducing bladder outlet esistance? Neurourol Urodyn. 2008;27:226. https://www.ncbi.nlm.nih.gov/pubmed/17638312
  35. Djavan B. et al. Longitudinal study of men with mild symptoms of bladder outlet obstruction treated with watchful waiting fo four years. Urology. 2004;64:1144. https://www.ncbi.nlm.nih.gov/pubmed/15596187
  36. Michel M.C. et al.Comparison of tamsulosin effi cacy in subgroups of patients with lower urinary tract symptoms. Prostate Cancer Prostatic Dis. 1998;1:332. https://www.ncbi.nlm.nih.gov/pubmed/12496876
  37. McConnell J.D. et al. The long-term eff ect of doxazosin, fi nasteride, and combination therapy on the clinical progression of benign prostatic hyperplasia. N Engl J Med. 2003;349:2387. https://www.ncbi.nlm.nih.gov/pubmed/14681504
  38. Boyle P. et al. Meta-analysis of randomized trials of terazosin in the treatment of benign prostatic hyperplasia. Urology. 2001;58:717. https://www.ncbi.nlm.nih.gov/pubmed/11711348
  39. Roehrborn C.G. Three months’ treatment with the alpha1-blocker alfuzosin does not affect total or transition zone volume of the prostate. Prostate Cancer Prostatic Dis. 2006;9:121. https://www.ncbi.nlm.nih.gov/pubmed/16304557
  40. Roehrborn C.G. et al. The effects of dutasteride, tamsulosin and combination therapy on lower urinary tract symptoms in men with benign prostatic hyperplasia and prostatic enlargement: 2-year results from the CombAT study. J Urol. 2008;179:616. https://www.ncbi.nlm.nih.gov/pubmed/18082216
  41. Roehrborn C.G. et al. The effects of combination therapy with dutasteride and tamsulosin on clinical outcomes in men with symptomatic benign prostatic hyperplasia: 4-year results from the CombAT study. Eur Urol. 2010;57:123. https://www.ncbi.nlm.nih.gov/pubmed/19825505
  42. Manjunatha R., Pundarikaksha H.P., Madhusudhana H.R., Amarkumar J., Hanumantharaju B.K., Manjunatha R., et al. A randomized, comparative, open-label study of efficacy and tolerability of alfuzosin, tamsulosin and silodosin in benign prostatic hyperplasia. Indian J Pharmacol. 201648(2):134-140. doi: 10.4103/0253-7613.178825.]
  43. Mari A., Antonelli A., Cindolo L. et al. Alfuzosin for the medical treatment of benign prostatic hyperplasia and lower urinary tract symptoms: a systematic review of the literature and narrative synthesis. Ther Adv Urol. 2021;13:1756287221993283.
  44. Roehrborn C.G., Van Kerrebroeck P., Nordling J. Safety and efficacy of alfuzosin 10 mg once-daily in the treatment of lower urinary tract symptoms and clinical benign prostatic hyperplasia: a pooled analysis of three doubleblind, placebo-controlled studies. BJU International. 2003;92(3):257-261. doi: 10.1046/j.1464-410x.2003.04309.x.
  45. Elhilali M., Emberton M., Matzkin H., et al. Longterm efficacy and safety of alfuzosin 10 mg once daily: a 2-year experience in “real-life” practice. BJU Int. 2006;97:513-519.
  46. Nickel J.C., et al. A meta-analysis of the vascular-related safety profi le and efficacy of alphaadrenergic blockers for symptoms related to benign prostatic hyperplasia.Int J Clin Pract. 2008;62:1547. https://www.ncbi.nlm.nih.gov/pubmed/18822025
  47. Barendrecht M.M. et al. Treatment oflower urinary tract symptoms suggestive of benign prostatic hyperplasia: the cardiovascular system. BJU Int. 2005;95(Suppl. 4):19. https://www.ncbi.nlm.nih.gov/pubmed/15871732
  48. Welk B. et al. The risk of fall and fracture with the initiation of a prostate-selective alpha antagonist: a population based cohort study. BMJ. 2015;351:h5398. https://www.ncbi.nlm.nih.gov/pubmed/26502947
  49. Abrams P.H., Feneley R.C.L. The Significance of the Symptoms Associated with Bladder Outflow Obstruction. Urologia Internationalis. 1978;33(1-3):171-174. doi: 10.1159/000280194.
  50. Officers A. Coordinators for the ALLHAT Collaborative Research Group: The Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial. Major outcomes in high-risk hypertensive patients randomized to angiotensin-converting enzyme inhibitor or calcium channel blocker vs diuretic: The Antihypertensive and Lipid-Lowering Treatment to Prevent Heart Attack Trial (ALLHAT). JAMA. 2002;288(23):2981-2997.
  51. Mondaini N., Giubilei G., Ungar A., et al. Alfuzosin (10 mg) does not affect blood pressure in young healthy men. Eur Urol. 2006;50:1292-1298.
  52. Sdnchez-Chapado M., Guil M., Alfaro V., Badiella L., Ferndndez-Hernando N. Safety and Efficacy of Sustained-Release Alfuzosin on Lower Urinary Tract Symptoms Suggestive of Benign Prostatic Hyperplasia in 3,095 Spanish Patients Evaluated during General Practice. European Urology. 2000;37(4):421-427. doi: 10.1159/000020163.
  53. Hartung R., Matzkin H., Alcaraz A., Emberton M.,Harving N.,van Moorselaar J., Vallancien G. Age, Comorbidity and Hypertensive Co-Medication do Not Affect Cardiovascular Tolerability of 10 Mg Alfuzosin Once Daily. The Journal of Urology. 2006;175(2):624-628. doi: 10.1016/s0022-5347(05)00155-2.
  54. Кузьменко К.Д., Кузьменко Д.Д., Гяургиев Т.К. Современные возможности терапии урологического пациента с сопутствующими заболеваниями сердечно-сосудистой системы. Урология 2021;6:78-84. Doi: https: //dx.doi.org/10.18565/urology.2021.6.78-84.

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