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α-Adrenoceptor Antagonists in the Treatment of Benign Prostatic Hyperplasia

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Abstract

Lower urinary tract symptoms secondary to benign prostatic hyperplasia (BP have a significant impact on the lifestyle of older men. Transurethral resection of the prostate (TURP) is the most effective surgical therapy for this condition but an increasing number of patients are electing conservative medical therapy. α-Adrenoceptor antagonists and 5α-reductase inhibitors are the 2 categories of drug therapy currently available for BPH. Use of α-adrenoceptor antagonists in the treatment of BPH is based on their ability to prevent the neural stimulation which induces prostate smooth muscle contraction, producing lower urinary tract symptoms. Several studies have demonstrated that α-receptors predominate in the prostatic stroma, capsule and bladder neck. Initial work focused on the use of phenoxybenzamine, a nonspecific α-blocker, in the treatment of BPH. While results were promising, significant adverse effects and concern over potential mutagenicity have resulted in a lack of use of this medication for this indication. Subsequent attention was directed towards the short-acting α-specific antagonist prazosin. Results conflicted regarding whether an actual sustained improvement in lower urinary tract symptoms could be achieved with this medication, and because of twice daily dosing compliance issues were a drawback. Thus, the mainstay in pharmacological treatment of BPH over the past decade has been 2 once-a-day α-specific antagonists, doxazosin and terazosin. Over 75% of all prescriptions written for BPH are for one of these 2 medications. Despite their tremendous success in both decreasing urinary symptoms and increasing urinary flow rates, systemic adverse effects can be bothersome. Recently, efforts have focused on use of α1A-urospecific antagonists such as tamsulosin and alfuzosin in an attempt to achieve similar clinical results as doxazosin and terazosin without systemic adverse effects. Thus far, results are promising, but long term studies must be done to determine whether pharmacological uroselectivity is actually clinically relevant.

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References

  1. Berry SJ, Coffey DS, Walsh PC, et al. The development of human benign prostatic hyperplasia with age. J Urol 1984; 132: 474–9

    PubMed  CAS  Google Scholar 

  2. Garraway WM, Russell EBAW, Lee RJ, et al. Impact of previously unrecognized benign prostatic hyperplasia on the daily activities of middle-aged and elderly men. Br J Gen Pract 1993; 43: 318–21

    PubMed  CAS  Google Scholar 

  3. McNeal JE, Leav I, Alroy J, et al. Differential lectin staining of central and peripheral zones of the prostate and alterations in dysplasia. Am J Clin Pathol 1988; 89: 41–8

    PubMed  CAS  Google Scholar 

  4. Kaplan SA, Goluboff ET, Olsson CA, et al. Effect of demographic factors, urinary peak flow rates, and Boyarsky symptorn scores on patient treatment choice in benign prostatic hyperplasia. Urology 1995; 45: 398–405

    Article  PubMed  CAS  Google Scholar 

  5. Eri LM, Tveter JK. Alpha blockade in the treatment of symptomatic benign prostatic hyperplasia. J Urol 1995; 154: 923–34

    Article  PubMed  CAS  Google Scholar 

  6. Caine M, Pfau A, Perlberg S. The use of alpha-adrenergic blockers in benign prostatic obstruction. Br J Urol 1976; 48: 255–63

    PubMed  CAS  Google Scholar 

  7. Abrams PH, Shah PJ, Stone R, et al. Bladder outflow obstruction treated with phenoxybenzamine. Br J Urol 1982; 54: 527–30

    Article  PubMed  CAS  Google Scholar 

  8. Boreham PF, Braithwaite P, Milewski P, et al. Alpha adrenergic blockers in prostatism. Br J Surg 1977; 64: 756–7

    Article  PubMed  CAS  Google Scholar 

  9. Lepor H, Auerbach S, Puras-Baez A, et al. A randomized, placebo-controlled multicenter study of the efficacy and safety of terazosin in the treatment of benign prostatic hyperplasia. J Urol 1992; 148: 1467–74

    PubMed  CAS  Google Scholar 

  10. McConnell JD, Barry MJ, Bruskewitz RC, et al. Benign prostatic hyperplasia: diagnosis and treatment. Clinical Practice Guideline no. 8. US Department of Health and Human Services, Agency for Health Care Policy and Research. No. 94-0582, 1994 Feb

  11. Lepor H, Tang R, Kobayashi S, et al. Localization of the alpha 1A-adrenoceptor in the human prostate. J Urol 1995; 154: 2096–9

    Article  PubMed  CAS  Google Scholar 

  12. Price DT, Schwinn DA, Lomasney JW, et al. Identification, quantification, and localization of mRNA for three distinct alpha-1-adrenergic receptor subtypes in human prostate. J Urol 1993; 150: 546–51

    PubMed  CAS  Google Scholar 

  13. Forray C, Bard JA, Wetzel JM, et al. The alpha-1-adrenergic receptor that mediates smooth muscle contraction in the human prostate has the pharmacological properties of the cloned human alpha-1-c subtype. Mol Pharmacol 1994; 45: 703–8

    PubMed  CAS  Google Scholar 

  14. Chappie CR, Burt RP, Andersson PO, et al. Alpha-1-adrenoreceptor subtypes in the human prostate. Br J Urol 1994; 74: 585–9

    Article  Google Scholar 

  15. Raz S, Zeigler M, Caine M. Pharmacological receptors in the prostate. Br J Urol 1973; 45: 663–7

    Article  PubMed  CAS  Google Scholar 

  16. Caine M, Raz S, Zeigler M. Adrenergic and cholinergic receptors in the human prostate, prostatic capsule and bladder neck. Br J Urol 1975; 47: 193–202

    Article  PubMed  CAS  Google Scholar 

  17. Lepor H, Gup DI, Baumann M, et al. Laboratory assessment of terazosin and alpha-1 blockade in prostatic hyperplasia. Urology 1988; 32 Suppl.: 21–6

    Article  PubMed  CAS  Google Scholar 

  18. Caine M, Perlberg S, Shapiro A. Phenoxybenzamine for benign prostatic obstruction. Urology 1981; 17: 542–6

    Article  PubMed  CAS  Google Scholar 

  19. Physicians Desk Reference. Montvale (NJ): Medical Economics Company, Inc., 1996

  20. Kirby RF, Coppinger SWC, Corcoran MO, et al. Prazosin in the treatment of prostatic obstruction. Br J Urol 1987; 60: 136–42

    Article  PubMed  CAS  Google Scholar 

  21. Chappie CR, Stott M, Abrams PH, et al. A 12-week placebo-controlled double-blind study of prazosin in the treatment of prostatic obstruction due to benign prostatic hyperplasia. Br J Urol 1992; 70: 285–94

    Google Scholar 

  22. Brawer MK, Adams G, Epstein H, et al. Terazosin in the treatment of benign prostatic hyperplasia. Arch Fam Med 1993; 2: 929–35

    Article  PubMed  CAS  Google Scholar 

  23. Roehrborn CG, Oesterling JE, Arbor A, et al. Evaluation of the clinical effectiveness of terazosin versus placebo in the treatment of patients with symptomatic benign prostatic hyperplasia [abstract no. 175]. J Urol 1995; 153 Suppl.: 272A

    Google Scholar 

  24. Lepor H. Long-term safety and effectiveness of terazosin for the treatment of benign prostatic hyperplasia: Terazosin Research Group. Urology 1995; 45: 406–13

    Article  PubMed  CAS  Google Scholar 

  25. Wilde MI, Fitton A, Sorkin EM. Terazosin: a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in benign prostatic hyperplasia. Drugs Aging 1993; 3: 258–77

    Article  PubMed  CAS  Google Scholar 

  26. Lowe FC. Safety assessments of terazosin in the treatment of patients with symptomatic benign prostatic hyperplasia: a combined analysis. Urology 1994; 44: 46–51

    Article  PubMed  CAS  Google Scholar 

  27. Christensen MM, Holme JB, Rasmussen PC, et al. Doxazosin treatment in patients with prostatic obstruction. Scand J Urol Nephrol 1993; 27: 39–44

    Article  PubMed  CAS  Google Scholar 

  28. Chappie CR, Carter P, Christmas TJ, et al. A three-month double-blind study of doxazosin as treatment for benign prostatic bladder outlet obstruction. Br J Urol 1994; 74: 50–6

    Article  Google Scholar 

  29. Gillenwater JY, Mobley DL. A sixteen-week, double-blind, placebo-controlled, dose-titration study using doxazosin tablets for the treatment of benign prostatic hyperplasia in normotensive males [abstract no. 447]. J Urol 1993; 149 Suppl.: 324A

    Google Scholar 

  30. Gillenwater JY, Conn RL, Chrysant SG, et al. Doxazosin for the treatment of benign prostatic hyperplasia in patients with mild to moderate essential hypertension: a double-blind, placebocontrolled, dose-response multicenter study. J Urol 1995; 154: 110–5

    Article  PubMed  CAS  Google Scholar 

  31. Rabasseda X, Fitzpatrick J. Tamsulosin: the first prostate-selective alpha la adrenoreceptor antagonist for the treatment of symptomatic benign prostatic hyperplasia. Drugs Today 1996; 32(3): 259–68

    CAS  Google Scholar 

  32. Lepor H, Tamsulosin Investigator Group. Clinical evaluation of tamsulosin, a prostate selective alpha 1c antagonist [abstract no. 182]. Proc Am Urol Assoc 1995; 153: 274A

    Google Scholar 

  33. Chappie CR, Wyndaele JJ, Nordling J, et al. Tamsulosin, the first prostate-selective alpha lA-adrenoceptor antagonist: a meta-analysis of two randomized, placebo-controlled, multi-centre studies in patients with benign prostatic obstruction (symptomatic BPH). European Tamsulosin Study Group. Eur Urol 1996; 29(2): 155–67

    Google Scholar 

  34. Schulman CC, Cortvriend J, Jonas U, et al. Tamsulosin, the first prostate-selective alpha 1A-adrenoceptor antagonist: analysis of a multinational, multicentre, open-label study assessing the long-term efficacy and safety in patients with benign prostatic obstruction (symptomatic BPH). European Tamsulosin Study Group. Eur Urol 1996; 29(2): 145–54

    CAS  Google Scholar 

  35. Lepor H. Phase III multicenter placebo-controlled study oftamsulosin in BPH. Urology 1998; 51: 892–900

    Article  PubMed  CAS  Google Scholar 

  36. Schulman CC, Lock TMTW, Buzelin J-M, et al. Tamsulosin 0.4mg once daily: 2-year follow-up efficacy and safety in 516 symptomatic BPH patients [abstract no. 535]. J Urol 1997; 157 Suppl.: 137

    Google Scholar 

  37. Jardin A, Bensadoun H, Delauche-Cavallier MC, et al. Affu-zosin for treatment of benign prostatic hypertrophy: the BPHALF Group. Lancet 1991; 337: 1457–61

    Article  PubMed  CAS  Google Scholar 

  38. Jardin A, Bensadoun H, Delauche-Cavallier MC, et al. Long-term treatment of benign prostatic hyperplasia with alfuzosin: a 24–30 month survey. The BPHALF group. Br J Urol 1994; 74: 579–84

    Article  PubMed  CAS  Google Scholar 

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Cooper, K.L., McKiernan, J.M. & Kaplan, S.A. α-Adrenoceptor Antagonists in the Treatment of Benign Prostatic Hyperplasia. Drugs 57, 9–17 (1999). https://doi.org/10.2165/00003495-199957010-00002

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