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Tamsulosin

A Review of its Pharmacology and Therapeutic Efficacy in the Management of Lower Urinary Tract Symptoms

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Summary

Abstract

Tamsulosin is a subtype-selective α1A- and α1D-adrenoceptor antagonist. α1-Receptors predominate in the prostate gland, prostatic capsule, prostatic urethra and bladder, and the relaxation of prostate and bladder smooth muscles is associated with improved maximal urine flow (Qmax) and alleviation of lower urinary tract symptoms (LUTS) in patients with benign prostatic hyperplasia (BPH).

Tamsulosin 0.4mg once daily in a modified-release formulation increased Qmax and improved symptom scores relative to baseline to a greater extent than placebo in 12- and 13-week double-blind, randomised, multicentre, clinical trials in patients with LUTS, with statistical significance between treatments for Qmax values in two of three published US and European studies. Tamsulosin is effective in patients with mild to severe LUTS associated with BPH, in patients with diabetes mellitus and in the elderly, and does not interfere with concomitant antihypertensive therapy. Pooled data based on patients receiving tamsulosin 0.4 or 0.8mg once daily indicate maintenance of efficacy for up to 6 years.

Tamsulosin 0.4mg once daily was of similar efficacy to alfuzosin 2.5mg three times daily, with less tendency to cause hypotensive effects, in a double-blind, randomised 12-week trial. Benefit of the drug has also been shown in patients with acute urinary retention or chronic abacterial prostatitis, those receiving high energy transurethral microwave thermotherapy, and in patients with prostate cancer with radiation-induced urethritis.

Dizziness and abnormal ejaculation are stated to be the most common adverse events, with asthenia, postural hypotension and palpitations being seen less frequently (1 to 2% incidence), in patients receiving tamsulosin 0.4mg once daily. Tamsulosin has not been associated with clinically significant changes in blood pressure in clinical trials.

Conclusion: The α1A- and α1D-adrenoceptor antagonist tamsulosin, given at a dosage of 0.4mg once daily in a modified-release formulation, is effective and well tolerated in the treatment of LUTS associated with BPH. Although the drug has been directly compared to date with one other agent only, data show overall that tamsulosin clearly offers advantages over other α1-adrenoceptor antagonists in terms of the need for a single daily dose only, and its low potential for hypotensive effects or interference with concomitant antihypertensive therapy. Dosage titration at the start of treatment is not necessary. Tamsulosin has a rapid onset of action and is effective in patients with moderate or severe symptoms. The drug is therefore a valuable therapeutic option, with both demonstrated and potential advantages over older nonselective agents, in the management of patients with LUTS associated with BPH.

Pharmacodynamic Properties

Tamsulosin is a subtype-selective α1-adrenoceptor antagonist with a greater selectivity for prostatic tissues (where α1A-adrenoceptors predominate) than for vascular tissues (α1B-predominant). In contrast, other α1-adrenoceptor antagonists (e.g. prazosin, terazosin, doxazosin and alfuzosin) show minimal subtype selectivity.

The efficacy of tamsulosin is attributable to the blockade of α1A-adrenoceptors in the prostate gland. This inhibits smooth muscle contraction and improves dynamic voiding, which leads in turn to an improvement in the maximum urinary flow rate (Qmax). The blockade of α1A- and α1D-adrenoceptors in the bladder results in the inhibition of detrusor muscle contractions, which leads to reduced detrusor muscle instability and reduction of storage symptoms.

Tamsulosin is associated with a low potential for vasodilation and associated cardiovascular adverse effects. The vascular α1-adrenoceptor activity of single doses of tamsulosin 0.2mg, assessed by finger skin vasoconstrictor response to cold stimulation and dorsal vein constrictor response to increasing doses of phenylephrine, was similar to that of placebo and less than that of doxazosin 1mg, terazosin 1mg or tamsulosin 0.6mg in studies in healthy volunteers.

Tamsulosin 0.4 mg/day does not appear to have any clinically significant effect on prostate specific antigen levels.

Pharmacokinetic Properties

Tamsulosin displays linear kinetics after administration of single and multiple doses. Plasma concentrations are associated with considerable interindividual variability, and steady-state plasma concentrations are generally reached within 4 to 7 days. In healthy volunteers aged 55 to 75 years, areas under plasma drug concentration versus time curves (AUCs) were 40% higher than in volunteers aged 20 to 32 years.

Metabolism of tamsulosin takes place in the liver via the cytochrome P450 (CYP) enzyme system (primarily CYP3A4 and CYP2D6), and most of the drug in plasma is unchanged. Unchanged drug accounted for 81% of radioactivity in plasma 0.5 to 4 hours after oral administration of an aqueous solution of radiolabelled tamsulosin 0.2mg; 62% of the drug was recovered in the urine, and unchanged tamsulosin accounted for 8.7% of the dose.

There are no clinically significant differences in the pharmacokinetics of tamsulosin between patients with normal renal function and those with moderate to severe renal impairment. Data indicate that unbound active plasma concentrations of tamsulosin are increased by a factor of 1.5, with increases in renal clearance and percentage excretion of tamsulosin, in patients with moderate hepatic dysfunction relative to healthy individuals. There are no pharmacokinetic data on tamsulosin in patients with severe hepatic impairment.

Therapeutic Efficacy

Once-daily administration of oral tamsulosin 0.4mg as the commercially available modified-release formulation increased Qmax and improved symptom scores to a greater extent than placebo in 12- and 13-week randomised, double-blind, multicentre studies in patients with lower urinary tract symptoms (LUTS) associated with benign prostatic hyperplasia (BPH). Mean increases in Qmax from baseline were greater with tamsulosin (1.4 to 1.75 ml/sec) than with placebo (0.4 to 0.93 ml/sec), with statistical significance (p < 0.05) between treatment arms being attained in two of three published European and US studies. In two of the three studies, significantly more patients were considered responders (≥30% increase in Qmax) in the tamsulosin 0.4mg once daily groups than in the placebo groups. The decrease (improvement) in total Boyarsky symptom score was significantly greater in all tamsulosin-treated groups (3.0 to 4.8 points) than in placebo recipients (1.9 to 3.2 points; p ≤ 0.002). 55 to 70% of tamsulosin recipients responded with ≥25% improvement in Boyarsky symptom score or International Prostate Symptom Score (IPSS), with these proportions of patients being significantly greater than the 40 to 51% of placebo recipients. Subset analysis has indicated improvements in IPSS with tamsulosin to be at least as great in patients with severe LUTS as in those with moderate symptoms. Tamsulosin 0.4mg once daily had a rapid onset of action in these studies, with a significant (p < 0.001 vs placebo) improvement in mean Qmax from baseline being measurable after the first dose of active treatment in one US study.

Meta-analysis of two randomised, double-blind, placebo-controlled European studies (one of which is published) has shown results similar to those reported for individual US and European trials.

Tamsulosin 0.4mg once daily demonstrated similar improvements in Qmax and total Boyarsky symptom score to those seen with alfuzosin 2.5mg three times daily in the treatment of 245 evaluable patients with LUTS in a double-blind, randomised 12-week study; 35 and 34% of patients in the respective treatment groups achieved increases of at least 30% relative to baseline in Qmax.

Improvements in efficacy parameters with tamsulosin 0.4mg once daily were maintained in long-term studies for up to 4 years, and preliminary pooled data from patients receiving either 0.4 or 0.8mg once daily indicate maintenance of efficacy for up to 6 years.

Tamsulosin was as effective in the treatment of LUTS associated with BPH in patients with diabetes mellitus and in the elderly as in patients without diabetes and in younger individuals in retrospective analyses of data from US placebo-controlled trials and in large observational studies. Six-month noncomparative Spanish data obtained in 2740 patients treated with tamsulosin 0.4mg once daily show reductions in IPSS from baseline of 50 to 56% in both the presence and absence of cardiovascular, neurological, psychiatric or diabetic comorbidities (no statistical analysis available).

Preliminary results suggest that the symptoms of radiation therapy-induced urethritis in patients treated for prostate cancer are improved by tamsulosin treatment. In addition, limited data are available to indicate benefit of tamsulosin in patients with acute urinary retention or chronic abacterial prostatitis, and in patients receiving high energy transurethral microwave thermotherapy.

Tolerability

European prescribing information states that dizziness and abnormal ejaculation have been reported most commonly, with headache, asthenia, postural hypotension and palpitations being seen less frequently (1 to 2% incidence) in patients receiving tamsulosin 0.4mg once daily. US prescribing data indicate that headache, dizziness, rhinitis, infection and abnormal ejaculation are the most common adverse events that are probably related to treatment with tamsulosin 0.4mg once daily. With the exception of dizziness, rhinitis and abnormal ejaculation, adverse events show similar incidences to those with placebo. Similar rates of treatment withdrawal were noted for tamsulosin 0.4mg once daily and placebo groups (8 vs 8.5%) in US studies.

Prescription event monitoring involving 7739 patients being prescribed tamsulosin for at least 6 months showed the most frequently reported adverse events to include dizziness, malaise/lassitude, headache/migraine, impotence/ejaculation failure and hypotension.

Long-term therapy with tamsulosin 0.4mg once daily appears on the basis of 4-year data to be well tolerated; the drug has also shown good tolerability in patients with cardiovascular disease or diabetes mellitus, and in patients receiving concomitant antihypertensive agents such as diuretics, β-blockers, calcium channel antagonists or ACE inhibitors.

According to retrospective clinical trial analysis, incidences of abnormal ejaculation with tamsulosin 0.4mg once daily and placebo were 4.5 and 1%, respectively, although there was no increase in sexual dysfunction in patients receiving tamsulosin. There were no statistically significant differences in the incidences of abnormal ejaculation, decreased libido or impotence, or in change in sexual function score, between patients receiving tamsulosin 0.4mg once daily and those receiving alfuzosin 2.5mg three times daily. Relative to placebo, there was a significant improvement (i.e. decrease) in mean total sexual function score in tamsulosin recipients (+0.49 vs −0.31; p = 0.042), although the baseline score was higher (i.e. worse) in the tamsulosin group than in the placebo group (3.35 vs 2.28). Withdrawal rates associated with sexual dysfunction were low with both placebo (0.5%) and tamsulosin (0.8%).

Tamsulosin is associated with a low risk of orthostatic hypotensive effects in patients with LUTS associated with BPH. In clinical trials, tamsulosin 0.4mg once daily showed no clinically relevant hypotensive effect, whereas alfuzosin 2.5mg three times daily was associated with clinically significant reductions in standing and supine diastolic blood pressure (DBP) in a 12-week double-blind comparison of the two drugs. Furthermore, alfuzosin had significantly greater effects on supine and standing systolic blood pressure (SBP) and DBP in patients aged 65 years and over. There were no significant differences between the two treatments with regard to reductions in SBP and DBP in patients with hypertension.

Dosage and Administration

Tamsulosin is indicated for the treatment of the functional symptoms of BPH. The recommended dosage in Europe is 0.4mg once daily after breakfast.

Dosage adjustments are not required on the basis of age or mild to moderate hepatic impairment/renal dysfunction, but hypotensive adverse effects are likely if tamsulosin is given with other α1-adrenoceptor antagonists. Dosage adjustments are also not necessary in patients receiving theophylline, furosemide, cimetidine, atenolol, enalapril or nifedipine. The presence of diclofenac or warfarin may increase the rate of elimination of tamsulosin, however.

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References

  1. Holtgrewe HL. Current trends in management of men with lower urinary tract symptoms and benign prostatic hyperplasia. Urology 1998; 51Suppl. 4A: 1–7

    Article  PubMed  CAS  Google Scholar 

  2. Khoury S, Cockett A, Aso Y, et al. International consultation on urological diseases: a decade of progress. Prostate 2000; 45: 194–9

    Article  PubMed  CAS  Google Scholar 

  3. Clifford GM, Logie J, Farmer RDT. How do symptoms indicative of BPH progress in real life practice? The UK experience. Eur Urol 2000; 38Suppl. 1: 48–53

    Article  PubMed  Google Scholar 

  4. Jepsen JV, Bruskewitz RC. Comprehensive patient evaluation for benign prostatic hyperplasia. Urology 1998 Apr; 51Suppl. 4A: 13–8

    Article  PubMed  CAS  Google Scholar 

  5. Blaivas JG. Obstructive uropathy in the male. Urol Clin North Am 1996 Aug; 23(3): 373–84

    Article  PubMed  CAS  Google Scholar 

  6. Barry MJ, Cockett ATK, Holtgrewe HL, et al. Relationship of symptoms of prostatism to commonly used physiological and anatomical measures of the severity of benign prostatic hyperplasia. J Urol 1993; 150: 351–8

    PubMed  CAS  Google Scholar 

  7. Chute CG, Panser LA, Girman CJ, et al. The prevalence of prostatism: a population-based survey of urinary symptoms. J Urol 1993 Jul; 150: 85–9

    PubMed  CAS  Google Scholar 

  8. Garraway M, Collins G, Lee R. High prevalence of benign prostatic hypertrophy in the community. Lancet 1991 Aug 24; 338: 469–71

    Article  PubMed  CAS  Google Scholar 

  9. Guess HA, Chute CG, Garraway WM, et al. Similar levels of urological symptoms have similar impact on Scottish and American men — although Scots report less symptoms. J Urol 1993; 150: 1701–5

    PubMed  CAS  Google Scholar 

  10. Sagnier PP, Girman CJ, Garraway M, et al. International comparison of the community prevalence of symptoms of prostatism in four countries. Eur Urol 1996; 29: 15–20

    PubMed  CAS  Google Scholar 

  11. Peters TJ, Donovan JL, Kay HE, et al. The International Continence Society ‘Benign Prostatic Hyperplasia’ Study: the bothersomeness of urinary symptoms. J Urol 1997 Mar; 157: 885–9

    Article  PubMed  CAS  Google Scholar 

  12. Jolleys JV, Donovan JL, Nanchahal K, et al. Urinary symptoms in the community: how bothersome are they? Br J Urol 1994; 74: 551–5

    Article  PubMed  CAS  Google Scholar 

  13. Madsen FA, Bruskewitz RC. Clinical manifestations of benign prostatic hyperplasia. Urol Clin North Am 1995 May; 22(2): 291–8

    PubMed  CAS  Google Scholar 

  14. Boehringer Ingelheim Pharmaceuticals Incorporated. Flomax (tamsulosin HCl): brief summary of prescribing information. Ridgefield, CT: Boehringer Ingelheim Pharmaceuticals Incorporated, 2000

  15. Rossi C, Kortmann BM, Sonke GS, et al. α-Blockade improves symptoms suggestive of bladder outlet obstruction but fails to relieve it. J Urol 2001 Jan; 165: 38–41

    Article  PubMed  CAS  Google Scholar 

  16. Andersson K-E. Mode of action of α1-adrenoreceptor antagonists in the treatment of lower urinary tract symptoms. BJU Int 2000; 85Suppl. 2: 12–8

    Article  PubMed  CAS  Google Scholar 

  17. Michel MC, Schafers RF, Goepel M. α-Blockers and lower urinary tract function: more than smooth muscle relaxation? BJU Int 2000; 86Suppl. 2: 23–30

    PubMed  CAS  Google Scholar 

  18. Chapple CR, Wyndaele JJ, Nordling J, et al. Tamsulosin, the first prostate-selective α1A-adrenoceptor antagonist. A metaanalysis of two randomized, placebo-controlled, multicentre studies in patients with benign prostatic obstruction (symptomatic BPH). Eur Urol 1996; 29: 155–67

    PubMed  CAS  Google Scholar 

  19. Wilde MI, McTavish D. Tamsulosin: a review of its pharmacological properties and therapeutic potential in the management of symptomatic benign prostatic hyperplasia. Drugs 1996; 52: 883–98

    Article  PubMed  CAS  Google Scholar 

  20. Lyseng-Williamson KA, Jarvis B, Wagstaff AJ. Tamsulosin: an update of its role in the management of lower urinary tract symptoms. Drugs 2002; 61(1): 135–67

    Article  Google Scholar 

  21. Chapple CR. Selective α1-adrenoceptor antagonists in benign prostatic hyperplasia: rationale and clinical experience. Eur Urol 1996; 29: 129–44

    PubMed  CAS  Google Scholar 

  22. Michel MC, Büscher R, Kerker J, et al. α1-Adrenoceptor subtype affinities of drugs for the treatment of prostatic hypertrophy: evidence for heterogeneity of chloroethylclonidine-resistantrat renal α1-adrenoceptor. Naunyn Schmiedebergs Arch Pharmacol 1993; 348: 385–95

    PubMed  CAS  Google Scholar 

  23. Foglar R, Shibata K, Horie K, et al. Use of recombinant α1-adrenoceptors to characterize subtype selectivity of drugs for the treatment of prostatic hypertrophy. Eur J Pharmacol Mol Pharmacol 1995; 288: 201–7

    Article  CAS  Google Scholar 

  24. García-Sáinz JA, Romero-Avila MT, Villalobos-Molina R, et al. α1-Adrenoceptor subtype selectivity of tamsulosin: studies using livers from different species. Eur J Pharmacol 1995; 289(1): 1–7

    Article  PubMed  Google Scholar 

  25. Han C, Hollinger S, Theroux TL, et al. 3H-tamsulosin binding to cloned α1-adrenergic receptor subtypes expressed in human embryonic kidney 293 cells: antagonist potencies and sensitivity to alkylating agents. Pharmacol Commun 1995; 5: 117–26

    CAS  Google Scholar 

  26. Michel MC, Insel PA. Comparison of cloned and pharmacologically defined rat tissue α1-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol 1994; 350: 136–42

    PubMed  CAS  Google Scholar 

  27. Richardson CD, Donatucci CF, Page SO, et al. Pharmacology of tamsulosin: saturation-binding isotherms and competition analysis using cloned α1-adrenergic receptor subtypes. Prostate 1997; 33: 55–9

    Article  PubMed  CAS  Google Scholar 

  28. Michel MC, Grübbel B, Taguchi K, et al. Drugs for treatment of benign prostatic hyperplasia: affinity comparison at cloned α1-adrenoceptor subtypes and in human prostate. J Auton Pharmacol 1996; 16: 21–8

    Article  PubMed  CAS  Google Scholar 

  29. Puppo P. Do we know everything about alpha-blockade in the management of lower urinary tract symptoms? Eur Urol 2001 Jan; 39Suppl. 2: 38–41

    Article  PubMed  Google Scholar 

  30. Schwinn DA, Michelotti GA. α1-adrenergic receptors in the lower urinary tract and vascular bed: potential role for the α1d subtype in filling symptoms and effects of ageing on vascular expression. BJU Int 2000; 85Suppl. 2: 6–11

    Article  PubMed  CAS  Google Scholar 

  31. Malloy BJ, Price DT, Price RR, et al. α1-Adrenergic receptor subtypes in human detrusor. J Urol 1998; 160: 937–43

    Article  PubMed  CAS  Google Scholar 

  32. Smith MS, Schambra UB, Wilson KH, et al. α1-Adrenergic receptors in human spinalcord: specific localized expression of mRNA encoding α1-adrenergic receptor subtypes at four distinct levels. Mol Brain Res 1999; 63: 254–61

    Article  PubMed  CAS  Google Scholar 

  33. Harada K, Ohmori M, Kitoh Y, et al. A comparison of the antagonistic activities of tamsulosin and terazosin against human vascular α1-adrenoceptors. Jpn J Pharmacol 1999; 80: 209–15

    Article  PubMed  CAS  Google Scholar 

  34. Harada K, Ohmori M, Fujimura A. Comparison of the antagonistic activity of tamsulosin and doxazosin at vascular α1-adrenoceptors in humans. Naunyn Schmiedebergs Arch Pharmacol 1996; 354: 557–61

    Article  PubMed  CAS  Google Scholar 

  35. Harada K, Kawaguchi A, Ohmori M, et al. Antagonistic activity of tamsulosin against human vascular α1-adrenergic receptors. Clin Pharmacol Ther 2000; 67: 405–12

    Article  PubMed  CAS  Google Scholar 

  36. Yamada S, Tanaka C, Kimura R, et al. Alpha1-adrenoceptors in human prostate: characterization and binding characteristics of alpha1-antagonists. Life Sci 1994; 54: 1845–54

    Article  PubMed  CAS  Google Scholar 

  37. Taguchi K, Schäfers RF, Michel MC. Radioreceptor assay analysis of tamsulosin and terazosin pharmacokinetics. Br J Clin Pharmacol 1998; 45: 49–55

    Article  PubMed  CAS  Google Scholar 

  38. Chapple CR. α-Adrenergic blocking drugs in bladder outflow obstruction: what potential has α1-adrenergic selectivity? Br J Urol 1995; 76: 47–55

    PubMed  Google Scholar 

  39. Yamada S, Suzuki M, Tanaka C, et al. Comparative study on α1-adrenoceptor antagonist binding in human prostate and aorta. Clin Exp Pharmacol Physiol 1994; 21: 405–11

    Article  PubMed  CAS  Google Scholar 

  40. Testa R, Poggesi E, Taddei C, et al. REC 15/2739, a new α1-antagonist selective for the lower urinary tract: in vitro studies. Neurourol Urodyn 1994; 13(4): 473–4

    Google Scholar 

  41. Noble AJ, Chess-Williams R, Couldwell C, et al. The effects of tamsulosin, a high affinity antagonist at functional α1- and α1D-adrenoceptor subtypes. Br J Pharmacol 1997; 120: 231–8

    Article  PubMed  CAS  Google Scholar 

  42. Davis BJ, Noble A, Chapple CR, et al. Human prostate-artery selectivity of tamsulosin, doxazosin and alfuzosin. Br J Pharmacol 2000; 129 Suppl.: 52P

    Google Scholar 

  43. Ohkura T, Yamada S, Deguchi Y, et al. Ex vivo occupancy by tamsulosin of α1-adrenoceptors in rat tissues in relation to the plasma concentration. Life Sci 1998; 63: 2147–55

    Article  PubMed  CAS  Google Scholar 

  44. Yamada S, Ohkura T, Deguchi Y, et al. In vivo measurement by [3H]tamsulosin of α1 adrenoceptors in rat tissues in relation to the pharmacokinetics. J Pharmacol Exp Ther 1999; 289: 1575–83

    PubMed  CAS  Google Scholar 

  45. Sironi D, Levorate CA, Deiana G, et al. The use of ultrasound estimated bladder weight (UEBW) in evaluation of change in bladder hypertrophy during treatment with an α1 blocker. Eur Urol 2000; 37Suppl. 2: 103

    Google Scholar 

  46. Schäfers RF, Fokuhl B, Wasmuth A, et al. Differential vascular α1-adrenoceptor antagonism by tamsulosin and terazosin. Br J Clin Pharmacol 1999; 47: 67–74

    Article  PubMed  Google Scholar 

  47. de Mey C, Michel MC, McEwen J, et al. A double-blind comparison of terazosin and tamsulosin on their differential effects on ambulatory blood pressure and nocturnal orthostatic stress testing. Eur Urol 1998; 33: 481–8

    Article  PubMed  Google Scholar 

  48. Denis L, Ziekenhuis M. Tamsulosin: effect on PSA levels in 3-month placebo-controlled studies and long-term follow-up of these studies. European Tamsulosin Study Group [abstract no. abstract]. Br J Urol 1997 Sep; 80Suppl. 2: 212

    Google Scholar 

  49. Yamanouchi Pharmaceutical Co. Ltd. Harnal® capsules 0.1 mg. Harnal® capsules 0.2 mg. Tokyo: Yamanouchi Pharmaceutical Co. Ltd, 2000 Jan

    Google Scholar 

  50. Wolzt M, Fabrizii V, Dorner GT, et al. Pharmacokinetics of tamsulosin in subjects with normal and varying degrees of impaired renal function: an open-label single-dose and multiple-dose study. Eur J Clin Pharmacol 1998; 54: 367–73

    Article  PubMed  CAS  Google Scholar 

  51. Matsushima H, Kamimura H, Soeishi Y, et al. Pharmacokinetics and plasma protein binding of tamsulosin hydrochloride in rats, dogs, and humans. Drug Metab Dispos 1998; 26: 240–5

    PubMed  CAS  Google Scholar 

  52. van-Hoogdalem EJ, Soeishi Y, Matsushima H, et al. Disposition of the selective α1A-adrenoceptor antagonist tamsulosin in humans: comparison with data from interspecies scaling. J Pharm Sci 1997; 86: 1156–61

    Article  PubMed  CAS  Google Scholar 

  53. Yamanouchi Europe BV. Tamsulosin: summary of product characteristics (SmPC). Leiderdorp, The Netherlands: Yamanouchi Europe BV, 1998 May 27

    Google Scholar 

  54. Soeishi Y, Matsushima H, Watanabe T, et al. Absorption, metabolism and excretion of tamsulosin hydrochloride in man. Xenobiotica 1996; 26: 637–45

    Article  PubMed  CAS  Google Scholar 

  55. Kamimura H, Oishi S, Matsushima H, et al. Identification of cytochrome P450 isozymes involved in metabolism of the α1-adrenoceptor blocker tamsulosin in human liver microsomes. Xenobiotica 1998; 28: 909–22

    Article  PubMed  CAS  Google Scholar 

  56. Miyazawa Y, Blum RA, Schentag JJ, et al. Pharmacokinetics and safety of tamsulosin in subjects with normal and impaired renal or hepatic function. Curr Ther Res 2001; 62(5): 603–21

    Article  CAS  Google Scholar 

  57. Flomax. In: Gillis MC, Welbanks L, Bergeron D, et al, editors. CPS compendium of pharmaceuticals and specialties 1999. 34th ed. Ottawa: Canadian Pharmacists Association, 1999: 669–71

  58. Miyazawa Y, Starkey LP, Forrest A, et al. Effects of the concomitant administration of tamsulosin (0.8 mg) on the pharmacokinetic and safety profile of intravenous digoxin (Lanoxin) in normal healthy subjects: a placebo-controlled evaluation. Tokyo, Japan: Yamanouchi Pharmaceutical Co. Ltd, 2001

    Google Scholar 

  59. Miyazawa Y, Starkey LP, Forrest A, et al. Effects of the concomitant administration of tamsulosin (0.8 mg/day) on the pharmacokinetic and safety profile of theophylline (5 mg/kg): a placebo-controlled evaluation. Tokyo: Yamanouchi Pharmaceutical Co. Ltd, 2001

    Google Scholar 

  60. Abrams P, Schulman CC, Vaage S, et al. Tamsulosin, a selective α1c-adrenoceptor antagonist: a randomized, controlled trial in patients with benign prostatic ‘obstruction’ (symptomatic BPH). European Tamsulosin Study Group. Br J Urol 1995; 76: 325–36

    Article  PubMed  CAS  Google Scholar 

  61. Narayan P, Tewari A. A second phase III multicenter placebo controlled study of 2 dosages of modified release tamsulosin in patients with symptoms of benign prostatic hyperplasia. United States 93-01 Study Group. J Urol 1998; 160: 1701–6

    Article  PubMed  CAS  Google Scholar 

  62. Lepor H. Phase III multicenter placebo-controlled study of tamsulosin in benign prostatic hyperplasia. Tamsulosin Investigator Group. Urology 1998; 51: 892–900

    Article  PubMed  CAS  Google Scholar 

  63. Narayan P, Lepor H. Long-term, open-label, phase III multicenter study of tamsulosin in benign prostatic hyperplasia. Urology 2001 Mar; 57(3): 466–70

    Article  PubMed  CAS  Google Scholar 

  64. Lepor H. Long-term evaluation of tamsulosin in benign prostatic hyperplasia: placebo-controlled, double-blind extension of phase III trial. Tamsulosin Investigator Group. Urology 1998; 51: 901–6

    Article  PubMed  CAS  Google Scholar 

  65. Schulman CC, Lock TMT, Buzelin J-M, et al. Long-term use of tamsulosin to treat lower urinary tract symptoms/benign prostatic hyperplasia. Urology 2001 Oct; 166: 1358–63

    Article  CAS  Google Scholar 

  66. Narayan P, Ranhosky A, Doyle CA. Long-term efficacy of tamsulosin: results of a 6-year experience. J Urol 2001 May; 165 Suppl.: 381

    Google Scholar 

  67. Schulman CC, Cortvriend J, Jonas U, et al. Tamsulosin, the first prostate-selective α1A-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). Eur Urol 1996; 29: 145–54

    PubMed  CAS  Google Scholar 

  68. Kawabe K, Ueno A, Takimoto Y, et al. Use of an α1-blocker, YM617, in the treatment of benign prostatic hypertrophy. J Urol 1990; 144: 908–12

    PubMed  CAS  Google Scholar 

  69. Buzelin JM, Fonteyne E, Kontturi M, et al. Comparison of tamsulosin with alfuzosin in the treatment of patients with lower urinary tract symptoms suggestive of bladder outlet obstruction (symptomatic benign prostatic hyperplasia). European Tamsulosin Study Group. Br J Urol 1997; 80: 597–605

    Article  PubMed  CAS  Google Scholar 

  70. Michel MC, Mehlburger L, Schumacher H, et al. Effect of diabetes on lower urinary tract symptoms in patients with benign prostatic hyperplasia. J Urol 2000; 163: 1725–9

    Article  PubMed  CAS  Google Scholar 

  71. Batista JF, Palacio A, Torrubia R, et al. Tamsulosin: does comorbidity affect outcomes? [abstract no. P1.4.12] BJU Int 2000 Nov; 86: 30

    Google Scholar 

  72. Michel MC, Mehlburger L, Bressel H-U, et al. Comparison of tamsulosin efficacy in subgroups of patients with lower urinary tract symptoms. Prostate Cancer Prostatic Dis 1998; 1: 332–5

    Article  PubMed  CAS  Google Scholar 

  73. Brooks SK. Effect of tamsulosin on AUA symptom score and BPH impact index as a function of symptom severity in patients with benign prostatic hyperplasia. J Urol 1999 Apr; 161 Suppl.: 267

    Article  Google Scholar 

  74. Prosnitz RG, Schneider L, Manola J, et al. Tamsulosin palliates radiation-induced urethritis in patients with prostate cancer: results of a pilot study. Int J Radiat Oncol Biol Phys 1999; 45: 563–6

    Article  PubMed  CAS  Google Scholar 

  75. Merrick GS, Butler WM, Lief JH, et al. Temporal resolution of urinary morbidity following prostate brachytherapy. Int J Radiat Oncol Biol Phys 2000; 47(1): 121–8

    Article  PubMed  CAS  Google Scholar 

  76. De Mey C. α1-Blocker therapy for lower urinary tract symptoms suggestive of benign prostatic obstruction: what are the relevant differences in randomised controlled trials? Eur Urol 2000; 38Suppl. 1: 25–39

    Article  PubMed  Google Scholar 

  77. Narayan P, Bruskewitz R. A comparison of two phase III multicenter, placebo-controlled studies of tamsulosin in BPH. Adv Ther 2000 Nov-2000 31; 17(6): 287–300

    Article  PubMed  CAS  Google Scholar 

  78. Abrams P, Speakman M, Stott M, et al. A dose-ranging study of the efficacy and safety of tamsulosin, the first prostate-selective α1A-adrenoceptor antagonist, in patients with benign prostatic obstruction (symptomatic benign prostatic hyperplasia). Br J Urol 1997; 80: 587–96

    Article  PubMed  CAS  Google Scholar 

  79. Arnold EP. Tamsulosin in men with confirmed bladder outlet obstruction: a clinical and urodynamic analysis from a single centre in New Zealand. BJU Int 2001 Jan; 87(1): 24–30

    Article  PubMed  CAS  Google Scholar 

  80. Lowe FC. Efficacy and tolerability of tamsulosin in patients <65 years and ≥65 years with benign prostatic hyperplasia. J Urol 1999; 161 (4 Suppl.): 267

    Article  Google Scholar 

  81. Lee WR, McQuellon RP, Case LD, et al. Early quality of life assessment in men treated with permanent source interstitial brachytherapy for clinically localized prostate cancer. J Urol 1999; 162: 403–6

    Article  PubMed  CAS  Google Scholar 

  82. Wallner K, Roy J, Harrrison L. Tumor control and morbidity following transperineal iodine 125 implantation for stage T1/T2 prostatic carcinoma. J Clin Oncol 1996; 14(2): 449–53

    PubMed  CAS  Google Scholar 

  83. Choong S, Emberton M. Acute urinary retention. BJU Int 2000; 85: 186–201

    Article  PubMed  CAS  Google Scholar 

  84. McNeill SA. Does acute urinary retention respond to alphablockers alone? Eur Urol 2001; 39Suppl. 6: 7–12

    Article  PubMed  CAS  Google Scholar 

  85. Kim HL, Kim JC, Benson DA, et al. Results of treatment with tamsulosin in men with acute urinary retention. Tech Urol 2001; 7(4): 256–60

    PubMed  CAS  Google Scholar 

  86. McNaughton Collins M, MacDonald R, Wilt TJ. Diagnosis and treatment of chronic abacterial prostatitis: a systematic review. Ann Intern Med 2000; 133: 367–81

    PubMed  CAS  Google Scholar 

  87. Stevermer JJ, Easley SK. Treatment of prostatitis. Am Fam Physician 2000; 61(10): 3015–22, 3025-6

    PubMed  CAS  Google Scholar 

  88. Lacquaniti S, Destito A, Servello C, et al. Terazosine and tamsulosin in non bacterial prostatitis: a randomized placebo-controlled study. Arch Ital Urol Androl 1999; 71(5): 283–5

    PubMed  CAS  Google Scholar 

  89. Neal Jr DE, Moon TD. Use of terazosin in prostatodynia and validation of symptom score questionnaire. Urology 1994; 43(4): 460–5

    Article  PubMed  Google Scholar 

  90. Tkachuk VN, Al-Shukri SKh, Kuznetsova MI, et al. Tamsulosin in the treatment of patients with chronic prostatitis [in Russian]. Urol Nefrol (Mosk) 2000 Sep-2000 31; (5): 18–20

    Google Scholar 

  91. Djavan B, Shariat S, Fakhari M, et al. Neoadjuvant and adjuvant α-blockade improves early results of high-energy transurethral microwave thermotherapy for lower urinary tract symptoms of benign prostatic hyperplasia: a randomized, prospective clinical trial. Urology 1999; 53(2): 251–9

    Article  PubMed  CAS  Google Scholar 

  92. Mann RD, Biswas P, Freemantle S, et al. The pharmacovigilance of tamsulosin: event data on 12 484 patients. BJU Int 2000; 85: 446–50

    Article  PubMed  CAS  Google Scholar 

  93. Michel MC, Mehlburger L, Bressel H-U, et al. Tamsulosin treatment of 19,365 patients with lower urinary tract symptoms: does comorbidity alter tolerability? J Urol 1998 May; 159 Suppl.: 257

    Google Scholar 

  94. Michel MC, Bressel H-U, Goepel M, et al. A 6-month large-scale study into the safety of tamsulosin. Br J Clin Pharmacol 2001; 51: 609–14

    Article  PubMed  CAS  Google Scholar 

  95. Höfner K, Claes H, De Reijke TM, et al. Tamsulosin 0.4 mg once daily: effect on sexual function in patients with lower urinary tract symptoms suggestive of benign prostatic obstruction. Eur Urol 1999; 36: 335–41

    Article  PubMed  Google Scholar 

  96. Yasukawa K, Swarz H, Ito Y. Review of orthostatic tests on the safety of tamsulosin, a selective α1A-adrenergic receptor antagonist, shows lack of orthostatic hypotensive effects. J Int Med Res 2001; 29: 236–51

    PubMed  CAS  Google Scholar 

  97. Michel MC, Bressel H-U, Mehlburger L, et al. Tamsulosin: real life clinical experience in 19,365 patients. Eur Urol 1998; 34Suppl. 2: 37–45

    Article  PubMed  CAS  Google Scholar 

  98. McConnell JD, Barry MJ, Bruskewitz RC, et al. Benign Prostatic hyperplasia: diagnosis and treatment. Clinical Practice Guidelines No. 8. Rockville, MD: Agency for Health Care Policy and Research, Public Health Service, US Dept. of Health and Human Services, 1994

    Google Scholar 

  99. Roehrborn CG. The Agency for Health Care Policy and Research. Clinical guidelines for the diagnosis and treatment of benign prostatic prostatic hyperplasia. Urol Clin North Am 1995 May; 22(2): 445–53

    PubMed  CAS  Google Scholar 

  100. Beduschi R, Beduschi MC, Oesterling JE. Benign prostatic hyperplasia: use of drug therapy in primary care. Geriatrics 1998; 53: 24–8,33-4,37-40

    PubMed  CAS  Google Scholar 

  101. Chapple CR. Real-life experience in lower urinary tract symptom management. Drugs Today 2001; 37Suppl. D: 47–9

    Google Scholar 

  102. Tammela T. Benign prostatic hyperplasia: practical treatment guidelines. Drugs Aging 1997; 10: 349–66

    Article  PubMed  CAS  Google Scholar 

  103. Fowler Jr FJ, Wennberg JE, Timothy RP, et al. Symptom status and quality of life following prostatectomy. JAMA 1988; 259: 3018–22

    Article  PubMed  Google Scholar 

  104. Roberts RG. BPH: new guidelines based on symptoms and patient preference. Geriatrics 1994 Jul; 49(7): 24–31

    PubMed  CAS  Google Scholar 

  105. Borboroglu PG, Kane CJ, Ward JF, et al. Immediate and postoperative complications of transurethral prostatectomy in the 1990s. J Urol 2000; 162(4): 1307–10

    Article  Google Scholar 

  106. Bruskewitz RC, Larsen EH, Madsen PO, et al. 3-Year followup of urinary symptoms after transurethral resection of the prostate. J Urol 1986; 136: 613–5

    PubMed  CAS  Google Scholar 

  107. Cooper KL, McKiernan JM, Kaplan SA. α-Adrenoceptor antagonists in the treatment of benign prostatic hyperplasia. Drugs 1999; 57: 9–17

    Article  PubMed  CAS  Google Scholar 

  108. Boyle P, Gould L, Roehrborn CG. Prostate volume predicts outcome of treatment of benign prostatic hyperplasia with finasteride: meta-analysis of randomized clinical trials. Urology 1996; 48: 398–405

    Article  PubMed  CAS  Google Scholar 

  109. Lieber MM. Pharmacologic therapy for prostatism. Mayo Clin Proc 1998; 73: 590–6

    Article  PubMed  CAS  Google Scholar 

  110. Berges RR, Windeler J, Trampisch HJ, et al. Randomised placebo-controlled, double-blind clinical trial of ß-sitosterol in patients with benign prostatic hyperplasia. Lancet 1995; 29: 231–40

    Google Scholar 

  111. Carraro J-C, Raynaud J-P, Koch G, et al. Comparison of phytotherapy (Permixon) with finasteride in the treatment of benign prostate hyperplasia: a randomized international study of 1,098 patients. Prostate 1996; 29: 231–40

    Article  PubMed  Google Scholar 

  112. Coulange C, Glémain P, Wetzel O, et al. What’s the benefit of combining tamsulosin with Serenoa repens? J Urol 2001 May; 165 Suppl.: 261–2

    Google Scholar 

  113. Bruskewitz R. Management of symptomatic BPH in the US: who is treated and how? Eur Urol 1999; 36Suppl. 3: 7–13

    Article  PubMed  Google Scholar 

  114. Gormley GJ, Stoner E, Bruskewitz RC, et al. The effect of finasteride in men with benign prostatic hyperplasia. N Engl J Med 1992; 327: 1185–91

    Article  PubMed  CAS  Google Scholar 

  115. Kirby R, Boyle P, Roehrborn C, et al. Results of the PREDICT (Prospective Randomised European Doxazosin and Combination) Study of medical therapy for BPH. Br J Urol 1999; 83Suppl. 4: 5

    Google Scholar 

  116. Debruyne F, Jardin A, Colloi D, et al. Sustained-release alfuzosin, finasteride and the combination of both in the treatment of benign prostatic hyperplasia. Eur Urol 1998; 34: 169–75

    Article  PubMed  CAS  Google Scholar 

  117. Lepor H, Williford WO, Barry MJ. The efficacy of terazosin, finasteride, or both in benign prostatic hyperplasia. N Engl J Med 1996 Aug 22; 335(8): 533–9

    Article  PubMed  CAS  Google Scholar 

  118. Djavan B, Marberger M. A meta-analysis on the efficacy and tolerability of α1-adrenoceptor antagonists in patients with lower urinary tract symptoms suggestive of benign prostatic obstruction. Eur Urol 1999; 36: 1–13

    Article  PubMed  CAS  Google Scholar 

  119. van Kerrebroeck P, Jardin A, Laval KU, et al. Efficacy and safety of a new prolonged release formulation of alfuzosin 10 mg once daily versus alfuzosin 2.5 mg thrice daily and placebo in patients with symptomatic benign prostatic hyperplasia. Eur Urol 2000; 37: 306–13

    Article  PubMed  Google Scholar 

  120. Roehrborn CG. Efficacy and safety of once-daily alfuzosin in the treatment of lower urinary tract symptoms and clinical benign prostatic hyperplasia: a randomized, placebo-controlled trial. Alfus Study Group. Urology 2001; 58: 953–9

    Article  PubMed  CAS  Google Scholar 

  121. Debruyne FM. Alpha blockers: are all created equal? Urology 2000 Nov 1; 56Suppl. 5A: 20–2

    Article  PubMed  CAS  Google Scholar 

  122. Tewari A, Narayan P. Alpha-adrenergic blocking drugs in the management of benign prostatic hyperplasia: interactions with antihypertensive therapy. Urology 1999; 53Suppl. 3A: 14–20

    Article  PubMed  CAS  Google Scholar 

  123. Michel MC, Flannery MT, Narayan P. Worldwide experience with alfuzosin and tamsulosin. Urology 2001; 58: 508–16

    Article  PubMed  CAS  Google Scholar 

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    Christopher J. Dunn, Anna Matheson & Diana M. Faulds

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Dunn, C.J., Matheson, A. & Faulds, D.M. Tamsulosin. Drugs & Aging 19, 135–161 (2002). https://doi.org/10.2165/00002512-200219020-00004

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