AN 1999404642 19991210. TI Subtype selective alpha1-adrenoceptor antagonists for the treatment of benign prostatic hyperplasia. AU Forray-C, Noble-S-A. IN C. Forray, Synaptic Pharmaceutical Corporation, Paramus, NJ 07652, United States. SO Expert Opinion on Investigational Drugs {EXPERT-OPIN-INVEST-DRUGS}, 1999, Vol/Iss/Pg. 8/12 (2073-2094), ISSN: 1354-3784. CD EOIDE. CP United Kingdom. YR 1999. LG ENGLISH. LS ENGLISH. MF Synthelabo; Smith Kline Beecham; Recordati; Glaxo; Kissei, Japan; Hoffmann La Roche; Pfizer; Ortho. TN sl 890591; rec 15 2739; gw 1818; kmd 3213; rs 100975; a 131701; snap 6201; snap 6991; l 757464; jth 601. DE Medical: prostate-hypertrophy*/drug therapy, surgery; micturition; quality-of-life; drug-efficacy; adrenergic-activity; vascular-smooth-muscle; side-effect/side effect; receptor-blocking; molecular-cloning; receptor-gene; smooth-muscle-contraction; pharmacodynamics; vertigo/side effect; muscle-weakness/side effect; fatigue/side effect; heart-palpitation/side effect; syncope/side effect; ejaculation; rhinitis/side effect; orthostatic-hypotension/side effect; human; nonhuman; male; intravenous-drug-administration; review. Drug: alpha-1-adrenergic-receptor-blocking-agent*/adverse drug reaction, drug therapy, pharmacology; alfuzosin/adverse drug reaction, clinical trial, drug therapy, pharmacology; terazosin/adverse drug reaction, clinical trial, drug therapy, pharmacology; doxazosin/adverse drug reaction, clinical trial, drug therapy, pharmacology; tamsulosin/adverse drug reaction, clinical trial, drug therapy, pharmacology; steroid-5alpha-reductase-inhibitor/drug therapy; phenoxybenzamine/adverse drug reaction, drug therapy; sl-890591+/drug development; 3-(2-(2,3,3a,4,5,9b-hexahydro-6-methoxy-1h-benz(e)isoindol-2-yl)ethyl) pyrido(3',4'-4,5)thieno(3,2-d)pyrimidine-2,4(1h,3h)-dione+/drug development; 8-(3-(4-(2-methoxyphenyl)-1-piperazinyl)propylcarbamoyl)-3- methylflavone/drug development; snap-6201+/drug development; snap-6991+/drug development; l-757464+/drug development; gw-1818+/drug development; kmd-3213+/drug development; rs-100975+/drug development; 3-(n-(2-(4-hydroxy-2-isopropyl-5-methylphenoxy)ethyl)-n- methylaminomethyl)-4-methoxy-2,5,6-trimethylphenol-hemifumarate+/drug development. SH 028 Urology and nephrology; 030 Clinical and experimental pharmacology; 037 Drug literature; 038 Adverse reaction titles. AB Benign prostatic hyperplasia (BPH) is highly prevalent in the male population beyond the age of 60. Impairment of urinary flow due to prostate enlargement gives rise to symptoms of 'prostatism' that have a detrimental impact on the quality of life. The current trend in the management of symptomatic BPH favours pharmacotherapy as a first line option, while the number of surgical procedures being performed has experienced a steady decline during the last ten years. Among the pharmacological treatments, the use of alpha1-adrenoceptor blockers has demonstrated to be an effective treatment option for BPH. These agents reduce the adrenergic tone to the prostate and increase urinary flow, with a concomitant reduction of lower urinary tract symptoms. The alpha1-blockers currently approved include compounds such as alfuzosin, terazosin and doxazosin, originally developed for the treatment of hypertension, and more recently tamsulosin an alpha1- subtype selective drug. The blockade of alpha1-adrenoceptors present in vascular smooth muscle is largely responsible for the most prominent side effects of current drugs, which can be severe and require patients dose titration. The limitation imposed by side effects naturally raises the possibility that complete blockade of prostatic alpha1 receptors is not attained at the maximum tolerated dose. The extensive efforts by the pharmaceutical industry towards the development of uroselective alpha1-blockers, is the subject of this review. Advances in the molecular cloning of genes encoding three alpha1-adrenoceptors led to the identification of the alpha1A-subtype as the predominant receptor responsible fur the contraction of prostate smooth muscle. In preclinical animal models, selective alpha1A-antagonists have consistently been found to have minimal cardiovascular effects, thus providing a pharmacological rationale for uroselectivity. It has also become apparent, however, that uroselectivity can emerge in a poorly understood manner from the pharmacodynamic properties of compounds without alpha1A-subtype selectivity. Clinical experience with tamsulosin, an alpha1A/alpha1D selective drug, has failed to demonstrate a significant improvement in efficacy beyond that demonstrated for non-subtype selective alpha1- blockers, and gives support to the notion that alpha1A-selective antagonists might achieve greater efficacy for the treatment of BPH. Given the demonstrated uroselectivity of alpha1A-selective antagonists in preclinical models, it is anticipated that third generation alpha1- blockers will exhibit improved urinary flow efficacy and be better tolerated than tamsulosin. The extent to which the improvement in urinary flow will translate to the relief of symptoms of prostatism, however, remains to be demonstrated in randomised placebo-controlled clinical trials of alpha1A-selective antagonists. RN alfuzosin 81403-80-7; terazosin 63074-08-8 63590-64-7; doxazosin 74191-85-8; tamsulosin 80223-99-0; phenoxybenzamine 59-96-1 63-92-3; 8-[3-[4-(2-methoxyphenyl)-1-piperazinyl! propylcarbamoyl!-3- methylflavone 152735-23-4. NU 216 References. PT J Journal. AT Review. AN 1999234068 19990722. TI BPH and sexuality. AU Zlotta-A-R, Schulman-C-C. IN Dr. A.R. Zlotta, Department of Urology, University Clinics of Brussels, Route de Lennik 808, B-1070 Brussels, Belgium. SO European Urology {EUR-UROL}, 1999, Vol/Iss/Pg. 36/SUPPL. 1 (107-112), ISSN: 0302-2838. CD EUURA. CP Switzerland. YR 1999. LG ENGLISH. LS ENGLISH. DE Medical: prostate-hypertrophy*/drug therapy, surgery, therapy; sexuality*; quality-of-life; sexual-function; side-effect/side effect; impotence/side effect; transurethral-resection; laser-surgery; transurethral-microwave-thermotherapy; transurethral-electrovaporization; human; male; clinical-trial; meta-analysis; conference-paper; priority-journal. Drug: finasteride/adverse drug reaction, drug comparison, drug therapy, pharmacokinetics; plant-extract/drug comparison, drug dose, drug therapy, pharmacokinetics; sabal/drug comparison, drug dose, drug therapy, pharmacokinetics; alpha-adrenergic-receptor-blocking-agent/adverse drug reaction, drug dose, drug therapy, pharmacokinetics; alfuzosin/adverse drug reaction, drug dose, drug therapy, pharmacokinetics; terazosin/adverse drug reaction, drug dose, drug therapy, pharmacokinetics; tamsulosin/adverse drug reaction, drug dose, drug therapy, pharmacokinetics; doxazosin/adverse drug reaction, drug dose, drug therapy, pharmacokinetics. SH 006 Internal medicine; 010 Obstetrics and gynecology; 028 Urology and nephrology; 037 Drug literature; 038 Adverse reaction titles. AB Quality of life has become a very important parameter in benign prostatic hyperplasia (BPH) and one of the major concepts identified by the patients to be important is related to sexuality after BPH therapy. The impact on sexuality resulting from the various treatment modalities of BPH, either medical, surgical or instrumental has been too often neglected in the past and poorly investigated. The present article reviews the influence on sexual function of current therapies for symptomatic BPH. RN finasteride 98319-26-7; alfuzosin 81403-80-7; terazosin 63074-08-8 63590-64-7; tamsulosin 80223-99-0; doxazosin 74191-85-8. NU 37 References. PT J Journal. AT Conference Paper.