α1-Rezeptorenblockade zur Therapie des BPH-Syndroms Richtige Dosierung für optimale Wirkung

Berges, Richard; Michel, Marion; Jonas, Udo

doi:10.1007/s00120-001-0151-5

Cited by 4 publications

(2 citation statements)

References 14 publications

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“…It was found that niguldipine is a potent antagonist for α 1 -AR with a 100-fold selectivity increase for α 1a -AR versus the other α 1 -AR subtypes. Several modifications yielded compound (13) [pK i 9.63 (α 1a ), 7.87 (α 1b ) and 7.18 (α 1d )] with preserved potency and selectivity for α 1a -AR but attenuated calcium channel activity. One significant drawback of compound (13), however, is its poor oral bioavailability in rats (5%), which may be due to the oxidative metabolic conversion of the dihydropyridine moiety into a pyridine [8,29] (Fig.…”

Section: Piperidinesmentioning

confidence: 99%

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Trends in the Development of New Drugs for Treatment of Benign Prostatic Hyperplasia

Kulig¹,

Malawska

2006

CMC

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Benign prostatic hyperplasia (BPH) is a common condition in aging men that is characterized by nonmalignant enlargement of the prostate gland, and is frequently accompanied by urinary obstruction, and lower urinary tract symptoms (LUST). Currently pharmacotherapy of BPH is based on two classes of drugs: alpha(1)-adrenoceptor (alpha(1)-AR) antagonists and 5alpha-reductase inhibitors. It has been shown that alpha(1)-AR antagonists reduce symptom scores and increase peak urinary flow rates in BPH. Of particular importance for BPH therapy are uroselective alpha(1)-AR antagonists for which the hypotensive related side-effect caused by alpha(1)-AR blockade is reduced. 5alpha-Reductase inhibitors reduce prostate volume and symptom scores, while increasing peak urinary flow rates. This review describes new alpha(1)-AR antagonists and 5alpha-reductase inhibitors in the treatment of BPH. The new alpha(1)-AR antagonists represent various structures such as quinazolines, phenylethylamines, piperidines, and arylpiperazines. 5alpha-Reductase inhibitors are classified into two groups: steroidal and non-steroidal. The newer non-steroidal inhibitors include derivatives of benzo[c]quinolizinones, benzo[f]quinolonones, piperidones and carboxylic acids. Besides the development of new compounds belonging to the above mentioned groups, new agents for BPH treatment are sought among combined 5alpha-reductase/alpha(1)-AR inhibitors, endothelins, androgen receptors antagonists, growth factors, estrogens and phosphodiesterase isoenzymes as well as several phytomedicines, used for prevention and treatment of prostate disorders. These new agents can be used for the design of future targets and development of new drugs in the treatment of BPH. The discovery of a number of active leads may also ultimately help in developing new safe and effective drugs.

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Section: Piperidinesmentioning

confidence: 99%

“…(1)). The α 1 -AR antagonists act on the dynamic component of bladder outlet obstruction, presumably by affecting the contraction of prostate and urethral smooth muscle produced by sympathetic nerve stimulation [11][12][13].…”

Section: Introductionmentioning

confidence: 99%

Trends in the Development of New Drugs for Treatment of Benign Prostatic Hyperplasia

Kulig¹,

Malawska

2006

CMC

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Pharmakologische Therapie des benignen Prostatasyndroms

Oelke¹,

Berges²,

Rosette³

2005

Pharmakotherapie in Der Urologie

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Medikamentöse BPS-Therapie

Berges¹,

Höfner

2005

Urologe [A]

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5alpha-Reductase inhibitors and alpha(1)-receptor blockers are established options for symptomatic treatment of benign prostatic hyperplasia (BPH). Achieving maximum efficacy is contingent on correct dosage and requires careful patient selection in view of the substance class employed. All applicable preparations exert only a low-grade effect on prostatic obstruction. This condition should be excluded by appropriate urological examination before treatment is initiated. If the patient's distress is minor, refraining from drug therapy can be considered. Symptomatic patients with small prostate volume are suited for monotherapy with alpha(1)-receptor blockers and symptomatic patients with large prostate volume profit from combination therapy. When 5alpha-reductase inhibitors are used, BPH patients should be made aware of the findings from the Prostate Cancer Prevention Trial.

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α1-Rezeptorenblockade zur Therapie des BPH-Syndroms Richtige Dosierung für optimale Wirkung

Cited by 4 publications

References 14 publications

Trends in the Development of New Drugs for Treatment of Benign Prostatic Hyperplasia

Trends in the Development of New Drugs for Treatment of Benign Prostatic Hyperplasia

Pharmakologische Therapie des benignen Prostatasyndroms

Medikamentöse BPS-Therapie

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