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WO2005018528A2 - Procédé de traitement, de prophylaxie et de diagnostic différentiel de la prostatite - Google Patents

Procédé de traitement, de prophylaxie et de diagnostic différentiel de la prostatite Download PDF

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Publication number
WO2005018528A2
WO2005018528A2 PCT/EP2004/009005 EP2004009005W WO2005018528A2 WO 2005018528 A2 WO2005018528 A2 WO 2005018528A2 EP 2004009005 W EP2004009005 W EP 2004009005W WO 2005018528 A2 WO2005018528 A2 WO 2005018528A2
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WO
WIPO (PCT)
Prior art keywords
prostatitis
active substance
treatment
prostate
use according
Prior art date
Application number
PCT/EP2004/009005
Other languages
German (de)
English (en)
Other versions
WO2005018528A3 (fr
Inventor
Kuno Kirschfeld
Original Assignee
Kuno Kirschfeld
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Kuno Kirschfeld filed Critical Kuno Kirschfeld
Publication of WO2005018528A2 publication Critical patent/WO2005018528A2/fr
Publication of WO2005018528A3 publication Critical patent/WO2005018528A3/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19—Carboxylic acids, e.g. valproic acid
    • A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate

Definitions

  • the present invention relates to the use of mucolytics for the treatment, differential diagnosis and prophylaxis of prostatitis.
  • prostatitis occurs in all age groups.
  • the cause and pathogenesis of their various forms are not yet known with the exception of the relatively rare acute (type I) or chronic (type II) bacterial prostatitis.
  • the biggest problem is chronic abacterial prostatitis (type III) (chronic pelvic pain syndrome). It can be inflammatory (III a) or non-flammable (III b).
  • Asymptomatic prostatitis (type IV) which can be discovered as a coincidence, plays no therapeutic role because of the absence of symptoms. While there are satisfactory treatment strategies for prostatitis types I and II, there is no satisfactory treatment management for prostatitis IM in either form.
  • prostatitis syndrome The pattern of the various symptoms in prostatitis is called prostatitis syndrome. Patients with chronic forms of prostatitis suffer a significant decrease in quality of life. The most common complaints include pain and sensations in the genital and anorectal area, disorders of libido, erection and ejaculation, micturition disorders and myalgiform complaints. The complaints can be so serious that they can lead to suicidality themselves.
  • the known therapies of prostatitis syndrome are against inflammation, anatomical changes (enlargement), symptomatic e.g. directed against pain, or aim to improve the blood flow to the prostate and the emptying of the bladder.
  • the preparations used in the treatment of prostatitis belong to the class of antibiotics, the alpha-receptor blockers, muscle relaxants, anti-inflammatory drugs or phytotherapeutics.
  • Analgesics and anticholinergics are also used.
  • psychosomatic or physical therapies, and ultimately also surgical procedures are used (Wagenlehner and Naber: therapy of prostate syndrome. Urologist (A) 40: 24-28 (2001)).
  • the object of the present invention is to provide a possibility for the effective treatment, prophylaxis and differential diagnosis of prostatitis.
  • a substance class is to be used, which according to prior art was not considered, and the mechanism of action for the treatment of prostatitis is novel.
  • the invention primarily proposes a use with the features mentioned in claim 1. Further developments of this use and pharmacological compositions are the subject of the remaining dependent and independent claims 2 to 11, the wording of which is made by reference to the content of the description.
  • Mucolytically active substances or mucolytics for short, are understood here and below to mean those active substances which change the physicochemical properties of mucous secretions, in particular secretions of the prostate, facilitate or accelerate their removal from the prostate or influence the secretion formation. According to the invention, the removal of the secretion from this gland is facilitated or accelerated by the therapy in the prostate.
  • the prostate is a composite gland that releases its secretion into the urethra when ejaculated and mixes it into the semen. Histologically, there are thickened, layered secretions in the lumen of the prostate glands (prostate stones, concretio prostaticä).
  • the use proposed here has the effect that the viscosity of the prostate secretion is reduced. This can improve the outflow of this secretion. In addition, it can be achieved in particular that prostate stones do not form or dissolve as far as possible. Both are beneficial in various ways. First, the tension and the associated tension pain decrease. Second, the prostate swells, which thirdly increases blood flow, and fourth, which Emptying the bladder is easier. Fifth, the improved blood flow leads to improved access of antibiotics to inflamed tissue.
  • mucolytically active substances and combinations thereof can be used.
  • Those mucolytic substances that additionally have anti-inflammatory properties can be used with particular advantage.
  • Particularly preferred are substances containing thiol groups and / or cysteine derivatives (or substances belonging to the substance class of cysteine derivatives), especially those with free thiol groups.
  • many thiols (substances with thiol groups or sulfhydryl groups), which also include cysteine, are known to have mucolytic properties.
  • cysteine derivatives which, in addition to the mucolytic, also have anti-inflammatory properties.
  • Acetylcysteine is particularly preferred (N-acetyl-L-cysteine, ACC® is a registered trademark of Hexal AG Germany).
  • Acetylcysteine is already used in humans for expectorant therapy for acute and chronic diseases of the bronchi. Acetylcysteine also exerts its mucolytic effect on secretion accumulations in the sinuses and middle ear. The anti-inflammatory effect of acetylcysteine represents a further advantage for the use of this substance in urology.
  • acetylcysteine The mechanism of action of acetylcysteine is essentially based on a reduction in the disulfide bonds between mucoproteins (glycoproteins) through its free sulfhydryl groups. As a result, mucoproteins are depolymerized and the viscosity of the mucus is reduced, for example in the sputum. Due to its antioxidant properties, acetylcysteine also has a local anti-inflammatory effect (DC Plumb: Veterinary Drug Handbook. PharmaVet Publishing, White Bear Lake, USA (1999)). Other advantages of acetylcysteine, which make its use in the treatment of prostatitis particularly advantageous, include minor side effects, which has been confirmed many years by years of use in other areas of indication.
  • salts of the active ingredient such as N-acetylcysteine-L-lysinate
  • salts of the active ingredient such as N-acetylcysteine-L-lysinate
  • other derivatives in particular thioethers and / or thioesters
  • Other thiols such as mercaptoethanesulfonic acid in particular, tiopronin and / or methylcysteine and / or derivatives thereof can also be used advantageously according to the invention.
  • Salts, thioethers and / or thioesters are particularly suitable as derivatives.
  • the mucolytically active substance promotes the formation of low-viscosity mucus.
  • the secretion viscosity in the prostate is reduced.
  • One active ingredient that is particularly suitable in this context is carbocysteine (S- (carboxymethyl) -L-cysteine). This substance does not have a thiol group and therefore does not react directly with slime molecules. However, it can be assumed that this substance intervenes intracellularly in the mucus synthesis and thereby promotes the formation of low-viscosity mucus. At the same time, the synthesis of highly viscous mucus is suppressed. This substance and / or comparable substances with similar mechanisms of action can thus be used with great advantage according to the invention. This takes place in a particularly advantageous manner in combination with other substances used according to the invention, as can be seen, for example, from the above description.
  • Derivatives of substances that promote the formation of low-viscosity mucus can also be used with advantage. From some of these Derivatives are already known to have mucolytic, analgesic, anti-inflammatory and / or antipyretic properties, so that they are of particular advantage for the treatment of prostatitis.
  • the at least one mucolytically active substance is used in combination with at least one antibiotic.
  • This combination can be administered to the patient, for example in the form of a single preparation or separately according to substances.
  • antibiotics and mucolytically active substances for example acetylcysteine
  • the antibiotics that have essentially no interactions with e.g. Have acetylcysteine and can thus advantageously be administered simultaneously with acetylcysteine include, for example, amoxicillin, erythrocycin and thiamphenicol.
  • the invention also includes a method for the treatment, prophylaxis and / or differential diagnosis of prostatitis, in which a therapeutically effective dose of at least one mucolytically active substance is administered.
  • the invention further comprises a pharmaceutical composition for the treatment, prophylaxis and / or differential diagnosis of prostatitis, which comprises a therapeutically effective dose of at least one mucolytically active substance.
  • this pharmaceutical composition comprises a pharmacologically acceptable carrier and / or auxiliary.
  • this pharmaceutical see composition intended for oral administration.
  • Mucolytics are preferably administered orally in a therapeutically effective dose and suitable formulation.
  • acetylcysteine is particularly suitable, which has already been successfully used in other indication areas in the form of capsules, effervescent or lozenges or juices.
  • other forms of administration are also encompassed by the invention.
  • the preparations containing mucolytics can further comprise at least one pharmacologically acceptable carrier and / or auxiliary.
  • PSA prostate-specific antigen
  • the PSA value cannot be influenced or can not be influenced significantly by antibiotics. Then the next necessary diagnostic step is the (multiple) punch biopsy. In the removed tissue malignant tissue can be identified and the diagnosis can thus be specified. Despite consistently high PSA values, it is often not possible to histologically verify prostate carcinoma; cancer therapy, for example through surgery, is then not indicated. These therapy-resistant cases are a common problem in urological practice.
  • the first attempt is made, using antibiotics, to bring a possible bacterial inflammation to subside. If symptoms and PSA levels remain high, a punch biopsy is not initially carried out as previously to verify or rule out carcinomatous events. Rather, mucolytics that work very quickly (1-2 days) are used. If the PSA level normalized and the symptoms subsided, the treatment was successful and a punch biopsy was not necessary. In this case, the mucolytics used in accordance with the invention help, in particular, to have a favorable influence on, or even to eliminate, painful and inflammatory processes caused by backflow.
  • the mucolytics are administered at the same time or in a suitable manner, time-shifted with antibiotics.
  • the advantage of this variant is that due to the expectorant effect of the mucolytics, the tissue tension of the prostate decreases and therefore the blood flow is increased, which improves the emptying of the bladder. WE Due to the improved blood circulation, antibiotics can reach the inflamed tissue better.
  • the mucolytic preparation is initially used for prostatic complaints, i.e. also in the event that the PSA value is not increased or it has possibly not yet been determined. Because of the fast action of the mucolytics, a differential diagnosis or prophylaxis is possible within a few days. In the best case, the symptoms subside after the medication. If symptoms persist, antibiotics only need to be used in the next step. This treatment regimen may be preferred because of minor side effects compared to antibiotics.
  • mucolytics For patients for whom mucolytic treatment has a positive effect, it may be advantageous to take mucolytics at regular, reasonable intervals (e.g. 2-4 times a month) when new symptoms begin or as a general prophylactic measure.
  • mucolytics thus includes the possibility of a gentle, efficient treatment of prostatitis, which after a short time can lead to significant improvement or even to the complete resolution of the symptoms. This treatment approach also results in a differential diagnosis.
  • the patient 68 years old, had been suffering from prostatitis with significant symptoms as described above for years.
  • the PSA values were around 10 ng / dl. This PSA value could not be influenced by using different antibiotics (see Table 1). Since the so-called free PSA was also relatively low (another indicator for prostate cancer), multiple punch biopsies were first performed in the specialist's practice, after some time at a university clinic. The histological findings spoke against carcinoma.

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Utilisation de certains mucolytiques ainsi que de compositions pharmaceutiques contenant ces mucolytiques pour le traitement, le diagnostic différentiel et / ou la prophylaxie de la prostatite. Les mucolytiques utilisés sont de préférence caractérisés en ce qu'ils contiennent au moins un groupe sulfhydryle. Il s'agit en particulier de dérivés de cystéine, par exemple d'acétylcystéine. La présente invention a pour objet de réduire, par l'utilisation de ces substances, la viscosité des sécrétions prostatiques. L'évacuation de ces sécrétions peut ainsi être améliorée. Il en résulte que la tension et la douleur associée à cette tension diminuent, que la prostate désenfle, que l'irrigation sanguine de la prostate augmente et que la vidange de la vessie s'en trouve facilitée.
PCT/EP2004/009005 2003-08-16 2004-08-12 Procédé de traitement, de prophylaxie et de diagnostic différentiel de la prostatite WO2005018528A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE10337638A DE10337638A1 (de) 2003-08-16 2003-08-16 Verfahren zur Behandlung der Prostatitis
DE10337638.0 2003-08-16

Publications (2)

Publication Number Publication Date
WO2005018528A2 true WO2005018528A2 (fr) 2005-03-03
WO2005018528A3 WO2005018528A3 (fr) 2005-04-07

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PCT/EP2004/009005 WO2005018528A2 (fr) 2003-08-16 2004-08-12 Procédé de traitement, de prophylaxie et de diagnostic différentiel de la prostatite

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DE (1) DE10337638A1 (fr)
WO (1) WO2005018528A2 (fr)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0271127A2 (fr) * 1986-11-07 1988-06-15 Irving M. Bush L'emploi de guaifenésine pour le traitement des troubles urologiques
WO2001080849A1 (fr) * 2000-04-26 2001-11-01 Charlotte-Mecklenburg Hospital Authority D/B/A Carolinas Medical Center Methode de traitement anticancereux
WO2003002125A2 (fr) * 2001-06-29 2003-01-09 Astion A/S Combinaison de sucres amines et cysteine ou de derives de cysteine
WO2003045359A2 (fr) * 2001-11-26 2003-06-05 Astion Oncology Aps Combinaison de derives de cimetidine et de cysteine pour traiter le cancer
US20030162732A1 (en) * 2001-07-05 2003-08-28 Astion Development A/S Combination of aminosugars and cysteine or cysteine derivatives

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0271127A2 (fr) * 1986-11-07 1988-06-15 Irving M. Bush L'emploi de guaifenésine pour le traitement des troubles urologiques
WO2001080849A1 (fr) * 2000-04-26 2001-11-01 Charlotte-Mecklenburg Hospital Authority D/B/A Carolinas Medical Center Methode de traitement anticancereux
WO2003002125A2 (fr) * 2001-06-29 2003-01-09 Astion A/S Combinaison de sucres amines et cysteine ou de derives de cysteine
US20030162732A1 (en) * 2001-07-05 2003-08-28 Astion Development A/S Combination of aminosugars and cysteine or cysteine derivatives
WO2003045359A2 (fr) * 2001-11-26 2003-06-05 Astion Oncology Aps Combinaison de derives de cimetidine et de cysteine pour traiter le cancer

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BUSH I M ET AL: "THE EFFECTS OF A MUCOLYTIC AGENT ON PROSTATIC OBSTRUCTION" 1989, JOURNAL OF UROLOGY, BALTIMORE, MD, US, PAGE(S) 535A , XP009041971 ISSN: 0022-5347 Zusammenfassung *
TOZAWA KEIICHI ET AL: "N-acetyl-L-cysteine enhances chemotherapeutic effect on prostate cancer cells." M{rz 2002 (2002-03), UROLOGICAL RESEARCH. MAR 2002, VOL. 30, NR. 1, PAGE(S) 53 - 58 , XP002316264 ISSN: 0300-5623 Seite 57, rechte Spalte, letzter Absatz *

Also Published As

Publication number Publication date
DE10337638A1 (de) 2005-03-24
WO2005018528A3 (fr) 2005-04-07

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