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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
  • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
  • A61K31/445—Non condensed piperidines, e.g. piperocaine
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
  • A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
• • 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
  • A61K31/33—Heterocyclic compounds
  • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
  • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
• • 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
  • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P15/00—Drugs for genital or sexual disorders; Contraceptives

Definitions

• This invention relates to the use of 3-methyl-f la- von-8-carboxyl ⁇ c acid and derivatives thereof for the preparation of a drug for the treatment and for the diagnosis of erectile impotence.
• the invention relates to pharma ⁇ ceutical compositions for the treatment of erectile impotence containing as the active principle 3-methylfla- von-8-carboxyl ⁇ c acid or a derivative thereof of formula I
• A is a linear or branched C -C alkyl residue
• Z is a dimethylamino, diethylammo, di-n-propylamino, di- lsopropylammo, piperidmo or morpholmo residue, or pharmaceutically acceptable salts thereof.
• Flavoxate is a very well tolerated drug; the large therapeutic index found in preclinical studies (C. Pietra et al., II Farmaco Ed. Prat., 4_1, 267, (1986)) and the absence of serious side effects during clinical application, attest its excellent tolerability. Particularly, cardiocirculatory complica ⁇ tions have never been reported. 3-methylflavon-8-carbo- xylic acid(MFCA) is the main metabolite of flavoxate. In terms of pharmacokinetics and - dynamics MFCA is most similar to flavoxate.
• Erectile dysfunction is a well known and common disease, of vascular, hormonal, neurogenic or psychogenic origin which causes impaired penile erection.
• the insufficient erectile ability of the penis has serious implications for psychological, physical and social well-being of the afflicted individuals. Self confidence in particular, and quality of life in general, are strongly reduced.
• Prosthetic devices that are implanted in the penis to mimic erection or are located outside in the scrotal sac or in an adjacent area to stimulate for instance to trasmitting electrical energy to the nervi erigentes.
• Pharmacological substances which are also injected directly into the corpora cavernosa, where they increase the inflow of blood and consequently generate tumescence of the penis, are also used.
• Human tissue was obtained from patients undergoing penile prothesis implantation.
• Biopsies of human corpus cavernosum tissue were obtained in the operating room and immediately placed in chilled (4°C) physiological salt solution of the following millimolar composition: NaCl 118.3; KC1 4.7; Mg ⁇ O 0.6; KH PO 1.2; CaCl 2.5; NaHCO 25.0; Calcium EDTA 0.026 and glucosio 11.1.
• the solution is gassed with 95% 0 , 5% CO ; pH maintained at 7.4 and temperature at 37°C.
• Isometric tension was measured throught the experiment with a tension transducer (Grass FT03, Quincy, MA) .
• the strips of corpus cavernosum were fixed with silk ties on one end to the electrode support and the other end to a wire connected to the force transducer.
• the strips were allowed to equilibrate for a period of approximately three hours.
• the optimal isometric tension for contraction was determined during this period by stepwise stretching of the tissue followed by
• Drugs were provided in powder form. Stock solutions were made in distilled water. For papaverine and flavoxate
• Flavoxate up to 10 M, induced relaxation of HCC contracted with norepinephrine, PG F2 alpha or potassium. Maximal relaxations to this concentration were: 73.1 +/- 7.7%, 66 +/- 13.2%, and 55.5 +/- 23% of maximal relaxation, respectively (see figures 1-3).
• the threshold for the response to flavoxate was approximately 3 x 10 M. The relaxation response was slow in onset and several minutes were required before the maximal relaxation
• 3-methylflavon-8-carboxylic acid and its basic esters of formula I, particularly flavoxate may be conveniently used in human therapy for the treatment of erectile impairments.
• pharmaceutical compositions suited for the oral, topical or parenteral (intracavernous) administration are provided.
• the oral administration is particularly convenient for its compliance and it is moreover useful as support therapy in patients who otherwise undergo papaverine or alpha-blockers injection. This regimen allows a reduction of the papaverine and alpha-blocker dosage and improves therefore the safe use of these agents.

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• Health & Medical Sciences (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)
• Veterinary Medicine (AREA)
• Epidemiology (AREA)
• Engineering & Computer Science (AREA)
• Bioinformatics & Cheminformatics (AREA)
• Chemical Kinetics & Catalysis (AREA)
• General Chemical & Material Sciences (AREA)
• Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
• Organic Chemistry (AREA)
• Urology & Nephrology (AREA)
• Endocrinology (AREA)
• Reproductive Health (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Applications Claiming Priority (2)

Publications (1)

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ID=11165532

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• 1988
  • 1988-04-22 IT IT20299/88A patent/IT1217190B/it active
• 1989
  • 1989-04-19 JP JP1504483A patent/JPH02504146A/ja active Pending
  • 1989-04-19 EP EP89904810A patent/EP0374210A1/en not_active Withdrawn
  • 1989-04-19 WO PCT/EP1989/000417 patent/WO1989010123A1/en not_active Application Discontinuation
  • 1989-04-19 AU AU34382/89A patent/AU3438289A/en not_active Abandoned
  • 1989-04-19 HU HU892651A patent/HU202754B/hu not_active IP Right Cessation
  • 1989-04-19 KR KR1019890702417A patent/KR900700098A/ko not_active Application Discontinuation
  • 1989-04-20 ZA ZA892911A patent/ZA892911B/xx unknown

Non-Patent Citations (1)

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