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
  • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
  • A61P31/04—Antibacterial agents

Definitions

• Bacterial infections of the lower urinary tract are very common. The majority of urinary tract infections are caused by gram- negative bacteria. Organisms gaining access to the urethra may colonize on the periurethral glands and produce acute and chronic infection. This condition is termed urethritis. Infections of the prostate gland give rise to the condition prostatitis. Enteric, gram-negative organisms are the most common cause of prostate infection. Merck Manual 5th Ed., p. 1610, Merck, Sharpe & Dohme Research Laboratories (1987) .
• lomefloxacin and quinoline antibiotics have several advantages, they also have disadvantages, namely, adverse effects.
• the adverse effects of quinoline antibiotics in general include arthropathy, headache, stomach discomfort, gastrointestinal disorders, hypoglycemia, renal and hepatic dysfunction, allergic reactions and respiratory distress, and central nervous system effects including convulsions, increased intracranial pressure, and toxic psychoses.
• the adverse effects of lomefloxacin in particular, include but are not limited to headache, stomach discomfort, gastrointestinal disorders, and arthropathy, such as cartilage lesions and erosion and abnormalities in bone growth in immature patients.
• it would be particularly desirable to find a compound with the advantages of the racemic mixture of lomefloxacin which would not have the aforementioned disadvantages.
• the present invention also encompasses an antibiotic composition for treating infection in a human which comprises, an amount of (S)-lomefloxacin or a pharmaceutically acceptable salt thereof, substantially free of its (R)-stereoisomer, said amount being sufficient to alleviate said infection but insufficient to cause adverse effects associated with lomefloxacin.
• any suitable route of administration may be employed for providing the patient with an effective dosage of (S)-lomefloxacin.
• oral, rectal, parenteral, transdermal, subcutaneous. intramuscular, and the like may be employed as appropriate.
• Dosage forms include tablets, coated tablets, troches, dispersions, suspensions, solutions, caplets, capsules, patches, and the like.
• the pharmaceutical compositions of the present invention comprise (S)-lomefloxacin as active ingredient, or a pharmaceutically acceptable salt thereof, and may also contain a pharmaceutically acceptable carrier, and optionally, other therapeutic ingredients.
• (S)-lomefloxacin hydrochloride is a pharmaceutically acceptable salt of (S)-lomefloxacin.
• the most preferred pharmaceutically acceptable salt of (S)-lomefloxacin is the monohydrochloride salt.
• salts refers to salts prepared from pharmaceutically acceptable non-toxic acids or bases including inorganic acids and bases and organic acids and bases. Since the compound of the present invention is both basic and acidic, salts may be prepared from pharmaceutically acceptable non-toxic acids or bases including inorganic and organic acids or inorganic and organic bases. Such salts may contain any of the following anions: acetate, benzensulfonate, benzoate, camphorsulfonate, citrate, fumarate, gluconate, hydrobromide, hydrochloride, lactate, maleate, mandelate, mucate, nitrate, pamoate, phosphate, succinate, sulfate, tartrate and the like.
• a suitable dosage range for use is e.g., from about 100 mg to about 400 mg total daily dose, given as a once daily administration in the morning or in divided doses if required.
• a dose of 400 mg is given as a once daily administration.
• a dose range of between about 100 mg to about 200 mg is given as a once daily administration or in divided doses if required.
• Patients may be upward titrated from below to within this dose range to a satisfactory control of symptoms.
• (S)-lomefloxacin can be combined as the active ingredient in intimate admixture with a pharmaceutical carrier according to conventional pharmaceutical compounding techniques.

Landscapes

• 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)
• Communicable Diseases (AREA)
• Epidemiology (AREA)
• Oncology (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)
• Plural Heterocyclic Compounds (AREA)
• Peptides Or Proteins (AREA)
• Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Applications Claiming Priority (3)

Publications (2)

Family

ID=25175406

Family Applications (1)

Country Status (5)

Families Citing this family (1)

Family Cites Families (5)

• 1992
  • 1992-11-25 EP EP9292925403A patent/EP0614364A4/de not_active Ceased
  • 1992-11-25 CA CA002124443A patent/CA2124443A1/en not_active Abandoned
  • 1992-11-25 WO PCT/US1992/010142 patent/WO1993010785A1/en not_active Ceased
  • 1992-11-25 AU AU31474/93A patent/AU3147493A/en not_active Abandoned
  • 1992-11-25 JP JP5510220A patent/JPH07503457A/ja active Pending
• 1997
  • 1997-03-07 AU AU15151/97A patent/AU1515197A/en not_active Abandoned

Also Published As

Similar Documents

Legal Events