Lomefloxacin Hydrochloride
Indications:
Lomefloxacin oral preparation is indicated for the treatment of:
Therapeutic Class: 4-Quinolone preparations, Aural Anti-bacterial preparations
Indications:
Lomefloxacin oral preparation is indicated for the treatment of:
- Uncomplicated urinary tract infections.
- Complicated including recurrent and pyelonephritis, urinary tract infections.
- Acute exacerbation of chronic bronchitis.
Description:
Lomefloxacin, a difluorinated quinolone derivative, is a bacterial gyrase inhibitor, effective against gram-positive and gram-negative bacteria. The acute toxicity of Lomefloxacin following systemic and topical ophthalmic application is low. Lomefloxacin interferes with bacterial DNA-related processes like initiation, elongation, and termination phases of replication, transcription, DNA repairing, recombination, transposition, supercoiling, and relaxation of DNA. The target molecule for quinolones is the A-subunit of bacterial enzyme gyrase (topoisomerase II). The forming of a stable complex between the quinolone and the whole gyrase tetramer A2B2 leads to impaired enzyme functions, resulting in the rapid killing of sensitive bacteria.
Cross-resistance has only been reported with other quinolones, but not with any other group of antibiotics. No clinical studies are available about the efficacy in cases of infections with chlamydia.
Dosage & Administration:
Typhoid fever: 400 mg once daily or 200 mg b.i.d 10-14 days.
UTI infections:
Acute exacerbation of chronic bronchitis: 400 mg once daily 7-10 days.
Skin and skin structure infections: 400 mg once daily 10-14 days.
Prophylaxis of UTI following surgery: 400 mg Single dose 2-6 hours prior to transurethral surgery.
Interaction:
Lomefloxacin does not alter theophylline clearance and concentration. No change in caffeine is reported. Sucralfate and antacid containing magnesium and aluminum interfere with their bioavailability. Enhances effects of warfarin. Probenecid slows renal elimination of Lomefloxacin.
Contraindications:
Lomefloxacin is contraindicated in patients with a history of hypersensitivity to Lomefloxacin or to other quinolones. Lomefloxacin like other drugs in its class causes arthropathy in juvenile animals. Therefore, its use in children, growing adolescents, and pregnant women is not recommended.
Side Effects:
Common side effects are Nausea, headache, photosensitivity, dizziness, diarrhea, dry mouth, fatigue, convulsions, CNS stimulation which may lead to tremors, restlessness, lightheadedness, confusion & hallucinations, and pseudomembranous colitis.
Pregnancy & Lactation:
Pregnancy Category C. Reproductive function studies have been performed in rats at doses up to 8 times the recommended human dose based on mg/m² (34 times the recommended human dose based on mg/kg), and no impaired fertility or harm to the fetus was reported due to lomefloxacin. Increased incidence of fetal loss in monkeys has been observed at approximately 3 to 6 times the recommended human dose based on mg/m² (6 to 12 times the recommended human dose based on mg/kg). No teratogenicity has been observed in rats and monkeys at up to 16 times the recommended human dose exposure. In the rabbit, maternal toxicity and associated fetotoxicity decreased placental weight, and variations of the coccygeal vertebrae occurred at doses 2 times the recommended human exposure based on mg/m². There are, however, no adequate and well-controlled studies in pregnant women. Lomefloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing mothers: It is not known whether lomefloxacin is excreted in human milk. However, it is known that other drugs of this class are excreted in human milk and that lomefloxacin is excreted in the milk of lactating rats. Because of the potential for serious adverse reactions from lomefloxacin in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Precautions & Warnings:
Alterations of the dosage regimen are recommended for patients with impairment of renal function (CrCl <40 ml/min/1.73 m2). Avoid exposure to excessive sunlight or artificial UV light. Phototoxicity reaction may occur if undue exposure occurs. The safety and efficacy of Lomefloxacin have not been established in children, pregnant and lactating women.
Use in Special Populations:
Should be stored in a cool and dry place
Lomefloxacin, a difluorinated quinolone derivative, is a bacterial gyrase inhibitor, effective against gram-positive and gram-negative bacteria. The acute toxicity of Lomefloxacin following systemic and topical ophthalmic application is low. Lomefloxacin interferes with bacterial DNA-related processes like initiation, elongation, and termination phases of replication, transcription, DNA repairing, recombination, transposition, supercoiling, and relaxation of DNA. The target molecule for quinolones is the A-subunit of bacterial enzyme gyrase (topoisomerase II). The forming of a stable complex between the quinolone and the whole gyrase tetramer A2B2 leads to impaired enzyme functions, resulting in the rapid killing of sensitive bacteria.
Cross-resistance has only been reported with other quinolones, but not with any other group of antibiotics. No clinical studies are available about the efficacy in cases of infections with chlamydia.
Dosage & Administration:
Typhoid fever: 400 mg once daily or 200 mg b.i.d 10-14 days.
UTI infections:
- Uncomplicated: 400 mg once daily or 200 mg b.i.d 3 days.
- Complicated: 400 mg once daily or 200 mg b.i.d 10-14 days.
Acute exacerbation of chronic bronchitis: 400 mg once daily 7-10 days.
Skin and skin structure infections: 400 mg once daily 10-14 days.
Prophylaxis of UTI following surgery: 400 mg Single dose 2-6 hours prior to transurethral surgery.
Interaction:
Lomefloxacin does not alter theophylline clearance and concentration. No change in caffeine is reported. Sucralfate and antacid containing magnesium and aluminum interfere with their bioavailability. Enhances effects of warfarin. Probenecid slows renal elimination of Lomefloxacin.
Contraindications:
Lomefloxacin is contraindicated in patients with a history of hypersensitivity to Lomefloxacin or to other quinolones. Lomefloxacin like other drugs in its class causes arthropathy in juvenile animals. Therefore, its use in children, growing adolescents, and pregnant women is not recommended.
Side Effects:
Common side effects are Nausea, headache, photosensitivity, dizziness, diarrhea, dry mouth, fatigue, convulsions, CNS stimulation which may lead to tremors, restlessness, lightheadedness, confusion & hallucinations, and pseudomembranous colitis.
Pregnancy & Lactation:
Pregnancy Category C. Reproductive function studies have been performed in rats at doses up to 8 times the recommended human dose based on mg/m² (34 times the recommended human dose based on mg/kg), and no impaired fertility or harm to the fetus was reported due to lomefloxacin. Increased incidence of fetal loss in monkeys has been observed at approximately 3 to 6 times the recommended human dose based on mg/m² (6 to 12 times the recommended human dose based on mg/kg). No teratogenicity has been observed in rats and monkeys at up to 16 times the recommended human dose exposure. In the rabbit, maternal toxicity and associated fetotoxicity decreased placental weight, and variations of the coccygeal vertebrae occurred at doses 2 times the recommended human exposure based on mg/m². There are, however, no adequate and well-controlled studies in pregnant women. Lomefloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Nursing mothers: It is not known whether lomefloxacin is excreted in human milk. However, it is known that other drugs of this class are excreted in human milk and that lomefloxacin is excreted in the milk of lactating rats. Because of the potential for serious adverse reactions from lomefloxacin in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Precautions & Warnings:
Alterations of the dosage regimen are recommended for patients with impairment of renal function (CrCl <40 ml/min/1.73 m2). Avoid exposure to excessive sunlight or artificial UV light. Phototoxicity reaction may occur if undue exposure occurs. The safety and efficacy of Lomefloxacin have not been established in children, pregnant and lactating women.
Use in Special Populations:
- Pediatric use: The safety and effectiveness of lomefloxacin in pediatric patients and adolescents less than 18 years of age have not been established. Lomefloxacin causes arthropathy in juvenile animals of several species.
- Geriatric use: Of the total number of subjects in clinical studies of lomefloxacin, 25% were ≥65 years and 9% were ≥ 75 years. No overall differences in safety or effectiveness were observed between these subjects and younger subjects, and other reported clinical experience has not identified differences in responses between the elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out.
Should be stored in a cool and dry place