Lomefloxacin-antimicrobial drug

Lomefloxacin

Pharmacodynamics

Lomefloxacin is a fluoroquinolone antibiotic used to treat chronic bronchitis, as well as complicated and uncomplicated urinary tract infections. It is also used as a prophylactic or preventative treatment to prevent urinary tract infections in patients undergoing transrectal or transurethral surgical procedures. Flouroquinolones such as lomefloxacin possess excellent activity against gram-negative aerobic bacteria such as E.coli and Neisseria gonorrhoea as well as gram-positive bacteria including S. pneumoniae and Staphylococcus aureus. They also posses effective activity against shigella, salmonella, campylobacter, gonococcal organisms, and multi drug resistant pseudomonas and enterobacter.

Mechanism of action

Lomefloxacin is a bactericidal fluoroquinolone agent with activity against a wide range of gram-negative and gram-positive organisms. The bactericidal action of lomefloxacin results from interference with the activity of the bacterial enzymes DNA gyrase and topoisomerase IV, which are needed for the transcription and replication of bacterial DNA. DNA gyrase appears to be the primary quinolone target for gram-negative bacteria. Topoisomerase IV appears to be the preferential target in gram-positive organisms. Interference with these two topoisomerases results in strand breakage of the bacterial chromosome, supercoiling, and resealing. As a result DNA replication and transcription is inhibited.

Absorption

Rapid and nearly complete with approximately 95% to 98% of a single oral dose being absorbed.

Protein binding

10%

Metabolism

Minimally metabolized although 5 metabolites have been identified in human urine. 65% appears as the parent drug in urine and 9% as the glucuronide metabolite.

Route of elimination

The urinary excretion of lomefloxacin was virtually complete within 72 hours after cessation of dosing, with approximately 65% of the dose being recovered as parent drug and 9% as its glucuronide metabolite.

Half life

8 hours

Toxicity

Adverse reactions include peripheral neuropathy, nervousness, agitation, anxiety, and phototoxic events (rash, itching, burning) due to sunlight exposure.

Drug drug interaction

lomefloxacin + bupropion = seizures

lomefloxacin + bedaquiline = increase the risk of an irregular heart rhythm that may be serious and potentially life-threatening

lomefloxacin + cortisone = increase the risk of tendinitis and tendon rupture

Food interaction

vitamins and minerals

Products that contain magnesium, aluminum, calcium, iron, and/or other minerals may interfere with the absorption of lomefloxacin and reduce its effectiveness

Therapeutic uses

Lomefloxacin is a fluoroquinolone antibiotic. It works by killing sensitive bacteria by stopping the production of essential proteins that the bacteria need to survive.

Reference- Tripathi KD "Essential of medical pharmacology" 7th edition, page no- 709,714