DESCRIPTION
A synthetic fluoroquinolone (fluoroquinolones) antibacterial agent that inhibits the supercoiling activity of bacterial DNA gyrase, halting DNA replication.
CATEGORIES
Anti-Bacterial Agents,Nucleic Acid Synthesis Inhibitors,Anti-Infective Agents,Anti-Infective Agents, Urinary,Quinolones.
CHEMICAL FORMULA
C18H20FN3O4
COMPOSITION
ofloxacin 0.3 % w/v
INDICATION
For the treatment of infections (respiratory tract, kidney, skin, soft tissue, UTI), urethral and cervical gonorrhoea.
PHARMACODYNAMICS
Ofloxacin is a quinolone/fluoroquinolone antibiotic. Ofloxacin is bactericidal and its mode of action depends on blocking of bacterial DNA replication by binding itself to an enzyme called DNA gyrase, which allows the untwisting required to replicate one DNA double helix into two. Notably the drug has 100 times higher affinity for bacterial DNA gyrase than for mammalian. Ofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria.
MECHANISM
Ofloxacin acts on DNA gyrase and toposiomerase IV, enzymes which, like human topoisomerase, prevents the excessive supercoiling of DNA during replication or transcription. By inhibiting their function, the drug thereby inhibits normal cell division.
ABSORPTION
Bioavailability of ofloxacin in the tablet formulation is approximately 98%
METABOLISM
Hepatic
ELIMINATION
Elimination is mainly by renal excretion. Between 65% and 80% of an administered oral dose of ofloxacin is excreted unchanged via the kidneys within 48 hours of dosing. Four to eight percent of an ofloxacin dose is excreted in the feces. This indicates a small degree of biliary excretion of ofloxacin.
HALF LIFE
9 hours
TOXICITY
LD50=5450 mg/kg (orally in mice)
FOOD INTERACTIONS
avoid alcohol
SIDE EFFECTS
Headache. Belly pain. Upset stomach or throwing up. Many small meals, good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. Loose stools (diarrhea). Yogurt or probiotics may help. You may get these products at health food stores or in some pharmacies. Tendons may rarely get irritated and tear. Unsafe allergic effects may rarely happen.