Trulev Mechanism of Action

Pharmacology: Pharmacodynamics: Mechanism of Action: Levofloxacin is the L-isomer of the racemate, a quinolone antibacterial agent. The antibacterial activity of Ofloxacin resides primarily in the L-isomer. The mechanism of action of Levofloxacin and other fluoroquinolone antimicrobials involves inhibition of bacterial topoisomerase, enzyme required for DNA replication, transcription, repair and recombination. Levofloxacin has in-vitro activity against a wide range of gram-negative and gram-positive microorganism. Levofloxacin is often bactericidal at concentrations equal to or slightly greater than inhibitory concentration.
Pharmacokinetics: Absorption: Levofloxacin is rapidly and essentially completely absorbed after oral administration. Peak plasma concentrations are usually attained one to two hours after oral dosing. The absolute bioavailability of a 500 mg tablet and a 750 mg tablet of levofloxacin are both approximately 99% demonstrating complete oral absorption of levofloxacin. Oral administration of 500 mg Levofloxacin with food prolongs the time to peak concentration by approximately 14% following tablet administration. Therefore Levofloxacin tablet can be administered without regard to food.
Distribution: The mean volume of distribution of Levofloxacin generally range from 74-112 L after single and multiple 500 mg or 750 mg doses, indicating widespread distribution to body tissues. Levofloxacin reaches its peak level in the skin tissue and in blister fluid or healthy subject at approximately 3 hours after dosing. The skin tissue biopsy to plasma AUC ratio is approximately 1 following multiple once-daily oral administration of 750 mg and 500 mg Levofloxacin, respectively to healthy subjects. Levofloxacin also penetrates well in the lung tissue. Levofloxacin is mainly bound to serum albumins in human. Levofloxacin binding to serum protein is independent of the drug concentration.
Metabolism: Levofloxacin is stereochemically stable in plasma and urine and does not invert metabolically to its enantiomer, D-ofloxacin. Levofloxacin undergoes limited metabolism in humans and primarily excreted as unchanged drug in the urine. Following oral administration approximately 87% of an administered dose was recovered as unchanged drug in urine within 48 hours, whereas less than 4% of the dose was recovered in feces in 72 hours. Less than 5% of an administered dose was recovered in the urine as the desmethyl and N-oxide metabolites have little relevant pharmacological activity.
Excretion: Levofloxacin is excreted largely as unchanged drug in the urine. The mean terminal plasma elimination half-life of Levofloxacin ranges from approximately 6-8 hours following single or multiple doses of Levofloxacin given orally. The mean apparent total body clearance and renal clearance range from approximately 144-226ml/min and 96-142ml/min, respectively.