Chemical formula: C₁₉H₂₂FN₃O₄ Molecular mass: 375.394 g/mol PubChem compound: 5379
Gatifloxacin is a sterile solution for topical ophthalmic use. Gatifloxacin is an 8-methoxy synthetic fluoroquinolone antibacterial agent with in vitro activity against gram-negative and grampositive, aerobic and anaerobic and clinically important atypical microorganisms.
The antibacterial action of gatifloxacin results from inhibition of DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division.
Gatifloxacin ophthalmic solutions 0.3% and 0.5% were administered to 1 eye of 6 healthy male subjects each. At all time points, serum gatifloxacin levels were below the lower limit of quantification (5 ng/mL) in all subjects.
Pharmacokinetic parameters for ophthalmic dosing could not therefore be calculated. There is no human pharmacokinetic data available with respect to tear concentration following ocular administration.
Gatifloxacin is well absorbed from the gastrointestinal tract after oral administration and can be given without regard to food. The absolute bioavailability of gatifloxacin is 96%. Peak plasma concentrations of gatifloxacin usually occur 1-2 hours after oral dosing.
The table below summarizes the single- and multiple-dose pharmacokinetic studies conducted to study the ocular absorption, distribution, metabolism and excretion of gatifloxacin following topical ophthalmic administration.
Preclinical Ocular Pharmacokinetic Studies:
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