Comparative pharmacokinetics of ciprofloxacin, ofloxacin and pefloxacin in human aqueous humour

Abstract

Eighty-five patients undergoing cataract surgery were given for prophylaxis of intraocular infection two intravenous doses each of 200 mg, 300 mg or 400 mg ciprofloxacin (35 patients), 400 mg or 800 mg pefloxacin (30 patients), or 400 mg ofloxacin (20 patients). Ciprofloxacin levels in aqueous humour ranged from 0.02 to 0.50 microgram/ml, pefloxacin levels from 1.04 to 7.80 micrograms/ml, and ofloxacin levels from 0.44 to 2.27 micrograms/ml with ratios of aqueous humour to serum levels ranging from 3.8% to 25%, 21% to 48.1% and 44% to 88.4%, respectively. It is concluded that the quinolones studied might be suitable for surgical prophylaxis or treatment of anterior chamber infections due to Enterobacteriaceae, while ciprofloxacin at high doses is preferable for Pseudomonas aeruginosa infections.

Chapter 4: Requirements Concerning Antiseptics for Periorbital, Orbital and Intraorbital Application. 4.4.: Pharmacokinetics of Ophthalmic Drugs

“…A clear relationship between the intravenous dose of quinoline antimicrobials and the mean concentration in the human aqueous humor was reported by Giamarellou et al [74], which indicates a passive diffusion of the drug into the aqueous chamber. From the pharmacokinetic point of view, pefloxacin and ofloxacin were more advantageous than ciprofloxacin.…”

Histological Toxicity of Grepafloxacin after Intravitreal Injection

“…In general, new third-generation quinolones, as GRE, exhibit greater activity than other commercially available antibiotics against a wide spectrum of gram-positive and gram-negative microorganisms [11]. They can be used by different routes of administration, achieving therapeutic levels in ocular tissues from systemic administration [6,7]. The side effects of GRE and other quinolones limit their use by systemic administration, but they can be an alternative for intravitreal injection [8].…”

“…Also, systemically administered quinolones can achieve therapeutic concentrations in ocular tissues because their molecular weights are low and they are highly lipophilic [6,7]. Nevertheless, GRE has shown adverse cardiac reactions, such as Q-T enlargement, that limit its systemic administration [8].…”

A UPLC–MS Method for the Determination of Ofloxacin Concentrations in Aqueous Humor

“…It is a racemic mixture, which consists of 50% levofloxacin and 50% of its “mirror image” or enantiomer, dextrofloxacin. Ofloxacin is one of the most commonly used topical fluoroquinolones because of its high potency, high stability, low toxicity, low allergenicity, high intrinsic solubility, low minimal inhibitory concentration, and long half life 4. There are several routes of administration of ofloxacin: oral, intravenous, and eye drops.…”

“…Ofloxacin is one of the most commonly used topical fluoroquinolones because of its high potency, high stability, low toxicity, low allergenicity, high intrinsic solubility, low minimal inhibitory concentration, and long half life. 4 There are several routes of administration of ofloxacin: oral, intravenous, and eye drops. Ofloxacin is used for the treatment of ocular infections and is commonly applied in several ophthalmic surgeries, pre-or postoperatively.…”