Ofloxacin

ATC CodeJ01MA01, S01AE01, S02AA16
CAS number82419-36-1
PUB number4583
Drugbank IDDB01165
Empirical formulaC18H20FN3O4
Molar mass (g·mol−1)361,4
Physical statesolid
Melting point (°C)254
PKS value5,35

Basics

Ofloxacin is an antibiotic used to treat bacterial infections in many parts of the body, including the respiratory tract, kidney, skin, soft tissue, and urinary tract.
Es wird weitgehend äußerlich als Augen- und Ohrentropfen eingesetzt.

Pharmacology

Pharmacodynamics

Ofloxacin is a broad-spectrum antibiotic that is active against both Gram-positive and Gram-negative bacteria. Its mode of action depends on blocking bacterial DNA replication (duplication) by binding itself to an enzyme called DNA gyrase. This enzyme allows the untwisting of the DNA double helix, which is necessary to replicate it into two.
Das Medikament hat eine 100-mal höhere Affinität für die bakterielle DNA-Gyrase als für die von Säugetieren.

Pharmacokinetics

The bioavailability in the tablet formulation is approximately 98%.
32% des Medikaments werden an Plasmaproteine gebunden.
Das Arzneimittel wird hauptsächlich renal ausgeschieden, wobei zwischen 65% und 80% einer verabreichten oralen Ofloxacin-Dosis innerhalb von 48 Stunden nach der Einnahme unverändert über den Urin ausgeschieden werden. Etwa 4-8 % einer Ofloxacin-Dosis werden mit den Fäzes ausgeschieden, das Arzneimittel unterliegt nur einer minimalen biliären Ausscheidung.

Interactions

Ofloxacin may interact with other drugs. Co-administration of some fluoroquinolone anti-infectives (e.g., ciprofloxacin, norfloxacin, ofloxacin) in patients taking theophylline may result in higher and prolonged serum theophylline concentrations, potentially increasing the risk of theophylline-related adverse reactions. The magnitude of this interaction varies considerably among commercially available fluoroquinolones; the effect is less pronounced with norfloxacin or ofloxacin than with ciprofloxacin.

Concomitant use of a fluoroquinolone with fenbufen (a nonsteroidal anti-inflammatory agent) may increase the risk of CNS stimulation (e.g., seizures).

Oral multivitamin and mineral supplements containing, for example, iron or zinc may decrease the oral absorption of ofloxacin, resulting in decreased serum concentrations of quinolone. Therefore, these multivitamins and/or mineral supplements should not be taken concomitantly with or within 2 hours of an ofloxacin dose.

In addition, the drug should not be taken with caffeinated beverages or foods, if possible.

Toxicity

Side effects

Adverse reactions include local reactions such as stinging, pain, hypersensitivity reactions, and rarely deposits.
Möglich, aber selten, sind systemische Nebenwirkungen wie allergische Reaktionen sowie Geruchs- und Geschmacksstörungen.

Bei 1 bis 2 % der mit Ofloxacin behandelten Patienten treten leichte Erhöhungen des ALT- und des alkalischen Phosphatasespiegel auf. Diese meist asymptomatischen Begleiterscheinungen klingen von selbst bei Fortsetzung der Therapie ab.

In rare cases, ofloxacin has been associated with acute liver injury.

Toxicological data

LD50 (rat, oral): 5450 mg/kg.

Markus Falkenstätter, BSc

Markus Falkenstätter, BSc

Mag. pharm. Stefanie Lehenauer

Mag. pharm. Stefanie Lehenauer



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