Quinolone pharmacokinetics and metabolism

Abstract

The pharmacokinetic properties of the new fluoroquinolones are characterized by a high volume of distribution, long biological half-life, low serum protein binding, elimination by renal and extrarenal mechanisms with high total and renal clearances, limited biotransformation and moderate to excellent bioavailability after oral administration. However, each quinolone derivative (ciprofloxacin, enoxacin, fleroxacin, norfloxacin, ofloxacin and pefloxacin) possesses individual pharmacokinetic parameters, which should be considered in the treatment of patients, especially when liver or renal dysfunction exists.

Pharmacokinetic Basis for Oral Perioperative Prophylaxis with Ofloxacin in General Surgery

“…These data are in accordance with other studies [37,39,40], suggesting that preoperative bowel preparation, fasting and premedication do not considerably affect resorption and bioavailability. This implies that even in long-lasting operative procedures such as pancreatic or colonic resections, preoperative oral prophylaxis with ofloxacin guarantees sufficient antibacterial protection.…”

“…An important advantage of oral perioperative prophylaxis is that the drug is given whilst the patient is still on the surgical ward, where the time of application can be determined exactly by the surgeon. Quinolones are characterized by a high intestinal resorption and high bioavailability after enteral administration [37]. They are also effective against gram-negative enteric and gram-positive epidermal flora [38].They therefore appear to be promising candidates for oral preoperative prophylaxis.…”

Quinolones: a class of antimicrobial agents

“…Enrofloxacin and pefloxacin are Ndealkylated to form ciprofloxacin and norfloxacin, respectively, similarly like fleroxacin (Lode et al, 1987;Küng et al, 1993). Other prominent metabolic pathways include oxidation to oxo-metabolites at the piperazine ring (Nix and Schentag, 1988), the major metabolites of ciprofloxacin, enoxacin, and norfloxacin (Lode et al, 1990;Anadón et al, 1995). Quite often, glucuronidation occurs, primarily on the carboxylic acid at position 3.…”

“…The oxidized metabolites (like many of the N-desmethyl metabolites) have an antibacterial activity (Prescott and Yielding, 1990;Küng et al, 1993;) whereas the glucuronide conjugates are devoid of any activity (Nix and Schentag, 1988;Venezia et al, 1989). Other metabolic pathways include sulfoxidation and acetylation (Lode et al, 1990).…”

A Case of Hemiballism as a Rare Side Effect of Ciprofloxacin in a Patient with Liver Cirrhosis

“…Ciprofloxacin is metabolized in the liver and excreted via the kidney. Bellmann et al [21] reported that the half-life of ciprofloxacin was prolonged by the presence of liver cirrhosis, and pharmacokinetic studies [22,23] showed a correlation of drug metabolism with the grade of cirrhosis according to the Child-Pugh classification. Therefore, careful dosing of ciprofloxacin in decompensated cirrhotic patients is warranted.…”