Renal Excretion Mechanism of Sparfloxacin.

Yamaguchi, Toshikazu; Yokogawa, Makiko; Sekine, Yutaka

doi:10.2133/dmpk.6.61

Cited by 2 publications

(1 citation statement)

References 4 publications

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“…This speculation is supported by animal model studies which use the stopflow method and the renal clearance method: sparfloxacin was scarcely secreted from the proximal tubules of nephrons, but it was reabsorbed at the distal tubules (Yamaguchi et al 1991d). Accordingly, the renal behaviour of sparfloxacin differs somewhat from that of other quinolones which undergo tubular secretion.…”

Section: Probenecidmentioning

confidence: 97%

Clinical Pharmacokinetics of Sparfloxacin

Shimada

Nogita

Ishibashi

1993

Clinical Pharmacokinetics

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Sparfloxacin is a recently developed fluoroquinolone. The drug has shown potent antimicrobial activity against a wide range of Gram-positive and Gram-negative bacteria, glucose non-fermenters, anaerobes, Legionella spp., Mycoplasma spp., Chlamydia spp. and Mycobacterium spp. Methicillin-resistant Staphylococcus aureus is also susceptible to sparfloxacin. Plasma sparfloxacin concentrations reach a peak (Cmax) of approximately 0.7 mg/L at 3 to 5 hours after a 200mg oral dose. This is followed by a monophasic slow decrease, with an elimination half-life (t1/2) of 15 to 20 hours. The Cmax and area under the plasma concentration-time curve show dose-related increases. Food intake does not affect the absorption and pharmacokinetics of sparfloxacin. Sparfloxacin binds weakly to plasma protein (37%), and exhibits excellent tissue distribution and effective penetration into extracellular fluids. Concentrations of the drug in most tissues are similar to, or higher than, concomitant plasma concentrations. Sparfloxacin distributes slightly into cerebrospinal fluid. The drug is metabolised to a glucuronide. The urinary excretion of the unchanged drug accounts for 10 to 14% of the given dose. The ratio of Cmax values after multiple and single oral doses is 1.3 to 1.4, but other pharmacokinetic parameters of sparfloxacin are not influenced by multiple doses. Even in patients with severe renal failure, no significant prolongation of the half-life is observed after oral administration. Sparfloxacin appears unlikely to affect the pharmacokinetics of theophylline. Antacids containing aluminium hydroxide reduce the oral bioavailability of sparfloxacin by 25 to 35%. Probenecid does not affect sparfloxacin pharmacokinetics. The pharmacokinetic properties of sparfloxacin allow once-daily administration in the treatment of various infections.

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Section: Probenecidmentioning

confidence: 97%

Clinical Pharmacokinetics of Sparfloxacin

Shimada

Nogita

Ishibashi

1993

Clinical Pharmacokinetics

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Sparfloxacin pharmacokinetics in healthy volunteers: the influence of acidification and alkalinization

Kamberi¹,

Kotegawa²,

Tsutsumi³

et al. 1998

European Journal of Clinical Pharmacology

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The urinary pH dependence of the renal clearance of sparfloxacin will be of minor clinical importance with regard to the low contribution of renal excretion to the overall elimination of sparfloxacin. On the other hand, the alteration in the environmental pH in the gastrointestinal tract, produced by the concomitant ingestion of ammonium chloride or sodium bicarbonate, influences the absorption and bioavailability of sparfloxacin. This effect is likely to be clinically significant.

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Renal Excretion Mechanism of Sparfloxacin.

Cited by 2 publications

References 4 publications

Clinical Pharmacokinetics of Sparfloxacin

Clinical Pharmacokinetics of Sparfloxacin

Sparfloxacin pharmacokinetics in healthy volunteers: the influence of acidification and alkalinization

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