Pharmacokinetics of lomefloxacin in renally compromised patients

Blum, Robert A.; Schultz, Rebecca; Schentag, Jerome J.

doi:10.1128/aac.34.12.2364

Cited by 27 publications

(9 citation statements)

References 11 publications

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“…As expected, strong positive correlations are observed between renal clearance and creatinine clearance as well as between total clearance and creatinine clearance (Blum 1992;Blum et al 1990;Leroy et al 1990;Nilsen et al 1992). 73m 2 (1.5 to 1.8 L/h/1.73m 2 ), and about 2 days in anuric individuals (Blum et al 1990). Consistent with changes in lomefloxacin clearance, tIll increases in relation to the degree of renal dysfunction.…”

Section: Renal Dysfunctionsupporting

confidence: 79%

“…This is evident from its apparent volume of distribution (Vd) which exceeds 70L (the volume of total body water) [Blum et al 1990;Gros & Carbon 1990;Leroy et al 1990]. This is evident from its apparent volume of distribution (Vd) which exceeds 70L (the volume of total body water) [Blum et al 1990;Gros & Carbon 1990;Leroy et al 1990].…”

Section: Distributionmentioning

confidence: 99%

“…The elimination of lomefloxacin occurs by both renal and nonrenal (gastrointestinal and hepatic) mechanisms (Blum et al 1990;Gros & Carbon 1990;Morrison et al 1988). The mean tl/, from serum or plasma ranges from 6 to 8h in healthy volunteers (tables I and II).…”

Section: Eliminationmentioning

confidence: 99%

“…The effect of renal dysfunction on lomefloxacin pharmacokinetics has been evaluated after administration of single doses to patients with varying degrees of renal function (Blum 1992;Blum et al 1990;Homer et al 1989;Leroy et al 1990;Metz et al 1989;Nilsen et al 1992). Since lomefloxacin is primarily excreted by the kidneys, changes in pharmacokinetic parameters are anticipated when renal function is altered.…”

Section: Renal Dysfunctionmentioning

confidence: 99%

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Lomefloxacin Clinical Pharmacokinetics

Freeman

Nicolau

Belliveau

et al. 1993

Clinical Pharmacokinetics

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Lomefloxacin is a quinolone antibiotic with chemical and microbiological properties similar to most commercially available agents of this class. There are differences, however, between lomefloxacin and other quinolones in activity against specific micro-organisms, a situation that is typical of most antibiotic classes. The pharmacokinetics of lomefloxacin support once- or twice-daily dosage, depending on the pathogen or site of infection. This is a result of its relatively high serum concentrations and long half-life. The outstanding pharmacokinetic features of lomefloxacin are its high degree of tissue distribution, lack of significant metabolism (and, therefore, no competitive drug interactions with other metabolised drugs showing a common metabolic pathway), and good oral absorption. Like most fluoroquinolones, lomefloxacin can chelate with heavy metals. However, this interaction can be eliminated by administering lomefloxacin 2h before the cation-containing products. Dosage adjustments are required in patients with renal dysfunction. However, patients with liver disease do not require alterations in lomefloxacin dosage regimens. The safety profile, lack of significant drug interactions and convenience of administration make lomefloxacin a useful agent in specific clinical settings.

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Section: Renal Dysfunctionsupporting

confidence: 79%

Section: Distributionmentioning

confidence: 99%

Section: Eliminationmentioning

confidence: 99%

Section: Renal Dysfunctionmentioning

confidence: 99%

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Lomefloxacin Clinical Pharmacokinetics

Freeman

Nicolau

Belliveau

et al. 1993

Clinical Pharmacokinetics

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“…After a single 400 mg dose, peak lomefloxacin levels in plasma are between 3.5 and 51ag/ml at 1 hour, more than 60% of the drug being recovered as unchanged compound (2,3). Concentrations of lomefloxacin in urine at 24 to 48 hours are 2.5/ag/ml and are above the minimum inhibitory concentrations (MICs) for most Enterobacteriaceae (3). Norfloxacin is also rapidly absorbed (30-40 %) after oral administration.…”

mentioning

confidence: 98%

Safety and efficacy of lomefloxacin versus norfloxacin in the treatment of complicated urinary tract infections

Hoepelman

Havinga²,

Benne³

et al. 1993

Eur. J. Clin. Microbiol. Infect. Dis.

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Seventy patients with complicated urinary tract infections were treated with either lomefloxacin (400 mg once daily) or norfloxacin (400 mg twice daily) for 10 to 14 days. A total of 19 (86%) of 22 patients treated with lomefloxacin and 20 (74%) of 27 patients treated with norfloxacin were cured, as defined by a negative culture five to nine days after completion of therapy (p = 0.09). After four to six weeks, the figures were 56% for lomefloxacin and 48% for norfloxacin. Adverse effects in the lomefloxacin group were observed on 20 occasions in 12 patients (one stopped treatment) compared to nine occasions in five patients treated with norfloxacin (difference not significant).

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Evaluation of a novel method to estimate absolute bioavailability of drugs from oral data

Hinderling¹

2002

Biopharm & Drug Disp

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The goal of this investigation was to evaluate the performance of a novel method allowing estimation of absolute bioavailability from oral data only. In contrast to the traditional method, which compares areas under the drug concentration time curves after oral and intravenous administration in subjects with normal renal function, the novel method uses total and renal clearance values following oral administration from subjects with varying renal functions to estimate bioavailability. The novel method can also provide estimates for nonrenal clearance.Published data on total clearance and renal clearance of drugs obtained from subjects with variable renal functions were collected, the novel method applied, estimates of bioavailability and nonrenal clearance obtained and compared with reported estimates by the traditional methods. In addition computations were performed to assess various factors that could possibly affect the reliability of the novel method. The results indicated that the novel method provides accurate estimates for bioavailability of drugs meeting the prerequisites: linear kinetics, predominant renal excretion in normals, absence of metabolic polymorphism and independence of bioavailability and nonrenal clearance from renal function. The average (standard deviation) of the prediction error and bias of the bioavailability estimates by the novel method was 7.8 (6.0) and -1.4 (9.8)%, respectively. The estimates for nonrenal clearance by the novel method were less accurate. The computations confirmed that the estimates by the novel method are sensitive to renal-function dependent changes in nonrenal clearance and bioavailability and also depend on the extent of renal excretion of a drug. In conclusion, the novel method's main use is to diagnose absence or presence of changes in bioavailability and non-renal clearance of drugs in populations with varying renal function.

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Pharmacokinetics of lomefloxacin in renally compromised patients

Cited by 27 publications

References 11 publications

Lomefloxacin Clinical Pharmacokinetics

Lomefloxacin Clinical Pharmacokinetics

Safety and efficacy of lomefloxacin versus norfloxacin in the treatment of complicated urinary tract infections

Evaluation of a novel method to estimate absolute bioavailability of drugs from oral data

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