Pharmacokinetics of ciprofloxacin after oral and intravenous administration in healthy volunteers

Wingender, W.; Graefe, Karl Heinz; Gau, Wolfgang; Förster, D; Beermann, D.; Schacht, P.

doi:10.1007/bf01977494

Cited by 149 publications

(72 citation statements)

References 10 publications

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“…A higher dose once a day might improve the urinary concentrations and making admini stration more easy. Extrarenal routes are important for the elimination of cipro ftoxacin (Wingender et al, 1984) and is confirmed in this study to account for nearly i of the total body clearance. Hence, ciproftoxacin may also be used in patients with impaired renal function (Gasser et al, 1987b), although reduction in dosage may be necessary.…”

Section: Discussionsupporting

confidence: 76%

“…Ciproftoxacin is rapidly excreted into the urine and high concentra tions were achieved even within 2 hours of drug intake. However, the half-life is considerably shorter in our patients (Table III) than in other studies where it was found to range between 3 and 5 hours (Wingender et al, 1984;Borner et al, 1986). High concentrations of ciproftoxacin were achieved in the urine and in most of the dosing interval by far exceeding the minimal concentrations necessary to inhibit growth of urinary tract pathogens (Wise et al, 1983;Fass, 1983).…”

Section: Discussioncontrasting

confidence: 60%

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Peroral treatment with ciprofloxacin of patients with spinal cord lesion and bacteriuria caused by multiply resistant bacteria

et al. 1990

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SummaryEleven patients, median age 38 years, with spinal cord lesion (SCL) and urinary tract infection (UT 1) caused by multiply resistant bacteria entered an open clinical trial of peroral ciprofloxacin 250 mg b.i.d. for 6 days. P. aeruginosa was the most prevalent bacteria. Ciprofloxacin was clinically effective in all patients who had symptoms of UTI at entry. Bacterial eradication was achieved in 9 out of 11 patients immediately after treatment. At 4 weeks post-treatment 5 patients had relapse of bacteriuria with the initial micro-organism and only 2 had long term eradication. One patient had transient elevation of transaminases, but no other adverse reactions were noted. Pharmacokinetic analysis showed that ciprofloxacin was readily absorbed with a terminal half life of 2·5 hours and considerable non renal elimination. The urinary concentration of ciprofloxacin was high during the whole dosing interval. Oral treatment with ciprofloxacin is an alternative to pa renteral antibiotics in SCL-patients with urinary tract infection caused by resistant bacteria.

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Section: Discussionsupporting

confidence: 76%

Section: Discussioncontrasting

confidence: 60%

Peroral treatment with ciprofloxacin of patients with spinal cord lesion and bacteriuria caused by multiply resistant bacteria

et al. 1990

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“…Compared with data derived from studies of young adult volunteers receiving single doses of intravenous ciprofloxacin (4,5,8,13,20), CLs, CLR, and V., were decreased in our study patients. In addition, the mean Cm.…”

Section: Discussioncontrasting

confidence: 56%

“…The pharmacokinetics of ciprofloxacin have been characterized in adults with normal and impaired renal function after single and multiple dose administration (4,5,8,9,11,13,14,16,20 ance of ciprofloxacin and a decreased apparent volume of distribution of the drug in elderly subjects.…”

mentioning

confidence: 99%

Steady-state pharmacokinetics of intravenous and oral ciprofloxacin in elderly patients

Hirata

Guay

Awni

et al. 1989

Antimicrob Agents Chemother

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The steady-state pharmacokinetics of ciprofloxacin were evaluated in nine elderly patients with lower respiratory tract infections after an intravenous dosage regimen of 200 mg every 12 h (n = 9) and an oral dosage regimen of 750 mg every 12 h (n = 6). Ciprofloxacin concentrations in serum and urine were measured by high-performance liquid chromatography. The peak concentration in serum, total body clearance (CLs), steady-state volume of distribution (V8,), and terminal elimination half-life after intravenous dosing were 3.5 + 0.8 ,ug/ml, 4.38 ± 1.80 ml/min per kg, 1.6 ± 0.6 liters/kg, and 5.8 ± 2.4 h, respectively. The peak concentration in serum, time to peak concentration in serum, absorption lag time, and absolute bioavailability (F) after oral dosing were 7.6 ± 2.2 ,Lg/ml, 1.9 ± 1.0 h, 0.4 ± 0.5 h, and 77.7 ± 24.2%, respectively. The elevated drug concentrations in serum samples from the elderly after oral dosing, compared with data obtained from younger subjects, appear to be a function of reduced CLs, renal clearance, and V,,. The increased F observed in some patients may be due to the effect of concomitant or proximate administration of tube feedings, medications which may alter gastric motility or acidity, or decreased first-pass metabolism. The results demonstrate that factors related to age and declining renal function, rather than infectious disease state, may be primary in determining alterations in pharmacokinetic parameters in the elderly. In elderly patients with normal renal function for their age, no dosage adjustment for intravenous or oral ciprofloxacin is necessary.Ciprofloxacin, a quinolone carboxylic acid derivative currently marketed in an oral dosage formulation and available as an investigational intravenous preparation, demonstrates in vitro activity against a broad spectrum of aerobic gramnegative and gram-positive bacteria, including strains resistant to aminoglycosides and beta-lactam antibiotics (6). The drug penetrates well into most tissues and is used clinically in the treatment of a variety of infections, including pneumonia (6).The pharmacokinetics of ciprofloxacin have been characterized in adults with normal and impaired renal function after single and multiple dose administration (4,5,8,9,11,13,14,16,20 ance of ciprofloxacin and a decreased apparent volume of distribution of the drug in elderly subjects.In a multiple dose study in elderly patients with serious infections, Guay et al. (12) characterized the pharmacokinetics of oral ciprofloxacin (750 mg every 12 h) during first dose (acutely ill phase) and maintenance dose (convalescentphase) therapy. No significant differences were noted between the first dose and steady-state pharmacokinetic parameters, with the exception of an increase in the apparent volume of distribution. The results were consistent with previous studies in healthy and mildly ill elderly subjects undergoing assessment after single doses of oral ciprofloxacin in that the maximum concentration of drug in serum (Cmax) and area under the concentration-time...

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“…Tubular transport of enoxacin, norfloxacin, ciprofloxacin, and ofloxacin has also been inferred by high CLR/CLCR ratios or has been confirmed by demonstration of significant reductions in CLR when coadministered with probenecid, an inhibitor of anionic tubular transport (5,18,23,25,28,29). Even fleroxacin, which has a CLR/CLCR ratio below unity, appears to have probenecid-sensitive tubular secretion (22).…”

Section: Discussionmentioning

confidence: 94%

Pharmacokinetics of temafloxacin in humans after multiple oral doses

Granneman

Carpentier

Morrison

et al. 1992

Antimicrob Agents Chemother

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The multiple-dose pharmacokinetics and tolerance of temafloxacin, a new fluoroquinolone antibacterial agent, were evaluated in healthy volunteers. Temafloxacin was found to be well tolerated when administered orally every 12 h for 7 days at doses of 100, 200, 300, 400, 600, and 800 mg. Steady-state maximum and minimum concentrations in plasma were proportional to dose, averaging slightly over 1.0 and 0.5 microgram/ml/100 mg administered. Analyses of variance found no significant differences among the dosage groups in total apparent clearances (CLT/F), renal clearances (CLR), or nonrenal clearances, which averaged 197, 119, and 78 ml/min, respectively. The half-life increased slightly with dose, averaging 8.4 h overall. The extent of absorption of temafloxacin was quite reproducible, with day-to-day intrasubject variability in minima averaging under 10%. Renal glomerular filtration of unbound drug was the dominant elimination process; however, tubular secretion and reabsorption also appear to occur. Secretion was estimated to account for about 12% of CLT/F during a regimen of 600 mg every 12 h. CLR was relatively constant for urine flow rates above 1 ml/min, but reabsorption appeared to occur under low-flow conditions, resulting in day-versus-night differences in CLR. Intersubject variability in CLT/F over the eightfold range in dosage was only 20%, and 60% of this variance was accounted for by differences in body surface area (or lean body mass), concentration in plasma, and urine flow rate. Overall, it appears that the pharmacokinetics of temafloxacin are essentially linear, reproducible within a subject, and predictable among subjects.

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Pharmacokinetics of ciprofloxacin after oral and intravenous administration in healthy volunteers

Cited by 149 publications

References 10 publications

Peroral treatment with ciprofloxacin of patients with spinal cord lesion and bacteriuria caused by multiply resistant bacteria

Peroral treatment with ciprofloxacin of patients with spinal cord lesion and bacteriuria caused by multiply resistant bacteria

Steady-state pharmacokinetics of intravenous and oral ciprofloxacin in elderly patients

Pharmacokinetics of temafloxacin in humans after multiple oral doses

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