Pharmacokinetics of Gatifloxacin and Interaction with an Antacid Containing Aluminum and Magnesium

Lober, Silke; Ziege, S.; Rau, Margot; Schreiber, G; Mignot, A.; Koeppe, P.; Lode, H.

doi:10.1128/aac.43.5.1067

Cited by 61 publications

(24 citation statements)

References 20 publications

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“…The activity of quinolones is reduced in the presence of certain metal ions by the formation of sparingly soluble metal complexes [5]. Also, metal ions (especially magnesium) can be involved in the mechanism of action of these drugs [6][7][8].…”

Section: Introductionmentioning

confidence: 99%

Study of inclusion complex of β-cyclodextrin and levofloxacin and its effect on the solution equilibria between gadolinium(III) ion and levofloxacin

et al. 2015

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The formation of host-guest inclusion complex of levofloxacin with b-cyclodextrin (b-CD) was studied by fluorescence spectroscopy in buffer solution (pH 7.4) at 298 K. The experimental results confirmed the existence of 1:1 inclusion complex of levofloxacin with b-CD. The association constant of the b-CD inclusion complex was obtained from the Benesi-Hildebrand equation. The formation of the inclusion complex was confirmed by the IR and 1 H NMR technique. The complex formation equilibria between Gd(III) ion and levofloxacin were investigated in aqueous solutions without and in the presence of b-cyclodextrin. The stoichiometry and stability constants of the formed complexes are reported, and the concentration distribution of the various complex species has been evaluated as a function of pH. The effect of b-cyclodextrin on dissociation constants, K a , of levofloxacin and stability constants of gadolinium(III)-levofloxacin complexes, b p,q,r , were examined. Furthermore, effect of levofloxacin on the speciation and distribution Gd(III) in human blood plasma was evaluated by computer simulation. Graphical abstract

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Section: Introductionmentioning

confidence: 99%

Study of inclusion complex of β-cyclodextrin and levofloxacin and its effect on the solution equilibria between gadolinium(III) ion and levofloxacin

et al. 2015

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“…Both M and G have shown excellent activity in vitro and in animal models of TB, a favorable pharmacokinetic, and good safety profiles [6]–[9], suggesting that they may prove useful in shortening the treatment duration for TB, when used along with other first-line anti-TB drugs. Since an O-containing 4-month regimen has been shown to be very effective [2], the substitution of either M or G for O could be expected to fare even better.…”

Section: Introductionmentioning

confidence: 99%

Randomized Clinical Trial of Thrice-Weekly 4-Month Moxifloxacin or Gatifloxacin Containing Regimens in the Treatment of New Sputum Positive Pulmonary Tuberculosis Patients

et al. 2013

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BackgroundShortening tuberculosis (TB) treatment duration is a research priority. This paper presents data from a prematurely terminated randomized clinical trial, of 4-month moxifloxacin or gatifloxacin regimens, in South India.MethodsNewly diagnosed, sputum-positive HIV-negative pulmonary TB patients were randomly allocated to receive gatifloxacin or moxifloxacin, along with isoniazid and rifampicin for 4 months with pyrazinamide for first 2 months (G or M) or isoniazid and rifampicin for 6 months with ethambutol and pyrazinamide for first 2 months (C). All regimens were administered thrice-weekly. Clinical and bacteriological assessments were done monthly during treatment and for 24 months post-treatment. The Data and Safety Monitoring Board recommended termination of the trial due to high TB recurrence rates in the G and M regimens.ResultsOf 416 patients in intent-to-treat analysis, 6 (5%) of 124, 2 (2%) of 110 and 2 (2%) of 137 patients with drug-susceptible TB in the G, M and C arms respectively had unfavorable response at the end of treatment; during the next 24 months, 17 (15%) of 115, 11 (11%) of 104 and 8 (6%) of 132 patients respectively, had TB recurrence. Of 38 drug-resistant patients 1 of 8 and 3 of 26 in the G and C arms respectively had unfavourable response at the end of treatment; and TB recurrence occurred in 2 of 7 and 2 of 23 patients, respectively. The differences in TB recurrence rates between the G and C arms was statistically significant (p = 0.02). Gastro-intestinal symptoms occurred in 23%, 22% and 9% of patients in the G, M and C arms respectively, but most reactions were mild and manageable with symptomatic measures; 1% required regimen modification.Conclusions4-month thrice-weekly regimens of gatifloxacin or moxifloxacin with isoniazid, rifampicin and pyrazinamide, were inferior to standard 6-month treatment, in patients with newly diagnosed sputum positive pulmonary TB.Trial RegistrationClinical Trials Registry of India CTRI/2012/10/003060

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“…The absorption of fluoroquinolones is affected by coadministration with aluminium, calcium and magnesium-containing antacids owing to the formation of cation-quinolone complexes. [272][273][274][275] Table V shows the pharmacokinetic profile of frequently used fluoroquinolones.…”

Section: Fluoroquinolonesmentioning

confidence: 99%

Commonly Used Antibacterial and Antifungal Agents for Hospitalised Paediatric Patients

et al. 2001

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Due to normal growth and development, hospitalised paediatric patients with infection require unique consideration of immune function and drug disposition. Specifically, antibacterial and antifungal pharmacokinetics are influenced by volume of distribution, drug binding and elimination, which are a reflection of changing extracellular fluid volume, quantity and quality of plasma proteins, and renal and hepatic function. However, there is a paucity of data in paediatric patients addressing these issues and many empiric treatment practices are based on adult data. The penicillins and cephalosporins continue to be a mainstay of therapy because of their broad spectrum of activity, clinical efficacy and favourable tolerability profile. These antibacterials rapidly reach peak serum concentrations and readily diffuse into body tissues. Good penetration into the cerebrospinal fluid (CSF) has made the third-generation cephalosporins the agents of choice for the treatment of bacterial meningitis. These drugs are excreted primarily by the kidney. The carbapenems are broad-spectrum beta-lactam antibacterials which can potentially replace combination regimens. Vancomycin is a glycopeptide antibacterial with gram-positive activity useful for the treatment of resistant infections, or for those patients allergic to penicillins and cephalosporins. Volume of distribution is affected by age, gender, and bodyweight. It diffuses well across serous membranes and inflamed meninges. Vancomycin is excreted by the kidneys and is not removed by dialysis. The aminoglycosides continue to serve a useful role in the treatment of gram-negative, enterococcal and mycobacterial infections. Their volume of distribution approximates extracellular space. These drugs are also excreted renally and are removed by haemodialysis. Passage across the blood-brain barrier is poor, even in the face of meningeal inflammation. Low pH found in abscess conditions impairs function. Toxicity needs to be considered. Macrolide antibacterials are frequently used in the treatment of respiratory infections. Parenteral erythromycin can cause phlebitis, which limits its use. Parenteral azithromycin is better tolerated but paediatric pharmacokinetic data are lacking. Clindamycin is frequently used when anaerobic infections are suspected. Good oral absorption makes it a good choice for step-down therapy in intra-abdominal and skeletal infections. The use of quinolones in paediatrics has been restricted and most information available is in cystic fibrosis patients. High oral bioavailability is also important for step-down therapy. Amphotericin B has been the cornerstone of antifungal treatment in hospitalised patients. Its metabolism is poorly understood. The half-life increases with time and can be as long as 15 days after prolonged therapy. Oral absorption is poor. The azole antifungals are being used increasingly. Fluconazole is well tolerated, with high bioavailability and good penetration into the CSF. Itraconazole has greater activity against aspergillus, blastomycosis,...

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Pharmacokinetics of Gatifloxacin and Interaction with an Antacid Containing Aluminum and Magnesium

Cited by 61 publications

References 20 publications

Study of inclusion complex of β-cyclodextrin and levofloxacin and its effect on the solution equilibria between gadolinium(III) ion and levofloxacin

Study of inclusion complex of β-cyclodextrin and levofloxacin and its effect on the solution equilibria between gadolinium(III) ion and levofloxacin

Randomized Clinical Trial of Thrice-Weekly 4-Month Moxifloxacin or Gatifloxacin Containing Regimens in the Treatment of New Sputum Positive Pulmonary Tuberculosis Patients

Commonly Used Antibacterial and Antifungal Agents for Hospitalised Paediatric Patients

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