Comparative Study on Salivary Distribution of Fluoroquinolones in Rats.

Li, Qiuhong; Naora, Kohji; Hirano, Hidenari; Okunishi, Hideki; Iwamoto, Kikuo

doi:10.1248/bpb.25.1084

Cited by 7 publications

(4 citation statements)

References 29 publications

(34 reference statements)

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“…General factors regarding the compounds (lipophilicity, molecular mass, degree of ionization, protein binding) and the body fluids (pH, flow rate) have been suggested to influence the distribution of fluoroquinolones (Sorgel et al. , 1989; Jusko & Milsap, 1993; Li et al. , 2002).…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of pradofloxacin and doxycycline in serum, saliva, and tear fluid of cats after oral administration

Hartmann

Krebber

Daube

et al. 2008

Vet Pharm & Therapeutics

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The pharmacokinetic properties of pradofloxacin and doxycycline were investigated in serum, saliva, and tear fluid of cats. In a crossover study design, six cats were treated orally with a single dose of pradofloxacin (Veraflox Oral Suspension 2.5%) and doxycycline (Ronaxan 100 mg) at 5 mg/kg body weight. Following administration, samples of serum, saliva, and tear fluid were taken in regular intervals over a period of 24 h and analysed by turbulent flow chromatography/tandem mass spectrometry. All values are given as mean +/- SD. Pradofloxacin reached a mean maximum serum concentration (C(max)) of 1.1 +/- 0.5 microg/mL after 1.8 +/- 1.3 h (t(max)). In saliva and tear fluid, mean C(max) was 6.3 +/- 7.0 and 13.4 +/- 20.9 microg/mL, respectively, and mean t(max) was 0.5 +/- 0 and 0.8 +/- 0.3 h, respectively. Doxycycline reached a mean C(max) in serum of 4.0 +/- 0.8 microg/mL after 4.3 +/- 3.2 h. Whilst only at two time-points doxycycline concentrations close to the limit of quantification were determined in tear fluid, no detectable levels were found in saliva. The high concentrations of pradofloxacin in saliva and tear fluid are promising to apply pradofloxacin for the treatment of conjunctivitis and upper respiratory tract infections in cats. As doxycycline is barely secreted into these fluids after oral application the mechanisms of its clinical efficacy remain unclear.

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Section: Discussionmentioning

confidence: 99%

Pharmacokinetics of pradofloxacin and doxycycline in serum, saliva, and tear fluid of cats after oral administration

Hartmann

Krebber

Daube

et al. 2008

Vet Pharm & Therapeutics

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“…Inhibitors of FQ in saliva or certain physicochemical properties (pH, fat solubility, etc.) could partly explain this phenomenon [48].…”

Section: Qualitative Effectmentioning

confidence: 96%

“…However, some molecules may be partially inactivated in stool by binding to feces, which could reduce their active fraction present in the gut [35]. Regarding other microbiota, concentrations of FQ in saliva, nasal secretions and sweat are of the same order of magnitude as the concentrations in plasma (Tables 2 & 3) [47], but the sampling site (including sweat and saliva) and variable properties in terms of lipophilicity of different molecules may account for significant variations of these concentrations [42,48]. Altogether, diffusion of a given antibiotic varies greatly by microbial ecosystem.…”

Section: Concentrations Of Fqs In the Microbial Ecosystemsmentioning

confidence: 99%

Impact of Fluoroquinolones on Human Microbiota. Focus on the Emergence of Antibiotic Resistance

Lastours

Fantin

2015

Future Microbiol.

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The aggregate of microorganisms residing on the surface of the skin, in the oropharynx and in the GI tract, known as the human microbiota, play a major role as natural reservoirs for bacterial resistance to antibiotics. Fluoroquinolones (FQ) are among the most prescribed antibiotics and a major increase in FQ resistance is occurring worldwide. High concentrations of FQ are found in microbial ecosystems explaining their profound effect on the clinically relevant bacteria that compose them. Yet, because of different local pharmacokinetics, distinct selective pressures occur in the different microbiota. Here we review the qualitative and quantitative impact of FQ on the three main human microbiota and their consequences, particularly in terms of emergence of antibiotic resistance. Finally, we review potential actions that could decrease the impact of FQs on microbiota.

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“…Penetration of the FQs into brain, cerebrospinal fluid, saliva, and vitreous humor is dependent on their lipophilic properties (Liu et al 1998;Li et al 2002). However, FQ-induced tendinopathy is a dose dependent adverse effect.…”

Section: Pharmacokinetics Safety Relationshipmentioning

confidence: 99%

Fluoroquinolone-Induced Tendinopathy: Etiology and Preventive Measures

Kaleagasioglu

Olcay

2012

Tohoku J. Exp. Med.

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Tendinopathy is a serious health problem and its etiology is not fully elucidated. Among intrinsic and extrinsic predisposing factors of tendinopathy, the impact of therapeutic agents, especially fluoroquinolone (FQ) group antibiotics, is recently being recognized. FQs are potent bactericidal agents widely used in various infectious diseases, including community acquired pneumonia and bronchitis, chronic osteomyelitis, traveler's diarrhea, typhoid fever, shigellosis, chronic bacterial prostatitis, uncomplicated cervical and urethral gonorrhea and prophylaxis of anthrax. FQs have an acceptable tolerability range. However, many lines of evidence for developing tendinitis and tendon rupture during FQ use have resulted in the addition of a warning in patient information leaflets. FQ-induced tendinopathy presents a challenge for the clinician because healing response is poor due to low metabolic rate in mature tendon tissue and tendinopathy is more likely to develop in patients who are already at high risk, such as elderly, solid organ transplant recipients and concomitant corticosteroid users. FQs become photo-activated under exposure to ultraviolet light, and this process results in formation and accumulation of intracellular reactive oxygen species (ROS). The subsequent FQ-related oxidative stress disturbs mitochondrial functions, leading to apoptosis. ROS overproduction also has direct cytotoxic effects on extracellular matrix components. Understanding the mechanisms of the FQ-associated tendinopathy may enable designing safer therapeutic strategies, hence optimization of clinical response. In this review, we evaluate multi-factorial etiology of the FQ-induced tendinopathy and discuss proposed preventive measures such as antioxidant use and protection from natural sunlight and artificial ultraviolet exposure.

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Comparative Study on Salivary Distribution of Fluoroquinolones in Rats.

Cited by 7 publications

References 29 publications

Pharmacokinetics of pradofloxacin and doxycycline in serum, saliva, and tear fluid of cats after oral administration

Pharmacokinetics of pradofloxacin and doxycycline in serum, saliva, and tear fluid of cats after oral administration

Impact of Fluoroquinolones on Human Microbiota. Focus on the Emergence of Antibiotic Resistance

Fluoroquinolone-Induced Tendinopathy: Etiology and Preventive Measures

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