Chloramphenicol Excretion in the Bile

Danopoulos, E; Angelopoulos, B; Ziordrou, Chr.; Peco-Antić, Amira

doi:10.1111/j.1476-5381.1954.tb01677.x

Cited by 3 publications

(2 citation statements)

References 3 publications

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“…Reported or equivalent serum (µM) 4,10,14,31,39,43,46 10 (TC) Hypotension, prolonged PR/QT intervals and QRS complex, bundle branch block, ventricular premature contraction, ventricular tachycardia and ventricular fibrillation (Danopoulos et al, 1954;Ortiz et al, 2017;Osadchii, 2018) 10 mg/L ∼31 (Mukerji et al, 1986;Ihama et al, 2007) 0.49-1.1 mg/mL…”

Section: Table 3 | Continuedmentioning

confidence: 99%

A Bitter Taste in Your Heart

2020

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The human genome contains ∼29 bitter taste receptors (T2Rs), which are responsible for detecting thousands of bitter ligands, including toxic and aversive compounds. This sentinel function varies between individuals and is underpinned by naturally occurring T2R polymorphisms, which have also been associated with disease. Recent studies have reported the expression of T2Rs and their downstream signaling components within non-gustatory tissues, including the heart. Though the precise role of T2Rs in the heart remains unclear, evidence points toward a role in cardiac contractility and overall vascular tone. In this review, we summarize the extra-oral expression of T2Rs, focusing on evidence for expression in heart; we speculate on the range of potential ligands that may activate them; we define the possible signaling pathways they activate; and we argue that their discovery in heart predicts an, as yet, unappreciated cardiac physiology.

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Section: Table 3 | Continuedmentioning

confidence: 99%

A Bitter Taste in Your Heart

2020

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“…(Plumb, 2011). The principal biotransformation pathway is liver glucuronidation, resulting in the formation of chloramphenicol glucuronides which, unlike the situation in humans, are excreted to a considerable extent (50 %) also via the bile together with other metabolites (mainly amino derivatives originating from the nitroreduction of chloramphenicol) and possibly chloramphenicol, giving rise to enterohepatic circulation (Danopoulos et al, 1954). Eight hours after the oral administration of 99 mg of chloramphenicol sodium succinate/kg b.w., dogs excrete on average 6.3 % of the unchanged drug in the urine as measured by a microbiological method (Ling et al, 1980).…”

Section: Companion Animalsmentioning

confidence: 99%

Scientific Opinion on Chloramphenicol in food and feed

2014

EFS2

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Chloramphenicol is an antibiotic not authorised for use in food-producing animals in the European Union (EU). However, being produced by soil bacteria, it may occur in plants. The European Commission asked EFSA for a scientific opinion on the risks to human and animal health related to the presence of chloramphenicol in food and feed and whether a reference point for action (RPA) of 0.3 µg/kg is adequate to protect public and animal health. Data on occurrence of chloramphenicol in food extracted from the national residue monitoring plan results and from the Rapid Alert System for Food and Feed (RASFF) were too limited to carry out a reliable human dietary exposure assessment. Instead, human dietary exposure was calculated for a scenario in which chloramphenicol is present at 0.3 µg/kg in all foods of animal origin, foods containing enzyme preparations and foods which may be contaminated naturally. The mean chronic dietary exposure for this worst-case scenario would range from 11 to 17 and 2.2 to 4.0 ng/kg b.w. per day for toddlers and adults, respectively. The potential dietary exposure of livestock to chloramphenicol was estimated to be below 1 µg/kg b.w. per day. Chloramphenicol is implicated in the generation of aplastic anaemia in humans and causes reproductive/hepatotoxic effects in animals. Margins of exposure for these effects were calculated at 2.4 × 10 5 or greater and the CONTAM Panel concluded that it is unlikely that exposure to food contaminated with chloramphenicol at or below 0.3 µg/kg is a health concern for aplastic anaemia or reproductive/hepatotoxic effects. Chloramphenicol exhibits genotoxicity but, owing to the lack of data, the risk of carcinogenicity cannot be assessed. The SUMMARYChloramphenicol is a broad-spectrum antibiotic effective against Gram-positive and Gram-negative bacteria and, in the past, has been widely used to treat infections in both humans and animals. Chloramphenicol is not authorised for use in food-producing animals in the European Union (EU) but may be used in human medicine and in treatments for non-food-producing animals. Apart from its potential occurrence as a residue in food from illicit treatment of food-producing animals, chloramphenicol has also been used in feed and food enzyme products and may occur naturally in plants from its production by the soil bacterium Streptomyces venezuelae.The EFSA Scientific Opinion entitled "Guidance on methodological principles and scientific methods to be taken into account when establishing Reference Points for Action (RPAs) for non-allowed pharmacologically active substances present in food of animal origin" identified an approach for establishing RPAs for various categories of non-allowed pharmacologically active substances. However, the opinion also identified certain categories of non-allowed pharmacologically active substances that are considered to be outside the scope of the procedure, including substances causing blood dyscrasias (aplastic anaemia) such as chloramphenicol. As chloramphenicol is excluded fro...

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Antibiotics in the Biliary Tract: A Review of the Pharmacokinetics and Clinical Outcomes of Antibiotics Penetrating the Bile and Gallbladder Wall

Thabit

2020

Pharmacotherapy

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Biliary tract infections (BTIs), including cholangitis and cholecystitis, are common causes of bacteremia. Bacteremic BTIs are associated with a mortality rate of 9–12%. The extent to which antibiotics are excreted in the bile and the ratio of their exposure to the minimum inhibitory concentration of the infecting organism are among the important factors for the treatment of BTIs. This review updates health care professionals on the distribution of antibiotics in the common bile duct, gallbladder, and gallbladder wall. Antibiotic efficacy in treating BTIs based on the latest available clinical studies is also discussed. The efficacy and pharmacokinetics of 50 antibiotics are discussed. Overall, most antibiotic classes exhibit biliary penetration that translates into clinical efficacy. Only seven antibiotics (amoxicillin, cefadroxil, cefoxitin, ertapenem, gentamicin, amikacin, and trimethoprim/sulfamethoxazole) had poor biliary penetration profiles. Three antibiotics (ceftibuten, ceftolozane/tazobactam, and doripenem) had positive clinical outcomes despite the lack of pharmacokinetic studies on their penetration into the biliary tract. Conflicting efficacy data were reported for ampicillin despite adequate biliary penetration, whereas conflicting pharmacokinetic data were reported with cefaclor and moxifloxacin. Even in the absence of supportive clinical studies, antibiotics with good biliary penetration profiles may have a place in the treatment of BTIs.

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Chloramphenicol Excretion in the Bile

Cited by 3 publications

References 3 publications

A Bitter Taste in Your Heart

A Bitter Taste in Your Heart

Scientific Opinion on Chloramphenicol in food and feed

Antibiotics in the Biliary Tract: A Review of the Pharmacokinetics and Clinical Outcomes of Antibiotics Penetrating the Bile and Gallbladder Wall

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