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Chemopreventive Agents
Published in David E. Thurston, Ilona Pysz, Chemistry and Pharmacology of Anticancer Drugs, 2021
Another concern is that there is evidence that ingestion of significant quantities of quercetin may cause interactions with certain medications. For example, there is some evidence that quercetin binds to the bacterial DNA gyrase enzyme and may interact with the fluoroquinolone antibiotics that target this enzyme. Quercetin has also been reported to inhibit the metabolic enzyme CYP2C8 and may potentially interfere with the pharmacokinetics of a wide range of drugs, including the anticancer agents taxol and paclitaxel. This is a potential problem, as some cancer patients prescribed taxol or paclitaxel may take a quercetin-containing supplement in the belief that it may be beneficial for their disease. However, as these anticancer agents are metabolized primarily by CYP2C8, their bioavailability may be increased unpredictably, potentially leading to harmful side effects.
Tendinopathy
Published in Kohlstadt Ingrid, Cintron Kenneth, Metabolic Therapies in Orthopedics, Second Edition, 2018
Consideration should be given to antibiotic selection. Fluoroquinolone antibiotics’ use can predispose to tendinopathy and tendon rupture. Since some causes of reactive arthritis have developed resistance to fluoroquinolones, these antibiotics are used less frequently in association with tendinopathy comorbid ities. Further, this class of antibiotics should be avoided in athletic individuals (van der Linden et al., 2001), as well as in the elderly, diabetic or the renal-function compromised patient. Cyclosporin and erythromycin are associated with rhabdomyolysis and may through this mechanism be anticipated to contribute to tendinopathy.
Positron Emission Tomography
Published in Graham Lappin, Simon Temple, Radiotracers in Drug Development, 2006
For pharmacokinetic studies the radionuclide must be an isotope of an element that is already present in the compound; otherwise, the radiolabeled derivate may behave very different from the parent compound, and no useful information can be derived from its biodistribution. Almost every compound contains carbon, and 11C has the most potential in drug development with positron emission tomography.6,7 The relatively short half-life of [11C]-carbon of about 20 min limits its use to intravenously administered or inhaled drugs. Another disadvantage may occur if the drug to be studied has a long half-life compared to the short physical half-life of [11C]-carbon,8 in which case PET studies would reveal only a snapshot of the initial distribution rather than the full tissue kinetics. [18F]-fluorine can be used if the substance has a fluoride atom and its longer half-life makes it the isotope of choice for investigating orally administered drugs, although the dose of radiation to the stomach wall needs to be considered. 18F has, for example, been used in the pharmacokinetic evaluation of orally administered fluoroquinolone antibiotics.9
Provider-directed analgesia for dental pain
Published in Expert Review of Clinical Pharmacology, 2023
The most common side effects of caffeine are nausea, anxiety, elevated blood pressure, tachycardia, bronchodilation, mild CNS stimulation, diuresis, wakefulness, euphoria, and addiction liability (Table 2) [119]. Caffeine’s alleviation of pain is believed to occur via antagonism of adenosine receptors in peripheral and central systems (Table 2) [120]. Caffeine is predominantly metabolized by CYP1A2 and therefore is subject to numerous drug interactions (Table 2) [121]. Among these include fluoroquinolone antibiotics such as ciprofloxacin that can slow caffeine clearance from the plasma, resulting in greater caffeine-related side effects [122]. Fluvoxamine, an SSRI used in the treatment of obsessive-compulsive disorder, has a dramatic effect on caffeine elimination by reducing clearance up to 90% and increasing half-life by >500% [123,124]. Examples of other caffeine drug interactions are with alcohol, cimetidine, anticonvulsants, CNS stimulants, sympathomimetic agents, theophylline, and oral contraceptives [125]. Caffeine also appears to improve the absorption of aspirin and slow the clearance of acetaminophen, both interactions of which could be considered beneficial in treating pain [121]. Several non-prescription products are readily available to consumers that contain a combination of caffeine and aspirin and/or acetaminophen. Ease of caffeine availability in tablet form without an official prescription is an advantage over some other adjuvant agents mentioned in this review, which require physician authorization in the US.
Re-assessing Evidence for Adverse Ocular Reactions Associated with Fluoroquinolones: Implications for Intracameral Use
Published in Ocular Immunology and Inflammation, 2022
Moxifloxacin is an 8-methoxyfluoroquinolone bactericidal antibiotic which inhibits DNA gryase and topisomerase IV. Moxifloxacin has broad spectrum activity against Gram-positive and Gram-negative bacteria, anaerobic bacteria and atypical organisms. Fluoroquinolone antibiotics are indicated for the treatment of complicated intra-abdominal infections, community acquired pneumonia, bacterial skin infections, acute bacterial exacerbations of chronic bronchitis, active tuberculosis, plague and conjunctivitis. Adverse events associated with systemic use of fluoroquinolones include tendonitis, tendon rupture, peripheral neuropathy and diplopia. Uveitis was not reported in pre-marketing trials of moxifloxacin, which was approved by the Food and Drug Administration in 1999.1 The first report of uveitis associated with orally administered moxifloxacin occurred in 2004. Subsequent reports expanded our understanding of clinical features of the condition and implicated additional drugs within the fluoroquinolone class.2,3
The pharmacology of antibiotic therapy in hidradenitis suppurativa
Published in Expert Review of Clinical Pharmacology, 2020
Claudio Marasca, Paolo Tranchini, Vincenzo Marino, Maria Carmela Annunziata, Maddalena Napolitano, Davide Fattore, Gabriella Fabbrocini
A combination therapy with rifampicin (10 mg/kg once daily), moxifloxacin (400 mg once daily), and metronidazole (500 mg thrice daily) administered for up to 12 weeks, with metronidazole discontinuation at week 6, may offer efficacy in Hurley stage I and II patient [68]. Moxifloxacin is a fluoroquinolone antibiotic. Quinolones act by binding and inhibiting two bacterial topoisomerases: Dna gyrase (topoisomerase 2, mainly in the gram-) and topoisomerase 4 (mainly in the gram +), determining the formation of pieces of DNA with activation of the bacterial cell apoptosis process. Furthermore, it has been demonstrated in vitro that moxifloxacin decreases the activity of TNF-α, IL-8, IL-1ß via stabilization of the IXb protein and prevents translocation of NF-κB to the nucleus. Moxifloxacin in particular has a bioavailability of 85%. It has a half-life of 9.6 h. the volume of distribution is rather high, even being able to overcome the blood–brain barrier. It is extensively metabolized, with the production of inactive metabolites and eliminated via the urine [69].