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Antimicrobials during Pregnancy
Published in “Bert” Bertis Britt Little, Drugs and Pregnancy, 2022
The frequency of birth defects with exposure to tetracyclines during the first trimester was reported in the Swedish Registry for 2920 infants (Kallen, 2019). This included 1653 infants exposed to doxycycline, 755 to lymecycline, 2 to metacycline, 36 to oxytetracycline, 344 to tetracycline, and 2 to minocycline. The type of tetracycline was not specified in 139 exposures.
High-Performance Liquid Chromatography
Published in Adorjan Aszalos, Modern Analysis of Antibiotics, 2020
Joel J. Kirschbaum, Adorjan Aszalos
Doxycycline in serum was quantified using an octylsilane column with a mobile phase of acetonitrile-0.1 M citric acid (24:76) flowing at 0.5 ml/min into a detector set to 350 nm [399]. This system can also separate OTC, TC, demeclocyline, methacycline, and a metabolite of doxycycline. The limit of detection is 50 ng/ml.
Classifications
Published in Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani, Pharmacology in 7 Days for Medical Students, 2018
Fazal-I-Akbar Danish, Ahmed Ehsan Rabbani
Based on sourceNaturalChlortetracyclineOxytetracyclineDemeclocyclineSemi-syntheticClomocyclineDoxycyclineLymecyclineMinocyclineMethacyclineTetracycline
Analysis of the clinical characteristics of tigecycline-induced hypofibrinogenemia
Published in Journal of Chemotherapy, 2023
Haibo Lei, Xiang Liu, Zuojun Li, Chunjiang Wang
Tigecycline belongs a new generation of tetracycline antibiotics developed after doxycycline, minocycline, and metacycline. It is derived by adding a 9-t-butyl-glycylamido side chain to the central skeleton of minocycline, which confers a broader spectrum of activity [17]. Tigecycline exhibits linear pharmacokinetics (PK) and has a high volume of distribution (7.2-8.6 L/kg), high plasma protein binding (71-89%) and a long half-life (t½) of 37-67 h [18]. It also undergoes rare metabolism and is mainly excreted by the liver. Twenty-two percent of the tigecycline prototype is excreted by the kidneys. No clinically relevant drug interactions have been identified, and PKs are not affected by renal dysfunction or removed by hemodialysis [19]. The currently recommended standard dose is an initial 100 mg loading followed by 50 mg IV every 12 hours by a 30-60 min infusion. In patients with severe liver damage (Child Pugh C), the initial dose of tigecycline remains unchanged, and the maintenance dose is reduced by 25 mg every 12 hours [20]. Recent studies have shown that high-dose tigecycline (HDT) (100-200 mg q24h daily after a loading dose of 200-400 mg) is the optimal dosing strategy for serious systemic infections or infections due to MDR or XDR gram-negative bacilli (GNB) since it permits prolonged exposure at effective serum/tissue concentrations [21].
Amiodarone induces epithelial-mesenchymal transition in A549 cells via activation of TGF-β1
Published in Drug and Chemical Toxicology, 2020
Jie Weng, Hao Chen, He Wu, Mengyun Tu, Zhibin Wang, Daqing Chen, Zhiyi Wang, Chan Chen
In 2005, Willis et al. have confirmed that E-cadherin and α-SMA were commonly expressed in IPF patients pulmonary tissues, meaning that epithelial cells undergo phenotype transformation in the IPF lung tissues and the possibility of EMT was first time described (Ramos et al., 2010). In 2006, Kim et al. (2006) reported AECs were progenitors of fibroblasts in vivo and ECM was a key regulator of EMT during fibrogenesis. Xi and colleagues identified methacycline could suppress the fibrogenesis by inhibiting EMT, and further supported the EMT signaling in the pulmonary fibrosis (Xi et al., 2014). So, more evidences to support that fibroblasts and myofibroblasts in the pulmonary fibrosis were originated from alveolar epithelial cells via EMT (Willis and Borok, 2007; Tanjore et al., 2009). To elucidate whether amiodarone induced EMT of A549 cells. After stimulation by amiodarone, A549 cells acquired spindle-shaped, elongated, fibroblast-like morphology, with low cell adhesion. We observed amiodarone could induce pulmonary fibrosis through EMT by increasing α-SMA and reducing the E-cadherin via immunocytochemical analysis. We further found that amiodarone regulated E-cadherin and α-SMA expression in dose- and time-dependent manner. Therefore, we considered that amiodarone-induced pulmonary fibrosis was related with EMT, may be a major cause. Next, we investigated the underlying molecular mechanism of AIPF.
The safety of antimicrobials for the treatment of community-acquired pneumonia
Published in Expert Opinion on Drug Safety, 2020
Carla Bastida, Dolors Soy, Antoni Torres
Tetracycline antimicrobials exhibit a broad spectrum of activity against numerous pathogens, including Gram-positive and Gram-negative bacteria as well as atypical organisms, and are used in the management of several infectious diseases. They were first obtained naturally from different species of Streptomyces spp. (i.e. chlortetracycline, oxytetracycline, tetracycline, and demeclocycline). Later, semi-synthetic tetracyclines were developed (i.e. lymecycline, methacycline, minocycline, rolitetracycline, and doxycycline), with doxycycline and minocycline currently the most frequently prescribed. Subsequent research and modifications within the four core rings of tetracyclines has led to the development of new analogs, including tigecycline (a glycylcycline), eravacycline (a fluorocycline), and omadacycline (an aminomethylcycline) [52]. The most recent agent to be approved for this antimicrobial class was omadacycline [53], which is indicated for the treatment of adults with CAP. Both oral and intravenous formulations are available, and it shares the mechanism of action and PK characteristics of the class. Table 3 provides an overview of the classification of tetracyclines by their PK properties and spectrum of activity [54,55].