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Antibiotic-Induced Endotoxin Release: Important Parameters Dictating Responses
Published in Helmut Brade, Steven M. Opal, Stefanie N. Vogel, David C. Morrison, Endotoxin in Health and Disease, 2020
Jesse J. Jackson, Helmut Kropp
Morphological variations and LPS release are associated with changes in antibiotic concentrations—especially at subinhibitory antibiotic levels where high amounts of endotoxin are also released (8–16). Pharmacokinetic studies in humans suggest that concentrations of important β-lactam antibiotics (i.e., imipenem, meropenem, and ceftazidime) exist in vivo below the effective inhibitory concentrations from one third to one half of the suggested dosing schedules (8,19–21).
Antimicrobials in Pregnant Women
Published in Firza Alexander Gronthoud, Practical Clinical Microbiology and Infectious Diseases, 2020
If antibacterial treatment is indicated, avoid quinolones, tetracyclines, voriconazole, flucytosine, ganciclovir, foscarnet and cidofovir. Aminoglycosides and fluconazole can be given for a short course. Safe to use are β -lactam, glycopeptides, daptomycin, nitrofurantoin, fosfomycin, metronidazole and clindamycin, acyclovir and amphotericin B. Trimethoprim/sulfamethoxazole may be used during the second trimester until 32 weeks’ gestation.
Urolithiasis
Published in Manit Arya, Taimur T. Shah, Jas S. Kalsi, Herman S. Fernando, Iqbal S. Shergill, Asif Muneer, Hashim U. Ahmed, MCQs for the FRCS(Urol) and Postgraduate Urology Examinations, 2020
Thomas Johnston, James Armitage, Oliver Wiseman
Beta (β)-lactam antibiotics contain a β-lactam ring in their molecular structure, which act as an irreversible inhibitor of the enzyme transpeptidase, which is used by the bacteria to cross-link peptidoglycan in their cell walls. β-lactam antibiotics include penicillin derivatives (penams such as amoxicillin), cephalosporins (cephems such as cephalexin) and carbapenems (such as meropenem or itrapenem). Aminoglycosides (gentamicin) are important treatments against Gram-negative infections. They act by inhibiting protein synthesis by binding to ribosomal RNA, which disrupts the integrity of the bacterial cell wall membrane. Sulphonamides are one of the oldest groups of antibiotic compounds (trimethoprim-sulphonamide) in use. They are structurally similar to para-aminobenzoic acid (PABA) and act as a false substrate for the enzyme dihydrofolate synthase, which blocks the synthesis of folate. This results in inhibition of DNA synthesis and therefore bacterial cell growth. Fluoroquinolone (ciprofloxacin) antibiotics inhibit the enzyme DNA gyrase, which is essential for transcription bacterial DNA synthesis, and results in irreversible damage and bacterial cell death. Nitrofurantoin is reduced inside the bacterial cell by flavoproteins (nitrofuran reductase) to multiple intermediates that attack ribosomal proteins (ribosomal subunit 50 S and target 23 S ribosomal RNA, DNA and pyruvate metabolism (Table 16.2).
Acute abdomen: a rare presentation of group a streptococcal infection
Published in Acta Chirurgica Belgica, 2023
Jelle Lubach, Marie Vannijvel, Hendrik Stragier, Yves Debaveye, Albert Wolthuis
Even though postponing surgery is controversial, taking blood, urinary and vaginal cultures and starting broad-spectrum antibiotics combined with supportive measures is essential. Of course, the choice of empirical antibiotic therapy should be conform institution guidelines with knowledge of local resistance patterns. A broad-spectrum antibiotic like a combination of piperacillin-tazobactam to treat septic patients with a likely abdominal focus should be started empirically. S. pyogenes is known to be susceptible to penicillin and is advised after cultures are positive. Clindamycin reduces streptococcus virulence factors and endotoxin production in patients with group A hemolytic streptoccus infections and most likely improves clinical outcome [12]. According to a large, retrospective multicentre cohort study from Babiker et al. [13], association to β-lactam antibiotics reduces in-hospital mortality significantly (6.5 vs 11.0%).
Jumping into the future: overcoming pharmacokinetic/pharmacodynamic hurdles to optimize the treatment of severe difficult to treat-Gram-negative infections with novel beta-lactams
Published in Expert Review of Anti-infective Therapy, 2023
The choice of appropriate antibiotic dosing in critically ill patients with severe AKI requiring CRRT is one of the most challenging scenarios for clinicians. Novel beta-lactams share common physicochemical and PK features. They are hydrophilic compounds with low molecular weight, limited volume of distribution, low plasma protein binding, and almost complete renal elimination. Overall, this makes them very prone to remarkable CRRT extraction [12]. Among novel agents, only FDC has specific dosing regimens labeled according to CRRT mode and/or effluent flow rate. Studies about the PKs of novel beta-lactams during CRRT are growing, but unfortunately mostly are limited to single case reports [12,87–90], and the findings are difficult to be applied extensively in daily clinical practice.
Design and biological evaluation of substituted 5,7-dihydro-6H-indolo[2,3-c]quinolin-6-one as novel selective Haspin inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2022
Sreenivas Avula, Xudan Peng, Xingfen Lang, Micky Tortorella, Béatrice Josselin, Stéphane Bach, Stephane Bourg, Pascal Bonnet, Frédéric Buron, Sandrine Ruchaud, Sylvain Routier, Cleopatra Neagoie
We have synthesised a series of new Lamellarin analogues using the indolo[2,3-c]quinolone-6-one core. The analogues were obtained after a sequence involving (i) a palladium catalysed cross coupling reaction between 2-indolic esters and 2-nitrophenyl boronic acids as building blocks, and (ii) a cyclic lactam formation involving a reduction and an annelation. Twenty-two novel derivatives were synthesised and evaluated for their inhibitory activity on Haspin kinase and on a panel of 7 other protein kinases for selectivity assessment. Among this series, 8 compounds inhibited Haspin kinase with IC50 below 10 nM. Docking studies showed a double hydrogen bond between the lactam and the hinge region of the kinase. The most active compounds 49 and 55 possess IC50 of 1 and 2 nM respectively with selectivity towards the parent kinases DYRK1A and CLK1 between a 13 and 65-fold factor. Furthermore, the most selective compound 55 exerted an interesting cellular effect on the osteosarcoma U-2 OS cell line as well as on U-2 OS and colorectal carcinoma HTC116 spheroid viability. Additionally, we further validated the functionality of compound 55 on endogenous Haspin activity in cells. This interesting Haspin inhibitor will be used in further studies to develop efficient and selective Haspin inhibitors.