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Pharmacology of Local Anesthetics
Published in Pamela E. Macintyre, Stephan A. Schug, Acute Pain Management, 2021
Pamela E. Macintyre, Stephan A. Schug
Amide local anesthetic drugs are metabolized in the liver and the elimination half-lives vary from about 1.5 to 3.5 hours. These drugs rarely, if ever, cause true allergic reactions confirmed by standardized tests, although patients may be allergic to the antioxidants and preservatives contained in some local anesthetic solutions (sulfites, latex particles, and benzoates) (Lirk et al, 2018). These were a particular problem with multidose vials, which have been discontinued in most countries. Some patients reporting an “allergy” to these drugs may have experienced effects due to the systemic absorption of epinephrine, a previous allergic reaction to an ester local anesthetic, or had a vasovagal response to the injection (Lirk et al, 2018).
Miscellaneous
Published in Bobby Krishnachetty, Abdul Syed, Harriet Scott, Applied Anatomy for the FRCA, 2020
Bobby Krishnachetty, Abdul Syed, Harriet Scott
The greater protein binding of bupivacaine and ropivacaine, compared with that of lidocaine, likely accounts for their lower fetal blood levels. Also, the esters are metabolised rapidly to have minimal effects on the fetus as very little remains in the maternal circulation to cross the placenta. Amide local anaesthetics are more likely to cross the placenta.
Role of Plant-Based Bioflavonoids in Combating Tuberculosis
Published in Megh R. Goyal, Durgesh Nandini Chauhan, Assessment of Medicinal Plants for Human Health, 2020
Alka Pawar, Yatendra Kumar Satija
Current cure for TB consists of four months of rigorous treatment with first-line drugs (namely: isoniazid, rifampicin, ethambutol, and pyrazin-amide), which is tailed by continuation phase of four to five additional months of treatment with second-line drug therapy (namely: isoniazid and rifampicin).12 The condition has worsened because of rise in drug resistance,15 HIV coinfection,45 patient defiance along chemotherapy, and variable effectiveness of BCG vaccine. There is utmost importance to (1) develop new anti-TB drugs, which should have prospects against both active and latent/persistent TB bacteria; (2) to reduce duration of therapy to encourage patient’s compliance; and (3) to minimize phenomenon of drug resistance in mycobacterium species.12,32 Therefore, the search for novel anti-tubercular drugs is an urgent need in order to fade out the menace of drug resistance and to eventually eliminate TB.
The in vitro anti-inflammatory activity of N-antipyrine-3,4-dichloromaleimide derivatives is due to an immunomodulatory effect on cytokines environment
Published in Immunopharmacology and Immunotoxicology, 2023
Eduarda Fratoni, Lais Cristina Theindl, Julia Salvan da Rosa, Marcus Vinicius Pereira dos Santos Nascimento, Tatiana da Rosa Guimarães Maciel, Fátima de Campos-Buzzi, Eduardo Monguilhott Dalmarco
Cyclic imides and their analogs have long been used by the pharmaceutical industry for the development of many drugs. Among these, the subclasses of maleimides have demonstrated therapeutic potential as antifungals, antibacterials, and insecticides [18,26]. In recent years, these compounds have also been investigated for their analgesic and anti-inflammatory action, particularly N-antipyrine-3,4-dichloromaleimide [19,20]. Mahle et al. synthesized twenty-two compounds derived from N-antipyrine-3,4-dichloromaleimide that were evaluated for their antifungal and analgesic activities [21]. Interestingly, in these experiments, many compounds produced a significant reduction in the second or late phase of the formalin test — an inflammatory environment orchestrated by the release of inflammatory mediators [27]. In this context, we decided to investigate more deeply the possible anti-inflammatory effect of the six selected compounds on the levels of important inflammatory mediators secreted by macrophages.
Promising therapeutic approaches for relapsed/refractory multiple myeloma
Published in Hematology, 2022
Multiple myeloma (MM), the second-most frequent hematologic tumor, is an incurable malignancy of the plasma cells, although several available treatments can provide remission and prolong survival [1]. In 2021, about 34,920 new cases will be diagnosed with MM and 12,410 people will die from MM in the U.S. The current 5-year survival rate (47%) is much better than in 1999 (31%) [2]. The availability of advanced agents, including proteasome inhibitors (PIs), immunomodulatory imide drugs (IMiDs) and monoclonal antibodies (MoAbs), are responsible for these substantially improved outcomes [3]. However, these conventional therapies are not curative and nearly every patient will eventually relapse and face a poor prognosis [4]. In addition, relapsed MM is typically characterized by genetic alterations that lead to subclonal evolution, making it more resistant to treatment. Consequently, patients experience shorter durations of remission and eventually develop relapsed/refractory MM (RRMM) [5].
Recent real-world treatment patterns and outcomes in US patients with relapsed/refractory multiple myeloma
Published in Expert Review of Hematology, 2020
Amanda S. Bruno, Jenny L. Willson, Joanna M. Opalinska, Jeanenne J. Nelson, Orsolya E. Lunacsek, Dana R. Stafkey-Mailey, Joanne P. Willey
Patient characteristics of the chart review population are provided in Table 1. During the study period, 183/456 (40.1%) patients received three lines, 75/456 (16.4%) four lines, 29/456 (6.4%) five lines, and 13/456 (2.9%) six lines of therapy. Consistent with findings in the EMR analysis, bortezomib and lenalidomide were the most commonly received agents during first-line treatment, 357/456 (78.3%) and 278/456 (61.0%) patients, respectively; the number of patients receiving these agents decreased in subsequent lines as greater use of newer treatments was noted in third, fourth, and fifth lines (Table 2). It should also be noted that few patients in clinical practice received chemotherapy in this study. Instead, use of immunomodulatory imide drugs (IMiDs) and proteasome inhibitors was much more commonly observed. Ongoing analyses (data on file) demonstrate similar trends relating to chemotherapy use.