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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
Because of its rapid onset, rapid metabolism, and short duration of action, chloroprocaine has been primarily used in obstetric epidural analgesia or regional anesthetic techniques for day surgery (Tonder et al, 2020). Neurotoxicity, with motor and sensory deficits, has followed accidental subarachnoid injection; the antioxidant sodium bisulfite in the anesthetic solution has been implicated as the cause. This has been replaced by ethylenediaminetetraacetic acid, usually abbreviated as EDTA, in recent formulations.
Local Anesthetics
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Elena González Burgos, Luis Luis García-García, M. Pilar Gómez-Serranillos, Francisca Gómez Oliver
Chloroprocaine (Fig. 15.8) is an ultrashort-acting and rapid onset amino ester LA. Chloroprocaine as injectable solution is used for spinal anesthesia in adults and for epidural anesthesia in infants and children. Regarding pharmacokinetic properties of chloroprocaine, it does not bind to plasma proteins and that it undergoes enzymatic degradation by plasmatic pseudocholinesterases resulting in the renal metabolites beta-dimethylaminoethanol and 2-chloro-4-aminobenzoic acid (Veneziano and Tobis, 2017).
Epidural Anesthesia
Published in Bernard J. Dalens, Jean-Pierre Monnet, Yves Harmand, Pediatric Regional Anesthesia, 2019
Bernard J. Dalens, Jean-Pierre Monnet, Yves Harmand
Direct toxicity of local anesthetics on nerve fibers has been suggested by several studies. However, clinical and experimental studies do not confirm this hypothesis provided excessive concentrations are not administered. Accidental intrathecal administration of 2-chloroprocaine may produce neurological complications (due to either the low pH of the solution, the preservative, or the local anesthetic itself).
A comparison of approaches to identify possible cases of local anesthetic systemic toxicity in the FDA Adverse Event Reporting System (FAERS) database
Published in Expert Opinion on Drug Safety, 2018
Simon Dagenais, Richard Scranton, Andrew R. Joyce, Catherine C. Vick
The FAERS database drug file was searched to identify reports involving LB, bupivacaine, and other local anesthetics commonly administered by injection, using both complete drug names and partial drug names with wildcards (e.g. exp*, bup*, *cain, *cane, and lipo*) to allow for misspellings of relevant brand names and generic names (note: search query available upon request). Medications identified by these queries were reviewed by both a clinical pharmacist and an anesthesiologist to confirm that they were injectable local anesthetics , although the specific route of administration used for cases in FAERS was not always reported. This search identified injectable local anesthetics other than LB and bupivacaine, including articaine, chloroprocaine, dibucaine, etidocaine, levobupivacaine, lidocaine, mepivacaine, prilocaine, procaine, and ropivacaine; other drugs included in a previously published analysis of LB and LAST by Aggarwal (e.g. cocaine) were also included to compare our results with the most current literature on this topic [18].
Lipid-based carriers for the delivery of local anesthetics
Published in Expert Opinion on Drug Delivery, 2019
Daniele Ribeiro de Araújo, Lígia Nunes de Morais Ribeiro, Eneida de Paula
The fast metabolism of aminoesters by serum esterases can be blamed for the decline in chloroprocaine (CLP) and procaine (PRC) use over the years, although such rapid hydrolysis and minimal placental transfer justify CLP use in obstetric epidurals and its approval for intrathecal administration by the FDA [29]. From the aminoester family, only the most hydrophobic agent tetracaine (TTC) remained popular due to its potency, being the most used LA in ophthalmic procedures [30]. BZC and its butyl-derivative butamben (BTB) are also esters, but the lack of the amine group allows them to remain uncharged at physiological pH, explaining their low water solubility and restricted (topical) application [31].
Beta-blocker carteolol and oxprenolol produce cutaneous analgesia in response to needle pinpricks in the rat
Published in Neurological Research, 2023
There are a few cases where short durations of local anesthesia are needed. Thus, 2-chloroprocaine is recommended in patients receiving a short ambulatory procedure [25]. Our resulting data indicated that carteolol produced a greater duration of cutaneous analgesia than bupivacaine, and oxprenolol had a similar duration of action when compared to bupivacaine. The duration of drug action depends on a variety of factors, including permeation efficiency and lipophilicity [26] and plasma protein binding [27].