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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
Allergic reactions are infrequent for amino ester LAs and almost exceptional in the ones that belong to amino amide group. In general, many of the reactions to LAs administrations are a consequence of the patient (anxiety, panic attack, or vasovagal responses) but they can be also the result of an unintended intravascular injection. Indeed, less than 1% of all reactions to LAs are considered as true allergic reactions (van Rooyen, 2010).
Local Anesthetics and Additives
Published in Bernard J. Dalens, Jean-Pierre Monnet, Yves Harmand, Pediatric Regional Anesthesia, 2019
Jean-Pierre Haberer, Bernard Jacques Dalens
Amino-esters are ester derivates of para-aminobenzoic acid (Table 3.1). Currently, cocaine (first clinical use in 1884), benzocaine (Americaine®, 1900), and procaine (Novocain®, 1905) are still used to some extent, but the most often used ester-linked agents are the following: Tetracaine (amethocaine, Pontocaine®, 1930) is used for spinal anesthesia.Chloroprocaine (Nesacaine®, 1955) is considered to be the least toxic local anesthetic, thus being usually recommended for short-duration procedures in poor-risk patients. However, there have been reports of neurological complications following accidental subarachnoidal administration (either due to the low pH of the anesthetic solution, the addition of preservatives, or the intrinsic neurotoxicity of this agent).10–12
Pharmacology for venous and lymphatic diseases
Published in Ken Myers, Paul Hannah, Marcus Cremonese, Lourens Bester, Phil Bekhor, Attilio Cavezzi, Marianne de Maeseneer, Greg Goodman, David Jenkins, Herman Lee, Adrian Lim, David Mitchell, Nick Morrison, Andrew Nicolaides, Hugo Partsch, Tony Penington, Neil Piller, Stefania Roberts, Greg Seeley, Paul Thibault, Steve Yelland, Manual of Venous and Lymphatic Diseases, 2017
Ken Myers, Paul Hannah, Marcus Cremonese, Lourens Bester, Phil Bekhor, Attilio Cavezzi, Marianne de Maeseneer, Greg Goodman, David Jenkins, Herman Lee, Adrian Lim, David Mitchell, Nick Morrison, Andrew Nicolaides, Hugo Partsch, Tony Penington, Neil Piller, Stefania Roberts, Greg Seeley, Paul Thibault, Steve Yelland
Local anaesthetics are weak bases, usually prepared as a hydrochloride salt to render them water-soluble. All act at neuronal cell membranes to inhibit sodium transfer, and reversibly decrease the rate of membrane depolarization and repolarization. Aminoamides are metabolized in the liver, while most amino-esters are metabolized by pseudocholinesterase.
Recent advances in polymeric materials for the delivery of RNA therapeutics
Published in Expert Opinion on Drug Delivery, 2019
David Ulkoski, Annette Bak, John T. Wilson, Venkata R. Krishnamurthy
A variety of hydrolysable gene delivery systems have been developed to increase biodegradability and facilitate payload release in endosomal environments. As previously discussed, polyesters and polyacrylates have been widely investigated due to their susceptibility to hydrolysis in basic and acidic conditions (i.e. poly(β-amino esters)). Acetals, ketals, and hydrazones have also been used thoroughly employed as pH-labile linkages for the delivery of nucleic acids (Figure 4(b)) [216–218]. Although coformulations with pH-labile systems can induce transfection, the endosmolytic activity of polyesters and polyacrylates by themselves are limited and require additional components that provide mechanistic responses (e.g. ionizability) to control nanoparticle disassembly and efficient release of the RNA cargo.
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
After the discovery of cocaine and the synthesis of the first synthetic LA in 1905 (procaine), new agents have been developed throughout the twentieth century [12], as depicted in Figure 1. The commercially available LA agents, mainly from the ester/aminoester and aminoamide families [13,14], have different physicochemical and pharmacological properties and are used in a variety of doses (Table 1) and routes of administration. The effects of local anesthetics are relatively brief, lasting for hours after a single administration, which is insufficient for the treatment of prolonged, acute, or chronic pain (Table 1). Among them, bupivacaine (BVC) and lidocaine (LDC) are the most used agents worldwide, for infiltrative anesthesia in surgical and ambulatory procedures, respectively [15]. Benzocaine (BZC) prevails in topical formulations [16,17] for the skin, although the eutectic mixture of LDC and prilocaine (PLC), known as EMLA®, has gained increasing importance for cutaneous anesthesia [18].
Lung cancer: active therapeutic targeting and inhalational nanoproduct design
Published in Expert Opinion on Drug Delivery, 2018
Nasser Alhajj, Chin Fei Chee, Tin Wui Wong, Noorsaadah Abd Rahman, Noor Hayaty Abu Kasim, Paolo Colombo
Direct conjugation involves covalent bond formation between the functional moieties of biomolecules and matrix materials of the nanocarrier. The chemical functional groups of the nanocarrier matrix that are suitable for direct conjugation include amine, aldehyde, carboxyl, and others. These functional groups can be coupled with carboxyl, isothiocyanate, hydrazide, or amine groups of the biomolecules (Table 1). The formation of amide bond through reacting an amine group with a N-hydroxysuccinimidyl-activated carboxylic compound is a very popular direct conjugation approach (Table 1a). Using this synthesis method, a carboxylic compound is first reacted with N-hydroxysuccinimide (NHS) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC) to produce an acyl amino ester. The intermediate is then reacted with a primary amine where amide bond is formed. This method receives a widespread application because it can be conducted in an aqueous medium with slightly alkaline conditions (pH 7 ~ 9) without the need for a complex solvent system, though it is challenging to align the binding orientation of the biomolecules on a nanocarrier matrix with multiple amine groups [108].