Anaesthetic agents local

The pseudo-barbiturate , 2-methyl-3-o-tolylquinazolin-4(3H)-one (methaqualone, Revonal 1017) has an even wider spectrum of activities than do the barbiturates proper it appears to be quite widely used as- a sedative, hypnotic, anticonvulsant, antispasmodic and local anaesthetic agent (63MI21301, b-75MI21301>. 

The site http //www.oyston.com/history has afascinating history of the topic, mentioning such early anaesthetics as ether, chloroform and nitrous oxide. Local anaesthetics are often injected in the form of liquids or solutions, see the article pharmacology of local anaesthetic agents by a British anaesthetist, Dr J. M. Tuckley, may be found... 

The analogous 4- (19, X = H2) and 5-phenyltetrahydro-l-benzazepines are less active than the 3-phenyl isomers [30]. The corresponding 4-phenyl-benzazepin-2-one (19, X = O) shows moderate antiarrhythmic activity [30] and is claimed to be useful for the treatment of neurogenic or carcinogenic auricular and ventricular fibrillation and as an antihistaminic or local anaesthetic agent [37]. Introduction of an aminoalkyl group, such as 2-piperidinyl-... 

Procaine is a derivative of p-aminobenzoic acid, and is a one of the oldest used ester-type local anaesthetic agents [1], The compound was originally developed by Einhom [2,3], and later with and Uhlfelder [4]. This anti-arrhythmic drug itself has a short half-life, but is able to form salts with other drugs which causes an increase in the duration of action [5]. 

Jellies are transparent or translucent, non-greasy medicated semi-solid preparation used externally, sometime containing local anaesthetic agent also e.g. Lignocaine jelly. 

Allergic reactions are characterised by cutaneous lesions, urticaria, edema or anaphylactoid reactions may occur as a result of sensitivity to local anaesthetic agent. 

Table 5.1 Pharmacokinetic characteristics of local anaesthetic agents...

Figure 5.4. Stmctures of cocaine (the first local anaesthetic), the standard local anaesthetic agent lidocaine, and the model compounds aniline and diethylamine.

Columb M O 2001 Local anaesthetic agents. Anaesthesia and Intensive Care Medicine 2 288-291... 

Reiz S, Nath S. Cardiotoxicity of local anaesthetic agents. Br J Anaesth 1986 58(7) 736 6. 

In accordance with the observation that the anti-microbial effect of gases like nitrogen dioxide, carbon dioxide or xenon can be related to the effects of general anaesthetics, it seems natural to relate the well-knovm anti-microbial effect of cationic surfactants to local anaesthetic agents. The first type of perturbants shifts the actual transition in the direction La - whereas the second t)rpe of agent is expected to shift the transition in the opposite direction. It should be mentioned that quaternary ammonium surfactants such as cetyltrimethyl ammonium bromide in micellar solution in water were found to transform the cubic phase into the La phase [34]. 

In summary, microemulsions exhibit a great potential in improving the delivery of local anaesthetic agents and the commercialisation of lidocaine microemulsion gel (Tropicaine ) is sufficient to establish their utility. 

In fact, N2O is usually employed alone as an anaesthetic agent during some special localized dental procedures only. However, most frequently N2O is utilized with other volatile anaesthetics to cause a sufficient desirable depth of anaesthesia essentially required for various surgical procedures . 

Local anaesthetics are used to abolish the sensation of pain in a restricted area of the body and for minor surgical operations when loss of consciousness is not desirable. The area is determined by the site and the technique of administration of the anaesthetic agent. The main uses are as follows ... 

It is regarded as an all-purpose soluble local anaesthetic agent. The onset and duration of action is almost similar to that of lignocaine. 

R. 1. Jeppsson, Comparison of pharmacological effects of some local anaesthetic agents when u.sing wafer and lipid emulsion as injection vehicles. Acta Pharmacol. Toxicol., 36 299-311, 1975. 

Carlsson, F., Elofsson, U., Arnebrant, T. and Malm-sten, M., Interactions between local anaesthetic agents and poly (A -isopropylacrylamide) through phase behaviour, surface tension, and adsorption measurement, J. Colloid Interface ScL, 233, 320-328 (2001). 

Uses cinchocaine is used as an anaesthetic agent for spinal anaesthesia a component in rectal medications used in inflammation of the anus and for the symptomatic treatment of hemorrhoids and fissures in the anus local anesthetic agent Cross lidocaine. PA A... 

A final example is the tme-step, three-component variant of the Ugi reacticm (Scheme 8.10), according to which an important local anaesthetic agent, xylocaine (28), was synthesized from formaldehyde, diethylamine and 2,6-dimethyl-pheny-lisocyanide [45]. 

Anaesthetic agents Liquid Gaseous Local Halothane Nitrous oxide Propellant 11 12... 

Rop, P.P. Grimaldi, F. Bresson, M. Fornaris, M. Viala, A. Liquid chromatographic analysis of cocaine, benzoylecgonine, local anaesthetic agents and some of their metabolites in biological fluids, J.Liq.Chro-matogr., 1993, 16, 2797—2811. 

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