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Local Anesthetic

A local anesthetic is a drug that causes reversible local anesthesia and a loss of nociception. When it is used on precise nerve pathways (nerve block), effects such as analgesia (loss of pain sensation) and paralysis (loss of muscle power) can be achieved.

Clinical local anesthetics fit in to one of two classes: aminoamide and aminoester local anesthetics. Synthetic local anesthetics are structurally related to cocaine. They differ from cocaine mostly in that they have no abuse possible and do not act on the sympathoadrenergic system, i.e. they do not create hypertension or local vasoconstriction, with the exception of Ropivacaine and Mepivacaine that do produce weak vasoconstriction.

Local anesthetics vary in their pharmacological properties and they are used in a variety of techniques of local anesthesia such as:

• Topical anesthesia (surface)
• Infiltration
• Plexus block
• Epidural (extradural) block
• Spinal anesthesia (subarachnoid block)

The local anesthetic lidocaine (lignocaine) is also used as a Class Ib antiarrhythmic drug.

In relieving local pains, lidocaine, single of ester type local anesthetics, has been used. To develop the lidocaine gels of improved local anesthetic effects, hydroxypropyl methylcellulose (HPMC) based bioadhesive polymer gel containing an enhancer was formulated. As the drug concentration in the gels increased up to 3%, the permeation rate of drug linearly increased, thereafter reaching a plateau. As the temperature of nearby solutions greater than before, the permeation of drug increased. The activation energy of drug permeation was 3.29 kcal/mol for lidocaine. The permeation rate of drug through skin was studied using various enhancers, such as glycols, non-ionic surfactants, and bile salts. Among the enhancers deliberate, diethylene glycol showed the greatest enhancing effects on drug permeation through skin.

The analgesic action was examined using a tail-flick analgesimeter. In the area under the efficacy curve (AUEC) of the rat-tail flick tests, lidocaine gel containing diethylene glycol showed about 3.89-fold increase in analgesic activity compared with the control. The adding of vasoconstrictor within the gels prolonged the analgesic effects. The result of this lessons supports that the bioadhesive gel with efficient anesthetic effect could be developed using HPMC with combination of enhancer and vasoconstrictor.

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