Lidocaine Anesthetic : what is it

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Author: seandrnumb

Lidocaine or lignocaine is a common local anesthetic and antiarrhythmic drug. Lidocaine is used topically to relieve itching, burning and pain from skin inflammations, injected as a dental anesthetic or as a local anesthetic for minor surgery. It is a substance that has been used for many years as anesthetics in medical and dental offices. Dr. Numb contains more of a pure form of lidocaine which acts as the numbing anesthetic cream for the skin. The purity is very important, because not all lidocaine is manufactured and refined as Dr. Numb has been. It is a NON-OILY topical anesthetic cream that contains purest Lidocaine and Prilocaine, the highest amount allowed by Food and Drug Administration.

High-quality Formulation and Manufacturing

The purity is very important, because not all lidocaine is manufactured.Commercially available Food and Drug Administration (FDA) approved numbing creams include various non-steroidal anti-inflammatory agents, DrNumb (5% lidocaine and 5% benzocaine), the Lidoderm Patch (Endo Pharmaceuticals, Chadds Ford, PA) and Capsaicin cream different doses. All lidocaine anesthetic is a membrane stabilizing drugs; they reversibly decrease the rate of depolarization and repolarization of excitable membranes (like nociceptors). Tho ugh many other drugs also have membrane stabilizing properties, all are not used as local anesthetics, for example propranolol. Lidocaine anesthetic drugs act mainly by inhibiting sodium influx through sodium-specific ion channels in the neuronal cell membrane, in particular the so-called voltage-gated sodium channels. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Lidocaine anesthetic drugs bind more readily to sodium channels in activated state, thus onset of neuronal blockade is faster in neurons that are rapidly firing. This is referred to as state dependent blockade.

Lidocaine anesthetics are weak bases and are usually formulated as the hydrochloride salt to render them water-soluble. At the chemical's pKa the protonated (ionised) and unprotonated (unionized) forms of the molecule exist in equilibrium but only the unprotonated molecule diffuses readily across cell membranes. Once inside the cell the lidocaine anesthetic will be in equilibrium, with the formation of the protonated (ionised form), which does not readily pass back out of the cell. This is referred to as "ion-trapping". In the protonated form, the molecule binds to the local anesthetic binding site on the inside of the ion channel near the cytoplasmic end. Acidosis such as caused by inflammation at a wound partly reduces the action of lidocaine anesthetics. This is partly because most of the lidocaine anesthetic is ionized and therefore unable to cross the cell membrane to reach its cytoplasmic-facing site of action on the sodium channel. All nerve fibers are sensitive to lidocaine anesthetics, but generally, those with a smaller diameter tend to be more sensitive than larger fibers. Lidocaine anesthetics block conduction in the following order: small myelinated axons (e.g. those carrying nociceptive impulses), non-myelinated axons, and then large myelinated axons. Thus, a differential block can be achieved (i.e. pain sensation is blocked more readily than other sensory modalities).

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