Introduction

Novacaine C13H20N2O2 . HCl, is a powerful pain killer, derived from cocaine, and is in the alkaloid family of drugs. It is a white crystaline, water soluble, odorless powder. On dissolution in water it forms an acidic solution.

Discovery

The anaesthetic properties of cocaine were demonstrated in 1884 by Dr. Carl Koller and was it regulary used until the end of the century, until the addictive properties made its use untenable.

Work began on formulating a chemically similar drug that had the anaesthetic qualities of cocaine, without its addictive properties. The first drug developed of any use was stovaine synthesised by Ernest Fourneau in 1904, this was followed by the similar procaine hydrochloride developed by Alfred Einhorn in 1905. He gave it the trade name 'Novocaine'; and it was introduced to the market by Heinrich Braun who showed it was a powerful anaesthetic, that was not addictive.

Mechanism And Use

Most commonly this drug is injected, and begins to work within about 2-5 minutes, its effects lasting for 1-2 hours (depending on dose of course). The anaesthetic properties are supposed to arise from the drug binding with the calcium receptors in cell membranes that affect the permeabilty of the membrane to sodium ions. As the nerve impulses are transmitted by an electrical potential formed from the concentration gradient of theseions inside and outside the nerve, novocaine helps block both the initiation and transmition of nerve impulses around its injection area. Novocaine is used for dentistry, childbirth, relief from lower back pain and with a vasoconstrictor drug can be used in minor surgery.

The Future

The synthetic cocaine analogues are still being developed and include such drugs as tropocaine, aucaine, monocaine, and lignocaine. These have such advantages as not eliciting a allergic response, which novocaine can in some people.

Structure



      O    O    
      \\  / \  /\   /\
       \\/   \/  \ /  \
         |        N
         |        |
        /\\       |
       /  \\       \
      ||    |       \
      ||    |
       \  //
        \//
         |
         |
         NH2 . HCl