Ropivacaine Analysis

Must be considered as a local anesthetic any substance placed in contact with the nerve fibers, their origins or their endings, is capable of specifically and temporarily suspend their operation.

Local anesthesia was discovered in 1880. The early substance used was cocaine. One significant concern with cocaine, however, was its capacity to be addictive.

Extracted from the leaves of coca Erythroxylon by Scherzer in 1850, and then synthesized in 1860 by Niemann, cocaine is the first Local Anesthetic discovered. It was used in eye surgery in 1884 in Vienna by Karl Köller. Through his experiences, Köller had demonstrated that it was possible to paralyze the nerve endings in the cornea or conjunctiva of the eye by flowing a few drops of an aqueous

Amides displacing esters.The synthesis of ropivacaine (France), is one of the most recent developments in Local Anesthetic.

Local anesthetics are esters (e.g procaine, tetracaine) or amides (e.g lidocaine, mepivacaine). LAs are weak bases, their molecular weight is between 200 and 300 Da. Their structure includes an aromatic ring (hydrophobic), an intermediate chain and a hydrophilic pole
Their power, their duration of action, toxicity and diffusion rate may vary with the considered molecule. In general, these substances can be divided into short-acting products (procaine), intermediate-acting (lidocaine, mepivacaine) and long-acting (bupivacaine, ropivacaine).
The inhibitory effect first reached the fibers of the autonomic nervous system and fibers sensitive to pain, cold, warm to the touch, and finally the motor fibers; and conversely when the action of the anesthetic disappears.
This stopping of the peripheral nerve transmission is from an inhibition of the excitation potential due to a blocking of the opening of the sodium

Procaine is one of these local anesthetics.
Procaine is a local anesthetic, In addition to its local anesthetic properties; procaine also has a vasodilatory and antihypertensive action.

It belongs to the family from amino ester. It is, a para-aminobenzoic acid derivative. Synthesized in 1904 by the German chemist A.Einhorn (1857-1917).

In 1904, when Heinrich Braun (1903) German specialist renowned in local anesthesia devised a procaine-adrenaline mixture marketed by Hoechst under the Novocaïne® brand that was to dominate the market for 50 years. The Brand Name of Procaine is - NOVOCAIN® - comes from the Latin word "Novus," meaning "new," plus "cocaine widely used until the 1960s.

Procaine has greater effectiveness in getting the effects of cocaine as a local anesthetic and did not provoke the addictive potential or the other negative side effects. But despite this fact its popularity diminished ‪afterward‬ because Procaine has been dethroned by compounds less toxic local anesthetic agents and longer duration of action