Local Anesthetics in Dentistry. Bach Van Pham Southern Methodist University November 30, 2004. What are local anesthetics?. Local anesthetic: produce loss of sensation to pain in a specific area of the body without the loss of consciousness. History. Coca leaves from the genus Erythroxylum
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Bach Van Pham
Southern Methodist University
November 30, 2004
Used nitrous oxide gases and ether for minor surgery in dentistry
Give a low concentration of cocaine; it slows down the release of the drug into the bloodstream causing little side effectsSide Effects of Cocaine and Solutions
In 1898, Professor Heinrich Braun introduced procaine as the first derivative of cocaine, also known as the first synthetic local anesthetic drug
Trade name is Novocaine®
Took too long to set (i.e. to produce the desired anesthetic result)
Wore off too quickly, not nearly as potent as cocaine
Classified as an ester; esters have high potential to cause allergic reactions
Caused high conc. of adrenaline resulted in increasing heart rate, make people feel nervous
Most dentists preferred not to used any local anesthetic at all that time; they used nitrous oxide gas.
Today, procaine is not even available for dental procedures.Procaine replaced Novocaine cocaine Problems
--Amide link b/t intermediate --Ester link b/t intermediate chain and chain and aromatic ring aromatic ring
--Metabolized in liver and very --Metabolized in plasma through soluble in the solution pseudocholinesterases and not
stable in the solution
--Cause allergic reactions
Side effects of epinephrine
---For adult whose weight is 150lbs and up, maximum dose Articaine and lidocaine is about 500mg
---For children, the dosage reduced to about 1/3 to ½ depending on their weight.
The doses are not considered lethal.
Some common toxic effects:
--light headedness ---shivering or twitching --seizures
--hypotension (low blood pressure) --numbness
--Produce very long acting anesthetic effect to delay the post operative pain from the surgery for as long as possible
--0.5% solution with vasoconstrictor
--toxicity showed by the pKa is very basic
--Onset time is longer than other drugs b/c most of the radicals (about 80%) bind to sodium channel proteins effectively
--most toxic local anesthetic drug
--Identical pKa and same conc. with lidocaine
--Almost same duration as lidocaine
--Less toxic in higher doses than lidocaine b/c small vasodilatory activity
--newest local anesthetic drug approved by FDA in 2000
--Same pKa and toxicity as lidocaine, but its half life is less than about ¼ of lidocaine
--Used with vasoconstrictor.
--Enters blood barrier smoothly
--The drug is widely used in most nations today