N OVOCAINE

A Description by Catherine
Pietrzak
Novocaine is a local anesthetic that is used in surgical and non-
surgical dental procedures, such as tooth restorations due to dental
caries or tooth extractions (i.e. removal of third molars).
Novocaine diminishes the pain due to the dental procedures.

BRIEF HISTORY In the early 1900s, Novocaine, scientifically known as Procaine,

OF NOVOCAINE was invented. German chemist, Alfred Einhorn developed the
chemical compound Procaine. Before this, Cocaine was once
the most used local anesthetic for common dental procedures.
Cocaine was used to numb tooth pain of the Incas and societies
that grew cocoa leaves. Cocaine constricts blood vessels to
reduce bleeding, but it has a major adverse effect of being
addictive. Due these unfavorable outcomes, a new product,
Procaine, was invented and upon the invention of the syringe,
Novocaine became available to the masses.

CHEMICAL The chemical structure of Novocaine is C13H20N2O2.

STRUCTURE
AND
PROPERTIES

http://upload.wikimedia.org/wikipedia/commons/7/77/Thc.pdb.gif

Figure 1: Structure of Novocaine

Novocaine is an odorless white, powdery substance. It is

chemically derived from Cocaine. It is also a water soluble
product. Typically, Novocaine is chemically combined with
hydrochloric acid to form Procaine hydrochloride. This is the
form that is typically administered to dental patients prior to
minor dental surgeries.

It is administered by injecting the mouth and gums using a

dental syinge. The Novocaine’s numbing effects will be felt
within 2-3 minutes and it will wear off in 2-3 hours after
application. Novocaine acts by blocking the nerves in the
mouth from so that the body will not feel any pain. Unlike
Cocaine, Novocaine also does not have a euphoric effect on
the brain and is therefore not addictive.
 HOW DOES The pain sensation is due to stimulation of the nerve receptors
NOVOCAINE in the targeted area of the body that send a pain signal to the
WORK IN brain. The signal is transmitted by moving neurotransmitters
from one nerve to the next. Essentially, neurotransmitters act
THE BRAIN? as the messengers of the brain. Neurotransmitters contain
chemicals that tell the brain how to respond to various stimuli.
In this case, the stimulus is pain.

In order to not feel pain, a pain-relieving drug, such as

Novocaine, acts by interfering with the brain’s pain receptors.
The drug may block the neurotransmitters that send the pain
signal from nerve to nerve by either inhibiting their release
from the original nerve (presynaptic vesicle) or by blocking the
neurotransmitter receptors on the next nerve (postsynaptic
vesicle) that will pass along the signal as depicted in Figure 2
below. A drug may also change the brain’s interpretation of
the signal. In this case, Novocaine acts by interfering with the
brain’s neurons to block neurotransmitter receptors on the
postsynaptic vesicle from accepting the signal. It also blocks
the sodium channel which constricts the movement of sodium
into the cell.

http://www.columbia.edu/cu/psychology/courses/1010/mangels/neuro/transmission/transmission.gif

Figure 2: The Process of Neurotransmission

 Novocaine also acts as a vasodilator. When vasodilation
occurs the blood vessels (arteries, arteriole, and veins) widen
which increases blood flow and decreases blood pressure in
the blood vessels. When working on a patient, vasodilation is
not optimal because more blood flows to the surgerical
wound, which makes the patient bleed out more. Due to this,
vasoconstrictor, epinephrine, is coadministered with
procaine. A vasoconstrictor acts to reduce the bleeding and
constrict vessels and increases blood pressure (As seen in
Figure 3).

http://www.nlm.nih.gov/medlineplus/ency/images/ency/fullsize/8983.jpg

Figure 3: Vasoconstriction
 The breakdown or metabolism of Novocaine in the body
occurs in the blood vessels. Specifically it is metabolized in
NOVOCAINE the blood plasma. Pseudocholinesterase (structure seen in
METABOLISM Figure 3) is an enzyme that breaks down novocaine into
para-amino benzoic acid (PABA) by hydrolysis. It is then
metabolized further by the kidneys and excreted from the
body in the urine.

http://en.academic.ru/pictures/enwiki/65/Acetylcholinesterase-1EA5.png

Figure 4: Structure of Pseudocholinesterase

Most allergic reactions caused by Novocaine are not due to

the Novocaine product itself, but instead it is due to
inefficient pseudochlolinesterase enzyme which does not
properly breakdown the Novocaine leading to increased
levels of the local anesthetic and increased toxicity.

WHEN NOT TO • The effects of Novocaine are not as effective when a

USE NOVOCAINE person has high levels of anxiety.
o It is recommended that dental patients come in
with a calm and clear mind so that fear does
not set in.
o Dentists should be informing and educating
their patients to the best of their ability to
lower the anxiety levels of their patients.
o Sedation dentistry is another option for patients
who have consistent dental anxiety.
• Some people may have an allergic reaction to
Novocaine and should stop avoid using it if certain
reactions occur such as:
o Flushing
o Hyperventilation
o Heart palpitations
o Swelling
o Itching
o Emergence of hives
o Anaphylaxis
 DEFINITIONS • Caries: Soft decayed area in a tooth, if left untreated
progressive decay may lead to the “death of a tooth”
due to permanent nerve damage
• Third molars: Also known as wisdom teeth. Generally
there are 4 third molars, but they may be absent or
they may be impacted, in which case they may need
to be surgically removed.
• Water Soluble Product: A substance that is easily
capable of being dissolved in water
• Neurotransmitter: Chemical messengers in the
nervous system that promote and permit nerve cell
communication from one nerve cell to another. (i.e.
dopamine, serotonin, epinephrine, etc).
• Vasodilator: An agent that causes blood vessels to
relax and dilate by relaxing the muscular walls of the
vessel, thereby, it increases the size of the vessel.
• Vasoconstrictor: An agent that causes blood vessels to
constrict their muscular wallsand decrease the
diameter of the blood vessel
• Plasma: It is the colorless, watery fluid of the blood
that does not contain any cells (red or white)
• Enzyme: It is a protein catalyst that increases the rate
of a reaction, but they are not consumed in the
reaction itself and will remain intact even after
chemical reaction takes place.
• Hydrolysis: A chemical reaction in which a water
molecule is chemically split into hydrogen and
hydroxide ions
• Hyperventilation: Increased rate of breathing greater
than demanded by the body. May cause dizziness or
tingling of the fingers and toes
• Heart palpitations:
H Uncomfortable sensation of the
heart beating too fast or out of sequence. A person
with heart palpitations will be conscious of the
increased heart rate.
• Anaphalysis: extreme allergic reaction that may result
in rapid decrease in blood pressure, decreased
amounts of oxygen exposure to the brain, heart strain,
swelling of the vocal cords, etc

To learn more about the FDA information on Novocaine visit:

http://www.drugs.com/pro/novocaine.html