Procaine
Procaine hydrochloride is a local anesthetic
used primarily in dentistry. It is primarily known as
novocaine, or by the trade name Novocain®.
Procaine was first synthesized in 1905,
and was the first injectable man-made local anesthetic
used. It was created by the German chemist Alfred Einhorn
(1857-1917) who gave the chemical the trade name Novocaine,
from the Latin 'Novus' (meaning New) plus 'caine' as in
"cocaine". It was introduced into medical use
by surgeon Heinrich Braun (1862-1934).
Procaine is rarely used today since more
effective (and hypoallergenic) alternatives such as lidocaine
(xylocaine) exist. Prior to the discovery of procaine,
cocaine was the most commonly used local anesthetic. Procaine
(like cocaine) has the advantage of constricting blood
vessels which reduces bleeding, unlike other local anesthetics
like lidocaine; without the euphoric and addictive qualities
of cocaine.
Procaine, an ester anesthetic, is metabolized
in the plasma by the enzyme pseudocholinesterase through
hydrolysis into para-aminobenzoic acid (PABA), which is
then excreted by the kidneys into the urine. Allergic
reactions to procaine are usually not in response to procaine
itself, but to PABA. About 1 in 3000 people have an atypical
form of pseudocholinesterase, which doesn't hydrolyze
ester anesthetics such as procaine, resulting in a prolonged
period of high levels of the anesthetic in the blood and
increased toxicity.
Procaine is the primary ingredient in
the controversial preparation Gerovital H3, which is claimed
by its advocates to remedy many effects of aging. The
mainstream medical view is that these claims were seriously
studied and discredited in the 1960s.
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Procaine
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2-diethylaminoethyl
4-aminobenzoate hydrochloride |
CAS number
59-46-1 or 51-05-8 (with HCl) |
ATC code
C05AD05, N01BA02, S01HA05 |
Chemical formula |
C13H20N2O2·HCl |
Molecular weight |
236.313 or 272.774 (with HCl) |
Bioavailability |
? |
Metabolism |
? |
Elimination half-life |
? |
Excretion |
Renal |
Pregnancy category |
? |
Legal status |
? |
Routes of administration |
? |
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