Everything about Procaine totally explained
| PubChem=4914
| DrugBank=APRD00650
| C = 13 | H = 20 | N = 2 | O = 2
| molecular_weight = 236.31 g/mol
| bioavailability = n/a
| metabolism =
Hydrolysis by plasma esterases
| elimination_half-life = 40–84 seconds
| excretion =
Renal
| pregnancy_AU = B2
| pregnancy_US = C
| legal_AU = S4
| routes_of_administration =
Parenteral
}}
Procaine is a
local anesthetic drug of the
amino ester group. It is used primarily to reduce the pain of
intramuscular injection of
penicillin, and is also used in
dentistry. Owing to the ubiquity of the
trade name Novocain, procaine is sometimes referred to generically as
novocaine.
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) and
caine, a common ending for
alkaloids used as anesthetics. It was introduced into medical use by surgeon
Heinrich Braun (1862–1934).
Procaine is used less frequently 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, and 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-amino benzoic 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.
Further Information
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