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Description: A local anesthetic of the ester type that has a slow onset and a short duration of action. It is mainly used for infiltration anesthesia, peripheral nerve block, and spinal block. (From Martindale, The Extra Pharmacopoeia, 30th ed, p1016). [PubChem]
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Procaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Procaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Procaine is an ester anesthetic. It 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.
Mechanism of Action: Procaine acts mainly by inhibiting sodium influx through voltage gated sodium channels in the neuronal cell membrane of peripheral nerves. When the influx of sodium is interrupted, an action potential cannot arise and signal conduction is thus inhibited. The receptor site is thought to be located at the cytoplasmic (inner) portion of the sodium channel. Procaine has also been shown to bind or antagonize the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.
Indication: Used as a local anesthetic primarily in oral surgery
Half Life: 7.7 minutes
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Thought leaders and organizations working on research involving procaine.

  • Claude Desplan
  • Roos van Swigchem
  • Christopher J Kirk
  • Rasmus Bro
  • Zhi Gao
  • Samaritan Pharmaceuticals, Inc
  • National Institute of Mental Health (NIMH)
  • L.A.L Clinica Pesquisa e Desenvolvimento Ltda.
  • Aga Khan University
  • GenVec
  • New York University
  • Purdue University
  • Albert Einstein College of Medicine
  • Saitama Medical University
  • University of Minnesota

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