Definition
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).
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 it is also used in dentistry. Owing to the ubiquity of the trade name Novocain, procaine is sometimes referred to generically as novocaine. It acts mainly by being a sodium channel blocker. Procaine was first synthesized in 1898[2] and was the first injectable man-made local anesthetic. It was created by the German chemist Alfred Einhorn (1856?1917) who gave the chemical the trade name Novocaine, from the Latin nov- (meaning new) and -caine, a common ending for alkaloids used as anesthetics. It was introduced into medical use by surgeon Heinrich Braun (1862?1934). Novocain application before removal of a decayed tooth 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. Like other local anesthetics (with the exception of cocaine), mepivacaine, and prilocaine, procaine is a vasodilator, and is often coadministered with epinephrine for the purpose of vasoconstriction. Vasoconstriction helps to reduce bleeding and prevents the drug from reaching systemic circulation in large amounts. Also unlike cocaine, procaine does not have the euphoric and addictive qualities that put it at risk for abuse. 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 does not 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 by Ana Aslan (Romania), 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. Procaine is occasionally added as an additive in illicit street drugs such as cocaine. (from wiki) [HMDB]
Description
Procaine is only found in individuals that have used or taken this drug. It is 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]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.
Top Gene Interactions
General Information
- Metabolism: Hydrolysis by plasma esterases to PABA Route of Elimination: With normal kidney function, the drug is excreted rapidly by tubular excretion. Half Life: 7.7 minutes
- Uses/Sources: It is used primarily to reduce the pain of intramuscular injection of penicillin, and it is also used in dentistry. [Wikipedia]
- Symptoms: An allergic reaction (difficulty breathing; closing of the throat; swelling of the lips, tongue, or face; or hives); chest pain or slow or irregular heartbeats; dizziness or drowsiness; anxiety or restlessness; nausea or vomiting; trembling, shaking, or seizures (convulsions). Other less serious side effects such as numbness, tingling, or minor pain at or around the injection site are more likely to occur.(L1459)
- Route of Exposure: Oral, Infiltration, Intramuscular
Toxicity
- Carcinogenicity: No indication of carcinogenicity to humans (not listed by IARC).
- Toxicity: LD50: 350 mg/kg (Oral, mouse).
Mechanism of Action
Target Name | Mechanism of Action | References |
---|---|---|
Neuronal acetylcholine receptor subunit alpha-2 DNA Calcium-activated potassium channel Phospholipase A2 Lysophospholipase Monoamine oxidase |
12941824 952985 2580269 952986 1109354 20045405 |
|
Glutamate receptor ionotropic, NMDA 3A Sodium channel protein type 10 subunit alpha Neuronal acetylcholine receptor subunit alpha-10 Sodium-dependent dopamine transporter 5-hydroxytryptamine receptor 3A |
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. |
17016423 16206183 17139284 7539114 16956595 10685879 |
Procaine Interacts with Diseases
Disease | Inference Score | References/Inference Genes |
Obesity | 7.25 |
|
Adenocarcinoma | 7.09 |
|
Infertility, Female | 6.83 |
|
Migraine disorder | 6.17 |
|
Hypophosphatasia, Adult | 6.13 |
|
Hypophosphatasia, Childhood | 6.13 |
|
Hypophosphatasia, Infantile | 6.13 |
|
Atrial Fibrillation, Familial, 6 | 6.03 |
|
Disease Models, Animal | 5.32 |
|
Atherosclerosis | 5.3 |
|
Inflammation | 5.12 |
|
Alveolar Bone Loss | 5.1 |
|
Pain | 5.06 |
|
Autism | 4.98 |
|
Carcinoma | 4.98 |
|
Jaundice, Neonatal | 4.98 |
|
Musculoskeletal Pain | 4.98 |
|
Mammary Neoplasms, Experimental | 4.96 |
|
Urinary Bladder Neoplasms | 4.89 |
|
Prostatic Neoplasms | 4.87 |
|