Allocaine - General Information
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).
Pharmacology of Allocaine
Allocaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Allocaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Allocaine 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.
Allocaine for patients
Concurrent use of procaine hydrochloride and anticholinesterase agents may result in increased systemic toxicity since anticholinesterases inhibit the breakdown of procaine hydrochloride.
Concurrent use of procaine hydrochloride and antimyasthenics may result in loss of control of symptoms of myasthenia gravis due to antagonism of the effects of antimyasthenics on skeletal muscle. Temporary dosage adjustment of antimyasthenics may be required. Also antimyasthenics may have anticholinesterase activity.
CNS depressant medications
Concurrent use of procaine hydrochloride and CNS depressant medications may result in additive depressant effects.
Hyaluronidase may increase the diffusion rate of procaine hydrochloride, resulting in a decreased time of onset, but an increase in systemic toxicity.
Neuromuscular blocking agents (such as suxamethonium chloride)
Concurrent use of procaine hydrochloride and neuromuscular blocking agents may result in prolongation or enhancement of the neuromuscular blockade.
Concurrent use of procaine hydrochloride and sulfonamides may result in a reduction of the antibacterial action of the sulfonamide.
Concurrent use of acetazolamide and procaine hydrochloride may extend the plasma half-life of procaine.
Additional information about Allocaine
Allocaine Indication: Used as a local anesthetic primarily in oral surgery
Mechanism Of Action: Allocaine 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. Allocaine 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.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Procaine
Synonyms: Not Available
Drug Category: Anesthetics; Local Anesthetics
Drug Type: Small Molecule; Approved; Investigational
Other Brand Names containing Procaine: Allocaine; Chloroprocaine Hcl; Diethylaminoethyl P-Aminobenzoate; Duracaine; Duracillin A.S.; Gerovital; Gerovital H-3; Jenacain; Jenacaine; Neocaine; Nesacaine; Nissocaine; Norocaine; Novocain; Novocaine; P-Aminobenzoyldiethylaminoethanol; Penicillin G Procaine; Pfizerpen-As; Procain; Procaine Hcl; Procaine Hydrochloride; Procaine, Base; Scurocaine; Spinocaine; Vitamin H3; Anticort;
Absorption: Not Available
Toxicity (Overdose): Not Available
Protein Binding: Not Available
Biotransformation: Hydrolysis by plasma esterases to PABA
Half Life: 7.7 minutes
Dosage Forms of Allocaine: Tablet, extended release Oral
Chemical IUPAC Name: 2-diethylaminoethyl 4-aminobenzoate
Chemical Formula: C13H20N2O2
Procaine on Wikipedia: http://en.wikipedia.org/wiki/Procaine
Organisms Affected: Humans and other mammals