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Other information

Indication
For the production of local anesthesia by infiltration and peripheral nerve block. They are not to be used for lumbar or caudal epidural anesthesia.

Pharmacology
Chloroprocaine is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Chloroprocaine (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Chloroprocaine is an ester anesthetic.

Mechanism Of Action
Chloroprocaine 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. Chloroprocaine 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 Category
Anesthetics; Local Anesthetics; ATC:N01BA04

Brand Names/Synonyms
Astracaine 4%; Astracaine 4% Forte; CHLOROPROCAINE; Carbocaine; Carbocaine with Neo-Cobefrin; Chirocaine; Chlor-Procaine; Chloroprocain; Chloroprocaine; Chloroprocaine Hcl; Chloroprocainum [Inn-Latin]; Chlorprocaine; Chlorprocainum; Citanest Forte; Citanest Plain; Cloroprocaina [Inn-Spanish]; Dalcaine; Dilocaine; Duranest; Duranest-Mpf; HSDB 3301; Halestyn; Isocaine; Isocaine 2%; Isocaine 3%; L-Caine; Lidoject-1; Lidoject-2; Marcaine; Marcaine Spinal; Nesacaine; Nesacaine-Ce; Nesacaine-Mpf; Novocain; Octocaine; Octocaine-100; Octocaine-50; Piocaine; Polocaine; Polocaine-Mpf; Pontocaine; Sensorcaine; Sensorcaine Forte; Sensorcaine-Mpf; Sensorcaine-Mpf Spinal; Septocaine; Ultracaine D-S; Ultracaine D-S Forte; Xylocaine; Xylocaine 5% Spinal; Xylocaine Test Dose; Xylocaine-Mpf; Xylocaine-Mpf with Glucose

Dosage Forms
LIQUID

Absorption
Not Available

Interactions
Interactions for Chloroprocaine:

The administration of local anesthetic solutions containing epinephrine or norepinephrine to patients receiving monoamine oxidase inhibitors, tricyclic antidepressants or phenothiazines may produce severe, prolonged hypotension or hypertension. Concurrent use of these agents should generally be avoided. In situations when concurrent therapy is necessary, careful patient monitoring is essential.

Concurrent administration of vasopressor drugs (for the treatment of hypotension related to obstetric blocks) and ergot-type oxytocic drugs may cause severe, persistent hypertension or cerebrovascular accidents.

The para-aminobenzoic acid metabolite of chloroprocaine inhibits the action of sulfonamides. Therefore, chloroprocaine should not be used in any condition in which a sulfonamide drug is being employed.

Chemical IUPAC Name
2-diethylaminoethyl4-amino-2-chloro-benzoate

Chemical Formula
C13H19ClN2O2

Half Life
21 +/- 2 seconds

Drug Type
Approved Drug

# Accession No
APRD00404

CAS Registry Number
133-16-4