Drug/Small Molecule:
chloroprocaine

2D structure

Overview

Generic Names: Chloroprocain; Chloroprocaine hydrochloride; Chlorprocaine
Trade Names: Halestyn; Nesacaine-CE; Nesacaine-MPF
PharmGKB Accession Id: PA448946

Description

Chloroprocaine hydrochloride is a local anesthetic given by injection during surgical procedures and labor and delivery. Chloroprocaine, like other local anesthetics, blocks the generation and the conduction of nerve impulses, presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse and by reducing the rate of rise of the action potential. (source: Drug Bank)

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. (source: Drug Bank)

ATC Therapeutic Category

  • N01BA:Esters of aminobenzoic acid

Pharmacology, Interactions, and Contraindications

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. (source: Drug Bank)

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. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Chloroprocaine is rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase. (source: Drug Bank)

Absorption

The rate of systemic absorption of local anesthetic drugs is dependent upon the total dose and concentration of drug administered, the route of administration, the vascularity of the administration site, and the presence or absence of epinephrine in the anesthetic injection. (source: Drug Bank)

Toxicity

In mice, the intravenous LD<sub>50</sub> of chloroprocaine HCl is 97 mg/kg and the subcutaneous LD<sub>50</sub> of chloroprocaine HCl is 950 mg/kg. (source: Drug Bank)

Isomeric SMILES Code:

CCN(CC)CCOC(=O)C1=C(C=C(C=C1)N)Cl (source: Drug Bank)

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
HTR3A Uncurated Annotation (source: Drug Bank)
CHRNA10 Uncurated Annotation (source: Drug Bank)
GRIN3A Uncurated Annotation (source: Drug Bank)
SCN10A Uncurated Annotation (source: Drug Bank)
SLC6A3 Uncurated Annotation (source: Drug Bank)

A list of non-curated publications that mention this drug along with other drugs is available.

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB01161
KEGG Drug ID:
D00732
PubChem Compound ID:
8612
PubChem Substance ID:
10079

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

PharmGKB integrates drug information from different sources: DrugBank, Open Eye Scientific Software.
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