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 |
|
(source: Drug Bank) |
| CHRNA10 |
|
(source: Drug Bank) |
| GRIN3A |
|
(source: Drug Bank) |
| SCN10A |
|
(source: Drug Bank) |
| SLC6A3 |
|
(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
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Non-Curated Publications
A list of non-curated publications that mention this drug is available.
