Chloroprocaine

307.21600

270.76

5YVB0POT2H

DTXSID8022799

N - Nervous system

2922499990

55.56000

3.80400

Solid

1.17g/cm3

173-174

402.6ºC at 760mmHg

197.3ºC

1.553

1.30e+00 g/L

1.08E-06mmHg at 25°C

ODORLESS

Crystals; mp: 176-178 °C (microstage); bitter taste; aq soln are just acid to litmus and turn yellow on standing; about 1 g sol in: 22 ml water @ 20 °C, 100 ml 95% ethanol /Hydrochloride/|WHITE /HCL/

AQ SOLN TURN YELLOW ON STANDING /HCL/

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

In mice, the intravenous LD50 of chloroprocaine HCl is 97 mg/kg and the subcutaneous LD50 of chloroprocaine HCl is 950 mg/kg.

NERVE BLOCKS LAST AN AVG OF 1 HR. THE ADDITION OF EPINEPHRINE 1:200,000 PROLONGS THE DURATION TO AS MUCH AS 1.5 HR. /HYDROCHLORIDE/|EFFECTS OF PROCAINE & PHYSOSTIGMINE ARE ANTAGONISTIC, & THOSE OF PROCAINE & CURARE ADDITIVE. /PROCAINE/|... /Procaine/ is hydrolyzed in vivo to produce paraaminobenzoic acid, which inhibits the action of sulfonamides. /Procaine/|BUPIVACAINE & OTHER AMIDE LOCAL ANESTHETICS INHIBIT HYDROLYSIS OF CHLOROPROCAINE BY HUMAN SERUM.|For more Interactions (Complete) data for CHLOROPROCAINE (19 total), please visit the HSDB record page.

LD50 Mouse ip 266 mg/kg|LD50 Mouse sc 1069 mg/kg

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

Anesthetics, Local|A LOCAL ANESTHETIC AGENT SIMILAR IN CHEM STRUCTURE & PHARMACOLOGICAL ACTION TO PARENT COMPD, PROCAINE HCL. IT IS MORE RAPID IN ONSET OF ACTION & HAS ANESTHETIC POTENCY AT LEAST TWICE THAT OF PROCAINE. TOXICITY IS LOW & QUALITATIVELY SIMILAR TO PROCAINE. /CHLOROPROCAINE HCL/|...USED TO PRODUCE ANESTHESIA BY TECHNIQUES OF INFILTRATION, FIELD BLOCK, & REGIONAL NERVE BLOCK, INCL CAUDAL & EPIDURAL BLOCK. /CHLOROPROCAINE HCL/|... ACT ON ANY PART OF THE NERVOUS SYSTEM & ON EVERY TYPE OF NERVE FIBER. /LOCAL ANESTHETICS/|For more Therapeutic Uses (Complete) data for CHLOROPROCAINE (13 total), please visit the HSDB record page.

A FEW CASES OF THROMBOPHLEBITIS HAVE BEEN REPORTED FOLLOWING IV REGIONAL ANESTHESIA. THIS REACTION MAY HAVE BEEN DUE TO ACIDITY OF SOLN. /CHLOROPROCAINE HCL/|... NOT EFFECTIVE TOPICALLY & HAS NOT BEEN STUDIED SUFFICIENTLY TO BE USED FOR SPINAL ANESTHETIC. /CHLOROPROCAINE HCL/|IN PRESENCE OF HEMORRHAGE, SYMPATHETIC BLOCK PRODUCED BY EPIDURAL ANESTHESIA BECOMES EXTREMELY SIGNIFICANT & MAY RESULT IN RAPID & DELETERIOUS CIRCULATORY CHANGES. /LOCAL ANESTHETICS/|ANIMALS WITH EXPTL PRODUCED HEPATIC DAMAGE ARE MUCH MORE SUSCEPTIBLE TO TOXIC ACTIONS OF LOCAL ANESTHETICS, SO THAT EXTENSIVE USE OF LOCAL ANESTHETIC IN PT WITH SEVERE HEPATIC DAMAGE SHOULD PERHAPS BE AVOIDED. /LOCAL ANESTHETICS/|For more Drug Warnings (Complete) data for CHLOROPROCAINE (19 total), please visit the HSDB record page.

Chloroprocaine is an ester type 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.

Drugs that block nerve conduction when applied locally to nerve tissue in appropriate concentrations. They act on any part of the nervous system and on every type of nerve fiber. In contact with a nerve trunk, these anesthetics can cause both sensory and motor paralysis in the innervated area. Their action is completely reversible. (From Gilman AG, et. al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 8th ed) Nearly all local anesthetics act by reducing the tendency of voltage-dependent sodium channels to activate. (See all compounds classified as Anesthetics, Local.)

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.|Chloroprocaine is rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase. Urinary excretion is affected by urinary perfusion and factors affecting urinary pH.|PROCAINE IS READILY ABSORBED FOLLOWING PARENTERAL ADMIN ... DOES NOT LONG REMAIN @ SITE OF INJECTION. ... FOLLOWING ABSORPTION, PROCAINE IS RAPIDLY HYDROLYZED ... /PROCAINE/|... Binding of the anesthetic to proteins in the serum and to tissues reduces the concentration of free drug in the systemic circulation and, consequently, reduces toxicity. ... /Ester local anesthetics/ are hydrolyzed and inactivated primarily by a plasma esterase, probably plasma cholinesterase. The liver also participates in hydrolysis of local anesthetics. /Local anesthetics/|THE SYSTEMIC TOXICITY OF CHLOROPROCAINE IS LESS THAN THAT OF ALL OTHER LOCAL ANESTHETICS BECAUSE OF ITS RAPID HYDROLYSIS BY PLASMA CHOLINESTERASE ... WHICH SHORTENS THE PLASMA HALF-LIFE.|... ENZYMATIC HYDROLYSIS OF PROCAINE /GIVES/ ... PARA-AMINOBENZOIC ACID & DIETHYLAMINOETHANOL. FORMER IS EXCRETED IN URINE TO EXTENT OF ABOUT 80%, EITHER UNCHANGED OR IN CONJUGATED FORM. ONLY 30% OF DIETHYLAMINOETHANOL CAN BE RECOVERED IN URINE; REMAINDER UNDERGOES METABOLIC DEGRADATION ... /PROCAINE/|For more Absorption, Distribution and Excretion (Complete) data for CHLOROPROCAINE (9 total), please visit the HSDB record page.

Chloroprocaine is rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase.|2-DIETHYLAMINOETHYL 4-AMINO-2-CHLOROBENZOATE YIELDS 4-AMINO-2-CHLOROBENZOIC ACID IN GUINEA PIGS. LIVETT, BH & RM LEE, BIOCHEM PHARMAC 17, 385 (1968). /FROM TABLE/|HYDROLYZED /CHIEFLY/ BY PLASMA PSEUDOCHOLINESTERASES /& ALSO BY ESTERASES IN LIVER/ AS DIETHYLAMINOETHANOL & 2-CHLORO-4-AMINOBENZOIC ACID /HUMAN, PARENTERAL. ANIMAL STUDIES SUGGEST THAT SOME LOCAL ANESTHETICS MAY UNDERGO BILIARY RECYCLING/ /CHLOROPROCAINE HCL/

21 +/- 2 seconds|... Plasma half-life /is/ approximately 25 seconds.

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. It is hypothesized that Chloroprocaine binds or antagonizes the function of N-methyl-D-aspartate (NMDA) receptors as well as nicotinic acetylcholine receptors and the serotonin receptor-ion channel complex.|Local anesthetics prevent the generation and the conduction of the nerve impulse. Their primary site of action is the cell membrane. ... Local anesthetics block conduction by decreasing or preventing the large transient increase in the permeability of excitable membranes to Na+ that normally is produced by a slight depolarization of the membrane. ... As the anesthetic action progressively develops in a nerve, the threshold for electrical excitability gradually increases, the rate of rise of the action potential declines, impulse conduction slows, and the safety factor for conduction decreases; these factors decrease the probability of propagation of the action potential, and nerve conduction fails. ... /Local anesthetics/ can block K+ channels. ... blockade of conduction is not accompanied by any large or consistent change in resting membrane potential due to block of K+ channels. /Local anesthetics/|... SITE AT WHICH LOCAL ANESTHETICS ACT, AT LEAST IN ... CHARGED FORM, IS ACCESSIBLE ONLY FROM THE INNER SURFACE OF THE MEMBRANE. ... LOCAL ANESTHETICS APPLIED EXTERNALLY FIRST MUST CROSS THE MEMBRANE BEFORE THEY CAN EXERT A BLOCKING ACTION. /LOCAL ANESTHETICS/|... /TWO POSSIBILITIES:/ ACHIEVE BLOCK BY INCR SURFACE PRESSURE OF LIPID LAYER THAT CONSTITUTES NERVE MEMBRANE ... CLOSING PORES THROUGH WHICH IONS MOVE. ... /OR:/ AFFECT PERMEABILITY BY INCR DEGREE OF DISORDER OF MEMBRANE. /LOCAL ANESTHETICS/|... ACID SALT MUST BE NEUTRALIZED IN TISSUE & FREE AMINE LIBERATED BEFORE DRUG CAN PENETRATE TISSUES & PRODUCE ANESTHETIC ACTION. ... FORM OF MOLECULE ACTIVE IN NERVE FIBERS IS CATION. ... CATION ... COMBINES WITH SOME RECEPTOR IN MEMBRANE TO PREVENT GENERATION OF ACTION POTENTIAL. /LOCAL ANESTHETICS/|... /SUGGESTED/ THAT PROCAINE ... DIMINISHES RELEASE OF ACETYLCHOLINE BY MOTOR-NERVE ENDINGS. /PROCAINE/

Sodium metabisulfate as a preservative in earlier formulations ... newer preparations ... contain calcium EDTA as the preservative.

2-chloroprocaine

NESACAINE (ASTRA): SOLUTION 1% AND 2% IN 30 ML CONTAINERS (2% NOT FOR CAUDAL OR EPIDURAL ANESTHESIA); NESACAINE MPF: SOLUTION 2% AND 3% IN 30 ML CONTAINERS FOR CAUDAL OR EPIDURAL ANESTHESIA (CONTAINS NO PRESERVATIVE) /CHLOROPROCAINE HCL/|NESACAINE (PENNWALT). SOLN 1% & 2% IN 30 ML MULTIPLE-DOSE CONTAINERS (NOT FOR CAUDAL OR EPIDURAL ANESTHESIA. NESACAINE-CE (PENNWALT). SOLN 2% & 3% IN 30 ML SINGLE-DOSE CONTAINERS (FOR CAUDAL OR EPIDURAL ANESTHESIA; CONTAINS NO PRESERVATIVE). /CHLOROPROCAINE HYDROCHLORIDE/

Chloroprocaine, an ester local anesthetic introduced in 1952, is a chlorinated derivative of procaine.

FLAME IONIATION GLC MEASUREMENT OF CHLOROPROCAINE IN PLASMA.|GLC PROCEDURE CAPABLE OF DETECTING 10 NG INTACT CHLOROPROCAINE/ML OF BLOOD.

Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients