Nesacaine-CE - General Information
Nesacaine-CE hydrochloride is a local anesthetic given by injection during surgical procedures and labor and delivery. Nesacaine-CE, 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.
Pharmacology of Nesacaine-CE
Nesacaine-CE is an anesthetic agent indicated for production of local or regional anesthesia, particularly for oral surgery. Nesacaine-CE (like cocaine) has the advantage of constricting blood vessels which reduces bleeding, unlike other local anesthetics like lidocaine. Nesacaine-CE is an ester anesthetic.
Nesacaine-CE for patients
When appropriate, patients should be informed in advance that they may experience temporary loss of sensation and motor activity, usually in the lower half of the body, following proper administration of epidural anesthesia.
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.
Nesacaine and Nesacaine-MPF Injections are contraindicated in patients hypersensitive (allergic) to drugs of the PABA ester group.
Lumbar and caudal epidural anesthesia should be used with extreme caution in persons with the following conditions: existing neurological disease, spinal deformities, septicemia, and severe hypertension.
Additional information about Nesacaine-CE
Nesacaine-CE 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.
Mechanism Of Action: Nesacaine-CE 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. Nesacaine-CE 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: Chloroprocaine
Synonyms: Chloroprocaine hydrochloride; Chloroprocain; Chlorprocaine
Drug Category: Anesthetics, Local
Drug Type: Small Molecule; Approved
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.
Toxicity (Overdose): In mice, the intravenous LD50 of chloroprocaine HCl is 97 mg/kg and the subcutaneous LD50 of chloroprocaine HCl is 950 mg/kg.
Protein Binding: Not Available
Biotransformation: Chloroprocaine is rapidly metabolized in plasma by hydrolysis of the ester linkage by pseudocholinesterase.
Half Life: 21 +/- 2 seconds
Dosage Forms of Nesacaine-CE: Injection, solution Intravenous
Chemical IUPAC Name: 2-diethylaminoethyl 4-amino-2-chlorobenzoate
Chemical Formula: C13H19ClN2O2
Chloroprocaine on Wikipedia: https://en.wikipedia.org/wiki/Chloroprocaine
Organisms Affected: Humans and other mammals