Arestocaine HCL - General Information
A local anesthetic that is chemically related to bupivacaine but pharmacologically related to lidocaine. It is indicated for infiltration, nerve block, and epidural anesthesia. Arestocaine HCL is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168)
Pharmacology of Arestocaine HCL
Mepivicaine is a local anesthetic of the amide type. Mepivicaine as a reasonably rapid onset and medium duration and is known by the proprietary names as Carbocaine and Polocaine. Mepivicaine is used in local infiltration and regional anesthesia. Systemic absorption of local anesthetics produces effects on the cardiovascular and central nervous systems. At blood concentrations achieved with normal therapeutic doses, changes in cardiac conduction, excitability, refractoriness, contractility, and peripheral vascular resistance are minimal.
Arestocaine HCL 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 caudal or epidural anesthesia. Also, when appropriate, the physician should discuss other information including adverse reactions listed in this package insert.
Arestocaine HCL Interactions
Arestocaine HCL Contraindications
Mepivacaine is contraindicated in patients with a known hypersensitivity to it or to any local anesthetic agent of the amide-type or to other components of mepivacaine solutions.
Additional information about Arestocaine HCL
Arestocaine HCL Indication: For production of local or regional analgesia and anesthesia by local infiltration, peripheral nerve block techniques, and central neural techniques including epidural and caudal blocks.
Mechanism Of Action: Local anesthetics block 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. In general, the progression of anesthesia is related to the diameter, myelination, and conduction velocity of affected nerve fibers. Clinically, the order of loss of nerve function is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Mepivacaine
Synonyms: Mepivacaina [INN-Spanish]; DL-Mepivacaine; Mepivacaine HCL; mepivacaine hydrochloride; Mepivacainum [INN-Latin]; Mepivicaine; S-Ropivacaine Mesylate
Drug Category: Anesthetics, Local
Drug Type: Small Molecule; Approved
Other Brand Names containing Mepivacaine: Arestocaine HCL; Carbocain; Carbocaine; Isocaine HCL; Polocaine; Polocaine-MPF; Scandicain; Scandicaine; Scandicane; Scandonest Plain;
Absorption: Absorbed locally. The rate of systemic absorption of local anesthetics 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 solution.
Toxicity (Overdose): The mean seizure dosage of mepivacaine in rhesus monkeys was found to be 18.8 mg/kg with mean arterial plasma concentration of 24.4 µg/mL. The intravenous and subcutaneous LD 50 in mice is 23 mg/kg to 35 mg/kg and 280 mg/kg respectively.
Protein Binding: Mepivacaine is approximately 75% bound to plasma proteins. Generally, the lower the plasma concentration of drug, the higher the percentage of drug bound to plasma.
Biotransformation: Rapidly metabolized, with only a small percentage of the anesthetic (5 percent to 10 percent) being excreted unchanged in the urine. The liver is the principal site of metabolism, with over 50% of the administered dose being excreted into the bile as metabolites.
Half Life: The half-life of mepivacaine in adults is 1.9 to 3.2 hours and in neonates 8.7 to 9 hours.
Dosage Forms of Arestocaine HCL: Solution Subcutaneous
Chemical IUPAC Name: N-(2,6-dimethylphenyl)-1-methylpiperidine-2-carboxamide
Chemical Formula: C15H22N2O
Mepivacaine on Wikipedia: http://en.wikipedia.org/wiki/Mepivacaine
Organisms Affected: Humans and other mammals