Product Information
Registration Status: ActiveISOCAINE (MEPIVACAINE HCL) INJECTION 3% is approved to be sold in Singapore with effective from 2014-10-24. It is marketed by N.K. LUCK (S) PTE LTD, with the registration number of SIN14649P.
This product contains Mepivacaine 30mg/mL in the form of INJECTION. It is approved for SUBCUTANEOUS use.
This product is manufactured by Novocol Pharmaceutical of Canada in CANADA.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Description
A local anesthetic that is chemically related to bupivacaine but pharmacologically related to lidocaine. It is indicated for infiltration, nerve block, and epidural anesthesia. Mepivacaine is effective topically only in large doses and therefore should not be used by this route. (From AMA Drug Evaluations, 1994, p168)
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.
Pharmacokinetics
- 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.
- Distribution
- Metabolism
- 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.
- Elimination
Toxicity
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.
Active Ingredient/Synonyms
(+-)-1-Methyl-2',6'-pipecoloxylidide | 1-methyl-2',6'-pipecoloxylidide | DL-Mepivacaine | Mepivacaina | Mepivacainum | N-(2,6-Dimethylphenyl)-1-methyl-2-piperidinecarboxamide | N-(2,6-Dimethylphenyl)-1-methylpiperidine-2-carboxamide | Mepivacaine |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.