Product Information
Registration Status: ActiveXYLOCAINE INJECTION 1% (5ML) is approved to be sold in Singapore with effective from 1991-05-04. It is marketed by DCH AURIGA SINGAPORE, with the registration number of SIN05616P.
This product contains Lignocaine 50mg/5ml in the form of INJECTION. It is approved for INTRADERMAL use.
This product is manufactured by ASTRAZENECA PTY LTD in AUSTRALIA.
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 and cardiac depressant used as an antiarrhythmia agent. Its actions are more intense and its effects more prolonged than those of procaine but its duration of action is shorter than that of bupivacaine or prilocaine. [PubChem]
Indication
For production of local or regional anesthesia by infiltration techniques such as percutaneous injection and intravenous regional anesthesia by peripheral nerve block techniques such as brachial plexus and intercostal and by central neural techniques such as lumbar and caudal epidural blocks.
Mechanism of Action
Lidocaine stabilizes the neuronal membrane by inhibiting the ionic fluxes required for the initiation and conduction of impulses thereby effecting local anesthetic action. Lidocaine alters signal conduction in neurons by blocking the fast voltage gated sodium (Na+) channels in the neuronal cell membrane that are responsible for signal propagation. With sufficient blockage the membrane of the postsynaptic neuron will not depolarize and will thus fail to transmit an action potential. This creates the anaesthetic effect by not merely preventing pain signals from propagating to the brain but by aborting their birth in the first place.
Pharmacokinetics
- Absorption
- Information derived from diverse formulations, concentrations and usages reveals that lidocaine is completely absorbed following parenteral administration, its rate of absorption depending, for example, upon various factors such as the site of administration and the presence or absence of a vasoconstrictor agent.
- Distribution
- * 0.7 to 2.7 L/kg [healthy volunteers]
- Metabolism
- Primarily hepatic.
- Elimination
Clearance
* 0.64 +/- 0.18 L/min
Toxicity
The oral LD 50 of lidocaine HCl in non-fasted female rats is 459 (346-773) mg/kg (as the salt) and 214 (159-324) mg/kg (as the salt) in fasted female rats. Symptoms of overdose include convulsions, hypoxia, acidosis, bradycardia, arrhythmias and cardiac arrest.
Active Ingredient/Synonyms
2-(Diethylamino)-2',6'-acetoxylidide | 2-(Diethylamino)-N-(2,6-dimethylphenyl)acetamide | alpha-diethylamino-2,6-dimethylacetanilide | Lignocaine | α-diethylamino-2,6-dimethylacetanilide | Lidocaine |
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.