Product Information
Registration Status: ActivePLIAGLIS CREAM 70MG/G + 70MG/G is approved to be sold in Singapore with effective from 2015-02-06. It is marketed by GALDERMA SINGAPORE PTE LTD, with the registration number of SIN14793P.
This product contains Lignocaine 7.00% w/w, and Tetracaine 7.00% w/w in the form of CREAM. It is approved for CUTANEOUS use.
This product is manufactured by Laboratoires Galderma in FRANCE.
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.
Description
Tetracaine is an ester local anaesthetic currently available in combination with lidocaine as a cream and patch.
Indication
The combination lidocaine and tetracaine patch is indicated for local dermal analgesia for superficial dermatological procedures and superficial venous access. The combination lidocaine and tetracaine cream is intended to provide topical local analgesia for superficial dermatological procedures.
Mechanism of Action
Tetracaine is an ester-type anesthetic and produces local anesthesia by blocking the sodium ion channels involved in initiation and conduction of neuronal impulses.
Pharmacokinetics
- Absorption
- Systemic absorption of anaesthetic from the combination cream is directly related to the duration and surface area of application. Although peak plasma concentrations for lidocaine were measured, plasma levels for tetracaine could not be determined due to low levels (<0.9 ng/mL)
- Distribution
- Tetracaine is rapidly hydrolyzed in the plasma; therefore, volume of distribution could not be determined.
- Metabolism
- Tetracaine is rapidly hydrolyzed by plasma esterases to the following primary metabolites: para-aminobenzoic acid and diethylaminoethanol. The activity of both metabolites is unspecified.
- Elimination
Clearance
Tetracaine is hydrolyzed rapidly in the plasma; therefore, clearance has not been determined.
Toxicity
The most common adverse effects with the combination cream are localized reactions such as: erythema (47%), skin discoloration (16%), and edema (14%). Systemic adverse events were less common, occurring at a rate of <1% and included vomiting, headache, dizziness, and fever. Similar to other amide and ester anesthetics, CNS excitation and/or depression may occur. It is not well known at which plasma concentration systemic toxicity occurs with tetracaine; however, the threshold is thought to be much lower than that of lidocaine which is 1000 ng/mL.
Active Ingredient/Synonyms
2-(dimethylamino)ethyl 4-(butylamino)benzoate | 2-(Dimethylamino)ethyl p-(butylamino)benzoate | Amethocaine | Amethocaine HCl | Diäthylaminoäthanol ester der p-butylaminobenzösäure | Dicaine | Medihaler-Tetracaine | Metraspray | p-(butylamino)benzoic acid β-(dimethylamino)ethyl ester | p-Butylaminobenzoyl-2-dimethylaminoethanol | Tetracaína | Tétracaïne | Tetracaine HCl | Tetracaine |
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.