Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2018 Publisher: Alliance Pharmaceuticals Limited, Avonbridge House, Bath Road, Chippenham, Wiltshire, SN15 2BB, United Kingdom
Tetracaine is a local anaesthetic and is believed to act by blocking nerve conduction mainly by inhibiting sodium ion flux across the axon membrane.
Tetracaine achieves this by acting upon specific receptors that control gating mechanisms responsible for conductance changes in specialised proteinaceous sodium channels.
Blocking sodium ion flux prevents the setting up of an action potential in the nerve axon, thus preventing pain receptors signalling to the central nervous system.
Tetracaine additionally has vasodilatory effects, which commonly results in a localised erythema.
The ester type ‘caine’ anaesthetics are rapidly metabolised in blood mainly by plasma pseudocholinesterase. A 3.33μM (1μg/ml) concentration of tetracaine was fully metabolised in human plasma within 20 seconds.
In vivo data has demonstrated that Ametop gel is 15 ± 11% bioavailable when administered to intact normal skin, with a mean absorption and elimination half life of 1.23 ± 0.28 hours.
Peak plasma levels of p-(n-butylamino) benzoic acid (BABA), the major metabolite of tetracaine are between 3-6 hours post dose.
None stated.
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