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Cocaine while used in local anaesthesia has a low therapeutic index and its use is also covered in the U.K. by the Misuse of Drugs Act 1971.


Cocaine is a tropane alkaloid that binds to the dopamine, serotonin, and norepinephrine transport proteins and inhibits the re-uptake of dopamine, serotonin, and norepinephrine into pre-synaptic neurons. This leads to an accumulation of the respective neurotransmitters in the synaptic cleft and increased postsynaptic receptor activation causing relatively brief but intense psychostimulation. Addiction can occur rapidly, perhaps after less than 2 weeks use. As a local anaesthetic it blocks the voltage-gated sodium channels in the neuronal cell membrane.