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Pathway Description
Prilocaine Action Pathway
Homo sapiens
Drug Action Pathway
Prilocaine exerts its local anaesthetic effect by blocking voltage-gated sodium channels in peripheral neurons. Prilocaine diffuses across the neuronal plasma membrane in its uncharged base form. Once inside the cytoplasm, it is protonated and this protonated form enters and blocks the pore of the voltage-gated sodium channel from the cytoplasmic side. For this to happen, the sodium channel must first become active so that so that gating mechanism is in the open state. Therefore prilocaine preferentially inhibits neurons that are actively firing.
References
Prilocaine Pathway References
Harmatz A: Local anesthetics: uses and toxicities. Surg Clin North Am. 2009 Jun;89(3):587-98. doi: 10.1016/j.suc.2009.03.008.
Pubmed: 19465198
Skidmore RA, Patterson JD, Tomsick RS: Local anesthetics. Dermatol Surg. 1996 Jun;22(6):511-22; quiz 523-4.
Pubmed: 8646465
Neuron Function References
Lovinger DM: Communication networks in the brain: neurons, receptors, neurotransmitters, and alcohol. Alcohol Res Health. 2008;31(3):196-214.
Pubmed: 23584863
Kress GJ, Mennerick S: Action potential initiation and propagation: upstream influences on neurotransmission. Neuroscience. 2009 Jan 12;158(1):211-22. doi: 10.1016/j.neuroscience.2008.03.021. Epub 2008 Mar 19.
Pubmed: 18472347
Platkiewicz J, Brette R: A threshold equation for action potential initiation. PLoS Comput Biol. 2010 Jul 8;6(7):e1000850. doi: 10.1371/journal.pcbi.1000850.
Pubmed: 20628619
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