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Local Anesthetics Classes Structure Examples and Properties
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Local anaesthetics are drugs which cause reversible local anaesthesia and a loss of nociception. Without loss of consciousness when they are used on specific nerve pathways, effects such as analgesia and paralysis can be achieved. • Analgesic drugs that suppress action potentials by blocking voltage-activated sodium ion (na+) channels in excitable tissues. • local anaesthetics do not diminish consciousness when administered correctly. • The blockade of voltage-activated Na+ channels accounts for both their analgesic effects, mediated through inhibition of action potentials in nociceptive neurones, and their systemic effects. inhibition of action potentials in the heart contributes to local anaesthetic toxicity and also accounts for the antiarrhythmic actions of intravenous lidocaine (a class 1b antiarrhythmic) • They are classified to two main classes based on their structure: esters and amides • Esters are hydrolyzed by plasma and tissue esterases. (Pseudocholinesterase enzyme). • Atypical pseudocholinesterase- less active enzyme- toxicity • Amides are primarily metabolized by liver amidases • Prilocaine may lead to methemoglobinemia- Hb doesn’t carry O2 well- Sad blueberry disease. • Local anaesthesias have three parts • Lipophilic part (aromatic benzene ring) • Hydrophilic part (amine group) • Linkage- Basis for naming • • SUBSCRIBE, LIKE and SHARE • Check our website for more medical lecture notes at https://medcrine.com • Follow us on twitter @medcrine • Instagram @medcrine • Telegram at t.me/medcrine • email us on [email protected]
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