Local+Anaesthetics

=Properties of Local ANasthetics= =Pharmacology of Cocaine= =Indiidual Local Anaesthetics=

Topical agents

 * The "IDEAL" Local Anesthtic
 * Eficacious with all administration routes
 * Suitable pharmacokinetics
 * Adequate potency
 * Safe
 * Non-allergenic
 * Requires no adjunct
 * Doesn't exist

>> Mucous membranes >> On skin
 * Administration ROutes**
 * Topical
 * iniltrate drug through skin
 * Regional conduction block
 * Spinal/epidural
 * IV regional anestheia

Prototype: Prociane, (NOVOCAIN) >> Procaine itself rarely used >> Others used ralatively rarely compared with amides
 * Class I: Esthers**
 * USes
 * Inactivated, detoxified by plasma esterases
 * Relatively higher allergenicity than amides

Other Esters: Chlorprocaine (Nesacaine) Tetracaine ({ontocaine)


 * Cocaine
 * Benzocaine

If there is only one 'i', it's an ester**
 * IFf drug's generic name ends in 'ciane', it's a local anesthetic.

SOme Other Amides: Pupi

General Principles: depends on drug pKa, local pH Nonionzied extracellularly, diffuse into neuron >> Bints to inactive state of Na_ channel >> Decrease Na+influx, depolarization >> No effect on resting nerve
 * Equiplibrium between Ionized, nonionized moleculaes of LA as administred...
 * Ionized intraneronally, the site of action