Local Anesthetics AM Fouda MD, PhD DDI Types of Anesthesia: | Affects the whole body including the i { brain; it is administered intravenously or through f /\ inhalation. There is complete loss of consclousness. } = Involves larger region of the body. It can be either: = Peripheral nerve block. — Spinal and epidural anesthesia. Local anesthesia ~ A type used in minor surgeries where a small part of the body e.g. these used in dentistry. Topical (surface) anesthesia - e.g. for skin or corneo, ‘Spinal anesthesia: is used for surgeries of the lower limb or pelvic structures. A local anesthetic is injected into the CSF space below the terminal end of the spinal cord (usually between 3rd and 4th lumbar vertebra). Epidural anesthesia: the anesthetic is infused (asually through a catheter) into the space between the dura mater and the connective tissue lining the vertebral canal. It gives of action than spinal anesthesia but with more delayed effect.General ° structure I Ma i & members Ce \ N Ester link ‘Amide link Procaine Prototype) Lidocaine Prototype) Cocaine - Tetracaine - Benzocaine __Mepivacaine - Bupivacaine - Ropivacaine Metabolism Plasma estrases Liver Duration Short Long eon 1 Local anesthetics block voltage dependent ‘Nat channels within the nerve fibers —| nerve conduction. = The drug must cross the lipid membrane to reach the cytoplasm; therefore, the more lipid- ‘soluble (non-ionized, uncharged) form cross the membrane more rapidly than the ionized form. Local anesthetic =O nat ™ Once inside, the non-ionized molecules are transformed into the more active ionized (charged) form, which binds to the inner vestibule of the sodium channel. In general, small nerve fibers (that carry pain sensation) are more J “ sensitive fo local anesthetics than aa large fibers (motor and other lp ] sensations).Administration: LAs are administered topically, by 8.C. infiltration, or by injection into spinal or epidural spaces. All LAs are vasodilators (except cocaine), so, it should be added to a vasoconstrictor (e.g. epinephrine) to reduce local blood flow and systemic absorption — || systemic toxicity and 11 the duration of action. 1 LAs that contain VCs should not be injected into fingers and toes that are supplied with end arteries, as it may cause tissue necrosis. Absortption: = Lipid-soluble anesthetics are usually more potent and have a longe on of action. = Most local anesthetics are weak bases, they are less effective when they are injected into Infected tissues because the low extracellular PH favors the charged form (ionized) which can not cross lipid membranes. = Addition of bicarbonate to the anesthetic solution maintains the anesthetic in the ate and this increases lipid non-lonized state solubility and enhances penetration of the anesthetic into the nerve sheath. a Dipset Local anesthetic cartridge | color codes Nevly mnt uniforn ten for eal aesbetic ‘aries ens the ADA Selo Aseopance™ PRODUCT Se _ Aidocte percent wien epaepnene see Normal Inflammation NormalCocaine Rarely used Procaine The first synthetic agent No longer used Benzocaine Used for surface anesthesia only Tetracaine Long duration of action Limited use Lidocaine Widely used local anesthetic ignocoine) Used also by IV for ventricular arrhythmia Long duration [Wa compared wh isons, boprcabe 7 he ma] Bupivacaine 127° cardiotoxte |i o Amides — Ropivacaine y-64 widely in obstetric anesthesia Widely used; not for obstetric analgesia because of Prilecaine risk of neonatal methaemoglobinaemia Widely used in dentistry eS Its structure contains both amide and ester bonds Esters Generally occur due to overdose or inadvertent injection into the vascular system. 1. CNS: dizziness, restlessness, tremor, and visual disturbances. Ss i ‘Severe hypotension can develop as a result of VD and cardiac lepression. ‘Spinal anesthesia: 1. Headache due to CSF leakage (the most common). 2. Spinal cord injury. 3. Infection (septic meningitis).