Local Anesthetic and Muscle Relaxant Flashcards
Spinal anesthesia
CSF in lumbar region→ blocks sympathetic fibers in subarachnoid space
Epidural anesthesia
injection into epidural space
Nerve block
Injection into peripheral nerve endings/ trunks
Infiltration anesthesia
Injection into tissue
Disadvantage of infiltration anesthesia
Requires large amount of drugs
Anesthesia w/o disrupting normal body function
Infiltration anesthesia
Bier’s block
IV regional anesthesia
Esters differ from amides b/c
Esters: shorter duration of action and increase systemic toxicity
Local anesthetic: weak acid or weak base
Weak base
LA: Predominantly ionized or non-ionized
Ionized
Hydrophobic pathway: In order for LA to cross the membrane, it must be ____ and once inside it becomes _____ (binds to Na+ ch)
Non-ionized, ionized
The closer the pka is to physio pH, the higher the concentration of the drug in the _____
non-ionized form (faster membrane transport –> faster onset of action)
Drug always in the non-ionized form; very lipphilic
Benzocaine
Topical use only
Benzocaine
Makes pH more basic and increase non-ionized drug concentration
Bicarbonate
LA: more effective in resting axon or rapidly firing axon
Rapidly firing axon
Potency of the LA drugs are correlated to
Lipid solubility and duration of action
LA duration of action is dependent on
site of action
LA toxic effects are dependent on
half life
Absorption is affected by:
dosage, site of injection, drug-tissue binding, chemical properties of the drug, local blood flow, vasoconstricting agents (epinephrine)
Vasoconstricting agent would do what to LA
Decrease diffusion of drug –> prolong duration of action
Decrease systemic absorption
Decreases risk of systemic toxicity
Amides metabolized by
CYP450s in the liver
Esters metabolized by
Butyrycholinesterases in the plasma
Metabolites of esters and amides excreted via
renal