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ODR
Pharm Local Anesthetics
25
Pharmacology
Graduate
12/12/2010

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Cards

Term
How do local anesthetics work?
Definition
They interrupt irritation & propagation of impulses in axons by blocking Na+ conduction into cell either physically or causing a conformational chnage
blockade is conc-dep and reversible
cell integrity/fxn is unaffected
Term
What are the physical properties of anesthetics?
Definition
weak bases/poorly H20 soluble
synthetic: derived from cocaine
hydrophilic and lipophilic ends joined by an ester or amide
aqueous solutions of HCl salts of tertiary amines
Term
What type of fibers are affected first by anesthetics?
Definition
small or unmyelinated (B&C)
- large myelinated (A fibers-motor) require larger amounts to be blocked
Term
What is the difference in metabolism between ester and amide anesthetics?
Definition
esters: hydrolysis by psuedocholinestserase
amides: metabolized by liver enzyme
Term
How does pKA affect the onset of anesthetics?
Definition
anesthetic must be in un-ionized form for nerve penetration; the cation form delays onset of action
high pKA= slow onset
Term
What are the symptoms of anesthetic toxicity?
Definition
initially: light headedness, dizziness, visual/aud disturbances, disorientation, drowsiness
higher doses: muscle twitching, convulsions, unconsciousness, coma, resp deperssion & arrest, CV depression & collapse
cardiac: myocardial depression, cardiac arrythmias, cardiotoxicity in pregnancy, negative inotrope (hypotension)
periph: vasoconstriction at low doses, vasodilation at high doses
methemoglobinemia
muscle necrosis (spont reversed in ~ 2 wks)
allergic rxns
Term
How is anesthetic toxicity treated?
Definition
stop injection, open airway/O2, seizures: benzodiazepene, CPR, intralipid (for bupivicane assoc cardiac arrest), methylene blue for methemoglobulinemia
Term
cocaine
Definition
naturally occurring anesthetic
vasoconstriction (blocks catech reuptake)
onset: 4-5min
AE: abuse
Term
procaine
tetracaine
2-cholorporcaine
benzocaine
Definition
esters
procaine: excreted by kidneys
tetracaine: high pKa/slow onset, long duration,excellent topical
2-cholor: 45-60 min duration but AE: thrombophlebitis, safest toxicity
benzocaine: effective only in high conc, used mostly in mucus membranes AE: methemoglobinemia
Term
which ester anesthetic has the safest toxicity?
Definition
2-chloroprocaine
Term
Which ester anesthetic is good for topical use?
Definition
tetracaine
Term
Which ester anesthetic has an AE of methemoglobinemia?
Definition
benzocaine
Term
lidocaine
Definition
an amide; metab in liver and excreted by kidneys
Term
dibucaine
Definition
an amide
high potency/toixicity; inhibits plasma cholinesterase
topical use only
Term
mepivacaine
Definition
similar to lidocaine but less vasodilation
useful in epidural, spinal, periph nerve blocks, local infiltration
AE: potential for accumulation, so unsuitable for prolonged epidural infusion
Term
Bupivicaine
Definition
greater potency/duration, but slow onset
good for spinal anesthesia as isobaric or hyperbaric solution
significant frequency-dependent block
AE: cardiac toxicity
Term
Which anesthestics are good for spinal anesthesia?
Definition
mepivicaine, bupivicaine
Term
Which anesthetics cause frequency-dependent block?
Definition
bupivicaine and ropivicaine
Term
What anesthetics cause methemoglobinemia?
Definition
benzocaine and prilocaine
Term
How do epinephrine and bicarbonate affect anesthetics?
Definition
epi: decreases absorption (via local vasoconstriction) and prolongs duration
bicarbonate: increases pH of solution and accelerates the onset, but may decrease duration; may precipitate ropivicaine and bupivacaine
Term
What local anesthetics are used topically?
Definition
tetracaine and dibucaine
Term
What drug is used for epidural, spinal and peripheral nerve block, and what are it's risks?
Definition
mepivocaine
risk of accumulation, so it is unsuitable for epidural infusion
Term
Which local anesthetics can cause methemoglobinemia?
Definition
benzocaine and prilocaine
Term
Which local anesthetic is cardiotoxic?
Definition
bupivicaine
Term
Which local anesthetic can cause thrombophlebitis?
Definition
2-chloroprocaine
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