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Pharm Exam #2 - LAs
local anesthetics
13
Pharmacology
Graduate
10/29/2010

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Term
Lidocaine (Xylocaine)
Definition
LOCAL ANESTHETIC
least toxic
first amide-type local anesthetic
Developed by Niles Lofgren 1943
Marketed in 1948
Metabolized in the liver
Excreted by the kidneys
LA by which all others are compared
Term
Mepivacaine
Definition
LOCAL ANESTHETIC
similar to lidocaine, but less vasodilation
slightly greater potency and duration
useful in epidural, spinal, peripheral nerve block and local infiltration
*potential for accumulation makes it unsuitable for prolonged epidural infusion*
Term
Ropivacaine
Definition
LOCAL ANESTHETIC
less potent but less toxic than bupivacaine(less cardiotoxic)
almost pure S isomer
better frequency-dependent block
several concentrations: 0.2% (relief post-op), 0.5% (block for surgery), 1%
Term
Bupivacaine
Definition
LOCAL ANESTHETIC
greater potency and duration
slower onset
several concentrations from 0.05 to 0.75% (0.75% is not recommended in obstetrics)
Good for spinal anesthesia as isobaric or hyperbaric solution
epinephrine adds little to duration (pre-treat with epinephrine to make it last longer)
Significant frequency-dependent block
cardiac toxicity issues (high systemic blood levels)
Term
Tetracaine
Definition
LOCAL ANESTHETIC
"forever-caine"
slow onset due to high pKa
Long duration
Maximum dose is 100mg
Excellent topical anesthestic
sometimes sensory will return before motor
Term
Cocaine
Definition
LOCAL ANESTHETIC
produces vasoconstriction
sometimes used in ENT or lung surgery
Term
Novocaine (Procaine)
Definition
LOCAL ANESTHETIC
fast acting, short acting
first injectable anesthetic to be synthesized
Classified as an ester - metabolized in the plasma by Pseudocholinesterase
Excreted by the Kidneys
Developed by Alfred Einhorn in 1904-1905
Term
2-Chloroprocaine
Definition
LOCAL ANESTHETIC
safe, duration short but not v. short
last of the esters introduced and one of the safest in terms of toxicity
Duration of 45-60 min
Rapid termination of effect
IV -- causes thrombophlebitis
Term
Benzocaine
Definition
LOCAL ANESTHETIC
(sore throat spray) not v. potent
first synthetic LA
Benzoic acid derivative
Effective only in high concentration
Used mostly in mucous membranes
Methemoglobinemia
Term
Dibucaine
Definition
LOCAL ANESTHETIC
high potency and toxicity
inhibitor of plasam cholinesterase
only for topical use as a cream (through skin, takes a long time to get through and start working)
test to see if proble with succinylcholine
Term
Prilocaine
Definition
LOCAL ANESTHETIC
Most rapidly metabolized amide LA
Has an Ortho-Toluidine ring, which produces methemoglobinemia
Term
Epinephrine
Definition
ADJUVANT
may decrease absorption and prolong duration, also used as a monitor
can increase HR
*many pts think they are allergic to LA, when it really was just a rxn to the epinephrine*
Term
Bicarbonate
Definition
ADJUVANT
Increases pH of the solution, accelerating onset
may decrease duration
may precipitate in Ropivacaine and Bupivacaine
(easier to go through cell membrane so works faster, only need little bit)
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