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Onset of action

 primarily a result of pKa, but dose and concentration are


also factors
 lower pKa, more rapid onset of action
 Lidocaine (pKa=7.4) has more rapid onset of action
than tetracaine (pKa= 8.6)

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Duration of action
 principally influenced by vasodilator effects of the individual drugs
 all local anesthetics cause some degree of vasodilation except cocaine
 degree of vasodilation is inversely related to duration of action
 the greater the degree of vasodilation, the greater the amount of
drug absorbed by the vascular system, leaving less drug to act on
the nerve cell

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Duration and potency summary

Agents with low Agents with Agents with high


potency and short moderate potency potency and a long
duration and duration duration

procaine (Novocain) lidocaine (Xylocaine) bupivacaine


(Marcaine)
chlorproocaine mepivacine etidocaine
prilocaine

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Effect of Total Dose

 probably the single most important factor in determining


satisfactory local anesthesia
 the greater the dose, other factors being equal, the faster
the onset of action.

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Addition of Epinephrine
 addition of vasoconstrictors is another factor determining the
performance of the local anesthetic
 by decreasing the rate of vascular absorption,
vasoconstrictors cause a higher concentration of local
anesthetic molecules to be available to act on the nerve cell
membrane

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Addition of Epinephrine
Epinephrine
 markedly prolongs duration of action of all local anesthetics when
used for local infiltration or peripheral nerve blocks
 frequently used in combination with local anesthetics at
concentrations of 1:100,000 or 1:200,000
 probably equally effective at much lower doses (1:1,000,000) and
might decrease the danger of an intravascular injection.

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Location of Injection
Intradermal injection
 allows for the most rapid onset of action but the shortest
duration
 more painful than subcutaneous injection
Brachial plexus block injections
 yield some of the longest durations and slowest onsets of
action

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