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34 Cards in this Set
- Front
- Back
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LAs are ____ metabolized and have a _____ toxicity
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Rapidly; low
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Block nerve conduction locally
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LAs
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LAs have a ______ onset; ______ duration
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Rapid; short
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Does not penetrate the skin, absorbs thru mucous membranes
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Cocaine
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Cocaine MOA acts at a ______, is specific. Decreases nerve cell ______
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Definite local receptor; excitability
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Cocaine has some:
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Toxicity and s/e
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Cocaine is used for ____ LA
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Opthalmic
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Cocaine is a potent _____, can be used in the eye and throat
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Vasoconstrictor
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Applied topically only, or in a lozenge. Has poor water solubility; not injectable.
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Benzocaine
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Modification of benzocaine that is stable in solution. Widely used. Can be autoclaved.
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Procaine - novocaine
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Procaine is poorly absorbed ______, used by ________
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Thru the skin; infiltration
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Procaine can be used with a vasoconstrictor such as ____ which would block the spread of the drug beyond the site of administration
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Epi
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In the blood stream, procaine is rapidly _____. May have reactions and sensitivity.
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Hydrolyzed
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Procaine's toxicity is r/t getting in the blood stream where it is metabolized to:
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Derivatives that area allergenic
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Procaine's duration
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Short, 30-60 min
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Better stability and significantly more potent than procaine
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Tetracaine - pontocaine
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Tetracaine has the same basic structure with additional _____ making it more _____.
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CH2 groups; hydrophobic
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Tetracaine is _____ times more potent than procaine.
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16
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Tetracaine structure that makes it longer acting, more hydrophobic
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8 CH groups and a benzene ring
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Tetracaine remains at the site of administration, has a slower ______
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Hydrolysis/metabolism
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Tetracaine is rapidly absorbed thru
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Mucous membranes
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Tetracaine can be used in
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Ointments
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Grandfather of amide subtypes of LAs
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Isogramine
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Has some water solubility, still has a long action tho. Resists hydrolysis, can be autoclaved.
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Mepivacaine
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Very hydrophobic, has an amine group so can form a salt. Resistant to change, hydrolysis, so can remain at site without a change in structure.
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Lidocaine
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Lidocaine can be
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Autoclaved and stored
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Lidocaine has ____ the potency of procaine
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Twice
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Lidocaine is somewhat more ___ than procaine
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Toxic
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Modest solubility, slightly irritating, not used by injecting (applied topically), fast acting, good on mucous membranes; ophthalmology uses
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Phenacaine
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______ can be used in the eye and topically for insect bites and hemorrhoids. Toxic
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Pramoxine
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Effective topically, onset rapid and duration is long
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Dyclomine
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Slight solubility in water, can be used in ointments and suppositories; autoclaved, stable
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Dibucaine
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Dibucaine is among the most _____ of its subtype, also among the most ______
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Potent; toxic
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Dibucaine is the ______ of them all
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Longest acting
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