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7 Cards in this Set
- Front
- Back
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LA MoA
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Esters or amides (-caines, wk bases) enter membrane + ionized state binds and holds voltage-gated Na2+ channels open on nociceptor axon to prevent AP propagation.
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Structure-Activity
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Inc PC / inc potency (penetrates). Inc PB / inc DoA (diffuses). Favor alkaline conditions
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Metabolism
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Esters metabolized by plasma buytrylcholinesterases quickly, before systemic fx can occur; lingering ring structure hypersensitivity rx. Amides metabolized by liver enzymes; responsible for peripheral toxicity
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Systemic Toxicity
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CNS excitation followed by depression. Preferably inhibit GABA -> deficient inhibition -> seizures (anti-seizure meds [diazepam or thiopental]). CV vasodilation, dec contractility, arrhythmias (pressor agents)
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Uses
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Topical anesthesia,* anesthesia before parenterals, IV regional anesthesia, peripheral (near nerve) or central (epidural, intrathecal) nerve blockades
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Benzocaine
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Localized due to lack of tertiary amine: may apply to open/irritated skin
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EMLA
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Eutectic mixture of LAs (lido + prilo) - solid with lower MP applied topically 30-60 mins before venipuncture oftentimes
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