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Pharm 212 Local Anesthetics
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Published
04/01/2024
ANESTHESIA (DEFINITION AND CATEGORIES) ❑ Anesthesia -- {{c1::reversible}} condition induced by {{c1::anesthetic drugs}} that cause {{c2::reduction}} o…
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LOCAL ANESTHETICS CHEMISTRY AND STRUCTURE{{c1::}}{{c1::lipophilic}} group -- {{c2::benzene ring}}{{c1::intermediate}} bond -- {{c2::ester}} or {{c2::a…
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ESTER VS AMIDE LOCAL ANESTHETICSamides are metabolized in the {{c1::liver}} and ester are metabolized in {{c1::plasma}}Esters and amides differ in the…
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Common Local Anesthetics: The “Caines”Amides {{c1::bupivacaine}}{{c1::levobupivacaine}}{{c1::mepivacaine}}{{c1::ropivacaine}}{{c2::etidocaine}}{{…
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“CAIN” ALTERNATIVES WITH LOCAL ANESTHETIC ACTIVITY (LESS ALLERGY)1) {{c1::Diphenhydramine}} {{c2::first-generation, sedating, oral antihistamine}}{{c2…
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{{c1::diphenylmethane}}
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{{c1::Phenothiazine}}
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LOCAL ANESTHETIC MECHANISM OF ACTION{{c1::Extracellular anesthetic}} exists in equilibrium between {{c2::charged}} and {{c2::uncharged}} formsThe {{c3…
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STRUCTURE ACTIVITY RELATIONSHIP Two important chemical properties of local anesthetics that impact activity, {{c1::intrinsic potency}}, {{c1::duration…
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LIPOPHILIC-HYDROPHOBIC BALANCE Lipophilic means “fat” loving and expresses the tendency of local anesthetic molecules to {{c1::bind with membrane lipi…
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HYDROGEN ION CONCENTRATION Local anesthetics exist as a {{c1::weak base}}in solution, LA exist in equilibrium between {{c2::basic non-ionized form (B)…
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IONIZED VS NON-IONIZED FORMS Each form has its own specific {{c1::mechanism of action.}}{{c1::Non-ionized (lipid soluble)}} penetrates the {{c2::neura…
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IONIZED VS NON-IONIZED FORMS pKa expresses the relationship between {{c1::ionized}} and {{c1::non-ionized}} forms of local anestheticpKa is the {{c2::…
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CLINICAL IMPLICATIONS OF IONIZED AND NON-IONIZED FORMS OF LAS Local anesthetics are prepared in a {{c1::water soluble HCl salt}} with a pH of {{c1::6-…
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OTHER FACTORS THAT AFFECT POTENCY OF LOCAL ANESTHETICS {{c1::Vasoconstrictor/vasodilator properties }}affects the {{c2::rate of vascular uptake}}…
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PHARMACOKINETICS Involves the {{c1::medication/body}} interaction or {{c1::how the body ‘handles’ the medication.}} Principles include {{c1::abso…
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LOCAL ANESTHETIC BLOOD CONCENTRATION DETERMINANTS Amount of {{c1::local anesthetic injected (dose and volume)}} {{c1::Absorption}} rate {{c1::Site of …
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PATIENT RELATED FACTORS CONCERNING BLOOD CONCENTRATION OF LOCAL ANESTHETICS ❑ {{c1::Age}} ❑ {{c1::CV (cardiovascular)}} status ❑ {{c1::Hepatic}} funct…
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SYSTEMIC ABSORPTION OF LOCAL ANESTHETICS ❑ Site of injection ❑ {{c1::Dose}} and {{c1::volume}} ❑ Addition of a {{c1::vasoconstrictor}} beneficial effe…
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SITE OF INJECTION great impact on the {{c1::blood levels}} of local anestheticsThe more {{c1::vascular}} the tissue, the greater the {{c1::uptake}} an…
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DOSE AND VOLUME ❑ The blood concentration of a local anesthetic is proportional to the {{c1::total dose}} of local anesthetic. ❑ Higher blo…
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ADVERSE EFFECTS OF LOCAL ANESTHETICS • Local Anesthetic Systemic Toxicity (LAST) -- {{c1::rapid onset of severe CNS depression, seizure…
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LOCAL ANESTHETIC TOXICITY ROPIVACAINE ❑ Ropivacaine has {{c1::similar structure}} to the {{c2::bupivacaine}} with {{c1::only one less carbon atom}} bu…
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LOCAL ANESTHETIC TOXICITY BUPIVACAINE ❑ With bupivacaine there is a small disparity in blood concentrations between {{c1::CNS signs}} and {{c1::sympto…
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LOCAL ANESTHETIC TOXICITY LIDOCAINE ❑ More later but signs and symptoms {{c1::vary}} among local anesthetics… ❑ With lidocaine there is a large dispar…
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