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Esters and Amides – Local Anesthetics

by Pravin Shukle, MD
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    So, let's talk about these drugs. There are the topical agents like cocaine and benzocaine. There are the parenteral agents like procaine and tetracaine. And then in terms of the amides, there are the medium acting drugs like lidocaine, and long acting drugs like bupivacaine. Let's focus on these esther type drugs, the topical agents cocaine and benzocaine. Now, cocaine is a very potent vasoconstrictor in tissues, and it has excellent anesthetic qualities. The best use is for mucous membrane surgical procedures. So, let's suppose we have an ENT surgeon who needs to do surgery on the inside of the nose or the nasal cavity. Now the problem with cocaine obviously is it's significant side effect profile. It's a drug of abuse as well as medicinal use. It has cardiovascular implication. It's a sympathomimetic, so you can have quite severe hypertension and quite severe arrhythmias with this drug. It can cause cerebrovascular issues such as an intracranial hemorrhage or stroke. This is in part related to its effect on blood pressure. It can cause psychiatric issues. At low doses, it causes euphoria, which is why cocaine is used as an illegal street drug. It can cause hyperexcitability, mania and psychosis. And of course, it has a high addictive potential. Benzocaine has become the replacement to cocaine, but we still use cocaine now and then. It is a low strength anesthetic. Instead of being a vasoconstrictor, it's actually a vasodilator. It has fairly good topical activity, and it also will block sodium channels. Now, we use this drug for cough drops. It's that brackish taste that you taste when you put in one of those cough drops into the back of your throat, and it sooths by actually anesthetizing the mucous membranes. It is found very commonly in over the counter...

    About the Lecture

    The lecture Esters and Amides – Local Anesthetics by Pravin Shukle, MD is from the course CNS - Pharmacology. It contains the following chapters:

    • Esters - Topical Agents
    • Esters - Parenteral Agents
    • Amides - Medium Action
    • Amides - Long Action

    Included Quiz Questions

    1. Ester anesthetics are generally considered short term anesthetics while amide anesthetics are considered medium or long term anesthetics.
    2. Amide anesthetics are more potent than ester anesthetics.
    3. Ester anesthetics are more potent than amide anesthetics.
    4. Amide anesthetics have a high potential for abuse.
    5. Amide anesthetics are generally considered short term anesthetics while ester anesthetics are considered medium or long term anesthetics.
    1. A 17 year old with nasal polyps and a history of substance abuse.
    2. A 44 year old female with a history of fibroids and dental caries.
    3. A 4 year old requiring direct nasal turbinate inspection with a nasal speculum and local anesthesia.
    4. A 78 year old female with iatrogenic gingival hyperplasia and a history of seizures.
    5. A 25 year old female with difficulty becoming pregnant.
    1. Cardiotoxicity
    2. Vasodilation
    3. Vasoconstriction
    4. Disruption of RAAS system
    5. Pulmonary fibrosis
    1. She is likely having a reaction to the ester anesthetic breakdown byproducts.
    2. This is probably an undiagnosed congenital metabolic disorder.
    3. This could be an idiopathic porphyria.
    4. She is likely having a reaction to the amide anesthetic breakdown byproducts.
    5. She is likely suffering from a factitious disorder.

    Author of lecture Esters and Amides – Local Anesthetics

     Pravin Shukle, MD

    Pravin Shukle, MD


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