Overview – Local Anesthetics

by Pravin Shukle, MD

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    Welcome to pharmacology by Lecturio. I'm Dr. PJ Shukle and we're going to talk about local anesthetics and oral analgesics. And I'm going to introduce you to the interesting world of controlling pain. Now, here's the problem with this particular type of patient. We need to get a drug across a lipid membrane and act on the inside of the cell, on the inside surface of a channel, to stop the movement of sodium ions. The problem is that the outside of the cell is water, the membrane is lipid, the inside is water. So, how do we change the properties of the drug to be both lipophilic and hydrophilic? Remember that membrane diffusion in this case is going to be a passive process. Unfortunately, there are no active transportase to bring the drug across the membrane. We want to block the receptor from the inside surface. And we want to block movement of sodium channels across that membrane. The reason why we do that is because blocking sodium channels will reduce membrane depolarization. And reducing membrane depolarization will prevent that nerve from firing and therefore the pain response will not reach your brain. We need the polar form of the drug to turn into a nonpolar drug, and then turn back into a polar drug and then do its job. How do we do that? Well, I'm going to bring back the pKa lecture. Now, you thought you got away with never having to deal with pKa once we finished our original pharmacology lectures, I think it was the second lecture we did. Well, here's where pKa really makes a different. So, lidocaine is a local anesthetic. It has a pKa of 7.7. And if you think back to that original lecture, remember that pKa means that 50% of...

    About the Lecture

    The lecture Overview – Local Anesthetics by Pravin Shukle, MD is from the course CNS - Pharmacology.

    Included Quiz Questions

    1. The medications change from nonpolar to polar, pass through the membrane, and then return to an active, nonpolar form.
    2. Active transport pumps the medication into the nerve cells.
    3. Endocytosis at the synaptic cleft.
    4. The medication is converted into a base locally, with the use of a bicarbonate adjuvant. Once modified the medication is activated in the kidney and returned to locally anesthetize the tissue.
    5. The medication interacts with the extracellular matrix, resulting in a secondary messengers cascade to cause anesthesia.
    1. Distribution of nodes of Ranvier
    2. Size of the fiber
    3. Methylation of the fiber
    4. Activity of the fiber
    5. Location of the fiber in the nerve bundle
    1. Hypercalcemia due to multiple myeloma
    2. Undiagnosed hyperkalemia
    3. Drug seeking behavior
    4. Anxiety
    5. Metabolic alkalosis
    1. Neural tissue
    2. Skeletal muscle
    3. Skin and adipose
    4. Tendons and ligaments
    5. Cardiac muscle

    Author of lecture Overview – Local Anesthetics

     Pravin Shukle, MD

    Pravin Shukle, MD

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