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Drug Metabolism – Biotransformation | Pharmacokinetics (PK)

by Pravin Shukle, MD
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    Welcome to pharmacology by leturio. Today's lecture is about biotransformation. Biotransformation is how the human body changes drugs into different molecules to either make them more useful or less useful to the human body. Now why do humans metabolize drugs? In order to understand that let's go back in time. Let's go back to the age of the cavemen. So you can see here I have a bunch of pictures that look remarkably like hospital administrators. And you can see that as they are evolving they were eating different types of food. It depended on where in the world they were. As we continue to evolve, we start to eat different types of food. Some of the foods were'nt originally meant for our biological system and there were toxins in some of this plants. As we went through the ages, we adapted to those new plants and as we spread out across the planet, we learn to eat different types of food, different types of toxins entered into our body and our body is adapted to metabolize these toxins. These toxins came from plants and when you think about it, it plants are the origin of 80% of drugs. Now how is it that we manage to break down drugs? It's the magic of the cytochrome P450 system. So the cytochrome molecule is an incredibly diverse and incredibly complicated molecule. It is actually a group of isoenzymes that are clumped together and they are coded by 57 different genes. Now in humans there is widespread cytochrome activity. They are found in all of the tissues. The liver, the brain. The only places where you don't see cytochrome is in the bones, muscles and in the red blood cells. Xenobiotics which are those toxins in the plant that I was talking...

    About the Lecture

    The lecture Drug Metabolism – Biotransformation | Pharmacokinetics (PK) by Pravin Shukle, MD is from the course Pharmacokinetics and Pharmacodynamics. It contains the following chapters:

    • Metabolism of Drugs
    • Cytochrome P450
    • 3 Phases of Metabolism
    • Question: Biotransformation

    Included Quiz Questions

    1. will make the drug more hydrophillic, through a phase II (phase 2) process.
    2. will make the drug more hydrophilic through a phase III (phase 3) process.
    3. will make the drug more hydrophilic through a phase I (phase 1) process.
    1. used in the excretion of drugs or toxins into the bile or other fluids, utilizing P-glycoprotiens
    2. useful to excrete drugs into the bile by adding glutathione to the drug or toxin, making it more water soluble.
    3. useful to excrete drugs into the bile by adding a methyl group to the drug or toxin, making it more water soluble.
    4. often used to inhibit the MDR-1 gene.

    Author of lecture Drug Metabolism – Biotransformation | Pharmacokinetics (PK)

     Pravin Shukle, MD

    Pravin Shukle, MD


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