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Factors Affecting Drug Efficacy
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Factors Affecting Drug Efficacy

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Questions and Answers

What is the primary function of Verapamil in the context of pharmacology?

  • Anticancer drug
  • P-glycoprotein inhibitor (correct)
  • Immune suppressive
  • Cytochrome P450 3A4 inhibitor

    • Which of the following drugs is an immune suppressive used in kidney and liver transplant patients?

  • Pioglitazone
  • Cerivastatin
  • Rosiglitazone
  • Tacrolimus (correct)

    • What is the primary consequence of Cytochrome P450 3A4 inhibition in clinical pharmacology?

  • Reduced drug efficacy
  • Increased drug toxicity
  • Pharmacokinetic-pharmacodynamic consequences (correct)
  • Enhanced drug activity

    • What is the role of transporters in drug interactions, according to Han (2011)?

    <p>Playing a crucial role in drug interactions</p> Signup and view all the answers

    Which of the following is a CP2C8 substrate?

    <p>Morphine</p> Signup and view all the answers

    What is the primary mechanism of action of dietary nutraceuticals in enhancing anticancer drug activity, according to Khan et al. (2015)?

    <p>Modulating P-glycoprotein</p> Signup and view all the answers

    Which enzyme is primarily responsible for metabolizing warfarin to 7-hydroxy warfarin?

    <p>CYP2C9</p> Signup and view all the answers

    What is the effect of carbamazepine on warfarin metabolism?

    <p>It reduces the effect of warfarin by inducing CYP1A2</p> Signup and view all the answers

    What is the effect of grapefruit juice on intestinal drug metabolism?

    <p>It inhibits both CYP3A4 and P-gp</p> Signup and view all the answers

    What percentage of variation in oral clearance of Cyclosporin A is accounted for by P-Glycoprotein (Pgp)?

    <p>17%</p> Signup and view all the answers

    What is the effect of St John's Wort on P-gp?

    <p>It induces P-gp</p> Signup and view all the answers

    Which of the following is an example of an extrinsic factor that can impact drug efficacy?

    <p>Foodstuff-drug interactions</p> Signup and view all the answers

    What happens to gemfibrozil upon phase II metabolism?

    <p>It becomes a potent inhibitor of CYP2C8</p> Signup and view all the answers

    What is the term for the exchange of DNA with neighbours?

    <p>Migration</p> Signup and view all the answers

    What is the effect of amiodarone on warfarin metabolism?

    <p>It prolongs the action of warfarin by inhibiting CYP2C9</p> Signup and view all the answers

    What is the name of the protein that pumps drugs back into the G.I. tract?

    <p>P-Glycoprotein (Pgp)</p> Signup and view all the answers

    What is the term for the process by which one allele has an advantage over another?

    <p>Selection</p> Signup and view all the answers

    What is an example of a 'consumer drug' that can interact with pharmaceutical drugs?

    <p>St. John's Wort</p> Signup and view all the answers

    What is the primary focus of the 2003 study mentioned in the text?

    <p>Investigating the toxicological relevance of CYP3A4 induction</p> Signup and view all the answers

    Which study found that prospective genetic screening decreases the incidence of abacavir hypersensitivity reactions?

    <p>The Western Australian HIV cohort study</p> Signup and view all the answers

    What is the topic of the 2010 review by Sivasubramanian et al.?

    <p>Abacavir/Lamivudine combination therapy in treating HIV</p> Signup and view all the answers

    What is the role of HLA B∗5701 status according to the 2013 study by The UK Collaborative HIV Cohort Study Steering Committee?

    <p>Determining disease progression and response to antiretroviral therapy</p> Signup and view all the answers

    What is the topic of the 2013 review by Yoshida et al.?

    <p>Hepatic and intestinal drug transporters: prediction of pharmacokinetic effects</p> Signup and view all the answers

    Which study discussed the importance of cancer drug resistance in the context of cancer treatment?

    <p>The 2013 study by Holohan et al.</p> Signup and view all the answers

    Humans are exposed to fewer than 100 different chemicals every day.

    <p>False</p> Signup and view all the answers

    P-Glycoprotein (Pgp) is a drug transporter that pumps drugs into the G.I. tract.

    <p>False</p> Signup and view all the answers

    Intrinsic factors that can impact drug efficacy include environmental factors such as grapefruit juice.

    <p>False</p> Signup and view all the answers

    Random Drift is a process where one allele has an advantage over another.

    <p>False</p> Signup and view all the answers

    Warfarin is an example of a 'perpetrator' drug in terms of drug-drug interactions.

    <p>False</p> Signup and view all the answers

    The primary focus of the lecture is to explain the rationale behind steps that can be taken to increase the risk of adverse effects or loss of efficacy in a drug.

    <p>False</p> Signup and view all the answers

    Warfarin is primarily metabolized by CYP3A4.

    <p>False</p> Signup and view all the answers

    Fluvoxamine is a substrate of CYP2C9.

    <p>True</p> Signup and view all the answers

    Carbamazepine increases the effect of warfarin by inhibiting CYP2C9.

    <p>False</p> Signup and view all the answers

    Grapefruit juice induces intestinal CYP3A4.

    <p>False</p> Signup and view all the answers

    Gemfibrozil becomes a potent inhibitor of CYP2C9 upon phase II metabolism.

    <p>False</p> Signup and view all the answers

    St. John's Wort is an inhibitor of P-gp.

    <p>False</p> Signup and view all the answers

    Tacrolimus is used to treat kidney and liver transplant patients and is a CP2C8 substrate

    <p>False</p> Signup and view all the answers

    Verapamil is a P-gp inhibitor that can increase the bioavailability of certain drugs

    <p>True</p> Signup and view all the answers

    Cytochrome P450 3A4 inhibition always leads to decreased drug efficacy

    <p>False</p> Signup and view all the answers

    Rosiglitazone is a CP2C8 substrate that can also inhibit P-gp

    <p>False</p> Signup and view all the answers

    Paclitaxel is a CP2C8 substrate that can be affected by the activity of P-gp

    <p>True</p> Signup and view all the answers

    Dietary nutraceuticals can always enhance the activity of anticancer drugs

    <p>False</p> Signup and view all the answers

    The study by Holohan et al. (2013) discusses the role of HLA B∗5701 status in disease progression.

    <p>False</p> Signup and view all the answers

    The 2003 study evaluated the toxicological relevance of CYP3A4 inhibition.

    <p>False</p> Signup and view all the answers

    The review by Sivasubramanian et al. (2010) focuses on the treatment of HIV using Abacavir/Lamivudine combination.

    <p>True</p> Signup and view all the answers

    The study by Rauch et al. (2006) found that prospective genetic screening increases the incidence of abacavir hypersensitivity reactions.

    <p>False</p> Signup and view all the answers

    The study by The UK Collaborative HIV Cohort Study Steering Committee (2013) found that HLA B∗5701 status has no impact on disease progression.

    <p>False</p> Signup and view all the answers

    The review by Yoshida et al. (2013) focuses on the role of transporters in drug interactions and genetic polymorphisms.

    <p>True</p> Signup and view all the answers

    Study Notes

    Factors Affecting Drug Efficacy

    • Drug interactions can occur with pharmaceuticals, consumer drugs, foodstuffs, and environmental chemicals, leading to adverse effects or loss of efficacy
    • Intrinsic factors, such as genetics, can impact drug interactions and efficacy
    • Extrinsic factors, such as environmental chemicals, can also affect drug interactions and efficacy

    Cellular Effects

    • Changes in metabolism enzymes can affect drug interactions and efficacy
    • Tissue effects, such as inflammation, can also impact drug interactions and efficacy

    Environmental Factors

    • Humans are exposed to thousands of chemicals daily, which can interact with biological systems
    • Pharmaceutical interactions can occur between different drugs, leading to adverse effects or loss of efficacy
    • Induction, inhibition, and food-drug interactions can all impact drug efficacy

    Intrinsic Factors: Genetics

    • Genetic mutations, errors in DNA copying, and genetic drift can all impact drug interactions and efficacy
    • Genetic variations can affect drug transporters, such as P-glycoprotein (Pgp), which pumps drugs out of the body
    • Genetic variations can also affect drug-metabolizing enzymes, such as CYP2C9, which can impact warfarin metabolism

    Drug Transporters

    • P-glycoprotein (Pgp) is a drug transporter that pumps drugs out of the body
    • Pgp can affect the oral clearance of drugs, such as Cyclosporin A
    • Inducers of Pgp, such as St. John's Wort, can decrease drug efficacy
    • Inhibitors of Pgp, such as grapefruit juice, can increase drug efficacy

    Warfarin Metabolism

    • Warfarin has a narrow therapeutic window and is metabolized by multiple enzymes, including CYP2C9
    • Substrates for CYP2C9, such as fluvoxamine, can interact with warfarin
    • Inhibitors of CYP2C9, such as gemfibrozil, can increase warfarin's effect
    • Inducers of CYP4A4 and CYP1A2, such as carbamazepine and clozapine, can decrease warfarin's effect

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    Description

    This quiz covers the factors that influence a drug's effectiveness in the body. Learn about intrinsic and extrinsic factors affecting drug interaction and how to minimize adverse effects and loss of efficacy. Test your knowledge of pharmacology!

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