Pharmacodynamics and Pharmacokinetics Quiz
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Questions and Answers

What is the primary effect of the first-pass effect on drug concentration?

  • It increases the concentration of the active drug in the systemic circulation.
  • It delays the absorption of the drug, leading to a slower release.
  • It has no effect on the concentration of the active drug.
  • It reduces the concentration of the active drug in the systemic circulation. (correct)
  • Which of the following is a consequence of enterohepatic recirculation?

  • Decreased drug half-life
  • Increased rate of drug metabolism
  • Increased drug half-life (correct)
  • Decreased drug absorption
  • Which of the following statements best describes the function of P-glycoprotein?

  • It transports only hydrophilic drugs across cell membranes.
  • It increases the concentration of drugs in the brain tissue.
  • It pumps drugs out of cells and back into the GI tract, reducing absorption. (correct)
  • It facilitates the absorption of drugs from the GI tract into the bloodstream.
  • What is the impact on dabigatran absorption when it is administered with rifampin, an inducer of P-glycoprotein?

    <p>Decreased dabigatran absorption (B)</p> Signup and view all the answers

    What factor directly affects the rate of drug delivery to tissues?

    <p>Cardiac output (B)</p> Signup and view all the answers

    What is the mechanism of drug transport through a biological membrane called?

    <p>Diffusion (B)</p> Signup and view all the answers

    A drug with high hepatic extraction ratio would be most affected by what?

    <p>First-Pass Effect (A)</p> Signup and view all the answers

    P-glycoprotein is located in multiple locations. Which location contains P-glycoprotein?

    <p>Esophagus (B)</p> Signup and view all the answers

    What is bioavailability in the context of drug absorption?

    <p>The degree to which a drug successfully enters systemic circulation and is available for use. (B)</p> Signup and view all the answers

    How does tight binding of a drug to plasma proteins impact its distribution?

    <p>It limits the drug's ability to reach target cells. (A)</p> Signup and view all the answers

    What is the primary purpose of drug metabolism in the body?

    <p>To protect the body by detoxifying small molecules. (B)</p> Signup and view all the answers

    Which of the following is an example of passive transport in drug absorption?

    <p>Diffusion through cell membranes. (D)</p> Signup and view all the answers

    Why are oral drugs often heavily metabolized during their first pass through the liver?

    <p>To reduce their bioavailability. (D)</p> Signup and view all the answers

    Which anatomical barrier protects the fetus from certain substances in a pregnant woman's bloodstream?

    <p>Blood-Placental Barrier (B)</p> Signup and view all the answers

    What is the primary pathway for the excretion of drugs and their metabolites?

    <p>Urination (A)</p> Signup and view all the answers

    What is the role of enzymes in drug metabolism?

    <p>To break down drugs into forms that the body can excrete. (D)</p> Signup and view all the answers

    What predominantly dictates the termination of a drug's action within the body?

    <p>Liver metabolism and kidney elimination. (B)</p> Signup and view all the answers

    Why do highly lipid-soluble drugs often require multiple metabolic processes?

    <p>To become sufficiently water-soluble for kidney excretion. (B)</p> Signup and view all the answers

    What does the half-life of a drug (t1⁄2) represent?

    <p>The time it takes for the amount of drug in the body to be reduced by half. (D)</p> Signup and view all the answers

    According to first-order elimination kinetics, approximately what percentage of a drug is eliminated after five half-lives?

    <p>97% (C)</p> Signup and view all the answers

    What patient-specific factors are important to consider when determining the half-life of a drug?

    <p>Age, kidney and/or liver function (A)</p> Signup and view all the answers

    What is the primary goal of therapeutic drug monitoring (TDM)?

    <p>To maintain a constant drug concentration in a patient’s bloodstream. (B)</p> Signup and view all the answers

    In what circumstance is therapeutic drug monitoring (TDM) most essential?

    <p>For drugs that cause therapeutic and adverse effects. (C)</p> Signup and view all the answers

    Where does the majority of aspirin absorption take place?

    <p>Small intestine (B)</p> Signup and view all the answers

    Which factor primarily determines a drug's ability to cross membranes during diffusion?

    <p>The drug's lipid solubility (B)</p> Signup and view all the answers

    How does the binding of a drug to plasma proteins like albumin affect its distribution and availability?

    <p>It limits the amount of free drug available for distribution to target tissues. (A)</p> Signup and view all the answers

    In a patient with liver disease and reduced albumin production, what is the likely impact on drug distribution for a drug that is normally highly protein-bound?

    <p>Increased risk of adverse effects due to elevated levels of free drug (D)</p> Signup and view all the answers

    A drug that exhibits high tissue binding may result in which of the following?

    <p>Prolonged drug action due to gradual release from the tissue (A)</p> Signup and view all the answers

    How does drug distribution affect both drug efficacy and potential toxicity?

    <p>By influencing the amount of drug reaching active sites and non-target tissues (A)</p> Signup and view all the answers

    Which of the following plasma proteins is considered the MOST important for drug binding?

    <p>Albumin (C)</p> Signup and view all the answers

    A basic drug is administered, and there is a transmembrane pH gradient, with the extracellular pH being more acidic than the intracellular pH. How will this affect the drug's distribution?

    <p>The drug will accumulate in the extracellular space. (A)</p> Signup and view all the answers

    A drug molecule of very large size is administered. What aspect of drug distribution will be MOST affected?

    <p>Ability to cross cell membranes (A)</p> Signup and view all the answers

    What is the primary distinction between a drug's potency and its efficacy?

    <p>Potency indicates the dose required for an effect, while efficacy denotes the maximum effect achievable. (A)</p> Signup and view all the answers

    What determines a ligand's receptor affinity?

    <p>The ligand's capability of binding and remaining bound to a receptor. (D)</p> Signup and view all the answers

    Why isn't a highly potent drug necessarily the most efficacious?

    <p>Because potency relates to the required dose for an effect, while efficacy relates to the maximum achievable effect, which are independent properties. (B)</p> Signup and view all the answers

    What happens when a ligand binds to and activates a receptor?

    <p>It may either increase or decrease a particular reaction or cell function. (B)</p> Signup and view all the answers

    Why is it important for drugs to exhibit relative selectivity, even if absolute specificity is rare?

    <p>To minimize the risk of interacting with multiple receptor subtypes and causing unintended effects. (C)</p> Signup and view all the answers

    A drug has high affinity but low efficacy. What can be inferred about its behaviour?

    <p>It likely acts as an antagonist, binding to the receptor but not fully activating it. (D)</p> Signup and view all the answers

    In the context of receptor binding, what does 'intrinsic activity' refer to?

    <p>The ability of a ligand to activate a receptor and elicit a biological response. (C)</p> Signup and view all the answers

    Which of the following statements correctly relates receptor affinity to ligand-receptor interaction?

    <p>When there is high receptor affinity, the ligand binds well and remains bound long enough to interact with the receptor. (C)</p> Signup and view all the answers

    Which statement accurately distinguishes between drug efficacy and potency?

    <p>Efficacy is the maximum effect a drug can produce, while potency is the amount of drug needed for a given response. (C)</p> Signup and view all the answers

    If two drugs act on the same receptor and produce the same maximal response, but drug A requires a lower dose to achieve 50% of that maximal response, how are the drugs described?

    <p>Drug A has higher potency than Drug B. (C)</p> Signup and view all the answers

    A full agonist is expected to possess which characteristic regarding efficacy when acting at a specific receptor?

    <p>The greatest efficacy, capable of producing the maximum response the receptor can achieve. (D)</p> Signup and view all the answers

    Which of the following factors is LEAST likely to directly influence a patient's response to a drug?

    <p>The drug's cost relative to other medications. (A)</p> Signup and view all the answers

    A doctor is trying to avoid drug interactions in their patient. Which action would be MOST effective in minimizing potential interactions?

    <p>Considering the patient's diet and supplement use. (C)</p> Signup and view all the answers

    A drug interaction occurs when Drug A inhibits the metabolism of Drug B. What is the MOST likely outcome of this interaction?

    <p>Increased plasma concentration of Drug B. (C)</p> Signup and view all the answers

    Which drug-specific factor is MOST likely to be altered to avoid a potential drug interaction?

    <p>The sequence of drug administration. (D)</p> Signup and view all the answers

    If a drug's dose-response curve shifts to the right compared to a reference drug, but both drugs still achieve the same maximal effect, it indicates that the drug:

    <p>Has lower potency. (B)</p> Signup and view all the answers

    Flashcards

    Topical Administration

    Administering drugs through skin or mucous membranes to nearby blood vessels.

    Oral Administration

    Drug absorption through the stomach or intestines lining.

    Bioavailability

    The proportion of a drug that enters systemic circulation and is available for use.

    Blood-Brain Barrier

    A barrier that blocks certain substances from entering brain tissue.

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    First-Pass Effect

    Metabolism of oral drugs in the liver during their first pass, reducing bioavailability.

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    Excretion

    The removal of drugs and their metabolites from the body.

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    Urination in Excretion

    Primary pathway for drug removal via the kidneys.

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    Active Transport

    Drug transport that requires energy to move through cell membranes.

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    Enterohepatic recirculation

    The recycling of drugs and substances from the liver back to circulation, enhancing drug absorption and prolonging effect.

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    P-glycoprotein

    A transmembrane efflux pump that regulates drug uptake and removal in the body.

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    Drug absorption

    The process of a drug entering systemic circulation after administration.

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    Perfusion

    The rate of delivery of blood to tissues, affecting drug distribution.

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    Diffusion in drug transport

    The movement of a drug from systemic circulation to tissues through biological membranes.

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    Capillary permeability

    The ability of substances to pass through capillary walls into tissues.

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    Diffusion

    The process by which drug molecules move from areas of high concentration to low concentration.

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    Lipid Solubility

    The ability of a drug to dissolve in fats, affecting its absorption and distribution.

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    Transmembrane pH Gradient

    The difference in pH across a membrane impacting weak acids/bases' distribution.

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    Molecular Size

    The size of the drug molecule affects its ability to diffuse across membranes.

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    Protein Binding

    The extent to which drugs attach to proteins in the bloodstream, affecting availability.

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    Albumin

    The most important protein in plasma that binds many drugs, affecting their distribution.

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    Tissue Binding

    The binding of drugs to specific tissues, which can influence their effects and side effects.

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    Adverse Effects

    Negative reactions resulting from drugs binding to unintended tissues.

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    Elimination

    The final step in pharmacokinetics that terminates a drug's action through excretion.

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    Half-Life

    The time it takes for half the drug in the body to be reduced, indicating drug elimination rate.

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    First-Order Elimination

    When a constant fraction of the drug is eliminated over time, not a constant amount.

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    Therapeutic Drug Monitoring (TDM)

    Measuring drug levels in the blood to ensure effective and safe dosages.

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    Lipid Soluble Drugs

    Drugs that are difficult to excrete due to their high fat solubility, requiring metabolism into water-soluble forms.

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    Factors Affecting Half-Life

    Includes dosing interval, drug duration, and patient-specific factors like age and organ function.

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    Absorption Process

    The method by which drugs enter the bloodstream after administration, crucial for drug effectiveness.

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    Villi in Small Intestine

    Tiny finger-like projections that increase surface area for maximum drug absorption.

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    Efficacy

    The extent to which a drug produces a response at full receptor occupancy (Emax).

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    Potency

    The amount of drug required to produce a specific response (e.g., EC50 or ED50).

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    Full Agonist

    A drug that produces the maximum response possible at a receptor when binding occurs.

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    Comparing Potency

    Less potent drugs can achieve similar efficacy if given in higher doses.

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    Dose-Response Curve

    A graph showing the relationship between drug dose and its effect, illustrating efficacy and potency.

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    Drug Interaction Factors

    Elements that can influence drug response include drugs, food, supplements, and disease.

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    Patient Factors

    Individual characteristics affecting drug interactions, like genetics and diet.

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    Metabolism and Drug Interactions

    Interactions often involve drug metabolism affecting drug response levels.

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    Affinity

    The strength with which a ligand binds to a receptor.

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    Intrinsic Activity

    The ability of a drug to activate a receptor after binding.

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    Receptor Specificity

    The ability of a ligand to bind only to certain receptors.

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    Receptor Affinity

    How well a ligand can bind and stay bound to a receptor.

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    Selectivity

    The preference of a drug to act on one type of receptor over others.

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    Ligands

    Molecules, including drugs, that bind to receptors to cause effects.

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    Study Notes

    Pharmacodynamics and Pharmacokinetics

    • Pharmacodynamics (PD) is the study of how a drug affects the body, including receptor binding, post-receptor effects, and chemical interactions.
    • Pharmacokinetics (PK) is the study of how the body affects a drug, including absorption, distribution, metabolism, and excretion (ADME).

    Drug-Receptor Interactions

    • Drugs interact with specific cellular receptors, typically proteins.
    • Agonists: Bind to receptors and activate them, mimicking endogenous substances.
    • Antagonists: Bind to receptors without activating them, blocking endogenous substances or agonists.

    Potency and Efficacy

    • Potency: The amount of a drug needed to produce a given effect. A higher potency means a lower dose is required.
    • Efficacy: The maximum effect a drug can produce. A drug can be potent but not efficacious.

    Receptor Affinity

    • Receptor affinity: The extent to which a ligand binds to a receptor.
    • High affinity means the ligand binds well and remains bound to the receptor long enough to interact with it.
    • Low affinity means poor bonding and the ligand does not interact with the receptor for a significant duration.

    Intrinsic Activity

    • Intrinsic activity is the extent to which a ligand activates the receptor.
    • Full agonists produce a large effect on the postsynaptic cell when they interact with a receptor.
    • Partial agonists produce a weaker effect compared to full agonists, and
    • Antagonists produce no effect of their own, only block the effects of other ligands from binding to a receptor.

    Drug Interactions

    • Drug interactions occur when a drug modifies the action of another drug or other substances.
    • Genetic factors, age, disease, diet, route of administration etc. are some factors can modify the actions of a drug.

    Pharmacogenomics

    • Pharmacogenomics is the study of how genes affect a person's response to drugs.
    • It involves identifying gene variations that influence how drugs are metabolized, transported, and interact with targets.
    • This can allow for tailored drug therapy to optimize efficacy and safety.

    ADME Summary

    • Absorption: The process by which a drug moves from its site of administration into systemic circulation.
    • Distribution: The process by which a drug moves from systemic circulation to the tissues.
    • Metabolism: The process by which the body changes a drug into a different form, usually to enhance excretion.
    • Excretion: The process by which a drug or its metabolites are removed from the body.

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