Pharmacology and Pharmacokinetics Overview
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Questions and Answers

What is a primary advantage of enteric-coated preparations?

  • They protect the drug from stomach acid. (correct)
  • They are less expensive than other formulations.
  • They allow for more frequent dosing.
  • They have a faster absorption rate than immediate-release drugs.
  • What is the main purpose of extended-release (ER) formulations?

  • To enhance first-pass metabolism.
  • To reduce the frequency of doses required. (correct)
  • To achieve higher peaks of drug concentration.
  • To provide immediate relief from symptoms.
  • Why are sublingual and buccal routes beneficial for drug administration?

  • They are less effective than oral medications.
  • They require more complex administration techniques.
  • They avoid first-pass metabolism and ensure rapid absorption. (correct)
  • They provide the slowest drug absorption.
  • Which drug is commonly cited as benefiting from parenteral administration due to poor absorption in the GI tract?

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

    What is a challenge associated with oral drug absorption that is highlighted in the content?

    <p>The complex pathways involved in absorption. (C)</p> Signup and view all the answers

    How do extended-release formulations maintain therapeutic drug concentrations?

    <p>By controlling the release rate of the drug. (D)</p> Signup and view all the answers

    What is a common example of a drug that is irritative to the stomach and may benefit from enteric-coating?

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

    In which scenario is parenteral administration most often utilized?

    <p>When quick action is required and oral medication is impractical. (D)</p> Signup and view all the answers

    Which form of a weak base is able to permeate through cell membranes more readily?

    <p>Uncharged form (B) (A)</p> Signup and view all the answers

    How does pH influence drug absorption in weak acids?

    <p>A higher pH decreases the proportion of uncharged forms. (C)</p> Signup and view all the answers

    Which of the following factors enhances drug absorption through the intestine?

    <p>Greater surface area due to microvilli (C)</p> Signup and view all the answers

    What role does P-glycoprotein play in drug absorption?

    <p>Reduces drug absorption by pumping drugs out of cells. (A)</p> Signup and view all the answers

    What happens to drug absorption in cases of severe diarrhea?

    <p>Absorption is decreased due to rapid movement through the GI tract. (D)</p> Signup and view all the answers

    Which property of weak bases is determined by its pKa?

    <p>The effective concentration of the uncharged and charged forms (A)</p> Signup and view all the answers

    Which statement correctly describes the absorption from the intestines compared to the stomach?

    <p>Drug absorption is favored from the intestine due to higher blood flow. (C)</p> Signup and view all the answers

    What is the main consequence of increased expression of P-glycoprotein at the absorption site?

    <p>Decreased drug absorption leading to lower effective doses. (D)</p> Signup and view all the answers

    What is the significance of first-pass metabolism in orally administered drugs?

    <p>It reduces the bioavailability of the drug. (B)</p> Signup and view all the answers

    Which factor does NOT influence the distribution of a drug from plasma to interstitium?

    <p>Drug stability in the stomach (B)</p> Signup and view all the answers

    How does the lipophilicity of a drug affect its distribution?

    <p>It enhances the drug's ability to enter the CNS. (D)</p> Signup and view all the answers

    What could lead to a decreased rate of absorption of a drug?

    <p>Improper salt form (D)</p> Signup and view all the answers

    Which of the following drugs is indicated to have chemical instability in the gastric environment?

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

    What factor contributes to the rapid distribution of propofol into the CNS?

    <p>High blood flow to the brain (A)</p> Signup and view all the answers

    What is the primary determinant of capillary permeability for drug distribution?

    <p>Capillary structure and drug nature (B)</p> Signup and view all the answers

    Which tissue type is likely to have the lowest rate of blood flow?

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

    What is the primary factor that differentiates bioavailability between oral and intravenous drug administration?

    <p>First-pass hepatic metabolism (A)</p> Signup and view all the answers

    What is meant by the term bioavailability in pharmacology?

    <p>The rate and extent to which a drug reaches systemic circulation (C)</p> Signup and view all the answers

    Which statement correctly explains why some orally administered drugs have low bioavailability?

    <p>They are poorly absorbed across the gastrointestinal tract. (D)</p> Signup and view all the answers

    How is bioavailability typically determined for a drug?

    <p>By comparing IV and oral administration plasma levels (A)</p> Signup and view all the answers

    What role does first-pass hepatic metabolism play in the bioavailability of orally administered drugs?

    <p>It can significantly decrease the amount of active drug reaching systemic circulation. (B)</p> Signup and view all the answers

    What characteristic is essential for a drug to be efficiently absorbed in the body?

    <p>The drug should be lipophilic but also have some aqueous solubility. (D)</p> Signup and view all the answers

    Which of the following would likely lead to a decrease in the bioavailability of a drug?

    <p>Rapid first-pass metabolism by the liver (D)</p> Signup and view all the answers

    What is the significance of the area under the curve (AUC) in determining bioavailability?

    <p>It reflects the concentration of the drug over time in the bloodstream. (D)</p> Signup and view all the answers

    Which route of drug excretion is primarily responsible for eliminating anesthetic gases?

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

    What is the equation used to calculate total body clearance?

    <p>CLtotal = CLhepatic + CLrenal + CLpulmonary + CLother (A)</p> Signup and view all the answers

    Which condition can lead to an increase in drug half-life?

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

    What is a potential risk of drug excretion into breast milk?

    <p>Potential exposure of the infant to medications (A)</p> Signup and view all the answers

    Which component is not included in the total body clearance equation?

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

    What might necessitate a decrease in drug dosage?

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

    What happens when a drug undergoes decreased metabolism due to a concomitant drug?

    <p>Drug half-life increases (B)</p> Signup and view all the answers

    What is a minor route of drug excretion compared to others?

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

    What does first-order kinetics of drug elimination indicate?

    <p>A constant fraction of the drug is eliminated per unit of time. (C)</p> Signup and view all the answers

    What is the formula for calculating the volume of distribution (Vd)?

    <p>Vd = Dose / C0 (D)</p> Signup and view all the answers

    Which method is typically used to analyze drug concentration elimination over time?

    <p>Plotting the log of plasma drug concentration versus time. (A)</p> Signup and view all the answers

    Which of the following does NOT serve as a major route of drug elimination?

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

    What are phase I and phase II reactions primarily responsible for?

    <p>Making lipophilic drugs more polar for elimination. (D)</p> Signup and view all the answers

    Why are lipophilic drugs less efficiently eliminated by the kidneys?

    <p>They are reabsorbed in the distal convoluted tubules. (D)</p> Signup and view all the answers

    What does clearance (CL) measure in drug elimination?

    <p>The volume of plasma from which the drug is completely removed per unit of time. (A)</p> Signup and view all the answers

    In which scenario would a drug exhibit zero-order kinetics?

    <p>When the drug is administered in high doses, such as aspirin. (A)</p> Signup and view all the answers

    Flashcards

    Enteric Coating

    A coating protecting the drug from stomach acid, releasing it in the intestine.

    Extended-Release

    A release mechanism that allows the drug to be absorbed slowly over a longer period of time.

    Oral Drug Administration

    Drug administration via the GI tract (Mouth, Stomach, Intestines)

    Sublingual Administration

    Drug administration under the tongue, bypassing stomach acid.

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    Buccal Administration

    Drug administration between the cheek and gum, similar to sublingual.

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    Parenteral Administration

    Injection of drugs directly into the body, bypassing the GI tract.

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    Drugs Suitable for Parenteral Administration

    Drugs poorly absorbed from the GI tract or unstable in stomach acid.

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    First-Pass Metabolism

    A process where drugs are metabolized by the liver before reaching systemic circulation.

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    Bioavailability

    The rate and extent a drug enters systemic circulation after administration.

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    Determining Bioavailability

    Comparing plasma levels after different routes of administration, especially IV vs. oral.

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    First-Pass Hepatic Metabolism

    Decreases bioavailability by breaking down the drug before it reaches systemic circulation.

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    Drug Solubility

    Hydrophilic drugs have difficulty crossing cell membranes, hindering absorption.

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    Drug Solubility

    Extremely lipophilic drugs struggle to dissolve in body fluids, hindering absorption.

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    Drug Solubility

    Optimal absorption requires a balance between lipophilicity and water solubility.

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    High First-Pass Metabolism

    Drugs with high first-pass metabolism require higher doses to reach their target.

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    Drug distribution

    The process by which a drug leaves the bloodstream and enters the interstitial fluid and tissues.

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    Blood flow in drug distribution

    The rate of blood flow to different tissues varies, impacting drug distribution.

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    Capillary permeability

    The ability of a drug to pass through the walls of capillaries depends on capillary structure and the drug's properties.

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    Plasma protein binding

    The extent to which a drug binds to plasma proteins affects its distribution.

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    Lipophilicity in drug distribution

    The tendency of a drug to dissolve in fats or lipids influences its distribution.

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    Tissue volume

    The volume of a tissue affects the amount of drug that can accumulate in it.

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    Nonionized weak base diffusion

    The process where a weak base's uncharged form crosses a cell membrane's lipid layer.

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    Effect of pH on drug absorption

    The pH of the environment influences the absorption of drugs, since most drugs are either weak acids or weak bases. The uncharged form of a drug is more likely to cross cell membranes.

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    Acidic drugs and absorption

    A weak acid releases a proton (H+), forming a charged anion. The uncharged protonated form (HA) can cross membranes, while the charged anion (A-) cannot.

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    Basic drugs and absorption

    A weak base can also release a proton. However, the protonated form is usually charged, and the uncharged base (B) can cross membranes.

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    Blood flow and drug absorption

    The intestines have a greater blood flow than the stomach, leading to faster drug absorption from the intestines.

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    Surface area and drug absorption

    Due to its larger surface area and microvilli, the intestines allow for more efficient drug absorption compared to the stomach.

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    Contact time and drug absorption

    Delayed transport of a drug through the GI tract can decrease absorption. Diarrhea speeds up transport, reducing absorption.

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    P-glycoprotein and drug absorption

    P-glycoprotein is a protein that 'pumps' drugs out of cells. It is found in various tissues and can prevent drug absorption by transporting them back into the blood.

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    First-order kinetics

    The process of eliminating a constant fraction of a drug from the body per unit of time. This means that the rate of elimination is proportional to the amount of drug present.

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    Volume of distribution (Vd)

    The volume of fluid that would be required to contain the total amount of drug in the body at the same concentration as in the plasma.

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    Clearance (CL)

    The amount of drug eliminated from the body per unit of time. It reflects the efficiency of drug elimination.

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    Drug metabolism

    The process of converting a drug into a more water-soluble form to facilitate its elimination from the body.

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    Phase I metabolism

    A series of enzymatic reactions that transform a drug into a more polar metabolite, often by introducing or exposing functional groups.

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    Phase II metabolism

    A series of reactions that typically conjugate a drug or its phase I metabolite with a polar molecule, such as glucuronic acid, to increase water solubility.

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    Renal excretion

    The elimination of drugs through the kidneys, primarily by filtration and secretion.

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    Drug polarity and renal excretion

    Drugs need to be sufficiently water-soluble (polar) to be efficiently eliminated by the kidneys.

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    Total Body Clearance (Cltotal)

    The total elimination rate of a drug from the body, representing the sum of clearances from all organs involved in drug metabolism and excretion.

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    Drug Half-Life

    The time it takes for the concentration of a drug in the body to reduce by half.

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    Drug Excretion

    The process by which the body eliminates drugs through various routes, including the kidneys, liver, lungs, intestines, and breast milk.

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    Hepatic Excretion

    The liver's role in drug elimination through metabolic processes and secretion into bile.

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    Increased Drug Half-Life

    A situation where a patient's body processes and eliminates a drug more slowly than usual, potentially leading to increased drug accumulation and possible toxicity.

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    Decreased Drug Half-Life

    A situation where a patient's body metabolizes and eliminates a drug more quickly than usual, potentially requiring higher doses to maintain the desired drug level.

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    Decreased Drug Clearance

    A condition where the body eliminates a drug at a slower rate, commonly due to impaired kidney or liver function.

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    Study Notes

    Pharmacology

    • Pharmacology is the study of substances interacting with living systems, particularly by binding to regulatory molecules, activating or inhibiting normal body processes.
    • Drug-body interactions are categorized into pharmacodynamic (drug on body) and pharmacokinetic (body on drug) processes.
    • Pharmacodynamic processes determine drug classification and appropriateness for specific symptoms/diseases.
    • Pharmacokinetic processes involve drug absorption, distribution, metabolism, and elimination.

    Pharmacokinetics

    • Absorption: Drug entry into plasma (directly or indirectly) from the site of administration.
    • Distribution: Drug movement from bloodstream to interstitial and intracellular fluids. Reversible process.
    • Metabolism: Drug biotransformation primarily by the liver (or other tissues).
    • Elimination: Drug and metabolite removal from the body (urine, bile, feces).

    Routes of Drug Administration

    • Enteral: Safest and most common, convenient, and economical method (e.g., oral, sublingual, buccal).
      • Oral: Fast self-administration; complex absorption pathways; complications include low gastric pH.
      • Enteric-coated: Protects drug from stomach acid, releases in the intestines.
      • Extended-release: Controls drug release, slower absorption, prolonged action, improves patient compliance.
    • Parenteral: Direct drug introduction into the body via injection.
      • Intravenous (IV): Rapid effect and maximum control; administered as a bolus or infusion.
      • Intramuscular (IM): Rapid or sustained release; appropriate for vaccines, medications requiring slow absorption.
      • Subcutaneous (SC): Slower absorption than IV; suitable for drugs needing sustained effects. Suitable for insulin or heparin.
      • Intradermal: Localized effect; used for diagnostic testing, desensitization.
    • Other: Oral inhalation, nasal preparations, topical, intrathecal/intraventricular.
      • Oral Inhalation/Nasal Preparations : Rapid delivery to mucous membranes, quick effects. Good for respiratory issues (e.g., asthma).
      • Intrathecal/Intraventricular: Used for local, rapid CNS effects. Bypasses blood-brain barrier.
      • Topical: Applied directly to the skin or other surface for local effect.
      • Transdermal (patch): Slower, sustained release across the skin; for systemic effect.

    Absorption Mechanisms

    • Passive Diffusion: Drugs move from high to low concentration across a membrane. Important for most drugs.
    • Facilitated Diffusion: Carrier proteins facilitate drug transport, not requiring energy. Dependent on concentration gradient.
    • Active Transport: Carrier proteins move drugs against concentration gradients, requiring energy.

    Bioavailability

    • Bioavailability: The fraction of administered drug reaching systemic circulation unchanged.
    • Factors affecting bioavailability: First-pass metabolism, drug solubility, total surface area at absorption site, contact time at absorption site, drug formulation, and expression of P-glycoprotein.

    Drug Distribution

    • Blood flow to the absorption site, total surface area for absorption, contact time at the absorption surface.
    • Capillary permeability: determined by capillary structure and chemical properties of the drug.
    • Drug binding to plasma and tissue proteins (e.g., albumin).
    • Lipophilicity: determines drug's ability to cross cell membranes.

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    Description

    This quiz explores the fundamentals of pharmacology and pharmacokinetics. It covers drug-body interactions, including pharmacodynamic and pharmacokinetic processes, as well as routes of drug administration. Understand how drugs affect the body and how the body processes drugs.

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