Pharmacokinetics Quiz
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Questions and Answers

Which of the following is NOT a key component of pharmacokinetics (ADME)?

  • Absorption
  • Excretion
  • Metabolism
  • Distribution
  • Elimination (correct)
  • The recommended analgesic adult dose of paracetamol is 500mg.

    True (A)

    What is the primary method by which most pharmacological agents cross cell membranes?

    Passive diffusion

    Diclofenac sodium 50mg tablets are administered ______ times daily, while diclofenac SR 100mg SR capsules are administered once a day.

    <p>2-3</p> Signup and view all the answers

    Match the following pharmacokinetic processes with their definitions:

    <p>Absorption = The movement of a drug from the site of administration into the bloodstream Distribution = The transport of a drug throughout the body to its site of action Metabolism = The conversion of a drug into a more soluble form for easier elimination Excretion = The removal of a drug from the body</p> Signup and view all the answers

    The movement of drug molecules from the site of administration into the bloodstream is known as ______.

    <p>drug absorption</p> Signup and view all the answers

    Which of the following is NOT a key factor that determines the intensity of a medicine's response?

    <p>Drug Cost (D)</p> Signup and view all the answers

    Which of the following is NOT a factor influencing a drug's absorption?

    <p>Blood type of the patient (A)</p> Signup and view all the answers

    Pharmacokinetics and pharmacodynamics are both important for understanding how drugs work in the body.

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

    What is the primary factor determining the rate of passive diffusion across a cell membrane?

    <p>The concentration gradient of the drug across the membrane.</p> Signup and view all the answers

    What is the primary objective of drug therapy?

    <p>To provide maximum benefit with minimum harm.</p> Signup and view all the answers

    Active transport requires energy to move a substance across a membrane against its concentration gradient.

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

    Drugs are ______ molecules that can influence biological processes in the body.

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

    Match the drug movement mechanisms with their key characteristics:

    <p>Diffusion through open ion pores = Small, water-soluble drug Passive Diffusion = Lipid-soluble drug Facilitated Diffusion = Requires a specific carrier protein Active Transport = Requires energy and moves against the concentration gradient</p> Signup and view all the answers

    What are the four primary components of pharmacokinetics, often referred to as ADME?

    <p>Absorption, Distribution, Metabolism, Excretion (B)</p> Signup and view all the answers

    Which of the following is an example of a drug that utilizes facilitated diffusion for transport?

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

    What is the relationship between the pH of a solution and the ionization state of a weak acid drug?

    <p>In acidic environments, a weak acid drug is mostly in its non-ionized form, while in alkaline environments, it is mostly ionized.</p> Signup and view all the answers

    Match the following pharmacokinetic concepts to their corresponding descriptions:

    <p>Absorption = The process by which a drug enters the bloodstream from its site of administration. Distribution = The movement of a drug from the bloodstream to the tissues and organs. Metabolism = The process by which a drug is chemically transformed in the body. Excretion = The process of eliminating a drug from the body.</p> Signup and view all the answers

    Give an example of a drug that works primarily in the gastrointestinal tract.

    <p>An antibiotic for diarrhea.</p> Signup and view all the answers

    The lipophilicity of a drug molecule generally increases its absorption through the cell membrane.

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

    Give an example of a drug that works primarily in the central nervous system.

    <p>An antibiotic for meningitis.</p> Signup and view all the answers

    Which of the following tissues can accumulate certain drugs due to their properties?

    <p>Bone (A), Adipose tissue (C)</p> Signup and view all the answers

    Tight junctions between cells in the CNS and placenta make these areas more permeable to drugs.

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

    What is the primary purpose of metabolism in the human body when it comes to drugs?

    <p>To transform drugs into a form that can be more easily eliminated from the body.</p> Signup and view all the answers

    The ______ is a theoretical volume of fluid into which the total drug administered would have to be diluted to produce the same concentration in plasma as in the body.

    <p>apparent volume of distribution (Vd)</p> Signup and view all the answers

    Match the following drug metabolism outcomes with their corresponding examples:

    <p>Active to Inactive = Morphine to morphine-3-glucuronide Active to Active = BZP to its active metabolite Prodrug to Active = Enalapril to Enalaprilat</p> Signup and view all the answers

    Which of the following are the two major sites of drug administration?

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

    The onset of action of a drug is primarily determined by its absorption.

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

    What is the key difference between diclofenac dispersable and diclofenac sustained release formulations?

    <p>Diclofenac dispersable tablets are designed to dissolve quickly in the mouth, allowing for rapid absorption. Diclofenac sustained release tablets are formulated to release the drug gradually over an extended period, providing longer-lasting pain relief.</p> Signup and view all the answers

    The drug ______ is known for its high water solubility, which can pose challenges for oral absorption.

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

    Match the following drug formulations with their characteristics:

    <p>Syrup = Liquid formulation, generally absorbed quickly Capsule = Solid formulation, containing the drug in a capsule shell Sustained release tablet = Formulated to release the drug gradually over an extended time, providing longer duration of action</p> Signup and view all the answers

    Which of the following factors can affect the absorption of a drug from the gastrointestinal tract?

    <p>All of the above (D)</p> Signup and view all the answers

    A drug that is highly ionized is more readily absorbed from the gastrointestinal tract.

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

    Explain why aspirin, a weak acid, is likely to be absorbed more readily in the stomach than in the intestines.

    <p>The stomach has a more acidic environment than the intestines. Aspirin, being a weak acid, will be mostly in its non-ionized form in the acidic stomach, allowing it to readily cross lipid membranes and be absorbed. In the more alkaline environment of the intestines, aspirin will be mostly ionized, making it less likely to be absorbed.</p> Signup and view all the answers

    Which of the following factors can influence drug metabolism?

    <p>All of the above (D)</p> Signup and view all the answers

    Grapefruit juice can increase the bioavailability of certain drugs.

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

    What is the definition of first-pass metabolism?

    <p>First-pass metabolism is the metabolic transformation of a drug that occurs in the liver before it reaches systemic circulation.</p> Signup and view all the answers

    Drugs with high first-pass metabolism often have ______ bioavailability when administered orally.

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

    Which of the following routes of administration can bypass first-pass metabolism?

    <p>Both B and C (A)</p> Signup and view all the answers

    Match the following routes of drug excretion with the corresponding excretory organ:

    <p>Urine = Kidney Bile = Liver Sweat, saliva, tears = Skin, salivary glands, lacrimal glands Milk = Mammary glands Stool = Intestines</p> Signup and view all the answers

    The kidneys are the only organ responsible for drug excretion.

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

    Explain how urine pH can affect drug excretion.

    <p>The pH of urine can influence the reabsorption of drugs, particularly those that are weak acids or weak bases. When the urine pH is similar to the drug's pKa, the drug is more likely to be reabsorbed back into the bloodstream, leading to reduced excretion. Conversely, when the urine pH is different from the drug's pKa, the drug is more likely to be ionized and excreted in the urine.</p> Signup and view all the answers

    Flashcards

    Paracetamol dosage

    Recommended adult dose of paracetamol is 500mg.

    Diclofenac administration frequency

    Diclofenac sodium 50mg is taken 2-3 times daily; SR 100mg once daily.

    ADME components

    Four key components of pharmacokinetics: Absorption, Distribution, Metabolism, Excretion.

    Absorption in pharmacokinetics

    Process of drug being absorbed into the bloodstream from the administration site.

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    Distribution in pharmacokinetics

    Transport of the drug throughout the body to sites of action in tissues and cells.

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    Metabolism in pharmacokinetics

    Biotransformation of drugs into soluble forms for easier elimination.

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    Excretion in pharmacokinetics

    The elimination of drugs from the body through relevant tissues.

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    Passive diffusion

    Main method used by drugs to cross cell membranes, driven by concentration gradient.

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    Volume of Distribution (Vd)

    A pharmacokinetic measure indicating how a drug distributes throughout the body relative to blood plasma volume.

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    Drug Accumulation in Tissues

    Some tissues, like adipose and bone, can store drugs, affecting their efficacy and duration.

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    Tight Junctions

    Cellular structures that prevent passive movement of substances between cells, important in CNS and placenta.

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    Metabolism of Drugs

    The chemical transformation of drugs in the body, which can convert active drugs to inactive or other active forms.

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    Drug Elimination

    The process of removing a drug from the body, primarily through metabolism and excretion.

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    Pharmacokinetics

    The study of drug absorption, distribution, metabolism, and excretion in the body.

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    ADME

    The four key components of pharmacokinetics: Absorption, Distribution, Metabolism, Excretion.

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    Drug Absorption

    The process of how a drug enters the bloodstream after administration.

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    Distribution

    How the drug disperses throughout the body after entering the bloodstream.

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    Metabolism

    The biochemical process of converting drugs into active or inactive forms.

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    Excretion

    The process through which drugs are eliminated from the body, primarily via urine or feces.

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    Therapeutic Range

    The range of drug concentration in the plasma that produces the desired effect without toxicity.

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    Loading and Maintenance Dose

    Loading dose is a higher initial dose to rapidly achieve therapeutic levels; maintenance dose is the regular dose sustaining those levels.

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    Enteral Administration

    Drug administration via the gastrointestinal tract.

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    Parenteral Administration

    Drug administration by injection, bypassing the GI tract.

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    Absorption

    The process by which a drug enters the bloodstream.

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    Factors Influencing Absorption

    Various factors affecting how well a drug is absorbed.

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    First Pass Metabolism

    Metabolism of a drug before it reaches systemic circulation.

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    Drug Distribution

    Movement of drugs throughout the body after absorption.

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    Factors Affecting Distribution

    Elements that influence how drugs are distributed in the body.

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    Solubility

    Ability of a drug to dissolve, affecting absorption.

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    Drug Metabolism

    The process by which the body breaks down drugs, primarily in the liver.

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    Bioavailability

    The proportion of a drug that enters circulation when introduced into the body and is available for use.

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    Excretion of Drugs

    The process of eliminating drugs from the body, either unchanged or as metabolites.

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    Renal Excretion

    Removal of drugs from the body through the kidneys, primarily via urine.

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    Drug pKa

    The pH at which half of a drug is ionized, affecting its solubility and excretion.

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    Urine pH Effect

    Urine pH can influence the extent of drug reabsorption and excretion.

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    Molecular Size and Excretion

    Drugs smaller than 300 Daltons are easily excreted in urine.

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    Lipophilicity

    The affinity of a drug molecule for lipid environments.

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    Ionization

    The process by which a drug becomes charged or uncharged, affecting solubility.

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    Facilitated Diffusion

    Movement of molecules across cell membranes via a carrier, along the concentration gradient.

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    Active Transport

    Movement of molecules against a concentration gradient requiring energy.

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    Filtration/Diffusion through Ion Pores

    Process where small, water-soluble drugs pass through aqueous channels in membranes.

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    Competitive Inhibition

    Situation where different substances compete for the same transport carrier.

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    Study Notes

    Introduction to Pharmacokinetics

    • Pharmacokinetics is the study of how drugs are absorbed, distributed, metabolized, and excreted (ADME) in the body.
    • Understanding ADME is crucial for optimizing drug therapy.

    Objectives

    • Explain the application of pharmacokinetics in clinical practice.
    • Describe the relationship between biopharmaceutics, pharmacokinetics, and pharmacodynamics.
    • Describe key requirements for a drug to work at its intended target site.
    • Discuss the key four components of pharmacokinetics (ADME).
    • Explain how substances travel across plasma membranes.
    • Discuss factors affecting drug absorption, metabolism, and their impact on pharmacotherapy.
    • Explain enterohepatic circulation and its effect on drugs.
    • Discuss how drugs are distributed throughout the body.
    • Describe how plasma proteins affect drug distribution.
    • Identify major processes by which drugs are excreted.
    • Explain how plasma half-life relates to drug therapy.
    • Explain how a drug reaches and maintains therapeutic range in the plasma.
    • Differentiate between loading and maintenance doses.

    Lesson Format

    • Preliminary introduction of principles.
    • Discussion on absorption and distribution.
    • Discussion on metabolism and excretion.

    Therapeutic Objective

    • To provide maximum benefit with minimal harm.
    • Key factors determining drug response intensity:
      • Administration (dosage size and route).
      • Pharmacokinetic processes
      • Pharmacodynamics.
      • Individual variations.

    Overview

    • The body consists of organized systems (organs, tissues, and cells).
    • Various body systems produce endogenous substances (enzymes, hormones, mediators) that play crucial roles in maintaining physiological processes.
    • Drugs are exogenous substances that can influence body processes.

    Basic Relationship Between Pharmacokinetics and Pharmacodynamics

    • A diagram illustrating the relationship:
      • Biopharmaceutics affects drug release and dissolution, leading to absorption
      • Absorption results in the drug being distributed into the systemic circulation.
      • Distribution of the drug into tissues leads to the drug's pharmacodynamic effect.
      • Elimination occurs via metabolism and excretion of the drug.
      • The outcome is a desired or undesired drug effect, which in turn affects the drug’s further handling in the body.

    Key Requirements for Drug Action

    • A diagram illustrating the key requirements:
      • The therapeutic site of action (receptor binding).
      • Tissue reservoirs with high concentration
      • Drug being transported to unwanted sites of action (non-specific binding or action).
      • Clearance (drug removal).
      • Excretion (drug removal by various systems).

    ADME Definitions

    • Absorption: Drug movement from administration site to bloodstream.
    • Distribution: Drug transport throughout the body to site of action.
    • Metabolism: Biotransformation of the drug (making it more soluble & easier to excrete).
    • Excretion: Removal of the drug and its metabolites from the body.

    Key Processes Facilitating ADME

    • Movement of drug molecules across cell membranes.
    • Binding of drugs to plasma proteins.
    • Partitioning into body fats and tissues.

    Movement of Drug Molecules Across Cell Membrane Barriers: Passive Diffusion

    • Passive diffusion is the primary mechanism for drug absorption.
    • Movement is driven by a concentration gradient.
    • Lipophilicity of the drug molecule affects movement.
    • pH and ionization affect drug solubility.

    Movement of Drug Molecules Across Cell Membrane Barriers: Facilitated Diffusion

    • Facilitated diffusion requires a physiological carrier.
    • It occurs along a concentration gradient.
    • It's selective and saturable.
    • Competitive inhibition is possible.
    • Energy is not required.

    Movement of Drug Molecules Across Cell Membrane Barriers: Active Transport

    • Active transport moves drugs against a concentration gradient.
    • Energy is required.
    • Examples include active secretion at renal tubules.

    Movement of Drug Molecules Across Cell Membrane Barriers: Filtration/Diffusion through Open Ion Pores

    • Small, water-soluble drugs (ionized or polar) are readily absorbed via aqueous channels/pores.

    Summary: Movement through Cell Membranes

    • Water-soluble drugs cross via aqueous channels/pores.
    • Lipid-soluble drugs cross via lipid membranes.
    • Facilitated diffusion needs similarity between drug & physiological substrate.

    Processes that Underlie ADME + Factors: Movement Across Cell Membrane Barriers

    • Exercise on key drug properties for drug action.
    • Identifying mechanisms for drug crossing.

    Absorption & Distribution of Drugs

    • Most drugs need to be absorbed to produce effects.
    • Drug absorption is the movement of drug from site of administration to bloodstream.
    • Two major sites are enteral and parenteral.
    • Absorption is the key pharmacokinetic parameter for onset of action.

    Absorption Following Oral Administration

    • Diagram illustrating various routes of drug administrations, showing different absorption patterns, including first pass metabolism in liver.

    Factors Influencing Absorption

    • Route of administration (e.g., sublingual vs. oral).
    • Drug formulation (e.g., liquid vs. capsule).
    • Solubility of the drug.
    • Gastrointestinal conditions & food.
    • Degree of ionization.
    • pH of the environment.
    • Physicochemical factors.
    • Drug-drug interactions (e.g., chelation).
    • First-pass metabolism.

    Reflection: Partitioning, pH, and Passive Diffusion

    • Aspirin is a weak acid and absorbs differently in acidic/alkaline environments.
    • Aspirin absorption is influenced by its ionization in the gut.

    Drug Distribution

    • Drug distribution refers to the specific locations of drugs in the body.
    • Drugs are transported in the bloodstream before reaching their target site.
    • Drugs are distributed in different body compartments (plasma, interstitial fluid, intracellular fluid, fat, CNS).

    Factors Affecting Drug Distribution

    • Blood flow to the organ.
    • Physicochemical properties of the drug (lipid solubility, protein binding, size).
    • Tissue ability to accumulate drugs.
    • Physiological barriers (blood-brain barrier, placenta).

    Absorption and Effect on Distribution– Movement Across Cell Barriers

    • Some tight junctions in the body limit drug distribution (e.g., CNS, placenta).
    • Other tissues are freely permeable to drugs (e.g., liver, spleen).
    • The vascular endothelium shows variability in permeability to drugs.

    Volume of Distribution

    • The apparent volume of distribution (Vd) is a theoretical volume that considers drug distribution between the plasma and other body compartments.
    • Vd helps to calculate the loading dose.

    Drug Elimination

    • Metabolism (biotransformation).
    • Excretion.

    Drug Metabolism

    • Consequences of drug metabolism:
      • Active to inactive (e.g., certain benzodiazepines).
      • Active to active (e.g., some benzodiazepines).
      • Prodrug to active.

    Drug Metabolism Introduction

    • Purpose of metabolism in the human body.
    • Three main purposes:
      • Energy production
      • Building blocks
      • Nitrogenous waste clearance

    Drug Metabolism Sites

    • Liver (main site).
    • Gut.
    • Plasma.
    • Lungs.

    Metabolism: Hepatic Enzymes

    • Nature - Cytochrome P450 superfamily.
    • Classification - Isoenzymes with different families and substrate specificity.
    • P450 and inter-individual variations.
    • Genetic polymorphism.
    • Enzyme inducibility/inhibition.

    Metabolism: Enzyme Induction

    • Mechanisms of enzyme induction.
    • Consequences of induction on drug action.
    • Clinical implications of drug interactions.
    • Exercise on drug interactions.

    Metabolism: Enzyme Inhibition

    • Mechanisms of enzyme inhibition.
    • Effects of competitive inhibitors on substrates.
    • Clinical implications of drug interactions.
    • Exercise on drug interactions.

    Factors Influencing Drug Metabolism - Internal

    • Internal factors (physiological and pathological): age, genetic factors, disease states (e.g., cirrhosis).
    • Impact on drug metabolism.

    Factors Influencing Drug Metabolism - External

    • External factors (diet, environmental factors, the drugs themselves): Enzyme induction or inhibition, self medication and alternative medicine.
    • Impact on drug metabolism and some examples are: St John's Wort, and Grapefruit juice.

    Illustration: First-Pass Metabolism

    • Diagram demonstrating the concept of First-Pass Metabolism.

    Drug Metabolism - 1st Pass Metabolism

    • Definition of First-Pass Metabolism.
    • Consequences of high first-pass metabolism on drug bioavailability.
    • Drugs affected by First-Pass metabolism (e.g., propranolol).

    Excretion of Drugs

    • Definition: Removal of drugs and metabolites from the body.
    • Processes:
      • Urine excretion.
      • Bile excretion.
      • Sweat, saliva, tears, milk.
    • Significance of excretion

    Renal Excretion Mechanisms

    • Diagram demonstrating the mechanisms of renal excretion.
    • Filtration.
    • Reabsorption.
    • Secretion.

    Factors Affecting Renal Excretion

    • Physicochemical properties of the drug.
    • Blood flow to the kidneys.
    • Biological factors.
    • Drug interactions.
    • Disease states.
    • Plasma concentration.
    • Urine pH.
    • Drug distribution and binding.

    Physicochemical Properties

    • Molecular size ( <300 Daltons excreted easily in urine).
    • Urine pH and drug pKa.
    • Mechanism of urine pH affecting drug excretion.
    • Example about aspirin excretion.

    Disease States

    • Renal dysfunction, impaired glomerular filtration, toxicity.
    • Impact of disease states on drug excretion.

    Excretion and Drug Interactions: Active Tubular Secretion of Drugs

    • Competition for active transport can cause drug interactions (e.g., probenecid and penicillin).
    • Other examples of drug interactions affecting excretion (e.g., thiazides and uric acid excretion).

    Processes that facilitate ADME: Plasma Protein Binding

    • The role of plasma proteins in drug transport.
    • Protein-bound drugs are unavailable for crossing cell membranes.
    • Effects of protein binding on drug availability/duration of action.
    • Clinical significance for highly protein-bound drugs.

    Excretion Drug Interactions

    • Forced diuresis (diuretics increase drug elimination).
    • Alteration of urine pH (acidification/alkalinization).

    Exercise

    • Explain how duration of action for some drugs can be increased in the case of renal failure.

    Nursing Implications: ADME

    • Drug-food interactions.
    • Drug interactions.
    • Dose variations between routes (oral and parenteral).
    • Hepatic/renal failure.
    • Adjustment of urinary pH to manage overdose.

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    Description

    Test your knowledge on pharmacokinetics, focusing on the key components such as absorption, distribution, metabolism, and excretion of drugs. This quiz includes questions about drug dosages, mechanisms of drug passage through cell membranes, and factors affecting drug response. Prepare to enhance your understanding of how medications interact within the body.

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