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Questions and Answers
Which of the following is NOT a key component of pharmacokinetics (ADME)?
Which of the following is NOT a key component of pharmacokinetics (ADME)?
The recommended analgesic adult dose of paracetamol is 500mg.
The recommended analgesic adult dose of paracetamol is 500mg.
True (A)
What is the primary method by which most pharmacological agents cross cell membranes?
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.
Diclofenac sodium 50mg tablets are administered ______ times daily, while diclofenac SR 100mg SR capsules are administered once a day.
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Match the following pharmacokinetic processes with their definitions:
Match the following pharmacokinetic processes with their definitions:
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The movement of drug molecules from the site of administration into the bloodstream is known as ______.
The movement of drug molecules from the site of administration into the bloodstream is known as ______.
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Which of the following is NOT a key factor that determines the intensity of a medicine's response?
Which of the following is NOT a key factor that determines the intensity of a medicine's response?
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Which of the following is NOT a factor influencing a drug's absorption?
Which of the following is NOT a factor influencing a drug's absorption?
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Pharmacokinetics and pharmacodynamics are both important for understanding how drugs work in the body.
Pharmacokinetics and pharmacodynamics are both important for understanding how drugs work in the body.
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What is the primary factor determining the rate of passive diffusion across a cell membrane?
What is the primary factor determining the rate of passive diffusion across a cell membrane?
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What is the primary objective of drug therapy?
What is the primary objective of drug therapy?
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Active transport requires energy to move a substance across a membrane against its concentration gradient.
Active transport requires energy to move a substance across a membrane against its concentration gradient.
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Drugs are ______ molecules that can influence biological processes in the body.
Drugs are ______ molecules that can influence biological processes in the body.
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Match the drug movement mechanisms with their key characteristics:
Match the drug movement mechanisms with their key characteristics:
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What are the four primary components of pharmacokinetics, often referred to as ADME?
What are the four primary components of pharmacokinetics, often referred to as ADME?
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Which of the following is an example of a drug that utilizes facilitated diffusion for transport?
Which of the following is an example of a drug that utilizes facilitated diffusion for transport?
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What is the relationship between the pH of a solution and the ionization state of a weak acid drug?
What is the relationship between the pH of a solution and the ionization state of a weak acid drug?
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Match the following pharmacokinetic concepts to their corresponding descriptions:
Match the following pharmacokinetic concepts to their corresponding descriptions:
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Give an example of a drug that works primarily in the gastrointestinal tract.
Give an example of a drug that works primarily in the gastrointestinal tract.
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The lipophilicity of a drug molecule generally increases its absorption through the cell membrane.
The lipophilicity of a drug molecule generally increases its absorption through the cell membrane.
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Give an example of a drug that works primarily in the central nervous system.
Give an example of a drug that works primarily in the central nervous system.
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Which of the following tissues can accumulate certain drugs due to their properties?
Which of the following tissues can accumulate certain drugs due to their properties?
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Tight junctions between cells in the CNS and placenta make these areas more permeable to drugs.
Tight junctions between cells in the CNS and placenta make these areas more permeable to drugs.
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What is the primary purpose of metabolism in the human body when it comes to drugs?
What is the primary purpose of metabolism in the human body when it comes to drugs?
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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.
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.
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Match the following drug metabolism outcomes with their corresponding examples:
Match the following drug metabolism outcomes with their corresponding examples:
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Which of the following are the two major sites of drug administration?
Which of the following are the two major sites of drug administration?
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The onset of action of a drug is primarily determined by its absorption.
The onset of action of a drug is primarily determined by its absorption.
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What is the key difference between diclofenac dispersable and diclofenac sustained release formulations?
What is the key difference between diclofenac dispersable and diclofenac sustained release formulations?
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The drug ______ is known for its high water solubility, which can pose challenges for oral absorption.
The drug ______ is known for its high water solubility, which can pose challenges for oral absorption.
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Match the following drug formulations with their characteristics:
Match the following drug formulations with their characteristics:
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Which of the following factors can affect the absorption of a drug from the gastrointestinal tract?
Which of the following factors can affect the absorption of a drug from the gastrointestinal tract?
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A drug that is highly ionized is more readily absorbed from the gastrointestinal tract.
A drug that is highly ionized is more readily absorbed from the gastrointestinal tract.
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Explain why aspirin, a weak acid, is likely to be absorbed more readily in the stomach than in the intestines.
Explain why aspirin, a weak acid, is likely to be absorbed more readily in the stomach than in the intestines.
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Which of the following factors can influence drug metabolism?
Which of the following factors can influence drug metabolism?
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Grapefruit juice can increase the bioavailability of certain drugs.
Grapefruit juice can increase the bioavailability of certain drugs.
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What is the definition of first-pass metabolism?
What is the definition of first-pass metabolism?
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Drugs with high first-pass metabolism often have ______ bioavailability when administered orally.
Drugs with high first-pass metabolism often have ______ bioavailability when administered orally.
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Which of the following routes of administration can bypass first-pass metabolism?
Which of the following routes of administration can bypass first-pass metabolism?
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Match the following routes of drug excretion with the corresponding excretory organ:
Match the following routes of drug excretion with the corresponding excretory organ:
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The kidneys are the only organ responsible for drug excretion.
The kidneys are the only organ responsible for drug excretion.
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Explain how urine pH can affect drug excretion.
Explain how urine pH can affect drug excretion.
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Flashcards
Paracetamol dosage
Paracetamol dosage
Recommended adult dose of paracetamol is 500mg.
Diclofenac administration frequency
Diclofenac administration frequency
Diclofenac sodium 50mg is taken 2-3 times daily; SR 100mg once daily.
ADME components
ADME components
Four key components of pharmacokinetics: Absorption, Distribution, Metabolism, Excretion.
Absorption in pharmacokinetics
Absorption in pharmacokinetics
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Distribution in pharmacokinetics
Distribution in pharmacokinetics
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Metabolism in pharmacokinetics
Metabolism in pharmacokinetics
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Excretion in pharmacokinetics
Excretion in pharmacokinetics
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Passive diffusion
Passive diffusion
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Volume of Distribution (Vd)
Volume of Distribution (Vd)
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Drug Accumulation in Tissues
Drug Accumulation in Tissues
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Tight Junctions
Tight Junctions
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Metabolism of Drugs
Metabolism of Drugs
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Drug Elimination
Drug Elimination
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Pharmacokinetics
Pharmacokinetics
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ADME
ADME
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Drug Absorption
Drug Absorption
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Distribution
Distribution
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Metabolism
Metabolism
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Excretion
Excretion
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Therapeutic Range
Therapeutic Range
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Loading and Maintenance Dose
Loading and Maintenance Dose
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Enteral Administration
Enteral Administration
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Parenteral Administration
Parenteral Administration
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Absorption
Absorption
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Factors Influencing Absorption
Factors Influencing Absorption
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First Pass Metabolism
First Pass Metabolism
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Drug Distribution
Drug Distribution
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Factors Affecting Distribution
Factors Affecting Distribution
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Solubility
Solubility
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Drug Metabolism
Drug Metabolism
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Bioavailability
Bioavailability
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Excretion of Drugs
Excretion of Drugs
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Renal Excretion
Renal Excretion
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Drug pKa
Drug pKa
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Urine pH Effect
Urine pH Effect
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Molecular Size and Excretion
Molecular Size and Excretion
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Lipophilicity
Lipophilicity
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Ionization
Ionization
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Facilitated Diffusion
Facilitated Diffusion
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Active Transport
Active Transport
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Filtration/Diffusion through Ion Pores
Filtration/Diffusion through Ion Pores
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Competitive Inhibition
Competitive Inhibition
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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.