Podcast
Questions and Answers
What is the primary goal of pharmacokinetics in patient care?
What is the primary goal of pharmacokinetics in patient care?
- To enhance the potency of drugs administered intravenously
- To ensure complete absorption of oral drugs
- To identify optimal drug dosages for all patients
- To minimize significant changes in baseline physiological status (correct)
Which phase of pharmacokinetics involves the alteration of the drug by the body?
Which phase of pharmacokinetics involves the alteration of the drug by the body?
- Absorption
- Distribution
- Metabolism (correct)
- Elimination
Which drug administration route bypasses the liver's first-pass effect directly into the bloodstream?
Which drug administration route bypasses the liver's first-pass effect directly into the bloodstream?
- Intravenous
- Intramuscular
- Oral
- Sublingual (correct)
What is the primary reason for using the intravenous route of drug administration?
What is the primary reason for using the intravenous route of drug administration?
Which mechanism is primarily responsible for drug absorption from the administration site to the bloodstream?
Which mechanism is primarily responsible for drug absorption from the administration site to the bloodstream?
Why is the intranasal route often preferred for certain medications in pediatric patients?
Why is the intranasal route often preferred for certain medications in pediatric patients?
Which of the following options correctly describes absorption in pharmacokinetics?
Which of the following options correctly describes absorption in pharmacokinetics?
What characterizes the first-pass effect on drugs administered orally?
What characterizes the first-pass effect on drugs administered orally?
What is the main factor affecting the time it takes for a drug to equilibrate in adipose tissue compared to the central nervous system?
What is the main factor affecting the time it takes for a drug to equilibrate in adipose tissue compared to the central nervous system?
To reach a steady state in drug administration, what must the infusion rate equal?
To reach a steady state in drug administration, what must the infusion rate equal?
How many half-lives does it typically take to reach a steady state?
How many half-lives does it typically take to reach a steady state?
What is the difference between first-order and zero-order kinetics in drug elimination?
What is the difference between first-order and zero-order kinetics in drug elimination?
What does context-sensitive half-time specifically refer to in the context of anesthesia?
What does context-sensitive half-time specifically refer to in the context of anesthesia?
In a 1 compartment model, if a patient's plasma drug level is reduced to 6.25% of the original dose, how many half-lives have elapsed?
In a 1 compartment model, if a patient's plasma drug level is reduced to 6.25% of the original dose, how many half-lives have elapsed?
If a drug is administered with a half-life of 20 hours, how long will it take for the plasma concentration to decrease to 50 mg from 200 mg?
If a drug is administered with a half-life of 20 hours, how long will it take for the plasma concentration to decrease to 50 mg from 200 mg?
What is the primary purpose of administering a loading dose of a drug?
What is the primary purpose of administering a loading dose of a drug?
Which statement about drug recovery following anesthesia is correct?
Which statement about drug recovery following anesthesia is correct?
What is the effect of maternal alkalosis and fetal acidosis on the ionization of a weak base drug?
What is the effect of maternal alkalosis and fetal acidosis on the ionization of a weak base drug?
Which factor does NOT directly influence the absorption of a drug?
Which factor does NOT directly influence the absorption of a drug?
How is drug bioavailability defined?
How is drug bioavailability defined?
What happens when two drugs highly bound to albumin are administered simultaneously?
What happens when two drugs highly bound to albumin are administered simultaneously?
Which drug transport mechanism is typically faster?
Which drug transport mechanism is typically faster?
In what scenario will a drug predominantly remain in the ionized form?
In what scenario will a drug predominantly remain in the ionized form?
Which protein is most commonly involved in drug binding within circulating plasma?
Which protein is most commonly involved in drug binding within circulating plasma?
Which characteristic of a drug will likely require active transport for membrane crossing?
Which characteristic of a drug will likely require active transport for membrane crossing?
How does malnutrition affect drug distribution?
How does malnutrition affect drug distribution?
What is true about the first-pass metabolism effect?
What is true about the first-pass metabolism effect?
What is a consequence of a drug being highly protein-bound?
What is a consequence of a drug being highly protein-bound?
Which factor is likely to diminish the absorption of orally administered drugs?
Which factor is likely to diminish the absorption of orally administered drugs?
Which variable does NOT affect the distribution of drugs in the body?
Which variable does NOT affect the distribution of drugs in the body?
What can result from competition for protein binding sites?
What can result from competition for protein binding sites?
What is primarily affected by the factor of drug ionization in drug diffusion across membranes?
What is primarily affected by the factor of drug ionization in drug diffusion across membranes?
What defines the volume of distribution for a drug that exceeds total body water?
What defines the volume of distribution for a drug that exceeds total body water?
Which patient characteristic can lead to an increased volume of distribution?
Which patient characteristic can lead to an increased volume of distribution?
How is the volume of distribution calculated?
How is the volume of distribution calculated?
What is the primary purpose of phase 1 metabolism during drug metabolism?
What is the primary purpose of phase 1 metabolism during drug metabolism?
What role does albumin play when it comes to drug action in the bloodstream?
What role does albumin play when it comes to drug action in the bloodstream?
Why is first pass metabolism significant for drugs absorbed through the gastrointestinal tract?
Why is first pass metabolism significant for drugs absorbed through the gastrointestinal tract?
What effect does lipophilicity have on drug dosing in relation to volume of distribution?
What effect does lipophilicity have on drug dosing in relation to volume of distribution?
Which of the following best describes the term 'target controlled infusion'?
Which of the following best describes the term 'target controlled infusion'?
Which factor is NOT necessary for a drug to move freely throughout the body?
Which factor is NOT necessary for a drug to move freely throughout the body?
What is the peak effect timing for Fentanyl post IV administration?
What is the peak effect timing for Fentanyl post IV administration?
What is the role of CYP 450 enzymes during phase 1 drug metabolism?
What is the role of CYP 450 enzymes during phase 1 drug metabolism?
What is the primary reason drugs need to be in a non-ionized form for effective absorption?
What is the primary reason drugs need to be in a non-ionized form for effective absorption?
What characteristic of Fentanyl contributes to its rapid peak concentration in the central nervous system?
What characteristic of Fentanyl contributes to its rapid peak concentration in the central nervous system?
Which statement accurately reflects the behavior of weak acids in solution?
Which statement accurately reflects the behavior of weak acids in solution?
What does a lower pKa value indicate about an acid?
What does a lower pKa value indicate about an acid?
In which pH environment is an acid more likely to remain in its non-ionized form?
In which pH environment is an acid more likely to remain in its non-ionized form?
What is the relationship between pH and the ionization of weak bases?
What is the relationship between pH and the ionization of weak bases?
What happens to an acid's ionization in a solution where the pH is equal to its pKa?
What happens to an acid's ionization in a solution where the pH is equal to its pKa?
What is the primary role of pKa in pharmacology?
What is the primary role of pKa in pharmacology?
What is a characteristic of strong acids compared to weak acids?
What is a characteristic of strong acids compared to weak acids?
Why is the concept of ionization important in drug absorption?
Why is the concept of ionization important in drug absorption?
How does a proton donor behave as an acid in the body?
How does a proton donor behave as an acid in the body?
Which of the following describes the interaction of weak acids in a solution with a pH above their pKa?
Which of the following describes the interaction of weak acids in a solution with a pH above their pKa?
What is the significance of the Henderson-Hasselbalch equation in pharmacology?
What is the significance of the Henderson-Hasselbalch equation in pharmacology?
What happens to a weak base as it accepts a proton in a low pH environment?
What happens to a weak base as it accepts a proton in a low pH environment?
What is the primary function of CYP 450 enzymes in drug metabolism?
What is the primary function of CYP 450 enzymes in drug metabolism?
What effect do enzyme inducers have on drug metabolism?
What effect do enzyme inducers have on drug metabolism?
Which of the following drugs is known to follow zero order kinetics?
Which of the following drugs is known to follow zero order kinetics?
What is considered when evaluating a drug's hepatic extraction ratio?
What is considered when evaluating a drug's hepatic extraction ratio?
In which situation would a patient struggle to metabolize drugs eliminated by Hoffman elimination?
In which situation would a patient struggle to metabolize drugs eliminated by Hoffman elimination?
What distinguishes drugs with low hepatic extraction ratios?
What distinguishes drugs with low hepatic extraction ratios?
What is meant by 'first pass metabolism'?
What is meant by 'first pass metabolism'?
What happens to the plasma concentration of drugs in the presence of enzyme inhibitors?
What happens to the plasma concentration of drugs in the presence of enzyme inhibitors?
Which of the following is NOT characteristic of drugs that follow first order kinetics?
Which of the following is NOT characteristic of drugs that follow first order kinetics?
How does organ blood flow relate to drug clearance?
How does organ blood flow relate to drug clearance?
Which of the following is the definition of clearance?
Which of the following is the definition of clearance?
Which enzyme is commonly associated with plasma drug metabolism through hydrolysis?
Which enzyme is commonly associated with plasma drug metabolism through hydrolysis?
What is the impact of enzyme inducers on the dosage requirement of certain medications?
What is the impact of enzyme inducers on the dosage requirement of certain medications?
What happens to an acid when the pH is above its pKa?
What happens to an acid when the pH is above its pKa?
Which statement is true regarding the ionization of drugs?
Which statement is true regarding the ionization of drugs?
How does the pH of the environment affect drug absorption?
How does the pH of the environment affect drug absorption?
What is a potential consequence of ion trapping in drug administration?
What is a potential consequence of ion trapping in drug administration?
Why is understanding pKa important in pharmaceutical studies?
Why is understanding pKa important in pharmaceutical studies?
What is primarily lost during high flow, dependent extraction before reaching systemic circulation?
What is primarily lost during high flow, dependent extraction before reaching systemic circulation?
What effect does an acidic environment have on a basic drug?
What effect does an acidic environment have on a basic drug?
What characteristic do ionized drugs possess?
What characteristic do ionized drugs possess?
What role do renal extraction ratios play in drug elimination?
What role do renal extraction ratios play in drug elimination?
Which type of drug is more likely to be excreted unchanged by the kidneys?
Which type of drug is more likely to be excreted unchanged by the kidneys?
What happens when an acid is in a solution with a pH lower than its pKa?
What happens when an acid is in a solution with a pH lower than its pKa?
Which of the following is true regarding ionized versus unionized drug forms?
Which of the following is true regarding ionized versus unionized drug forms?
How does urine pH affect acidic drugs in an acidic environment?
How does urine pH affect acidic drugs in an acidic environment?
How can ion trapping pose a challenge in obstetric care?
How can ion trapping pose a challenge in obstetric care?
What is the expected outcome when administering ammonium chloride to a patient?
What is the expected outcome when administering ammonium chloride to a patient?
What does a larger volume of distribution indicate about a drug's half-life?
What does a larger volume of distribution indicate about a drug's half-life?
Which factor is primarily considered when studying pharmacokinetics of drugs?
Which factor is primarily considered when studying pharmacokinetics of drugs?
What is the key effect of pKa in relation to drug formulations?
What is the key effect of pKa in relation to drug formulations?
What effect does decreased renal blood flow have on drug half-life?
What effect does decreased renal blood flow have on drug half-life?
In drug absorption, what is meant by 'ion trapping'?
In drug absorption, what is meant by 'ion trapping'?
What is true regarding the relationship between drug clearance and half-life?
What is true regarding the relationship between drug clearance and half-life?
In a one compartment model, the concentration of a drug is assumed to be:
In a one compartment model, the concentration of a drug is assumed to be:
What can cause drug displacement from albumin that increases half-life?
What can cause drug displacement from albumin that increases half-life?
What happens during redistribution of a drug in a two compartment model after an IV bolus is given?
What happens during redistribution of a drug in a two compartment model after an IV bolus is given?
What is a consequence of alkaline urine on drug absorption?
What is a consequence of alkaline urine on drug absorption?
How long does it roughly take to eliminate 97% of a drug from the body?
How long does it roughly take to eliminate 97% of a drug from the body?
What effect does a decrease in cardiac output have on drug metabolism?
What effect does a decrease in cardiac output have on drug metabolism?
Flashcards
Pharmacokinetics
Pharmacokinetics
The study of how the body affects a drug, including absorption, distribution, metabolism, and elimination.
Pharmacodynamics
Pharmacodynamics
The effect of a drug on the body, including both desired clinical effects and potential side effects.
Absorption
Absorption
The process by which a drug enters the bloodstream.
Bioavailability
Bioavailability
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Diffusion
Diffusion
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Active Transport
Active Transport
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First Pass Effect
First Pass Effect
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Depot Preparations
Depot Preparations
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Drug Ionization
Drug Ionization
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pKa
pKa
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Ionization Rule
Ionization Rule
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Unionized Drug Absorption
Unionized Drug Absorption
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Ion Trapping
Ion Trapping
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Ion Trapping in Fetal Circulation
Ion Trapping in Fetal Circulation
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Ion Trapping and Toxicity
Ion Trapping and Toxicity
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Ionized Drugs: Hydrophilic
Ionized Drugs: Hydrophilic
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Unionized Drugs: Lipophilic
Unionized Drugs: Lipophilic
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Drug Distribution
Drug Distribution
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Drug Elimination
Drug Elimination
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Drug Efficacy
Drug Efficacy
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Drug Concentration at Target Site
Drug Concentration at Target Site
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Importance of Drug Ionization and pKa
Importance of Drug Ionization and pKa
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What is ionization?
What is ionization?
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What are acids and bases in terms of ionization?
What are acids and bases in terms of ionization?
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How does pH influence ionization?
How does pH influence ionization?
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What is pKa and how is it related to acidity?
What is pKa and how is it related to acidity?
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What happens when the pH and pKa are equal?
What happens when the pH and pKa are equal?
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Why is the non-ionized form of a drug more easily absorbed?
Why is the non-ionized form of a drug more easily absorbed?
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What is active transport?
What is active transport?
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Which form of a drug is usually pharmacologically active?
Which form of a drug is usually pharmacologically active?
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What equation is used to calculate ionized and non-ionized forms?
What equation is used to calculate ionized and non-ionized forms?
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Why are weak acids and bases important?
Why are weak acids and bases important?
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What happens to a weak acid in a higher pH environment?
What happens to a weak acid in a higher pH environment?
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How does the Cookie Monster analogy help understand pKa?
How does the Cookie Monster analogy help understand pKa?
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What is the significance of pKa?
What is the significance of pKa?
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How does pKa affect drug behavior in the body?
How does pKa affect drug behavior in the body?
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Why is understanding ionization and pKa important in pharmacology?
Why is understanding ionization and pKa important in pharmacology?
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Drug Absorption
Drug Absorption
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First-Pass Metabolism
First-Pass Metabolism
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Passive Diffusion
Passive Diffusion
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Protein Binding
Protein Binding
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Protein Binding Competition
Protein Binding Competition
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Therapeutic Dose
Therapeutic Dose
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Toxic Dose
Toxic Dose
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Body Water Compartments
Body Water Compartments
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Tissue Distribution
Tissue Distribution
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Enzyme Inducers
Enzyme Inducers
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Enzyme Inhibitors
Enzyme Inhibitors
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Renal Extraction Ratio
Renal Extraction Ratio
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Zero Order Kinetics
Zero Order Kinetics
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Renal Elimination
Renal Elimination
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First Order Kinetics
First Order Kinetics
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Glomerular Filtration
Glomerular Filtration
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Drug Excretion
Drug Excretion
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Drug Clearance
Drug Clearance
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Urine pH and Drug Excretion
Urine pH and Drug Excretion
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Extraction Ratio
Extraction Ratio
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High Extraction Ratio Drugs
High Extraction Ratio Drugs
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Half-Life
Half-Life
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Volume of Distribution
Volume of Distribution
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Low Extraction Ratio Drugs
Low Extraction Ratio Drugs
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Drug Clearance
Drug Clearance
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Plasma Concentration
Plasma Concentration
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Plasma Metabolism
Plasma Metabolism
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Hoffman Elimination
Hoffman Elimination
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One Compartment Model
One Compartment Model
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Multi Compartment Model
Multi Compartment Model
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CYP 450 Enzymes
CYP 450 Enzymes
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Hoffman Elimination
Hoffman Elimination
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Redistribution
Redistribution
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Two Compartment Model
Two Compartment Model
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What is the definition of volume of distribution?
What is the definition of volume of distribution?
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Explain the difference between the central and peripheral compartments.
Explain the difference between the central and peripheral compartments.
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Explain the relationship between drug accumulation and the peripheral compartment.
Explain the relationship between drug accumulation and the peripheral compartment.
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How is the volume of distribution calculated?
How is the volume of distribution calculated?
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What is the relationship between volume of distribution and loading dose?
What is the relationship between volume of distribution and loading dose?
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Explain how fentanyl reaches its peak effect.
Explain how fentanyl reaches its peak effect.
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Why do lipophilic drugs have a larger volume of distribution?
Why do lipophilic drugs have a larger volume of distribution?
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What factors influence the volume of distribution?
What factors influence the volume of distribution?
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What factors affect drug movement?
What factors affect drug movement?
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What role does albumin play in drug binding?
What role does albumin play in drug binding?
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Describe the first pass effect and its impact on bioavailability.
Describe the first pass effect and its impact on bioavailability.
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Explain the different phases of drug metabolism.
Explain the different phases of drug metabolism.
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What factors determine drug diffusion across cell membranes?
What factors determine drug diffusion across cell membranes?
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Explain the relationship between volume of distribution and drug elimination.
Explain the relationship between volume of distribution and drug elimination.
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Explain the role of ionization in drug diffusion.
Explain the role of ionization in drug diffusion.
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Three-Compartment Model
Three-Compartment Model
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Steady State
Steady State
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Loading Dose
Loading Dose
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Context-Sensitive Half-Time
Context-Sensitive Half-Time
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Study Notes
Medication Safety and Drug Regulation
- Nursing knowledge is crucial for medication safety, especially in anesthesia.
- Drug errors occur even after reviews, demanding careful practice.
- Maintaining safety is paramount to avoid future errors.
Pharmacokinetics
- Pharmacokinetics describes the body's actions on a drug.
- The goal is to maintain a stable physiological state during procedures.
- Key phases are absorption, distribution, metabolism, and elimination.
- Pharmacodynamics describes the drug's effects on the body.
Routes of Drug Administration
- Oral administration undergoes first-pass liver metabolism, reducing efficacy.
- Sublingual and nasal routes avoid the intestine and liver, promoting rapid absorption.
- Intramuscular delivery allows for sustained release, suitable for patients without IV access.
- Intravenous administration avoids first-pass metabolism, crucial for direct effects.
- Intranasal administration is useful for local or systemic effects, common in pediatrics.
- Inhaled drugs minimize systemic effects and are suited for patients with respiratory issues.
Absorption Mechanisms
- Absorption is drug movement from site to bloodstream.
- Bioavailability for IV drugs is complete, while oral bioavailability can be partial.
- Molecules move via diffusion from high to low concentration.
- Active transport requires energy to move drugs against concentration gradients.
- Ionization, influenced by pH, significantly affects drug absorption.
Acid-Base Chemistry in Pharmacology
- Weak acids and bases partially dissociate in solution. Drugs shift between ionized and non-ionized states depending on pH.
- Non-ionized drugs are more lipid-soluble, enabling easier passage across membranes.
- pKa is the dissociation constant, representing the strength of a compound's interaction with a proton.
- When pKa equals pH, half the drug is ionized.
- Drug behavior in different pH environments (acidic or alkaline) explains how a drug can be more or less bound to proteins , depending on the tissue conditions.
Ion Trapping
- Ion trapping occurs when drug ionization prevents its movement across a membrane.
- In an acidic environment, a basic drug will become more ionized. This trapping can increase drug concentrations to toxic levels.
Drug Properties and Drug Ionization
- Ionized drugs (hydrophilic) are water-soluble but less active.
- Non-ionized drugs are lipid-soluble and active and usually easily diffuse across lipid membranes.
- Drug ionization changes in different environments (e.g., maternal vs. fetal).
Factors Affecting Drug Absorption & Distribution
- Factors affecting absorption: route, blood flow, heat, and surface area.
- Factors affecting distribution: blood flow, capillary permeability, drug structure, and protein binding.
- Drugs move throughout the body to an effect site. Drugs that are protein bound move slower or not at all.
- Small drugs readily diffuse, while larger ones usually require active transport.
Compartmentalization in Pharmacokinetics
- The body is comprised of several compartments (intracellular, extracellular, etc.).
- Central compartments receive more blood flow (e.g., lungs), while peripheral compartments receive less.
- Drug accumulation in peripheral compartments can be difficult to remove due to lower blood flow.
Volume of Distribution
- Volume of distribution is a theoretical concept representing the drug distribution in the body.
- Loading dose and volume of distribution correlate; larger volumes need larger doses to reach desired plasma concentrations.
- Lipophilic drugs have volumes exceeding total body water and necessitate higher doses.
Case Study: Fentanyl
- Fentanyl is highly lipophilic, rapidly distributing into the central nervous system.
- Target-controlled infusion systems allow for precise maintenance of drug concentrations.
Drug Metabolism and Elimination
-
First-pass metabolism in the liver reduces the bioavailability of orally administered drugs.
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Metabolic phases: Phase 1 (modification) and Phase 2 (conjugation).
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CYP450 enzymes are crucial in drug metabolism.
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Enzyme inducers and inhibitors affect drug metabolism rates; this requires consideration when prescribing.
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Drug Elimination: Primary routes include kidneys, liver, intestines, and lungs.
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Clearance: The volume of plasma cleared of drug per unit time, related to organ blood flow.
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Extraction Ratio: Indicates how efficiently a drug is cleared by an organ. High extraction ratios typically indicate flow-limited clearance (highly dependent on blood flow).
Renal Elimination
- Renal elimination factors include drug polarity, urine pH, and glomerular filtration.
- Urine pH greatly influences the ionization and thus excretion of basic versus acidic drugs.
Half-Life and Clearance
-
Half-life (t1/2) is the time needed for plasma concentration to decrease by 50%.
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Volume of distribution (Vd) and Clearance (Cl) relate to half-life; greater Vd, longer half-life.
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Drug kinetics: Drug elimination is often described by zero- or first-order kinetics.
Pharmacokinetics and Clinical Implications
- Several factors affect the speed at which a drug reaches a specific site of action or steady state.
- Dosing consideration is influenced by patient conditions like liver disease, age, and kidney function.
- Volume of distribution calculations aid in calculating loading doses.
- Understanding drug kinetics (movement, effects, and elimination) is key to safe and effective treatment.
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