Pharmacokinetics in Patient Care Quiz

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Questions and Answers

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?

  • Absorption
  • Distribution
  • Metabolism (correct)
  • Elimination

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?

<p>To avoid first-pass metabolism effectively (D)</p> Signup and view all the answers

Which mechanism is primarily responsible for drug absorption from the administration site to the bloodstream?

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

Why is the intranasal route often preferred for certain medications in pediatric patients?

<p>It minimizes systemic side effects and absorption. (B)</p> Signup and view all the answers

Which of the following options correctly describes absorption in pharmacokinetics?

<p>Absorption is the process of drug transfer from the site of administration to the bloodstream. (B)</p> Signup and view all the answers

What characterizes the first-pass effect on drugs administered orally?

<p>It reduces the concentration of active drug before it reaches systemic circulation. (C)</p> Signup and view all the answers

What is the main factor affecting the time it takes for a drug to equilibrate in adipose tissue compared to the central nervous system?

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

To reach a steady state in drug administration, what must the infusion rate equal?

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

How many half-lives does it typically take to reach a steady state?

<p>4 to 5 half-lives (B)</p> Signup and view all the answers

What is the difference between first-order and zero-order kinetics in drug elimination?

<p>First-order eliminates a constant fraction; zero-order eliminates a constant amount. (A)</p> Signup and view all the answers

What does context-sensitive half-time specifically refer to in the context of anesthesia?

<p>The time for plasma concentration to decrease by half after steady state IV infusion (A)</p> Signup and view all the answers

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?

<p>4 half-lives (B)</p> Signup and view all the answers

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?

<p>20 hours (B)</p> Signup and view all the answers

What is the primary purpose of administering a loading dose of a drug?

<p>To quickly achieve therapeutic levels (D)</p> Signup and view all the answers

Which statement about drug recovery following anesthesia is correct?

<p>Recovery may not align with context-sensitive half-time. (B)</p> Signup and view all the answers

What is the effect of maternal alkalosis and fetal acidosis on the ionization of a weak base drug?

<p>It favors the ionized form in the fetal environment. (B)</p> Signup and view all the answers

Which factor does NOT directly influence the absorption of a drug?

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

How is drug bioavailability defined?

<p>The fraction of drug reaching systemic circulation unchanged. (A)</p> Signup and view all the answers

What happens when two drugs highly bound to albumin are administered simultaneously?

<p>They will compete for binding, potentially increasing activity of one drug. (D)</p> Signup and view all the answers

Which drug transport mechanism is typically faster?

<p>Active transport (D)</p> Signup and view all the answers

In what scenario will a drug predominantly remain in the ionized form?

<p>In an alkaline environment for a weak acid. (B)</p> Signup and view all the answers

Which protein is most commonly involved in drug binding within circulating plasma?

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

Which characteristic of a drug will likely require active transport for membrane crossing?

<p>High molecular weight and lipophilic nature (D)</p> Signup and view all the answers

How does malnutrition affect drug distribution?

<p>It leads to decreased availability of binding proteins. (A)</p> Signup and view all the answers

What is true about the first-pass metabolism effect?

<p>It refers to the metabolism of a drug before it reaches systemic circulation. (C)</p> Signup and view all the answers

What is a consequence of a drug being highly protein-bound?

<p>It limits the free drug available for pharmacological activity. (D)</p> Signup and view all the answers

Which factor is likely to diminish the absorption of orally administered drugs?

<p>Presence of food in the stomach (D)</p> Signup and view all the answers

Which variable does NOT affect the distribution of drugs in the body?

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

What can result from competition for protein binding sites?

<p>Increased pharmacological effects of one drug. (A)</p> Signup and view all the answers

What is primarily affected by the factor of drug ionization in drug diffusion across membranes?

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

What defines the volume of distribution for a drug that exceeds total body water?

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

Which patient characteristic can lead to an increased volume of distribution?

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

How is the volume of distribution calculated?

<p>Amount of drug given divided by plasma concentration (D)</p> Signup and view all the answers

What is the primary purpose of phase 1 metabolism during drug metabolism?

<p>Increase water solubility and polarity (A)</p> Signup and view all the answers

What role does albumin play when it comes to drug action in the bloodstream?

<p>Binds drugs and influences distribution (A)</p> Signup and view all the answers

Why is first pass metabolism significant for drugs absorbed through the gastrointestinal tract?

<p>Reduces the bioavailability of drugs (A)</p> Signup and view all the answers

What effect does lipophilicity have on drug dosing in relation to volume of distribution?

<p>Requires a higher loading dose (B)</p> Signup and view all the answers

Which of the following best describes the term 'target controlled infusion'?

<p>Dosing algorithms based on plasma and effect site concentrations (C)</p> Signup and view all the answers

Which factor is NOT necessary for a drug to move freely throughout the body?

<p>Protein binding (D)</p> Signup and view all the answers

What is the peak effect timing for Fentanyl post IV administration?

<p>Equilibrium at peak effect in 3.5 minutes (A)</p> Signup and view all the answers

What is the role of CYP 450 enzymes during phase 1 drug metabolism?

<p>Oxidizing drugs to increase water solubility (A)</p> Signup and view all the answers

What is the primary reason drugs need to be in a non-ionized form for effective absorption?

<p>Non-ionized drugs can easily pass through lipid membranes. (C)</p> Signup and view all the answers

What characteristic of Fentanyl contributes to its rapid peak concentration in the central nervous system?

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

Which statement accurately reflects the behavior of weak acids in solution?

<p>Weak acids can exist in both ionized and non-ionized forms depending on pH. (A)</p> Signup and view all the answers

What does a lower pKa value indicate about an acid?

<p>It is stronger and holds protons more tightly. (D)</p> Signup and view all the answers

In which pH environment is an acid more likely to remain in its non-ionized form?

<p>At pH levels well below its pKa. (A)</p> Signup and view all the answers

What is the relationship between pH and the ionization of weak bases?

<p>Weak bases become positively charged in acidic conditions. (A)</p> Signup and view all the answers

What happens to an acid's ionization in a solution where the pH is equal to its pKa?

<p>50% of the acid exists in ionized form and 50% in non-ionized form. (C)</p> Signup and view all the answers

What is the primary role of pKa in pharmacology?

<p>To assess the strength of an acid's interaction with protons. (B)</p> Signup and view all the answers

What is a characteristic of strong acids compared to weak acids?

<p>Strong acids completely dissociate in solution. (A)</p> Signup and view all the answers

Why is the concept of ionization important in drug absorption?

<p>Ionized drugs cannot cross lipid membranes effectively. (D)</p> Signup and view all the answers

How does a proton donor behave as an acid in the body?

<p>It donates a proton and becomes its conjugate base. (A)</p> Signup and view all the answers

Which of the following describes the interaction of weak acids in a solution with a pH above their pKa?

<p>Weak acids tend to release protons, becoming more ionized. (D)</p> Signup and view all the answers

What is the significance of the Henderson-Hasselbalch equation in pharmacology?

<p>It helps predict the ionization state of drugs at different pH levels. (D)</p> Signup and view all the answers

What happens to a weak base as it accepts a proton in a low pH environment?

<p>It gains a positive charge. (C)</p> Signup and view all the answers

What is the primary function of CYP 450 enzymes in drug metabolism?

<p>Facilitate both oxidation and reduction reactions (C)</p> Signup and view all the answers

What effect do enzyme inducers have on drug metabolism?

<p>Increase the activity of enzymes involved in drug metabolism (B)</p> Signup and view all the answers

Which of the following drugs is known to follow zero order kinetics?

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

What is considered when evaluating a drug's hepatic extraction ratio?

<p>Volume of blood flow into the liver (C)</p> Signup and view all the answers

In which situation would a patient struggle to metabolize drugs eliminated by Hoffman elimination?

<p>When acidotic and hypothermic (D)</p> Signup and view all the answers

What distinguishes drugs with low hepatic extraction ratios?

<p>Their metabolism is capacity dependent on liver enzymes (D)</p> Signup and view all the answers

What is meant by 'first pass metabolism'?

<p>Initial metabolism of orally administered drugs in the liver (B)</p> Signup and view all the answers

What happens to the plasma concentration of drugs in the presence of enzyme inhibitors?

<p>Increases due to decreased metabolism (A)</p> Signup and view all the answers

Which of the following is NOT characteristic of drugs that follow first order kinetics?

<p>Metabolism is unaffected by enzyme concentration (A)</p> Signup and view all the answers

How does organ blood flow relate to drug clearance?

<p>Increased blood flow enhances drug clearance efficiency (B)</p> Signup and view all the answers

Which of the following is the definition of clearance?

<p>The volume of plasma cleared of drug per unit of time (B)</p> Signup and view all the answers

Which enzyme is commonly associated with plasma drug metabolism through hydrolysis?

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

What is the impact of enzyme inducers on the dosage requirement of certain medications?

<p>Higher doses may be required due to increased metabolic activity (B)</p> Signup and view all the answers

What happens to an acid when the pH is above its pKa?

<p>It favors deprotonation and produces more ionized forms. (D)</p> Signup and view all the answers

Which statement is true regarding the ionization of drugs?

<p>Ionized drugs are hydrophilic and typically cannot diffuse across lipid membranes. (A)</p> Signup and view all the answers

How does the pH of the environment affect drug absorption?

<p>The pH affects the ionization state of the drug, influencing its solubility and absorption. (A)</p> Signup and view all the answers

What is a potential consequence of ion trapping in drug administration?

<p>Drugs becoming trapped in tissues, risking toxicity. (A)</p> Signup and view all the answers

Why is understanding pKa important in pharmaceutical studies?

<p>It influences how much of the drug becomes ionized based on the environment. (D)</p> Signup and view all the answers

What is primarily lost during high flow, dependent extraction before reaching systemic circulation?

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

What effect does an acidic environment have on a basic drug?

<p>It can lead to the drug becoming trapped in its ionized form. (B)</p> Signup and view all the answers

What characteristic do ionized drugs possess?

<p>They are hydrophilic and water-soluble. (A)</p> Signup and view all the answers

What role do renal extraction ratios play in drug elimination?

<p>They indicate the volume of plasma cleared from the drug (C)</p> Signup and view all the answers

Which type of drug is more likely to be excreted unchanged by the kidneys?

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

What happens when an acid is in a solution with a pH lower than its pKa?

<p>The acid retains its protons and exists in a non-ionized form. (A)</p> Signup and view all the answers

Which of the following is true regarding ionized versus unionized drug forms?

<p>Unionized drugs are usually pharmacologically active and lipid-soluble. (A)</p> Signup and view all the answers

How does urine pH affect acidic drugs in an acidic environment?

<p>They become ionized and trapped for excretion (B)</p> Signup and view all the answers

How can ion trapping pose a challenge in obstetric care?

<p>Acidic fetal circulation can trap basic drugs, leading to potential toxicity. (C)</p> Signup and view all the answers

What is the expected outcome when administering ammonium chloride to a patient?

<p>Excretion of acidic drugs (B)</p> Signup and view all the answers

What does a larger volume of distribution indicate about a drug's half-life?

<p>It correlates with a longer half-life (A)</p> Signup and view all the answers

Which factor is primarily considered when studying pharmacokinetics of drugs?

<p>The pKa and pH interaction and their impact on drug behavior. (D)</p> Signup and view all the answers

What is the key effect of pKa in relation to drug formulations?

<p>It influences the solubility of drugs within various physiological environments. (D)</p> Signup and view all the answers

What effect does decreased renal blood flow have on drug half-life?

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

In drug absorption, what is meant by 'ion trapping'?

<p>Accumulation of an ionized drug in one area due to unfavorable pH. (B)</p> Signup and view all the answers

What is true regarding the relationship between drug clearance and half-life?

<p>Clearance is inversely related to half-life (D)</p> Signup and view all the answers

In a one compartment model, the concentration of a drug is assumed to be:

<p>Uniformly distributed across all tissues (D)</p> Signup and view all the answers

What can cause drug displacement from albumin that increases half-life?

<p>Increased free drug availability (A)</p> Signup and view all the answers

What happens during redistribution of a drug in a two compartment model after an IV bolus is given?

<p>Plasma concentration initially drops as drug equilibrates (A)</p> Signup and view all the answers

What is a consequence of alkaline urine on drug absorption?

<p>Promotes absorption of acidic drugs (A)</p> Signup and view all the answers

How long does it roughly take to eliminate 97% of a drug from the body?

<p>5 half-lives (C)</p> Signup and view all the answers

What effect does a decrease in cardiac output have on drug metabolism?

<p>It prolongs drug half-life (D)</p> Signup and view all the answers

Flashcards

Pharmacokinetics

The study of how the body affects a drug, including absorption, distribution, metabolism, and elimination.

Pharmacodynamics

The effect of a drug on the body, including both desired clinical effects and potential side effects.

Absorption

The process by which a drug enters the bloodstream.

Bioavailability

The percentage of a drug that reaches the bloodstream after administration.

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Diffusion

Movement of molecules from an area of high concentration to low concentration.

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Active Transport

This method of drug transport requires energy to move molecules across cell membranes.

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First Pass Effect

The reduction in drug efficacy due to metabolism by the liver before it reaches systemic circulation.

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Depot Preparations

Dosage forms that allow for slow and sustained release of a drug.

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Drug Ionization

The tendency of a drug to exist in its ionized form, which affects its absorption, distribution, and elimination.

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pKa

The pH at which 50% of a drug exists in its ionized form and 50% in its unionized form.

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Ionization Rule

An acidic environment (lower pH) favors the ionized form of basic drugs, while a basic environment (higher pH) favors the ionized form of acidic drugs.

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Unionized Drug Absorption

The process of drug absorption is enhanced by the presence of a higher concentration of the unionized form of the drug.

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Ion Trapping

The phenomenon where a drug's ionized form accumulates in a compartment with a different pH than its site of administration.

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Ion Trapping in Fetal Circulation

Ion trapping can occur when a basic drug is administered in an acidic environment, such as fetal circulation, leading to a higher concentration of the drug in the acidic compartment.

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Ion Trapping and Toxicity

Ion trapping can contribute to drug toxicity by increasing the concentration of the drug in a specific tissue or organ.

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Ionized Drugs: Hydrophilic

The ionized form of a drug is hydrophilic, water-soluble, and less likely to cross membranes.

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Unionized Drugs: Lipophilic

The unionized form of a drug is lipophilic, fat-soluble, and more readily crosses membranes.

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Drug Distribution

The process of a drug moving from its site of administration to its target site.

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Drug Elimination

The process by which the body eliminates a drug, including metabolism and excretion.

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Drug Efficacy

The ability of a drug to reach its site of action and produce a therapeutic effect.

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Drug Concentration at Target Site

The concentration of a drug at its target site is influenced by its pKa and the pH of the surrounding environment.

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Importance of Drug Ionization and pKa

Understanding drug ionization and pKa helps to optimize drug formulations for better absorption, distribution, and efficacy.

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What is ionization?

Ionization is the process of adding or removing a charge from a drug molecule. It happens when a drug gains or loses a hydrogen ion (H+).

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What are acids and bases in terms of ionization?

Acids are proton donors, meaning they have an H+ attached and can give it away. Bases are proton acceptors, they take in the H+.

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How does pH influence ionization?

The pH of a solution determines whether a drug will be ionized or not. For example, an acidic drug will be less ionized in an acidic solution.

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What is pKa and how is it related to acidity?

The pKa of a drug tells us how strongly it holds onto its hydrogen ion (H+). A lower pKa means the drug is more acidic, and will be ionized at a lower pH.

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What happens when the pH and pKa are equal?

When the pH of the solution is equal to the pKa of the drug, the drug will be 50% ionized and 50% non-ionized.

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Why is the non-ionized form of a drug more easily absorbed?

The non-ionized form of a drug is more likely to pass through cell membranes because it is lipid-soluble and can easily move through the fatty layer of the cell.

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What is active transport?

Active transport requires energy to move drugs against a concentration gradient. It is crucial when a drug needs to be transported from an area of low concentration to an area of high concentration.

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Which form of a drug is usually pharmacologically active?

The non-ionized form of a drug is generally the pharmacologically active form, meaning it can interact with its target in the body to exert its effects.

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What equation is used to calculate ionized and non-ionized forms?

The Henderson-Hasselbalch equation is used to calculate the ratio of ionized and non-ionized drug molecules in a solution at a given pH.

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Why are weak acids and bases important?

Most drugs are weak acids or bases, meaning they partially dissociate in solution. This means they exist in both ionized and non-ionized forms.

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What happens to a weak acid in a higher pH environment?

A weak acid will give up a proton (H+) more easily in an environment with a higher pH, because there is more base available to accept it.

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How does the Cookie Monster analogy help understand pKa?

Cookie Monster analogy: Think of Cookie Monster as an acid. When he gets a cookie (H+), he's non-ionized. When he loses a cookie (H+), he's ionized.

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What is the significance of pKa?

A drug's pKa is a constant that tells us how much of it will be ionized at a given pH. The lower the drug's pKa, the more acidic it is.

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How does pKa affect drug behavior in the body?

The pKa of a drug helps us understand how it will be absorbed, distributed, and eliminated by the body.

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Why is understanding ionization and pKa important in pharmacology?

Drugs can have different properties depending on their ionization state. Understanding pKa helps us predict how drugs will behave in different parts of the body.

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Drug Absorption

The process by which a drug moves from its administration site into the bloodstream.

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First-Pass Metabolism

The process of a drug being broken down by the liver before it reaches systemic circulation.

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Passive Diffusion

The process of drugs moving across cell membranes from areas of high concentration to low concentration, without energy expenditure.

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Protein Binding

The binding of a drug to proteins in the bloodstream, primarily albumin.

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Protein Binding Competition

The competition between drugs for binding to proteins in the bloodstream, potentially affecting drug efficacy.

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Therapeutic Dose

The dosage range of a drug that produces the desired therapeutic effect without causing toxicity.

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Toxic Dose

The dosage range of a drug that causes harmful side effects.

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Body Water Compartments

The total amount of water in the body, divided into intracellular and extracellular compartments, which further subdivide into interstitial and plasma.

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Tissue Distribution

The tendency of a drug to accumulate in specific tissues or organs.

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Enzyme Inducers

Drugs that increase the activity of enzymes involved in drug metabolism, leading to faster breakdown of the drug and potentially requiring a higher dose.

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Enzyme Inhibitors

Drugs or conditions that decrease the activity of enzymes involved in drug metabolism, leading to slower breakdown and potentially higher blood levels of the drug.

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Renal Extraction Ratio

The fraction of drug removed from the plasma during a single pass through an organ.

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Zero Order Kinetics

A type of drug metabolism where a fixed amount of drug is eliminated per unit of time, regardless of the drug concentration.

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Renal Elimination

Elimination of drugs through the kidneys, influenced by factors like drug polarity, pH, and whether the drug is hydrophilic or lipophilic.

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First Order Kinetics

A type of drug metabolism where a constant fraction of drug is eliminated per unit of time, resulting in a gradual decrease in concentration.

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Glomerular Filtration

The process by which substances in the blood are filtered into the urine filtrate.

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Drug Excretion

The process of eliminating a drug from the body, usually via the kidneys, liver, intestines, or lungs.

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Drug Clearance

The volume of plasma cleared of drug per unit of time, measuring the efficiency of drug removal.

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Urine pH and Drug Excretion

The pH of the urine impacts drug excretion. Acidic urine promotes excretion of basic drugs, while basic urine promotes excretion of acidic drugs.

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Extraction Ratio

The fraction of drug removed from the blood as it passes through a specific organ, usually the liver.

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High Extraction Ratio Drugs

Drugs with a high hepatic extraction ratio are mainly cleared by the liver, their clearance is dependent on blood flow.

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Half-Life

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

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Volume of Distribution

The volume of distribution is related to how much drug is distributed to the body tissues. A larger volume of distribution means that the drug is going to be distributed to more areas of the body.

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Low Extraction Ratio Drugs

Drugs with a low hepatic extraction ratio are cleared by the liver and other organs, their clearance is dependent on liver enzyme activity.

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Drug Clearance

The ability of the body to clear a drug from the blood.

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Plasma Concentration

The concentration of a drug in the plasma (blood) changes over time due to distribution, metabolism, and excretion.

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Plasma Metabolism

A type of drug metabolism occurring in the bloodstream, primarily by hydrolysis.

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Hoffman Elimination

A spontaneous chemical reaction that breaks down certain drugs, dependent on pH and temperature.

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One Compartment Model

A simplified model of drug distribution assuming the drug is evenly distributed throughout the body.

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Multi Compartment Model

A more complex model of drug distribution where the drug is distributed to multiple compartments in the body.

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CYP 450 Enzymes

Membrane-bound enzymes found in the liver and other organs, involved in Phase 1 metabolism.

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Hoffman Elimination

A method of drug elimination that involves a spontaneous chemical reaction, dependent on pH and temperature.

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Redistribution

The redistribution of a drug from the plasma to other compartments in the body over time.

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Two Compartment Model

A model of drug distribution that considers two compartments, usually the plasma and the tissues.

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What is the definition of volume of distribution?

A theoretical volume that reflects the total body space that a drug would occupy if it were uniformly distributed throughout the body.

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Explain the difference between the central and peripheral compartments.

The central compartment receives a higher blood flow compared to the peripheral compartment. Examples of central compartments include the lungs and endocrine glands. The peripheral compartment encompasses skin, fat, and muscles.

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Explain the relationship between drug accumulation and the peripheral compartment.

Drugs tend to accumulate in the peripheral compartment, making it challenging for them to distribute back to the central compartment due to reduced blood flow.

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How is the volume of distribution calculated?

The amount of drug given divided by the desired plasma concentration.

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What is the relationship between volume of distribution and loading dose?

A larger volume of distribution indicates that a higher loading dose is required to achieve the desired plasma concentration.

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Explain how fentanyl reaches its peak effect.

Plasma concentration in the central compartment, particularly in the central nervous system, reaches its peak effect faster due to the drug's affinity for the central nervous system.

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Why do lipophilic drugs have a larger volume of distribution?

Lipophilic drugs, like propofol, have a large volume of distribution because they move freely and distribute extensively.

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What factors influence the volume of distribution?

The volume of distribution is influenced by a number of factors, including the drug's properties, patient characteristics, and disease states.

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What factors affect drug movement?

A drug's movement across membranes is affected by several factors, including ionization, lipid solubility, molecular weight, and protein binding.

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What role does albumin play in drug binding?

Albumin is the primary protein involved in drug binding. The degree of protein binding is influenced by albumin levels in the plasma.

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Describe the first pass effect and its impact on bioavailability.

The first pass effect describes the metabolism of orally administered drugs in the liver before they reach systemic circulation. This can significantly reduce the drug's bioavailability.

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Explain the different phases of drug metabolism.

Phase 1 metabolism modifies the drug molecule, primarily to increase its water solubility. Phase 2 metabolism further enhances water solubility through conjugation with substrates.

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What factors determine drug diffusion across cell membranes?

Factors that affect drug diffusion across membranes include: ionization, lipid solubility, molecular weight, protein binding, concentration gradient, and membrane thickness.

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Explain the relationship between volume of distribution and drug elimination.

The volume of distribution influences elimination. A larger volume leads to a more difficult excretion process.

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Explain the role of ionization in drug diffusion.

Ionization is a crucial factor in drug diffusion. An ionized form is hydrophilic and less likely to cross membranes, while a non-ionized form is lipophilic and more readily crosses membranes.

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Three-Compartment Model

A model used to describe drug distribution where the drug moves between different compartments (e.g., blood, tissues) at different rates.

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Steady State

The point where the rate of drug entering the body equals the rate of drug leaving the body, resulting in a stable plasma concentration.

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Loading Dose

The amount of drug needed to quickly achieve a therapeutic concentration, often given initially.

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Context-Sensitive Half-Time

The time it takes for the plasma concentration of a drug to decrease by 50% following an IV infusion at steady state.

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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.

  • Metabolic phases: Phase 1 (modification) and Phase 2 (conjugation).

  • CYP450 enzymes are crucial in drug metabolism.

  • Enzyme inducers and inhibitors affect drug metabolism rates; this requires consideration when prescribing.

  • Drug Elimination: Primary routes include kidneys, liver, intestines, and lungs.

  • Clearance: The volume of plasma cleared of drug per unit time, related to organ blood flow.

  • 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%.

  • Volume of distribution (Vd) and Clearance (Cl) relate to half-life; greater Vd, longer half-life.

  • 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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