Podcast
Questions and Answers
What is the most important mechanism for drug absorption across the placenta?
What is the most important mechanism for drug absorption across the placenta?
- Facilitated diffusion
- Endocytosis
- Active transport
- Passive diffusion (correct)
Which factor decreases free drug concentration in fetal circulation?
Which factor decreases free drug concentration in fetal circulation?
- Increased body fat
- Increased protein binding (correct)
- Lower body water content
- Higher cardiac output
The metabolism of some drugs in the fetus operates at what capacity compared to adult levels?
The metabolism of some drugs in the fetus operates at what capacity compared to adult levels?
- Completely inactive
- Always higher than adults
- Functionally at adult levels (correct)
- Always lower than adults
What occurs during the elimination phase of pharmacokinetics in fetuses?
What occurs during the elimination phase of pharmacokinetics in fetuses?
Which of the following statements regarding first-pass metabolism is correct?
Which of the following statements regarding first-pass metabolism is correct?
Which of the following could increase drug delivery to the fetal brain?
Which of the following could increase drug delivery to the fetal brain?
Ion trapping in amniotic fluid refers to which of the following?
Ion trapping in amniotic fluid refers to which of the following?
Which of the following best describes the physiological change affecting drug metabolism in fetuses experiencing hypoxia?
Which of the following best describes the physiological change affecting drug metabolism in fetuses experiencing hypoxia?
Which channels open as a delayed response causing the membrane potential to become more negative?
Which channels open as a delayed response causing the membrane potential to become more negative?
What process returns the neuron back to its resting membrane potential?
What process returns the neuron back to its resting membrane potential?
What is the term for the delay between peak plasma concentration and peak central nervous system concentration?
What is the term for the delay between peak plasma concentration and peak central nervous system concentration?
Which anesthetic achieves rapid equilibration between plasma and effect site?
Which anesthetic achieves rapid equilibration between plasma and effect site?
What describes the term 'ke0' in effect-site elimination?
What describes the term 'ke0' in effect-site elimination?
What generally affects the time to peak effect site concentration?
What generally affects the time to peak effect site concentration?
Which statement is true regarding the mechanisms of drug clearance?
Which statement is true regarding the mechanisms of drug clearance?
How is the time to reach 50% of plasma concentration defined mathematically?
How is the time to reach 50% of plasma concentration defined mathematically?
Which anesthetics are characterized by slow equilibration between plasma and effect site?
Which anesthetics are characterized by slow equilibration between plasma and effect site?
What is the relationship between a drug's half-life and dosing interval?
What is the relationship between a drug's half-life and dosing interval?
Which of the following best describes Phase II reactions in drug metabolism?
Which of the following best describes Phase II reactions in drug metabolism?
Which factor does NOT directly affect the extraction capacity of a drug?
Which factor does NOT directly affect the extraction capacity of a drug?
Which of these processes is associated with the termination of drug action?
Which of these processes is associated with the termination of drug action?
When considering the neuronal action potential, what is the first action that occurs?
When considering the neuronal action potential, what is the first action that occurs?
What factor primarily affects the spontaneous chemical reactions involved in drug metabolism?
What factor primarily affects the spontaneous chemical reactions involved in drug metabolism?
Which of the following is NOT a typical outcome of drug metabolism?
Which of the following is NOT a typical outcome of drug metabolism?
Which of the following statements about ionized drugs is true?
Which of the following statements about ionized drugs is true?
Which of the following is NOT a characteristic of unionized drugs?
Which of the following is NOT a characteristic of unionized drugs?
At pH 2.5, is aspirin primarily in a lipid-soluble form?
At pH 2.5, is aspirin primarily in a lipid-soluble form?
At pH 7.4, how does the ionization of the basic drug promethazine (pKa 9.1) compare to its ionization at pH 2?
At pH 7.4, how does the ionization of the basic drug promethazine (pKa 9.1) compare to its ionization at pH 2?
Is absorption of a weakly basic drug likely to occur faster from the stomach than from the intestine?
Is absorption of a weakly basic drug likely to occur faster from the stomach than from the intestine?
Does acidification of the urine accelerate the secretion of a weak base with a pKa of 8?
Does acidification of the urine accelerate the secretion of a weak base with a pKa of 8?
What term describes the process when a ligand binds to a receptor and enhances cellular response?
What term describes the process when a ligand binds to a receptor and enhances cellular response?
Which statement regarding the distribution of drugs to specific tissues is false?
Which statement regarding the distribution of drugs to specific tissues is false?
What is characterized as the amount of a drug divided by the desired plasma concentration?
What is characterized as the amount of a drug divided by the desired plasma concentration?
What is the role of an intracellular chemical messenger following receptor activation?
What is the role of an intracellular chemical messenger following receptor activation?
What is the immediate consequence of activating a G-protein coupled receptor?
What is the immediate consequence of activating a G-protein coupled receptor?
Which neurotransmitter-receptor complex is considered inhibitory?
Which neurotransmitter-receptor complex is considered inhibitory?
What term refers to the maximum response a drug can produce, regardless of the dose given?
What term refers to the maximum response a drug can produce, regardless of the dose given?
What can be inferred if drug X is significantly more effective than drug Y at lower dosages?
What can be inferred if drug X is significantly more effective than drug Y at lower dosages?
What describes a drug that acts as a full receptor activator?
What describes a drug that acts as a full receptor activator?
What is the therapeutic index primarily a measure of?
What is the therapeutic index primarily a measure of?
Flashcards
Drug Elimination
Drug Elimination
The process by which a drug is eliminated from the body.
Drug Metabolism
Drug Metabolism
The process by which a drug is chemically altered in the body.
Drug Distribution
Drug Distribution
The movement of a drug from the bloodstream to other tissues.
Drug Half-Life
Drug Half-Life
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Drug Clearance
Drug Clearance
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Steady-State Concentration
Steady-State Concentration
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Extraction Ratio
Extraction Ratio
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Peak Effect
Peak Effect
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What is pharmacokinetics?
What is pharmacokinetics?
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Absorption
Absorption
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Distribution
Distribution
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Metabolism
Metabolism
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Elimination
Elimination
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What is the typical sequence of drug transfer and absorption for a PO drug?
What is the typical sequence of drug transfer and absorption for a PO drug?
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Do intravenous drugs undergo first-pass hepatic metabolism?
Do intravenous drugs undergo first-pass hepatic metabolism?
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How do inhaled drugs (INH) reach the bloodstream?
How do inhaled drugs (INH) reach the bloodstream?
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pKa
pKa
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Lipophilic
Lipophilic
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Hydrophilic
Hydrophilic
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Non-ionized drugs
Non-ionized drugs
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Ionized drugs
Ionized drugs
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First-order kinetics
First-order kinetics
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Loading dose
Loading dose
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Signal Amplification
Signal Amplification
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Signal Integration
Signal Integration
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Signal Relay
Signal Relay
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Antagonist
Antagonist
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Max Efficacy
Max Efficacy
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Drug Potency
Drug Potency
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Therapeutic Index
Therapeutic Index
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Partial Agonist
Partial Agonist
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Repolarization
Repolarization
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Sodium-potassium pump
Sodium-potassium pump
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Effect Site
Effect Site
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T 1/2 ke0
T 1/2 ke0
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Hysteresis
Hysteresis
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Effect-Site Elimination
Effect-Site Elimination
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Effect-Site Equilibration
Effect-Site Equilibration
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ke0
ke0
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Study Notes
Pharmacokinetics & Dynamics Review
- Pharmacokinetics is the study of how the body processes drugs.
- This includes absorption, distribution, metabolism, and elimination.
Spotlight on Fetal Pharmacokinetics
- Absorption:
- The placenta is the primary absorption route.
- Passive diffusion is the primary mechanism.
- Anesthetics, opioids, benzodiazepines quickly cross the placenta.
- Neuromuscular blockers cross slowly.
- Distribution:
- Increased delivery to the fetal brain, related to cardiac output.
- Decreased protein binding increases free drug concentration.
- Lower body fat and higher body water can affect distribution.
- Ion trapping in amniotic fluid serves as a reservoir for water-soluble drugs.
- Metabolism:
- Fetal enzyme function may be at adult levels, or less active with delayed metabolism (e.g., opiates, NSAIDs, local anesthetics).
- Drug clearance is decreased in hypoxia.
- Elimination:
- Fetal renal excretion into amniotic fluid.
- Drug transfer to the mother via umbilical vessels and placenta.
- Drug recirculation via amniotic fluid re-ingestion is possible.
Questions & Answers
-
Question #1: Drugs taken orally most likely follow the sequence Gut > liver > vein > heart > lung > heart > artery. (C)
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Question #2: Intravenous drugs do not undergo first pass hepatic metabolism. (B)
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Question #3: Match drug routes (PO, IV, inhalation) to their corresponding absorption/distribution curves. Relevant information on slide.
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Question #4: Nonionized drugs are more lipophilic. (C)
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Question #5: Hydrophilic is NOT a characteristic of unionized drugs. (B)
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Question #6: BH+ readily crosses the placenta. (A)
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Question #7: Aspirin (acetylsalicylic acid, pKa 3.5) is primarily in a lipid-soluble form at pH 2.5. (A)
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Question #8: Promethazine (pKa 9.1) is more ionized at pH 7.4 than at pH 2. (A)
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Question #9: Absorption of a weakly basic drug is faster from the stomach than the intestine. (A)
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Question #10: Acidification of the urine accelerates the secretion of a weak base (pKa 8). (A)
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Question #11: Uncharged molecules readily cross cell membranes. (A)
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Question #12: Distribution of drugs to tissues depends on the unbound drug concentration gradient between plasma and tissues. (C)
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Question #13: Drugs must be excreted to terminate drug action. (A)
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Question #14: Ligand binding to a receptor to increase cellular response is known as amplification. (A)
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Question #15: Receptor activation causes another intracellular chemical messenger to cause a cellular or tissue response. This is known as Relay. (C)
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Question #16: Conformational change happens when receptor is activated immediately. (D)
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Question #17: Drug X is 100 times more potent than Drug Y. (B)
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Question #18: Partial competitive agonist. (C)
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Question #19: Max efficacy. (B)
Additional Concepts
- Volume of distribution: The theoretical volume of fluid required to contain the drug if it were uniformly distributed at the same concentration as in plasma.
- Water vs. Lipid solubility: Lipid-soluble drugs distribute more extensively than water-soluble drugs.
- Matching: Review the provided matching key for specific definitions.
Other Topics Mentioned
- Pharmacodynamics: Study of how drugs affect the body (i.e., dose, activity, mechanisms).
- Neuron Action Potential: (depolarization by Na, repolarization by K) & Na-K pumps
- Hotspot Matching of Nervous System Components: Review diagram.
- Biophase & Anesthetics: Relevant information related to effects and action.
Further Study Points
- Review the provided diagrams and figures/tables related to these concepts.
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