Podcast
Questions and Answers
What primarily causes the repolarization of a neuron after depolarization?
What primarily causes the repolarization of a neuron after depolarization?
- Calcium influx
- Increased sodium influx
- Potassium efflux (correct)
- Chloride efflux
What is the result of potassium channels being slower to respond compared to sodium channels?
What is the result of potassium channels being slower to respond compared to sodium channels?
- Prolonged depolarization
- Immediate sodium influx
- Hyperpolarization (correct)
- Early repolarization
How does the sodium-potassium pump contribute to membrane potential?
How does the sodium-potassium pump contribute to membrane potential?
- It prevents any ion movement across the membrane.
- It exchanges sodium for potassium to maintain homeostasis. (correct)
- It allows sodium influx while preventing potassium efflux.
- It exclusively pumps potassium into the cell.
What happens to the sodium channel after it becomes inactivated during the action potential?
What happens to the sodium channel after it becomes inactivated during the action potential?
What ion is typically more abundant outside the cell at resting membrane potential?
What ion is typically more abundant outside the cell at resting membrane potential?
What characteristic of potassium channels contributes to the overshoot of repolarization leading to hyperpolarization?
What characteristic of potassium channels contributes to the overshoot of repolarization leading to hyperpolarization?
What does a hyperpolarized state indicate about the electrical charge of the neuron?
What does a hyperpolarized state indicate about the electrical charge of the neuron?
Which statement correctly describes the difference between sodium and potassium channels during action potential?
Which statement correctly describes the difference between sodium and potassium channels during action potential?
At a pH of 7.2, what form of an acid-base equilibrium is more predominant?
At a pH of 7.2, what form of an acid-base equilibrium is more predominant?
What happens to the concentration of A minus as the pH approaches 7.4 compared to 7.2?
What happens to the concentration of A minus as the pH approaches 7.4 compared to 7.2?
What characteristic of the plasma at a pH of 7.4 can be implied regarding H plus ions?
What characteristic of the plasma at a pH of 7.4 can be implied regarding H plus ions?
In the discussion of acid-base equilibrium, what is the role of the blood-brain barrier mentioned?
In the discussion of acid-base equilibrium, what is the role of the blood-brain barrier mentioned?
What implication can be drawn from the statement that pH 7.4 is slightly basic compared to pH 7.2?
What implication can be drawn from the statement that pH 7.4 is slightly basic compared to pH 7.2?
What is a primary reason for preferring shorter-acting alpha blockers over phenoxybenzamine?
What is a primary reason for preferring shorter-acting alpha blockers over phenoxybenzamine?
Which type of bond is generally considered the strongest in receptor interactions?
Which type of bond is generally considered the strongest in receptor interactions?
Why is esketamine preferred over the racemic mixture of ketamine?
Why is esketamine preferred over the racemic mixture of ketamine?
Which factor describes the term 'chirality' in molecules?
Which factor describes the term 'chirality' in molecules?
What is the significance of a racemic mixture in pharmacology?
What is the significance of a racemic mixture in pharmacology?
What distinguishes phenoxybenzamine as an alpha blocker?
What distinguishes phenoxybenzamine as an alpha blocker?
What does the term 'ES' refer to in reference to ketamine?
What does the term 'ES' refer to in reference to ketamine?
Which drug is often associated with significant cardiotoxicity when overdosed?
Which drug is often associated with significant cardiotoxicity when overdosed?
Which characteristic defines non-competitive drugs in relation to receptor binding?
Which characteristic defines non-competitive drugs in relation to receptor binding?
In which scenario would prolonged drug binding generally be undesirable?
In which scenario would prolonged drug binding generally be undesirable?
What type of interaction significantly affects drug formulation and manufacturing?
What type of interaction significantly affects drug formulation and manufacturing?
What describes the 'S-ketamine' and 'R-ketamine' forms of ketamine?
What describes the 'S-ketamine' and 'R-ketamine' forms of ketamine?
Which of the following compounds is known to have chirality?
Which of the following compounds is known to have chirality?
Which statement about drug-receptor interactions is accurate?
Which statement about drug-receptor interactions is accurate?
What type of receptor is described as crossing a membrane seven times?
What type of receptor is described as crossing a membrane seven times?
Which type of molecular interaction helps maintain the structure of globular proteins primarily?
Which type of molecular interaction helps maintain the structure of globular proteins primarily?
What describes an aceptor in pharmacology?
What describes an aceptor in pharmacology?
Which is true about nonpolar tails in a biochemical context?
Which is true about nonpolar tails in a biochemical context?
Which drug is noted for its covalent bonding characteristics in the context of receptor interactions?
Which drug is noted for its covalent bonding characteristics in the context of receptor interactions?
In drug pharmacology, which type of molecular bond is the least common for receptor interaction?
In drug pharmacology, which type of molecular bond is the least common for receptor interaction?
Which factor contributes to a drug's long duration of action regarding receptor binding?
Which factor contributes to a drug's long duration of action regarding receptor binding?
Which of the following interactions is considered the weakest?
Which of the following interactions is considered the weakest?
When discussing drug molecules, what is an essential requirement for pharmacological activity?
When discussing drug molecules, what is an essential requirement for pharmacological activity?
In the context of pharmacology, which force is primarily responsible for the non-specific interactions between molecules?
In the context of pharmacology, which force is primarily responsible for the non-specific interactions between molecules?
Which statement is correct regarding the influences of drug size on membrane permeability?
Which statement is correct regarding the influences of drug size on membrane permeability?
What physiological condition is associated with catecholamine depletion leading to fatigue in heart failure patients?
What physiological condition is associated with catecholamine depletion leading to fatigue in heart failure patients?
What kind of interaction can typically disrupt hydrogen bonds during receptor binding?
What kind of interaction can typically disrupt hydrogen bonds during receptor binding?
Which molecular property is crucial for a drug to bind effectively to its receptor?
Which molecular property is crucial for a drug to bind effectively to its receptor?
In the context of aging, what role do catecholamines play when referring to chronic illness or acute disease?
In the context of aging, what role do catecholamines play when referring to chronic illness or acute disease?
What is the goal of post-titanic facilitation in monitoring neuromuscular blockade?
What is the goal of post-titanic facilitation in monitoring neuromuscular blockade?
What can cause decreased excitability of neurons aside from fatigue and neurotransmitter depletion?
What can cause decreased excitability of neurons aside from fatigue and neurotransmitter depletion?
Which factor is NOT typically involved in determining a receptor's sensitivity?
Which factor is NOT typically involved in determining a receptor's sensitivity?
What component of the phospholipid bilayer is primarily responsible for the membrane's selective permeability?
What component of the phospholipid bilayer is primarily responsible for the membrane's selective permeability?
What determines the specificity of a receptor's response?
What determines the specificity of a receptor's response?
In the context of receptor pharmacology, which statement is true regarding selectivity?
In the context of receptor pharmacology, which statement is true regarding selectivity?
What effect does ligand binding typically have on a receptor?
What effect does ligand binding typically have on a receptor?
Which of the following ions generally causes depolarizing effects when entering the cell?
Which of the following ions generally causes depolarizing effects when entering the cell?
What happens to receptors when there is a significant increase in neurotransmitter concentration due to post-titanic facilitation?
What happens to receptors when there is a significant increase in neurotransmitter concentration due to post-titanic facilitation?
Which neurotransmitter is recognized as the primary excitatory neurotransmitter in the central nervous system?
Which neurotransmitter is recognized as the primary excitatory neurotransmitter in the central nervous system?
Which statement accurately describes the structure of the phospholipid bilayer?
Which statement accurately describes the structure of the phospholipid bilayer?
What is the primary effect of hypocalcemia on sodium channels during action potentials?
What is the primary effect of hypocalcemia on sodium channels during action potentials?
What is the general result of activating G protein-coupled receptors?
What is the general result of activating G protein-coupled receptors?
How does hypercalcemia affect cell membrane permeability to sodium?
How does hypercalcemia affect cell membrane permeability to sodium?
What physiological effect may an alkalosis condition have on neuronal excitability?
What physiological effect may an alkalosis condition have on neuronal excitability?
What is the consequence of hypokalemia on the resting membrane potential?
What is the consequence of hypokalemia on the resting membrane potential?
What role do additional receptors outside the synapse play after neurotransmitter flooding?
What role do additional receptors outside the synapse play after neurotransmitter flooding?
Which of the following receptors is predominantly inhibitory?
Which of the following receptors is predominantly inhibitory?
Which mechanism allows neurotransmitters to be released into the synaptic cleft?
Which mechanism allows neurotransmitters to be released into the synaptic cleft?
Which of the following scenarios may impair the ability of neurons to respond effectively?
Which of the following scenarios may impair the ability of neurons to respond effectively?
What physiological response can occur as a result of receptor activation?
What physiological response can occur as a result of receptor activation?
Which type of ion channels respond to changes in the membrane potential?
Which type of ion channels respond to changes in the membrane potential?
Which condition may contribute to long-term neurotransmitter depletion in chronic illnesses?
Which condition may contribute to long-term neurotransmitter depletion in chronic illnesses?
What role do reuptake pumps serve at the presynaptic membrane?
What role do reuptake pumps serve at the presynaptic membrane?
What occurs during synaptic modulation?
What occurs during synaptic modulation?
What role does acetylcholine play in the nervous system?
What role does acetylcholine play in the nervous system?
What is a common mechanism by which ligands promote intracellular signaling?
What is a common mechanism by which ligands promote intracellular signaling?
What is the purpose of the slight delay in neuron communication across the synapse?
What is the purpose of the slight delay in neuron communication across the synapse?
Which channel type is affected predominantly by local anesthetics?
Which channel type is affected predominantly by local anesthetics?
What impact does downregulation of receptors have on a neuron?
What impact does downregulation of receptors have on a neuron?
Which of the following best describes the role of the postsynaptic density?
Which of the following best describes the role of the postsynaptic density?
Which is NOT a mechanism through which activated receptors can mediate effects in cells?
Which is NOT a mechanism through which activated receptors can mediate effects in cells?
What is primarily responsible for generating an action potential in the postsynaptic cell?
What is primarily responsible for generating an action potential in the postsynaptic cell?
Which of the following effects is most closely associated with excitatory neurotransmitters?
Which of the following effects is most closely associated with excitatory neurotransmitters?
How do ligand-gated ion channels typically operate upon ligand binding?
How do ligand-gated ion channels typically operate upon ligand binding?
What happens to a neuron if sodium channels are blocked?
What happens to a neuron if sodium channels are blocked?
Which is a common terminal effect of receptor signaling in cells?
Which is a common terminal effect of receptor signaling in cells?
What typically occurs during excessive stimulation of a postsynaptic cell?
What typically occurs during excessive stimulation of a postsynaptic cell?
What initial change occurs when an action potential reaches the presynaptic membrane?
What initial change occurs when an action potential reaches the presynaptic membrane?
Why is it difficult to generate an action potential during hypokalemia?
Why is it difficult to generate an action potential during hypokalemia?
What is receptor upregulation primarily a response to?
What is receptor upregulation primarily a response to?
What is the goal of down regulation in cellular responses?
What is the goal of down regulation in cellular responses?
What type of drug is propofol considered?
What type of drug is propofol considered?
In a graded dose response curve, what typically happens at the plateau phase?
In a graded dose response curve, what typically happens at the plateau phase?
Why is individualization of drug therapy important in clinical practice?
Why is individualization of drug therapy important in clinical practice?
What does receptor upregulation typically NOT involve?
What does receptor upregulation typically NOT involve?
When does a cell undergo down regulation?
When does a cell undergo down regulation?
What effect does metallas metallism have on furosemide?
What effect does metallas metallism have on furosemide?
Which mechanism primarily describes the relationship between drug potency and receptor affinity?
Which mechanism primarily describes the relationship between drug potency and receptor affinity?
What aspect does titration in pharmacology primarily address?
What aspect does titration in pharmacology primarily address?
On which axis is drug potency depicted on a dose response curve?
On which axis is drug potency depicted on a dose response curve?
Which axis typically represents drug dose in a dose response curve?
Which axis typically represents drug dose in a dose response curve?
What effect does constant antagonism have on receptor numbers?
What effect does constant antagonism have on receptor numbers?
What does a leftward shift in a dose response curve indicate?
What does a leftward shift in a dose response curve indicate?
What does a steep slope on a dose-response curve typically indicate regarding receptor binding?
What does a steep slope on a dose-response curve typically indicate regarding receptor binding?
In a quantal dose-response curve, what is the primary focus of the plotted data?
In a quantal dose-response curve, what is the primary focus of the plotted data?
Which of the following is NOT a superpower mentioned as a preference?
Which of the following is NOT a superpower mentioned as a preference?
What happens to the dose response curve when a competitive antagonist is introduced?
What happens to the dose response curve when a competitive antagonist is introduced?
What term describes the effective dose that yields the desired response in 50% of a population?
What term describes the effective dose that yields the desired response in 50% of a population?
What is the primary definition of efficacy in pharmacology?
What is the primary definition of efficacy in pharmacology?
What happens when a drug reaches a therapeutic plateau in a dose response curve?
What happens when a drug reaches a therapeutic plateau in a dose response curve?
What type of information would you be least likely to find in drug trials?
What type of information would you be least likely to find in drug trials?
Which of the following best describes the therapeutic index?
Which of the following best describes the therapeutic index?
What does the slope of a dose response curve represent?
What does the slope of a dose response curve represent?
When discussing dose response curves, what does the log scale often represent?
When discussing dose response curves, what does the log scale often represent?
What does partial efficacy mean in the context of drug response?
What does partial efficacy mean in the context of drug response?
How does a non-competitive antagonist alter a dose response curve?
How does a non-competitive antagonist alter a dose response curve?
What is identified by the therapeutic index?
What is identified by the therapeutic index?
How is potency best defined in pharmacology?
How is potency best defined in pharmacology?
How does receptor upregulation primarily affect a cell's response?
How does receptor upregulation primarily affect a cell's response?
What describes tachyphylaxis in pharmacology?
What describes tachyphylaxis in pharmacology?
Which statement regarding agonists is true?
Which statement regarding agonists is true?
Which statement is true regarding a racemic mixture?
Which statement is true regarding a racemic mixture?
What is indicated by an inverse agonist on a dose-response curve?
What is indicated by an inverse agonist on a dose-response curve?
Why is the ED50 significant in drug studies?
Why is the ED50 significant in drug studies?
What is indicated by a decreased slope on the dose response curve?
What is indicated by a decreased slope on the dose response curve?
What is the primary focus of pharmacogenetics?
What is the primary focus of pharmacogenetics?
In the context of anesthetics, what does the expression 'spectrum from awake to totally unconscious' refer to?
In the context of anesthetics, what does the expression 'spectrum from awake to totally unconscious' refer to?
Which factor influences the shape of a dose-response curve significantly?
Which factor influences the shape of a dose-response curve significantly?
What should researchers primarily study to assess potential toxic side effects of a drug?
What should researchers primarily study to assess potential toxic side effects of a drug?
Why might researchers prefer to use LD50 over TD50 in calculating the therapeutic index?
Why might researchers prefer to use LD50 over TD50 in calculating the therapeutic index?
What is a common feature of receptor pharmacology that underlies the application of agonists?
What is a common feature of receptor pharmacology that underlies the application of agonists?
What is the primary effect of a full agonist on a receptor?
What is the primary effect of a full agonist on a receptor?
What is the result of continuous administration of a full agonist?
What is the result of continuous administration of a full agonist?
What characterizes a partial agonist compared to a full agonist?
What characterizes a partial agonist compared to a full agonist?
What issue may arise if a patient on buprenorphine undergoes surgery without stopping the medication?
What issue may arise if a patient on buprenorphine undergoes surgery without stopping the medication?
How do antagonists typically interact with receptors?
How do antagonists typically interact with receptors?
What happens when a non-competitive antagonist is introduced in the presence of an agonist?
What happens when a non-competitive antagonist is introduced in the presence of an agonist?
What is the primary distinction between competitive and non-competitive antagonism?
What is the primary distinction between competitive and non-competitive antagonism?
In a dose-response curve, what effect does introducing a competitive antagonist have?
In a dose-response curve, what effect does introducing a competitive antagonist have?
Why might a partial agonist not be appropriate for pain management in opioid-dependent patients?
Why might a partial agonist not be appropriate for pain management in opioid-dependent patients?
What role do catecholamines play in the body related to agonism?
What role do catecholamines play in the body related to agonism?
What best describes a scenario of a patient experiencing a femur fracture while on buprenorphine?
What best describes a scenario of a patient experiencing a femur fracture while on buprenorphine?
What can occur as a result of receptor downregulation after continuous administration of an agonist?
What can occur as a result of receptor downregulation after continuous administration of an agonist?
What is the effect of a mixed agonist-antagonist on receptor activation?
What is the effect of a mixed agonist-antagonist on receptor activation?
What defines the 'ceiling effect' of a partial agonist?
What defines the 'ceiling effect' of a partial agonist?
What factors determine the time limit for the exam?
What factors determine the time limit for the exam?
In terms of expectation management, what advice was humorously suggested for students?
In terms of expectation management, what advice was humorously suggested for students?
When will students typically find out their exam grades?
When will students typically find out their exam grades?
What is the correct physiological pH referenced in the discussion concerning weak acids?
What is the correct physiological pH referenced in the discussion concerning weak acids?
What pharmacokinetic factor could significantly influence a patient's drug response aside from age and weight?
What pharmacokinetic factor could significantly influence a patient's drug response aside from age and weight?
Which side of the blood-brain barrier is expected to have a greater fraction of ion trapping for a weak acid with a pKa of 9?
Which side of the blood-brain barrier is expected to have a greater fraction of ion trapping for a weak acid with a pKa of 9?
What did the instructor emphasize about the use of study materials for the exam?
What did the instructor emphasize about the use of study materials for the exam?
Which population is more likely to be classified as ultra-rapid metabolizers of certain medications?
Which population is more likely to be classified as ultra-rapid metabolizers of certain medications?
What will the instructor provide concerning the exam format before the exam date?
What will the instructor provide concerning the exam format before the exam date?
What is a single nucleotide polymorphism (SNP)?
What is a single nucleotide polymorphism (SNP)?
What is likely to happen if a question from the practice examples is found confusing?
What is likely to happen if a question from the practice examples is found confusing?
How do hormonal differences between sexes potentially affect drug response?
How do hormonal differences between sexes potentially affect drug response?
What could indicate that a patient is not responding to a medication as expected?
What could indicate that a patient is not responding to a medication as expected?
For a weak acid, which parameter is essential for determining if it is ionized or non-ionized in solution?
For a weak acid, which parameter is essential for determining if it is ionized or non-ionized in solution?
What potential issue arises if a student focuses only on lecture content and neglects other materials?
What potential issue arises if a student focuses only on lecture content and neglects other materials?
Why might a patient require higher anesthesia doses based on genetic factors?
Why might a patient require higher anesthesia doses based on genetic factors?
Which drugs are commonly studied for genetically based treatment algorithms?
Which drugs are commonly studied for genetically based treatment algorithms?
What is the expected range of questions students can anticipate in the upcoming exam?
What is the expected range of questions students can anticipate in the upcoming exam?
Why might students not receive preliminary results immediately after the exam?
Why might students not receive preliminary results immediately after the exam?
What can lead to differences in how quickly patients emerge from anesthesia?
What can lead to differences in how quickly patients emerge from anesthesia?
How does population-based variability influence pharmacologic dosing?
How does population-based variability influence pharmacologic dosing?
What humorous method did the instructor suggest they could use to motivate students?
What humorous method did the instructor suggest they could use to motivate students?
In the context of pharmacogenomics, what do variances in CYP450 isoenzymes typically affect?
In the context of pharmacogenomics, what do variances in CYP450 isoenzymes typically affect?
In ion trapping, which solution would potentially hold more of a weak acid's non-ionized form?
In ion trapping, which solution would potentially hold more of a weak acid's non-ionized form?
Which factor does NOT contribute to pharmacologic response variability among individuals?
Which factor does NOT contribute to pharmacologic response variability among individuals?
What percentage of Caucasians might be classified as poor metabolizers for certain drugs metabolized by CYP2D6?
What percentage of Caucasians might be classified as poor metabolizers for certain drugs metabolized by CYP2D6?
Which term refers to the scientific study of how genetic differences affect individual responses to drugs?
Which term refers to the scientific study of how genetic differences affect individual responses to drugs?
What might clinicians do if they observe a patient requiring unusually high doses of opioids post-operatively?
What might clinicians do if they observe a patient requiring unusually high doses of opioids post-operatively?
What effect do positive allosteric modulators have on GABA receptors?
What effect do positive allosteric modulators have on GABA receptors?
How does the interaction between anesthetic gases illustrate additive effects?
How does the interaction between anesthetic gases illustrate additive effects?
Which of the following interactions is an example of a synergistic effect?
Which of the following interactions is an example of a synergistic effect?
What is the primary characteristic of tachyphylaxis in drug administration?
What is the primary characteristic of tachyphylaxis in drug administration?
What is an example of potentiation in pharmacological terms?
What is an example of potentiation in pharmacological terms?
Which of the following best describes antagonistic effects in drug interactions?
Which of the following best describes antagonistic effects in drug interactions?
In the context of anesthesia, why is it important to monitor the use of propofol and fentanyl together?
In the context of anesthesia, why is it important to monitor the use of propofol and fentanyl together?
What should be considered if phenylephrine's effectiveness appears to diminish at high doses?
What should be considered if phenylephrine's effectiveness appears to diminish at high doses?
What is the primary mechanism by which tachyphylaxis may occur?
What is the primary mechanism by which tachyphylaxis may occur?
What is the risk of using high doses of multiple vasopressors like phenylephrine?
What is the risk of using high doses of multiple vasopressors like phenylephrine?
What can be suggested if a patient on phenylephrine is not responding at high doses?
What can be suggested if a patient on phenylephrine is not responding at high doses?
Which situation summarizes a misunderstanding related to how GABA agonists and benzodiazepines interact?
Which situation summarizes a misunderstanding related to how GABA agonists and benzodiazepines interact?
How do drugs combined for antiretroviral therapy function typically?
How do drugs combined for antiretroviral therapy function typically?
Why is understanding the concept of synergistic effects crucial for anesthetists?
Why is understanding the concept of synergistic effects crucial for anesthetists?
How does a competitive antagonist affect catecholamine potency on alpha and beta receptors?
How does a competitive antagonist affect catecholamine potency on alpha and beta receptors?
What happens to receptors when there is continuous blockade by antagonists?
What happens to receptors when there is continuous blockade by antagonists?
What characterizes inverse agonists compared to traditional antagonists?
What characterizes inverse agonists compared to traditional antagonists?
Which action is NOT characteristic of antagonists?
Which action is NOT characteristic of antagonists?
In a competitive antagonism scenario, what is required to achieve a therapeutic effect when a patient is on metoprolol?
In a competitive antagonism scenario, what is required to achieve a therapeutic effect when a patient is on metoprolol?
How do allosteric modulators function compared to traditional agonists?
How do allosteric modulators function compared to traditional agonists?
What is the consequence of using an opioid antagonist like Narcan in a patient with significant opioid exposure?
What is the consequence of using an opioid antagonist like Narcan in a patient with significant opioid exposure?
Which statement is true regarding beta blockers like metoprolol?
Which statement is true regarding beta blockers like metoprolol?
What is an effect of using neostigmine in the context of neuromuscular junction antagonism?
What is an effect of using neostigmine in the context of neuromuscular junction antagonism?
In what situation might antagonists and agonists coexist at a receptor site?
In what situation might antagonists and agonists coexist at a receptor site?
What role do inverse agonists play in receptor pharmacology?
What role do inverse agonists play in receptor pharmacology?
What differentiates an agonist from an inverse agonist regarding their effects on cyclic AMP?
What differentiates an agonist from an inverse agonist regarding their effects on cyclic AMP?
Why is it challenging to achieve a clinical effect with high opioid concentrations?
Why is it challenging to achieve a clinical effect with high opioid concentrations?
What is a potential outcome of prolonged antagonist use on receptor systems?
What is a potential outcome of prolonged antagonist use on receptor systems?
What effect does progesterone have on the sensitivity to general anesthetics during pregnancy?
What effect does progesterone have on the sensitivity to general anesthetics during pregnancy?
Why might pregnant patients at risk for emergent procedures require less general anesthetic?
Why might pregnant patients at risk for emergent procedures require less general anesthetic?
What is one reason that neonates may struggle with drug elimination compared to older children?
What is one reason that neonates may struggle with drug elimination compared to older children?
What are the characteristics of drugs that do not undergo metabolism?
What are the characteristics of drugs that do not undergo metabolism?
How does the volume of distribution for propofol compare to that of rocuronium?
How does the volume of distribution for propofol compare to that of rocuronium?
What is the primary reason for keeping anesthetic levels low in pregnant patients under general anesthesia?
What is the primary reason for keeping anesthetic levels low in pregnant patients under general anesthesia?
What might increase the risk of awareness during general anesthesia in a pregnant patient?
What might increase the risk of awareness during general anesthesia in a pregnant patient?
In neonates, what characteristic of renal function affects drug excretion?
In neonates, what characteristic of renal function affects drug excretion?
Why would it be important to consider drug ionization in neonates?
Why would it be important to consider drug ionization in neonates?
What is the relationship between drug solubility and its elimination by renal systems?
What is the relationship between drug solubility and its elimination by renal systems?
How does the effect site concentration relate to the volume of distribution of a drug?
How does the effect site concentration relate to the volume of distribution of a drug?
How might the immaturity of neonatal renal systems specifically impact drug management?
How might the immaturity of neonatal renal systems specifically impact drug management?
What conclusion can be drawn regarding drug metabolism in neonates compared to adults?
What conclusion can be drawn regarding drug metabolism in neonates compared to adults?
Flashcards
Hyperpolarization
Hyperpolarization
The state of a neuron where it is more negative than its resting potential. This occurs after an action potential due to the continued outflow of potassium ions, making the cell more negative than usual.
Sodium-Potassium Pump
Sodium-Potassium Pump
A protein embedded in the cell membrane that pumps sodium ions out of the cell and potassium ions into the cell. It helps restore the resting membrane potential after an action potential.
Potassium Channel
Potassium Channel
A type of ion channel that allows potassium ions to move across the cell membrane. It plays a role in repolarizing the neuron after an action potential.
Sodium Channel
Sodium Channel
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Inactivated State (Sodium Channel)
Inactivated State (Sodium Channel)
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Closed State (Sodium Channel)
Closed State (Sodium Channel)
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Resting Membrane Potential
Resting Membrane Potential
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Repolarization
Repolarization
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Hypocalcemia's effect on action potentials
Hypocalcemia's effect on action potentials
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How hypercalcemia impacts neuron excitability
How hypercalcemia impacts neuron excitability
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Hypokalemia effect on resting membrane potential
Hypokalemia effect on resting membrane potential
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Sodium channel blockade & action potential
Sodium channel blockade & action potential
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What is a synapse?
What is a synapse?
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Neurotransmitter release at the synapse
Neurotransmitter release at the synapse
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Role of reuptake pumps at the synapse
Role of reuptake pumps at the synapse
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Synaptic modulation
Synaptic modulation
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Synaptic delay
Synaptic delay
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Synaptic fatigue
Synaptic fatigue
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Downregulation of receptors
Downregulation of receptors
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Action potential
Action potential
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Efferent action potential
Efferent action potential
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Afferent action potential
Afferent action potential
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Postsynaptic density
Postsynaptic density
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Neuronal Fatigue
Neuronal Fatigue
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Catecholamine Depletion
Catecholamine Depletion
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Post-tetanic Facilitation (PTF)
Post-tetanic Facilitation (PTF)
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Neuronal Responsiveness
Neuronal Responsiveness
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Ligands
Ligands
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Sensitivity (of a Receptor)
Sensitivity (of a Receptor)
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Selectivity (of a Receptor)
Selectivity (of a Receptor)
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Specificity (of a Receptor)
Specificity (of a Receptor)
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Ligand-Receptor Bond Strength
Ligand-Receptor Bond Strength
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Polar Heads of Phospholipids
Polar Heads of Phospholipids
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Nonpolar Tails of Phospholipids
Nonpolar Tails of Phospholipids
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Channel/Carrier Protein
Channel/Carrier Protein
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Lipid Solubility
Lipid Solubility
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Diffusion
Diffusion
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Conformational Change
Conformational Change
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Ligand-gated Ion Channel
Ligand-gated Ion Channel
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Inactivated State
Inactivated State
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Open State
Open State
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G Protein-coupled Receptor
G Protein-coupled Receptor
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Kinase-linked Receptor
Kinase-linked Receptor
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Nuclear Receptor
Nuclear Receptor
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Cation
Cation
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Anion
Anion
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Glutamate
Glutamate
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GABA
GABA
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Glycine
Glycine
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Drug-Receptor Binding
Drug-Receptor Binding
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Lipophilic
Lipophilic
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Hydrogen bonding
Hydrogen bonding
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Aceptor binding
Aceptor binding
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Acceptors
Acceptors
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G Protein-Coupled Receptor (GPCR)
G Protein-Coupled Receptor (GPCR)
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Voltage-Gated Ion Channel
Voltage-Gated Ion Channel
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Van der Waals London Dispersion Forces
Van der Waals London Dispersion Forces
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Covalent Bonding
Covalent Bonding
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Non-competitive antagonist
Non-competitive antagonist
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Duration of Action
Duration of Action
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Dipole-Dipole Interactions
Dipole-Dipole Interactions
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Hydrophobic
Hydrophobic
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Prolonged Effect Drug
Prolonged Effect Drug
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Alpha Blocker
Alpha Blocker
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Prolonged Side Effects
Prolonged Side Effects
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Irreversible Drug Binding
Irreversible Drug Binding
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Stereochemistry
Stereochemistry
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Chiral Molecule
Chiral Molecule
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Enantiomers
Enantiomers
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Racemic Mixture
Racemic Mixture
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S Isomer
S Isomer
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R Isomer
R Isomer
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Racemic Ketamine
Racemic Ketamine
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Esketamine
Esketamine
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Arbupivacaine
Arbupivacaine
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Levobupivacaine
Levobupivacaine
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Receptor Upregulation
Receptor Upregulation
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Receptor Downregulation
Receptor Downregulation
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Agonist
Agonist
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Antagonist
Antagonist
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Phase I Clinical Trial
Phase I Clinical Trial
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Titration
Titration
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Graded Dose Response Curve
Graded Dose Response Curve
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Plateau
Plateau
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Pharmacology
Pharmacology
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Individualized Drug Therapy
Individualized Drug Therapy
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Clinical Pharmacology
Clinical Pharmacology
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GABA Agonist
GABA Agonist
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Pharmaceutics
Pharmaceutics
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Pharmacokinetics
Pharmacokinetics
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Pharmacodynamics
Pharmacodynamics
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Slope of dose-response curve
Slope of dose-response curve
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Efficacy
Efficacy
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Potency
Potency
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EC50 or C50
EC50 or C50
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ED50
ED50
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Therapeutic Index
Therapeutic Index
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Full Agonist
Full Agonist
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Partial Agonist
Partial Agonist
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Inverse Agonist
Inverse Agonist
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Spectrum of drug effects
Spectrum of drug effects
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Variability in drug effects
Variability in drug effects
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Dose-response curve application
Dose-response curve application
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Competitive Antagonist
Competitive Antagonist
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Upregulation
Upregulation
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Allosteric Modulator
Allosteric Modulator
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Neostigmine
Neostigmine
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Naloxone
Naloxone
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Upregulation
Upregulation
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Allosteric Modulator
Allosteric Modulator
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Neostigmine
Neostigmine
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Naloxone
Naloxone
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Partial Agonist - Blocking Effect
Partial Agonist - Blocking Effect
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Dose-Response Curve Changes
Dose-Response Curve Changes
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Anesthetic
Anesthetic
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Esmolol
Esmolol
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Norepinephrine
Norepinephrine
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Succinylcholine
Succinylcholine
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Positive Allosteric Modulation (PAM)
Positive Allosteric Modulation (PAM)
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Negative Allosteric Modulation
Negative Allosteric Modulation
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Additive Effect
Additive Effect
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Antagonistic Effect
Antagonistic Effect
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Synergistic Effect
Synergistic Effect
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Potentiation
Potentiation
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Tachyphylaxis
Tachyphylaxis
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Tachyphylaxis (with phenylephrine)
Tachyphylaxis (with phenylephrine)
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Combination Therapy (Potentiation)
Combination Therapy (Potentiation)
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Metoxolone (Potentiating Diuretics)
Metoxolone (Potentiating Diuretics)
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Drug Interactions (Synergy)
Drug Interactions (Synergy)
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Tolerance
Tolerance
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Metal
Metal
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What is C50?
What is C50?
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What is an agonist?
What is an agonist?
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What is potency?
What is potency?
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What is efficacy?
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What is the therapeutic index?
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What is an antagonist?
What is an antagonist?
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What is tachyphylaxis?
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What is pharmacogenetics?
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Population-based differences in metabolism
Population-based differences in metabolism
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Pharmacodynamic differences
Pharmacodynamic differences
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Precision medicine
Precision medicine
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Effect of a competitive antagonist on a dose-response curve
Effect of a competitive antagonist on a dose-response curve
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Effect of a non-competitive antagonist on a dose-response curve
Effect of a non-competitive antagonist on a dose-response curve
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What does the slope of a dose-response curve tell us?
What does the slope of a dose-response curve tell us?
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pH and Ionization in Plasma
pH and Ionization in Plasma
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Blood-Brain Barrier
Blood-Brain Barrier
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Drug Binding to Albumin
Drug Binding to Albumin
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Polymorphisms
Polymorphisms
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SNP
SNP
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What is Cyp2D6?
What is Cyp2D6?
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Poor Metabolizer
Poor Metabolizer
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Ultra-Rapid Metabolizer
Ultra-Rapid Metabolizer
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What to consider when patients need more drugs than expected?
What to consider when patients need more drugs than expected?
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Population-Based Variability
Population-Based Variability
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Influences on pharmacologic response
Influences on pharmacologic response
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Unanticipated drug responses
Unanticipated drug responses
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Individualized therapy
Individualized therapy
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Genetically based treatment algorithms
Genetically based treatment algorithms
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Sex differences in drug response
Sex differences in drug response
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Red hair and anesthesia
Red hair and anesthesia
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Why are pregnant women at higher risk of awareness under general anesthesia?
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How does progesterone impact anesthetic sensitivity in labor?
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Why do newborns have difficulty eliminating uncharged drugs?
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Why are uncharged drugs a concern in newborns?
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How does an immature kidney affect drug elimination?
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Why does propofol have a high volume of distribution?
Why does propofol have a high volume of distribution?
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What does volume of distribution indicate?
What does volume of distribution indicate?
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Why does rocuronium have a low volume of distribution?
Why does rocuronium have a low volume of distribution?
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How does volume of distribution affect drug dosing?
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Why is rocuronium's water solubility significant?
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How does a high volume of distribution affect drug action?
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How does volume of distribution affect the duration of action?
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How does a low volume of distribution affect the duration of action?
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How does volume of distribution affect elimination?
How does volume of distribution affect elimination?
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Ion trapping
Ion trapping
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Ionization
Ionization
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pKa
pKa
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Drug compartment with greater fraction trapped
Drug compartment with greater fraction trapped
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Receptor sensitivity
Receptor sensitivity
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Receptor selectivity
Receptor selectivity
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Receptor specificity
Receptor specificity
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Study Notes
Repolarization and Action Potentials
- Cations are lost, specifically potassium, causing the cell to repolarize (return to a negative membrane potential).
- Potassium channels are slower than sodium channels. Sodium channels open rapidly, flooding the cell with sodium, then inactivate. Potassium channels take longer to both open and close.
- Potassium efflux can lead to hyperpolarization—the cell becomes more negative than its resting potential.
- The sodium-potassium pump restores the resting membrane potential by pumping sodium out and potassium in.
- Sodium channels transition from inactivated to closed state, preparing for the next stimulus
Electrolyte Abnormalities and Neuronal Responsiveness
- Hypocalcemia: Prevents sodium channels from closing between action potentials, causing repetitive firing (tetany).
- Hypercalcemia: Decreases cell membrane permeability to sodium, hindering neuronal excitation..
- Hypokalemia: Leads to a more negative resting membrane potential, decreasing neuronal excitability due to hyperpolarization.
- Sodium channel blockade: Prevents reaching threshold potential, inhibiting action potential generation.
Synaptic Transmission
- Presynaptic cells release neurotransmitters into the synaptic cleft via vesicles.
- Calcium influx triggers the fusion of vesicles with the cell membrane.
- Reuptake pumps bring neurotransmitters back into the presynaptic cell for reuse or breakdown.
- Acetylcholine is an example of a neurotransmitter that's broken down and reabsorbed.
Postsynaptic Density and Synaptic Modulation
- Postsynaptic density maintains homeostasis and integrity in the postsynaptic region.
- Synaptic modulation refers to changes in synaptic function, including signaling, depolarization, and responses.
- Synaptic delay is a slight delay between neural communication, beneficial in reducing fatigue and constant triggering of the postsynaptic cell.
- Tachyphylaxis can also occur with repetitive stimulation or depletion of neurotransmitters.
Receptor Pharmacology
- Receptors are proteins that bind endogenous chemicals or drugs.
- Receptor properties include:
- Sensitivity: Concentration needed for cellular response.
- Selectivity: Ability of a molecule to fit into the receptor opening.
- Specificity: Cellular response dependent on tissue type.
- Receptor binding often involves hydrophobic bonding, for lipid-soluble drugs
- Acceptors are alternative drug binding sites.
- Different receptor types exist (G protein-coupled, ligand-gated ion channels, voltage-gated ion channels, kinase-linked, and nuclear receptors).
Receptor Activation and Cellular Responses
- Ligand binding causes a conformational change in the receptor.
- Receptors transduce signals, amplifying or integrating biochemically pathways, causing changes in gene expression, cellular metabolism, and even apoptosis.
- Ion channels (sodium, calcium, chloride, potassium) play a critical role; cations (sodium & calcium) are excitatory, anions (chloride) are inhibitory.
- Different conformations can affect their pharmacologic effects.
Receptor Upregulation and Downregulation
- Upregulation: Increases receptor number and sensitivity in response to insufficient agonist stimulation or consistent antagonist blockade.
- Downregulation: Decreases receptor number and sensitivity in response to excessive agonist stimulation.
Receptor Types (Agonists, Partial Agonists, Antagonists, Inverse Agonists)
- Agonists: Activate the receptor. Examples include catecholamines, propofol, and fentanyl. Continuous administration may cause downregulation.
- Partial agonists: Limited receptor activation, cannot reach maximal response. Examples include buprenorphine.
- Antagonists: Block receptor activation and prevent agonist binding. Examples include beta-blockers (esmolol, metoprolol) and competitive antagonists like Narcan.
- Inverse agonists: Decrease receptor activity. Examples include certain beta blockers (like carvedilol and propranolol).
Allosteric Modulators
- Allosteric modulators bind to a different site on a receptor than the agonist, modifying the agonist's effect.
- Benzodiazepines are an example of positive allosteric modulators of GABA receptors.
Drug Interactions and Variability
- Additive effects: Summation of drug effects.
- Antagonistic effects: One drug blocks the response of another.
- Synergistic effects: Combined effect is greater than the sum of individual effects (common with anesthetics and opioids).
- Potentiation: One drug enhances the effect of another. Examples include antiretroviral therapies.
- Tachyphylaxis: Decreased efficacy after repeated drug administration.
- Pharmacogenetics/pharmacogenomics: Study of genetic variations in drug response; metabolism, absorption, distribution, and excretion can all be affected. Polymorphisms, particularly SNPs, play an important role.
Population-based Variability and Pharmacokinetics/Pharmacodynamics
- Consideration of age, sex, weight, body surface area, and other factors in drug administration for optimal response.
- Clinical responses vary greatly in diverse populations due to genetic variations. CYP enzymes, like CYP2D6, affect drug metabolism and responses.
Clinical Example of Receptor Interactions
- Competitive antagonism: Beta-blocker (esmolol) may require higher doses of catecholamines (epinephrine) to overcome the blockade and stimulate the heart.
- Noncompetitive antagonism (not common clinically): A scenario where the patient is receiving an irreversible competitive antagonist, for example, Succinylcholine, which is being blocked by an irreversible competitive antagonist, Rocuronium, which is hard to overcome the blockade and may require Neostigmine to reverse the block.
Stereochemistry and Chirality
- Stereochemistry: Describes the 3D molecular structure of molecules like drugs and endogenous substances.
- Chirality: Molecules with 3D asymmetry (e.g., enantiomers).
- Racemic mixtures: 50/50 mix of enantiomers. Example: Ketamine.
- Certain enantiomers (e.g., S-ketamine) may be more potent or produce fewer side effects than others (e.g., R-ketamine).
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