Podcast
Questions and Answers
What is the primary inhibitory neurotransmitter in the brain?
What is the primary inhibitory neurotransmitter in the brain?
- Dopamine
- Glutamate
- Serotonin
- GABA (correct)
What does the efficacy of a drug refer to?
What does the efficacy of a drug refer to?
- The duration of action of the drug
- The maximal response when all receptor sites are occupied (correct)
- The chemical composition of the drug
- The route of administration for the drug
How is the primary mechanism of termination of action of a bolus dose of an anesthetic induction agent achieved?
How is the primary mechanism of termination of action of a bolus dose of an anesthetic induction agent achieved?
- Redistribution to the vessel intermediate group (correct)
- Metabolism by the liver
- Reabsorption into the central nervous system
- Excretion through the kidneys
What does volume of distribution represent?
What does volume of distribution represent?
Which type of drugs activate the GABAA receptor?
Which type of drugs activate the GABAA receptor?
Which measure is considered the best measure of renal function?
Which measure is considered the best measure of renal function?
What is the most reliable measure of glomerular filtration rate?
What is the most reliable measure of glomerular filtration rate?
What is a pharmacokinetic model that can adequately describe the pharmacokinetics of most anesthetic drugs?
What is a pharmacokinetic model that can adequately describe the pharmacokinetics of most anesthetic drugs?
What does the lag between peak plasma concentration and peak effect represent from a pharmacodynamic standpoint?
What does the lag between peak plasma concentration and peak effect represent from a pharmacodynamic standpoint?
Which type of receptors bind an extracellular molecule (ligand) and convert this input into a change in intracellular behavior?
Which type of receptors bind an extracellular molecule (ligand) and convert this input into a change in intracellular behavior?
Which family of receptors acts through activation or inhibition of an enzyme, ion channel, or other target?
Which family of receptors acts through activation or inhibition of an enzyme, ion channel, or other target?
Which type of receptors are typically a tyrosine kinase that phosphorylates an intracellular second messenger?
Which type of receptors are typically a tyrosine kinase that phosphorylates an intracellular second messenger?
What is the best measure for determining proper bolus dosing for a drug?
What is the best measure for determining proper bolus dosing for a drug?
Which type of drug is poorly absorbed from the GI tract?
Which type of drug is poorly absorbed from the GI tract?
Where is the principle site of absorption for oral drug administration?
Where is the principle site of absorption for oral drug administration?
Which route of administration bypasses the liver?
Which route of administration bypasses the liver?
In which of the following does the slowest equilibration of a drug occur?
In which of the following does the slowest equilibration of a drug occur?
Which compartment is the slowly equilibrating compartment?
Which compartment is the slowly equilibrating compartment?
What is the primary mechanism of termination of action of a bolus dose of an induction agent?
What is the primary mechanism of termination of action of a bolus dose of an induction agent?
What is the function of the apparent volume of distribution (Vd)?
What is the function of the apparent volume of distribution (Vd)?
Which of the following does not affect the volume of distribution of a drug?
Which of the following does not affect the volume of distribution of a drug?
'Only free drug can cross cell membranes' - this statement refers to which phenomenon?
'Only free drug can cross cell membranes' - this statement refers to which phenomenon?
'Most drugs are protein bound to some extent' - what reduces the concentration of plasma proteins?
'Most drugs are protein bound to some extent' - what reduces the concentration of plasma proteins?
Which type of receptor consists of a protein linked to 7 transmembrane spanning domains?
Which type of receptor consists of a protein linked to 7 transmembrane spanning domains?
What results in a conformational change in the G protein-coupled receptor, allowing substitution of GTP for GDP on the Gα protein?
What results in a conformational change in the G protein-coupled receptor, allowing substitution of GTP for GDP on the Gα protein?
Which neurotransmitter acts as the primary excitatory neurotransmitter in the central nervous system and is important in learning, memory, and central pain transduction?
Which neurotransmitter acts as the primary excitatory neurotransmitter in the central nervous system and is important in learning, memory, and central pain transduction?
Which ion channel opens when ions flow in or out based on their concentration gradients?
Which ion channel opens when ions flow in or out based on their concentration gradients?
Entry of which ion inhibits the cell?
Entry of which ion inhibits the cell?
Which type of receptor is associated with rapid synaptic transmission, synaptic plasticity, and long-term potentiation?
Which type of receptor is associated with rapid synaptic transmission, synaptic plasticity, and long-term potentiation?
What activates the Gα protein which then activates or inhibits an enzyme, ion channel, or other target?
What activates the Gα protein which then activates or inhibits an enzyme, ion channel, or other target?
What characterizes an agonist according to the receptor theory?
What characterizes an agonist according to the receptor theory?
What is the defining factor for potency according to the receptor theory?
What is the defining factor for potency according to the receptor theory?
Which type of antagonist can be overcome by large doses of agonist?
Which type of antagonist can be overcome by large doses of agonist?
What is the main difference between partial and full agonists?
What is the main difference between partial and full agonists?
In pharmacokinetics, what does the term 'volume of distribution' refer to?
In pharmacokinetics, what does the term 'volume of distribution' refer to?
Which type of drugs come in an acidic solution to render them more water soluble?
Which type of drugs come in an acidic solution to render them more water soluble?
What does $pKa - pH$ indicate when it's a negative number for weak bases?
What does $pKa - pH$ indicate when it's a negative number for weak bases?
Which enzyme is responsible for the metabolism of the majority of drugs?
Which enzyme is responsible for the metabolism of the majority of drugs?
Which phase of drug metabolism increases the drugs polarity preparing it for phase II reactions?
Which phase of drug metabolism increases the drugs polarity preparing it for phase II reactions?
What is the formula for hepatic extraction ratio (ER)?
What is the formula for hepatic extraction ratio (ER)?
Which type of drug metabolism is more affected by changes in liver blood flow?
Which type of drug metabolism is more affected by changes in liver blood flow?
Which drug is categorized as a low hepatic extraction ratio (HER) drug?
Which drug is categorized as a low hepatic extraction ratio (HER) drug?
Which process involves the passive reabsorption of water-soluble drugs from the tubules?
Which process involves the passive reabsorption of water-soluble drugs from the tubules?
What is the formula for Calculated Creatinine Clearance?
What is the formula for Calculated Creatinine Clearance?
What is the main purpose of concentration-response relationships in pharmacodynamics?
What is the main purpose of concentration-response relationships in pharmacodynamics?
Which term describes the maximum effect a drug can produce?
Which term describes the maximum effect a drug can produce?
What is the therapeutic index of a drug?
What is the therapeutic index of a drug?
What is the main focus of response surface models?
What is the main focus of response surface models?
What does ED50 stand for in pharmacology?
What does ED50 stand for in pharmacology?
What is the time required for the drug concentration to decrease by 50% following termination of a steady state infusion?
What is the time required for the drug concentration to decrease by 50% following termination of a steady state infusion?
Which mathematical technique is sometimes labeled non-compartmental and may avoid some of the confusion related to trying to perceive a compartment as specific tissues?
Which mathematical technique is sometimes labeled non-compartmental and may avoid some of the confusion related to trying to perceive a compartment as specific tissues?
What do isoconcentration nomograms plot?
What do isoconcentration nomograms plot?
What is used to compensate for distribution to peripheral tissues in the BET dosing scheme?
What is used to compensate for distribution to peripheral tissues in the BET dosing scheme?
What is the main consideration when determining the initial infusion rate in practice?
What is the main consideration when determining the initial infusion rate in practice?
What is the primary mechanism for patient controlled sedation with propofol?
What is the primary mechanism for patient controlled sedation with propofol?
What is used to control drug delivery in closed-loop infusions for anesthetic purposes?
What is used to control drug delivery in closed-loop infusions for anesthetic purposes?
What does hysteresis/biophase refer to in combined pharmacokinetic/pharmacodynamic models?
What does hysteresis/biophase refer to in combined pharmacokinetic/pharmacodynamic models?
Study Notes
Neurotransmitters
- The primary inhibitory neurotransmitter in the brain is GABA (gamma-aminobutyric acid).
- Glutamate serves as the primary excitatory neurotransmitter in the central nervous system, crucial for learning and memory.
Drug Mechanisms and Efficacy
- Efficacy of a drug refers to its ability to produce a desired therapeutic effect.
- GABAA receptors are activated by sedative-hypnotic drugs, benzodiazepines, and barbiturates.
- Partial agonists produce a less than maximal response compared to full agonists at the same receptor.
Pharmacokinetics
- The volume of distribution (Vd) represents the degree to which a drug spreads into body tissues.
- The primary mechanism of termination for bolus doses of anesthetic induction agents is redistribution away from the site of action.
- Renal function is best measured using creatinine clearance or estimated glomerular filtration rate (GFR).
Administration and Absorption
- The principal site for oral drug absorption is the small intestine, where most nutrients and drugs are absorbed.
- Drugs poorly absorbed from the gastrointestinal tract often include large molecules or those with poor solubility.
- The intravenous route of administration bypasses the liver, leading to immediate bioavailability.
Drug Distribution and Compartment Theory
- The slowly equilibrating compartment refers to areas where drug distribution occurs slower, often including fat tissues.
- Volume of distribution impacts drug dosing and effectiveness; only free drugs can cross cell membranes to exert their effects.
Receptor Types and Functions
- Receptors that bind extracellular ligands and trigger intracellular changes include ionotropic and metabotropic receptors.
- G protein-coupled receptors are characterized by a protein linked to seven transmembrane domains.
- Tyrosine kinase receptors, which phosphorylate intracellular messengers, are associated with growth factors.
Pharmacodynamics
- The time lag between peak plasma concentration and peak effect reflects the pharmacodynamic response time.
- Agonists activate receptors, while antagonists inhibit them; competitive antagonists can be overcome by increasing agonist concentrations.
- The therapeutic index indicates drug safety, defined as the ratio of toxic dose to effective dose.
Drug Metabolism
- Phase I metabolism modifies drug structures to increase polarity, preparing for Phase II reactions, which involve conjugation.
- Cytochrome P450 enzymes are primarily responsible for metabolizing most drugs.
- Low hepatic extraction ratio (HER) drugs are less affected by changes in liver blood flow.
Clinical Measurements
- ED50 refers to the dose of a drug that produces 50% of its maximal effect.
- Creatinine clearance is calculated using renal function formulas to assess kidney health.
- Hysteresis in pharmacokinetic/pharmacodynamic models refers to the lag in drug effect compared to plasma concentration changes.
Drug Delivery Systems
- Concentration-response relationships assess how the dose correlates with drug effects.
- Patient-controlled analgesia with propofol allows patients to self-administer sedation effectively through closed-loop infusion systems.
- BET dosing schemes adjust for distribution to peripheral tissues to optimize drug delivery.
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