Podcast
Questions and Answers
Why would sodium bicarbonate injections increase renal excretion in a pentobarbital overdose?
Why would sodium bicarbonate injections increase renal excretion in a pentobarbital overdose?
- Bicarbonate alkalinizes the urine, increasing ionization and excretion of the weak acid. (correct)
- Bicarbonate directly binds to pentobarbital, forming a readily excretable complex.
- Bicarbonate increases glomerular filtration rate, enhancing drug clearance.
- Bicarbonate acidifies the urine, promoting excretion of the weak acid.
A drug is known to have poor absorption in the intestines due to its large molecular size. Which drug transport mechanism would be LEAST effective for this drug?
A drug is known to have poor absorption in the intestines due to its large molecular size. Which drug transport mechanism would be LEAST effective for this drug?
- Paracellular transport (correct)
- Transcellular transport
- Vesicular transport
- Carrier-mediated transport
A patient with compromised renal function has a glomerular filtration rate (GFR) significantly lower than the normal rate of 120 mL/min. Which of the following adjustments to drug therapy is MOST appropriate?
A patient with compromised renal function has a glomerular filtration rate (GFR) significantly lower than the normal rate of 120 mL/min. Which of the following adjustments to drug therapy is MOST appropriate?
- Administer the drug via intravenous bolus to bypass renal filtration.
- Switch to a drug that is primarily metabolized by the liver.
- Increase the dose to compensate for reduced filtration.
- Decrease the dose to prevent drug accumulation. (correct)
A patient is using a fentanyl patch for chronic pain management. What is the primary reason transdermal patches are suitable for this?
A patient is using a fentanyl patch for chronic pain management. What is the primary reason transdermal patches are suitable for this?
A highly lipophilic drug is extensively bound to plasma proteins. How does this protein binding MOST likely affect the drug's distribution and elimination?
A highly lipophilic drug is extensively bound to plasma proteins. How does this protein binding MOST likely affect the drug's distribution and elimination?
A drug undergoes enterohepatic recirculation. What is the MOST significant consequence of this process on the drug's action?
A drug undergoes enterohepatic recirculation. What is the MOST significant consequence of this process on the drug's action?
A drug is a known substrate of Multidrug Resistance Protein (MDR). What effect would increased expression of MDR in the intestines have on the drug's oral bioavailability?
A drug is a known substrate of Multidrug Resistance Protein (MDR). What effect would increased expression of MDR in the intestines have on the drug's oral bioavailability?
During a Phase I clinical trial, what is the PRIMARY focus when administering increasing doses of a new drug to a small group of healthy volunteers?
During a Phase I clinical trial, what is the PRIMARY focus when administering increasing doses of a new drug to a small group of healthy volunteers?
A sulfonamide drug is less effective in the presence of high concentrations of para-aminobenzoic acid (PABA) because:
A sulfonamide drug is less effective in the presence of high concentrations of para-aminobenzoic acid (PABA) because:
A bacterium produces beta-lactamase, resulting in resistance to penicillin. What is the MOST likely mechanism of this resistance?
A bacterium produces beta-lactamase, resulting in resistance to penicillin. What is the MOST likely mechanism of this resistance?
How does the presence of a highly expressed Multidrug Resistance Protein (MDR) in kidney cells affect drug elimination?
How does the presence of a highly expressed Multidrug Resistance Protein (MDR) in kidney cells affect drug elimination?
If a drug is known to undergo extensive first-pass metabolism, which route of administration would likely result in the highest bioavailability?
If a drug is known to undergo extensive first-pass metabolism, which route of administration would likely result in the highest bioavailability?
A drug is predominantly metabolized by CYP3A4 in the liver. If a patient starts taking ketoconazole, a strong CYP3A4 inhibitor, what change in the drug's half-life and plasma concentration would be expected?
A drug is predominantly metabolized by CYP3A4 in the liver. If a patient starts taking ketoconazole, a strong CYP3A4 inhibitor, what change in the drug's half-life and plasma concentration would be expected?
A patient with liver cirrhosis exhibits decreased production of albumin. How will this condition MOST likely influence the volume of distribution ($V_d$) of a highly protein-bound drug?
A patient with liver cirrhosis exhibits decreased production of albumin. How will this condition MOST likely influence the volume of distribution ($V_d$) of a highly protein-bound drug?
A drug that acts as a 'suicide inhibitor' does so by which mechanisms?
A drug that acts as a 'suicide inhibitor' does so by which mechanisms?
A new drug is developed that binds to an allosteric site of a receptor and enhances the receptor's response to its natural ligand. This drug is best described as:
A new drug is developed that binds to an allosteric site of a receptor and enhances the receptor's response to its natural ligand. This drug is best described as:
In a clinical trial, a drug shows a high degree of efficacy but causes a significant adverse effect in a notable percentage of patients. In which phase of clinical trials would this typically be identified and thoroughly evaluated?
In a clinical trial, a drug shows a high degree of efficacy but causes a significant adverse effect in a notable percentage of patients. In which phase of clinical trials would this typically be identified and thoroughly evaluated?
Which of the following is a key distinction between polypharmacy and polypharmacology?
Which of the following is a key distinction between polypharmacy and polypharmacology?
How does the mechanism of action of vancomycin differ from that of penicillin?
How does the mechanism of action of vancomycin differ from that of penicillin?
Which of the following methods for discovering new drug leads involves modifying the chemical structure of an existing drug to improve its efficacy or reduce its side effects?
Which of the following methods for discovering new drug leads involves modifying the chemical structure of an existing drug to improve its efficacy or reduce its side effects?
How does altering urine pH affect the excretion of weakly acidic drugs?
How does altering urine pH affect the excretion of weakly acidic drugs?
What is the primary role of the paracellular pathway in drug transport across the capillary endothelium?
What is the primary role of the paracellular pathway in drug transport across the capillary endothelium?
How does glomerular filtration rate (GFR) relate to renal plasma flow?
How does glomerular filtration rate (GFR) relate to renal plasma flow?
Why are transdermal drug delivery systems particularly suitable for long-term therapy?
Why are transdermal drug delivery systems particularly suitable for long-term therapy?
How does the binding of drugs to plasma proteins affect their distribution to extravascular tissues?
How does the binding of drugs to plasma proteins affect their distribution to extravascular tissues?
What is the effect of enterohepatic recirculation on drug clearance?
What is the effect of enterohepatic recirculation on drug clearance?
How does first-pass metabolism affect the bioavailability of a drug?
How does first-pass metabolism affect the bioavailability of a drug?
What is the primary function of Multidrug Resistance Protein (MDR) transporters in drug action?
What is the primary function of Multidrug Resistance Protein (MDR) transporters in drug action?
During Phase I clinical trials, what is the PRIMARY objective when administering a new drug to a small group of healthy volunteers?
During Phase I clinical trials, what is the PRIMARY objective when administering a new drug to a small group of healthy volunteers?
How do allosteric modulators affect receptor activity?
How do allosteric modulators affect receptor activity?
A drug is known to bind to plasma proteins. Which of the following is a potential consequence of this binding on drug distribution?
A drug is known to bind to plasma proteins. Which of the following is a potential consequence of this binding on drug distribution?
How does the administration of a drug via the transdermal route affect its rate of absorption and duration of action?
How does the administration of a drug via the transdermal route affect its rate of absorption and duration of action?
If a weakly acidic drug is administered to a patient, how would increasing the pH of the urine affect its excretion?
If a weakly acidic drug is administered to a patient, how would increasing the pH of the urine affect its excretion?
A drug user has developed resistance to a certain antibiotic due to increased expression of efflux pumps. How do these efflux pumps affect drug concentrations in bacterial cells?
A drug user has developed resistance to a certain antibiotic due to increased expression of efflux pumps. How do these efflux pumps affect drug concentrations in bacterial cells?
A new drug is undergoing Phase II clinical trials. What is the primary objective of this phase?
A new drug is undergoing Phase II clinical trials. What is the primary objective of this phase?
A patient is taking a drug that undergoes enterohepatic recirculation. How does this process most likely affect the drug's half-life and duration of action?
A patient is taking a drug that undergoes enterohepatic recirculation. How does this process most likely affect the drug's half-life and duration of action?
What is the most significant implication of a drug undergoing extensive first-pass metabolism?
What is the most significant implication of a drug undergoing extensive first-pass metabolism?
A drug molecule only binds the allosteric site of a receptor to cause a functional change, what is this interaction called?
A drug molecule only binds the allosteric site of a receptor to cause a functional change, what is this interaction called?
A research team is trying to identify a new drug target using recombinant DNA techniques. Which biological molecule would be MOST appropriate for them to focus on?
A research team is trying to identify a new drug target using recombinant DNA techniques. Which biological molecule would be MOST appropriate for them to focus on?
A drug is designed to resemble the transition state of an enzyme's normal reaction. How does this characteristic affect the drug's interaction with the enzyme?
A drug is designed to resemble the transition state of an enzyme's normal reaction. How does this characteristic affect the drug's interaction with the enzyme?
How does an increase in urine pH affect the renal excretion of a weak base?
How does an increase in urine pH affect the renal excretion of a weak base?
Why is the paracellular pathway particularly significant for drug transport across the capillary endothelium?
Why is the paracellular pathway particularly significant for drug transport across the capillary endothelium?
What is the relationship between glomerular filtration rate (GFR) and renal plasma flow?
What is the relationship between glomerular filtration rate (GFR) and renal plasma flow?
How does the lipophilicity of a drug typically affect its binding to plasma proteins?
How does the lipophilicity of a drug typically affect its binding to plasma proteins?
What is the primary effect of reduced albumin production in a patient with liver cirrhosis on the distribution of a highly protein-bound drug?
What is the primary effect of reduced albumin production in a patient with liver cirrhosis on the distribution of a highly protein-bound drug?
How does enterohepatic recirculation affect the duration of action and clearance of a drug?
How does enterohepatic recirculation affect the duration of action and clearance of a drug?
How does first-pass metabolism influence the oral bioavailability of a drug?
How does first-pass metabolism influence the oral bioavailability of a drug?
What is the functional consequence of a drug being a substrate for Multidrug Resistance Protein (MDR) in the gastrointestinal tract?
What is the functional consequence of a drug being a substrate for Multidrug Resistance Protein (MDR) in the gastrointestinal tract?
During Phase II clinical trials, what is the primary goal regarding the tested drug?
During Phase II clinical trials, what is the primary goal regarding the tested drug?
If a drug binds to the allosteric site of a receptor and reduces the receptor's response to its natural agonist, how is this interaction categorized?
If a drug binds to the allosteric site of a receptor and reduces the receptor's response to its natural agonist, how is this interaction categorized?
How does increased expression of efflux pumps affect the intracellular concentration of drugs in resistant bacteria?
How does increased expression of efflux pumps affect the intracellular concentration of drugs in resistant bacteria?
If a patient with normal renal function takes a drug that is freely filtered at the glomerulus but also actively secreted in the proximal tubule, how would probenecid, a drug that inhibits active secretion, affect the plasma clearance of the first drug?
If a patient with normal renal function takes a drug that is freely filtered at the glomerulus but also actively secreted in the proximal tubule, how would probenecid, a drug that inhibits active secretion, affect the plasma clearance of the first drug?
A drug is designed to bind to a receptor with very high affinity and induce a conformational change that prevents the binding of the endogenous ligand. Which term BEST describes this type of drug?
A drug is designed to bind to a receptor with very high affinity and induce a conformational change that prevents the binding of the endogenous ligand. Which term BEST describes this type of drug?
A weak acid with a pKa of 4.5 is administered to a patient. If the pH of the patient's urine is 6.5, what can be predicted about the drug's excretion?
A weak acid with a pKa of 4.5 is administered to a patient. If the pH of the patient's urine is 6.5, what can be predicted about the drug's excretion?
Which of the following BEST describes the primary mechanism by which first-pass metabolism affects drug bioavailability?
Which of the following BEST describes the primary mechanism by which first-pass metabolism affects drug bioavailability?
How does the presence of a drug-drug interaction causing displacement of a highly protein-bound drug MOST likely affect the drug's volume of distribution ($V_d$) and potential for toxicity?
How does the presence of a drug-drug interaction causing displacement of a highly protein-bound drug MOST likely affect the drug's volume of distribution ($V_d$) and potential for toxicity?
A company is developing a new drug and discovers that it is a substrate for P-glycoprotein (P-gp). What effect would they expect to see on the oral bioavailability of this drug?
A company is developing a new drug and discovers that it is a substrate for P-glycoprotein (P-gp). What effect would they expect to see on the oral bioavailability of this drug?
During drug development, a medication is found to have a narrow therapeutic index. What implications does this have for its clinical use regarding dosing and monitoring?
During drug development, a medication is found to have a narrow therapeutic index. What implications does this have for its clinical use regarding dosing and monitoring?
A patient is prescribed a drug that undergoes extensive enterohepatic recirculation. Which of the following adjustments might be necessary due to this pharmacokinetic property?
A patient is prescribed a drug that undergoes extensive enterohepatic recirculation. Which of the following adjustments might be necessary due to this pharmacokinetic property?
In the context of drug discovery, what is the significance of identifying a 'transition state analog' as a potential drug candidate?
In the context of drug discovery, what is the significance of identifying a 'transition state analog' as a potential drug candidate?
How does urinary pH influence the excretion of a weakly acidic drug?
How does urinary pH influence the excretion of a weakly acidic drug?
A patient with normal renal function has a GFR of 120 mL/min. What does this value represent?
A patient with normal renal function has a GFR of 120 mL/min. What does this value represent?
How do transdermal drug delivery systems facilitate relatively constant drug delivery?
How do transdermal drug delivery systems facilitate relatively constant drug delivery?
How does plasma protein binding typically affect the distribution of a drug to extravascular tissues?
How does plasma protein binding typically affect the distribution of a drug to extravascular tissues?
What effect does enterohepatic recirculation typically have on a drug's duration of action?
What effect does enterohepatic recirculation typically have on a drug's duration of action?
How does extensive first-pass metabolism primarily affect the oral bioavailability of a drug?
How does extensive first-pass metabolism primarily affect the oral bioavailability of a drug?
What is the primary function of Multidrug Resistance Protein (MDR) transporters in the gastrointestinal tract?
What is the primary function of Multidrug Resistance Protein (MDR) transporters in the gastrointestinal tract?
A drug binds to a receptor at a location separate from the agonist binding site and enhances the receptor's response to the agonist. How is this interaction categorized?
A drug binds to a receptor at a location separate from the agonist binding site and enhances the receptor's response to the agonist. How is this interaction categorized?
Flashcards
Urine pH's influence on weakly basic drug absorption
Urine pH's influence on weakly basic drug absorption
Weakly basic drugs are more ionized in acidic urine, leading to less reabsorption and increased excretion.
Paracellular drug transport
Paracellular drug transport
This type of drug transport uses aqueous space between cells and is most relevant in capillary endothelium.
Glomerular filtration principles
Glomerular filtration principles
Fine sieves allow the glomerular filtration of small molecules (<70 kDa). Glomerular filtration rate (GFR) is ~120 mL/min in adults.
Drug transport by ionization
Drug transport by ionization
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Protein binding's effect on drug distribution
Protein binding's effect on drug distribution
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Enterohepatic recirculation
Enterohepatic recirculation
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Multidrug Resistance Protein (MDR) function
Multidrug Resistance Protein (MDR) function
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Orthosteric (Active) Sites
Orthosteric (Active) Sites
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Phase I drug trials
Phase I drug trials
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Sulfonamide mechanism of action
Sulfonamide mechanism of action
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Glomerular Filtration Rate (GFR)
Glomerular Filtration Rate (GFR)
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Transdermal Drug Absorption
Transdermal Drug Absorption
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First-Pass Metabolism
First-Pass Metabolism
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Investigational New Drug (IND)
Investigational New Drug (IND)
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Transition State Analog
Transition State Analog
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Irreversible Inhibition
Irreversible Inhibition
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Beta-lactamase Resistance
Beta-lactamase Resistance
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Polypharmacy
Polypharmacy
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Polyene Antifungals
Polyene Antifungals
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Urine pH on Drug Excretion
Urine pH on Drug Excretion
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Transdermal Absorption
Transdermal Absorption
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What is Enterohepatic Recirculation?
What is Enterohepatic Recirculation?
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Mode of Action of Penicillins
Mode of Action of Penicillins
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Allosteric Site Modulation
Allosteric Site Modulation
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IND Application
IND Application
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Polypharmacology
Polypharmacology
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Vancomycin Action
Vancomycin Action
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How does Daptomycin function?
How does Daptomycin function?
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Drug membrane transport
Drug membrane transport
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Plasma protein binding
Plasma protein binding
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Allosteric Modulation
Allosteric Modulation
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PABA increase outcome
PABA increase outcome
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Rectal route disadvantages
Rectal route disadvantages
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DNA alkylator targets
DNA alkylator targets
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Non-competitive inhibition
Non-competitive inhibition
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Antagonists
Antagonists
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Urine pH adjust drug excretion
Urine pH adjust drug excretion
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Transdermal drug delivery
Transdermal drug delivery
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First-pass effect
First-pass effect
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MDR Transporters' Drug Action
MDR Transporters' Drug Action
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Sulfonamide Drug Action
Sulfonamide Drug Action
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Beta-Lactamase Enzyme's Effect
Beta-Lactamase Enzyme's Effect
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Polypharmacy Definition
Polypharmacy Definition
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Vancomycin Inhibits Gram + Bacteria
Vancomycin Inhibits Gram + Bacteria
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Increase PABA Outcome
Increase PABA Outcome
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Paracellular transport
Paracellular transport
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Sulfonamide MOA
Sulfonamide MOA
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Polypharmacology Definition
Polypharmacology Definition
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Daptomycin Function
Daptomycin Function
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Effects of Protein Binding
Effects of Protein Binding
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Suicide Inhibition
Suicide Inhibition
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Enzymatic Modification of Drug
Enzymatic Modification of Drug
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Study Notes
- The questions and topics are designed to assist in exam preparation.
pH Influence on Weakly Basic Drug Absorption
- Basic drugs are more ionized in acidic urine and therefore less reabsorbed and more readily excreted.
- For altering urine pH in clinical settings, urine acidifiers like ammonium chloride or urine alkalinizers such as sodium bicarbonate are used.
- Renal excretion of pentobarbital, a weak acid, increases in overdose cases through sodium bicarbonate injections.
Paracellular Drug Transport
- Drugs can cross membranes by diffusing through the aqueous space between cells.
- The paracellular pathway is significant for drug transport in capillary endothelium.
Principles of Filtration at the Glomerulus
- The glomerulus acts as a fine molecular sieve allowing filtration of small molecules (<70 kDa).
- Kidneys receive ~20% of cardiac output.
- Only ~20% of plasma flowing through the kidneys becomes filtrate (urine).
- Normal renal plasma flow is 600 mL/min.
- Glomerular Filtration Rate (GFR) is ~120 mL/min in an adult with normal renal function.
- GFR is the volume of plasma filtered by the kidneys per minute, not the renal flow.
- GFR indicates how much filtrate is removed from the blood each minute, not how much blood passes through the kidneys.
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