Podcast
Questions and Answers
What is the approximate volume of plasma in the body?
What is the approximate volume of plasma in the body?
- 29 L
- 12 L
- 3 L (correct)
- 9 L
What does a small volume of distribution (Vd) indicate about a drug's distribution?
What does a small volume of distribution (Vd) indicate about a drug's distribution?
- The drug readily crosses the blood-brain barrier.
- The drug has a high affinity for fat tissues.
- The drug is mainly confined to the vascular compartment. (correct)
- The drug is extensively distributed into tissues.
A drug with a large volume of distribution (Vd) is MOST likely to:
A drug with a large volume of distribution (Vd) is MOST likely to:
- Have extensive tissue distribution. (correct)
- Be confined to the vascular compartment.
- Be rapidly cleared by the kidneys.
- Undergo efficient hemodialysis in case of toxicity.
In cases of drug toxicity, when is hemodialysis MOST effective?
In cases of drug toxicity, when is hemodialysis MOST effective?
Which plasma protein is MOST significant for drug binding?
Which plasma protein is MOST significant for drug binding?
Which of the following conditions can lead to an increase in the free concentration of a drug in the body?
Which of the following conditions can lead to an increase in the free concentration of a drug in the body?
Which statement accurately describes drugs bound to plasma proteins?
Which statement accurately describes drugs bound to plasma proteins?
A drug is 99% bound to plasma proteins. Displacement of the drug by another agent increases the free fraction by 1%. What is the potential consequence?
A drug is 99% bound to plasma proteins. Displacement of the drug by another agent increases the free fraction by 1%. What is the potential consequence?
Why are non-ionized, highly lipid-soluble drugs able to cross the blood-brain barrier (BBB)?
Why are non-ionized, highly lipid-soluble drugs able to cross the blood-brain barrier (BBB)?
What is a potential consequence of drugs crossing the placental barrier?
What is a potential consequence of drugs crossing the placental barrier?
Why do basic drugs tend to accumulate in breast milk?
Why do basic drugs tend to accumulate in breast milk?
What is the initial distribution pattern of thiopental due to its high lipid solubility and high blood flow to the brain?
What is the initial distribution pattern of thiopental due to its high lipid solubility and high blood flow to the brain?
Why does the duration of action of thiopental depend more on redistribution than on metabolism or excretion?
Why does the duration of action of thiopental depend more on redistribution than on metabolism or excretion?
What is the primary site of drug metabolism (biotransformation) in the body?
What is the primary site of drug metabolism (biotransformation) in the body?
What is the MOST common consequence of biotransformation?
What is the MOST common consequence of biotransformation?
Which of the following is an example of a drug being metabolized into a toxic metabolite?
Which of the following is an example of a drug being metabolized into a toxic metabolite?
What term defines the volume of body fluids at which a drug appears to be distributed?
What term defines the volume of body fluids at which a drug appears to be distributed?
Which characteristic is typically associated with drugs that have a volume of distribution exceeding 40 liters?
Which characteristic is typically associated with drugs that have a volume of distribution exceeding 40 liters?
What is a primary clinical significance of understanding a drug's volume of distribution (Vd)?
What is a primary clinical significance of understanding a drug's volume of distribution (Vd)?
How does hypoalbuminemia affect the distribution of a drug that is normally highly protein-bound?
How does hypoalbuminemia affect the distribution of a drug that is normally highly protein-bound?
A drug is described as having 'redistribution'. What does this mean in a pharmacokinetic context?
A drug is described as having 'redistribution'. What does this mean in a pharmacokinetic context?
Which of the following statements regarding the passage of drugs into breast milk is correct?
Which of the following statements regarding the passage of drugs into breast milk is correct?
A patient with malnutrition has low serum albumin. They are given a drug that is normally 95% bound to albumin. What effect will malnutrition likely have on the drug's free concentration and potential for toxicity?
A patient with malnutrition has low serum albumin. They are given a drug that is normally 95% bound to albumin. What effect will malnutrition likely have on the drug's free concentration and potential for toxicity?
A drug is known to induce teratogenicity. What route of exposure is its MOST likely cause for its related adverse developmental effects?
A drug is known to induce teratogenicity. What route of exposure is its MOST likely cause for its related adverse developmental effects?
After intravenous administration, a highly lipophilic drug rapidly enters the brain, producing a short period of anesthesia. Over time, consciousness is regained, even though plasma concentrations of the drug remain high. What is the MOST likely explanation for this phenomenon?
After intravenous administration, a highly lipophilic drug rapidly enters the brain, producing a short period of anesthesia. Over time, consciousness is regained, even though plasma concentrations of the drug remain high. What is the MOST likely explanation for this phenomenon?
A patient is taking warfarin, which is 99% bound to albumin in plasma. A second drug is administered that displaces warfarin from albumin, increasing the free fraction of warfarin from 1% to 2%. What is the expected change in warfarin's effect, assuming no other factors are changed?
A patient is taking warfarin, which is 99% bound to albumin in plasma. A second drug is administered that displaces warfarin from albumin, increasing the free fraction of warfarin from 1% to 2%. What is the expected change in warfarin's effect, assuming no other factors are changed?
A researcher is studying a new drug and finds that it has a very high affinity for plasma proteins. Which of the following is a likely consequence of this high affinity?
A researcher is studying a new drug and finds that it has a very high affinity for plasma proteins. Which of the following is a likely consequence of this high affinity?
A drug with a very large volume of distribution is unlikely to be effectively removed from the body during hemodialysis because:
A drug with a very large volume of distribution is unlikely to be effectively removed from the body during hemodialysis because:
A drug that undergoes first-pass metabolism is given intravenously instead of orally. Which of the following pharmacokinetic parameters is MOST likely to be significantly different?
A drug that undergoes first-pass metabolism is given intravenously instead of orally. Which of the following pharmacokinetic parameters is MOST likely to be significantly different?
A drug is known to be a substrate of P-glycoprotein (P-gp). Which of the following effects would you expect from a P-gp inhibitor?
A drug is known to be a substrate of P-glycoprotein (P-gp). Which of the following effects would you expect from a P-gp inhibitor?
Considering that only the unbound fraction of a drug is able to exert a pharmacological effect, which scenario would lead to a SUPRISINGLY greater-than-expected effect of a drug? NOTE that this is something that would be hard to predict without actually seeing it happen.
Considering that only the unbound fraction of a drug is able to exert a pharmacological effect, which scenario would lead to a SUPRISINGLY greater-than-expected effect of a drug? NOTE that this is something that would be hard to predict without actually seeing it happen.
A drug is known to undergo significant first-pass metabolism. If the drug is administered intravenously instead of orally, how would you MOST expect the volume of distribution to change (if at all - assume distribution to tissues is related to the amount of drug in the systemic circulation)?
A drug is known to undergo significant first-pass metabolism. If the drug is administered intravenously instead of orally, how would you MOST expect the volume of distribution to change (if at all - assume distribution to tissues is related to the amount of drug in the systemic circulation)?
Which of the following drugs would be MOST readily cleared by hemodialysis?
Which of the following drugs would be MOST readily cleared by hemodialysis?
A new drug is developed that is actively transported into cells via a specific transporter protein found in various tissues, including the brain, liver, and kidneys. One potential safety concern is 'oversaturation' of this transporter. Which of the following could occur due to transporter saturation?
A new drug is developed that is actively transported into cells via a specific transporter protein found in various tissues, including the brain, liver, and kidneys. One potential safety concern is 'oversaturation' of this transporter. Which of the following could occur due to transporter saturation?
Warfarin is a drug with a narrow therapeutic index and is highly bound to albumin. A patient stabilized on warfarin develops a severe infection and is prescribed a sulfonamide antibiotic, which is also highly albumin-bound and known to displace warfarin. In this scenario, what change would we expect?
Warfarin is a drug with a narrow therapeutic index and is highly bound to albumin. A patient stabilized on warfarin develops a severe infection and is prescribed a sulfonamide antibiotic, which is also highly albumin-bound and known to displace warfarin. In this scenario, what change would we expect?
A physician prescribes Drug X, a weak base with a pKa of 8.0, to a nursing mother. Drug X distributes into the breast milk. Assuming the pH of plasma is 7.4 and the pH of breast milk is 7.0, which of the following statements BEST describes the distribution of Drug X?
A physician prescribes Drug X, a weak base with a pKa of 8.0, to a nursing mother. Drug X distributes into the breast milk. Assuming the pH of plasma is 7.4 and the pH of breast milk is 7.0, which of the following statements BEST describes the distribution of Drug X?
A patient with chronic kidney disease has significantly reduced albumin levels. They require treatment with a drug that is normally highly protein-bound. What potential adjustment to the drug regimen might be necessary?
A patient with chronic kidney disease has significantly reduced albumin levels. They require treatment with a drug that is normally highly protein-bound. What potential adjustment to the drug regimen might be necessary?
A study shows that a new drug, primarily distributed in the extracellular fluid (ECF), has a volume of distribution of approximately 14 liters in a 70 kg individual. Which of the following BEST describes the drug's distribution characteristics?
A study shows that a new drug, primarily distributed in the extracellular fluid (ECF), has a volume of distribution of approximately 14 liters in a 70 kg individual. Which of the following BEST describes the drug's distribution characteristics?
A patient is taking a drug that induces CYP3A4 enzymes. The patient begins taking another drug that is metabolized by CYP3A4. How would you MOST expect the second drug to be affected?
A patient is taking a drug that induces CYP3A4 enzymes. The patient begins taking another drug that is metabolized by CYP3A4. How would you MOST expect the second drug to be affected?
Flashcards
What is drug distribution?
What is drug distribution?
The process by which a drug reversibly leaves the bloodstream and enters the tissues of the body.
What is the apparent volume of distribution (Vd)?
What is the apparent volume of distribution (Vd)?
The theoretical volume that would be necessary to contain the total amount of an administered drug at the same concentration that it is observed in the plasma.
Why estimate site of drug distribution from Vd?
Why estimate site of drug distribution from Vd?
Estimate location where a drug is distributed in the body.
What does a small Vd indicate?
What does a small Vd indicate?
Signup and view all the flashcards
What does a Large Vd indicate?
What does a Large Vd indicate?
Signup and view all the flashcards
Why calculate the total amount of drug?
Why calculate the total amount of drug?
Signup and view all the flashcards
When is hemodialysis useful?
When is hemodialysis useful?
Signup and view all the flashcards
What are Plasma proteins?
What are Plasma proteins?
Signup and view all the flashcards
What is Albumin?
What is Albumin?
Signup and view all the flashcards
What is Hypoalbuminaemia?
What is Hypoalbuminaemia?
Signup and view all the flashcards
List Criteria of drugs bound to plasma protein (4 NOT):
List Criteria of drugs bound to plasma protein (4 NOT):
Signup and view all the flashcards
Give an example of high plasma protein binding?
Give an example of high plasma protein binding?
Signup and view all the flashcards
What can result from displacement by other drugs?
What can result from displacement by other drugs?
Signup and view all the flashcards
Passage across what?
Passage across what?
Signup and view all the flashcards
Passage to what across placental barrier?
Passage to what across placental barrier?
Signup and view all the flashcards
What can Drugs that pass placental barrier cause?
What can Drugs that pass placental barrier cause?
Signup and view all the flashcards
What is passage of drugs through?
What is passage of drugs through?
Signup and view all the flashcards
Redistribution of which drugs?
Redistribution of which drugs?
Signup and view all the flashcards
Importance of what?
Importance of what?
Signup and view all the flashcards
What is BIOTRANSFORMATION (METABOLISM)?
What is BIOTRANSFORMATION (METABOLISM)?
Signup and view all the flashcards
What are the sites of metabolism?
What are the sites of metabolism?
Signup and view all the flashcards
First consequence of biotransformation?
First consequence of biotransformation?
Signup and view all the flashcards
Second consequence of biotransformation?
Second consequence of biotransformation?
Signup and view all the flashcards
Third consequence of biotransformation?
Third consequence of biotransformation?
Signup and view all the flashcards
Forth consequence of biotransformation?
Forth consequence of biotransformation?
Signup and view all the flashcards
What volume of distribution?
What volume of distribution?
Signup and view all the flashcards
Study Notes
- General pharmacology focuses on pharmacokinetics (2).
Distribution
- Drugs mainly distribute throughout body fluids.
- Plasma volume is 3L.
- Interstitial fluid volume is 9L.
- Intracellular fluid volume is 29L.
- Apparent Volume of distribution (Vd) is the volume of body fluids at which the drug is distributed.
Clinical Significance of Vd
- Vd estimates the site of drug distribution.
- Drugs with small Vd are confined to the vascular compartment, resulting in minimal tissue distribution.
- Drugs with large Vd have extensive tissue distribution intracellularly.
- Vd calculates the total amount of drug in the body using the formula: Vd = total amount of drug / plasma concentration.
- In toxicity cases, hemodialysis is helpful for drugs with small Vd but less significant for drugs with large Vd.
Plasma Proteins Binding
- Drugs may bind to plasma proteins upon entering the bloodstream.
- Albumin is the most crucial plasma protein for drug binding.
- Hypoalbuminemia (e.g., in starvation or malnutrition) increases the free drug concentration, potentially changing a therapeutic dose to a toxic one.
- Drugs bound to plasma proteins are not active, as only the free part produces pharmacological effects
- Drugs bound to plasma proteins are:
- Not diffusible, decreasing distribution to tissues
- Not metabolized, decreasing uptake by liver cells which prolongs the drug effect
- Not excreted, decreasing renal filtration which prolongs the drug effect
- Some drugs exhibit high plasma protein binding, such as warfarin (99%), an oral anticoagulant.
- Only the free part of a drug is pharmacologically active; only 1% in the case of warfarin.
- Displacing even 1% of a highly bound drug can lead to toxicity
- Exercise caution because drugs with high affinity for plasma protein binding, like aspirin, can displace other drugs like warfarin.
Distribution to Specialized Areas
- Passage across the blood-brain barrier (BBB).
- Non-ionized, highly lipid-soluble drugs can pass through the BBB and affect the CNS.
- Passage to the fetus across the placental barrier:
- Non ionized, lipid-soluble drugs can pass through the placental barrier and affect the fetus.
- Drugs crossing the placental barrier can cause teratogenicity, for example, phenytoin.
- Passage of drugs through breast milk:
- Milk has a more acidic pH than plasma; therefore, basic drugs ionize and accumulate in milk, a process known as ion trapping.
- First-generation antihistamines can sedate a lactating baby, and morphine can cause addiction.
Redistribution of Drugs
- Highly lipid-soluble drugs, such as thiopental, can undergo redistribution.
- Initially, thiopental accumulates in the brain (due to high lipid solubility and blood flow) and then redistributes to poorly perfused adipose tissue.
- Duration depends on the rate of redistribution rather than metabolism or excretion.
- Thiopental acts as an ultrashort-acting anesthetic because of redistribution.
Biotransformation (Metabolism)
- The liver is the primary site of drug metabolism.
- Other organs, such as the kidneys and lungs, also contribute.
- Active drugs can be inactivated.
- Active drugs can be transformed to produce active metabolites.
- Active drugs can be transformed to produce toxic metabolites, such as paracetamol.
- Inactive drugs can be activated (i.e., pro-drugs).
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.