Podcast
Questions and Answers
What is the primary factor determining drug distribution to peripheral compartments?
What is the primary factor determining drug distribution to peripheral compartments?
Which of the following compartments has the largest volume of water in the body?
Which of the following compartments has the largest volume of water in the body?
What is the primary reason why some drugs are restricted to the extracellular fluid?
What is the primary reason why some drugs are restricted to the extracellular fluid?
Drugs that can easily penetrate the blood-brain barrier are typically characterized by:
Drugs that can easily penetrate the blood-brain barrier are typically characterized by:
Signup and view all the answers
Which of the following processes can lead to increased drug concentration within cells?
Which of the following processes can lead to increased drug concentration within cells?
Signup and view all the answers
What is the relationship between drug distribution and drug action?
What is the relationship between drug distribution and drug action?
Signup and view all the answers
What is the main reason why drug molecules exist in both bound and free forms in the body?
What is the main reason why drug molecules exist in both bound and free forms in the body?
Signup and view all the answers
How does the interstitial fluid contribute to drug distribution?
How does the interstitial fluid contribute to drug distribution?
Signup and view all the answers
What is a major factor affecting the distribution of large molecules like heparin?
What is a major factor affecting the distribution of large molecules like heparin?
Signup and view all the answers
Which of the following tissues receives the slowest blood flow?
Which of the following tissues receives the slowest blood flow?
Signup and view all the answers
What is the primary function of plasma protein binding of drugs?
What is the primary function of plasma protein binding of drugs?
Signup and view all the answers
Which of the following factors can significantly influence drug distribution?
Which of the following factors can significantly influence drug distribution?
Signup and view all the answers
Which of the following statements is TRUE regarding drug distribution?
Which of the following statements is TRUE regarding drug distribution?
Signup and view all the answers
Which of the following drugs are most likely to bind to albumin?
Which of the following drugs are most likely to bind to albumin?
Signup and view all the answers
What is the clinical significance of a drug having a high binding affinity to plasma proteins?
What is the clinical significance of a drug having a high binding affinity to plasma proteins?
Signup and view all the answers
Which of the following statements is TRUE regarding drug interactions due to plasma protein binding?
Which of the following statements is TRUE regarding drug interactions due to plasma protein binding?
Signup and view all the answers
Why is hemodialysis less effective in treating drug poisoning for drugs with a large volume of distribution (Vd)?
Why is hemodialysis less effective in treating drug poisoning for drugs with a large volume of distribution (Vd)?
Signup and view all the answers
Which of the following factors influences the volume of distribution (Vd) of a drug?
Which of the following factors influences the volume of distribution (Vd) of a drug?
Signup and view all the answers
Which of the following is an example of a drug interaction caused by displacement from plasma protein binding sites?
Which of the following is an example of a drug interaction caused by displacement from plasma protein binding sites?
Signup and view all the answers
What happens to the concentration of free drug in the plasma when a patient has hypoalbuminemia?
What happens to the concentration of free drug in the plasma when a patient has hypoalbuminemia?
Signup and view all the answers
Which of the following statements is FALSE regarding the volume of distribution (Vd)?
Which of the following statements is FALSE regarding the volume of distribution (Vd)?
Signup and view all the answers
Which of the following drugs accumulates in liver tissue?
Which of the following drugs accumulates in liver tissue?
Signup and view all the answers
Which of the following statements accurately describes the blood-brain barrier (BBB)?
Which of the following statements accurately describes the blood-brain barrier (BBB)?
Signup and view all the answers
Which of the following factors can disrupt the integrity of the blood-brain barrier?
Which of the following factors can disrupt the integrity of the blood-brain barrier?
Signup and view all the answers
What is the primary reason why water-soluble drugs have difficulty crossing the blood-brain barrier?
What is the primary reason why water-soluble drugs have difficulty crossing the blood-brain barrier?
Signup and view all the answers
What is the likely consequence of a drug having a high volume of distribution (Vd)?
What is the likely consequence of a drug having a high volume of distribution (Vd)?
Signup and view all the answers
A patient with a high volume of distribution (Vd) for a particular drug would likely require:
A patient with a high volume of distribution (Vd) for a particular drug would likely require:
Signup and view all the answers
Which of the following statements accurately describes the placental barrier?
Which of the following statements accurately describes the placental barrier?
Signup and view all the answers
Which of the following factors can increase the bioavailability of an oral drug?
Which of the following factors can increase the bioavailability of an oral drug?
Signup and view all the answers
Flashcards
Drug Distribution
Drug Distribution
The movement of drug from blood to tissues for action.
Central Compartment
Central Compartment
The bloodstream where drugs are initially found before distribution.
Peripheral Compartments
Peripheral Compartments
Tissues and organs where drugs travel after the bloodstream.
Lipid Solubility
Lipid Solubility
Signup and view all the flashcards
Blood-Brain Barrier (BBB)
Blood-Brain Barrier (BBB)
Signup and view all the flashcards
Ion Trapping
Ion Trapping
Signup and view all the flashcards
Active Transport
Active Transport
Signup and view all the flashcards
Total Body Water Distribution
Total Body Water Distribution
Signup and view all the flashcards
Ionization (pKa)
Ionization (pKa)
Signup and view all the flashcards
Blood Flow Distribution
Blood Flow Distribution
Signup and view all the flashcards
Free vs Bound Drug
Free vs Bound Drug
Signup and view all the flashcards
Plasma Protein Binding
Plasma Protein Binding
Signup and view all the flashcards
Factors Affecting Drug Distribution
Factors Affecting Drug Distribution
Signup and view all the flashcards
Acidic Drugs
Acidic Drugs
Signup and view all the flashcards
Basic Drugs
Basic Drugs
Signup and view all the flashcards
Volume of Distribution (Vd)
Volume of Distribution (Vd)
Signup and view all the flashcards
Drug Displacement Interaction
Drug Displacement Interaction
Signup and view all the flashcards
Hypoalbuminemia
Hypoalbuminemia
Signup and view all the flashcards
Significance of Protein Binding
Significance of Protein Binding
Signup and view all the flashcards
Free Drug Action
Free Drug Action
Signup and view all the flashcards
Tissue Drug Accumulation
Tissue Drug Accumulation
Signup and view all the flashcards
Digoxin
Digoxin
Signup and view all the flashcards
Chloroquine
Chloroquine
Signup and view all the flashcards
Iodine
Iodine
Signup and view all the flashcards
Tetracycline
Tetracycline
Signup and view all the flashcards
Blood-Brain Barrier Disruption
Blood-Brain Barrier Disruption
Signup and view all the flashcards
Placental Barrier
Placental Barrier
Signup and view all the flashcards
Water-Soluble Drug Limitations
Water-Soluble Drug Limitations
Signup and view all the flashcards
Study Notes
Drug Distribution
-
Drug distribution is the key factor in the onset of drug action. It involves the movement of a drug from the bloodstream to tissues.
-
Drugs are distributed to organs and tissues via the bloodstream, diffusing into interstitial fluid and cells.
-
Most drugs are not evenly distributed throughout the body's water content. Some drugs are limited to the extracellular fluid or plasma.
-
Drugs with high lipid solubility easily diffuse through cell membranes.
-
Other drugs concentrate within cells due to ion trapping.
-
Active transport mechanisms also move drugs into cells.
Drug Distribution and Body Water
-
Water in the body is divided into compartments: intravascular, interstitial, and intracellular.
-
The total body water is approximately 70% of total body weight in healthy subjects.
-
Extracellular fluid makes up about 25% of the total body water, while intracellular fluid constitutes about 45%.
Factors Affecting Drug Distribution
-
Lipid solubility: Highly lipophilic drugs readily cross the blood-brain barrier (BBB).
-
Polar and ionized drugs often cannot cross the BBB as easily.
-
Ionization (pKa): Molecular size influences distribution, with extremely large molecules like heparin often confined to the plasma.
-
Organ blood flow: High blood flow to organs like the brain, heart, liver, and kidneys leads to rapid distribution and faster onset of action. Distribution is slower in tissues with lower blood flow.
-
Binding to plasma and tissue proteins: Drugs can bind reversibly to proteins in plasma or tissues, altering the effective concentration in target areas. Active transport and drug metabolism are also relevant.
Drugs in Vascular Space
-
Drugs exist in two forms in the blood: free and bound.
-
Free drugs are active, diffusible, and available for metabolism and excretion.
-
Bound drugs are mainly bound to albumin, acting as a reservoir.
-
Bound drugs are non-diffusible and thus not usable for metabolism or excretion.
Plasma Protein Binding
-
Drug binding to plasma proteins is reversible (D + P ⇌ DP).
-
The unbound/free drug is the pharmaceutically active form.
-
Binding sites on plasma proteins become saturated with higher drug concentrations.
-
Highly bound drugs stay in the blood for longer which results in a lower therapeutic activity.
-
Acidic drugs often bind to albumin.
-
Basic drugs frequently bind to α1-glycoprotein.
Significance of Plasma Protein Binding
-
Highly bound drugs persist longer in the body, lowering therapeutic activity and making them less accessible to dialysis.
-
Hypoalbuminemia (low albumin) leads to a higher concentration of free drug, potentially increasing the risk of side effects.
Clinically Important Drug Interactions Due to Displacement
-
Drugs can displace each other from plasma protein binding sites.
-
Acidic drugs do not usually displace basic drugs, and vice versa.
-
Drug interactions can affect the efficacy or toxicity of other drugs.
Volume of Distribution (Vd)
-
Vd is a measure of the apparent volume in the body that would be needed to contain the total amount of drug at a plasma concentration equal to the concentration in the body.
-
Vd is a critical pharmacokinetic parameter.
-
High Vd indicates extensive distribution throughout the body.
-
Lower Vd indicates more drug is retained in the blood, affecting the efficacy and potential toxicity of the drug.
Clinical Significance of Vd
-
A large volume of distribution suggests that the drug is distributed extensively throughout the body, reducing the efficacy of dialysis in cases of drug poisoning.
-
The volume of distribution correlates to the drug's binding capacity and other properties.
Drugs Accumulated in Tissues
- Certain drugs (e.g., digoxin, chloroquine, iodine, chloroquine, tetracycline) accumulate in specific tissues, and these tissues' accumulation can increase the volume of distribution.
Barriers to Drug Distribution
-
The blood-brain barrier (BBB) and placental barrier limit drug distribution.
-
Tight junctions of endothelial cells limit permeability.
-
Inflammation can decrease this barrier function.
-
Lipid-soluble drugs cross the barriers more easily than water-soluble or protein-bound drugs.
Placental Barrier
-
The placental barrier allows free passage for lipid-soluble drugs.
-
The barrier for water-soluble or protein-bound drugs is not easily crossed.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
Related Documents
Description
Explore the essential concepts of drug distribution in the human body through this quiz. Understand how drugs move from the bloodstream to various tissues and the factors influencing this process. Delve into the significance of body water compartments and the impact of drug solubility on distribution.