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Questions and Answers
What characterizes the distribution of a drug that has central and peripheral compartments?
What characterizes the distribution of a drug that has central and peripheral compartments?
Which statement accurately describes first order elimination kinetics?
Which statement accurately describes first order elimination kinetics?
In a semi-log plot for first order kinetics, what does the graphical representation look like?
In a semi-log plot for first order kinetics, what does the graphical representation look like?
What is true regarding zero order elimination kinetics?
What is true regarding zero order elimination kinetics?
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What does bioavailability refer to in pharmacokinetics?
What does bioavailability refer to in pharmacokinetics?
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What is the bioavailability of drugs administered intravenously?
What is the bioavailability of drugs administered intravenously?
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In a first order elimination process, which equation best describes the relationship between drug concentration and time?
In a first order elimination process, which equation best describes the relationship between drug concentration and time?
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What does the term 'bioavailability' in pharmacokinetics refer to?
What does the term 'bioavailability' in pharmacokinetics refer to?
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In a one-compartment model, what happens to the plasma concentration of a drug when it follows first-order kinetics?
In a one-compartment model, what happens to the plasma concentration of a drug when it follows first-order kinetics?
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How is the elimination rate constant related to the half-life of a drug?
How is the elimination rate constant related to the half-life of a drug?
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What is a key characteristic of a two-compartment model?
What is a key characteristic of a two-compartment model?
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What is the primary principle of pharmacokinetics regarding drug effects?
What is the primary principle of pharmacokinetics regarding drug effects?
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What is the purpose of administering a drug by IV and another route for comparison?
What is the purpose of administering a drug by IV and another route for comparison?
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How is bioavailability generally expressed mathematically?
How is bioavailability generally expressed mathematically?
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What is the percent of a drug remaining in the body after three half-lives?
What is the percent of a drug remaining in the body after three half-lives?
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What does bioavailability indicate when a drug is administered orally?
What does bioavailability indicate when a drug is administered orally?
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What does the half-life of a drug represent?
What does the half-life of a drug represent?
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Which of the following describes the volume of distribution (Vd) of a drug?
Which of the following describes the volume of distribution (Vd) of a drug?
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After four half-lives, what fraction of the drug remains in the body?
After four half-lives, what fraction of the drug remains in the body?
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What formula is used to calculate the half-life of a drug in a one compartment model?
What formula is used to calculate the half-life of a drug in a one compartment model?
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Which statement is true regarding drugs with high volume of distribution?
Which statement is true regarding drugs with high volume of distribution?
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What is a characteristic of half-life when determined graphically?
What is a characteristic of half-life when determined graphically?
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What is the formula used to calculate the fraction of a drug eliminated from the body?
What is the formula used to calculate the fraction of a drug eliminated from the body?
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In the equation Ct = C0 e(-kxt), what does Ct represent?
In the equation Ct = C0 e(-kxt), what does Ct represent?
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Why is bioavailability important in pharmacology?
Why is bioavailability important in pharmacology?
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What does the area under the curve (AUC) indicate in pharmacokinetics?
What does the area under the curve (AUC) indicate in pharmacokinetics?
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What factor may influence the bioavailability of a drug when it is administered orally?
What factor may influence the bioavailability of a drug when it is administered orally?
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Study Notes
Pharmacokinetics Overview
- Pharmacokinetics quantifies relationships among absorption, distribution, and elimination of drugs over time.
- Blood concentration of a drug is directly related to its therapeutic effect, influencing efficacy and safety.
Key Pharmacokinetic Parameters
- Bioavailability (F): Fraction of unchanged drug reaching systemic circulation post-administration; intravenous (IV) drugs have F = 1, others < 1.
- Half-Life (t1/2): Time required for plasma drug concentration to decrease by 50%; determined using ke (elimination rate constant).
- Clearance (CL): Volume of plasma cleared of drug per unit time; inversely related to steady-state concentration.
- Volume of Distribution (Vd): Apparent volume in which drug distributes; large Vd indicates high lipophilicity or low protein binding.
- Elimination Rate Constant (ke): Rate at which drug concentration decreases over time; key in predicting drug clearance.
- Steady State Concentration (Css): Stable level of drug in the body during continuous administration; reached after 4-5 half-lives.
Compartment Models
- One-Compartment Model: Assumes rapid equilibrium between plasma and tissues; characterized by linear decline in plasma concentration in semi-log plots.
- Two-Compartment Model: Drug distributes between a central and a peripheral compartment; displays a biphasic decline in plasma concentration.
Kinetics
- First Order Kinetics: Rate of drug elimination is proportional to its concentration; results in a linear semi-log plot.
- Zero Order Kinetics: Constant amount of drug eliminated regardless of concentration; occurs when elimination pathways are saturated.
Relationship Between Parameters
- Clearance, half-life, volume of distribution, and plasma concentration are interrelated, affecting drug dosing and frequency.
- Decreases in clearance will double Css if dosing rate remains constant.
Calculating Pharmacokinetic Parameters
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Formulas:
- Half-Life: t1/2 = 0.693 / ke
- Clearance: CL = Dose / Css
- Bioavailability: F = AUC (oral) / AUC (IV)
- Volume of Distribution calculation: Vd = Dose / (Css x ke).
Practical Applications
- Administer IV loading doses considering volume of distribution to achieve desired Css levels quickly.
- Importance of bioavailability assessment for effective drug formulation comparison and understanding absorption variability.
Additional Information
- Four half-lives rule: After 4 half-lives, a drug is considered essentially eliminated, retaining only 6% in the body.
- Knowledge of pharmacokinetics is crucial for appropriate drug therapy management, individualization of dose regimens, and optimization of therapeutic outcomes.
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Description
This quiz covers the key concepts and parameters in pharmacokinetics, including bioavailability, half-life, clearance, and volume of distribution. Understanding these parameters is essential for evaluating drug efficacy and safety. Test your knowledge of how drugs are absorbed, distributed, and eliminated from the body.