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Questions and Answers
What is a characteristic of drugs that demonstrate first-order kinetics?
What is a characteristic of drugs that demonstrate first-order kinetics?
What is the term for the rate of elimination that is constant regardless of concentration?
What is the term for the rate of elimination that is constant regardless of concentration?
What is the typical pattern of concentration decrease for drugs that demonstrate zero-order elimination?
What is the typical pattern of concentration decrease for drugs that demonstrate zero-order elimination?
What is the purpose of a two-compartment model in pharmacokinetics?
What is the purpose of a two-compartment model in pharmacokinetics?
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What is a characteristic of the elimination phase of a first-order drug when plotted on a logarithmic axis?
What is a characteristic of the elimination phase of a first-order drug when plotted on a logarithmic axis?
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What is the term for the time it takes for the concentration of a drug to decrease by 50%?
What is the term for the time it takes for the concentration of a drug to decrease by 50%?
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What is the characteristic of drugs with first-order kinetics?
What is the characteristic of drugs with first-order kinetics?
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What is the characteristic of zero-order elimination?
What is the characteristic of zero-order elimination?
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What is the initial curvilinear portion of the serum concentration-time curve representing?
What is the initial curvilinear portion of the serum concentration-time curve representing?
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What is the primary function of the Food and Drug Administration (FDA) in the United States?
What is the primary function of the Food and Drug Administration (FDA) in the United States?
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How is the elimination half-life typically measured?
How is the elimination half-life typically measured?
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What type of elimination is characterized by a constant rate of elimination, regardless of concentration?
What type of elimination is characterized by a constant rate of elimination, regardless of concentration?
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What is the goal of rational molecular design or screening?
What is the goal of rational molecular design or screening?
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What is a prerequisite for a new drug to be approved for regular therapeutic use in humans?
What is a prerequisite for a new drug to be approved for regular therapeutic use in humans?
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What is the characteristic of 'me-too' drugs?
What is the characteristic of 'me-too' drugs?
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What is the purpose of constructing accurate mathematical models in pharmacokinetics?
What is the purpose of constructing accurate mathematical models in pharmacokinetics?
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What is the significance of a drug being distributed to only one compartment?
What is the significance of a drug being distributed to only one compartment?
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What is the significance of the linear portion of the serum concentration-time curve?
What is the significance of the linear portion of the serum concentration-time curve?
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Study Notes
Drug Elimination
- Drugs with first-order elimination have a constant half-life of elimination, regardless of the amount of drug in the body.
- The concentration of a first-order elimination drug in the blood decreases by 50% for every half-life.
- Most drugs in clinical use demonstrate first-order kinetics.
- Zero-order elimination involves a constant rate of elimination, regardless of concentration.
- Zero-order elimination drugs do not have a constant half-life, and their concentrations in plasma decrease in a linear fashion over time.
Pharmacokinetic Models
- A two-compartment model is used to simulate the distribution and elimination phases of a drug.
- The two compartments consist of the blood and the extravascular tissues.
- Each phase has a characteristic half-life: 1/2a for the first phase, and 1/2β for the second phase.
- When concentration is plotted on a logarithmic axis, the elimination phase for a first-order drug is a straight line.
Distribution Models
- Some drugs behave as if they were distributed to only 1 compartment (e.g., if they are restricted to the vascular compartment).
- Others have more complex distributions that require more than 2 compartments for accurate mathematical models.
Drug Development and Regulation
- The sale and use of drugs are regulated in almost all countries by governmental agencies, such as the FDA in the United States.
- New drugs are developed in industrial or academic laboratories, and must undergo a series of animal and experimental human studies (clinical trials) before being approved for therapeutic use.
- New drugs can emerge from a variety of sources, including the identification of a new target for a disease.
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Description
Understand the concepts of first-order and zero-order elimination in pharmacokinetics, including their characteristics and effects on drug concentration in the body.