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Questions and Answers
Drug elimination is the process of removing a drug from the body. What are the major routes of drug elimination?
Drug elimination is the process of removing a drug from the body. What are the major routes of drug elimination?
What is the term used to describe the theoretical volume of plasma from which a drug is completely removed in unit time?
What is the term used to describe the theoretical volume of plasma from which a drug is completely removed in unit time?
Clearance (CL)
The ______ filtration rate (GFR) is a measure of the kidneys' ability to filter waste products from the blood.
The ______ filtration rate (GFR) is a measure of the kidneys' ability to filter waste products from the blood.
glomerular
Tubular reabsorption is a process by which drugs are actively transported back into the bloodstream from the tubules in the kidneys.
Tubular reabsorption is a process by which drugs are actively transported back into the bloodstream from the tubules in the kidneys.
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Tubular secretion is the process by which drugs are passed from the bloodstream into the tubules of the kidney.
Tubular secretion is the process by which drugs are passed from the bloodstream into the tubules of the kidney.
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Which of these is an example of a drug that is often eliminated via the lungs?
Which of these is an example of a drug that is often eliminated via the lungs?
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What is the difference between first-order and zero-order kinetics in drug elimination?
What is the difference between first-order and zero-order kinetics in drug elimination?
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The time it takes for the plasma concentration of a drug to decrease by half is known as its ______.
The time it takes for the plasma concentration of a drug to decrease by half is known as its ______.
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What is the term used to describe the stable concentration of a drug in the body after repeated doses?
What is the term used to describe the stable concentration of a drug in the body after repeated doses?
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A loading dose aims to rapidly achieve the therapeutic concentration of a drug.
A loading dose aims to rapidly achieve the therapeutic concentration of a drug.
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What is the purpose of a maintenance dose?
What is the purpose of a maintenance dose?
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Which of the following is NOT an advantage of using a drug delivery system that prolongs drug action?
Which of the following is NOT an advantage of using a drug delivery system that prolongs drug action?
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Which of these is a method to prolong drug action in the body?
Which of these is a method to prolong drug action in the body?
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Study Notes
Drug Elimination
- Drug elimination is the process of removing a drug from the body
Objectives
- Understand drug clearance by various organs (kidney, liver, etc.)
- Compare and contrast first-order and zero-order kinetics
- Calculate loading dose, maintenance dose, and steady-state concentration
- Identify methods for prolonging drug action
Excretion
- Excretion is the passage of absorbed drugs and their metabolites out of the body
- Drugs and metabolites are excreted through:
- Urine (primarily via the kidney)
- Feces
- Exhaled air
- Saliva
- Sweat
- Milk
- Specific examples of drug excretion include:
- Erythromycin and ampicillin (via feces)
- General anesthetics and alcohol (via exhaled air)
- Lithium, potassium iodide (via saliva and sweat)
- Amphetamine and chloramphenicol (via milk)
Renal Excretion
- Renal excretion involves three main processes:
- Glomerular filtration: Drugs pass through the glomerular capillaries into the filtrate.
- Tubular reabsorption: Drugs are reabsorbed from the filtrate back into the blood.
- Tubular secretion: Drugs move from the blood into the filtrate
- Net renal excretion = (glomerular filtration + tubular secretion) - tubular reabsorption
Renal Excretion (Glomerular Filtration)
- Glomerular capillaries have large pores
- Drug filtration depends on plasma protein binding and renal blood flow
- Glomerular filtration rate (GFR) is typically 120 mL/min and decreases with age and in renal failure
Renal Excretion (Tubular Reabsorption)
- Primarily passive diffusion
- Influenced by lipid solubility and ionization
- Lipid-soluble, unionized drugs are readily reabsorbed
- Clinical significance in poisoning
- Urine alkalization for barbiturates poisoning (acidic drugs)
- Urine acidification for morphine poisoning (basic drugs)
Renal Excretion (Tubular Secretion)
- Active transport process
- Primarily occurs in the proximal tubules.
- Important for removing protein-bound drugs
Kinetics of Elimination
- Clearance (CL): Theoretical volume of plasma from which a drug is completely removed per unit time
- CL = Rate of elimination / plasma concentration
First-Order Kinetics
- The rate of elimination is directly proportional to drug concentration.
- Constant fraction of drug is eliminated per unit time.
- Clearance remains constant
- Follows an exponential decay curve
Zero-Order Kinetics
- The rate of elimination is constant, irrespective of drug concentration.
- A constant amount of drug is eliminated per unit time.
- Clearance decreases with increasing concentration
- Follows a linear decline
Plasma Half-Life
- Time required for the plasma concentration of a drug to decrease by half
- Multiple half-lives (4-5) result in near-complete drug elimination
Steady-State Plasma Concentration (Cpss)
- Achieved after repeated dosing when elimination equals input.
- Cpss = Dose rate / Clearance
Loading Dose
- Used to quickly achieve target concentration.
- Loading dose = (Vd) x (desired plasma concentration) / bioavailability
Maintenance Dose
- Maintains steady-state plasma concentration
- Dosing rate = (CL) x (desired plasma concentration) / bioavailability
- CL = clearance
Prolongation of Drug Action
- Methods for maintaining a drug's effect over time:
- Prolonging absorption rate at the site of administration
- Increasing plasma protein binding
- Retarding metabolism
- Retarding renal excretion
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Description
This quiz covers the essential concepts of drug elimination, focusing on how drugs are cleared by various organs like the kidneys and liver. You will explore first-order vs. zero-order kinetics, calculate loading and maintenance doses, and understand methods to prolong drug action. Test your knowledge on the mechanisms of drug excretion and renal processes involved.