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Questions and Answers
Which transportation process requires ATP to pump material?
Which transportation process requires ATP to pump material?
What is a characteristic of substances that undergo passive diffusion?
What is a characteristic of substances that undergo passive diffusion?
Which route of administration is recognized for providing a local effect?
Which route of administration is recognized for providing a local effect?
Which of the following is NOT a type of drug transporter?
Which of the following is NOT a type of drug transporter?
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What is an example of a drug that undergoes active transport?
What is an example of a drug that undergoes active transport?
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What is a common method of parenteral drug administration?
What is a common method of parenteral drug administration?
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What are the four key processes involved in pharmacokinetics?
What are the four key processes involved in pharmacokinetics?
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What does 'bioavailability' refer to in pharmacokinetics?
What does 'bioavailability' refer to in pharmacokinetics?
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Which type of transport typically occurs along a concentration gradient?
Which type of transport typically occurs along a concentration gradient?
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Which process is responsible for the transfer of drug from the site of administration to the general circulation?
Which process is responsible for the transfer of drug from the site of administration to the general circulation?
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Which is a reason for multidrug resistance in therapeutic settings?
Which is a reason for multidrug resistance in therapeutic settings?
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Which of the following statements is true regarding first-pass metabolism?
Which of the following statements is true regarding first-pass metabolism?
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Which term describes the removal of drug from the body, which may include metabolism or excretion?
Which term describes the removal of drug from the body, which may include metabolism or excretion?
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What is primarily measured to assess how a patient's response to a drug changes over time?
What is primarily measured to assess how a patient's response to a drug changes over time?
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Which of the following correctly describes a method of drug absorption through membranes?
Which of the following correctly describes a method of drug absorption through membranes?
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What physiological process does pharmacodynamics mainly focus on?
What physiological process does pharmacodynamics mainly focus on?
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Which route of administration is characterized by the quickest absorption?
Which route of administration is characterized by the quickest absorption?
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What is a significant factor affecting the absorption of drugs from the gut?
What is a significant factor affecting the absorption of drugs from the gut?
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Which of the following drugs is most likely to be affected by first-pass metabolism?
Which of the following drugs is most likely to be affected by first-pass metabolism?
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How does food typically affect drug absorption when taken orally?
How does food typically affect drug absorption when taken orally?
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Which drug is known to have variable absorption due to being charged in the stomach?
Which drug is known to have variable absorption due to being charged in the stomach?
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What is a characteristic of the intradermal route of administration?
What is a characteristic of the intradermal route of administration?
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Which metabolic process occurs when a drug is absorbed through the GI tract before reaching systemic circulation?
Which metabolic process occurs when a drug is absorbed through the GI tract before reaching systemic circulation?
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Which of the following administration routes bypasses first-pass metabolism?
Which of the following administration routes bypasses first-pass metabolism?
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What is bioavailability (F)?
What is bioavailability (F)?
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Which of the following equations represents the calculation of % Bioavailability?
Which of the following equations represents the calculation of % Bioavailability?
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What is the bioavailability percentage for intravenous (IV) administration?
What is the bioavailability percentage for intravenous (IV) administration?
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Why is bioavailability important when considering drug dosages?
Why is bioavailability important when considering drug dosages?
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How does the bioavailability of propranolol differ between oral and sublingual administration?
How does the bioavailability of propranolol differ between oral and sublingual administration?
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What are the four key processes involved in pharmacokinetics?
What are the four key processes involved in pharmacokinetics?
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What is a significant factor that can influence plasma drug levels following absorption?
What is a significant factor that can influence plasma drug levels following absorption?
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What does a lower bioavailability percentage indicate about a drug's route of administration?
What does a lower bioavailability percentage indicate about a drug's route of administration?
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What is the primary advantage of intravenous administration?
What is the primary advantage of intravenous administration?
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Which route of administration is suitable only for lipid-soluble drugs?
Which route of administration is suitable only for lipid-soluble drugs?
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What is the term used to describe the amount of drug that reaches systemic circulation after administration?
What is the term used to describe the amount of drug that reaches systemic circulation after administration?
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What is the effect of first pass metabolism?
What is the effect of first pass metabolism?
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Which route of administration typically has a delayed onset of action?
Which route of administration typically has a delayed onset of action?
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Which of the following correctly describes absorption in pharmacokinetics?
Which of the following correctly describes absorption in pharmacokinetics?
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When after administration does maximum plasma concentration (Cmax) occur for intravenous doses?
When after administration does maximum plasma concentration (Cmax) occur for intravenous doses?
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Which route of administration is most useful for patients who are vomiting or fitting?
Which route of administration is most useful for patients who are vomiting or fitting?
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What does the area under the curve (AUC) in a plasma concentration-time plot represent?
What does the area under the curve (AUC) in a plasma concentration-time plot represent?
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Which of the following routes allows for controlled release of medication?
Which of the following routes allows for controlled release of medication?
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What is the main focus of pharmacodynamics?
What is the main focus of pharmacodynamics?
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Which term describes the volume of distribution in pharmacokinetics?
Which term describes the volume of distribution in pharmacokinetics?
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What major processes constitute drug elimination?
What major processes constitute drug elimination?
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How does absorption influence plasma drug levels?
How does absorption influence plasma drug levels?
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What is first-pass metabolism?
What is first-pass metabolism?
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What are the primary characteristics of passive diffusion?
What are the primary characteristics of passive diffusion?
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What factor affects bioavailability?
What factor affects bioavailability?
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Which route of administration is classified as enteral?
Which route of administration is classified as enteral?
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What is the relationship between dosage and effect in pharmacokinetics?
What is the relationship between dosage and effect in pharmacokinetics?
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What is the role of organic anion transporters (OATs)?
What is the role of organic anion transporters (OATs)?
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What role does clearance (Cl) play in pharmacokinetics?
What role does clearance (Cl) play in pharmacokinetics?
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Which of the following correctly describes a characteristic of parenteral routes of administration?
Which of the following correctly describes a characteristic of parenteral routes of administration?
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What characteristic distinguishes ATP binding cassette transporters (ABCs)?
What characteristic distinguishes ATP binding cassette transporters (ABCs)?
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Which type of drug transport process relies on solute carrier transporters (SLCs)?
Which type of drug transport process relies on solute carrier transporters (SLCs)?
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Which of the following is an example of a topical route of administration?
Which of the following is an example of a topical route of administration?
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What differentiates active transport from passive diffusion in drug absorption?
What differentiates active transport from passive diffusion in drug absorption?
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What is the main disadvantage of oral drug administration compared to alternative routes?
What is the main disadvantage of oral drug administration compared to alternative routes?
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What primarily affects the absorption of weak acids and weak bases in the digestive tract?
What primarily affects the absorption of weak acids and weak bases in the digestive tract?
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Why might gastric emptying influence the rate of drug absorption?
Why might gastric emptying influence the rate of drug absorption?
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What is the purpose of first-pass metabolism in the pharmacokinetic process?
What is the purpose of first-pass metabolism in the pharmacokinetic process?
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Which of the following drugs is likely not significantly affected by first-pass metabolism?
Which of the following drugs is likely not significantly affected by first-pass metabolism?
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What role do digestive enzymes play in drug absorption?
What role do digestive enzymes play in drug absorption?
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What characteristic makes intravenous administration advantageous compared to other routes?
What characteristic makes intravenous administration advantageous compared to other routes?
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Which factor is least likely to influence gastric emptying and thus drug absorption?
Which factor is least likely to influence gastric emptying and thus drug absorption?
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What does bioavailability measure in pharmacokinetics?
What does bioavailability measure in pharmacokinetics?
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What is the maximum bioavailability percentage possible for any non-intravenous route of administration?
What is the maximum bioavailability percentage possible for any non-intravenous route of administration?
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Which of the following routes of administration typically has a higher bioavailability than oral administration?
Which of the following routes of administration typically has a higher bioavailability than oral administration?
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How is the percentage bioavailability calculated?
How is the percentage bioavailability calculated?
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What is the significance of the area under the curve (AUC) in a plasma concentration-time plot?
What is the significance of the area under the curve (AUC) in a plasma concentration-time plot?
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Why is first-pass metabolism considered important in pharmacokinetics?
Why is first-pass metabolism considered important in pharmacokinetics?
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What is the expected bioavailability of a drug administered intravenously?
What is the expected bioavailability of a drug administered intravenously?
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What does a lower bioavailability percentage typically indicate about a drug's route of administration?
What does a lower bioavailability percentage typically indicate about a drug's route of administration?
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What is the primary characteristic that determines the choice of a drug's route of administration?
What is the primary characteristic that determines the choice of a drug's route of administration?
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Which of the following routes of administration is known for avoiding first-pass metabolism?
Which of the following routes of administration is known for avoiding first-pass metabolism?
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What can the area under the curve (AUC) in a plasma concentration-time plot best be defined as?
What can the area under the curve (AUC) in a plasma concentration-time plot best be defined as?
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When is the onset of action typically observed following drug administration?
When is the onset of action typically observed following drug administration?
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What is a significant advantage of intravenous drug administration?
What is a significant advantage of intravenous drug administration?
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Which of the following routes is most effective for providing localized effects while still allowing for potential systemic effects?
Which of the following routes is most effective for providing localized effects while still allowing for potential systemic effects?
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What characterizes the absorption rate of drugs administered via the intramuscular route?
What characterizes the absorption rate of drugs administered via the intramuscular route?
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What is the significance of achieving high drug concentrations at particular sites of action?
What is the significance of achieving high drug concentrations at particular sites of action?
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Which of the following describes a disadvantage of the transdermal route of administration?
Which of the following describes a disadvantage of the transdermal route of administration?
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How does first-pass metabolism influence drug effectiveness?
How does first-pass metabolism influence drug effectiveness?
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What is the primary role of pharmacodynamics in drug therapy?
What is the primary role of pharmacodynamics in drug therapy?
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Which factor is crucial in determining bioavailability (F) of a drug?
Which factor is crucial in determining bioavailability (F) of a drug?
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How does first-pass metabolism affect a drug's efficacy after oral administration?
How does first-pass metabolism affect a drug's efficacy after oral administration?
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What does Plasma Half-Life (t1/2) indicate in pharmacokinetics?
What does Plasma Half-Life (t1/2) indicate in pharmacokinetics?
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In pharmacokinetics, which process describes the transfer of a drug from the circulation into various organs?
In pharmacokinetics, which process describes the transfer of a drug from the circulation into various organs?
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What is a key determinant of drug clearance (Cl) in pharmacokinetics?
What is a key determinant of drug clearance (Cl) in pharmacokinetics?
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Which of the following processes is involved in the elimination of drugs from the body?
Which of the following processes is involved in the elimination of drugs from the body?
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What is the significance of the area under the curve (AUC) in plasma concentration-time plots?
What is the significance of the area under the curve (AUC) in plasma concentration-time plots?
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What is the primary purpose of solute carrier transporters (SLCs) in drug absorption processes?
What is the primary purpose of solute carrier transporters (SLCs) in drug absorption processes?
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Which route of drug administration is categorized as having a non-local effect?
Which route of drug administration is categorized as having a non-local effect?
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Which type of transport process relies on the hydrolysis of ATP to move substances across membranes?
Which type of transport process relies on the hydrolysis of ATP to move substances across membranes?
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Which of the following is a characteristic feature of parenteral routes of administration?
Which of the following is a characteristic feature of parenteral routes of administration?
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Which transport mechanism is commonly associated with causing multidrug resistance?
Which transport mechanism is commonly associated with causing multidrug resistance?
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What defines the absorption process of a drug through the lipid bilayer?
What defines the absorption process of a drug through the lipid bilayer?
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Which statement best describes the absorption characteristics associated with inhalation as a route of administration?
Which statement best describes the absorption characteristics associated with inhalation as a route of administration?
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What is the main function of organic cation transporters (OCTs) in pharmacokinetics?
What is the main function of organic cation transporters (OCTs) in pharmacokinetics?
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Which factor most significantly affects the absorption rate of a drug taken orally?
Which factor most significantly affects the absorption rate of a drug taken orally?
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What is the major effect of first-pass metabolism on drug availability?
What is the major effect of first-pass metabolism on drug availability?
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Which route of drug administration ensures 100% bioavailability?
Which route of drug administration ensures 100% bioavailability?
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Why are weak acids generally better absorbed in the stomach than weak bases?
Why are weak acids generally better absorbed in the stomach than weak bases?
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Which of the following drugs would likely experience variability in absorption due to its ionization in the stomach?
Which of the following drugs would likely experience variability in absorption due to its ionization in the stomach?
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What is one consequence of slower gastric emptying on drug absorption?
What is one consequence of slower gastric emptying on drug absorption?
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Which statement accurately describes the characteristics of intradermal drug administration?
Which statement accurately describes the characteristics of intradermal drug administration?
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Which of the following is a characteristic of drugs that undergo first-pass metabolism?
Which of the following is a characteristic of drugs that undergo first-pass metabolism?
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Which route of administration notably avoids first-pass metabolism?
Which route of administration notably avoids first-pass metabolism?
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What does the area under the curve (AUC) in a plasma concentration-time curve indicate?
What does the area under the curve (AUC) in a plasma concentration-time curve indicate?
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Intravenous administration is characterized by which of the following advantages?
Intravenous administration is characterized by which of the following advantages?
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When does the onset of action occur after drug administration?
When does the onset of action occur after drug administration?
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Which one of these routes is primarily unsuitable for lipid-soluble drugs?
Which one of these routes is primarily unsuitable for lipid-soluble drugs?
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What is the primary function of using inhalation as a route of administration?
What is the primary function of using inhalation as a route of administration?
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What characteristic of a drug does NOT determine its route of administration?
What characteristic of a drug does NOT determine its route of administration?
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Which route of administration may have unreliable absorption but is useful in specific clinical situations?
Which route of administration may have unreliable absorption but is useful in specific clinical situations?
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In pharmacokinetics, what process is described as the removal of a drug from the body?
In pharmacokinetics, what process is described as the removal of a drug from the body?
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Which route of administration is noted for both localized effect and systemic absorption?
Which route of administration is noted for both localized effect and systemic absorption?
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What does a lower bioavailability percentage indicate about a drug's route of administration?
What does a lower bioavailability percentage indicate about a drug's route of administration?
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Which route of administration is likely to show the highest variability in bioavailability for the same drug?
Which route of administration is likely to show the highest variability in bioavailability for the same drug?
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How is bioavailability (F) defined in pharmacokinetics?
How is bioavailability (F) defined in pharmacokinetics?
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What is the significance of determining bioavailability using intravenous (IV) administration as a reference?
What is the significance of determining bioavailability using intravenous (IV) administration as a reference?
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What does the equation % Bioavailability = (AUCoral / AUCIV) x 100 measure?
What does the equation % Bioavailability = (AUCoral / AUCIV) x 100 measure?
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Why is the concept of bioavailability particularly important for drugs administered via the oral route?
Why is the concept of bioavailability particularly important for drugs administered via the oral route?
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For which of the following drugs would you expect the intravenous bioavailability (F) to be 100%?
For which of the following drugs would you expect the intravenous bioavailability (F) to be 100%?
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Which factor most directly affects the bioavailability of a drug administered orally compared to intravenously?
Which factor most directly affects the bioavailability of a drug administered orally compared to intravenously?
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Study Notes
Pharmacokinetics vs. Pharmacodynamics
- Pharmacokinetics describes how the body affects a drug.
- Pharmacodynamics describes how a drug affects the body.
Four Basic Pharmacokinetic Processes (ADME)
- Absorption: Movement of drug from administration site to circulation.
- Distribution: Movement of drug from circulation to different organs.
- Metabolism: Breakdown of a drug within the body.
- Excretion: Elimination of drug from the body.
Drug Passage Across Membranes
- Passive Diffusion: Movement along a concentration gradient, requires some lipid solubility.
-
Carrier-Mediated Processes: Involve transporters that facilitate or actively move drugs across membranes.
- Solute Carrier Transporters (SLCs): Facilitate transport down a concentration gradient.
- ATP Binding Cassette Transporters (ABCs): Require ATP to pump material against a concentration gradient.
Routes of Administration
- Enteral: Administration through the digestive tract. Examples: oral, rectal, sublingual.
- Parenteral: Administration outside the digestive tract. Examples: intravenous, intramuscular, subcutaneous, intradermal, inhalation, transdermal.
Factors Influencing Drug Absorption from the Gut
- Drug Structure: Highly polar or ionized compounds are poorly absorbed.
- Formulation: Capsules and tablets must disintegrate for absorption.
- Gastric Emptying: Can affect the rate of absorption, but not the quantity absorbed.
First-Pass Metabolism
- Definition: Metabolism of a drug before it reaches systemic circulation.
- Locations: Intestinal lumen, intestinal wall, and liver.
- Consequences: Decreases the bioavailability of orally administered drugs.
Advantages of Different Routes of Administration
- Intravenous: 100% bioavailability, rapid onset, controlled release.
- Sublingual: Escapes first-pass metabolism, rapid onset.
- Intramuscular: Good bioavailability, controlled release.
- Transdermal: Controlled release, localized effects.
- Inhalation: Rapid onset, localized effects, can avoid first-pass metabolism.
Bioavailability
- Definition: The fraction of a drug dose that reaches systemic circulation.
- Calculated as: AUC (oral) / AUC (IV) x 100
- Importance: Determines the dose required for different routes of administration.
Drug Plasma Concentration vs. Time Plots
- Oral Administration: Shows the time to reach peak plasma concentration (Cmax) and time at or above the minimum effective concentration (MEC).
- IV Administration: Shows a rapid rise in plasma concentration, since the drug bypasses first-pass metabolism.
Pharmacokinetics and Pharmacodynamics
- Pharmacokinetics is the effect of the body on a drug. It describes the movement of drugs into, around, and out of the body.
- Pharmacodynamics is the effect of a drug on the body. It describes the physiological and biochemical effects alongside the drug's interactions with 'targets'.
Four Key Processes Involved in Pharmacokinetics
- Absorption: Transfer of a drug from the site of administration into the general circulation. Bioavailability is the proportion of a drug that enters the bloodstream after administration.
- Distribution: The transfer of a drug from the general circulation into different organs of the body.
- Metabolism: The breakdown of a drug from its original form.
- Excretion: Removal of a drug from the body.
Routes of Drug Administration
- There are three main categories of drug administration: topical, enteral, and parenteral.
- Topical administration applies directly to the area where it is needed. Examples include skin creams, eye drops, and nasal sprays.
- Enteral administration involves giving medication through the digestive tract. Examples include oral, sublingual, and rectal routes.
- Parenteral administration refers to any route other than the digestive tract. Examples include inhalation, injection (IV, IM, SC, and ID injections).
- Oral administration (by mouth) is the most common and convenient.
- Sublingual administration (under the tongue) bypasses the first pass metabolism.
- Rectal administration can be used for localized or systemic effects.
- Intravenous (IV) administration is directly into a vein.
- Intramuscular (IM) injection is given into large muscle masses.
- Subcutaneous (SC/SQ) injection is given below the dermis, allowing for slow and prolonged effects.
- Intradermal (ID) injection is given into the dermis, used for allergy testing and local anesthesia.
Drug Absorption
- Drug passage across the membranes is important for absorption, distribution, and excretion.
- Lipid bilayer: drugs can diffuse through pores or ion channels, pass through the lipid bilayer itself, or be transported by carrier molecules.
- Passive diffusion: Movement of drugs across membranes from high concentration to low concentration.
- Carrier-mediated transport includes solute carrier transporters (SLCs) which facilitate the transport of drugs down the concentration gradient, and ATP binding cassette transporters (ABCs) which require ATP to pump material.
- P-glycoproteins are a type of ABC transporter which contributes to multidrug resistance.
First Pass Metabolism
- **Drug is metabolized in the liver before reaching systemic circulation **after oral administration. Only a proportion of the drug reaches the circulation.
- Alternative routes of administration such as intravenous, intramuscular, and sublingual avoid this effect.
Bioavailability (F)
- The fraction of the administered dose that reaches the systemic circulation as intact drug.
- Determined by comparing plasma levels after different routes of administration to plasma levels after intravenous administration.
- Bioavailability is the fraction of drug reaching systemic circulation as the parent drug.
- Bioavailability can be expressed as a decimal (0.25) or a percentage (25%).
- IV administration has a bioavailability of 100%. Non-IV routes range from 0-100%.
Area Under The Curve (AUC)
- A measure of the total amount of drug that enters the body after administration.
- Calculated from a plasma concentration-time curve.
- Units are concentration × time (e.g., mg.hr L−1).
- The AUC is higher with IV administration than with oral doses.
Drug Plasma Concentration vs Time Plots
- Typical plasma level curve after IV administration: Maximum plasma concentration occurs at time = 0, immediately after dosing.
- Typical plasma level curve after oral administration: maximum plasma concentration (Cmax) is reached at a time tmax after administration.
Plasma Concentration - Time Curve After Oral Administration
- Onset of action occurs when plasma levels reach the minimum effective concentration (MEC).
- Duration of action is the time period the plasma level remains at or above the MEC.
- Maximum safe concentration (MSC) is the point above which adverse effects occur and the concentration should remain below to minimize adverse reactions.
Pharmacokinetics vs. Pharmacodynamics
- Pharmacokinetics: The study of how the body affects a drug.
- Pharmacodynamics: The study of how a drug affects the body.
Four Key Processes of Pharmacokinetics
- Absorption: How a drug enters the bloodstream.
- Distribution: How the drug moves around the body.
- Metabolism: How the drug is broken down by the body.
- Elimination: How the body gets rid of the drug.
Routes of Administration
- Topical: Applied directly to the skin, eyes, nose, or other areas for a local effect.
- Enteral: Given through the digestive tract (e.g., swallowed).
- Parenteral: Given by routes other than the digestive tract (e.g., injection, inhalation).
Factors Affecting Absorption from the Gut
- Drug structure: Highly polar or ionized drugs are poorly absorbed.
- Formulation: Capsules and tablets must disintegrate for absorption.
- Gastric emptying: Food slows down absorption by delaying gastric emptying.
First-Pass Metabolism
- Drugs absorbed from the gut first pass through the liver before entering systemic circulation.
- The liver can metabolize some drugs, reducing the amount that reaches the bloodstream.
- This can be avoided by giving drugs intravenously, sublingually, or rectally.
Bioavailability
- The proportion of an administered drug dose that reaches the systemic circulation in its active form.
- Measured as a percentage or a decimal.
- Bioavailability determines the required dose for different routes of administration.
Bioavailability and First-Pass Metabolism
- Intravenous administration: 100% bioavailability (no first-pass metabolism).
- Oral administration: Bioavailability can vary due to first-pass metabolism, ranging from 0 to 100%.
Importance of Bioavailability
- The true dose is not the amount swallowed, but the drug available to exert its effects.
- Understanding bioavailability is essential for prescribing the correct dose for different drug formulations and administration routes.
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Test your understanding of pharmacokinetics and pharmacodynamics, including the four basic processes of pharmacokinetics: absorption, distribution, metabolism, and excretion. Explore drug passage across membranes and various routes of administration. Enhance your knowledge in pharmacology through this informative quiz.