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The document discusses nonlinear pharmacokinetics, highlighting the differences between drugs that follow nonlinear versus linear pharmacokinetics, and poses various learning questions related to drug absorption, distribution, and elimination. It also addresses the effects of drug interactions, enzyme induction/inhibition, and the implications of dose changes on pharmacokinetic parameters. Additionally, it includes specific case studies and theoretical scenarios to illustrate these concepts.

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Heba Alhemady
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18 views

Learning Questions

The document discusses nonlinear pharmacokinetics, highlighting the differences between drugs that follow nonlinear versus linear pharmacokinetics, and poses various learning questions related to drug absorption, distribution, and elimination. It also addresses the effects of drug interactions, enzyme induction/inhibition, and the implications of dose changes on pharmacokinetic parameters. Additionally, it includes specific case studies and theoretical scenarios to illustrate these concepts.

Uploaded by

Heba Alhemady
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as PDF, TXT or read online on Scribd
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Applied Biopharmaceutics & Pharmacokinetics, 6e

Chapter 9. Nonlinear Pharmacokinetics

Learning Questions
1. Define nonlinear pharmacokinetics. How do drugs that follow nonlinear pharmacokinetics differ from drugs that follow linear pharmacokinetics?

a. What is the rate of change in the plasma drug concentration with respect to time, dCp/dt, when Cp « KM?

b. What is the rate of change in the plasma drug concentration with respect to time, dCp/dt, when Cp » KM?

2. What processes of drug absorption, distribution, and elimination may be considered “capacity limited,” “saturated,” or “dose dependent”?

3. Drugs, such as phenytoin and salicylates, have been reported to follow dose­dependent elimination kinetics. What changes in pharmacokinetic
parameters, including t1/2, VD, AUC, and Cp, could be predicted if the amounts of these drugs administered were increased from low
pharmacologic doses to high therapeutic doses?

4. A given drug is metabolized by capacity­limited pharmacokinetics. Assume KM is 50 μg/mL, Vmax is 20 μg/mL per hour, and the apparent VD is 20
L/kg.

a. What is the reaction order for the metabolism of this drug when given in a single intravenous dose of 10 mg/kg?

b. How much time is necessary for the drug to be 50% metabolized?

5. How would induction or inhibition of the hepatic enzymes involved in drug biotransformation theoretically affect the pharmacokinetics of a drug
that demonstrates nonlinear pharmacokinetics due to saturation of its hepatic elimination pathway?

6. Assume that both the active parent drug and its inactive metabolites are excreted by active tubular secretion. What might be the consequences of
increasing the dosage of the drug on its elimination half­life?

7. The drug isoniazid was reported to interfere with the metabolism of phenytoin. Patients taking both drugs together show higher phenytoin levels
in the body. Using the basic principles in this chapter, do you expect KM to increase or decrease in patients taking both drugs? (Hint: see Fig. 9­4.)

8. Explain why KM sometimes has units of mM/mL and sometimes mg/L.

9. The Vmax for metabolizing a drug is 10 mmol/h. The rate of metabolism (v) is 5 μmol/h when drug concentration is 4 μmol. Which of the following
statements is/are true?

a. KM is 5 μmol for this drug.

b. KM cannot be determined from the information given.

c. KM is 4 μmol for this drug.

10. Which of the following statements is/are true regarding the pharmacokinetics of diazepam (98% protein bound) and propranolol (87% protein
bound)?

a. Diazepam has a long elimination half­life because it is difficult to be metabolized due to extensive plasma–protein binding.

b. Propranolol is an example of a drug with high protein binding but unrestricted (unaffected) metabolic clearance.
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d. All of the above.
10. Which of the following statements is/are true regarding the pharmacokinetics of diazepam (98% protein bound) and propranolol (87% protein
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bound)?

a. Diazepam has a long elimination half­life because it is difficult to be metabolized due to extensive plasma–protein binding.

b. Propranolol is an example of a drug with high protein binding but unrestricted (unaffected) metabolic clearance.

c. Diazepam is an example of a drug with low hepatic extraction.

d. All of the above.

e. a and c .

f. b and c .

11. Which of the following statements describe(s) correctly the properties of a drug that follows nonlinear or capacity­limited pharmacokinetics?

a. The elimination half­life will remain constant when the dose changes.

b. The area under the plasma curve (AUC) will increase proportionally as dose increases.

c. The rate of drug elimination = Cp × KM.

d. All of the above.

e. a and b .

f. None of the above.

12. The hepatic intrinsic clearances of two drugs are

drug A: 1300 mL/min

drug B: 26 mL/min

Which drug is likely to show the greatest increase in hepatic clearance when hepatic blood flow is increased from 1 L/min to 1.5 L/min?

a. Drug A

b. Drug B

c. No change for both drugs

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