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This chapter will be most useful after having a basic understanding of the material in Chapter 2, Pharmacokinetics in Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition. This chapter also draws from content in Chapter 5, Membrane Transporters and Drug Response; Chapter 6, Drug Metabolism; and parts of Chapter 7, Pharmacogenetics. The drugs presented in this chapter are used to illustrate general pharmacokinetic principles. The pharmacokinetic, pharmacodynamic, and therapeutic uses of drugs described in Chapter 2 are discussed in more detail in subsequent chapters. Neither a Mechanisms of Action Table nor a Clinical Summary Table is included in this chapter because this information is provided in subsequent chapters.
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In addition to the material presented here, the 12th Edition contains:
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A review in Chapter 2 of cell membranes and their physicochemical properties that affect the movement of drugs to their site of action
A discussion in Chapter 2 of different routes of drug administration and their relative advantages and disadvantages
A detailed discussion in Chapter 2 of renal drug excretion, biliary and fecal excretion, and excretion by other routes
A comprehensive discussion of design and optimization of dosage regimens in Chapter 2, including examples of dosing calculations that take into consideration bioavailability, clearance, and distribution
Appendix II Design Optimization of Dosage Regimens: Pharmacokinetic Data in Goodman & Gilman’s The Pharmacological Basis of Therapeutics, 12th Edition provides a summary of basic pharmacokinetic data for a number of drugs that are in common clinical use, as well as information that is useful in individualizing dosing in a given patient
Chapter 5 contains a detailed review of membrane transporters, including their role in absorption, distribution, and clearance of xenobiotics, and their role in adverse drug responses
Table 5-1 Regulation of Transporter Expression by Nuclear Receptors provides detailed information about drug regulation of transporter expression mediated through specific nuclear receptors
A description in Chapter 5 of the role of efflux transporters in the blood-brain barrier (BBB) and blood-cerebrospinal fluid (CSF) barrier
Chapter 6 provides a comprehensive discussion of drug metabolism enzymes and illustrations that show many of the key chemical reactions catalyzed by these enzymes
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Understand key concepts and terms that determine drug pharmacokinetics, including absorption, distribution, metabolism, and excretion.
Understand the mechanisms by which drugs cross membranes and the physicochemical factors that influence this transfer.
Be able to predict the ionization state of a drug that is a weak acid or base knowing the drug’s pKa and the pH of the fluid.
Describe the role of membrane transporters in drug absorption, distribution, and clearance.
Know the major mechanisms by which drugs are metabolized and excreted from the body.
Understand the major pharmacokinetic mechanisms that can result in drug interactions.
Know the pharmacokinetic mechanisms that give rise to interpatient variability in drug response and toxicity.
Understand the clinical pharmacokinetic principles used to calculate dosing required ...