, Ignacio Flores2 and Roser Ribosa-Nogué3 (1) Barcelona, Spain (2) Servicio de Neurología, Hospital San Martín, La Plata, Buenos Aires, Argentina (3) Unitat de Memòria, Servei de Neurologia, Hospital de la Santa…
(1) Southhampton, United Kingdom 5.1 Introduction Memantine is a noncompetitive, voltage-dependent N-methyl-D-aspartate (NMDA) receptor antagonist. It is licensed for the treatment of moderate to severe AD in the USA…
Orthosteric Drug Effects Outline Bi-Molecular Systems51 New Terminology52 What is Drug Antagonism?53 Antagonist Potency53 Mechanism(s) of Receptor Antagonism54 Orthosteric (Competitive and Non-Competitive) Antagonism56 Slow Dissociation Kinetics and Non-Competitive Antagonism62 Partial…
Distribution and Multiple Dosing Outline Drugs in Motion: In Vivo Pharmacokinetics155 New Terminology156 The Central Compartment and In Vivo Clearance156 Renal Excretion159 Drug Distribution162 Pharmacokinetics In Vivo166 Scaling Data to…
185 New Terminology188 The “Dose” in Dose–Response189 What Constitutes Drug Response?194 The Importance of Kinetics In Vivo199 Summary207 The ultimate therapeutic value of a molecule is determined by its effect…
19 New Terminology20 Agonist Selectivity20 Affinity20 Efficacy26 Drugs with Multiple Efficacies29 Quantifying Agonist Activity32 Descriptive Pharmacology: II34 Summary35 This chapter specifically discusses the concepts of affinity (expressed as a ratio…
Permeation and Metabolism Outline The Importance of Drug Concentration125 New Terminology132 “Drug-Like” Properties of Molecules133 Drug Absorption135 Drug Metabolism142 Oral Bioavailability150 Summary152 This chapter discusses how the body is a…
105 New Terminology105 Enzyme Kinetics107 Enzymes as Drug Targets109 Reversible Enzyme Inhibition112 Irreversible Enzyme Inhibition117 Intracellular Effects of Enzyme-Active Drugs120 Summary123 This chapter considers how enzymes can be therapeutic drug…
81 New Terminology82 Protein Allosterism82 Types of Allosteric Modulators84 Unique Effects of Allosteric Modulators87 Detecting Allosterism93 Quantifying Allosteric Effect98 Descriptive Pharmacology: V101 Summary102 This chapter begins with a discussion of…
37 New Terminology39 The Black–Leff Operational Model of Agonism40 Applying the Black–Leff Model to Predict Agonism43 Descriptive Pharmacology: III49 Summary50 This chapter discusses the use of the Black–Leff operational model…
