The primary objective of this 4-volume book series is to educate PharmD students on the subject of medicinal chemistry. The book set serves as a reference guide to pharmacists on aspects of the chemical basis of drug action. Medicinal Chemistry of Drugs Affecting the Nervous System is the second volume of the series and it presents 8 chapters focusing on a comprehensive account of drugs affecting the nervous system. The volume informs readers about the medicinal chemistry of relevant drugs, which includes the mechanism of drug action, detail structure-activity relationships and metabolism as well as clinical significance of drugs affecting the autonomic and central nervous system.
Chapters in this volume cover cholinergic drugs, adrenergic drugs, antipsychotics, antidepressants, sedatives, hypnotics, anxiolytics, antiepileptic drugs, anaesthetics and antiparkinsonian drugs, respectively. Students and teachers will be able to integrate the knowledge presented in the book and apply medicinal chemistry concepts to understand the pharmacodynamics and pharmacokinetics of therapeutic agents in the body. The information offered by the book chapters will give readers a strong neuropharmacology knowledge base required for a practising pharmacist.
Table of Contents
Chapter 1 Drugs Affecting the Cholinergic System
- Historical Perspectives
- Introductory Concepts
- Choline and Acetylcholine
- Acetylcholine and Neurotransmission
- Cholinergic Neurochemistry: Ach Biosynthesis, Storage, Release, and Metabolism
- Cholinergic Receptors - Muscarinic and Nicotinic Subtypes
- Clinical Use of Acetylcholine
- Muscarinic Receptor Agonists
- Muscarinic Receptor Antagonists (Anticholinergics)
- Acetylcholinesterase (Ache) Inhibitors
- Reversible Noncovalent Inhibitors
- Reversible Covalent Inhibitors
- Irreversible Covalent Inhibitors
- Neuromuscular Blocking Agents
- Depolarizing Muscle Nicotinic Receptor Neuromuscular Blocking Agents
- Non-Depolarizing Muscle Nicotinic Receptor Neuromuscular Blocking Agents
- Ganglionic-Nicotinic Receptor Blocking Agents
- Treatment of Alzheimer's Disease (Ad)
- Epidemiology
- Pathophysiology
- Β-Amyloid Hypothesis
- Cholinergic Hypothesis
- Other Hypothesis
- Pharmacotherapy
- Acetyl Cholinesterase (Ache) Inhibitors
- Donepezil (Aricept ® )
- Pharmacokinetics
- Side Effects/Drug Interactions
- Rivastigmine (Exelon ® ) 2000, Oral; 2008, Patch
- Pharmacokinetics
- Side Effects/Drug Interactions
- Galantamine (Razadyne) 2001
- Pharmacokinetics
- Side Effects/Drug-Interactions
- Nmda Receptor Antagonist: Memantine (Namenda®) 2003
- Pharmacokinetics
- Side Effects/Drug Interactions
- Place in Therapy
- Case Study
- What Therapeutic Modifications Would You Make at this Time and Why?
- Drug Discovery Case Study
- The Quaternary Advantage - Ipratropium and the Kinetic Selectivity of Tiotropium
- Student Self Study Guide
- Practice Questions
- Cory R. Theberge, Kim Lindsey-Goodrich and Ashok E. Philip
- Notes
- Consent for Publication
- Conflict of Interest
- Acknowledgements
- References
Chapter 2 Drugs Affecting Adrenergic System
- Historical Background
- The Introductory Concepts
- Adrenergic Neurotransmitters
- Adrenergic Receptors (Ars)
- Drugs Affecting Adrenergic System: Structures, Activity,
- Metabolism and Related Therapeutic Considerations
- The Antiadrenergics Affecting Synthesis, Storage, or Release of Ne
- Metyrosine
- Reserpine
- Mechanism of Action
- Pharmacokinetics
- Guanethidine and Guanadrel
- Direct-Acting Sympathomimetic Agents
- The General Mechanism and Sar of Β-Phenylethylamine Derivatives (Direct And
- Indirect Acting Agonists)
- Sar 1
- Sar 2
- Sar 3
- Sar 4
- Sar 5
- Sar 6
- Sar 7
- Sar 8
- Sar 9
- Therapeutic Evaluation of the Β-Phenylethylamine Direct Acting Adrenergic Agonists
- Β2 Adrenergic Agonist and Cardiac Function
- Long Acting Β2-Adrenoceptor Agonists (Labas)
- Β3 Adrenergic Receptor Agonist
- The General Sar of Imidazolines (Α Adrenergic Agonist and Antagonists)
- Sar 1
- Sar 2
- Sar 3
- Therapeutic Evaluation of the Imidazoline Α Adrenergic Agonists
- Indirect-Acting Sympathomimetics
- Adrenergic Receptor Antagonists
- The Α Adrenergic Antagonists
- Β-Adrenergic Receptor Antagonists (Β-Blockers)
- Sar 1
- Sar 2
- Sar 3
- Sar 4
- Sar 5
- Nonselective Β-Blockers
- M. O. Faruk and Les Ramos
- Selective Β1-Blockers (Cardioselective Β-Blockers)
- Black Box Warning with Systemic Use Β-Blockers
- Case Studies
- Drug Discovery Case Studies
- Discovery of Adrenergic Agonists
- Discovery of Adrenergic Antagonists - the Discovery of Propranolol
- Student Self-Study Guide
- Student Self-Assessment Questions
- The Duration of Action of X,Y,Z is in the Order (Longest to Shortest)
- References
Chapter 3 Phenothiazines and Related Antipsychotic Drugs
- Historical Backgrounds
- Introductory Concepts
- Psychotic Disorders and Relevant Terminologies
- Dopamine Hypothesis of Psychosis and Site of Action of Antipsychotics
- Schizophrenia-Associated Neurotransmitters and Circuitry in the Brain
- Evidence Against the Hypothesis
- The Dopaminergic Neurons, Synthesis, and Degradation of Dopamine
- Receptors of Dopamine
- The Interaction of Dopamine Receptor and Antipsychotic Agents
- Other Receptors Involved in Antipsychotic Drug Action
- The Antipsychotic Drugs
- Classes of Antipsychotic Drugs
- First Generation (Typical) Antipsychotic Drugs
- Potency Comparison of Piperazine, Aliphatic and Piperidine Type Antipsychotic Agents
- Butyrophenone Antipsychotics and Related Sar
- Second Generation (Atypical) Antipsychotics
- General Mechanisms of Action and Side Effects
- Selected Clinically Used Second-Generation Antipsychotics
- Clozapine and Olanzapine
- Quetiapine
- Asenapine
- Cariprazine
- Risperidone Paliperidone and Ziprasidone
- Lurasidone
- Iloperidone
- Aripiprazole
- Brexpiprazole
- Selected Antipsychotic Drugs and Their Interaction with Dopamine and Other Receptors
- Case Studies
- Clinically Relevant Case Studies
- Drug Discovery Case Studies
- Discovery of Haloperidol
- Discovery of Ziprasidone
- Student Self-Study Guide
- Students Self-Assessment Questions
- Notes
- Consent for Publication
- Mamoon Rashid, Mehbuba Rahman and M. O. Faruk Khan
- Conflict of Interest
- Acknowledgements
- References
Chapter 4 Antidepressant Drugs
- Historical Perspective
- Introductory Concepts
- Affective Disorders
- Pathophysiology - Biogenic Amine Hypothesis
- Classification of Antidepressants
- Consequence of Ring Geometry of Tca
- Serotonin and Norepinephrine Reuptake Inhibitors (Snris)
- Tricyclic Antidepressants (Tcas)
- Mechanism of Action
- Adverse Effects
- General Sar of Tcas
- Ring Substitutions
- Γ-Nitrogen Substituents
- Individual Clinically Used Tcas
- Imipramine (Tofraniltm)
- Clomipramine (Anafraniltm)
- Amitriptyline
- Protriptyline (Vivactiltm)
- Trimipramine (Surmontiltm)
- Doxepin (Prudoxintm)
- Maprotiline (Ludiomiltm)
- Amoxapine (Asendintm)
- Phenylalkylamine Snris
- Venlafaxine (Effexortm)
- Milnacipran (Savellatm)
- Duloxetine (Cymbaltatm)
- Selective Norepinephrine Reuptake Inhibitor (Nris)
- Phenoxyphenylpropylamines
- Mechanism of Action
- Adverse Effects
- Atomoxetine (Stratteratm)
- Reboxetine (Edronaxtm)
- Selective Serotonin Reuptake Inhibitors (Ssris)
- Mechanism of Action
- Adverse Effects
- Phenoxyphenylalkylamines
- Sar of Phenoxyphenylalkylamines
- Fluoxetine (Prozactm)
- Disorder (Ocd)
- Paroxetine (Paxiltm)
- Citalopram (Celexatm)
- Phenylalkylamines
- Sertraline (Zolofttm)
- Fluvoxamine (Luvoxtm)
- Monoamine Oxidase Inhibitors (Maois)
- Horrick Sharma, Michaela Leffler and M. O. Faruk Khan
- Mechanism of Action
- Adverse Effects
- Phenelzine and Tranylcypromine
- Miscellaneous Agents
- Trazodone (Desyreltm)
- Mirtazapine (Remerontm)
- Bupropion (Wellbutrintm)
- Case Studies
- Case 1
- Case 2
- Case 3
- Drug Discovery Case Study
- Discovery of Ssris and Fluoxetine
- Student Self Study Guide
- Students Self-Assessment Questions
- Consent for Publication
- Conflict of Interest
- Acknowledgements
- References
Chapter 5 Sedatives, Hypnotics and Anxiolytics
- Historical Background
- Introductory Concepts
- Sedative-Hypnotics
- Anxiolytics
- Mechanisms of Action
- Γ-Amino Butyric Acid (Gaba) Receptor Modulation
- Melatonin Mt1/Mt2 Receptor Activation
- 5-Ht1A Receptor Activation
- Barbiturates
- Individual Barbiturate Drugs (Mechanism, Metabolism, Drug Interactions)
- Long Acting Barbiturates (Doa> 6 H)
- Intermediate Acting Barbiturates (Doa 3-6H)
- Short Acting Barbiturates (Doa< 3 H)
- Barbiturate Sar
- Benzodiazepines
- Individual Benzodiazepine Drugs (Mechanisms, Metabolism, and Drug Interactions)
- Long-Acting Bzds (T1/2 >24 Hours)
- Quazepam (Doral)
- Intermediate Acting Bzds (T1/2 5-24 Hours)
- Short-Acting Bzds (T1/2 < 5 Hours)
- Benzodiazepine Sar
- Non-Benzodiazepines
- Individual Non-Benzodiazepine Drugs (Mechanisms, Metabolism, Drug Interactions)
- Zolpidem Tartrate (Ambien®)
- Zaleplon (Sonata®)
- Eszopiclone (Lunesta®)
- Meprobamate (Equanil)
- Ramelteon (Rozerem®)
- Buspirone (Buspar®)
Samples
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Author
- Ashok E. Philip
- M. O. Faruk Khan
