Description
In line with other volumes in the Neuroscience Perspectives Series, this volume covers the background, pharmacology, molecular biology, and biochemistry of antipsychotic drugs, together with an overview assessment of the therapeutic considerations. Over the past 40 years, the effectiveness of conventional neuroleptic agents for psychotic illness has been offset by a wide range of adverse side-effects, including motor side-effects like parkinsonism. Studies show that lowering doses may still produce the antipsychotic effect while lessening the risk of side-effects. As all available antispychotic drugs are able to block dopamine, specifically D2 receptors, doses below the threshold level for producing acute motor disorder can still be therapeutically effective. With the identification and characterization of multiple dopamine receptors, the possibility of more selective drugs with better side-effect potential has arisen. Other novel antipsychotic agents include D1 receptor blockers, partial dopamine agonists and non-dopamine drugs such as 5-HT receptor blockers, sigma receptor antagonists and NMDA receptor agonists. This volume reviews both the basic science of the conventional and atypical neuroleptics and their present and potential therapeutic use.
Chapter
Neuroscience Editorial Advisory Board
CHAPTER 1. THE PHARMACOLOGY OF THE PHENOTHIAZINES, BUTYROPHENONES, THIOXANTHINES AND DIPHENYLBUTYLPIPERIDINES
1.2 Effects of neuroleptics on dopaminergic and other neurotransmitter systems
1.3 Heterogeneity of dopaminergic neurons in the mesocortical system
1.4 Interaction of neuroleptics with non-dopaminergic receptors
1.5 Action of neuroleptics on different types of neurotransmitter receptor
1.6 Structure-activity relationships and pharmacokinetic aspects
1.7 Behavioural and pharmacological properties of the neuroleptics
1.8 Clinical pharmacology of the neuroleptics
1.9 Hormonal changes resulting from neuroleptic treatment
CHAPTER 2. THE PHARMACOLOGY OF CLOZAPINE-LIKE,ATYPICAL ANTIPSYCHOTICS
2.2 Neuroleptic-like properties in animal studies
2.3 Atypical properties of clozapine
2.4 Neurotransmitter interactions of clozapine and related agents
2.5 Mechanisms underlying clozapine's atypicality
CHAPTER 3. PHARMACOLOGY AND CLINICAL PROPERTIES OF SELECTIVE DOPAMINE ANTAGONISTS WITH FOCUS ON SUBSTITUTED BENZAMIDES
3.2 Antagonisms of dopamine receptors
3.3 Conclusion and future trends
CHAPTER 4. PRE- AND POSTSYNAPTIC D, TO D5 DOPAMINE RECEPTOR MECHANISMS IN RELATION TO ANTIPSYCHOTIC ACTIVITY
4.1 Pharmacological characteristics of dopamine receptor subtypes
4.2 D1 receptor antagonists as putative antipsychotic agents
4.3 'Selective' D2 autoreceptor agonists, antagonists andpartial agonists as putative antipsychotic agents
4.4 Implications for the dopamine hypothesis ofschizophrenia
CHAPTER 5. PREDICTION OF ANTIPSYCHOTIC ACTIVITY
5.2 Preclinical screens for antipsychotic drugs
5.3 Desirable preclinical profile using dopamine antagonist screens
5.4 Preclinical profiles of novel agents suggesting antipsychotic activity
5.5 Discussion and targets for future research
CHAPTER 6. EFFECTS OF NEUROLEPTICS ON NEURONAL AND SYNAPTIC STRUCTURE
6.1 Neuroleptic effects on neurons
6.2 Neuroleptic effects on synapses
6.3 Neuroleptic effects in human brain
6.4 Neuroleptics and gene expression
CHAPTER 7. BRAIN IMAGING AND ANTIPSYCHOTIC DRUGS
7.2 Brain-imaging techniques
7.3 Effects of antipsychotic drugs on brain activity
7.4 Occupation of neuroreceptors by antipsychotic drugs
7.5 Conclusions regarding antipsychotic drug action
CHAPTER 8. PHARMACOKINETICS OF ANTIPSYCHOTIC DRUGS
8.3 Neuroleptic drug metabolites
8.4 Presystemic elimination (first-pass effect)
8.6 Binding to plasma protein
8.7 pH-dependent phenomena
8.8 Elimination half-life
8.9 U-shaped clinical-chemical relationships
8.10 Changeover from oral medication to depot neuroleptics
8.12 Therapeutic monitoring
CHAPTER 9. THE ASSESSMENT OF ANTIPSYCHOTIC MEDICATION IN CLINICAL TRIALS
9.6 Fixed- versus flexible-dose studies
9.10 Clinical designs for specific purposes
9.11 Other measures of pharmacological efficacy
CHAPTER 10. INDICATIONS FOR ANTIPSYCHOTIC DRUGS
10.3 Delusional depression
10.4 Functional psychosis
10.6 Miscellaneous indications
CHAPTER 11. ACUTE TREATMENT
11.5 Antipsychotic drug dosage equivalencies
11.6 Strategies for treating non-responsive patients
CHAPTER 12. MAINTENANCE ANTIPSYCHOTIC MEDICATION
12.2 Time-course of relapse
12.3 Indications for maintenance
12.5 Dosage of medication
12.6 Choice of medication
12.7 Effect of antipsychotic drugs on the course ofschizophrenia
12.8 Maintenance drug and psychosocial treatment
12.9 Postpsychotic depression
CHAPTER 13. DEPOT NEUROLEPTICS
13.4 Risk of side-effects
CHAPTER 14. THE SIDE-EFFECTS OFANTIPSYCHOTIC DRUGS.I. CNS AND NEUROMUSCULAR EFFECTS
14.1 Neuropsychiatrie effects
14.2 Neuromuscular effects
CHAPTER 15. THE SIDE-EFFECTS OF ANTIPSYCHOTIC DRUGS. II. EFFECTS ON OTHER PHYSIOLOGICAL SYSTEMS
15.1 Endocrine and metabolic disorders
15.2 Immunological reactions
15.4 Ophthalmological reactions
15.5 Haematological reactions
15.7 Respiratory reactions
15.8 Gastrointestinal reactions
15.11 Effects on the embryo and newborn
Antipsychotic Drugs and Their Side-Effects
( Neuroscience Perspectives )
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