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Clinical Psychopharmacology: A Practical Approach

Clinical Psychopharmacology: A Practical Approach

Escobar Javier I | Marin Humberto

(2013)

Additional Information

Book Details

Abstract

This book aims to provide comprehensive, up-to-date information on psychotropic drugs and inform clinical decisions for the treatment of mental disorders using a problem-solving approach.In order to accomplish these goals, the book has three central characteristics:More than a textbook, it is meant to serve as a practical tool for professionals working in the mental health field.

Table of Contents

Section Title Page Action Price
Contents xi
Preface vii
Chapter 1 Absorption, Transformation, and Elimination of Psychotropic Medications 1
1.1 Absorption 1
1.1.1 Oral administration 1
1.1.2 Sublingual administration (“under the tongue”) 2
1.1.3 Transdermal administration 3
1.1.4 Respiratory administration, intranasal or inhalation 3
1.1.5 Short-acting injectable forms 3
1.1.6 Long-acting injectable preparations 3
1.2 Distribution: Differences Between Serum and Cerebrospinal Fluid/Brain Concentrations 4
1.3 Metabolism and Elimination 4
1.3.1 Phase I metabolism 5
1.3.1.1 Inhibition and induction of CYP450 enzymes 6
1.3.2 Phase II metabolism (conjugation) 6
1.3.2.1 Inhibition and induction of conjugation enzymes 7
1.4 Additional Concepts in Pharmacokinetics 7
1.4.1 Steady state 7
1.4.2 Dose–response relationship 8
1.4.3 Therapeutic margin 8
Chapter 2 Neurotransmitters, Receptors, and Transporters 9
2.1 Main Types of Receptors in the Brain 9
2.1.1 Division of receptors according to the processes they trigger 10
2.1.1.1 Ionotropic receptors 10
2.1.1.2 Metabotropic receptors 10
2.1.1.3 Receptor tyrosine kinases 10
2.1.1.4 Nuclear receptors 10
2.1.1.5 Receptors associated with neurotransmitter pumps 10
2.1.2 Division of receptors according to their localization in pre- or post-synaptic neurons 10
2.1.2.1 Autoreceptors 11
2.1.2.2 Heteroreceptors 11
2.2 Neurotransmitters 11
2.2.1 Serotonin 12
2.2.1.1 Types of serotonin receptors 12
2.2.2 Dopamine 13
2.2.2.1 Types of dopamine receptors 14
2.2.3 Norepinephrine 15
2.2.3.1 Types of norepinephrine receptors 15
2.2.4 Acetylcholine 16
2.2.4.1 Types of cholinergic receptors 16
2.2.5 Glutamate 17
2.2.5.1 Glutamate activity and neuroplasticity 17
2.2.5.2 Types of glutamate receptors 18
2.2.6 GABA 19
2.2.6.1 Types of GABA receptors 19
2.2.7 Histamine 20
2.2.7.1 Types of histamine receptors 20
2.3 Neurotransmitter Reuptake Transporters 21
References 22
Chapter 3 Antipsychotics: A General View of Therapeutic and Adverse Effects 23
3.1 Classic Antipsychotics 23
3.2 New Antipsychotics 24
3.3 Are the New Antipsychotics Clinically Different from the Old Ones? 27
3.4 Current Concepts Regarding Antipsychotic Action and the D2 Receptor 29
3.5 Comparison Between Typical and Atypical Antipsychotics 30
3.5.1 Are there differences in the general efficacy and effectiveness of typical and atypical antipsychotics? 30
3.5.2 Are there differences in the cognitive effects of typical and atypical antipsychotics? 32
3.5.3 Are there differences in the acute toxicity of typical and atypical antipsychotics? 33
3.6 Metabolic Side Effects of Antipsychotic Drugs 33
3.6.1 Weight gain risk with antipsychotics 35
3.6.2 Antipsychotic-induced diabetes mellitus and metabolic syndrome 37
3.7 Extrapyramidal Symptoms of Antipsychotics 39
3.7.1 Are there any differences in the risk for EPS among typical and atypical antipsychotics? 39
3.7.2 Acute dystonia 42
3.7.3 Parkinsonism (slowness, tremor, and rigidity) 43
3.7.4 Akathisia 43
3.7.4.1 Clozapine 44
3.7.4.2 Risperidone 44
3.7.4.3 Olanzapine 44
3.7.4.4 Quetiapine 45
3.7.4.5 Ziprasidone 45
3.7.4.6 Aripiprazole 45
3.7.4.7 Recently introduced new antipsychotics (paliperidone, iloperidone, asenapine, and lurasidone) 45
3.7.4.8 Management of akathisia 45
3.7.5 Tardive dyskinesia 46
3.8 Neuroleptic Malignant Syndrome 47
3.9 Catatonia 49
3.10 Antipsychotic-Induced Hyperprolactinemia 49
3.11 Sexual Side Effects of Antipsychotics 51
3.12 Antihistamine Adverse Effects of Antipsychotics 52
3.13 Anticholinergic Adverse Effects of Antipsychotics: Cognitive and Peripheral 53
3.14 Antipsychotics and the Risk of Seizures 54
3.15 Vascular Side Effects of Antipsychotics 55
3.16 Antipsychotics and the Risk of Malignant Arrythmia and Sudden Cardiac Death 55
3.17 Antipsychotics and Increased Morbidity and Mortality in Patients with Dementia 57
3.18 Antipsychotics and Suicide 59
3.19 Antipsychotics and the Risk of Cancer 60
References 60
Chapter 4 Description of Individual Antipsychotics 67
4.1 Typical Antipsychotics 67
4.1.1 Chlorpromazine 68
4.1.2 Haloperidol 69
4.1.3 Loxapine 70
4.1.4 Molindone 71
4.1.5 Perphenazine 72
4.1.6 Pimozide 72
4.1.7 Other high-potency D2 blockers: Fluphenazine, thiothixene, and trifluoperazine 73
4.1.8 Antipsychotics to avoid: Mesoridazine and thioridazine 73
4.1.9 “Hidden” antipsychotics: Metoclopramide and prochlorperazine 73
4.2 Atypical Antipsychotics 74
4.2.1 Clozapine 74
4.2.1.1 Side effects of clozapine 75
4.2.2 Risperidone and paliperidone 78
4.2.3 Olanzapine 78
4.2.4 Quetiapine 79
4.2.5 Ziprasidone 81
4.2.6 Aripiprazole 81
4.2.7 Iloperidone 83
4.2.8 Asenapine 83
4.2.9 Lurasidone 84
References 85
Chapter 5 Treatment of Schizophrenia with Antipsychotic Medications 87
5.1 Choice of an Antipsychotic for the Initial Treatment of Schizophrenia 87
5.2 Dosing in the Initial Antipsychotic Treatment of Schizophrenia 88
5.3 How Long Does It Take to Respond to an Antipsychotic? 88
5.4 Monitoring Antipsychotic Treatment 90
5.5 Maintenance of Antipsychotic Treatment of Schizophrenia 90
5.6 Combination of Antipsychotic Drugs in Schizophrenia (“Polypharmacy”) 91
5.7 Pharmacological Management of Treatment-Resistant Schizophrenia 92
5.8 Use of Long-Acting Injectable Antipsychotics in Schizophrenia 92
References 93
Chapter 6 Antidepressants: Selective Serotonin Reuptake Inhibitors and Serotonin–Norepinephrine Reuptake Inhibitors 95
6.1 Introduction 95
6.2 Pharmacodynamics of SSRIs and SNRIs (Receptor Affinity) 96
6.3 Pharmacokinetics of SSRIs and SNRIs 97
6.4 Use of SSRIs in Mental Disorders 98
6.4.1 SSRIs in the treatment of depression 99
6.4.2 SSRIs in the treatment of anxiety disorders 99
6.4.3 Use of SSRIs in other disorders or conditions 100
6.5 Use of SNRIs in Mental Disorders 100
6.6 Dosing of SSRIs and SNRIs 101
6.7 Adverse Effects of SSRIs and SNRIs 101
6.7.1 Antidepressants and the risk of suicide 102
6.7.2 Serotonergic side effects of SSRIs and SNRIs 104
6.7.2.1 Mental (cognitive) 104
6.7.2.2 Neuromuscular 105
6.7.2.3 Gastrointestinal 105
6.7.2.4 Sexual 106
6.7.2.5 Syndrome of inappropriate antidiuretic hormone secretion 106
6.7.2.6 Headaches 107
6.7.2.7 Weight changes 107
6.7.2.8 Risk of bleeding 107
6.7.2.9 QT prolongation and risk of malignant arrhythmia 108
6.7.2.10 Osteoporosis and risk of fractures 109
6.7.2.11 Diabetes 109
6.7.2.12 Cataracts 110
6.7.3 Noradrenergic side effects of SNRIs 110
6.8 Discontinuation Syndrome with SSRIs and SNRIs 110
6.9 Toxicity of SSRIs and SNRIs and Serotonin Syndrome 111
6.10 Precautions with SSRIs and SNRIs 112
6.11 Use of SSRIs and SNRIs During Pregnancy and Lactation 113
6.11.1 SSRIs and SNRIs and risk for preeclampsia 114
References 115
Chapter 7 Bupropion 119
7.1 Introduction 119
7.2 Pharmacology 120
7.2.1 Pharmacokinetics 121
7.3 Approved Indications and Other Possible Uses 121
7.3.1 Major depressive disorder 122
7.3.2 Bupropion as an add-on in depression 122
7.3.3 Anxiety disorders 123
7.3.4 Seasonal affective disorder 123
7.3.5 Smoking cessation 123
7.3.6 Attention deficit hyperactivity disorder 123
7.3.7 Sexual dysfunction 124
7.3.8 Weight loss 124
7.3.9 Addictions (cocaine and amphetamines) 124
7.3.10 Restless legs syndrome 125
7.4 Dosing and Available Forms of Bupropion 125
7.5 Side Effects and Adverse Reactions 125
7.5.1 Risk of seizures 126
7.6 Contraindications, Warnings, and Precautions 126
7.7 Use of Bupropion During Pregnancy 127
References 127
Chapter 8 Mirtazapine, Trazodone, and Nefazodone 129
8.1 Mirtazapine 129
8.1.1 Pharmacokinetics 130
8.1.2 Indications and uses 130
8.1.2.1 Depression 130
8.1.2.2 Anxiety disorders 130
8.1.2.3 Emesis 131
8.1.2.4 Antipsychotic-induced akathisia 131
8.1.2.5 Neuropathic pain 131
8.1.2.6 Add-on to antipsychotics in schizophrenia 131
8.1.2.7 Insomnia 132
8.1.3 Dosing 132
8.1.4 Side effects, adverse reactions, warnings, and precautions 132
8.1.5 Use of mirtazapine during pregnancy 133
8.2 Trazodone 133
8.2.1 Pharmacokinetics 134
8.2.2 Indications and uses 134
8.2.2.1 Depression 134
8.2.2.2 Anxiety disorders 134
8.2.2.3 Insomnia 135
8.2.2.4 Other uses of trazodone 135
8.2.3 Side effects and adverse reactions 135
8.3 Nefazodone 136
8.3.1 Pharmacokinetics 137
8.3.2 Indications and uses 137
8.3.3 Dosing 137
8.3.4 Adverse reactions, side effects, and precautions 137
References 138
Chapter 9 Monoamine Oxidase Inhibitors and Tricyclic Antidepressants 141
9.1 Monoamine Oxidase Inhibitors 141
9.1.1 Pharmacokinetics of the nonselective irreversible MAOIs: Isocarboxazid, phenelzine, and tranylcypromine 143
9.1.2 Partially selective irreversible transdermal MAOI: Selegiline 144
9.1.3 Side effects and adverse reactions 144
9.1.4 Precautions 145
9.1.5 Hypertensive crisis 145
9.1.6 Use of MAOIs during pregnancy 145
9.1.7 What is the role of MAOIs in today’s clinical practice? 145
9.2 Tricyclic Antidepressants 146
9.2.1 General characteristics and classification 146
9.2.1.1 Receptor binding profile 146
9.2.2 Pharmacokinetics 148
9.2.3 Dosing 148
9.2.3.1 Therapeutic drug monitoring 149
9.2.4 Side effects 149
9.2.5 Serotonin syndrome with TCAs 150
9.2.6 Precautions with TCAs in liver disease 150
9.2.7 Contraindications 150
9.2.8 Toxicity 150
9.2.9 Use of TCAs during pregnancy 151
9.2.10 What is the role of TCAs in today’s clinical practice? 152
References 153
Chapter 10 Individualized Treatment of Depression 155
10.1 Patient Factors to Consider 156
10.1.1 Depressive symptom profile 156
10.1.2 Patient’s and family histories of response 157
10.1.3 Comorbid psychiatric conditions 157
10.1.4 Medical conditions 158
10.1.5 Concurrent medications and supplements 158
10.1.6 Tolerability of side effects 159
10.1.7 Medication adherence 159
10.1.8 Cost and access to medication 160
10.2 Second-Generation Antidepressants: Doses and Duration 160
10.3 Hypnotics and Other Symptom-Specific Medications 162
10.4 Partial Response to Antidepressant Treatment: What to Do? 162
10.4.1 Give the antidepressant more time 163
10.4.2 Add another antidepressant 164
10.4.3 Add symptom-specific medications 164
10.4.4 Switch antidepressants 165
10.5 No Response to Initial Antidepressant Treatment: What to Do? 165
10.6 What About Adding Atypical Antipsychotics in the Initial Treatment of Depression? 165
10.7 Other Non-Antidepressant Drugs Recently Tried in Depression 166
10.7.1 Buspirone 167
10.7.2 Methylfloate (Levomefolic acid) 167
10.7.3 Ketamine 167
10.8 Once the Patient Gets Better, How to Stop Antidepressant Treatment? 168
References 168
Chapter 11 Benzodiazepines, Buspirone, and Miscellaneous Medications Used in Anxiety Disorders 171
11.1 Benzodiazepines 171
11.1.1 Pharmacology 172
11.1.1.1 Pharmacokinetics and drug–drug interactions 173
11.1.2 Adverse effects 175
11.1.2.1 Psychomotor effects 175
11.1.2.2 Abuse/dependence 176
11.1.2.3 Sleep-related behaviors and automatisms 176
11.1.2.4 Disinhibition syndrome 176
11.1.2.5 Potential for criminal use 176
11.1.3 Toxicity 177
11.1.4 Selection and use 177
11.1.4.1 Equivalent doses of benzodiazepines and switching between benzodiazepines 179
11.1.5 Indications 180
11.1.5.1 Generalized anxiety disorder 180
11.1.5.2 Panic disorder 180
11.1.5.3 Social anxiety disorder 181
11.1.6 Warnings and contraindications 182
11.2 Buspirone 182
11.2.1 Pharmacology 182
11.2.2 Clinical uses 183
11.3 Antiepileptic Drugs 184
11.3.1 Pregabalin 184
11.3.2 Gabapentin 185
11.4 Antihistamines 186
11.5 Prazosin for Nightmares in Post-Traumatic Stress Disorder 186
11.6 Do Antipsychotics Have a Role in Anxiety? 187
11.7 Beta-Blockers 187
References 188
Chapter 12 Medication Treatment of Anxiety Disorders 191
General Considerations Prior to Starting Drug Treatment 191
Other Considerations 191
12.1 Approved and Potential Uses of Antidepressants and Other Medications 192
12.1.1 SSRIs 192
12.1.2 SNRIs 193
12.1.3 Mirtazapine and trazodone 193
12.1.4 Bupropion 193
12.1.5 TCAs and MAOIs 193
12.1.6 Benzodiazepines 194
12.1.7 Antihistamines and anticonvulsants 194
12.1.8 Antipsychotics 194
12.2 Drug Treatment of Individual Anxiety Disorders 194
12.2.1 Generalized anxiety disorder 194
12.2.2 Social anxiety disorder 195
12.2.3 Panic disorder 196
12.2.4 Specific phobias 196
12.2.5 Post-traumatic stress disorder 196
12.2.6 Obsessive–compulsive disorder 197
References 198
Chapter 13 Medications Used in the Treatment of Mania 199
13.1 Lithium 199
13.1.1 Toxicity 201
13.1.2 Adverse effects 201
13.1.3 Drug–drug interactions 203
13.1.4 Dosing 204
13.2 Antipsychotics 205
13.3 Carbamazepine 206
13.3.1 Dosing 208
13.4 Oxcarbazepine 209
13.5 Valproic Acid (Divalproex, Valproate) 209
13.5.1 Adverse effects 210
13.5.2 Dosing 211
13.6 Tamoxifen 211
References 212
Chapter 14 Medications Used in Bipolar Depression, Mixed States, and Rapid Cycling 213
14.1 Electroconvulsive Therapy 213
14.2 Lithium 215
14.3 Quetiapine 215
14.4 Lamotrigine 216
14.5 Valproate 217
14.6 Antidepressants 217
14.7 Ketamine in Bipolar and Treatment-Resistant Depression 219
14.8 Pharmacological Treatment of Mixed States and Rapid Cycling Bipolar Disorder 219
References 220
Chapter 15 Medications Used in the Treatment of Insomnia 223
15.1 General Rules 223
15.2 Antihistamines as Hypnotics 224
15.3 Sedating Antidepressants (Trazodone and Mirtazapine) 225
15.4 Melatonin Receptor Agonists 225
15.4.1 Melatonin 225
15.4.2 Ramelteon 226
15.5 GABA Receptor Agonists 227
15.5.1 Benzodiazepines 227
15.5.2 GABA hypnotics 228
15.5.2.1 Clinical effects 228
15.5.2.2 Dosing and timing 229
15.5.2.3 Tolerance to the hypnotic effect 230
15.5.2.4 Unintended overdose 230
15.5.2.5 Adverse effects and risks 230
15.5.2.6 Sleep-related behaviors 231
References 232
Chapter 16 Medications Used in the Treatment of Attention Disorders 235
16.1 Stimulant Medications (Psychostimulants) 235
16.1.1 Pharmacokinetics and drug–drug interactions 236
16.1.2 Adverse effects 237
16.1.3 Clinical use 239
16.2 Atomoxetine 241
16.3 Bupropion 242
16.4 Modafinil 242
16.5 α2-Adrenergic Agonists (Guanfacine and Clonidine) 243
References 244
Chapter 17 Medications Used in the Treatment of Dementia 245
17.1 Side Effects 246
17.2 Pharmacokinetics 247
17.3 Pointers for Clinical Use 247
References 247
Chapter 18 Medications Used in Smoking Cessation and Alcohol Use Disorders 249
18.1 Medications Used in the Treatment of Nicotine Dependence (Smoking Cessation) 249
18.1.1 Varenicline 250
18.1.2 Bupropion 251
18.1.3 Nicotine replacement therapy 251
18.1.3.1 Nicotine gum 252
18.1.3.2 Nicotine lozenges 252
18.1.3.3 Nicotine nasal spray 253
18.1.3.4 Nicotine inhaler 253
18.1.3.5 Nicotine patch 253
18.2 Medications Used in the Treatment of Alcohol Use Disorders 254
18.2.1 Disulfiram 254
18.2.2 Naltrexone 255
18.2.3 Acamprosate 257
References 257
Chapter 19 Drug–Drug Interactions 259
19.1 Pharmacokinetic Drug–Drug Interactions 260
19.1.1 DDIs during absorption of psychotropic medications 262
19.1.2 DDIs during excretion of psychotropic medications 262
19.1.3 DDIs involving transport proteins 263
19.1.4 DDIs involving inhibition or induction of oxidative CYP450 enzymes 263
19.1.5 DDIs involving inhibition or induction of conjugation enzymes (phase II metabolism) 270
19.2 Pharmacodynamic DDIs Involving Psychotropic Drugs 272
19.3 Drug–Drug Interactions due to Cumulative Toxicity 273
19.4 Drug–Drug Interactions Related to Food Supplements and Substances of Abuse 273
Appendix: DDI Review Questions 275
Answers to DDI Review Questions 278
References 278
About the Authors 281
Index of Psychotropic Drugs, Substances, and Supplements 283