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