| Section | Topics | Pages |
| Abstract | 1 | |
| 1. | Introduction | 3 |
| 2. | Neurotransmitter (NT) Reuptake Inhibitors | 4 |
| 2.1. | Serotonin-Norepinephrine Reuptake Inhibitors | 4 |
| 2.1.1. | Imipramine and Amitriptyline | 4, 5 |
| 2.1.2 | Clomipramine | 6 |
| 2.1.3 | Venlafaxine | 6, 7 |
| 2.1.4. | Doxepin | 7 |
| 2.2. | Selective Norepinephrine Reuptake Inhibitors | 7 |
| 2.2.1 | Maprotiline | 7, 8 |
| 2.2.2. | Atomoxetine | 8 |
| 2.3. | Selective Serotonin Reuptake Inhibitors | 9 |
| 2.3.1. | Fluoxetine | 9 |
| 2.3.2. | Citalopram/Escitalopram | 9, 10 |
| 2.3.3. | Sertraline | 10 |
| 2.3.4. | Fenfluramine | 10, 11 |
| 3. | Dopaminergic, Serotonergic, Adrenergic and N-methyl-D-aspartate (NMDA) Receptor Blockers | 11 |
| 3.1. | Loxapine/Amoxapine | 11 |
| 3.2. | Clozapine | 11, 12 |
| 3.3. | Mianserin | 12 |
| 3.4. | Mirtazapine | 12, 13 |
| 3.5. | Olanzapine | 13 |
| 3.6. | Ketamine | 14 |
| 3.7. | Chlorpromazine | 14, 15 |
| 3.8. | Promazine | 15 |
| 4. | Histamine-1 Receptor Antagonists | 16 |
| 4.1. | Diphenhydramine | 16 |
| 4.2. | Azelastine | 16, 17 |
| 4.3. | Prometazine | 17 |
| 5. | Opioid-mu-Receptor Agonists | 17 |
| 5.1. | Morphine/Codeine | 17, 18 |
| 5.2. | Tramadol | 18 |
| 5.3. | Propoxyphene | 19 |
| 5.4. | Meperidine | 19 |
| 6. | Calcium-Channel Blockers | 20 |
| 6.1. | Verapamil | 20 |
| 6.2. | Diltiazem | 20 |
| 6.3. | Amiodarone | 21 |
| 7. | Drugs That Act at Sodiuzm Channels | 21 |
| 7.1. | Local Anesthetics | 21 |
| 7.1.1 | Lidocaine | 21 |
| 8. | Drugs That Act at GABAnergic Receptors | 22 |
| 8.1. | Zopiclone | 22 |
| 9. | Muscarinic-Receptor Blockers | 22 |
| 9.1. | Tolterodine/Fesoterodine | 22, 23 |
| 9.2. | Oxybutynin | 23 |
| 10. | “If” Channel Blockers | 23 |
| 10.1. | Ivabradine | 23, 24 |
| 11. | Drugs That Act as Enzyme Inhibitors | 24 |
| 11.1. | Sildenafil | 24 |
| 12. | Drugs That Act on Microorganisms | 24 |
| 12.1. | Chloroquine/Hydroxychloroquine | 24–26 |
| 13. | Anticancer Drugs | 26 |
| 13.1. | Imatinib | 26 |
| 13.2. | Dacarbazine | 26, 27 |
| 13.3. | Tamoxifen | 27 |
| 13.4. | Tormifene | 27, 28 |
| 14. | Metabolic N-dealkylation and N-oxidation | 28 |
| 14.1. | Metabolic N-dealkylation | 28, 29 |
| 14.1.1. | Focused N-dealkylation cases | 30 |
| 14.1.1.1. | Loss of Pharmacologic Activity | 30 |
| 14.1.1.2. | Modification of Receptor Inhibition Selectivity | 30, 31 |
| 14.1.1.3. | Activation of Prodrugs | 31 |
| 14.1.1.4. | Potential Drug Candidates (Metabolite Drugs) | 31 |
| 14.2. | N-Oxidation Of Tertiary-Alkylamino-Moiety-Containing Drug | 32 |
| 15. | Conclusions | 33 |