Sources: Drug Bioavailability t1/2 (hr) for parent drug (active metabolite) Vd (L/kg unless otherwise specified) Cp (ng/mL) parent drug (active metabolite) Tmax Protein binding Parent drug (active metabolite(s)) Excretion Enzymes responsible for metabolism Enzymes inhibited Tricyclic antidepressant (TCAs) Amitriptyline 30-60% 9-27 (26-30) 100-250 4 hr >90% (93-95%) Urine (18%) Amoxapine 8 (30) 0.9-1.2 200-500 90 mins 90% Urine (60%), faeces (18%) Clomipramine 50% 32 (70) 17 100-250 (230-550) 2-6 hr 97-98% Urine (60%), faeces (32%) CYP2D6 Desipramine 30 125-300 4-6 hr Urine (70%) CYP2D6 Doxepin 18 (30) 11930 150-250 2 hr 80% Urine Imipramine High 12 (30) 18 175-300 1-2 hr 90% Urine Lofepramine 7% 1.7-2.5 (12-24) 30-50 (100-150) 1 hr 99% (92%) Urine CYP450 Maprotiline High 48 200-400 8-24 hr 88% Urine (70%); faeces (30%) Nortriptyline 28-31 21 50-150 7-8.5 hr 93-95% Urine, faeces CYP2D6 Protriptyline High 80 100-150 24-30 hr 92% Urine Tianeptine 99% 2.5-3 0.5-1 1-2 hr 95-96% Urine (65%) Trimipramine 41% 23-24 (30) 17-48 100-300 2 hr 94.9% Urine Monoamine oxidase inhibitors (MAOIs) Moclobemide 55-95% 2 1-2 hr 50% Urine, faeces (Selective serotonin reuptake inhibitors (SSRIs) Citalopram 80% 35-36 12 75-150 2-4 hr 80% Urine (15%) Escitalopram 80% 27-32 20 40-80 3.5-6.5 hr 56% Urine (8%) Fluoxetine 72% 24-72 (single doses), 96-144 (repeated dosing) 12-43 100-500 6-8 hr 95% Urine (15%) CYP2D6 Fluvoxamine 53% 18 25 100-200 3-8 hr 80% Urine (85%) Paroxetine 17 8.7 30-100 5.2-8.1 (IR); 6-10 hr (CR) 93-95% Urine (64%), faeces (36%) CYP2D6 Sertraline 44% 23-26 (66) 25-50 4.5-8.4 hr 98% Urine (12-14% unchanged), faeces (40-45%) Serotonin-norepinephrine reuptake inhibitors (SNRIs) Desvenlafaxine 80% 11 3.4 7.5 hr 30% Urine (69%) CYP3A4 Duloxetine High 11-12 3.4 6 hr (empty stomach), 10 hr (with food) >90% Urine (70%; Others Agomelatine ≥80% 1-2 hr 35 L 1-2 hr 95% Urine (80%) Bupropion 8-24 (IR; 20, 30, 37), 21±7 (XR) 20-47 75-100 2 hr (IR), 3 hr (XR) 84% Urine (87%), faeces (10%) CYP2B6 Mianserin 20-30% 21-61 3 hr 95% Faeces (14-28%), urine (4-7%) CYP2D6 Mirtazapine 50% 20-40 4.5 2 hr 85% Urine (75%), faeces (15%) Nefazodone 20% (decreased by food) 2-4 0.22-0.87 1 hr >99% Urine (55%), faeces (20-30%) CYP3A4 Reboxetine 94% 12-13 26 L (R,R diastereomer), 63 L (S,S diastereomer) 2 hr 97% Urine (78%; 10% as unchanged) CYP3A4 Trazodone 6-10 800-1600 1 hr (without food), 2.5 hr (with food) 85-95% Urine (75%), faeces (25%) CYP2D6 Vilazodone 72% (with food) 25 4-5 hr 96-99% Faeces (2% unchanged), urine (1% unchanged) Vortioxetine 66 2600 L 7-11 hr 98% Urine (59%), faeces (26%)
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Management of depression
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