ANTIDEPRESSANTS - SWAP n STOP

AGOMELATINE BUPROPION

AGOMELATINE
BUPROPION
CLOMIPRAMINE Cross-taper cautiously Cross-taper cautiously
FLUOXETINE Stop A. 4-7ºd: start B
FLUVOXAMINE Taper, stop A; 4ºd: start B Direct switch
MAOIs (other than moclobemide) Cross-taper cautiously
FROM ("A")

MOCLOBEMIDE T
MIRTAZAPINE Cross-taper cautiously
REBOXETINE Cross-taper cautiously Direct switch
TRAZODONE Cross-taper cautiously

SSRI (other than fluoxetine and fluvoxamine), SNRI

Cross-taper cautiously Direct switch
and VORTIOXETINE

ADTC (except clomipramine) Cross-taper cautiously Halve A, add B, then slow withdraw A

STOPPING Abrupt 4 weeks

 TO ("B")

CLOMIPRAMINE FLUOXETINE FLUVOXAMINE

Stop A
Cross-taper cautiously Cross-taper cautiously Cross-taper cautiously
Taper and stop A. Start B at 10mg/d Taper and stop A; start B low dose
Stop A. 2ºw: start B low dose Stop A. 4-7ºd: start B
Taper, stop A. Start B low dose Direct switch
Taper, stop A; 2ºw: sta
Taper, stop; 24ºh: start B

Cross-taper cautiously Cross-taper cautiously Cross-taper cautiously

Taper, stop A. Start B low dose Direct switch Direct switch

Direct switch Halve A, add B, then slow withdraw B Cross-taper cautiously

4 weeks 20mg: abrupt; >20mg: 2 weeks 4 weeks

 TO ("B")
MAOIs (other than
moclobemide)
Taper and stop A; 2ºw: start B
Taper and stop A; 3ºw: start B
Stop A. 5-6ºw: start B
Stop A. 1ºw: start B
Taper, stop A; 2ºw: start B (clomipramine: 3ºw)
Taper, stop A. 24ºh: start B
Taper, stop A; 2ºw: start B
Taper, stop A; 1ºw: start B
Taper, stop A; 1ºw: start B
Taper, stop A; 2ºw: start B
4 weeks
MOCLOBEMIDE MIRTAZAPINE REBOXETINE
Stop A, start B
Taper and stop A; start B
Cross-taper cautiously Cross-taper cautiously
Stop A. 5-6ºw: start B
Taper and stop A. 1ºw: start B
Taper, stop MAOI;
Taper and stop A. 1ºw: start B
Cross-taper cautiously
Cross-taper cautiously
Taper and stop A. 1ºw: start B Cross-taper cautiously Cross-taper cautiously
Taper and stop A. 1ºw: start B Cross-taper cautiously Cross-taper cautiously
4 weeks 4 weeks 4 weeks
 SSRI (other than fluoxetine and fluvoxamine), SNRI and
TRAZODONE ADTC (except clomipramine)
VORTIOXETINE

Cross-taper cautiously
Cross-taper cautiously
Taper, stop A. Start B low dose
Cross-taper cautiously
Stop A. 4-7ºd: start B low dose Stop A. 4-7ºd: start B low dose
Direct switch Cross-taper cautiously

Taper, stop MAOI; 24ºh: start B

Cross-taper cautiously
Cross-taper cautiously Cross-taper cautiously

Cross-taper cautiously Direct switch Cross-taper cautiously

SNRI: Cross-taper cautiously. The rest: Halve A, add B,

Halve A, add B, then slow withdraw B Direct switch
then slow withdraw B
4 weeks 4 weeks 4 weeks
 CyP
INHIBIDORES SELECTIVOS RECAPTACION SEROTONINA (ISR
SERTRALINA 2D6… 3A4
PAROXETINA 2D6… 2C9
ESCITALOPRAM 2C19… 2D6, 3A4
CITALOPRAM 2C19… 2D6, 3A4
FLUOXETINA 2D6, 2C19, 3A4
FLUVOXAMINA 1A2… 2D6
INHIBIDORES RECAPTACION SEROTONINA y NORADRENALINA
VENLAFAXINA 2D6… 3A4
DESVENLAFAXINA 3A4
DULOXETINA 1A2, 2D6
ANTIDEPRESIVOS HETEROCICLICOS
AMITRIPTILINA 2D6, 1A2, 2C19
IMIPRAMINA 2D6, 1A2, 3A4
CLOMIPRAMINA 2D6, 1A2, 2C19
TRIMIPRAMINA 2D6, 2C19, 2C9
DOXEPINA 2D6, 1A2, 2C19
NORTRIPTILINA 2D6
AMOXAPINA 2D6
MIANSERINA 1A2, 2D6
MIRTAZAPINA 1A2, 2D6, 3A4
MAPROTILINA 2D6, 1A2, 2C19, 3A4
OTROS ANTIDEPRESIVOS
BUPROPION 2B6…1A2, 2A9, 2C19, 2E1 3A4
REBOXETINA 3A4
ATOMOXETINA 2D6
VILAZODONA 3A4
TRAZODONA 3A4, 2D6
NEFAZODONA 3A4
VORTIOXETINA 2D6… 3A4, 2C9
MOCLOBEMIDA 2C19… 2D6
TRANILCIPROMINA -
AGOMELATINA 1A2, 2C9, 2C19
 Metabolito (negrita: activos) (VM) f (%) Tmax (h) Vd (L/kg) Cl (mL/min)
INHIBIDORES SELECTIVOS RECAPTACION SEROTONINA (ISRS, SSRI)
Nor-X, OH-X 44 6--8 >20 23
Inactivos 50 4--5 3--28 40
Nor-X 80 4 12--26 40
Nor-X, N-óxido-X, didesmetil- 80 1--4 9--17 -
Nor-X (10 días) 80 6--8 12--42 16
Inactivos. 94 1.5-8 18-40 9
INHIBIDORES RECAPTACION SEROTONINA y NORADRENALINA (IRSN, SNRI)
Desvenlafaxina (Nor-X), N-desmetil-X 92 2-2.5 6--8 0.5-2.5
N-O-didesmetil-venlafaxina 80 7.5 3.4 -
Inactivos 32-80 6 - 33-261
ANTIDEPRESIVOS HETEROCICLICOS
Nortriptilina, 10-OH-X 37-59 3--4 12--16 11--15
Desipramina (nor-X), 2-OH-X (17-27h) 19-35 0.5-1 15-31 11--19
Nor-X (36h), 8-OH-X 40-60 3--4 12--17 17
Nor-X, 2-OH-X, 2-OH-nor-X 80 1--6 17--48 13--16
Nor-X (34h), 8-OH-X 17-37 1--4 12--28 11--17
10-OH-X (10h) 45-55 4--8 20-57 9--12
8-OH-X
Nor-X, 8-OH-X 30-70 2--3 10--30 17
Nor-X, 8-OH-X, N-óxido-X 50 2.2-2.9 - -
Nor-X, 3-OH-X 37 8 15-25 4--15
OTROS ANTIDEPRESIVOS
OH-X, treo-OH-X 87 2.5-3 25 200
O-desetil-X 60 - - -
4-OH-X (5h)
Inactivo
N-clorofenil-piperacina (mCPP, 4-8h) - 1--2 1-1.5 1.7
N-clorofenil-piperacina (mCPP, 4-8h), OH-X (2-4h)
Inactivo 75 7--11 2600 33
Inactivos 70 1--2 1.1-1.3 20-50
Inactivos - 1--3 1--5 7--21
Nor-X, OH-X <5 - 0.7 -
T1/2 (h) U (%) FP (%)
f: biodisponibilidad;
24 0 95 Tmax: tiempo hasta Cmax;
Vd: volumen de distribucion,
9--16 2 95
T1/2: vida media de
25-30 <5 <80 eliminacion,
35 20 71--77 U: eliminacion urinaria,
FP: fijacion a proteinas.
4 10 94
17-22 1 80 NOR = desmetil-
OH = hidroxi.
2.7-4 5 30
11 45 30
8--17 <5 96

9--36 <1 94
11--23 <2 95
12--36 <1 97
9--12 0 95
11--23 0 -
18-70 3 90

6--40 <5 90
20-40 4 85
27-58 <1 90

20 <1 84
13 90 97

5--9 <1 90

<5 33 98
2--4 <1 50
1.5-3 <2 50-60
1--2 <5 95
 CyP
ANTIPSICOTICOS DE PRIMERA G
CLORPROMACINA 2D6… 1A2

FLUFENAZINA (decanoato) -

LEVOMEPROMACINA -
PERFENACINA -
TRIFLUOROPERAZINA -

HALOPERIDOL 2D6… 1A2

TIAPRIDA -
AMILSUPIRIDA -
SULPIRIDA -

ZUCLOPENTIXOL (decanoato) 2D6… 1A2

TIORIDACINA 2D6
PIMOZIDA 3A4
ANTIPSICOTICOS DE SEGUNDA G
CLOZAPINA 1A2… 2C19, 3A4, 2D6
OLANZAPINA 1A2… 2D6
QUETIAPINA 3A4
RISPERIDONA 2D6, 3A4
PALIPERIDONA (oral) 3A4… 2D6
LURASIDONA 3A4

ZIPRASIDONA (oral/depot) 3A4, 1A2

SERTINDOL 2D6, 3A4

ASENAPINA 1A2… 2D6, 3A4 (inh 2D6 debil)
LOXAPINA Multiples vias
ANTIPSICOTICOS DE TERCERA GENERACION: AGONIST
ARIPIPRAZOL 2D6, 3A4
CARIPRAZINA 3A4, 2D6
 Metabolito (negrita: activos) (VM) f (%) Tmax (h) Vd (L/kg)
ANTIPSICOTICOS DE PRIMERA GENERACION (AP1G)
- 25-65 2--4 (50-300ng/mL) 10--35

- - 1--4 -

- 50 1--4 20-45
- 30-40 3--5 10--36
- 1.2-3.1 2--4 10
oral: 3-6h; IM: 30 minutos (5-
OH-X 40-80 15-20
20ng/mL)
- 75 2 1.5
- 48 2--6 6
- 25-35 3 1

10--60 2--4 10
- 40-50 6 20-40
ANTIPSICOTICOS DE SEGUNDA GENERACION (AP2G)
Nor-X 50 2.5 15-30
Nor-X, 2-OH-X 50 6.5 -
Varios inactivos; 2 activos (Nor-X) 9 1.4 10
9-OH-X (paliperidona) 75-90 1--2 1.1
- 28 24 487
ID-14283, ID-14326, ID-20219, ID-20220 - 2 6000
60 horas / 100
Varios inactivos 6-8horas /0.5-1hora -
horas
Dehidro-, Nor-X (desalquil) - 10 20
Nor-X 35 1 24
Amoxapina - 2 -
ANTIPSICOTICOS DE TERCERA GENERACION: AGONISTAS DOPAMINERGICOS PARCIALES (AP-DPA)
Dehidro-, OPC-3373 87 3--5 5
Desmetil- (DCAR), didesmetil- (DDCAR) - 3--8 465-1568
 Cl (mL/min) T1/2 (h) U (%) FP (%)

6--12 12--36 <1 98

oral: 13-58h,
- <10 >90
depot: 14 días

- 15-30 1 -
26 10--20 <1 >90
147 7--18 <5 >99

9--15 15-30 0 10

280 2.5-4 75 <10

300 12 90 16
126 7 95 14--40

- 10--30
- 30-150 4 -

26 8--12 <1 >90

- 34 43 93
- 7 1 83
0.8-5 3 5 85
- 24 59 74
- 20-40 5 99

- 9 - -

- 72 4 100
52 24 5--16 95
- 6--8 - 97
DPA)
- 75-146 1 99
- 1--3 1.2 92-97
 Efecto clínico
AP 1ºG (Ki) Receptores dopaminergicos Receptores serotonine
D2-R D3-R D4-R 5HT-1A 5HT-2A
CLOPROMACINA 7.2 6.9 32.3 3115 2.75
FENOTIACINAS

PROMETACINA 260 190 - 1485 20

CIAMEMACINA 5.8 2.5 5.3 520 1.5
PERFENACINA 0.765 0.13 17 420 5.6
FLUPENTIXOL 0.35 1.75 66 8030 87.5
TIOTIXENO 0.7 93 275 650 70
CLORPROTIXENO 4.3 3.3 0.65 185 0.35
HALOPERIDOL 0.7 0.2 7 1927 53
FENONAS
BUTIRO-

BENPERIDOL 0.027 - 0.06 - 3.75

MELPERONA 195 350 555 2200 230
ESPIPERONA 0.15 0.35 1.4 17.3 1.17
AMISULPIRIDA 3 3.5 2370 >10000 8304

Efecto clínico
AP 2ºG (Ki) Receptores dopaminergicos Receptores serotonine
D2-R D3-R D4-R 5HT-1A 5HT-2A
CLOZAPINA 160 270 26 125 5.4
Norclozapina 101 194 64 14 11
PINAS

OLANZAPINA 55 50 25 2390 13
QUETIAPINA 245 410 1202 375 98
Norquetiapina 196 570 1297 45 48
ASENAPINA 1.3 0.42 1.1 2.5 0.06
RISPERIDONA 3.6 3.6 4.7 423 0.17
PALIPERIDONA 1.6 3.5 54 617 1.1
DONAS

LURASIDONA 1.68 15.7 30 6.75 2

ZIPRASIDONA 4.8 4.6 52.5 40.5 0.75
ILOPERIDONA 6.3 7.1 25 168 5.6
ARIPIPRAZOL 3.3 5.25 279 3.65 20
DPAs

BREXPIPRAZOL 0.3 1.1 6.3 0.12 0.47

CARIPRAZINA 0.5 0.085 - 2.6 19

D2-R D3-R D4-R 5HT-1A 5HT-2A

CLOZAPINA 160 270 26 125 5.4
CIAMEMACINA 5.8 2.5 5.3 520 1.5
CLORPROTIXENO 4.3 3.3 0.65 185 0.35
OLANZAPINA 55 50 25 2390 13
Norquetiapina 196 570 1297 45 48
CLOPROMACINA 7.2 6.9 32.3 3115 2.75
Norclozapina 101 194 64 14 11
ZIPRASIDONA 4.8 4.6 52.5 40.5 0.75
QUETIAPINA 245 410 1202 375 98
PERFENACINA 0.765 0.13 17 420 5.6
 TIOTIXENO 0.7 93 275 650 70
ARIPIPRAZOL 3.3 5.25 279 3.65 20
FLUPENTIXOL 0.35 1.75 66 8030 87.5
BREXPIPRAZOL 0.3 1.1 6.3 0.12 0.47
RISPERIDONA 3.6 3.6 4.7 423 0.17
ESPIPERONA 0.15 0.35 1.4 17.3 1.17
BENPERIDOL 0.027 - 0.06 - 3.75
ILOPERIDONA 6.3 7.1 25 168 5.6
ASENAPINA 1.3 0.42 1.1 2.5 0.06
PALIPERIDONA 1.6 3.5 54 617 1.1
CARIPRAZINA 0.5 0.085 - 2.6 19
MELPERONA 195 350 555 2200 230
HALOPERIDOL 0.7 0.2 7 1927 53
LURASIDONA 1.68 15.7 30 6.75 2
AMISULPIRIDA 3 3.5 2370 >10000 8304
ínico
Efectos secundarios
Receptores serotoninergicos
MELTZER
5HT-2C 5HT-7 M1 H1 Alfa-1
25 21 0.4 47 4.25 0.28
6.5 - 0.1 3.3 0,3-1,4 21
12 22 0.3 13 9.3 2.3
130 23 7.3 2000 8 10
102 - 250.0 - 0.86 -
1400 15 100.0 2820 8 20
4.5 5.3 0.1 18.5 2.5 1
>10000 377 75.7 >10000 1800 12
- - 138.9 - - -
2100 580 1.2 >10000 580 180
920 110 7.8 - 270 3.1
>10000 11.5 2768.0 >10000 >10000 >10000

ínico
Efectos secundarios
Receptores serotoninergicos
MELTZER
5HT-2C 5HT-7 M1 H1 Alfa-1
9.5 18 0.03 6.2 1.1 1.6
12 60 0.11 67 3.4 85
18 235 0.24 38 2.8 112
2500 307 0.40 860 6.7 22
107 76 0.24 40 3.5 40
0.03 0.13 0.05 >10000 1 1.2
12 6.6 0.05 - 20 >10000
48 2.7 0.69 >10000 19 2.5
415 0.5 1.19 >10000 >10000 48
6 7.5 0.16 300 75 9
- 22 0.89 - - 0.36
100 25 6.06 6780 45 26
23 3.7 1.57 - 19 2.2
135 111 38.00 >10000 23 155

5HT-2C 5HT-7 M1 H1 Alfa-1

9.5 18 6.2 1.1 1.6
12 22 13 9.3 2.3
4.5 5.3 18.5 2.5 1
18 235 38 2.8 112
107 76 40 3.5 40
25 21 47 4.25 0.28
12 60 67 3.4 85
6 7.5 300 75 9
2500 307 860 6.7 22
130 23 2000 8 10
 1400 15 2820 8 20
100 25 6780 45 26
102 - - 0.86 -
23 3.7 - 19 2.2
12 6.6 - 20 >10000
920 110 - 270 3.1
- - - - -
- 22 - - 0.36
0.03 0.13 >10000 1 1.2
48 2.7 >10000 19 2.5
135 111 >10000 23 155
2100 580 >10000 580 180
>10000 377 >10000 1800 12
415 0.5 >10000 >10000 48
>10000 11.5 >10000 >10000 >10000