Table 3.
Neuroleptics metabolized via enzymes of the CYP gene family and other gene‐related enzymes [4, 15, 161, 162]
| Drugs | Pharmacological category | Major substrate | Minor substrate | Inhibitors | Other genes |
|---|---|---|---|---|---|
| Aripiprazole | Atypical antipsychotic | CYP2D6, CYP3A4 | ADRA1A, DRD2, DRD3, HTR1A, HTR2A, HTR2C | ||
| Benperidol | Neuroleptic antipsychotic | DRD2 | |||
| Bromperidol | Antipsychotic, neuroleptic butyrophenone | ABCB1, HTR2, DRD2 | |||
| Chlorpromazine | Phenothiazine antipsychotic | CYP2D6 | CYP1A2, CYP3A4 | CYP2D6, CYP2E1 | ABCB1, ACACA, ADRA1, BDNF, DRD2, DRD3, HTR2C, KCNE2, LEP, NPY, SCN5A |
| Clozapine | Atypical antipsychotic | CYP1A2 | CYP2A6, CYP2C8/9, CYP2C19, CYP2D6, CYP3A4 | CYP1A2, CYP2C8/9, CYP2C19, CYP2D6, CYP2E1, CYP3A4 | ADRA1, ADRB3, APOA5, APOD, APOC3, DRD2, DRD3, DRD4, GNB3, GNAS1, HLAA1, HRH1, HRH2, HTR1A, HTR2A, HTR2C, HTR6, RGS2, SLC6A2, SLC6A4, TNF‐A |
| Droperidol | Atypical antipsychotic | ADRA1,DRD2,KCNE2, KCNH, SCN5A | |||
| Fluphenazine | Typical antipsychotic phenothiazine | CYP2D6 | CYP1A2, CYP2C9, CYP2D6, CYP2E1 | DRD1, DRD2 | |
| Flupenthixol | Typical antipsychotic | DRD1 | |||
| Haloperidol | Typical antipsychotic | CYP2D6, CYP3A4 | CYP1A2 | CYP2D6, CYP3A4 | ABCB1, ADR1A, DRD1, DRD2, DRD4, DTNBP1, GRIN2B, HTR2A, IL1RN, KCNE2, SCN5A |
| Loxapine | Typical antipsychotic | ADR1A, DRD1, DRD2, HTR2A,,KCNE2, SCN5A | |||
| Mesoridazine | Typical antipsychotic | ADR1A, DRD2, KCNE2, SCN5A | |||
| Molindone | Typical antipsychotic | ADRA1, DRD2 | |||
| Olanzapine | Atypical antipsychotic | CYP1A2 | CYP1A2, CYP2D6 | CYP1A2, CYP2C8/9, CYP2C19, CYP2D6, CYP3A4 | ABCB1, ADRA1, ADRB3, APOA5, APOC3, COMT, DRD2, DRD3, GNB3, GRM3, HRH1, HRH2, HTR2A, HTR2C, HTR6, LEP, LEPR, LPL, RGS2, SLC6A2, TNF‐A |
| Paliperidone | Atypical antipsychotic | ADRA1A, ADRA1B, ADRA1D, DRD2, HRH1, HTR2A, | |||
| Perphenazine | Typical antipsychotic phenothiazine | CYP2D6 | CYP1A2, CYP2C8/9, CYP2C19, CYP3A4 | CYP1A2, CYP2D6 | ADRA1A, DRD1, DRD2, DRD3 |
| Periciazine | Typical, antipsychotic phenothiazine, piperidine | CYP2D6, CYP3A4 | DRD1, DRD2 | ||
| Pimozide | Typical antipsychotic | CYP1A2, CYP3A4 | CYP2C19, CYP2D6, CYP2E1, CYP3A4 | ADRA1A, DRD2, KCNE1, KCNE2, KCNQ1, KCNH2, SCN5A | |
| Pipotiazine | Typical antipsychotic | CYP2D6, CYP3A4 | DR | ||
| Prochlorperazine | Typical antipsychotic | ADRA1A, ABCB1, DRD2 | |||
| Quetiapine | Atypical antipsychotic | CYP3A4 | CYP2D6 | ADRA1A, DRD1, DRD2, HRH1, HTR1A, HTR2A, HTR2B, KCNE1, KCNE2, KCNH2, KCNQ1, SCN5A | |
| Risperidone | Atypical antipsychotic | CYP2D6 | CYP2A4 | CYP2D6, CYP3A4 | ABCB1, ADRA1A, ADRA1B, DRD2, DRD3, DRD4, HTR1A, HTR2A, HTR2C, KCNE2, RGS2, SLC6A2, SCN5A |
| Sulpiride | Atypical antipsychotic | DRD2 | |||
| Thioridazine | Typical antipsychotic phenothiazine | CYP2D6 | CYP2C19 | CYP1A2, CYP2C8/9, CYP2D6, CYP2E1 | ADRA1A, DRD2, KCNE2, SCN5A |
| Thiothixene | Typical antipsychotic | CYP1A2 | CYP2D6 | ADRA1A, DRD2, KCNE2, KCNQ1, KCNH6, SCN5A, | |
| Trifluoperazine | Typical antipsychotic phenothiazine | CYP1A2 | ADRA1A, DRD2 | ||
| Ziprasidone | Atypical antipsychotic | CYP1A2, CYP3A4 | CYP2D6, CYP3A4 | ADRA1, AOX1, DRD2, DRD3, HTR2C, HTR1A, HTR2A, KCNE2, KCNH2, RGS4, SCN5A | |
| Zonisamide | Anticonvulsant | CYP3A4 | CYP2C19 | ||
| Zuclopenthixol | Typical antipsychotic | CYP2D6 | ADRA1, DRD1, DRD2, KCNE2, SCN5A |
ABCB1, ATP‐binding cassette, sub‐family B (MDR/TAP), member 1; ACACA, Acetyl‐Coenzyme A carboxylase alpha; ADRA1, Adrenergic, alpha‐1 receptor; ADRA1A, Adrenergic, alpha‐1A‐, receptor; ADRA1B, Adrenergic, alpha‐1B‐, receptor; ADRB3, Adrenergic, beta‐3‐, receptor; ADRA1D, Adrenergic, alpha‐1D‐, receptor; AOX1, Aldehyde oxidase 1; APOA5, Apolipoprotein A‐V; APOC3, Apolipoprotein C‐III; APOD, Apolipoprotein D; BDNF, Brain‐derived neurotrophic factor; COMT, Catechol‐O‐methyltransferase; CYP1A2, Cytochrome P450, family 1, subfamily A, polypeptide 2; CYP2A6, Cytochrome P450, family 2, subfamily A, polypeptide 6; CYP2C19, Cytochrome P450, family 2, subfamily C, polypeptide 19; CYP2C8, Cytochrome P450, family 2, subfamily C, polypeptide 8; CYP2C9, Cytochrome P450, family 2, subfamily C, polypeptide 9; CYP2D6, Cytochrome P450, family 2, subfamily D, polypeptide 6; CYP2E1, Cytochrome P450, family 2, subfamily E, polypeptide 1; CYP3A4, Cytochrome P450, family 3, subfamily A, polypeptide 4; DR, Dopamine receptor; DRD1, Dopamine receptor D1; DRD2, Dopamine receptor D2; DRD3, Dopamine receptor D3; DRD4, Dopamine receptor D4; DTNBP1, Dystrobrevin binding protein 1; GNAS, GNAS complex locus; GNB3, Guanine nucleotide binding protein (G protein), beta polypeptide 3; GRIN2B, Glutamate receptor, ionotropic, N‐methyl D‐aspartate 2B; GRM3, Glutamate receptor, metabotropic 3; HLA, Major histocompatibility complex; HRH1, Histamine receptor H1; HRH2, Histamine receptor H2; HTR1A, 5‐Hydroxytryptamine (serotonin) receptor 1A; HTR2A, 5‐Hydroxytryptamine (serotonin) receptor 2A; HTR2B, 5‐Hydroxytryptamine (serotonin) receptor 2B; HTR2C, 5‐Hydroxytryptamine (serotonin) receptor 2C; HTR6, 5‐Hydroxytryptamine (serotonin) receptor 6; IL1RN, Interleukin 1 receptor antagonist; KCNE1, Potassium voltage‐gated channel, Isk‐related family, member 1; KCNE2, Potassium voltage‐gated channel, Isk‐related family, member 2; KCNH, Potassium voltage‐gated channel, subfamily H (eag‐related), member 1–8; KCNH2, Potassium voltage‐gated channel, subfamily H (eag‐related), member 2; KCNH6, Potassium voltage‐gated channel, subfamily H (eag‐related), member 6; KCNQ1, Potassium voltage‐gated channel, KQT‐like subfamily, member 1; LEP, Leptin; LEPR, Leptin receptor; LPL, Lipoprotein lipase; NPY, Neuropeptide Y; RGS2, Regulator of G‐protein signaling 2, 24kDa; RGS4, Regulator of G‐protein signaling 4; SCN5A, Sodium channel, voltage‐gated, type V, alpha subunit; SLC6A2, Solute carrier family 6 (neurotransmitter transporter, noradrenalin), member 2; SLC6A4, Solute carrier family 6 (neurotransmitter transporter, serotonin), member 4; TNF, Tumor necrosis factor (TNF superfamily, member 2).