10
Treatment
Antipsychotic medications: available oral and short-acting
intramuscular formulations*
Genric name
Trade name
(most common in
U.S., may change)
Metabolic enzymes/
transporters
Available U.S.
formulations
(mg, unless otherwise
noted)
First-generation antipsychotics
Chlorpromazine
Thorazine
CYP2D6 (Major), CYP1A2
(Minor), CYP3A4 (Minor)
substrate
Tablet: 10, 25, 50, 100, 200
Short-acting injection (HCl):
25/mL (1 mL, 2 mL)
Fluphenazine
Prolixin
CYP2D6 (Major) substrate Tablet: 1, 2.5, 5, 10
Oral concentrate: 5/mL
(120 mL)
Elixir: 2.5/5 mL (60 mL)
Short-acting injection (HCl):
2.5/mL (10 mL)
Haloperidol
Haldol
CYP2D6 (Major), CYP3A4
(Major), CYP1A2 (Minor)
substrate; 50-60%
glucuronidation
Tablet: 0.5, 1, 2, 5, 10, 20
Oral concentrate: 2/mL
(5 mL, 15 mL, 120 mL)
Short-acting injection
(lactate):
5/mL (1 mL, 10 mL)
Loxapine
Loxitane
CYP1A2 (Minor), CYP2D6
(Minor), CYP3A4 (Minor)
substrate; P-glycoprotein
inhibitor
Capsule: 5, 10, 25, 50
Aerosol powder breath-
activated inhalation: 10
Molindone
Moban
CYP2D6 substrate Tablet: 5, 10, 25
Perphenazine
Trilafon
CYP2D6 (Major), CYP1A2
(Minor), CYP2C19 (Minor),
CYP2C9 (Minor), CYP3A4
(Minor) substrate
Tablet: 2, 4, 8, 16
Pimozide
Orap
CYP1A2 (Major), CYP2D6
(Major), CYP3A4 (Major)
substrate
Tablet: 1, 2
Thioridazine
Mellaril
CYP2D6 (Major) substrate
and moderate inhibitor,
CYP2C19 (Minor) substrate
Tablet: 10, 25, 50, 100
Thiothixene
Navane
CYP1A2 (Major) substrate Capsule: 1, 2, 5, 10
Trifluoperazine
Stelazine
CYP1A2 (Major) substrate Tablet: 1, 2, 5, 10
