Chloropromazine

• Thorazine
• Low potency drug (100mg)
• Dose Range(mg/day) : 60-2000
• Maximum Dose: 2000mg
• Adverse Effects
  • Sedative and ACh- High
  • EPS- Low
  • Hypotension- IM=high; PO=Mod.
• CYP metabolism: 2D6;1A2;3A4
• CYP inhibition: 2D6;2E1

Fluphenazine

• Prolixin
• High potency (2mg)
• Dose Range: 1-50
• Max. Dose: 100mg
• Adverse Effect
  • Low Sedative, ACh, & Hypotensive 
  • High EPS
• CYP metabolism:2D6
• CYP inhibition: 1A2;2C9;2D6;2E1

Haloperidol

• Haldol
• High potency (2mg)
• Dose Range: 1-100mg
• Max Dose: 100mg
• Adverse Effect
  • Very low- Sedative, ACh, Hypotensive
  • Very High EPS
• CYP metabolism:2D6;1A2;3A4
• CYP inhibition: 2D6;3A4

Loxapine

• Loxitane
• Medium potency (10mg)
• Dose Range: 20-250mg
• Max. Dose: 250mg
• Adverse Effect
  • Moderate- Sedative, EPS, hypotensive
  • Low- ACh
• CYP metabolism: Extensive
• CYP inhibition: Unknown

Molindone

• Moban
• Medium Potency (10mg)
• Dose Range: 15-225
• Max Dose: 225
• Adverse effect
  • Very low- Sedative
  • Low- ACh and Hypotensive
  • Moderate- EPS
• CYP metabolism:2D6
• CYP inhibition: unknown

Perphenazine

• Trilafon
• Medium potency (8-10mg)
• Dose Range: 8-64mg
• Max Dose: 100mg
• Adverse Effect
  • Low- Sedative, ACh, Hypotensive
  • High-EPS
• CYP metabolism: 2D6
• CYP inhibition: 2D6

Pimozide

• Orap
• High potency (2mg)
• Dose Range: 2-10
• Max dose: 20mg
• Adverse effect
  • Very low- Hypotensive
  • Low- Sedative, ACh
  • High- EPS
• CYP metabolism: 3A4;1A2
• CYP inhibition: 2D6

Thioridazine

• Mellaril
• Low potency (100mg)
• Dose Range: 50-800mg
• Max Dose: 800mg
• Adverse effect
  • Low- EPS
  • High- Sedative, ACh, Hypotensive
• CYP metabolism: 2D6;2C19
• CYP inhibition: 2D6;1A2;2C9,2E1

Thiothixene

• Navane
• Medium potency (4mg)
• Dose Range: 5-60mg
• Max Dose: 100mg
• Adverse effect
  • Low- Sedative, ACh, Hypotensive
  • High- EPS
• CYP metabolism: 1A2
• CYP inhibition: 2D6

Trifluoperazine

• Stelazine
• Medium Potency (5mg)
• Dose Range: 2-80mg
• Max. Dose: 100mg
• Adverse effect
  • Low- Sedative, ACh, Hypotensive
  • High- EPS
• CYP metabolism: 1A2
• CYP inhibition: No known

Pharmacokinetics of all FGA

• Renal insufficiency may require decreased dose
• Use with caution in pts with liver dysfunction

Haloperidol (Haldol)-PK

• t_1/2=12-36hrs
• tmax= 2-6hrs oral; 7 days decanoate
• Metabolized by CYP 1A2, 2D6,3A4

Phenothiazines- PK

• t_1/2=8-35hrs
• Metabolized by liver enzymes CYP 3A4, 2D6 and conjugation
• Highly protein bound
• Chlorpromazine, Fluphenazine, Perphenazine, Thioridazine, Thiothixene, Trifluoperazine

Loxapine-PK

• Biphasic T_1/2
  • Initial- 5hrs
  • Terminal- 12-19hrs

Thiothixene-PK

• t_1/2 >24hrs with chronic use