trifluoperazine STELAZINE

Class: First Generation Antipsychotic/​Phenothiazine
FDA Indications: Schizophrenia, Short-term Treatment Of Generalized Non-psychotic Anxiety
Off-Label Use: Bipolar Mania
Prescribing
Forms: 1, 2, 5, 10mg tablet; 2mg/mL IM
Dose Range: 2-20 mg/day
Starting: 2 mg daily (if clinical situation permits) or twice a day
Hold for 5-7 days
Switch to once-daily dosing with gradual increments (over 5-7 days)
Therapeutic: conventional view of 20-30 mg/ day may be unduly high. Consider holding at 10-15 mg and assessing
Stopping: Taper 6-8 weeks, rapid d/c can lead to rebound psychosis
Monitoring:

NAMI drug fact sheet

Precautions
Contraindications: In patients with suspected or established subcortical brain damage, in patients receiving large doses of hypnotics, and in comatose or severely depressed states. Phenothiazines are contraindicated with significant hepatic impairment.
Serious Side Effects: , , , Cardiac Arrhythmias, Neutropenia and/or Agranulocytosis (rare), Hyperprolactinemia
There have been case reports of abnormal ECG changes with therapeutic doses of trifluoperazine
Side Effects: dizziness, visual changes, weakness/asthenia, anorexia, fatigue, EPS, galactorrhea, amenorrhea, drowsiness
Pharmacodynamics
1° MOA: Dopamine 2 (D2) receptor antagonism in mesolimbic area
Target: D2 (very high), 5HT2 (very high), D4 (high), H1 (moderate), α1 (low-moderate), M1 (low)
Pharmacokinetics
t½: 12.5° TMAX: 1.5-4.5°
Substrate of: UDP1A4
Inhibits: ∅ ; Induces:
Active Metabolites: N-desmethyltrifluoperazine, 7-hydroxyrifluoperazine
DDIs
  • - Caution when co-prescribing with antihypertensives (due to its α1 blockade)
  • - Caution when coprescribing with other CNS depressants
Misc
  • - a higher potency phenothiazine (20x more potent than chlorpromazine)
  • - although not systematically studied, may cause less weight gain than other antipsychotics
  • - one of the least sedating antipsychotics
  • - has purported anxiolytic actions (yet mechanism never elucidated)
  • - high risk of EPS: with doses above 5-6 mg/day, consider prophylactic anticholinergic
Special Populations

Category C—Although some reports have attempted to link trifluoperazine with congenital defects, most evidence suggests that the drug is safe for the mother and low risk for the embryo-fetus.

No reports describing the use of trifluoperazine during lactation have been located. The molecular weight (about 408 for the free base) is low enough that passage into milk should be expected. In 2001 the American Academy of Pediatrics classified trifluoperazine as a drug for which the effect on nursing infants is unknown but may be of concern.

Elderly patients with dementia-related psychosis treated with antipsychotic drugs are at an increased risk of death. Dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic function, concomitant disease or other drug therapy.

No dosage adjustment necessary.


Use with caution in patients with hepatic impairment.

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Last updated August 27 2018 18:45:06. Disclaimer: This website does not provide medical advice, nor is it a substitute for clinical judgment.