Trifluoperazine
- Atc Codes:N05AB06
- CAS Codes:440-17-5#117-89-5
- PHARMGKB ID:440-17-5#117-89-5
Table of contents
- Brand Names
- Drug Combinations
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Cyprus: Stelazine, Trifluoperazine; Greece: Stelazine, Stelium; Ireland: Stelazine; Italy: Modalina, Triflu C; Malta: Stelazine; Poland: Trifluoperazine; UK: Stelazine, Trifluoperazine.
North America
Canada: Novo-Trifluzine, Terfluzine, Trifluoperazine; USA: Trifluoperazine.
Latin America
Argentina: Stelazine, Trifluoperazina; Brazil: Stelazine; Mexico: Flupazine, Stelazine.
Asia
Japan: Trifluoperazine.
Drug combinations
Trifluoperazine and Tranylcypromine
Chemistry
Trifluoperazine Hydrochloride: C~21~H~24~F~3~N~3~S 2HCl. Mw: 480.42. (1) 10H-Phenothiazine, 10-[3-(4-methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-, dihydrochloride; (2) 10-[3-(4-Methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)phenothiazine dihydrochloride. CAS-440-17-5; CAS-117-89-5 (trifluoperazine).
Pharmacologic Category
Antipsychotics; Phenothiazines. (ATC-Code: N05AB06).
Mechanism of action
Blocks postsynaptic mesolimbic dopaminergic receptors in brain. Exhibits α-adrenergic-blocking effect and depresses release of hypothalamic and hypophyseal hormones.
Therapeutic use
Treatment of schizophrenia.
Pregnancy and lactiation implications
Use with caution in pregnancy. Enters breast milk (not recommended in nursing women).
Unlabeled use
Management of psychotic disorders. Behavioral symptoms associated with dementia behavior (elderly). Psychosis/agitation related to Alzheimer’s dementia.
Contraindications
Hypersensitivity to trifluoperazine or any component of the formulation (cross-reactivity between phenothiazines may occur). Severe CNS depression. Bone marrow suppression. Blood dyscrasias. Severe hepatic disease. Coma.
Warnings and precautions
Use with caution in risk of seizures, including patients with history of seizures, head trauma, brain damage, alcoholism, or concurrent therapy with medications which may lower seizure threshold. May alter cardiac conduction (life-threatening arrhythmias occurred). Use with caution in myasthenia gravis (may be exacerbated by cholinergic blockade). May cause anticholinergic effects (constipation, xerostomia, blurred vision, urinary retention). Use with caution in decreased gastrointestinal motility, paralytic ileus, urinary retention, BPH, xerostomia, or visual problems. Relative to other antipsychotics, trifluoperazine has low potency of cholinergic blockade. Blood dyscrasias might occur. Use contraindicated in bone marrow suppression. Antipsychotic use associated with esophageal dysmotility and aspiration. Use with caution in risk of pneumonia. May cause extrapyramidal symptoms, including pseudoparkinsonism, acute dystonic reactions, akathisia, and tardive dyskinesia. Use with caution in breast cancer or other prolactin-dependent tumors (elevates prolactin levels). May be associated with neuroleptic malignant syndrome. May cause orthostatic hypotension (use with caution in risk of this effect or in patients who would not tolerate transient hypotensive episodes). Use with caution in respiratory disease. May be associated with pigmentary retinopathy. Use with caution in Parkinson’s disease (may be more sensitive to adverse effects). May cause sedation. Impaired core body temperature regulation may occur. Use with caution in severe cardiovascular disease. Elderly patients with dementia-related psychosis treated with antipsychotics are at increased risk of death compared to placebo. Increased incidence of cerebrovascular adverse events (including fatalities) reported in elderly patients with dementia-related psychosis. Trifluoperazine not approved for this indication. Use with caution in narrow-angle glaucoma (may be exacerbated by cholinergic blockade), and in hepatic and renal impairment. May mask toxicity of other drugs or conditions due to antiemetic effects. Effects may be potentiated when used with other sedative drugs or ethanol.