Trifluoperazine

Trifluoperazine

Trifluoperazine
Systematic (IUPAC) name
10-[3-(4-methylpiperazin-1-yl)propyl]-
2-(trifluoromethyl)-10H-phenothiazine
Clinical data
AHFS/Drugs.com
MedlinePlus
Pregnancy
category
  • AU: C
  • US: C (Risk not ruled out)
Legal status
Routes of
administration
oral, IM
Pharmacokinetic data
Metabolism Hepatic
Biological half-life 10–20 hours
Identifiers
CAS Registry Number  YesY
ATC code N05
PubChem CID:
IUPHAR/BPS
DrugBank  YesY
ChemSpider  YesY
UNII  YesY
ChEBI  YesY
ChEMBL  YesY
PDB ligand ID TFP (, )
Chemical data
Formula C21H24F3N3S
Molecular mass 407.497 g/mol
 YesY   

Trifluoperazine (Eskazinyl, Eskazine, Jatroneural, Modalina, Stelazine, Terfluzine, Trifluoperaz, Triftazin) is a typical antipsychotic of the phenothiazine chemical class.

Uses

The primary application of trifluoperazine is for schizophrenia. Other official indications may vary country by country, but generally it is also indicated for use in agitation and patients with behavioural problems, severe nausea and vomiting as well as severe anxiety. Trials have shown a moderate benefit of this drug in patients with borderline personality disorder.[1] Its use in many parts of the world has declined because of highly frequent and severe early and late tardive dyskinesia, a type of extrapyramidal symptom. The annual development rate of tardive dyskinesia may be as high as 4%.

A 2005 study of patients with generalized anxiety disorder [2]

noted that:

A 2006 study suggested that trifluoperazine may be able to reverse addiction to opioids.[3]

A multi-year UK study by the Alzheimer's Research Trust suggested that this and other antipsychotic drugs commonly given to patients with Alzheimer's disease with mild behavioural problems often make their condition worse.[4] The study concluded that

Pharmacology

Trifluoperazine has central [9]

Effects

Comparison of trifluoperazine to placebo[10]
Measured outcome Findings in words Findings in numbers Quality of evidence
Global effects
Clinical improvement at 19 weeks 4.5 times more likely to have a clinical significant response with trifluoperazine RR 4.61 CI 1.54 to 13.84 Low
Relapse or worsening at 5 months 65% less likely to have relapse or worsening of symptoms with trifluoperazine RR 0.34 CI 0.23 to 0.49
Significant response in psychotic symptoms No more likely to experience ‘intensified psychotic symptoms’ with trifluoperazine RR 1.05 CI 0.54 to 2.05 Very Low
Adverse effects
Severe adverse effects at 2 months 30% more likely to experience severe adverse effects with trifluoperazine RR 1.31 CI 0.22 to 7.80 Very low
Agitation or distress Twice more likely to experience clinically significant agitation or distress with trifluoperazine RR 2.00 CI 0.19 to 20.72

Side effects

A 2004 meta-analysis of the studies on trifluoperazine found that it is more likely than placebo to cause extrapyramidal side effects such as akathisia, dystonia, and Parkinsonism.[9] It is also more likely to cause somnolence and anticholinergic side effects such as red eye and xerostomia (dry mouth).[9] All antipsychotics can cause the rare and sometimes fatal neuroleptic malignant syndrome.[11] Trifluoperazine can lower the seizure threshold.[12] The antimuscarinic action of trifluoperazine can cause excessive dilation of the pupils (mydriasis), which increases the chances of patients with hyperopia developing glaucoma.[13]

Contraindications

Trifluoperazine is contraindicated in CNS depression, coma, and blood dyscrasias. Trifluoperazine should be used with caution in patients suffering from renal or hepatic impairment.

Formulations

In the United Kingdom and some other countries, Trifluoperazine is sold and marketed under the brand 'Stelazine'.

The drug is sold as tablet, liquid and 'Trifluoperazine-injectable USP' for deep intramuscular short-term use.

In the past, trifluoperazine was used in fixed combinations with the MAO inhibitor (antidepressant) tranylcypromine to attenuate the strong stimulating effects of this antidepressant. This combination was sold under the brand name Jatrosom N. Likewise a combination with amobarbital (potent sedative/hypnotic agent) for the amelioration of psychoneurosis and insomnia existed under the brand name Jalonac. In Italy the first combination is still available, sold under the brand name Parmodalin (10 mg of Tranylcypromine and 1 mg of Trifluoperazine).

References

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  10. ^ Koch K, Mansi K, Haynes E, Adams CE, Sampson S, Furtado VA (2014). "Trifluoperazine versus placebo for schizophrenia". Cochrane Database of Systematic Reviews (1) doi: 10.1002/14651858.CD010226.pub2. Retrieved 19 November 2014.
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