trifluoperazine
Trade name: stelazine
Approved
Apr 16, 1959
Trifluoperazine (Eskazinyl, Eskazine, Jatroneural, Modalina, Stelazine, Terfluzine, Trifluoperaz, Triftazin) is a typical antipsychotic of the phenothiazine chemical class used for the short-term treatment of certain types of anxiety. Trifluoperazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; depresses the release of hypothalamic and hypophyseal hormones and is believed to depress the reticular activating system thus affecting basal metabolism, body temperature, wakefulness, vasomotor tone, and emesis. 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 behavioral 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. 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. It is also more likely to cause somnolence and anticholinergic side effects such as red-eye and xerostomia (dry mouth). — NCATS
Clinical trial activity
2 trials · 3 clinical orgs · 12 marketing orgs
Earliest trial started Jun 1, 2019 (NCT03966053)
Timeline
1950s
- Apr 16, 1959
GlaxoSmithKline — Earliest FDA Approval
- Apr 16, 1959
GlaxoSmithKline — NDA Secondary Org
- Apr 16, 1959
GlaxoSmithKline — NDA Organization
1980s
- Nov 20, 1981
Sandoz — Marketing Organization
- Apr 15, 1982
Fosun — Marketing Organization
- Apr 15, 1982
Chartwell Pharmaceuticals — Marketing Organization
- Nov 19, 1982
Ivax — Marketing Organization
- Jul 26, 1983
Wockhardt — Marketing Organization
- Apr 23, 1985
Duramed Research — Marketing Organization
1990s
2010s
- Jan 1, 2019
Earliest Phase 1 Sponsor(trial)
2020s
- Jan 1, 2025
Earliest Phase 2 Sponsor(trial)
Indications
Approved for
Mechanism of action
- Serotonin 2a (5-HT2a) receptorANTAGONIST
HTR2A antagonist
- Serotonin 2c (5-HT2c) receptorANTAGONIST
HTR2C antagonist
- D2-like dopamine receptorANTAGONIST
D2-like dopamine receptor antagonist
Approval history
- approvedApr 16, 1959
Chemistry & pharmacology
SMILES
CN1CCN(CCCN2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1.Cl.Cl- Mol. weight
- 480.43 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral, Parenteral
- Availability
- Prescription Only
Oral
Yes
Parenteral
Yes
Topical
No
Sources
- ChEMBLCHEMBL1257040 ↗
- WikipediaTrifluoperazine ↗
- NCATS214IZI85K3 ↗
- ChEMBLCHEMBL422 ↗
- ChEMBLCHEMBL1710 ↗
Also known as
- 10-[3-(4-methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-10h-phenothiazine
- 10-[3-(4-methyl-1-piperazinyl)propyl]-2-(trifluoromethyl)-10h-phenothiazine
- 10-[3-(4-methyl-piperazin-1-yl)-propyl]-2-trifluoromethyl-10h-phenothiazine
- 10-[3-(4-methyl-piperazin-1-yl)-propyl]-2-trifluoromethyl-10h-phenothiazine
- amylozine
- flupazine
- stelazine
- stelazine
- stelazine
- stelazine
- stelazine fte
- trifluoperazin
- trifluoperazina
- trifluoperazina
- trifluoperazine
- trifluoperazine
- trifluoperazine
- trifluoperazine
- trifluoperazine
- trifluoperazine
- trifluoperazine
- trifluoperazine
- trifluoperazine
- trifluoperazine
- trifluoperazine
- trifluoperazine dihydrochloride
- trifluoperazine hcl
- trifluoperazine hcl
- trifluoperazine hcl
- trifluoperazine hydrochloride
- trifluoperazine hydrochloride
- trifluoperazine hydrochloride
- trifluoperazine hydrochloride
- trifluoperazine maleate
- trifluoperazine maleate
- trifluoperazinum
- trifluoperazinum
- trifluoromethyl-10-(3'-(1-methyl-4-piperazinyl)propyl)phenothiazine
- trifluoromethyl-10-(3'-(1-methyl-4-piperazinyl)propyl)phenothiazine
- trifluoromethylperazine
- trifluoroperazine
- trifluoroperazine
- trifluoroperazine
- trifluperazine
- trifluperazine
- trifluperazine
- triflurin
- triperazine
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07008235 | Phase 2/Phase 3 (Phase 3) | Jul 1, 2025 | Dhaka Medical College |
| NCT03966053 | Phase 1/Phase 2 (Phase 2) | Jun 1, 2019 | Feinstein Institute for Medical Research, Northwell Health |
Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Dhaka Medical College | Academic/Hospital | 1 | 1 | 1 | 2025 |
| Feinstein Institute for Medical Research | Academic/Hospital | 1 | 1 | 1 | 2019 |
| Northwell Health | Academic/Hospital | 1 | 0 | 1 | 2019 |
Marketing (13)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Athem | For profit | MKTG | Oct 25, 1996 |
| Athenex, Inc. | For profit | MKTG | — |
| Chartwell Pharmaceuticals | For profit | MKTG | Apr 15, 1982 |
| Duramed Research | For profit | MKTG | Apr 23, 1985 |
| Fosun | For profit | MKTG | Apr 15, 1982 |
| GlaxoSmithKline | For profit | NDA2 | Apr 16, 1959 |
| GlaxoSmithKline | For profit | NDA | Apr 16, 1959 |
| Invatech | For profit | MKTG | Oct 25, 1996 |
| Ivax | For profit | MKTG | Nov 19, 1982 |
| Mylan | For profit | MKTG | Jul 7, 1997 |
| Sandoz | For profit | MKTG | Nov 20, 1981 |
| Watson Pharmaceuticals | For profit | MKTG | — |
| Wockhardt | For profit | MKTG | Jul 26, 1983 |