thioridazine
Trade name: mellaril
Approved
Mar 15, 1962
Thioridazine (Mellaril or Melleril) is a piperidine typical antipsychotic drug belonging to the phenothiazine drug group and was previously widely used in the treatment of schizophrenia and psychosis. Thioridazine blocks postsynaptic mesolimbic dopaminergic D1 and D2 receptors in the brain; blocks alpha-adrenergic effect 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. Thioridazine primary use in medicine was the treatment of schizophrenia. Thioridazine was also tried with some success as a treatment for various psychiatric symptoms seen in people with dementia, but chronic use of thioridazine and other antipsychotics in people with dementia is not recommended. Thioridazine prolongs the QTc interval in a dose-dependent manner. It produces significantly less extrapyramidal side effects than most first-generation antipsychotics. Its use, along with the use of other typical antipsychotics, has been associated with degenerative retinopathies. It has a higher propensity for causing anticholinergic side effects coupled with a lower propensity for causing extrapyramidal side effects and sedation than chlorpromazine but also has a higher incidence of hypotension and cardiotoxicity. It is also known to possess a relatively high liability for causing orthostatic hypotension compared to other antipsychotics. Similarly to other first-generation antipsychotics, it has a relatively high liability for causing prolactin elevation. It is the moderate risk of causing weight gain. — NCATS
Clinical trial activity
5 trials · 8 clinical orgs · 23 marketing orgs
Earliest trial started Jun 1, 2013 (NCT01765803)
Timeline
1960s
1980s
- Apr 14, 1983
Ani Pharmaceuticals — Marketing Organization
- Apr 26, 1983
Alpharma — Marketing Organization
- Jul 5, 1983
Wockhardt — Marketing Organization
- Aug 23, 1983
Actavis — Marketing Organization
- Aug 30, 1983
Fosun — Marketing Organization
- Aug 30, 1983
Chartwell Pharmaceuticals — Marketing Organization
- Nov 8, 1983
Watson Pharmaceuticals — Marketing Organization
- Nov 8, 1983
Teva — Marketing Organization
- Nov 8, 1983
Heritage Pharma — Marketing Organization
- Nov 16, 1983
Mutual Pharmaceutical — Marketing Organization
- Nov 18, 1983
Mylan — Marketing Organization
- Nov 18, 1983
Sun Pharmaceuticals — Marketing Organization
- Mar 21, 1984
Sandoz — Marketing Organization
- Jul 2, 1985
Superpharm — Marketing Organization
- Dec 16, 1985
Roxane Laboratories — Marketing Organization
- Dec 16, 1985
Boehringer Ingelheim — Marketing Organization
1990s
- Aug 16, 1996
Hi Tech Pharmaceuticals — Marketing Organization
- Aug 16, 1996
Akorn, Inc. — Marketing Organization
- Aug 16, 1996
Epic Pharma Llc — Marketing Organization
- Aug 28, 1997
Pharmaceutical Associates — Marketing Organization
Indications
Approved for
Mechanism of action
- Serotonin 2c (5-HT2c) receptorANTAGONIST
HTR2C antagonist
- Serotonin 2a (5-HT2a) receptorANTAGONIST
HTR2A antagonist
- D2-like dopamine receptorANTAGONIST
D2-like dopamine receptor antagonist
Approval history
- approvedPriority reviewMar 15, 1962
Chemistry & pharmacology
SMILES
CSc1ccc2c(c1)N(CCC1CCCCN1C)c1ccccc1S2- Mol. weight
- 370.59 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Racemic Mixture
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL479 ↗
- WikipediaThioridazine ↗
- NCATS4WCI67NK8M ↗
- ChEMBLCHEMBL1200916 ↗
Also known as
- 10-[2-(1-methyl-2-piperidyl)ethyl]-2-methylsulfanyl-phenothiazine
- 10-[2-(1-methyl-2-piperidyl)ethyl]-2-methylsulfanyl-phenothiazine
- 2-methylmercapto-10-(2-(n-methyl-2-piperidyl)ethyl)phenothiazine
- 2-methylmercapto-10-(2-(n-methyl-2-piperidyl)ethyl)phenothiazine
- 3-methylmercapto-n-(2'-(n-methyl-2-piperidyl)ethyl)phenothiazine
- 3-methylmercapto-n-(2'-(n-methyl-2-piperidyl)ethyl)phenothiazine
- dl-thioridazine
- malloryl
- meleril
- mellaril
- mellaril
- mellaril
- mellaril
- mellaril-s
- mellaril-s
- melleril
- melleril
- rideril
- rideril
- thioridazin
- thioridazin
- thioridazin
- thioridazine
- thioridazine
- thioridazine
- thioridazine
- thioridazine
- thioridazine
- thioridazine
- thioridazine
- thioridazine
- thioridazine
- thioridazine
- thioridazine
- thioridazine hcl
- thioridazine hcl
- thioridazine hcl
- thioridazine hydrochloride
- thioridazine hydrochloride
- thioridazine hydrochloride
- thioridazine hydrochloride
- thioridazine hydrochloride intensol
- thioridazine hydrochloride intensol
- thioridazinum
- thioridazinum
- tioridazina
- tioridazina
- tp-21
- tp-21
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT02435095 | Phase 4 | May 1, 2015 | RWTH Aachen University |
| NCT02374567 | Phase 3 | Jan 1, 2015 | Gottfried Wilhelm Leibniz Universität Hannover |
| NCT02307396 | Phase 4 | Nov 1, 2014 | Technical University of Munich |
| NCT02096289 | Phase 1 | Jul 1, 2014 | Hamilton Health Sciences Corporation, McMaster University |
| NCT01765803 | Early Phase 1 (Phase 1) | Jun 1, 2013 | New Mexico Cancer Care Alliance, Oxnard Foundation, University of New Mexico |
Organizations
Research & Development (8)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Gottfried Wilhelm Leibniz Universität Hannover | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Hamilton Health Sciences Corporation | Academic/Hospital | 1 | 0 | 1 | 2014 |
| McMaster University | Academic/Hospital | 1 | 1 | 1 | 2014 |
| New Mexico Cancer Care Alliance | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Oxnard Foundation | Academic/Hospital | 1 | 0 | 1 | 2013 |
| RWTH Aachen University | Academic/Hospital | 1 | 1 | 1 | 2015 |
| Technical University of Munich | Academic/Hospital | 1 | 1 | 1 | 2014 |
| University of New Mexico | Academic/Hospital | 1 | 0 | 1 | 2013 |
Marketing (26)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Actavis | For profit | MKTG | Aug 23, 1983 |
| Akorn, Inc. | For profit | MKTG | Aug 16, 1996 |
| Alpharma | For profit | MKTG | Apr 26, 1983 |
| Ani Pharmaceuticals | For profit | MKTG | Apr 14, 1983 |
| Ani Pharmaceuticals | For profit | SYN | Apr 14, 1983 |
| Boehringer Ingelheim | For profit | MKTG | Dec 16, 1985 |
| Chartwell Pharmaceuticals | For profit | MKTG | Aug 30, 1983 |
| Epic Pharma Llc | For profit | MKTG | Aug 16, 1996 |
| Fosun | For profit | MKTG | Aug 30, 1983 |
| Heritage Pharma | For profit | SYN | Nov 8, 1983 |
| Heritage Pharma | For profit | MKTG | Nov 8, 1983 |
| Hi Tech Pharmaceuticals | For profit | MKTG | Aug 16, 1996 |
| Mutual Pharmaceutical | For profit | MKTG | Nov 16, 1983 |
| Mylan | For profit | MKTG | Nov 18, 1983 |
| Novartis | For profit | NDA2 | Mar 15, 1962 |
| Novartis | For profit | NDA | Mar 15, 1962 |
| Par Pharmaceuticals | For profit | MKTG | — |
| Pharmaceutical Associates | For profit | MKTG | Aug 28, 1997 |
| Roxane Laboratories | For profit | MKTG | Dec 16, 1985 |
| Sandoz | For profit | MKTG | Mar 21, 1984 |
| Sun Pharmaceuticals | For profit | MKTG | Nov 18, 1983 |
| Superpharm | For profit | MKTG | Jul 2, 1985 |
| Teva | For profit | MKTG | Nov 8, 1983 |
| Watson Pharmaceuticals | For profit | MKTG | Nov 8, 1983 |
| West-Ward Pharmaceutical | For profit | MKTG | — |
| Wockhardt | For profit | MKTG | Jul 5, 1983 |