Thiethylperazine
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| Clinical data | |
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| Trade names | Torecan, Norzine |
| AHFS/Drugs.com | Micromedex Detailed Consumer Information |
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| Pharmacokinetic data | |
| Protein binding | 60% |
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| CompTox Dashboard (EPA) | |
| ECHA InfoCard | 100.014.381 |
| Chemical and physical data | |
| Formula | C22H29N3S2 |
| Molar mass | 399.62 g·mol−1 |
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Thiethylperazine (Torecan, Norzine) is an antiemetic[1] of the phenothiazine class. It is an antagonist of dopamine receptors (DRD1, DRD2, DRD4) as well as of 5-HT2A, 5-HT2C receptors, mAChRs (1 through 5), α1 adrenergic receptor and H1 receptor.
Thiethylperazine activates the transport protein ABCC1 that clears beta-amyloid from brains of mice.[2]
Pharmacokinetics[3]
Distribution
This drug is highly lipofilic and it binds with membranes and serum proteins (over 85%). It accumulates in organs with high blood flow and penetrates the placenta. It cannot be removed with dialysis.
Metabolism
It is mainly metabolised in the liver and only 3% is eliminated unchanged. Torecan's half-life is 12 h.
Teratogenicity
In toxic doses above the terapeutic window, it increases the rate of cleft palate occurence.
Antypsychotic activity
Theithylperazine may possess antypsychotic activity[4] due to the antagonism of 5-HT2 and D2 receptors. Because of this, it would not cause extrapyramidal symptoms. Nevertheless, it was never marketed as such drug.
One cause of acute dystonia occured in a 19-year-old male patient after discontinuation of this drug.[5]
Overdose
Signs of acute thiethylperazine overdose include: extrapyramidal symptoms, confusion, convulsions, respiratory depression and hypotension.
References
- ^ Tamboline, B. L.; McGillivray, D. C.; Bogoch, A. (1965-02-20). "The Effects of Thiethylperazine Dimaleate (Torecan) on Nausea and Vomiting". Canadian Medical Association Journal. 92 (8): 422–423. ISSN 0008-4409. PMC 1928133. PMID 14261157.
- ^ Krohn M, Lange C, Hofrichter J, Scheffler K, Stenzel J, Steffen J, et al. (October 2011). "Cerebral amyloid-β proteostasis is regulated by the membrane transport protein ABCC1 in mice". The Journal of Clinical Investigation. 121 (10): 3924–31. doi:10.1172/JCI57867. PMC 3195473. PMID 21881209.
- "Alzheimer disease: Transport protein ABCC1 plays key role in clearing beta-amyloid from brains of mice". ScienceDaily (Press release). September 1, 2011.
- ^ https://rejestrymedyczne.ezdrowie.gov.pl/enwiki/api/rpl/medicinal-products/6729/characteristic.
{{cite web}}: Missing or empty|title=(help) - ^ Rotrosen, J.; Angrist, B. M.; Gershon, S.; Aronson, M.; Gruen, P.; Sachar, E. J.; Denning, R. K.; Matthysse, S.; Stanley, M.; Wilk, S. (September 1978). "Thiethylperazine; clinical antipsychotic efficacy and correlation with potency in predictive systems". Archives of General Psychiatry. 35 (9): 1112–1118. doi:10.1001/archpsyc.1978.01770330086008. ISSN 0003-990X. PMID 99115.
- ^ Khanderia, Ujjaini (July 1985). "Recurrent Dystonic Reactions Induced by Thiethylperazine". Drug Intelligence & Clinical Pharmacy. 19 (7–8): 550–551. doi:10.1177/106002808501900708. ISSN 0012-6578.
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