Products
Thiethylperazine was commercially available in the form of dragées, as a solution for injection, and as suppositories (Torecan, Novartis). It had been approved in many countries since 1960. The suppositories went out of circulation in 2010 due to lack of demand. The other dosage forms were withdrawn from the market in 2014.
Structure and properties
Thiethylperazine (C22H29N3S2, Mr = 399.6 g/mol) is present in drugs as thiethylperazine maleate. Thiethyl perazine dihydrogen maleate is a white to pale yellowish or greenish yellowish crystalline or granular powder that is very slightly soluble in water. Thiethylperazine belongs to group of phenothiazines and carries a piperazine side chain.
Effects
Thiethylperazine (ATC R06AD03) has antiemetic and antipsychotic properties. The effects are due to antagonism at dopamine receptors. Thiethylperazine also interacts with other receptors. It has a half-life of approximately 12 hours.
Indications
For the treatment of nausea, vomiting, and dizziness of various causes. Thiethylperazine, like other phenothiazines, has also been used as an antipsychotic.
Dosage
According to the prescribing information. The dragées are administered one to three times daily.
Contraindications
Thiethylperazine is contraindicated in hypersensitivity, hypersensitivity to phenothiazines, comatose states, in children under 15 years of age, and during breastfeeding. For complete precautions, see the drug label.
Interactions
Pharmacodynamic drug-drug interactions are possible with centrally depressant drugs and with CYP2D6 inhibitors.
Adverse effects
Possible adverse effects include dry mouth, drowsiness, somnolence, and extrapyramidal symptoms. Liver dysfunction and the occurrence of malignant neuroleptic syndrome have been reported rarely.
