thiethylperazine

Thiethylperazine is a piperazine phenothiazine derivative classified as a phenothiazine antiemetic and dopamine antagonist. It is primarily used for the relief and prevention of nausea and vomiting, including that associated with anesthesia, cancer chemotherapy, radiation therapy, and toxins. Thiethylperazine acts mainly by blocking postsynaptic dopamine D2 receptors in the medullary chemoreceptor trigger zone (CTZ), thereby reducing stimulation of the vomiting center in the brain. It also antagonizes other targets including dopamine receptors (D1, D2, D4), serotonin 5-HT2A/2C receptors, muscarinic acetylcholine receptors (M1–M5), alpha-1 adrenergic receptor, and histamine H1 receptor. This broad antagonism contributes to its antiemetic effects as well as its side effect profile. Although it has antipsychotic activity due to these actions—particularly at serotonin 5-HT2 and dopamine D2 receptors—it has not been marketed or widely used as an antipsychotic agent[1][3][4][5]. The drug is available in oral tablet form, intramuscular injection form (for deep IM use only), and rectal suppositories[6][7]. Its pharmacokinetics include high protein binding (~60–85%), hepatic metabolism with minimal renal excretion of unchanged drug (~3%), placental transferability, a half-life around 12 hours[5], and elimination primarily via urine.

Brand names

TorecanNorzine

Other names

thiethylperazine maleate