Drug intelligence / Profile preview

pipotiazine

Development stage
Discontinued
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Pipotiazine is a typical antipsychotic of the phenothiazine class, specifically a piperidine phenothiazine derivative, used primarily for the management and maintenance treatment of chronic, non-agitated schizophrenia and other psychoses[1][3][4]. It acts as an antagonist at multiple postsynaptic receptors including dopaminergic (D1, D2, D3, D4), serotonergic (5‑HT1 and 5‑HT2), histaminergic (H1), alpha adrenergic (α1/α2), and muscarinic cholinergic (M1/M2) receptors[1][8]. Its antipsychotic effect is mainly attributed to dopamine receptor antagonism in the brain. Pipotiazine was available in both oral forms and as long‑acting injectable esters such as pipotiazine palmitate; the latter allowed for monthly dosing due to slow release from intramuscular depot injections[4][7]. Compared to other phenothiazines, it has less sedative effect but a higher risk of extrapyramidal side effects. Production of some formulations like pipotiazine palmitate was discontinued in 2015 due to supply issues[4].

Brand names
PiportilPiportil L4Piportil SpéciaPiportil depotLonseren
Other names
pipotiazine palmitatepiportyl palmitatpiportil longum‐4piportil M2
02

Targets

HRH1 (Histamine H1 Receptor)ADRA1A (α1A)mAChR (Muscarinic acetylcholine receptors)DRD2 (Dopamine D2 Receptor)DRD3 (Dopamine receptor D3)5-HT2 (5-HT2 receptor family)

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