Pipotiazine (Piportil), also known as pipothiazine, is a typical antipsychotic of the phenothiazine class used in the United Kingdom and other countries for the treatment of schizophrenia. Its properties are similar to those of chlorpromazine. A 2004 systematic review investigated its efficacy for people with schizophrenia: + Pipotiazine palmitate compared to oral antipsychotics for schizophrenia SummaryAlthough well-conducted and reported randomized trials are still needed to fully inform practice (no trial data exists reporting hospital and services outcomes, quality of life, satisfaction with care and economics) pipotiazine palmitate is a viable choice for both clinician and person with schizophrenia. Outcome Findings in words Findings in numbers Quality of evidence Global outcomes No important clinical responseFollow-up: by 3 week) There is no clear difference between people given pipotiazine palmitate and those receiving oral antipsychotics. These findings are based on data of low quality. RR 2.57 (0.76 to 8.63) Low Leaving the study earlyFollow-up: up to 5 weeks Pipotiazine palmitate may increase the chance of leaving the study early but the difference between people given pipotiazine palmitate and those receiving oral antipsychotics is not clear. These findings are based on data of low quality. RR 3.85 (0.46 to 32.22) Low Mental state RelapseFollow-up: by 18 months) Pipotiazine palmitate has not more - or less - effect on risk of relapse than oral antipsychotics. These findings are based on data of low quality. RR 1.55 (0.76 to 3.18) Low Adverse effects Tardive dyskinesia Oral antipsychotic drugs and pipotiazine palmitate carry similar risks of this problematic movement disorder. These findings are based on data of low quality. RR 1.03 (0.22 to 4.92) Low Dystonia Pipotiazine palmitate may slightly reduce the chance of experiencing this movement disorder but there is no clear difference between people given pipotiazine palmitate and those receiving oral antipsychotics. These findings are based on data of low quality. RR 0.32 (0.04 to 2.89) Low
Medical uses Pipotiazine palmitate is used to treat schizophrenia.
Contraindications Pipotiazine palmitate is contraindicated in people with circulatory collapse (shock), altered states of consciousness, including drug intoxication, or other serious health conditions (liver disease, kidney disease, pheochromocytoma, severe cardiovascular disease, or blood dyscrasias). It is contraindicated in people with severe depression. Pipotiazine palmitate should not be used in people who have a history of allergic reactions to any component of the medicine or to chemically similar medicines (phenothiazines).
Pharmacokinetics Pipotiazine was available as a long-acting injectable formulation (pipotiazine palmitate). After deep intramuscular injection, pipotiazine palmitate reaches maximum plasma concentration in 7-14 days, has an elimination half-life of 15 days, and reaches steady-state levels after 2 months of usual dosing (given every 4 weeks).
Synthesis Synthesis of pipotiazine has been reported. (1970)ZA6801990 idem Jean-Claude Rene Georg Blondel, 2 More », (1975 to Rhone Poulenc Sa)Schussen, & Li Haixia, et al. (2019 to YUEYANG XINHUADA PHARMACEUTICAL CO Ltd).
The alkylation of 2-dimethylaminosulfonylphenthiazine (1) with 1-bromo-3-chloropropane (2) gives 10-(3-chloropropyl)-N,N-dimethylphenothiazine-2-sulfonamide (3). Alkylation with 4-piperidineethanol (4) completes the synthesis of pipothiazine (5).
History The long-acting injectable formulation of pipotiazine (pipotiazine palmitate) was withdrawn from all markets globally in March 2015 due to a shortage of the active ingredient.
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