Pipotiazine Explained
Pipotiazine (Piportil), also known as pipothiazine, is a typical antipsychotic of the phenothiazine class[1] 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[2] | Summary |
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| Although 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 |
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| Global outcomes |
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No important clinical response
Follow-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 early
Follow-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 |
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Relapse
Follow-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 |
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| 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 | | 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 | |
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Medical uses
Pipotiazine palmitate is used to treat schizophrenia.[3]
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).[4]
Synthesis
The alkylation of 2-Dimethylaminosulfonylphenthiazine [1090-78-4] (1) with 1-Bromo-3-chloropropane (2) gives 10-(3-chloropropyl)-N,N-dimethylphenothiazine-2-sulfonamide [40051-12-5] (3). Alkylation with 4-Piperidineethanol [622-26-4] (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.[5]
Notes and References
- Bechelli LP, Ruffino-Netto A, Hetem G . A double-blind controlled trial of pipotiazine, haloperidol and placebo in recently-hospitalized acute schizophrenic patients . Brazilian Journal of Medical and Biological Research . 16 . 4 . 305–11 . December 1983 . 6143579 .
- Dinesh M, David A, Quraishi SN . Depot pipotiazine palmitate and undecylenate for schizophrenia . The Cochrane Database of Systematic Reviews . 3 . 4 . CD001720 . October 2004 . 15495016 . 10.1002/14651858.CD001720.pub2 . 7025786 .
- Web site: Piportil® L4 (pipotiazine palmitate) . https://web.archive.org/web/20211202083516/http://products.sanofi.ca/en/piportil-l4.pdf . 11 December 2023. 2021-12-02 .
- Web site: White J . Guidance on the Administration to Adults of Oil-based Depot and other Long-acting Intramuscular Antipsychotic Injections 7th Edition . www.reach4resource.co.uk . 11 December 2023 . July 2022.
- Haddad P, Taylor M, Patel MX, Taylor D . Guidance on switching away from Piportil Depot® (pipotiazine palmitate) injection . The British Journal of Psychiatry . 206 . 6 . 521 . June 2015 . 26034183 . 10.1192/bjp.206.6.521 . free .
