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棕榈酸哌泊噻嗪:一种新型长效肌肉注射抗精神病药物在重症精神分裂症患者中的评估

Pipotiazine palmitate: an evaluation of a new long acting intramuscular antipsychotic agent in severely ill schizophrenic patients.

作者信息

Gallant D M, Mielke D, Bishop G, Oelsner T, Guerrero-Figueroa R

出版信息

Dis Nerv Syst. 1975 Apr;36(4):193-6.

PMID:1090427
Abstract

Findings in this study support earlier investigations in attesting to the antipsychotic efficacy and relatively low toxicity of pipotiazine palmitate. Results with all efficacy measures utilized were consistent in indicating a high level of efficacy for this investigational compound. Pipotiazine palmitate apparently has an average duration of action that extends beyond 4 weeks in severely ill schizophrenic patients. This particular long acting IM antipsychotic preparation appears to have an even longer duration of activity than some of the other available standard long acting agents. The optimal dosage range for severely ill schizophrenic patients appears to be between 100 and 600 mg once monthly. While this type of drug (as is the case with many antipsychotic drugs) does reduce the psychotic symptomatology and improves the thought associations sufficient to enable the patient to leave the hospital, it should be re-emphasized that socioeconomic and guidance counseling services are necessary to maintain the patient in the community. The availability of this type of long acting preparation is not only economical in terms of nursing care and hospital cost but it should also increase the efficacy of psychopharmacologic treatment of schizophrenics by reducing both patient errors and staff errors in administration of medication. In addition, this IM preparation should prove to be of invaluable help in maintaining the schizophrenic patient in his community by reducing the relapse and the rehospitalization rates. It should be noted that there are schizophrenic patients who either absorb compounds from the gastrointestinal tract in a very poor manner or too rapidly metabolize the antipsychotic agents with resultant suboptimal blood levels and these subjects may be called "drug refractory." This type of long acting medication is an ideal preparation for the schizophrenic patient who has these types of absorption or metabolic problems since the "circulatory pass" through the liver is minimal after IM medication as compared to that encountered by an orally administered agent. The clinical disadvantage of pipotiazine palmitate is the delay in onset of therapeutic activity after injection. Significant improvement is first noted after 3 to 4 days after the highest IM dosage administration. Therefore, it may be necessary to use an oral or IM preparation of a neuroleptic with a more rapid onset of activity or utilize an oral dosage of the pipotiazine salt during the first week following IM administration of pipotiazine palmitate.

摘要

本研究结果支持了早期的调查,证实了棕榈酸哌泊噻嗪的抗精神病疗效和相对较低的毒性。所采用的所有疗效指标的结果均一致表明,这种研究用化合物具有很高的疗效。对于重症精神分裂症患者,棕榈酸哌泊噻嗪的平均作用持续时间显然超过4周。这种特殊的长效肌肉注射抗精神病制剂的活性持续时间似乎比其他一些现有的标准长效制剂还要长。重症精神分裂症患者的最佳剂量范围似乎是每月100至600毫克。虽然这类药物(与许多抗精神病药物一样)确实能减轻精神病症状,并充分改善思维联想,使患者能够出院,但应再次强调,社会经济和指导咨询服务对于患者在社区中的维持是必要的。这种长效制剂的可用性不仅在护理和医院成本方面具有经济性,而且还应通过减少患者用药错误和工作人员给药错误来提高精神分裂症患者的心理药物治疗效果。此外,这种肌肉注射制剂应能通过降低复发率和再住院率,在维持精神分裂症患者在社区生活方面证明具有巨大帮助。应当指出,有些精神分裂症患者要么胃肠道对化合物的吸收很差,要么抗精神病药物代谢过快,导致血药浓度不理想,这些患者可称为“药物难治性”患者。对于有这类吸收或代谢问题的精神分裂症患者,这种长效药物是一种理想的制剂,因为与口服药物相比,肌肉注射药物后通过肝脏的“循环通路”最小。棕榈酸哌泊噻嗪的临床缺点是注射后治疗活性起效延迟。在给予最高剂量肌肉注射后3至4天首次观察到明显改善。因此,在肌肉注射棕榈酸哌泊噻嗪后的第一周,可能有必要使用起效更快的口服或肌肉注射抗精神病制剂,或者使用棕榈酸哌泊噻嗪盐的口服剂量。

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