Milton G V, Jann M W
Southern School of Pharmacy, Mercer University, Atlanta, Georgia, USA.
Clin Pharmacokinet. 1995 Jun;28(6):494-504. doi: 10.2165/00003088-199528060-00007.
Psychotic symptoms related to mental and medical disorders can pose a medical emergency. Selecting an appropriate antipsychotic medication to treat this emergency is based on the clinical situation, preferred route of administration, pharmacokinetic profile of the antipsychotic and the medications currently being taken by the patient. Intramuscular preparations are usually preferred over oral medication when the patients are not co-operative and require drugs with a faster onset of action and good bioavailability. High potency antipsychotics such as haloperidol and fluphenazine are effective in stabilising patients with psychotic symptoms quickly. Loxapine is an alternative when sedation is necessary and molindone is useful if a short-acting antipsychotic is required. Rapid neuroleptisation with intramuscular preparations of antipsychotic achieves therapeutic drug concentrations more rapidly, and also provides optimal control of psychotic symptoms. If the patient is cooperative, liquid oral preparations can be used; they are as effective as intramuscular formulations. If long term treatment with an antipsychotic in necessary and patients are stabilised, they can be switched from intramuscular to oral preparations. The oral dose is usually 1.5 to 5 times the total intramuscular dose per day, based on the bioavailability of the antipsychotic medication. If the patient is currently taking antipsychotic medication when the emergency situation occurs, it is usually adequate to increase the dose of antipsychotic drug. Appropriate dose adjustment or antipsychotic selection is necessary when drug interactions are expected. An in-depth knowledge of the pharmacokinetic profile and drug interaction profile of antipsychotic in necessary for the selection of the appropriate antipsychotic for any given emergency situation.
与精神和医学疾病相关的精神病性症状可能会引发医疗急症。选择合适的抗精神病药物来治疗这种急症,需基于临床情况、首选给药途径、抗精神病药物的药代动力学特征以及患者目前正在服用的药物。当患者不配合且需要起效更快、生物利用度良好的药物时,通常优先选择肌内注射制剂而非口服药物。高效能抗精神病药物如氟哌啶醇和氟奋乃静,在快速稳定有精神病性症状的患者方面很有效。当需要镇静作用时,洛沙平是一种选择;若需要短效抗精神病药物,吗茚酮会很有用。用抗精神病药物的肌内注射制剂进行快速神经阻滞能更快达到治疗药物浓度,还能对精神病性症状提供最佳控制。如果患者配合,可以使用液体口服制剂;它们与肌内注射制剂效果相同。如果需要用抗精神病药物进行长期治疗且患者病情稳定,可从肌内注射制剂转换为口服制剂。根据抗精神病药物的生物利用度,口服剂量通常为每日总肌内注射剂量的1.5至5倍。如果在紧急情况发生时患者正在服用抗精神病药物,通常增加抗精神病药物的剂量就足够了。当预期有药物相互作用时,需要进行适当的剂量调整或选择合适的抗精神病药物。对于为任何给定紧急情况选择合适的抗精神病药物而言,深入了解抗精神病药物的药代动力学特征和药物相互作用特征是必要的。