通过延长剂量间隔来实施长效注射抗精神病药物的逐渐,过度缩小:一个在中建模研究
James R O'Neill1, David M Taylor2, Mark A Horowitz3
1South West Yorkshire Partnership NHS Foundation Trust, Newton Lodge, Ouchthorpe Lane, Wakefield WF1 3SP, UK.
Therapeutic advances in psychopharmacology
|September 18, 2023
概括
长效阿里皮普拉注射剂 (ALAI) 的过度缩减可以降低戒断风险. 这种方法,使用延长的间隔和剂量调整,为患者提供了一种更安全的替代方案,而不是突然停止治疗.
科学领域:
- 药理学 药理学是指药理学的学科.
- 神经科学是一个神经科学.
- 临床药房 临床药房
背景情况:
- 逐渐缩减的目的是通过保持生理平衡来最大限度地减少戒断效应和复发风险.
- 长效注射抗精神病药 (LAI) 需要在停用期间进行谨慎管理.
- 阿里皮普拉长效注射剂 (ALAI) 是一种常见的LAI,用于精神病治疗.
研究的目的:
- 为了开发临床戒断方案,将*in silico*的过度缩小原理应用于ALAI.
- 为了模拟突然停止ALAI与逐渐逐渐减少对多巴胺D2受体占用量的影响.
- 设计从ALAI到口服抗精神病药物的安全过渡策略.
主要方法:
- 从现有研究和专家共识中推导出逐渐缩小率的门.
- 使用ALAI的药理动力学数据用于*in silico*建模.
- 模拟ALAI的突然停止,剂量间隔延长和剂量减少.
主要成果:
- 突然停止ALAI导致D2占用率迅速减少 (16.8%/月).
- 延长ALAI的剂量间隔 (例如400mg从4到7周) 减缓了D2占用率的减少.
- 模拟的超标渐变疗法涉及间隔延长和随后的剂量减少 (300mg) 与口服切换.
结论:
- 通过调整剂量间隔和剂量,可以实现ALAI的过度缩小.
- 这种逐步的方法可以减轻与突然停止LAI相关的风险.
- 过渡到口服药物对于管理药物残留水平和防止D2占用率快速变化至关重要.
相关概念视频
One-Compartment Open Model for IV Bolus Administration: Estimation of Elimination Rate Constant, Half-Life and Volume of Distribution
323
The one-compartment open model is a simplified approach used in pharmacokinetics to understand the distribution and elimination of a drug administered through an intravenous bolus. This model assumes rapid drug dispersal throughout the body and elimination using a first-order process. Key pharmacokinetic parameters, such as the elimination rate constant (k), half-life (t1/2), and the apparent volume of distribution (Vd), can be estimated from this model. The elimination rate is calculated...
323
One-Compartment Open Model for IV Bolus Administration: General Considerations
240
The one-compartment model is a pharmacokinetic tool that models the body as a single, uniform compartment, facilitating the understanding of drug distribution and elimination. This model is particularly beneficial for intravenous (IV) bolus administration, where the drug rapidly circulates throughout the body.
The drug's presence in the body is defined by an equation representing the difference between the rates of drug entry and exit. Key parameters—elimination rate constant,...
The drug's presence in the body is defined by an equation representing the difference between the rates of drug entry and exit. Key parameters—elimination rate constant,...
240
Nonlinear Pharmacokinetics: Drug Elimination for IV Bolus Injection
91
In pharmacokinetics, the elimination rate of a drug following a capacity-limited model is primarily controlled by two parameters: Vmax and KM. These parameters are crucial in how the drug behaves inside the body after administration.
Following the administration of a single intravenous (IV) bolus injection, we can determine the concentration of the drug in the plasma at any given time. This calculation is achieved using a specific equation that integrates the values of Vmax and KM.
We can also...
Following the administration of a single intravenous (IV) bolus injection, we can determine the concentration of the drug in the plasma at any given time. This calculation is achieved using a specific equation that integrates the values of Vmax and KM.
We can also...
91
Two-Compartment Open Model: IV Bolus Administration
572
The two-compartment model for intravenous (IV) bolus administration illustrates drug distribution in the body, subdividing it into central and peripheral compartments. This model operates on the concept of two-compartment kinetics. The drug's plasma concentration shows a bi-exponential decline following IV bolus administration, signaling the presence of two disposition processes: distribution and elimination.
The disparity between drug input and the sum of drug transfer rates between...
The disparity between drug input and the sum of drug transfer rates between...
572
Desensitization and Tachyphylaxis
1.8K
Tachyphylaxis is described as a rapid decrease in response to a drug after repeated or continuous administration of the same drug dose. It is a phenomenon where the body becomes less responsive to a particular substance or intervention over time, requiring higher doses or stronger interventions to achieve the same effect. It results from adaptive changes in the body's receptors, signaling pathways, or physiological processes that occur in response to prolonged exposure to a stimulus.
1.8K
Pharmacokinetic Models: Overview
770
Pharmacokinetic models utilize mathematical analysis to achieve a detailed quantitative understanding of a drug's life cycle within the body. They are instrumental in simulating a drug's pharmacokinetic parameters, predicting drug concentrations over time, optimizing dosage regimens, linking concentrations with pharmacologic activity, and estimating potential toxicity.
There are three primary types of models: empirical, compartment, and physiological. Empirical models, with minimal...
There are three primary types of models: empirical, compartment, and physiological. Empirical models, with minimal...
770


