耐药性:哪些药物是P-糖蛋白的基质,哪些不是?
Javier Aylón Val1, Virgilio Hernando-Requejo2,3,4
1Department of Internal Medicine, Severo Ochoa University Hospital, Leganés, Madrid, Spain.
Current neuropharmacology
|July 2, 2025
概括
通过限制大脑访问,P-glycoprotein (P-gp) 影响抗发作药物耐药性. 本综述澄清了哪些抗发作药物是P-gp基质,根据现有证据确定了可能的基质和非基质.
科学领域:
- 神经科学是一个神经科学.
- 药理学 药理学是指药理学的学科.
- 遗传学 遗传学 是一个
背景情况:
- P-glycoprotein (P-gp) 是抗发作药物耐药性的关键因素,影响药物进入中枢神经系统.
- 现有的文献提供了不清楚的答案,关于哪些抗发作药物是P-gp的基质.
研究的目的:
- 为了澄清哪些抗发作药物是P-糖蛋白的基质.
- 根据抗发作药物与P-gp的相互作用提供抗发作药物的可能分类.
主要方法:
- 对涉及细胞系,动物模型 (老鼠,狗,灵长类动物) 和人类志愿者的研究进行系统审查.
- 对药物动力学数据,耐药性模型,P-gp淘汰研究和人类等位基因变异研究的分析.
- 权衡证据,优先考虑人类研究而不是动物或矛盾的发现.
主要成果:
- 芬尼托因,芬诺巴比塔尔,奥克斯卡巴兹,拉莫特里金,托皮拉和潜在的拉科萨米德可能是P-gp基质.
- 布里瓦拉cetam,Zonisamide,瓦尔酸,Perampanel,加巴丁和维加巴特林可能不是P-gp基质.
- 对于卡巴马兹平,埃斯利卡巴兹平,莱维特拉塞坦,蒂亚加宾,费尔巴马特,普雷加巴林,鲁菲纳米德,埃佐加宾和雷蒂加宾的数据还不够.
结论:
- 在抗发作药物的有效性中P-gp的作用是复杂的,需要仔细考虑单个药物的特性.
- 本综述提供了一个可能的分类,以指导临床和研究努力管理耐药性.
- 对于缺乏关于P-gp基质状态的证据的药物,需要进一步研究.
相关概念视频
Antiepileptic Drugs: GABAergic Pathway Potentiators
671
γ-aminobutyric acid or GABA, plays a pivotal role as an inhibitory neurotransmitter in the brain. GABA pathway potentiators, also known as GABAergic drugs, are a class of pharmaceutical agents designed to enhance the functioning of the GABAergic system. These medications primarily treat epilepsy, a neurological disorder characterized by recurrent seizures.
The key GABA pathway potentiators used in epilepsy management are as follows.
Benzodiazepines are a well-known class of drugs used for...
The key GABA pathway potentiators used in epilepsy management are as follows.
Benzodiazepines are a well-known class of drugs used for...
671
Antiepileptic Drugs: Glutamate Antagonists
526
Glutamate is a fundamental neurotransmitter in the central nervous system, playing a vital role in neuronal communication and various cognitive processes. Glutamate stands as the principal excitatory neurotransmitter in the brain. Its presence is crucial for the communication between neurons, underpinning essential processes such as synaptic transmission, neuronal excitability, and plasticity. These functions are vital for higher-order cognitive processes, including learning and memory. The...
526
Antiepileptic Drugs: Potassium Channel Activators
286
Ezocgabine or retigabine, an antiepileptic drug of remarkable efficacy, has revolutionized the management of seizures. It is a potassium channel activator, explicitly targeting the family of Q subtype potassium channels. It enhances the transmembrane potassium currents, regulating neuronal excitability. This action stabilizes the resting membrane potential, a pivotal factor in mitigating the hyperexcitability that characterizes epilepsy.
Ezogabine has gained approval as an adjunctive treatment...
Ezogabine has gained approval as an adjunctive treatment...
286
Antiepileptic Drugs: Modulators of Neurotransmitter Release Mediated by SV2A Protein
459
Antiepileptic drugs, such as levetiracetam (Keppra) and brivaracetam (Briviact), have emerged as crucial tools in managing epilepsy. These medications exert their therapeutic effects by targeting the synaptic vesicle protein SV2A, a transmembrane glycoprotein primarily found in the brain.
SV2A is a transmembrane glycoprotein located predominantly in the brain, modulating the release of neurotransmitters for neuronal communication. Both levetiracetam and brivaracetam exhibit a high affinity for...
SV2A is a transmembrane glycoprotein located predominantly in the brain, modulating the release of neurotransmitters for neuronal communication. Both levetiracetam and brivaracetam exhibit a high affinity for...
459
Antiepileptic Drugs: Sodium Channel Blockers
927
Antiepileptic drugs are specialized medications that prevent seizures in individuals diagnosed with epilepsy. These drugs primarily function by blocking the movement of sodium ions through channels in the neuronal membrane, inhibiting the repetitive firing of action potentials often associated with seizures.
Sodium channel blockers modulate ion channels, particularly voltage-gated sodium channels. They block only sodium ion movement.
Among the most commonly prescribed antiepileptic drugs are...
Sodium channel blockers modulate ion channels, particularly voltage-gated sodium channels. They block only sodium ion movement.
Among the most commonly prescribed antiepileptic drugs are...
927
Antiepileptic Drugs: Calcium Channel Blockers
648
Calcium channel blockers, a class of antiepileptic drugs, regulate the flow of calcium ions within neurons.
Calcium channel blockers exert their antiepileptic effects by targeting T-type calcium channels, which are integral to transmitting nerve signals in the central nervous system. These channels allow the passage of calcium ions, which are vital for neuronal communication. By inhibiting T-type calcium channels, calcium channel blockers effectively reduce the release of neurotransmitters and...
Calcium channel blockers exert their antiepileptic effects by targeting T-type calcium channels, which are integral to transmitting nerve signals in the central nervous system. These channels allow the passage of calcium ions, which are vital for neuronal communication. By inhibiting T-type calcium channels, calcium channel blockers effectively reduce the release of neurotransmitters and...
648


