Barcia Juan A, Gallego José M
Servicio de Neurocirugía and Instituto de Neurociencias, Hospital Clínico San Carlos, Universidad Complutense de Madrid, 28040 Madrid, Spain.
Neurotherapeutics. 2009 Apr;6(2):337-43. doi: 10.1016/j.nurt.2009.01.015.
A means to avoid the pharmacokinetic problems affecting the anti-epileptic drugs may be their direct intracerebroventricular (ICV) or intracerebral delivery. This approach may achieve a greater drug concentration at the epileptogenic area while minimizing it in other brain or systemic areas, and thus it could be an interesting therapeutic alternative in drug-resistant epilepsies. The objective of this article is to review a series of experiments, ranging from actute ICV injection to continuous intracerebral infusion of anti-epileptic drugs or grafting of neurotransmitter producing cells, in experimental models, especially in the kindling model of epilepsy in the rat. Acute ICV injection of phenytoin, phenobarbital or carbamacepine is able to diminish the intensity of kindling seizures, but it is also associated with a high neurologic toxicity, especially phenobarbital. Continuous ICV infusion of anti-epileptic drugs can effectively control seizures, but neurologic toxicity is not improved compared with systemic delivery. However, systemic toxicity may be improved, as in the case of valproic acid, whose continuous ICV infusion results in very low plasmatic or hepatic drug concentrations. Continuous intracerebral infusion at the epileptogenic area was studied as an alternative to minimize neurologic toxicity. Thus, intra-amygdalar infusion of gamma-aminobutyric acid (GABA) controls seizures with minimal neurotoxicity in amygdala-kindled rats. Similarly, continuous infusion of GABA into the dorsomedian nucleus of the thalamus improves seizure spread, while not affecting the local epileptogenic activity at the amygdala. Grafting of GABA releasing cells may reduce kindling parameter severity without behavioral side effects. We may conclude that ICV or intracerebral delivery of anti-epileptic drugs or neurotransmitters may be a useful technique to modulate epilepsy.
避免抗癫痫药物所面临的药代动力学问题的一种方法可能是将其直接脑室内(ICV)或脑内给药。这种方法可以在癫痫病灶区域实现更高的药物浓度,同时将其他脑区或全身区域的药物浓度降至最低,因此在耐药性癫痫中可能是一种有趣的治疗选择。本文的目的是回顾一系列实验,从急性脑室内注射到抗癫痫药物的持续脑内输注或神经递质产生细胞的移植,这些实验均在实验模型中进行,尤其是在大鼠癫痫点燃模型中。急性脑室内注射苯妥英、苯巴比妥或卡马西平能够降低点燃性癫痫发作的强度,但也伴有较高的神经毒性,尤其是苯巴比妥。持续脑室内输注抗癫痫药物可以有效控制癫痫发作,但与全身给药相比,神经毒性并未改善。然而,全身毒性可能会改善,如丙戊酸的情况,其持续脑室内输注导致血浆或肝脏药物浓度非常低。研究了在癫痫病灶区域进行持续脑内输注作为降低神经毒性的一种替代方法。因此,在杏仁核点燃的大鼠中,向杏仁核内输注γ-氨基丁酸(GABA)可在最小神经毒性的情况下控制癫痫发作。同样,向丘脑背内侧核持续输注GABA可改善癫痫发作的扩散,同时不影响杏仁核局部的癫痫病灶活动。移植释放GABA的细胞可能会降低点燃参数的严重程度且无行为副作用。我们可以得出结论,抗癫痫药物或神经递质的脑室内或脑内给药可能是调节癫痫的一种有用技术。