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尼莫地平在耳鼻喉科:从既往证据到临床展望

Nimodipine in otolaryngology: from past evidence to clinical perspectives.

作者信息

Monzani D, Genovese E, Pini L A, Di Berardino F, Alicandri Ciufelli M, Galeazzi G M, Presutti L

机构信息

Unità Operativa Complessa di Otorinolaringoiatria. Azienda Ospedaliero-Universitaria Policlinico di Modena, Italy;

Cattedra di Farmacologia Clinica, Azienda Ospedaliero-Universitaria Policlinico di Modena, Italy;

出版信息

Acta Otorhinolaryngol Ital. 2015 Jun;35(3):135-45.

Abstract

As L-type voltage-gated calcium channels (VGCCs) control Ca(2+) influx and depolarisation of cardiac and vascular smooth muscle, they represent a specific therapeutic target for calcium channel blockers (CCBs), which are approved and widely used to treat hypertension, myocardial ischaemia and arrhythmias. L-type currents also play a role in calcium entry in the sensory cells of the inner ear. In hair cells of both cochlea and labyrinth, calcium cytoplasmic influx is the first physiological process that activates complex intracellular enzymatic reactions resulting in neurotransmitter release. Excessive calcium ion entry into sensory cells, as a consequence of L-VGCCs malfunction is responsible for over-activation of phospholipase A2 and C, protein kinase II and C, nitric oxide synthase and both endonucleases and depolymerases, which can cause membrane damage and cellular death if the cytoplasmic buffering capacity is overcome. Nimodipine, a highly lipophilic 1-4 dihydropyridine that easily crosses the brain-blood barrier, is generally used to reduce the severity of neurological deficits resulting from vasospasm in patients with subarachnoid haemorrhage. Moreover, due to its selective blocking activity on L-channel calcium currents, nimodipine is also suggested to be an effective countermeasure for cochlear and vestibular dysfunctions known as channelopathies. Indeed, experimental data in amphibians and mammalians indicate that nimodipine has a stronger efficacy than other CCBs (aminopyridine, nifedipine) on voltage-dependent whole-cell currents within hair cells at rest and it is the only agent that is also effective during their mechanically induced depolarisation. In humans, the efficacy of nimodipine is documented in the medical management of peripheral vestibular vertigo, sensorineural hearing loss and tinnitus, even in a pathology as complex as Ménière's disease. Nimodipine is also considered useful in the prophylaxis of damage to the facial and cochlear nerves caused by ablative surgery of cerebellopontine tumours; it has been recently hypothesised to accelerate functional recovery of recurrent nerve lesions during thyroid cancer surgery. Further trials with adequate study design are needed to test the efficacy of nimodipine in the treatment of vertigo due to cerebrovascular disease and vestibular migraine.

摘要

由于L型电压门控钙通道(VGCCs)控制着心脏和血管平滑肌中的Ca(2+)内流和去极化,它们是钙通道阻滞剂(CCBs)的特定治疗靶点,钙通道阻滞剂已被批准并广泛用于治疗高血压、心肌缺血和心律失常。L型电流在内耳感觉细胞的钙内流中也起作用。在耳蜗和迷路的毛细胞中,钙细胞质内流是激活复杂细胞内酶促反应导致神经递质释放的第一个生理过程。由于L-VGCCs功能障碍,过多的钙离子进入感觉细胞会导致磷脂酶A2和C、蛋白激酶II和C、一氧化氮合酶以及核酸酶和解聚酶的过度激活,如果细胞质缓冲能力被克服,这可能会导致膜损伤和细胞死亡。尼莫地平是一种高度亲脂性的1-4二氢吡啶,很容易穿过血脑屏障,通常用于降低蛛网膜下腔出血患者因血管痉挛导致的神经功能缺损的严重程度。此外,由于其对L通道钙电流的选择性阻断活性,尼莫地平也被认为是治疗称为通道病的耳蜗和前庭功能障碍的有效对策。事实上,两栖动物和哺乳动物的实验数据表明,尼莫地平在静息状态下对毛细胞内电压依赖性全细胞电流的疗效比其他CCBs(氨基吡啶、硝苯地平)更强,并且它是唯一在机械诱导去极化期间也有效的药物。在人类中,尼莫地平在外周前庭性眩晕、感音神经性听力损失和耳鸣的药物治疗中,甚至在像梅尼埃病这样复杂的病症中,其疗效都有记录。尼莫地平也被认为可用于预防桥小脑肿瘤切除手术对面神经和耳蜗神经造成的损伤;最近有人推测它可加速甲状腺癌手术中喉返神经损伤的功能恢复。需要进一步进行设计充分的试验来测试尼莫地平在治疗脑血管疾病和前庭性偏头痛引起的眩晕方面的疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6fda/4510937/501b70552066/0392-100X-35-135-g001.jpg

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