Introduction: In cerebrovascular disorders, special attention is paid to a hypertensive cerebrovascular crisis, which combines a vascular injury of the brain and hypertension. The paper studies the cerebrovascular properties of the calcium channel blocker of S-Amlodipine nicotinate antihypertensive agent. Materials and methods: Tests were performed on 96 nonlinear male rats, measuring local blood flow in the cerebral cortex in 36 awake animals, using a laser Doppler flowmeter. Cerebral circulation was recorded in the animals when modeling ischemic and hemorrhagic brain injuries. Results and discussion: S-Amlodipine nicotinate (0.1 mg/kg i/v) shows a pronounced cerebrovascular activity in the models of ischemic and hemorrhagic injuries of the brain. In terms of the vasodilating effect in ischemic brain injury, the drug is comparable to mexidol, nimodipine, picamilon, but is superior to nimodipine and picamilon in terms of duration of action, and in the model of hemorrhagic stroke, S-Amlodipine nicotinate is superior to nimodipine and is comparable to picamilon and mexidol. The analysis of the mechanism of action of the agent revealed the participation of GABA A-receptors in the implementation of cerebrovascular properties of the agent. Conclusion: Significant cerebrovascular activity of S-Amlodipine nicotinate (0.1 mg/kg i/v) antihypertensive agent was revealed. The presence of GABAergic mechanism on cerebral blood flow in the agent action along with blockade of slow calcium channels ensures its high efficacy in treatment of both ischemic and hemorrhagic brain injuries.
Aim. To examine the cerebrovascular, neuroprotective and antiarrhythmic properties of fabomotizole (brand name Afobazole). Materials and methods. A comprehensive study of fabomotizole's effects on the blood supply, morphology and neuropsychology of the rat brain in various experimental disorders. We recorded cerebral blood flow and studied brain morphology in models of local permanent and global transient ischaemia, haemorrhagic brain damage, combined cerebrovascular and cardiovascular pathology, cardiac arrhythmias, and assessed the neuropsychological status. We measured the levels of GABA, glutamic acid, nerve growth factor, and heat shock protein (HSP70). Results. Fabomotizole improves blood supply, limits the area of injury, normalizes pathological brain changes in localized cerebral ischaemia, and eliminates neuropsychological damage in models of ischaemic and haemorrhagic stroke. The drug increases cerebral blood flow in ischaemic and haemorrhagic stroke, myocardial infarction and, to a greater extent, in combined cerebrovascular and coronary disease. Fabomotizole acts through the cerebrovascular GABAAergic system, as well as having significant antiarrhythmic properties. Conclusions. Fabomotizole should be considered not only as an anxiolytic, but also as a drug with potential clinical efficacy in cerebrovascular disease, with concomitant coronary disease and cardiac arrhythmias.
Introduction: The aim of this review article was to analyze in details the mechanism of drugs’ effects in the treatment and prevention of a migraine attack, as well as to discuss the hypotheses of migraine pathogenesis. Migraine attack treatment agents: The main agents for migraine attack treatment have an anti-nociceptive activity. Agents for migraine preventive treatment: β-blocker propranolol also has anti-serotonin and analgesic activities, and most drugs used for the prophylactic treatment of migraine have a vasodilating activity. Vascular hypothesis of migraine pathogenesis: Despite numerous studies that have expanded our understanding of migraine pathogenesis, the importance of the vascular component in the pathogenesis of this disease has not questioned yet. Neurogenic hypotheses of cortical spreading depression: It is necessary to take into account the points of this hypothesis in the context of the pathophysiology of migraine. Neurochemical serotonin hypotheses of migraine pathogenesis: Serotonin plays an important role in the pathogenesis of migraine. Trigemino-vascular hypotheses of migraine pathogenesis: The trigemino-vascular hypothesis claims to solve the problem of migraine pain. Migraine and ischemic brain damage: Migraine is a risk factor for ischemic stroke and cognitive disorders. Search for the new anti-ischemic anti-migraine preparations: A methodology for the search for new anti-ischemic anti-serotonin drugs for the treatment of migraine is proposed. Conclusion: Belonging of a drug to one or another pharmacological group does not always correspond to its therapeutic effect on the pathogenetic processes of migraine. Migraine with its variety of forms cannot fit only one of the proposed hypotheses on the pathogenesis of this disease. Graphical abstract:
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