Abstract
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
Highlights
In cerebrovascular disorders, special attention is paid to a hypertensive cerebrovascular crisis, which combines a vascular injury of the brain and hypertension
Research Results in Pharmacology 5(2): 71–77 besylate; nimodipine; mexidol; picamilon, which were administered through a polyethylene catheter into the femoral vein of animals
The study showed that S-Amlodipine nicotinate is superior to amlodipine besylate in efficacy and duration of the hypotensive effect, which corresponds to the literature data (Kim et al 2008)
Summary
Special attention is paid to a hypertensive cerebrovascular crisis, which combines a vascular injury of the brain and hypertension. Restoration of blood supply to the affected area of the brain for the rapid supply of oxygen and glucosein is a generally recognized strategy in the treatment of patients with ischemic cerebrovascular disorders This is shown by the high efficacy of reperfusion therapy which includes a combination of systemic thrombolysis and mechanical thrombectomy using stent retrievers (Lee 2017, Skvortsova et al 2018). Mexidol (Tanashyan et al 2012, Voronina 2000), picamilon (Gusev et al 2018, Mirzoyan et al 2018) and a calcium channel blocker nimodipine (Nishizawa et al 2008, Scriabine and van den Kerckhoff 1988), which possess significant cerebrovascular antiischemic activity (Mirzoyan et al 2018) It is well-known that an inhibitory neurotransmitter – GABA – is involved in the regulation of cerebral circulation, dilating cerebral vessels as a result of interaction with GABA A-receptors located in the vessels (Krause et al.1980, Mirzoyan et al 1970, Napoleon et al 1987). Agents with a GABAergic component in the mechanism of action in the cerebral ischemic injury, by activating the GABAergic system, contribute to the restoration of balance between inhibitory and excitatory processes in the central nervous system
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