<p>Despite significant experimental achievements in the study of glutamate neurotoxicity and oxidative stress, neither glutamate receptor antagonists nor antioxidants have been used in the treatment of ischemic stroke because glutamate receptor antagonists block not only glutamate neurotoxicity but also excitatory processes, which leads to disorganization of the CNS function. As for oxidative stress, the high efficiency of arterial recanalization in ischemic stroke has proved the need to restore cerebral circulation. This has led to the transformation of the negative meaning of the term reperfusion into a positive one, i.e., reperfusion therapy. The incomparable effectiveness of eliminating the root cause of ischemic stroke (recanalization) has restored the importance of pharmacological effects on the blood supply to the brain. In this regard, the article discusses some pathophysiological aspects of the development of vascular pathology of the brain, in particular, the neurovascular unit and Virchow’s triad, as well as the mechanisms of action of known cerebrovascular drugs (nimodipine, picamilon, and mexidol). A new compound is also discussed, i.e., the succinic acid ester of 5-hydroxyadamantan-2-one, which has a unique combination of cerebrovascular and antiarrhythmic properties. Special attention is paid to models of cerebrovascular disorders closest to clinical conditions, in particular, to combined vascular lesions of the brain and heart. The key role of the GABA_A-ergic system in the regulation of cerebral circulation and in the mechanism of action of cerebrovascular drugs is discussed. The properties of the endogenous neuroprotector discovered by us, <i>N</i>-arachidonoyl-GABA, are presented in detail. Finally, it is quite obvious that the treatment of cerebrovascular diseases should be aimed at eliminating the root cause of the pathology, i.e., cerebral blood flow deficiency.</p>