The major efforts to selectively deliver drugs to the brain in the past decade have relied on smart molecular techniques to penetrate the blood-brain barrier, whereas intraarterial drug delivery has drawn relatively little attention. Meanwhile, rapid progress has been made in the field of endovascular surgery. Modern endovascular procedures can permit highly targeted drug delivery by the intracarotid route. Intracarotid drug delivery can be the primary route of drug delivery or it could be used to facilitate the delivery of smart neuropharmaceuticals. There have been few attempts to systematically understand the kinetics of intracarotid drugs. Anecdotal data suggest that intracarotid drug delivery is effective in the treatment of cerebral vasospasm, thromboembolic strokes, and neoplasms. Neuroanesthesiologists are frequently involved in the care of such high-risk patients. Therefore, it is necessary to understand the applications of intracarotid drug delivery and the unusual kinetics of intracarotid drugs.