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Background: Elevated blood pressure is common in patients with acute ischemic stroke. Thrombolytic therapy is contraindicated in patients with a systolic blood pressure greater than 185 mmHg or diastolic blood pressure greater than 110 mmHg. Elevated blood pressure can lead to a delay in thrombolytic therapy, which is associated with increased morbidity. There is currently insufficient evidence to support the use of a specific antihypertensive agent in this setting. Objective: This study aimed to compare the effects of labetalol, nicardipine, or hydralazine on time to target blood pressure before alteplase administration in patients with acute ischemic stroke. Methods: A retrospective chart review was conducted to identify patients who received labetalol, nicardipine, or hydralazine to treat elevated blood pressure (systolic blood pressure > 185 or diastolic blood pressure > 110) before intravenous alteplase therapy for ischemic stroke. Data collection included time to blood pressure control, door-to-needle time, total dose administered, and use of additional antihypertensive agent(s). Results: Most patients in this study received labetalol (25/29). Median time to blood pressure control was 10, 22, and 15 minutes in the labetalol, nicardipine, and hydralazine groups, respectively. Among patients who received labetalol, the average time to blood pressure control was 10 minutes longer in those who received 10 mg initially versus those who received 20 mg. Patients who required higher total doses of labetalol tended to achieve blood pressure control more slowly, had longer door-to-needle times, and required additional antihypertensive agents. Conclusions: Adequate initial dosing of antihypertensive treatment has the potential to reduce time to blood pressure control and possibly time to alteplase therapy. The optimal antihypertensive regimen for controlling blood pressure before alteplase therapy remains unclear.