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Background: Smoking cessation is considered as a good solution for stroke prevention. Unfortunately, first-line therapies to reduce cigarette smoking are not always useful. Some clinical effects of these drugs are able to produce cardiovascular adverse events. Case Report: We present the case of a woman with hypertension, well treated with bisoprolol, who has a nonfatal hemorrhagic stroke event due to an exacerbation of baseline hypertension. The addition of an atypical antidepressant for smoking cessation to her antihypertensive treatment would be the cause of this cerebrovascular accident. Conclusions: Drug therapy is a logical approached. A rational therapeutic decision includes selecting patients and specific drugs. Perhaps, bupropion, an atypical antidepressant, may not be useful for smoking cessation if patients are hypertensives and well treated with specific drugs. This drug is unable to reduce cardiovascular risks in those patients.