Alzheimer's disease (AD) is the most common cause of dementia in the elderly. AD afflicts 0.3 to 0.5 million people in Korea, and the number is projected to increase to 2 million by the year of 2050. This article provides a brief overview of the most popular drug therapies in the treatment of AD including cholinesterase inhibitors (AchEIs) (donepezil, galantamine, rivastigmine), NMDA receptor antagonist (memantine), acetyl-l-carnitine, antioxidant vitamins, and Ginko biloba. Based on a review of relevant papers in the literature, this article presents pharmacological and clinical safety profiles of these agents and prescribing tips as well as a final summary on the effectiveness, safety, and alerts for clinicians. AchEIs as well as memantine will continue to play an important role in the treatment armamentarium for AD, even though newer strategies are being explored. There is not enough evidence supporting the continuous use of other drugs such as acetyl-l-carnitine, antioxidant vitamins, and Ginko biloba for the treatment of AD.