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Alzheimer's disease (AD) is the most common cause of late‐life dementia. Characterized by progressive neurodegeneration, the disease is expressed as gradual memory loss together with decline in cognitive abilities and other brain functions. Despite extensive research over the past decade, the cause and cure of AD both remain largely unknown. Several AD‐associated deficits have been targeted for interventions, including those based on amyloid‐beta, tau, and inflammation hypotheses. Only 2 types of medications—cholinesterase inhibitors and memantine—have been approved, to control the cognitive symptoms of AD such as the loss of memory, language, and executive function. Noninvasive in vivo functional magnetic resonance imaging (MRI) technologies, including the blood oxygen level‐dependent functional MRI, arterial spin labeling‐based perfusion MRI, and the proton magnetic resonance spectroscopy have been used to study the effect of ChEIs and memantine in the brain. Most of these studies have demonstrated increased functional activation and connectivity, increased regional brain blood flow and volume post‐treatment, and positive responses of critical brain metabolites reflecting neuronal status and functionality in patients with AD and mild cognitive impairment. The findings have contributed to the understanding of the mechanisms underlying the medication treatments and support the crucial role of functional MRI technologies in the development and refinement of AD medication therapies.