Droxidopa is a synthetic prodrug of norepinephrine used to treat symptomatic neurogenic orthostatic hypotension (nOH) by increasing vascular tone and blood pressure, reducing dizziness and fainting. Developed in Japan in the 1980s and approved in the U.S. in 2014, it offered a targeted alternative for patients with nOH due to Parkinson’s disease, multiple system atrophy, or autonomic failure. Orally administered, droxidopa is well absorbed, metabolized to norepinephrine, and primarily excreted via the kidneys, providing symptom relief without the broad cardiovascular effects of older sympathomimetic agents. Its development represents a milestone in prodrug therapies that restore deficient neurotransmitters for improved autonomic function.