Mechanism of action: Droxidopa balliculeVisual mnemonic: Droxidopa mascot “Northern Drox” drox = dog/fox hybrid general color scheme of the norepinephrine ballicule → metabolized to NE
What it isNorepinephrine prodrug; neurogenic orthostatic hypotension.
Why this oneUnlike midodrine, it crosses the blood-brain barrier and replaces norepinephrine rather than directly constricting vessels.
What limits itSupine hypertension — the last dose must be at least three hours before lying down. Benefit may wane over months.
BOXED WARNING Supine hypertension — monitor supine blood pressure before and during treatment; elevate head of bed; reduce or discontinue if uncontrolled.
FDA dosing
Population
Start
Target
Max
Neurogenic orthostatic hypotension
Adults
100 mg TID
Titrate to symptomatic response
600 mg TID (1,800 mg/day)
Titration Titrate in 100 mg TID increments every 24 to 48 hours
Renal GFR <30 mL/min: dosing recommendations cannot be provided
Hepatic Undefined
Instructions
Take consistently with or without food
Swallow capsule whole
Give last dose at least 3 hours before bedtime and elevate head of bed
Available strengths
cap 100, 200, 300 mg
Cautions
Supine hypertension and possible increased cardiovascular/stroke risk if unmanaged
Hyperpyrexia and confusion (NMS-like symptom complex)
May exacerbate ischemic heart disease, arrhythmias, and CHF
Allergic reactions including anaphylaxis/angioedema
Adverse reactions
Headache
Dizziness
Nausea
Hypertension
Pregnancy No human data; animal studies showed reduced live fetuses/embryofetal deaths.
Defining liabilityGenerally tolerated at therapeutic doses; clinically important risks are agent-specific and increase with interactions or organ impairment.