Droxidopa is a synthetic amino acid precursor which acts as a prodrug to the neurotransmitter norepinephrine (noradrenaline).
L-DOPS
It is used to increase the concentrations of these neurotransmitters in the body and brain.
Unlike norepinephrine, Droxidopa is capable of crossing the blood–brain barrier.
Trade name Northera.
Bioavailability 90%
Metabolism-liver
Elimination half-life 1.5 hours
Excretion- Kidney
Indications: Neurogenic orthostatic hypotension (NOH) of dopamine beta hydrolase deficiency, multiple system atrophy (MSA), familial amyloid polyneuropathy (FAP), pure autonomic failure (PAF), hemodialysis-induced hypotension.
The use of droxidopa and midodrine compared: have found that midodrine was more likely to cause supine hypertension than droxidopa in patients with neurogenic orthostatic hypotension.
Midodrine was also found to be slightly more effective at raising blood pressure.
Patients with neurogenic orthostatic hypotension have depleted levels of norepinephrine which leads to decreased blood pressure or hypotension upon orthostatic challenge.
Droxidopa works by increasing the levels of norepinephrine in the peripheral nervous system (PNS).
It enables the body to maintain blood flow upon and while standing.
It can cross the blood–brain barrier (BBB) where it is converted to norepinephrine from within the brain.
Increased levels of norepinephrine in the central nervous system (CNS) may be beneficial to patients in a wide range of indications.
It can be coupled with a peripheral aromatic L-amino acid decarboxylase inhibitor or DOPA decarboxylase inhibitor, such as carbidopa to increase central norepinephrine concentrations while minimizing increases of peripheral levels.
The most common side effects reported in clinical trials include headache, dizziness, nausea, hypertension and fatigue.