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Northera (DROXIDOPA)
Northera works by increasing the levels of certain neurotransmitters in the brain, such as norepinephrine, to help regulate blood pressure and movement.
Northera (Droxidopa) is a small molecule catecholamine developed by Lundbeck NA Ltd, targeting the muscarinic acetylcholine receptor M1. It is FDA-approved for treating orthostatic hypotension and Parkinson's disease. As an off-patent medication, Northera is available from multiple generic manufacturers. The drug has a half-life of 2.5 hours and high bioavailability of 90%. Key safety considerations include its potential to increase blood pressure and heart rate.
At a glance
| Generic name | DROXIDOPA |
|---|---|
| Sponsor | Lundbeck Na Ltd |
| Drug class | Catecholamine |
| Target | Muscarinic acetylcholine receptor M1 |
| Modality | Small molecule |
| Therapeutic area | Metabolic |
| Phase | FDA-approved |
| First approval | 2014 |
Mechanism of action
The exact mechanism of action of Droxidopa capsule in the treatment of neurogenic orthostatic hypotension is unknown. Droxidopa is synthetic amino acid analog that is directly metabolized to norepinephrine by dopa-decarboxylase, which is extensively distributed throughout the body. Droxidopa is believed to exert its pharmacological effects through norepinephrine and not through the parent molecule or other metabolites. Norepinephrine increases blood pressure by inducing peripheral arterial and venous vasoconstriction. Droxidopa in humans induces small and transient rises in plasma norepinephrine.
Approved indications
- Orthostatic dizziness, lightheadedness, or the feeling of about to black out due to nOH
Boxed warnings
- WARNING: SUPINE HYPERTENSION WARNING: SUPINE HYPERTENSION See full prescribing information for complete boxed warning. Monitor supine blood pressure prior to and during treatment and more frequently when increasing doses. Elevating the head of the bed lessens the risk of supine hypertension, and blood pressure should be measured in this position. If supine hypertension cannot be managed by elevation of the head of the bed, reduce or discontinue droxidopa [see Warnings and Precautions (5.1) ].
Common side effects
- Falls
- Urinary tract infections
- Headache
- Syncope
- Dizziness
- Hypertension
- Nausea
- Chest pain
- Blurred vision
- Pancreatitis
- Abdominal pain
- Vomiting
Drug interactions
- norepinephrine, ephedrine, midodrine, triptans
- DOPA decarboxylase inhibitors
- non-selective MAO inhibitors, linezolid
Key clinical trials
- Phase I/II Study of NORTHERA (DROXIDOPA) for Dysautonomia in Pediatric Survivors of Menkes Disease. (PHASE1,PHASE2)
- Effects of Midodrine and Droxidopa on Splanchnic Capacitance in Autonomic Failure (PHASE1)
- NORTHERA (DROXIDOPA) for Dysautonomia in Adult Survivors of Menkes Disease and Occipital Horn Syndrome (PHASE1,PHASE2)
- Autonomic Dysfunction in Patients Following Bariatric Surgery: The ADiPOSE Study
- Droxidopa / Pyridostigmine in Orthostatic Hypotension (PHASE2)
- Droxidopa to Increase Mean Arterial Pressure in Decompensated Cirrhosis Patients With Acute Kidney Injury (PHASE2)
- Northera Improves Postural Tachycardia Syndrome (POTS) and Postural Vasovagal Syncope (VVS) (PHASE2)
- Dose Response to the Norepinephrine Precursor Droxidopa in Hypotensive Individuals With Spinal Cord Injury (PHASE4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |