Droxidopa
(Redirected from
L-DOPS
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| Clinical data | |
|---|---|
| Trade names | Northera |
| Other names | β,3-Dihydroxytyrosine |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a614025 |
| License data | |
| Routes of administration | By mouth |
| ATC code | |
| Legal status | |
| Legal status | |
| Pharmacokinetic data | |
| Bioavailability | 90% |
| Metabolism | Liver |
| Elimination half-life | 1.5 hours |
| Excretion | Kidney |
| Identifiers | |
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JSmol) | |
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Droxidopa (
INN; trade name Northera; also known as L-DOPS, L-threo-dihydroxyphenylserine, L-threo-DOPS and SM-5688) is a synthetic amino acid precursor which acts as a prodrug to the neurotransmitter norepinephrine (noradrenaline).[2] Unlike norepinephrine, droxidopa is capable of crossing the protective blood–brain barrier (BBB).[2]
Medical uses
- Neurogenic orthostatic hypotension (NOH) in dopamine beta hydroxylase deficiency,[3] as well as NOH associated with multiple system atrophy (MSA),[4] familial amyloid polyneuropathy (FAP), pure autonomic failure (PAF).[5]
- Intradialytic hypotension (IDH) or hemodialysis-induced hypotension.
- Freezing of gait in Parkinson's disease (off-label)
Side effects
With over 20 years on the market, droxidopa has proven to have few side effects of which most are mild. The most common side effects reported in clinical trials include headache, dizziness, nausea, hypertension and fatigue.[6][7][8]
Pharmacology
Droxidopa is a
Droxidopa can also cross the
DOPA decarboxylase inhibitor (DDC) such as carbidopa (Lodosyn) to increase central norepinephrine concentrations while minimizing increases of peripheral levels.[citation needed
]
Chemistry
Droxidopa, also known as L-threo-dihydroxyphenylserine (L-DOPS), is chemically analogous to
levodopa (L-3,4-dihydroxyphenylalanine; L-DOPA). Whereas levodopa functions as a precursor and prodrug to dopamine, droxidopa is a precursor and prodrug of norepinephrine.[citation needed
]
History
Droxidopa was developed by Sumitomo Pharmaceuticals for the
Dainippon Sumitomo Pharma licensed droxidopa to Chelsea Therapeutics to develop and market it worldwide except in Japan, Korea, China, and Taiwan. In February 2014, the Food and Drug Administration approved droxidopa for the treatment of symptomatic neurogenic orthostatic hypotension.[10]
Clinical trials
A
clinical trials comparing the clinical use of droxidopa and midodrine have found that midodrine was more likely to cause supine hypertension than droxidopa in patients with NOH. Midodrine was also found to be slightly more effective at raising blood pressure but not statistically significantly so.[11]
Chelsea Therapeutics obtained
orphan drug status (ODS) for droxidopa in the US for NOH, and that of which associated with PD, PAF, and MSA. In 2014, Chelsea Therapeutics was acquired by Lundbeck along with the rights to droxidopa which was launched in the US in Sept 2014.[12]
Research
Droxidopa alone and in combination with carbidopa has been studied in the treatment of attention deficit hyperactivity disorder (ADHD).[13][14]
References
- FDA. Retrieved 22 Oct 2023.
- ^ PMID 17214596.
- ^ S2CID 29861644.
- S2CID 189866517.
- PMID 31996627.
- PMID 24944260.
- S2CID 2828467.
- ^ "Highlights of prescribing information for Northeratm (droxidopa)" (PDF). Chelsea Therapeutics, Inc. 2014.
- ^ S2CID 15693501.
- ^ "FDA grants accelerated approval to NORTHERA (droxidopa) for patients with symptomatic NOH". news-medical.net. February 18, 2014.
- S2CID 49674644.
- ^ "Lundbeck Announces Availability of NORTHERATM (droxidopa) Capsules in the U.S. for Symptomatic Neurogenic Orthostatic Hypotension" (PDF). Lundbeck NA Ltd. Archived from the original (PDF) on 2018-09-20. Retrieved 2015-11-02.
- S2CID 33004517.
- S2CID 20990991.
External links
- "Droxidopa". Drug Information Portal. U.S. National Library of Medicine.
