Drug/Small Molecule:
droxidopa

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PharmGKB contains no Clinical Variants that meet the highest level of criteria.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • Droxydopa
  • L-DOPS
  • L-dihydroxyphenylserine
  • L-threo-3,4-dihydroxyphenylserine
Trade Names
  • Dops
Brand Mixture Names

PharmGKB Accession Id:
PA164748386

Description

Droxidopa is a precursor of noradrenaline that is used in the treatment of Parkinsonism. It is approved for use in Japan and is currently in trials in the U.S. The racaemic form (dl-threo-3,4-dihydroxyphenylserine) has also been used, and has been investigated in the treatment of orthostatic hypotension. There is a deficit of noradrenaline as well as of dopamine in Parkinson's disease and it has been proposed that this underlies the sudden transient freezing seen usually in advanced disease.

Source: Drug Bank

Indication

For treatment of neurogenic orthostatic hypotension (NOH) associated with various disorders including Multiple System Atrophy, Familial Amyloid Polyneuropathy, hemodialysis induced hypotension and Parkinson's Disease. Also investigated for use/treatment in neurologic disorders, nephropathy, blood (blood forming organ disorders, unspecified), and dizzy/fainting spells.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Droxidopa crosses the blood-brain barrier where it is converted to norepinephrine via decarboxylation by L-aromatic-amino-acid decarboxylase. Increased levels of norepinephrine in the central nervous system (CNS) may be beneficial to patients in a wide range of indications. Norephinephrine acts at alpha-adrenergic receptors as a vasoconstrictor and at beta-adrenergic receptors as a heart stimulator and artery dilator.

Source: Drug Bank

Pharmacology

Droxidopa is an orally active synthetic precursor of norepinephrine that increases the deficient supply of norepinephrine in patients with NOH, thereby improving orthostatic blood pressure and alleviating associated symptoms of lightheadedness, dizziness, blurred vision, and syncope through the induction of tachycardia (increased heart rate) and hypertension.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Droxidopa is metabolized by aromatic L-amino acid decarboxylase.

Source: Drug Bank

Absorption

Oral bioavailability is 90%.

Source: Drug Bank

Half-Life

2-3 hours.

Source: Drug Bank

Toxicity

Droxidopa has minimal toxic effects and an acute, oral LD50 of more than 5 g/kg in mice, rats, dogs, and monkeys. Side effects occur in in 0.78% of patients and include nausea, headache, increased blood pressure, hallucination, and anorexia.

Source: Drug Bank

Route of Elimination

Droxidopa is mainly excreted in the urine, with the main metabolite being 3-O-methyldihydroxyphenylserine.

Source: Drug Bank

Chemical Properties

Chemical Formula

C9H11NO5

Source: Drug Bank

Isomeric SMILES

c1cc(c(cc1C(C(C(=O)O)N)O)O)O

Source: OpenEye

Canonical SMILES

N[C@H]([C@@H]

Source: Drug Bank

Average Molecular Weight

213.1873

Source: Drug Bank

Monoisotopic Molecular Weight

213.063722467

Source: Drug Bank

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB06262
KEGG Drug:
D01277
PubChem Compound:
443940
PubChem Substance:
24560805
99443239
ChemSpider:
391994

Clinical Trials

These are trials that mention droxidopa and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.