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Entacapone

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Information about Entacapone

Droxidopa is an orally available prodrug of norepinephrine that is used in the treatment of symptomatic orthostatic hypotension due to neurogenic causes of autonomic failure. 

Entacapone
Entacapone

Liver safety of Entacapone

Droxidopa has had limited clinical use, but has not been linked to serum enzyme elevations nor to instances of clinically apparent acute liver injury.

Mechanism of action of Entacapone

Droxidopa (drox" i doe' pa) is a prodrug of norepinephrine (noradrenaline) a major adrenergic neurotransmitter important in maintenance of sympathetic autonomic tone and normal blood pressure.  Unlike norepinephrine, however, droxidopa does not cross the blood-brain barrier, so that its effects are restricted to the periphery where it acts on the smooth muscle of arteries and arterioles to maintain blood pressure, particularly in response to standing.  In short term clinical trials, droxidopa showed modest effects in improving symptoms of postural hypotension in patients with neurogenic causes.  The neurogenic causes of primary autonomic failure include Parkinson disease and multiple systemic atrophy (Shy Drager syndrome). 

FDA approval information for Entacapone

Droxidopa was approved for use in the United States in 2014 and current recommendations are limited to treatment of orthostatic hypotension due to neurogenic causes. 

Dosage and administration for Entacapone

Droxidopa is available as capsules of 100, 200 and 300 mg.  The typical initial dose is 100 mg three times daily, with subsequent titration based upon efficacy and tolerance to as much as 600 mg three times daily. 

Side effects of Entacapone

Common side effects include headache, dizziness, nausea and hypertension.  Rare instances of neuroleptic malignant syndrome have been reported with its use.

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