entacapone


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Related to entacapone: amantadine, pramipexole, Selegiline

entacapone

 [en-tak´ah-pōn]
an antidyskinetic agent used in conjunction with levodopa and carbidopa to enhance dopaminergic stimulation of the brain and the antiparkinsonian activity of levodopa in the treatment of idiopathic Parkinson's disease, administered orally.

entacapone

Comtan, Comtess (UK)

Pharmacologic class: Catechol O-methyltransferase (COMT) inhibitor

Therapeutic class: Antidyskinetic

Pregnancy risk category C

Action

Inhibits COMT, the primary enzyme involved in metabolizing levodopa. This inhibition increases levodopa blood level and duration of action, easing symptoms of Parkinson's disease.

Availability

Tablets: 200 mg

Indications and dosages

Adjunctive treatment of idiopathic Parkinson's disease in patients experiencing wearing off of carbidopa-levodopa effects

Adults: 200 mg P.O. with each carbidopa-levodopa dose, to a maximum of eight times daily (1,600 mg)

Contraindications

• Hypersensitivity to drug

Precautions

Use cautiously in:
• hepatic or renal dysfunction, hypertension, heart disease
• pregnant and breastfeeding patients.

Administration

• Give without regard to food.
• Administer at same time as carbidopa-levodopa. Make sure patient swallows tablet whole.

Don't withdraw drug abruptly.

Adverse reactions

CNS: dizziness, depression, drowsiness, disorientation, memory loss, agitation, delusions, hallucinations, paranoia, euphoria, dyskinesia, hyperkinesia, light-headedness, paresthesia, heaviness of limbs, numbness of fingers

CV: tachycardia, orthostatic hypotension, hypertension

GI: nausea, vomiting, epigastric pain, flatulence

GU: urine discoloration

Respiratory: upper respiratory tract infection, dyspnea, sinus congestion

Other: fever

Interactions

Drug-drug.Ampicillin, chloramphenicol, cholestyramine, erythromycin, probenecid, rifampin: decreased entacapone excretion

Bitolterol, dobutamine, dopamine, epinephrine, isoetherine, isoproterenol, methyldopa, norepinephrine: increased heart rate, increased risk of arrhythmias, excessive blood pressure changes

MAO inhibitors: increased risk of toxicity

Drug-behaviors.Alcohol use: increased risk of adverse reactions

Patient monitoring

• Monitor vital signs, watching especially for orthostatic hypotension.
• Evaluate neurologic status closely. Check for hallucinations and new onset or exacerbation of dyskinesia.
• Assess respiratory status, particularly for dyspnea and signs and symptoms of upper respiratory tract infection.
• Monitor nutritional and hydration status if patient experiences vomiting.

Patient teaching

• Instruct patient to swallow tablet whole and to take it at same time as carbidopa-levodopa.

Caution patient not to stop taking drug abruptly.
• Advise patient to move slowly when sitting up or standing, to avoid dizziness or light-headedness from sudden blood pressure decrease.
• Caution patient to avoid driving and other hazardous activities until drug no longer affects concentration and alertness.

Instruct patient (and caregiver) to institute safety measures at home to prevent injury related to disease or drug's adverse CNS effects.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and behaviors mentioned above.

entacapone

/en·tac·a·pone/ (en-tak´ah-pōn) an antidyskinetic used in conjunction with levodopa and carbidopa in the treatment of idiopathic Parkinson's disease.

entacapone

an antiparkinson agent.
indications It is used to treat parkinsonism in patients who are experiencing end-of-dose decreased effect.
contraindication Known hypersensitivity to this drug prohibits its use.
adverse effects Serious adverse effects include psychosis, hallucination, hypomania, severe depression, dizziness, gastritis, GI disorders, alopecia, dark urine, back pain, dyspnea, purpura, fatigue, asthenia, and bacterial infection. Common side effects include involuntary choreiform movements, hand tremors, fatigue, headache, anxiety, twitching, numbness, dyskinesia, hypokinesia, hyperkinesia, weakness, confusion, agitation, nightmares, nausea, vomiting, anorexia, abdominal distress, dry mouth, flatulence, bitter taste, diarrhea, constipation, dyspepsia, and orthostatic hypotension.

entacapone

A nitrocatechol-class COMT (catechol-O-methyltransferase) inhibitor used to improve motor performance in Parkinson patients receiving l-DOPA/carbidopa.

Adverse effects
Dyskinesia, which often resolves with ongoing therapy; diarrhoea, nausea and abdominal pain; asymptomatic red-brown urine.

entacapone

Comtan® Neurology A COMT inhibitor which may improve motor performance in Parkinson Pts receiving levodopa/carbidopa. See Parkinson's disease.
References in periodicals archive ?
Contract award: completion of a non-exclusive discount agreement pursuant to A* 130a sgb v, section 8 to finished drug products with derwirkstoffkombination levodopa / carbidopa / entacapone (accession).
For by the tenderer in more detail in Appendix 2 to be designated for contract drug to the active ingredient og (Levodopa / Carbidopa / Entacapone - ATC code N04BA03) intends DAK health, however, pending the entry into force of occurrence of new drug discount agreements with most other, at least all interested pharmaceutical companies drug discount contracts to complete.
Administration of ND0612 together with repeated dosing of oral entacapone 200 mg showed an increase in LD plasma concentrationof ~50%, with corresponding decrease in 3-OMD plasma concentration.
The GWQ Service Plus AG intends to conduct a Europe-wide, open procurement process for the active ingredient combination levodopa / carbidopa / entacapone with contract start to 07/01/2015.
Conclusion of a non exclusive discount contract pursuant to A* 130a sgb v, section 8 to medicines with active ingredient combination of levodopa, carbidopa and entacapone (atc code: n04ba03) within the zeitraumesvom 7.
It is intended with pharmaceutical companies to conclude exclusive drug selective discount agreements within the meaning of A* 130a section 8 SGB V for the supply of medicinal products with the active ingredient combination levodopa / carbidopa / entacapone after implementation of a Europe-wide, open procurement procedure with contract start to 07/01/2015.
Contract award: statements non-exclusive discount agreements pursuant to A* 130a paragraph 8 sgb v as part of the approval procedure for drug entacapone -.
In ASCEND-PD, a trial of 91 randomized patients with advanced Parkinson's disease having "off" time, compared IPX066 versus levodopa-carbidopa plus entacapone (LCE).
Persons who used levodopa, entacapone, tolcapone, ropinirole, pramipexole, apomorphine, bromocriptine, or selegiline were directly contacted by phone and invited to be examined by a neurologist unless a) they reported taking small doses of dopamine agonists for restless leg syndrome, b) treatment was discontinued after [less than or equal to] 1 month, or c) there was a documented history of drug-induced parkinsonism.
Furthermore, the bioavailability of luteolin was significantly increased by entacapone, which inhibits the methylation of luteolin by catechol-O-methyltransferase (Chen et al.
an international pharmaceutical company strongly committed to the CNS therapeutic area, announced today that the EU Committee for Medicinal Products for Human Use (CHMP) recommended that the European Commission approve the use of Xadago(TM) (safinamide) as add-on to L-dopa alone or in combination with dopamine agonists, entacapone, amantadine, and/or anticholinergics, for the treatment of patients with mid-late stage Parkinson's disease experiencing motor fluctuations despite being stabilized on 'Standard of Care'.
COMT inhibitors: Entacapone is a peripherally acting COMT inhibitor, while tolcapone is able to cross the blood-brain barrier and acts both peripherally and in the CNS.