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 ?
Persons with at least one delivery of levodopa, entacapone, tolcapone, ropinirole, pramipexole, apomorphine, bromocriptine, or selegiline.
A randomized double-blinded trial followed 423 patients for 39 weeks to compare the combination of the catechol-O-methyltransferase (COMT) inhibitor entacapone and levodopa/carbidopa (LCE) with levodopa/ carbidopa alone (LC).
In my own clinical area of neurology, a recent report stated that the effect of the drug entacapone, which inhibits catechol-O-methyltransferase, in prolonging the effectiveness of L-dopa in Parkinson disease is enhanced in patients with specific polymorphisms in this enzyme (2).
15 August 2011 - US-based Impax Pharmaceuticals, the division of Impax Laboratories Inc (NASDAQ: IPXL), and UK-based healthcare company GlaxoSmithKline plc (LON:GSK), announced today top-line results of the ASCEND-PD Phase III clinical study of IPX066 versus carbidopa-levodopa plus entacapone (CLE), in patients with advanced Parkinson's disease.
Two COMT inhibitors marketed in the United States are entacapone (Comtan [R]) and tolcapone (Tasmar [R]).
Tolcapone or Entacapone can be prescribed in conjunction with levodopa, and can be useful to prevent the fluctuations in symptoms.
The Food and Drug Administration is continuing to review the cardiovascular safety of Stalevo, a three-drug-in-one pill for Parkinson's disease, after completing a meta-analysis that failed to resolve the issue of whether adding entacapone to a carbidopa/levodopa combination increases cardiovascular risk, the agency announced last month.
Vitamins and entacapone in levodopa-induced hyperhomocysteinemia: a randomized controlled study.
9 % de los pacientes reciben Levodopa carbidopa entacapone para prolongar la vida media de la Levodopa y obtener una estimulacion continua con un menor riesgo de complicaciones.
Both products contain entacapone, a COMT enzyme inhibiting agent developed and patented by Orion.
The COMT inhibitors tolcapone and entacapone are other new additions.
They have discovered that the two commercially available drugs, entacapone and tolcapone, have the potential to treat multi-drug resistant and extensively drug resistant tuberculosis.