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

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 ?
* Rasagiline and entacapone are a good place to start and should be offered to patients to reduce off-time symptoms, according to the AAN (a Level A recommendation based on multiple high-level studies; see page 276 for an explanation of Strength of Recommendation).
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.
Among them, Wockhardt's LEC (generic of Novartis's Parkinson's drug Stalevo), the first authorised generic, contributed a great deal to its revenues, followed by Entacapone (copy of another Parkinson's drug Comtan).Subsequently, the company's revenues soared and its business mix changed.
Table 1 Participant Characteristics P1 P2 P3 Gender Male Female Female Age 83 56 72 H&Y 3 2 2.5 UPDRS 46 22 26 Years with PD 5 6 12 Medication Levodopa Levodopa 300 Levodopa 400 mg/day mg/day, 300 mg/day Pramipexole 0.25 mg/day P4 P5 Gender Male Male Age 72 73 H&Y 2 2.5 UPDRS 33 33 Years with PD 10 9 Medication Levodopa Levodopa 700 800 mg/day, mg/day, Pramipexole Entacapone 4.5 mg/day, 1400 mg/day Amantadine 300 mg/day Note.
Furthermore, the bioavailability of luteolin was significantly increased by entacapone, which inhibits the methylation of luteolin by catechol-O-methyltransferase (Chen et al.
Tolcapone e Administrados Tolcapone: alcanca Entacapone concomitantemente a nivel serico maximo (Inibidores da COMT) L-Dopa, sao eficazes em 1,4 a 1,8h.
Surana, "Development and validation of zero and first order derivative: area under curve spectrophotometric methods for the determination of Entacapone in bulk material and in tablets," Pharmaceutical Methods, vol.
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.
Current treatments for PD involve dopamine agonists--drugs such as Mirapex (pramipexole) and Requip (ropinirole), which functionally mimic the effects of dopamine in the brain--and Comtan (entacapone) in conjunction with levodopa, the widely-used and effective PD medication that converts to dopamine.
Drugs used in Parkinson's Disease Group Drug Dopamine receptor agonists Apomorphine, pramipexole, ropinirole, rotigotine N-Methyl-D-aspartate (NMDA) Amantadine hydrochloride receptor antagonist Levodopa Co/benedopa (levodopa/ benzeraside), co/careldopa (levodopa/carbidopa) Monoamine oxidase B inhibitors Rasagiline, selegiline (MAO-B) hydrochloride Catechol-O-methyltransferase Entacapone, tolcapone (COMT) inhibitors Antimuscarinic drugs Benztropine mesylate, orphenadrine, procyclidine, trihexyphenidyl Table 2.
Entacapone Tablets USP, 200 mg Sun Pharma Global Comtan Tablets
Miljanic, "Quantitative analysis of entacapone isomers using surface-enhanced Raman spectroscopy and partial least squares regression," Applied Spectroscopy, vol.