Entacapone/Levodopa/Carbidopa

Entacapone/Levodopa/Carbidopa

DEA Class;  Rx

Common Brand Names; Stalevo

  • Antiparkinson Agents, COMT Inhibitors; 
  • Decarboxylase Inhibitors; 
  • Antiparkinson Agents, Dopamine Precursors
Oral combination of levodopa-carbidopa therapy with a COMT inhibitor (entacapone)
Used for adults with Parkinson’s disease
Addition of a COMT inhibitor helpful for patients whoexperience the end-of dose ‘wearing off’ effect of levodopa

Indicated for the treatment of idiopathic Parkinson’s disease.

Hypersensitivity

Concurrency with nonselective MAOIs (discontinue 2 weeks before starting treatment)

Narrow angle glaucoma

Undiagnosed skin lesions, history of melanoma

Entacapone

  • Dyskinesia (25%)
  • Nausea (14%)
  • Diarrhea (10%)
  • Hyperkinesia (10%)
  • Urine discoloration (10%)
  • Hypokinesia (9%), dizziness (8%), Fatigue (6%), hallucinations (1-4%), anxiety (2%), somnolence (2%), asthenia (2%), agitation (1%)
  • Increased sweating (2%)
  • Purpura (2%)
  • Abdominal pain (8%), constipation (6%), vomiting (4%), dry mouth (3%), dyspepsia (2%), flatulence (2%), taste perversion (1%), gastritis (1%)
  • Back pain (4%)
  • Dyspnea (3%)
  • Bacterial infection (1%)

Levodopa/Carbodopa

  • Edema
  • Agitation, anxiety, ataxia, bruxism, confusion, daytime somnolence decreased attention span, dyskinesia, dystonia, euphoria, insomnia, fainting, fatigue, increased trembling of hands, insouciance, malaise, memory loss, nightmares, nervousness, restlessness, trismus, vivid dreams
  • Alopecia, hot flushes, increased &/or dark perspiration, skin eruptions
  • Abdominal pain & discomfort, burning feeling in tongue, constipation, diarrhea, dysgeusia, dry mouth, dysphagia, hiccups, meteorism, sialorrhea, nausea, weight loss
  • Muscular spasms, muscular cramp
  • Hematuria, dark urine, incontinence, priapism, urine retention
  • Blurred vision, diplopia, dilated pupil, oculogyric problems

Hepatic disease, severe cardiovascular/pulmonary disease, bronchial asthma, renal/endocrine disease, open-angle glaucoma

Age >75 yr

History/active psychoses, history of MI or peptic ulcer

Residual atrial, nodal, ventricular arrhythmias

Risk of uncontrollable sexual, gambling or other urges

May be linked to higher melanoma risk in patient with Parkinson disease

May cause NMS if reduced abruptly or discontinued

Risk of syncope

Risk of developing prostate cancer

Diarrhea may occur and be associated entacapone; may cause weight loss, dehydration, and hypokalemia; if severe, may be a sign of drug-induced microscopic colitis

There are no adequate data on developmental risk associated with use of drug in pregnant women

Levodopa has been detected in human milk after administration of carbidopa-levodopa; there are no data on presence of entacapone or carbidopa in human milk, effects of levodopa, carbidopa, or entacapone on breastfed infant, or on milk production; however, inhibition of lactation may occur because levodopa decreases secretion of prolactin; carbidopa and entacapone are excreted in rat milk; in lactating rat, oral administration of radiolabeled entacapone resulted in levels of entacapone and/or metabolites in milk up to 2 to 3 times that in plasma;

Adults

Do not exceed 1 tablet of carbidopa; levodopa; entacapone per dose. Daily limits: 300 mg/day PO carbidopa; 1,200 mg/day PO levodopa; 1,600 mg/day PO of entacapone. The maximum for tablets (50-, 75-, 100- or 150-mg of levodopa) is 8 tablets/day PO. The maximum for tablets with 200-mg of levodopa is 6 tablets/day PO.

Geriatric

Do not exceed 1 tablet of carbidopa; levodopa; entacapone per dose. Daily limits: 300 mg/day PO carbidopa; 1,200 mg/day PO levodopa; 1,600 mg/day PO of entacapone. The maximum for tablets (50-, 75-, 100- or 150-mg of levodopa) is 8 tablets/day PO. The maximum for tablets with 200-mg of levodopa is 6 tablets/day PO.

Adolescents

Safe and effective use has not been established.

Children

Safe and effective use has not been established.

Infants

Not indicated.

Levodopa/carbidopa/entacapone

tablet

  • 50mg/12.5mg/200mg
  • 75mg/18.75mg/200mg
  • 100mg/25mg/200mg
  • 125mg/31.25mg/200mg
  • 150mg/37.5mg/200mg
  • 200mg/50mg/200mg
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