Trade Names:Stalevo 50- Tablets carbidopa 12.5 mg/levodopa 50 mg/entacapone 200 mg
Trade Names:Stalevo 75- Tablets carbidopa 18.75 mg/levodopa 75 mg/entacapone 200 mg
Trade Names:Stalevo 100- Tablets carbidopa 25 mg/levodopa 100 mg/entacapone 200 mg
Trade Names:Stalevo 125- Tablets carbidopa 31.25 mg/levodopa 125 mg/entacapone 200 mg
Trade Names:Stalevo 150- Tablets carbidopa 37.5 mg/levodopa 150 mg/entacapone 200 mg
Trade Names:Stalevo 200- Tablets carbidopa 50 mg/levodopa 200 mg/entacapone 200 mg
Inhibits peripheral decarboxylation of levodopa, making more levodopa available for transport to the brain.Levodopa
Precursor of dopamine, which is deficient in parkinsonism patients.Entacapone
Inhibits the enzyme that metabolizes levodopa (catechol-O-methyltransferase [COMT]), which increases and prolongs levodopa plasma levels.
Treatment of idiopathic Parkinson disease to substitute (with equivalent strength of each of the 3 immediate-release components) for the previously administered individual products, or to replace immediate-release carbidopa/levodopa therapy (without entacapone) when patients experience signs and symptoms of end-of-dose “wearing-off” (only for patients taking a total daily dose of levodopa 600 mg or less and not experiencing dyskinesias).
Narrow-angle glaucoma; patients with history of melanoma or suspicious, undiagnosed skin lesions; hypersensitivity to any component of the product; discontinued nonselective monoamine oxidase inhibitors (MAOIs) (eg, phenelzine) at least 2 wk prior to initiating therapy with carbidopa/levodopa/entacapone.
PO 1 tablet should be administered at each dosing interval. The product is available in 6 strengths, each in a 1:4 ratio of carbidopa to levodopa and combined with entacapone 200 mg. Generally, the product should be used to substitute for patients already stabilized on equivalent doses of carbidopa/levodopa and entacapone. However, some patients stabilized on a given dose of carbidopa/levodopa may be treated with this product if a decision to add entacapone has been made. The optimum daily dosage must be determined by careful titration in each patient. Therapy should be individualized and adjusted according to the desired therapeutic response.Transferring Patients to Carbidopa/Levodopa/EntacaponeAdults
PO There is no experience in transferring patients currently treated with standard formulations of carbidopa/levodopa other than immediate-release carbidopa/levodopa with a 1:4 ratio and entacapone to carbidopa/levodopa/entacapone. Patients who are taking entacapone 200 mg with each dose of standard-release carbidopa/levodopa can be directly switched to the corresponding strength of Stalevo containing the same amounts of levodopa and carbidopa.Transferring Patients Not Currently Taking EntacaponeAdults
PO Patients should be titrated individually with a carbidopa/levodopa product (ratio 1:4) and an entacapone product. Then, once the patient has stabilized, transfer patient to a corresponding dose of carbidopa/levodopa/entacapone. Since entacapone prolongs and enhances the effects of levodopa, therapy should be individualized and adjusted, if necessary, according to the desired therapeutic response.
Store at controlled room temperature (59° to 86°F).
Symptomatic postural hypotension may occur when adding carbidopa/levodopa; therefore, be prepared to adjust antihypertensive therapy as needed.Dopamine D2 receptor antagonists (eg, butyrophenones, isoniazid, phenothiazines, risperidone), papaverine, phenytoin
May reduce the therapeutic effects of levodopa.Drugs known to interfere with biliary excretion, glucuronidation, and intestinal beta-glucuronidase (eg, ampicillin, chloramphenicol, cholestyramine, erythromycin, probenecid, rifampin)
Because entacapone is excreted via the bile, use drugs known to interfere with biliary excretion, glucuronidation, and intestinal beta-glucuronidase with caution.Drugs metabolized by COMT (eg, alpha-methyldopa, apomorphine, bitolterol, dobutamine, dopamine, epinephrine, isoproterenol, isotharine)
Increased heart rate, possible arrhythmia, and excessive BP changes may occur.Iron salts
May reduce the bioavailability of levodopa; however, the clinical importance is unclear.MAOIs
Concurrent therapy with nonselective MAOIs (eg, phenelzine) is contraindicated. Discontinue therapy with MAOIs 2 wk prior to starting carbidopa/levodopa/entacapone.Metoclopramide
May increase levodopa bioavailability by increasing gastric emptying and because of its dopamine receptor antagonistic properties; metoclopramide may also adversely affect disease control.Pyridoxine
Pyridoxine in doses of 10 to 25 mg may reverse the effects of levodopa; however, carbidopa inhibits this effect of levodopa. Therefore, supplemental pyridoxine can be given concurrently.Tricyclic antidepressants (TCAs) (eg, amitriptyline)
Rare reports of adverse reactions, including hypertension and dyskinesia, have been noted with concomitant use of levodopa/carbidopa and TCAs.
False-positive reactions for urinary ketone bodies may occur when a test tape is used for ketonuria determination; false-positive Coombs test results may occur; because falsely diagnosed pheochromocytoma has occurred, exercise caution when interpreting plasma and urine levels of catecholamines and their metabolites.
Cardiac irregularities, hypertension, hypotension, orthostatic hypotension, palpitation, phlebitis, syncope.Levodopa
Abnormal dreams (including nightmares), agitation, asthenia, bradykinetic episodes (“on-off” phenomenon), confusion, convulsions, dementia, depression with and without suicidal tendencies, dizziness, dyskinesia, hallucinations, headache, increased libido, insomnia, NMS, paranoid ideation, paresthesia, psychotic episodes (including delusions), somnolence.Entacapone
Dyskinesia (25%); hyperkinesia (10%); hypokinesia (9%); dizziness (8%); fatigue (6%); anxiety, asthenia, somnolence (2%); agitation (1%).Levodopa
Abnormal gait, activation of latent Horner syndrome, anxiety, ataxia, blepharospasm, decreased mental acuity, disorientation, euphoria, extrapyramidal disorder, falling, fatigue, increased tremor, malaise, memory impairment, muscle twitching, nervousness, numbness, peripheral neuropathy, sense of stimulation, trismus.
Alopecia, dark-colored sweat, increased sweating, rash.Entacapone
Increased sweating (2%).Levodopa
Flushing, malignant melanoma.
Blurred vision, dilated pupils, diplopia, oculogyric crisis.
Anorexia, constipation, dark saliva, diarrhea, dry mouth, duodenal ulcer, dyspepsia, GI bleeding, nausea, taste alterations, vomiting.Entacapone
Nausea (14%); diarrhea (10%); abdominal pain (8%); constipation (6%); vomiting (4%); dry mouth (3%); dyspepsia, flatulence (2%); gastritis, GI disorders, taste perversion (1%).Levodopa
Abdominal pain and distress, burning sensation of the tongue, clenching/grinding of teeth, dysphagia, flatulence, GI pain, heartburn, hiccups, sialorrhea.
Dark urine, urinary frequency, UTI.Entacapone
Urinary discoloration (10%).Levodopa
Priapism, urinary incontinence, urinary retention.
Agranulocytosis, hemolytic anemia, leukopenia, nonhemolytic anemia, thrombocytopenia.Entacapone
Angioedema, bullous lesions (including pemphigus-like reactions), Henoch-Schönlein purpura, pruritus, urticaria.
Abnormalities in alkaline phosphatase ALT, AST, bilirubin, BUN, Coombs test, and lactic dehydrogenase; decreased hemoglobin and hematocrit; elevated serum glucose; bacteria, blood, and white blood cells in the urine.Levodopa
Decreased serum potassium and WBC; increased protein, serum creatinine, uric acid, and urine glucose.
Edema, weight gain, weight loss.
Back pain, muscle cramps, shoulder pain.Entacapone
Back pain (4%).
Dyspnea; upper respiratory tract infection.Entacapone
Cough, pharyngeal pain.
Bacterial infection (1%).Levodopa
Bizarre breathing patterns, faintness, hoarseness, hot flashes.
Assess parkinsonian symptoms before and periodically during therapy.Routine tests
Ensure that liver, CV, hematopoietic, and renal function are assessed before and periodically during therapy.Neurological status
Assess neurological status before and during treatment. Observe for involuntary body and facial movements, depression, hallucinations, or dizziness.
Category C .
Safety and efficacy not established.
Use with caution; AUC and C max of entacapone approximately doubled.
Use with caution in patients with severe CV or pulmonary disease; bronchial asthma; biliary obstruction; renal, hepatic, or endocrine disease; administer cautiously to patients with history of MI who have residual atrial, nodal, or ventricular arrhythmias and to patients with wide-angle glaucoma.
If general anesthesia is required, carbidopa/levodopa/entacapone may be continued as long as the patient is permitted to take fluids and medication by mouth. If therapy is interrupted, observe the patient for symptoms of NMS. Resume therapy at the usual dose as soon as the patient is able to take oral medication.
May be an early sign of excessive dosage, which may indicate the need for dosage reduction.
Diarrhea has been reported and may occur as early as the first week or many months after starting entacapone treatment.
Entacapone may potentiate the dopaminergic side effects of levodopa, exacerbating preexisting dyskinesia; dosage reduction may be required.
Cases of retroperitoneal fibrosis, pulmonary infiltrates, pleural effusion, and pleural thickening have been reported.
Dopaminergic therapy has been associated with hallucinations.
Prolactin secretion may be decreased, while growth hormone levels may be increased.
Elevated temperature, muscular rigidity, altered consciousness, and elevated CPK have been reported with rapid dose reduction or withdrawal of other dopaminergic drugs.
Observe carefully for the development of depression with concomitant suicidal tendencies, or with past or current psychosis.
A symptom complex resembling NMS has been reported in association with dose reductions or withdrawal of carbidopa/levodopa therapy.
The risk of upper GI hemorrhage may be increased.
Severe cases have been reported in patients receiving entacapone in combination with levodopa.
Syncope has been reported and may be frequent in patients with a history of hypotension.
CNS disturbances, COMT inhibition, CV disturbances (eg, hypotension, tachycardia), dopaminergic overstimulation, rhabdomyolysis, severe psychiatric problems, transient renal insufficiency.
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