Names and pronunciation
(lee-voe-doe′pa-kar-bi-doe′pa- en-ta′ka-pone) Stalevo
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Drug reference
(lee-voe-doe′pa-kar-bi-doe′pa- en-ta′ka-pone) Stalevo
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Func. class.: Antiparkinson agent
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Chem. class.: COMT inhibitor/decar- boxylase inhibitor/dopamine precursor
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ACTION Levodopa: The precursor of dopamine, a chemical depleted in Parkinson dis- ease. Levodopa is able to circulate in the plasma and cross the blood–brain bar- rier, converted by striatal enzymes to dopamine Carbidopa: Inhibits the peripheral plasma breakdown of levodopa by inhib- L iting its decarboxylation; increases avail- able levodopa at the blood–brain barrier Entacapone: A reversible and selective inhibitor of catechol-O-methyltransfer- ase (COMT). Alters the pharmacokinet- ics of levodopa, resulting in more sus- tained levodopa serum levels and increased concentrations available for absorption across the blood–brain barrier
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USES: Parkinson disease
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CONTRAINDICATIONS: Hyper- sensitivity, malignant melanoma, history of malignant melanoma or undiagnosed skin lesions resembling melanoma Precautions: Pregnancy, breastfeeding, diabetes, closed-angle glaucoma, respi- ratory/cardiac/renal/hepatic disease, MI with dysrhythmias, seizures, peptic ulcer, depression
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SIDE EFFECTS CNS: Involuntary choreiform movements, hand tremors, fatigue, headache, anxiety, twitching, numbness, weakness, confu- sion, agitation, insomnia, nightmares, psy- chosis, hallucination, hypomania, severe depression, dizziness, impulsive behav- iors, neuroleptic malignant syndrome, sui cidal ideation CV: Orthostatic hypotension, tachycar- dia, hypertension, palpitation, MI EENT: Blurred vision, diplopia, dilated pupils GI: Nausea, vomiting, anorexia, abdomi- nal distress, dry mouth, flatulence, dys- phagia, bitter taste, diarrhea, constipa- tion, GI bleeding HEMA: Hemolytic anemia, leukopenia, agranulocytosis, thrombocytopenia INTEG: Rash, sweating, alopecia MISC: Urinary retention, incontinence, weight change, dark urine, increased libido, hypersensitivity, dark sweat
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DOSAGE AND ROUTES Adult: PO max daily dose: 8 tablets of Stalevo 50, 75, 100, 125, or 150, or 6 tablets of Stalevo 200, those receiving <70 to 100 mg of the carbidopa compo- nent may experience nausea and vomit- ing; those previously treated with carbidopa/levodopa immediate- release tablets (ratio of 1:4): with current entacapone therapy: May switch directly to corresponding strength of combination tablet; without entaca- pone therapy: If current levodopa dose is >600 mg daily or history of moderate or severe dyskinesias: levodopa dose reduction may be required when adding entacapone to therapy; titrate dose using individual products, first carbidopa/ levodopa immediate release with a ratio of 1:4 plus entacapone 200 mg; then transfer to combination product once stabilized; if current levodopa dose is <600 mg and without a history of dyski- nesias: May transfer to corresponding dose of combination product
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Available forms: Tablets 50, 75, 100, 125, 150, 200 mg
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Administer: • Administer whole; do not cut, break, or crush • Avoid giving with a high-fat meal
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Assess: • Parkinson symptoms: tremors, pill rolling, drooling, akinesia, rigidity; shuf- fling gait before, during treatment • B/P, respiration; orthostatic B/P • Mental status: affect, mood, behav- ioral changes, depression, complete sui- cide assessment • Toxicity: muscle twitching, blepharo spasm • Renal, hepatic, hematopoietic tests; also for diabetes, acromegaly if on long- term therapy • End-of-dose akinesia; on/off phenom enon, akinesia paradoxica • Pregnancy/breastfeeding: use only if benefits outweigh fetal risk; product is excreted in breast milk
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Evaluate: • Therapeutic response: decrease in akathisia/bradykinesis, tremor, rigidity, improved mood
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Patient and caregiver information: • To change positions slowly to prevent orthostatic hypotension, especially dur- ing beginning of treatment • To report side effects: twitching, eye spasms because these indicate overdose • That falling asleep when engaged in activities may occur • To use product as prescribed; not to double doses; if discontinued abruptly, parkinsonian crisis, neuroleptic malignant syndrome (NMS) may occur; to gradually taper • That urine, sweat may darken • To use physical activities to maintain mobility, lessen spasms • To use with meals to decrease GI up- set; do not use high-protein meals, dis- tribute protein throughout the day
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PHARMACOKINETICS PO: Onset unknown, peak 1-3 hr, dura- tion unknown Interactions Increase: hypertensive crisis—nonselec- tive MAOIs Increase: risk for sedation—CNS depressants Increase: hypotension—antihypertensives Increase: CV reactions—dobutamine, dopamine, epinephrine, isoproterenol, norepinephrine, TCAs Increase: effects of levodopa—antacids, metoclopramide Decrease: effects of levodopa—anticho- linergics, hydantoins, papaverine, pyri- doxine, benzodiazepines, antipsychotics Drug/Lab Test Increase: BUN, AST, ALT, bilirubin, alk phos, LDH, serum glucose Decrease: BUN, creatinine, uric acid False positive: urine ketones (dip- stick), Coombs’ test False negative: urine glucose False increase: urine protein Drug/Food Decrease: absorption of levodopa—protein NURSING CONSIDERATIONS
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