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NERVOUS SYSTEM › ANTI-PARKINSON DRUGS › DOPAMINERGIC AGENTS › Dopa and dopa derivatives
levodopa, decarboxylase inhibitor and COMT inhibitor
N04BA03
Forms & Strengths
- Carbidopa/Levodopa/Entacapone (Stalevo) tablets: 12.5/50/200 mg, 18.75/75/200 mg, 25/100/200 mg, 31.25/125/200 mg, 37.5/150/200 mg, 50/200/200 mg
Adult Dosing
- Individualized based on previous therapy
- One tablet of chosen strength administered orally with each levodopa dose
- Maximum 8 tablets daily across all available strengths
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Treatment of Parkinson's disease as substitution for equivalent doses of levodopa/carbidopa and entacapone
- Management of patients with end-of-dose motor fluctuations not stabilized by levodopa/carbidopa alone
Mechanism of Action
- Levodopa is the metabolic precursor of dopamine, crossing the blood-brain barrier to be decarboxylated to dopamine in the brain
- Carbidopa is an aromatic L-amino acid decarboxylase inhibitor preventing peripheral conversion of levodopa, increasing central availability
- Entacapone is a reversible and selective inhibitor of catechol-O-methyltransferase (COMT), reducing peripheral metabolism of levodopa
Contraindications
- Concomitant use with non-selective monoamine oxidase (MAO) inhibitors
- History of neuroleptic malignant syndrome and/or non-traumatic rhabdomyolysis
- Narrow-angle glaucoma
- Hypersensitivity to levodopa, carbidopa, or entacapone
Adverse Reactions
- Dyskinesias
- Nausea and diarrhea
- Chromaturia (brownish-orange urine discoloration)
- Orthostatic hypotension
- Somnolence and sudden onset of sleep
- Psychotic episodes and impulse control disorders
Drug Interactions
- Non-selective MAO inhibitors may cause hypertensive crisis
- Dopamine D2 receptor antagonists (e.g., phenothiazines, butyrophenones, risperidone) may reduce therapeutic efficacy
- Iron salts may chelate entacapone and levodopa, reducing their gastrointestinal absorption
- Drugs metabolized by COMT (e.g., isoproterenol, epinephrine) may have potentiated effects
Curated Content: Needs Vetting Before Put to Clinical Use