Entacapone

FDA label

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Renal Undefined

Hepatic Caution — entacapone AUC and Cmax approximately doubled in documented liver disease

Limited clinical experience with daily doses above 1,600 mg.

Instructions

• Always administer with levodopa/carbidopa — entacapone has no antiparkinsonian effect of its own
• May take with or without food
• Can be combined with immediate- or sustained-release levodopa/carbidopa
• Levodopa dose reduction (average ~25%) often needed, especially if levodopa >=800 mg/day or preexisting moderate-severe dyskinesia
• Withdraw slowly — rapid withdrawal may cause re-emergence of PD signs and an NMS-like syndrome (hyperpyrexia, confusion); adjust other dopaminergic therapy on discontinuation

Cautions

• Ordinarily do not combine with non-selective MAOIs (phenelzine, tranylcypromine) — both catecholamine pathways inhibited; selective MAO-B inhibitors (selegiline) may be used
• Caution with COMT-metabolized drugs (epinephrine, isoproterenol, norepinephrine, dopamine, dobutamine, methyldopa, apomorphine) — increased heart rate, arrhythmias, blood-pressure changes
• Falling asleep during activities of daily living / somnolence — caution driving
• Hypotension, orthostatic hypotension, syncope
• Hallucinations and psychotic-like behavior; avoid in major psychotic disorder
• Impulse-control and compulsive behaviors (gambling, sexual, spending urges)
• Diarrhea — may signal drug-induced microscopic (lymphocytic) colitis; discontinue if prolonged
• May cause or exacerbate dyskinesia (may persist despite levodopa reduction)
• Rhabdomyolysis reported; hyperpyrexia/confusion (NMS-like) with rapid withdrawal

Adverse reactions

• Dyskinesia (25%), hyperkinesia (10%)
• Nausea (14%), diarrhea (10%), abdominal pain (8%), vomiting (4%), dry mouth (3%)
• Urine discoloration (10%)
• Dizziness (8%), somnolence, anxiety
• Postmarketing: hepatitis with mainly cholestatic features

Pregnancy Category C — fetal variations and eye anomalies in animal studies; use only if potential benefit justifies fetal risk.

Lactation Excreted in rat milk; unknown in humans — use caution.