Levodopa
in SINEMET
What it isDopamine precursor, given with carbidopa to block peripheral decarboxylation; Parkinson disease.
Why this oneThe most effective symptomatic treatment in Parkinson disease, and nothing else comes close.
What limits itMotor fluctuations and dyskinesia accumulate with duration of therapy. Protein competes for absorption; never stop abruptly.
FDA-approved for
- Parkinson disease (1970)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Parkinson's disease — intermittent OFF episodes (adjunct to carbidopa/levodopa) | Adults | 84 mg (two 42 mg capsules) PRN per OFF period | 84 mg PRN per OFF period, up to 5x/day | 84 mg per OFF period; 420 mg/day |
Renal Undefined
Hepatic Undefined
Max 84 mg per OFF period; max 420 mg/day (up to 5 uses/day).
Instructions
- Oral inhalation only using the INBRIJA inhaler; do NOT swallow capsules.
- Use only in combination with oral carbidopa/levodopa.
- Avoid sudden discontinuation or rapid dose reduction (withdrawal-emergent hyperpyrexia/confusion).
- Store capsules in blister until immediately before use.
Contraindications
- MAOIs (concurrently or within 14 days)
- Current or recent (within 2 weeks) use of a nonselective MAO inhibitor (e.g., phenelzine, tranylcypromine) — risk of hypertension
Cautions
- Falling asleep during activities of daily living / somnolence
- Withdrawal-emergent hyperpyrexia and confusion with rapid dose reduction
- Hallucinations/psychosis — avoid in major psychotic disorder
- Impulse control/compulsive behaviors
- May cause or exacerbate dyskinesia
- Bronchospasm — not recommended in asthma/COPD/chronic lung disease
- May increase intraocular pressure in glaucoma
Adverse reactions
- Cough, discolored sputum
- Nausea, vomiting
- Upper respiratory tract infection
Pregnancy No adequate human data; carbidopa/levodopa developmentally toxic/teratogenic in animals.
Lactation Levodopa detected in human milk; may interfere with lactation (prolactin-lowering).
NO BOXED WARNINGS
Principal riskDyskinesia and motor fluctuation with cumulative exposure
Cost, est. cash$300–$5,000/month
Generic entry2032 est.
Classes and tags
Clinical profile
Legacy pregnancy categoryUnknown / historical label unavailable
Defining liabilityOrthostasis, hallucinations, dyskinesia and impulse-control symptoms; abrupt withdrawal can be hazardous.
Active metabolites
Mechanism of action: Levodopa ballicule
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Memory aids: mascots and interaction avatars
