Section 03 · Monograph

Ropinirole

Reviewed Nov 2026FDA label

RequipDopamine agonist

Indications

Treatment of the signs and symptoms of idiopathic Parkinson's diseaseFDA-labeled

Ropinirole is a non-ergoline dopamine agonist with high relative in vitro specificity for the D2 and D3 dopamine receptor subtypes, binding with higher affinity to D3 than D2 or D4 receptors
Stimulates dopamine receptors within the caudate-putamen in the brain, though the precise mechanism of antiparkinsonian action is not fully established
Extensively metabolized by CYP1A2; eliminated with a terminal half-life of approximately 6 hours; <10% excreted unchanged in urine

Immediate-release: start 0.25 mg three times daily
Titration (Weeks 1–4): Week 1 — 0.25 mg TID (0.75 mg/day); Week 2 — 0.5 mg TID (1.5 mg/day); Week 3 — 0.75 mg TID (2.25 mg/day); Week 4 — 1 mg TID (3 mg/day)
After Week 4, may increase by up to 1.5 mg/day at weekly intervals up to 9 mg/day, then by up to 3 mg/day weekly thereafter as needed/tolerated
Maximum dose: 24 mg/day (8 mg three times daily)
Hemodialysis/ESRD: do not exceed 18 mg/day
Discontinuation: taper gradually — reduce frequency from three times daily to twice daily for 4 days, then once daily for 3 days before stopping

Known hypersensitivity/allergic reaction (e.g., urticaria, angioedema, rash, pruritus) to ropinirole or its components

CYP1A2 inhibitors (e.g., ciprofloxacin): increase ropinirole AUC by ~84% and Cmax by ~60%; dose adjustment may be needed
Smoking (CYP1A2 induction): reduces ropinirole exposure by approximately 30–38%; dose adjustment may be needed with changes in smoking status
Estrogens (e.g., hormone replacement therapy): can reduce ropinirole clearance by up to ~36%; reassess dose when starting or stopping estrogen therapy
Dopamine antagonists (neuroleptics, metoclopramide): may reduce ropinirole efficacy

Impulse control/compulsive behaviors: intense urges to gamble, increased sexual urges, urges to spend money, binge/compulsive eating
Sudden onset of sleep during activities of daily living, including driving, sometimes without warning signs; somnolence reported in up to 40% of early PD patients vs 6% placebo
Orthostatic hypotension and syncope — syncope occurred in 12% of early PD patients vs 1% placebo, often associated with bradycardia and more common after dose increases
Hallucinations/psychotic-like behavior — early PD 5.2% vs 1.4% placebo; advanced PD 10.1% vs 4.2% placebo; elderly (>65) at increased risk (~10% vs 2%)
Dyskinesia — 34% of advanced PD patients on ropinirole plus levodopa vs 13% placebo
Nausea, dizziness, asthenia, leg edema, vomiting, dyspepsia
Withdrawal symptoms with discontinuation: insomnia, apathy, anxiety, depression, fatigue, sweating, pain — generally unresponsive to levodopa

Direct questioning about drowsiness and sudden sleep episodes before driving or operating machinery
Blood pressure monitoring, particularly during dose titration, for orthostatic hypotension and syncope risk
Cardiovascular assessment in patients with underlying heart disease given syncope/bradycardia risk
Screen for hallucinations and psychotic symptoms, especially in elderly patients
Regular, direct screening for impulse control/compulsive behaviors in patient and caregiver
Monitor for dyskinesia, especially when combined with levodopa
Monitor for withdrawal symptoms during dose reduction or discontinuation
Renal function assessment in patients with impairment (dose cap with hemodialysis)

No adequate human pregnancy data; teratogenic and embryolethal effects (digit, cardiovascular, neural tube defects) observed in rats at high, clinically irrelevant multiples of the human dose — use only if benefit justifies potential risk
No human milk data; ropinirole inhibits prolactin secretion and suppresses lactation; drug/metabolites present in rat milk — breastfeeding not recommended during treatment