ropinirole

General Information

Ropinirole (brand Requip) is a non-ergoline dopamine agonist indicated for Parkinson’s disease and moderate-to-severe primary RLS (label).

In RLS, dopamine agonists can improve symptoms but require long-term risk management. A key concern is augmentation, which shapes follow-up plans and influences drug selection frameworks (guideline/clinical).

Clinically important adverse effects include somnolence/sudden sleep onset, orthostatic hypotension, hallucinations/psychosis, and impulse-control symptoms; these risks can be especially relevant in serious mental illness (label/clinical).

Ropinirole is metabolized primarily by CYP1A2, so interaction review includes CYP1A2 inhibitors/inducers and smoking status (label/clinical).

The ropinirole compare view, evidence feed, and print page support side-by-side review of RLS options and monitoring topics.

In RLS, ropinirole can be effective but is usually paired with explicit monitoring for augmentation and neuropsychiatric adverse effects. In patients with mood or psychotic disorders, dopaminergic activation risks can be clinically limiting and may shift preference toward non-dopaminergic strategies (guideline/clinical).

Mechanism of Action

Refer to the Glossary entry on Neurotransmitters for background on receptor systems involved in serious mental illness.

Dopamine agonist activity with relative D2/D3 receptor affinity (label/class).

Dopaminergic therapies can precipitate or worsen hallucinations, impulsivity, and mood destabilization in vulnerable patients, which is relevant in serious mental illness (label/clinical).

• Dopamine receptor agonism (D2/D3; class-level).

Metabolism and Pharmacokinetics

• Elimination half-life is approximately 6 hours (label).
• Metabolism is primarily via CYP1A2; inhibitors can increase exposure and smoking can increase clearance via CYP1A2 induction (label).
• Less than 10% of dose is excreted unchanged in urine; metabolites are excreted in urine (label).

Dosing and Administration

• RLS: start 0.25 mg once daily 1 to 3 hours before bedtime; titrate based on response/tolerability up to a maximum recommended dose of 4 mg once daily (label).
• Parkinson’s disease uses different titration schedules and higher total daily doses than RLS; indication-specific dosing is important (label).
• Abrupt discontinuation can be associated with withdrawal/emergent symptoms; tapering is often used when stopping dopaminergic therapy (label/clinical).

Monitoring & Labs

• Somnolence and sudden sleep onset monitoring; driving safety review (label).
• Orthostatic blood pressure and dizziness/falls risk monitoring (label/clinical).
• Hallucinations/psychosis and mood destabilization monitoring, especially in serious mental illness (label/clinical).
• Impulse-control symptom monitoring (new compulsive behaviors) (label/clinical).
• RLS symptom timing tracking to detect augmentation (earlier onset, increased severity, spread) (guideline/clinical).
• CYP1A2 interaction review, including smoking status changes (label/clinical).

Adverse Effects

Interactions

• CYP1A2 inhibitors (e.g., ciprofloxacin, fluvoxamine) can increase exposure; monitoring for increased adverse effects is commonly considered when these are started or stopped (label).
• CYP1A2 induction (including cigarette smoking) can reduce exposure and may reduce efficacy; follow-up is often needed when smoking status changes (label/clinical).
• Additive sedation can occur with alcohol and other CNS depressants (label/clinical).

Other Useful Information

• RLS care frameworks emphasize screening for contributors (iron deficiency, sleep apnea, medication triggers) and tracking symptom timing to detect augmentation early (guideline/clinical).
• AASM guidance and updated algorithms support use of non-dopaminergic options when augmentation risk or psychiatric vulnerability is high (guideline).
• When ropinirole is used for chronic persistent RLS, dose strategies often aim to minimize augmentation: keep doses low, avoid rapid escalation, and reassess iron status and triggers before increasing. If augmentation develops, clinicians often shift to an alpha-2-delta ligand or another strategy rather than simply increasing the dopamine agonist (guideline/clinical).

References

1. Ropinirole tablets prescribing information — DailyMed (2025)
2. Treatment of restless legs syndrome and periodic limb movement disorder: an American Academy of Sleep Medicine clinical practice guideline — Journal of Clinical Sleep Medicine (2025)
3. The Management of Restless Legs Syndrome: An Updated Algorithm — Mayo Clinic Proceedings (2021)
4. Randomized, Double Blind, Placebo Controlled, Short Term Trial OF Ropinirole IN Restless Legs Syndrome — Sleep Medicine (2005)