Is four years of daily 4 mg extended‑release ropinirole for restless‑legs syndrome in a 62‑year‑old patient considered too long?

Four Years of Daily 4 mg Ropinirole XR for RLS in a 62-Year-Old Is Too Long

You should transition this patient away from ropinirole to an alpha-2-delta ligand (gabapentin, pregabalin, or gabapentin enacarbil) because the 2025 American Academy of Sleep Medicine guidelines now conditionally recommend against standard use of ropinirole due to a 7–10% annual augmentation risk, and after four years this patient faces a cumulative augmentation risk exceeding 25%. 1

Why Ropinirole Is No Longer Recommended for Long-Term Use

• The 2025 AASM guidelines represent a major paradigm shift: dopamine agonists like ropinirole, previously considered first-line, are now recommended against for standard use (conditional recommendation, moderate certainty of evidence). 1

• Augmentation—a paradoxical worsening of RLS characterized by earlier daily symptom onset (afternoon instead of evening), increased intensity, and spread to arms or trunk—occurs in approximately 7–10% of patients per year on dopamine agonists. 1

• After four years, the cumulative risk of augmentation is substantial, and the 2025 guidelines explicitly state that ropinirole may be considered "only for short-term use" in patients who prioritize immediate relief over long-term safety. 1

• The FDA-approved titration schedule for ropinirole (0.25 mg escalating to 4 mg daily) predates the current evidence demonstrating high augmentation risk; contemporary guidelines now supersede this older labeling. 1

Current First-Line Therapy: Alpha-2-Delta Ligands

• Alpha-2-delta ligands (gabapentin, gabapentin enacarbil, pregabalin) are now strongly recommended as first-line therapy for RLS (strong recommendation, moderate certainty of evidence) because they provide equivalent or superior symptom control without augmentation risk. 1, 2, 3

• Gabapentin dosing: start 300 mg three times daily; increase by 300 mg/day every 3–7 days; target maintenance 1800–2400 mg/day divided TID; maximum studied dose 3600 mg/day. 1, 3

• Pregabalin offers twice-daily dosing and superior bioavailability compared to regular gabapentin, which may improve adherence in a 62-year-old patient. 1, 3

• Gabapentin enacarbil (extended-release prodrug) is also strongly recommended and may provide more consistent 24-hour coverage. 1

Structured Transition Algorithm

Step 1: Assess Iron Status Before Any Medication Change

• Check morning fasting ferritin and transferrin saturation after withholding iron supplements for ≥24 hours. 1, 2, 3

• If ferritin ≤75 ng/mL or transferrin saturation <20%, initiate oral ferrous sulfate 325–650 mg daily or consider IV ferric carboxymaltose 750–1000 mg (strong recommendation, moderate certainty) for rapid correction. 1, 3

• Iron optimization alone may significantly reduce RLS symptoms and facilitate the transition off ropinirole. 1, 3

Step 2: Initiate Alpha-2-Delta Ligand Before Tapering Ropinirole

• Start gabapentin 300 mg TID (or pregabalin 50 mg TID or 75 mg BID) and titrate upward every 3–7 days until reaching therapeutic dose (gabapentin 1800–2400 mg/day; pregabalin up to 600 mg/day). 1, 3

• Do not taper ropinirole until the new medication reaches therapeutic dose and symptom control is achieved—this prevents rebound RLS and insomnia. 1, 2

Step 3: Taper Ropinirole Very Slowly

• Once gabapentin/pregabalin provides adequate control, reduce ropinirole by 0.25–0.5 mg every 1–2 weeks. 1, 2

• Anticipate rebound RLS symptoms during the taper; temporary use of immediate-release ropinirole or low-dose opioid (e.g., tramadol) may serve as bridge therapy but should be discontinued once transition is complete. 1

Step 4: Monitor for Augmentation During Transition

• Watch for earlier symptom onset (afternoon instead of evening), increased intensity, or spread to arms/trunk—these are hallmarks of augmentation. 1, 2

• Do not increase ropinirole dose if symptoms worsen during taper, as this reflects augmentation and will worsen the problem. 1, 2

What If the Patient Has Already Developed Augmentation?

• If augmentation is present (earlier onset, increased intensity, spread to upper extremities), bypass gradual taper and transition directly to an alpha-2-delta ligand or consider a low-dose opioid (extended-release oxycodone 5–10 mg at bedtime) for severe cases. 1

• Opioids are conditionally recommended (moderate certainty) for refractory RLS or augmentation management, with long-term data showing low abuse risk and minimal dose escalation over 2–10 years when patients are appropriately screened. 1

Evidence Supporting This Recommendation

• A 2013 International RLS Study Group guideline established ropinirole as effective for up to 6 months (Level A evidence) and probably effective for 1 year (Level B), but did not support use beyond 1 year due to augmentation concerns. 4

• A 52-week open-label study showed ropinirole was well-tolerated with maintained efficacy, but this predates the 2025 AASM guidelines that now recommend against standard use due to cumulative augmentation risk. 5

• The 2025 AASM guidelines are the highest-quality, most recent evidence and should supersede older research when making clinical decisions about long-term ropinirole use. 1

Critical Pitfalls to Avoid

• Do not continue ropinirole indefinitely simply because the patient is currently stable—augmentation risk accumulates over time and may present suddenly after years of effective treatment. 1

• Do not increase ropinirole dose if symptoms worsen; this likely reflects augmentation and will worsen the condition. 1, 2

• Do not abruptly discontinue ropinirole without first establishing therapeutic levels of an alternative agent, as this causes severe rebound RLS. 1, 2

• Do not use benzodiazepines (e.g., clonazepam) as monotherapy for RLS in a 62-year-old; they provide only sedation without addressing the underlying disorder and increase fall risk and cognitive impairment. 1, 2, 3

Special Considerations for a 62-Year-Old Patient

• Fall risk is a critical concern in older adults; alpha-2-delta ligands have a better safety profile than dopamine agonists regarding orthostatic hypotension and impulse control disorders. 2, 3

• Start with lower doses and titrate slowly to minimize dizziness and somnolence, which are common side effects of gabapentin/pregabalin. 1, 3

• Monitor for drug interactions with other medications commonly used in this age group. 2

• Recheck ferritin every 6–12 months, as brain iron deficiency may persist despite clinical improvement. 1, 3