What is the dosage and treatment regimen for Ropark (Ropinirole) tablets in patients with Parkinson's disease or restless legs syndrome?

Ropark (Ropinirole) Dosing and Treatment Regimen

Critical Update: Ropinirole is NO LONGER Recommended as First-Line Therapy

The American Academy of Sleep Medicine now recommends AGAINST the standard use of ropinirole for restless legs syndrome due to the high risk of augmentation (paradoxical worsening of symptoms with long-term use), and it should only be considered for short-term treatment in patients who prioritize immediate symptom relief over long-term adverse effects. 1

Current Treatment Paradigm

For Restless Legs Syndrome (RLS)

• First-line therapy is now alpha-2-delta ligands (gabapentin, gabapentin enacarbil, or pregabalin), NOT dopamine agonists like ropinirole. 1
• Ropinirole carries a conditional recommendation AGAINST standard use with moderate certainty of evidence. 1
• The shift away from dopamine agonists occurred because augmentation develops commonly with long-term use, causing earlier onset of symptoms during the day, increased symptom intensity, and spread to other body parts. 2, 1

If Ropinirole Must Be Used (Against Current Guidelines)

FDA-Approved Dosing for RLS:

• Start at 0.25 mg once daily, taken 1-3 hours before bedtime. 3
• After 2 days, increase to 0.5 mg once daily if needed. 3
• At end of Week 1, increase to 1 mg once daily. 3
• Continue weekly titration: Week 2 (1 mg), Week 3 (1.5 mg), Week 4 (2 mg), Week 5 (2.5 mg), Week 6 (3 mg), Week 7 (4 mg maximum). 3
• Maximum dose: 4 mg once daily for RLS. 3
• Doses above 4 mg daily have not been established as safe or effective for RLS. 3

Clinical trial data showed mean effective dose of 1.90 mg/day for RLS. 4

For Parkinson's Disease

FDA-Approved Dosing:

• Start at 0.25 mg three times daily (0.75 mg total daily dose). 3
• Week 2: 0.5 mg three times daily (1.5 mg total). 3
• Week 3: 0.75 mg three times daily (2.25 mg total). 3
• Week 4: 1 mg three times daily (3 mg total). 3
• After Week 4, increase by 1.5 mg/day weekly up to 9 mg/day, then by 3 mg/day weekly up to maximum of 24 mg/day (8 mg three times daily). 3
• Maximum dose: 24 mg/day divided three times daily. 3

Special Populations

Renal Impairment

• Moderate impairment (CrCl 30-50 mL/min): No dose adjustment needed. 3
• End-stage renal disease on hemodialysis (RLS): Start 0.25 mg once daily, maximum 3 mg/day. 3
• End-stage renal disease on hemodialysis (Parkinson's): Start 0.25 mg three times daily, maximum 18 mg/day. 3
• Supplemental doses after dialysis are NOT required. 3
• Severe renal impairment without dialysis has not been studied. 3

Discontinuation Protocol

For RLS:

• Gradual reduction of daily dose is recommended to avoid withdrawal symptoms. 3

For Parkinson's Disease:

• Taper over 7 days: reduce from three times daily to twice daily for 4 days, then once daily for 3 days before complete withdrawal. 3

Common Adverse Effects

• Nausea (most common). 4, 5
• Headache. 4
• Dizziness and somnolence (increases fall risk, particularly concerning in older adults). 1
• Orthostatic hypotension. 2
• Compulsive behaviors. 2

Critical Safety Considerations

Augmentation Risk

• Monitor for worsening symptoms, earlier onset during the day, increased intensity, or spread to other body parts. 2, 1
• If augmentation occurs, consider switching to alpha-2-delta ligands or opioids rather than increasing ropinirole dose. 2, 1

Drug Interactions

• Particular consideration needed in older patients for drug interactions and orthostasis risk. 2

Therapeutic Drug Monitoring

• Therapeutic plasma levels: 0.4-6 ng/mL. 6
• A fatal case reported peripheral blood concentration of 64 ng/mL. 6

Administration

• Can be taken with or without food. 3
• For RLS, take 1-3 hours before bedtime. 3

Recommended Alternative Approach (2025 Guidelines)

Before considering any pharmacologic therapy:

1. Check serum ferritin and transferrin saturation (morning, fasting). 1
2. Supplement iron if ferritin ≤75 ng/mL or transferrin saturation <20%. 1
3. Address exacerbating factors: alcohol, caffeine, antihistamines, SSRIs, antipsychotics, untreated sleep apnea. 1

First-line pharmacologic therapy:

• Gabapentin, gabapentin enacarbil, or pregabalin (strong recommendation, moderate certainty). 1

Reserve ropinirole only for patients who:

• Place higher value on short-term symptom reduction. 1
• Place lower value on long-term adverse effects. 1
• Understand and accept augmentation risk. 1