ropinirole
Brand: Requip, Requip XL
Beers Criteria Prototype: levodopa-carbidopa
Drug Class: dopamine agonist
Drug Family: antiparkinsonian
Subclass: non-ergot D2/D3 dopamine receptor agonist
Organ Systems: cns
Mechanism of Action
Selective agonist at D2 and D3 dopamine receptors in the striatum; pharmacological profile and clinical use very similar to pramipexole, but metabolized by CYP1A2 (vs. pramipexole's renal elimination), creating different drug interaction concerns.
D2 dopamine receptorD3 dopamine receptor
Indications
- Parkinson's disease (early and advanced)
- restless legs syndrome (moderate to severe)
Contraindications
- no absolute contraindications beyond hypersensitivity
Adverse Effects
Common
- nausea
- somnolence
- dizziness
- syncope
- hallucinations
- peripheral edema
Serious
- sudden onset sleep
- impulse control disorders
- hypotension
- psychosis
Pharmacokinetics (ADME)
| Absorption | well absorbed orally; bioavailability ~55%; food has minimal effect on extent |
| Distribution | protein binding ~40%; Vd ~7.5 L/kg |
| Metabolism | primarily CYP1A2; inactive metabolites |
| Excretion | renal (~88% as metabolites) |
| Half-life | 6 hours |
| Onset | weeks for Parkinson's effect |
| Peak | 1-2 hours (IR); 6 hours (XL) |
| Duration | 8 hours (IR); 24 hours (XL) |
| Protein Binding | 40% |
| Vd | 7.5 L/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| CYP1A2 inhibitors (fluvoxamine, ciprofloxacin, estrogens) | increase ropinirole levels significantly | major |
| tobacco smoking (CYP1A2 inducer) | decreases ropinirole levels by ~30-40%; smoking cessation increases levels | moderate |
| dopamine antagonists | pharmacodynamic antagonism | major |
Nursing Considerations
- Same monitoring for impulse control disorders, sudden onset sleep, and orthostatic hypotension as pramipexole.
- Smoking status affects ropinirole levels via CYP1A2 induction; if a patient on ropinirole stops smoking, levels will increase significantly — monitor for increased adverse effects.
- Ciprofloxacin and fluvoxamine (common drugs in hospital settings) are CYP1A2 inhibitors that can increase ropinirole levels 2-3 fold — perform medication reconciliation.
- For RLS, take 1-3 hours before bedtime; dose late in the day to match therapeutic coverage to symptom timing.
Clinical Pearls
- Ropinirole's CYP1A2 dependence creates a clinically important interaction with smoking cessation; patients who stop smoking during ropinirole therapy need monitoring for toxicity as CYP1A2 induction reverses.
- Both pramipexole and ropinirole are equally effective for Parkinson's disease and RLS; the choice between them is largely based on renal function (pramipexole requires renal dose adjustment), drug interactions, and tolerability.
Safety Profile
Pregnancy avoid
Lactation avoid
Renal Adjustment Not required
Hepatic Adjustment Required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.