ROPINIROLE HYDROCHLORIDE
| ROPINIROLE HYDROCHLORIDE (ro-pi'ni-role) Requip Classifications: dopamine receptor agonist; antiparkinson agent; Therapeutic: antiparkinson agent Prototype: Levodopa Pregnancy Category: C |
Availability
0.25 mg, 0.5 mg, 1 mg, 2 mg, 5 mg tablets
Action
Nonergot dopamine receptor agonist used for treatment of Parkinson's disease. It has high affinity for the D2 subfamily of dopamine receptors and higher binding affinity to D3 than to D2 or D4 receptor subtypes, but its precise mechanism is unknown.
Therapeutic Effect
Indicated by improvement in idiopathic Parkinson's disease.
Uses
Idiopathic Parkinson's disease, restless legs syndrome.
Contraindications
Hypersensitivity to ropinirole or pramipexole; lactation, pregnancy (category C).
Cautious Use
Hepatic impairment; severe renal impairment; mental instability; concomitant use of CNS depressants. Safety and efficacy in children are not established.
Route & Dosage
| Parkinson's Disease Adult: PO Start with 0.25 mg t.i.d., titrate up by 0.25 mg/dose t.i.d. qwk to a target dose of 1 mg t.i.d.; if response is still not satisfactory, may continue to increase by 1.5 mg/d qwk to a dose of 9 mg/d, and then by ≤3 mg/d weekly (max: dose of 24 mg/d) Restless Legs Syndrome Adult: PO Take 0.25 mg 1–3 h before bed x 2 d, increase to 0.5 mg for the first wk, then increase by 0.5 mg qwk to a maximum of 4 mg. |
Administration
Oral- Give with food to reduce occurrence of nausea.
- Titrate dose as needed at weekly intervals (see ROUTE & DOSAGE).
- Discontinue drug gradually over 7 d by decreasing from t.i.d. to b.i.d. dosing for 4 d, and then to q.d. dosing for 3 d.
- Note: Lower initial and maintenance doses with moderate to severe renal impairment.
- Store at 15°–30° C (59°–86° F).
Adverse Effects (≥1%)
Body as a Whole: Increased sweating, dry mouth, flushing, asthenia, fatigue, pain, edema, malaise, viral infection, UTI, impotence. CNS: Dizziness, somnolence, sudden sleep attacks, hallucinations, confusion, amnesia, hypesthesia, yawning, hyperkinesia, impaired concentration, vertigo, hallucinations. CV: Syncope, chest pain, orthostatic symptoms, hypertension, palpitations, atrial fibrillation, extrasystoles, hypotension, tachycardia, peripheral edema, peripheral ischemia. GI: Nausea, vomiting, dyspepsia, abdominal pain, anorexia, flatulence. Respiratory: Pharyngitis, rhinitis, sinusitis, bronchitis, dyspnea. Special Senses: Abnormal vision, xerophthalmia, eye abnormality.Interactions
Drug: Ropinirole levels may be increased by estrogens, quinolone antibiotics, cimetidine, diltiazem, erythromycin, fluvoxamine, mexiletine, tacrine; effects may be antagonized by phenothiazines, butyrophenones, metoclopramide.Pharmacokinetics
Absorption: Rapidly from GI tract; 55% bioavailability. Peak: 1–2 h. Distribution: 30–40% protein bound. Metabolism: In liver (CYP1A2). Elimination: Primarily in urine. Half-Life: 6 h.Nursing Implications
Assessment & Drug Effects
- Lab test: Periodically monitor BUN and creatinine, hepatic function.
- Schedule periodic eye exams and chest x-rays during long-term use.
- Monitor carefully for orthostatic hypotension, especially during dose escalation.
Patient & Family Education
- Be aware that hallucinations are a possible adverse effect and occur more often in older adults.
- Make position changes slowly, especially after long periods of lying or sitting. Postural hypotension is common, especially during early treatment.
- Exercise caution with hazardous activities requiring alertness since drowsiness and sedation are common adverse effects. Effects are additive with alcohol or other CNS depressants.
- Immediately notify physician if you become pregnant.
Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; 
Canadian drug name; 
Prototype drug