ROPINIROLE HYDROCHLORIDE
(ro-pi'ni-role)
Requip
Classifications: autonomic nervous system agent; anticholinergic (parasympathomimetic); antiparkinsonism agent
Prototype: Levodopa
Pregnancy Category: C
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0.25 mg, 0.5 mg, 1 mg, 2 mg, 5 mg tablets
Nonergot dopamine receptor agonist structurally similar to pramipexole, 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. The precise mechanism of action is not known.
Indicated by improvement in Parkinson's disease.
Idiopathic Parkinson's disease, restless legs syndrome.
Hypersensitivity to ropinirole or pramipexole; lactation, pregnancy (category C).
Renal and hepatic impairment; concomitant use of CNS depressants. Safety and efficacy in children are not established.
Parkinson's Disease
Adult: PO Start with 0.25 mg t.i.d., may 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 q wk 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 week, then increase by .05 mg qwk
to a maximum of 4 mg
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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.
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Note: Lower initial and maintenance doses with moderate-to-severe renal impairment.
- Store at 15°–30° C (59°–86° F).
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.
Drug: Ropinirole levels may be increased by estrogens, quinolone antibiotics, cimetidine,
diltiazem,
erythromycin,
fluvoxamine,
mexiletine,
tacrine; effects may be antagonized by phenothiazines, butyrophenones, metoclopramide.
Absorption: Rapidly absorbed from GI tract; 55% bioavailability. Peak: 1–2 h. Distribution: 30–40% protein bound. Metabolism: Metabolized in the liver by CYP1A2. Elimination: Primarily excreted in urine. Half-Life: 6 h.
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.
- Do not breast feed while taking this drug.
1%)
Canadian drug name; 
Prototype drug