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

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