roe-PIN-i-role

Therapeutic Classification: antiparkinson agents

Pharmacologic Classification: dopamine agonists

• Parkinson’s disease.
• Restless leg syndrome (immediate-release only).

• Stimulates dopamine receptors in the brain.

• Decreased tremor and rigidity in Parkinson’s disease.
• Decreased leg restlessness.

Absorption: 55% absorbed following oral administration.

Distribution: Widely distributed to tissues.

Metabolism/Excretion: Extensively metabolized by the liver primarily by the CYP1A2 isoenzyme; <10% excreted unchanged in urine.

Half-life: 6 hr.

Contraindicated in:

• Hypersensitivity
• Major psychotic disorder
• Impulsive control/compulsive behaviors.

Use Cautiously in:

• Hepatic impairment (slower titration may be required)
• Severe cardiovascular disease
• OB: Safety not established in pregnancy
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant; may inhibit lactation
• Pedi: Safety and effectiveness not established in children
• Geri: ↑risk of hallucinations in older adults.

CV: orthostatic hypotension, hypertension, peripheral edema, syncope.

Derm: sweating.

EENT: abnormal vision.

GI: constipation, dry mouth, dyspepsia, nausea, vomiting.

Neuro: dizziness, syncope, aggression, agitation, confusion, delirium, delusions, disorientation, drowsiness, dyskinesia, fatigue, hallucinations, headache, impulse control disorders (gambling, sexual, uncontrolled spending, binge/compulsive eating), insomnia, paranoid ideation, psychosis, SLEEP ATTACKS, somnolence, weakness.

Drug-Drug:

• CYP1A2 inhibitors, including ciprofloxacin may ↑ levels and risk of toxicity.
• CYP1A2 inducers, including cigarette smoke may ↓ levels and effectiveness.
• Estrogens may ↑ levels and risk of toxicity.
• Phenothiazines, butyrophenones, thioxanthenes, or metoclopramide may ↓ effectiveness.
• May ↑ effects of levodopa; consider ↓ dose of levodopa.

Parkinson's Disease

• PO (Adults): Immediate-release: 0.25 mg 3 times daily for 1 wk, then 0.5 mg 3 times daily for 1 wk, then 0.75 mg 3 times daily for 1 wk, then 1 mg 3 times daily for 1 wk; then may ↑ by 1.5 mg/day every wk up to 9 mg/day; then may ↑ by up to 3 mg/day every wk up to 24 mg/day; Extended-release: 2 mg once daily for 1–2 wk; may ↑ by 2 mg/day; do not exceed 8 mg/day in patients with advanced Parkinson's disease or 12 mg/day in patients with early Parkinson's disease.

Restless Leg Syndrome

• PO (Adults): Immediate-release: 0.25 mg once daily initially, 1–3 hr before bedtime. After 2 days, ↑ to 0.5 mg once daily and to 1 mg once daily by the end of first wk of dosing, then ↑ by 0.5 mg weekly, up to 4 mg/day as needed/tolerated.

(Generic available)

• Immediate-release tablets: 0.25 mg; 0.5 mg; 1 mg; 2 mg; 3 mg; 4 mg; 5 mg;
• Extended-release tablets: 2 mg; 4 mg; 6 mg; 8 mg; 12 mg;

• Assess BP periodically during therapy.
• Assess patient for drowsiness and sleep attacks. Drowsiness is a common side effect of ropinirole, but sleep attacks or episodes of falling asleep during activities that require active participation may occur without warning. Assess patient for concomitant medications that have sedating effects or may increase serum ropinirole levels (see Interactions). May require discontinuation of therapy.
• Assess patient for signs and symptoms of psychotic-like behavior (confusion, paranoid ideation, delusions, hallucinations, psychotic-like behavior, disorientation, aggressive behavior, agitation, delirium, hallucinations). Risk of symptoms increases with age. Notify health care professional if these occur.
• Parkinson's Disease: Assess patient for signs and symptoms of Parkinson’s disease (tremor, muscle weakness and rigidity, ataxic gait) prior to and during therapy.
• Restless Leg Syndrome: Assess sleep patterns and frequency of restless leg disturbances.
• Monitor for augmentation (earlier onset of symptoms in the evening or afternoon), increase in symptoms, and spread of symptoms to involve other extremities and rebound (new onset of symptoms in the early morning hr). If symptoms occur, consider dose adjustment or discontinuation of therapy.

• May cause ↑ BUN.

• Do not confuse ropinirole with Risperdal or risperidone.
• PO: May be administered with or without food. Administration with food may decrease nausea. DNC: Swallow extended-release tablets whole; do not break, crush, or chew.
• Taper or discontinuation may cause withdrawal symptoms (apathy, anxiety, depression, fatigue, insomnia, sweating, pain); symptoms do not respond to levodopa. Trial readministration of ropinirole at lowest dose may be considered.

• Instruct patient to take medication exactly as directed. Missed doses should be taken as soon as possible, but not if almost time for next dose. Do not double doses. Do not stop abruptly; may cause hyperpyrexia and confusion. Taper doses gradually over 7 days.
• Caution patient to change positions slowly to minimize orthostatic hypotension.
• May cause drowsiness and unexpected episodes of falling asleep. Caution patient to avoid driving or other activities requiring alertness until response to medication is known. Advise patient to notify health care professional if episodes of falling asleep occur.
• Advise patient to avoid alcohol and other CNS depressants concurrently with ropinirole.
• Advise patient that increasing fluids, sugarless gum or candy, ice, or saliva substitutes may help minimize dry mouth. Consult health care professional if dry mouth continues for >2 wk.
• Advise patient to have periodic skin exams to check for lesions that may be melanoma.
• Advise patient to notify health care professional if new or increased gambling, sexual, or other impulse control disorders or psychotic-like behaviors occur.
• Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected, or if breastfeeding. Advise patients that ropinirole could inhibit lactation because ropinirole inhibits prolactin secretion.

• Decreased tremor and rigidity in Parkinson’s disease.
• Decrease in restless legs and improved sleep.

Requip, Requip XL