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ropinirole (Requip, Requip-XL)

Tradename: Requip. Indications: - symptomatic treatment of idiopathic Parkinson's disease - parkinsonism - treatment of restless legs syndrome [7] Contraindications: 1) pregnancy 2) lactation Dosage: 1) week 1: 0.25 mg PO TID 2) week 2: 0.5 mg PO TID 3) week 3: 0.75 mg PO TID 4) week 4: 1.0 mg PO TID 5) increase by 1.5 mg/day weekly up to 9 mg/day 6) increase by 3 mg/day weekly up to a maximum of 24 mg/day 7) decrease L-dopa as tolerated 8) for discontinuation, taper over a 7 day period 9) may be taken with or without food Tabs: 0.25 mg, 0.5 mg, 1 mg, 2 mg, 5 mg. (not scored) Requip-XL, QD dosing Pharmacokinetics: -> metabolized in the liver by cyt P450 1A2 Adverse effects: 1) common (> 10%) - nausea/vomiting, syncope*, dyspepsia, somnolence, dizziness, fatigue, dyskinesia, headache, viral infection 2) less common (1-10%) - hallucinations, confusion, falls, yawning, impaired concentration, amnesia, anxiety, nervousness, anemia, elevated alkaline phosphatase, abdominal pain, anorexia, flatulence, diarrhea, constipation, flushing, asthenia, chest pain, dependent edema, leg edema, malaise, orthostatic hypotension#, paresis, tremor, hyperesthesia, vertigo, impotence, bronchitis, dyspnea, peripheral ischemia, eye abnormality, visual disturbance, diplopia, xerophthalmia, pyuria, urinary tract infection 3) other - sudden sleep attacks have been reported [3] - compulsive behavior - punding * syncope may be associated with bradycardia # orthostatic hypotension may be related to dopaminergic agonist tendency to impair regulation of systemic blood pressure Drug interactions: 1) any drug which inhibits cyt P450 1A2 can increase ropinirole levels 2) any drug which induces cyt P450 1A2 can diminish ropinirole levels 3) ciprofloxacin increases serum ropinirole (60%) 4) estrogens decrease clearance of roprinole (36%) 5) dopamine antagonists are expected to reduce effectiveness a) neuroleptics 1] phenothiazines 2] butyrophenones 3] thiothixenes b) metoclopramide 5) ropinirole may potentiate adverse effects of L-dopa Mechanism of action: 1) dopamine D2 receptor agonist 2) may have neuroprotective effects

Interactions

drug adverse effects (more general classes)

Related

cytochrome p450 1A2 (cytochrome P3-450, phenacetin deethylase, cytochrome p450-4, CYP1A2) Parkinson's disease (paralysis agitans, PD)

General

dopaminergic receptor agonist pharmacologic agents for treatment of Parkinson's disease

Properties

AGONIST-FOR: adrenergic receptor MISC-INFO: pregnancy-category - safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  2. Prescriber's Letter 13(3): 2006 Cytochrome P450 drug interactions Detail-Document#: 220233 (subscription needed) http://www.prescribersletter.com
  3. Prescriber's Letter 9(3):17 2002
  4. Bronstein J, In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 29-Oct 2, 2004
  5. Medical Knowledge Self Assessment Program (MKSAP) 16 American College of Physicians, Philadelphia 2012
  6. Deprecated Reference
  7. Bogan RK, Fry JM, Schmidt MH et al Ropinirole in the treatment of patients with restless legs syndrome: a US-based randomized, double-blind, placebo- controlled clinical trial. Mayo Clin Proc. 2006 Jan;81(1):17-27. PMID: 16438474