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Ropinirole
Systematic (IUPAC) name
4-[2-(dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one
Identifiers
CAS number 91374-21-9
ATC code N04BC04
PubChem 5095
DrugBank APRD00302
Chemical data
Formula C 16H24N2O 
Mol. mass 260.375 g/mol
Pharmacokinetic data
Bioavailability 50%[1]
Metabolism hepatic (CYP1A2)[1]
Half life 5-6 hours[1]
Excretion  ?
Therapeutic considerations
Pregnancy cat. C
Legal status Prescription only
Routes Oral
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Ropinirole (Requip, Ropark, Adartrel) is a non-ergoline dopamine agonist. It is manufactured by GlaxoSmithKline (GSK) and Sun Pharmaceutical. It is used in the treatment of Parkinson's disease. Ropinirole is also one of two medications in the United States (U.S.) with an Food and Drug Administration (FDA) approved indication for the treatment of restless legs syndrome (RLS), the other being pramipexole (Mirapex). The discovery of the drug's utility in RLS has been used as a successful example of drug repurposing.[2]

Ropinirole's patent expired in May 2008, and the drug is now available in generic form.[3]

Contents

Dosage

Ropinirole in the Requip form is available in various preparations, ranging from a 0.25 mg tablet to a 5 mg tablet. The primary reason for such is dose titration. This implies that the person taking Requip has to closely interact and communicate with the primary care physician with regard to how much should actually be taken by the patient.

For restless legs syndrome (RLS), the maximum recommended dose is 4 mg per day, taken 1 to 3 hours before bedtime. A 52-week open label study had a mean dosage of 1.90 mg, once daily 1 to 3 hours before bedtime.[4]

For Parkinson's disease (PD), the maximum recommended dose is 24 mg per day, taken in three separate doses spread throughout the day.

Pharmacology

Ropinirole acts as a non-ergoline D2, D3, and D4 dopamine receptor agonist with highest affinity for D3. It has moderate in vitro affinity for the opioid receptors. Ropinirole is weakly active at the 5-HT2, and α2 receptors and is said to have virtually no affinity for the 5-HT1, benzodiazepine, GABA, muscarinic, α1, and β-adrenoreceptors.[5]

Ropinirole is metabolized primarily by cytochrome P450 CYP1A2, and at doses higher than clinical, is also metabolized by CYP3A4. At doses greater than 24 mg, CYP2D6 may be inhibited, although this has only been tested in vitro.[1]

Side Effects

Ropinirole can cause nausea, dizziness, hallucinations, orthostatic hypotension, and sudden sleep attacks during the daytime. Rarer and more unusual side effects specific to D3-preferring agonists such as ropinirole and pramipexole can include hypersexuality and compulsive gambling, even in patients without a prior history of these behaviours.[6]

References

  1. ^ a b c d Tompson, Debra J. et al. (2007). "Steady-State Pharmacokinetic Properties of a 24-Hour Prolonged-Release Formulation of Ropinirole: Results of Two Randomized Studies in Patients with Parkinson’s Disease". Clinical Pharmacokinetics 29: 2654. doi:10.1016/j.clinthera.2007.12.010.  
  2. ^ Lipp, Elizabeth (2008-08-01), "Novel Approaches to Lead Optimization", Genetic Engineering & Biotechnology News, Drug Discovery (Mary Ann Liebert) 28 (14): 20, ISSN 1935-472X, http://www.genengnews.com/articles/chitem.aspx?aid=2550, retrieved 2008-09-28   Note: The opinion that ropinirole's use in RLS was a successful example of drug repurposes was reported as being that of Josef Scheiber, a post-doctoral fellow at the Novartis Institutes for BioMedical Research.
  3. ^ New pharmaceutical products: Ceftriaxon-Rocephin, Granisetron-Kytril, Ipratropium-Albuterol
  4. ^ Garcia-Borreguero D, Grunstein R, Sridhar G, et al. (November 2007). "A 52-week open-label study of the long-term safety of ropinirole in patients with restless legs syndrome". Sleep Med. 8 (7-8): 742–52. doi:10.1016/j.sleep.2006.09.009. PMID 17512789. http://linkinghub.elsevier.com/retrieve/pii/S1389-9457(06)00622-8.  
  5. ^ Eden, R. J. et al. (1991). "Preclinical Pharmacology of Ropinirole (SK&F 101468-A) a Novel Dopamine D 2 Agonist". Pharmacology Biochemistry & Behavior 38: 147–154. doi:10.1016/0091-3057(91)90603-Y.  
  6. ^ Bostwick JM, Hecksel KA, Stevens SR, Bower JH, Ahlskog JE. Frequency of new-onset pathologic compulsive gambling or hypersexuality after drug treatment of idiopathic Parkinson disease. Mayo Clinic Proceedings. 2009 Apr;84(4):310-6. PMID 19339647

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