Ropinirole

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Ropinirole
Systematic (IUPAC) name
4-(2-dipropylaminoethyl)-1,3-dihydroindol-2-one
Identifiers
CAS number 91374-21-9
ATC code N04BC04
PubChem 5095
DrugBank APRD00302
Chemical data
Formula C16H24N2O 
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

Ropinirole (marketed under the brand names Requip and Ropark, in extended release form as Requip XL) is a non-ergoline dopamine agonist. It is manufactured by GlaxoSmithKline and Sun Pharmaceuticals. It is used in the treatment of Parkinson's disease. Ropinirole and is also one of two medications in the United States with an FDA-approved indication for the treatment of restless legs syndrome (RLS), the other being pramipexole. 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

Dosing

Requip (it is marketed as Adartrel in Europe for the restless legs syndrome indication and as Requip for the anti-Parkinson indication) is available in various preparations, ranging from the .25 mg tablet to the 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 1.90mg, once daily 1-3 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.

Mechanism

Ropinirole acts as an agonist at the D2 and D3 dopamine receptor subtypes, binding with higher affinity to D3 than to D2 or D4 and It has no affinity for D1 receptors. It has medium in vitro affinity to opioid receptors. Ropinirole is weakly active at the 5-HT2, and α2 receptors and is said to have virtually no affinity to 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 24mg, CYP2D6 may be inhibited, although this has only been tested in vitro.[1]

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 on 28 September 2008  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, Diego et al. (2007). "A 52-week open-label study of the long-term safety of ropinirole in patients with restless legs syndrome". Sleep Medicine 8: 742–752. doi:10.1016/j.sleep.2006.09.009. 
  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. 

External links

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Antiparkinson drugs: dopaminergic agents (N04B)
Dopa and derivatives
Adamantane derivatives
Dopamine agonists
MAOIs (B)
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Wikipedia content modification information:

  • This page was last modified on 28 September 2008, at 19:50.

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