It was approved for medical use in the United States in 1997.[4] It is available as a generic medication.[3] In 2022, it was the 163rd most commonly prescribed medication in the United States, with more than 3million prescriptions.[6][7]
A 2008 meta-analysis found that ropinirole was less effective than pramipexole in the treatment of restless legs syndrome.[9]
Side effects
Ropinirole can cause nausea, dizziness, hallucinations, orthostatic hypotension, and sudden sleep attacks during the daytime. Unusual side effects specific to D3 agonists such as ropinirole and pramipexole can include hypersexuality, punding and compulsive gambling, even in patients without a history of these behaviours.[10]
Ropinirole is also known to cause an effect known as "augmentation" when used to treat restless legs syndrome, where over time treatment with dopamine agonists will cause restless legs syndrome symptoms to become more severe. This usually leads to constant dosage increases in an attempt to offset the symptom progression. Symptoms will return to the level of severity they were experienced at before treatment was initiated if the drug is stopped; however, both ropinirole and pramipexole are known to cause painful withdrawal effects when treatment is stopped and the process of taking a patient who has been using the medication long-term off of these drugs is often very difficult and generally should be supervised by a medical professional.[11]
Ropinirole is metabolized primarily by cytochrome P450CYP1A2 to form two metabolites; SK&F-104557 and SK&F-89124, both of which are renally excreted,[17] and at doses higher than clinical, is also metabolized by CYP3A4. At doses greater than 24mg, CYP2D6 may be inhibited, although this has been tested only in vitro.[2]
In November 2012, GlaxoSmithKline was ordered by a Rennes appeals court to pay Frenchman Didier Jambart 197,000 euros ($255,824); Jambart had taken ropinirole from 2003 to 2010 and exhibited risky hypersexual behavior and gambled excessively until stopping the medication.[19] This behavior displayed is character of Dopamine Dysregulation Syndrome.[20]
1 2 3 4 Tompson DJ, Vearer D (December 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 Therapeutics. 29 (12): 2654–2666. doi:10.1016/j.clinthera.2007.12.010. PMID18201581.
↑ Clinical trial number NCT00334048 at ClinicalTrials.gov - "Treating Sexual Dysfunction From SSRI Medication: a Study Comparing Requip CR to Placebo"
↑ Quilici S, Abrams KR, Nicolas A, Martin M, Petit C, Lleu PL, etal. (October 2008). "Meta-analysis of the efficacy and tolerability of pramipexole versus ropinirole in the treatment of restless legs syndrome". Sleep Med. 9 (7): 715–26. doi:10.1016/j.sleep.2007.11.020. PMID18226947.
↑ "What is Augmentation?"(PDF). Austin, Texas: Restless Legs Syndrome (RLS) Foundation. Archived from the original(PDF) on 9 May 2018. Retrieved 8 May 2018.
↑ Eden RJ, Costall B, Domeney AM, Gerrard PA, Harvey CA, Kelly ME, etal. (January 1991). "Preclinical pharmacology of ropinirole (SK&F 101468-A) a novel dopamine D2 agonist". Pharmacology, Biochemistry, and Behavior. 38 (1): 147–154. doi:10.1016/0091-3057(91)90603-Y. PMID1673248. S2CID26842270.
↑ Bender AM, Parr LC, Livingston WB, Lindsley CW, Merryman WD (August 2023). "2B Determined: The Future of the Serotonin Receptor 2B in Drug Discovery". J Med Chem. 66 (16): 11027–11039. doi:10.1021/acs.jmedchem.3c01178. PMC11073569. PMID37584406. S2CID260924858. Functionally Biased Agonists. Conversely, a compound presenting as an agonist in 5-HT2B functional assays does not necessarily pose a risk for valvulopathy. In 5-HT2B calcium flux assays, certain known VHD-associated compounds displayed an agonist profile comparable to that of ropinirole, an approved treatment for Parkinson's disease (PD) and restless leg syndrome.122 Because ropinirole is not known to be associated with VHD or similar cardiopathies, it is thought that calcium flux may not be the optimal assay for screening 5-HT2B agonists for potential VHD-related risks. In additional readouts of 5-HT2B receptor activation (calcium-sensitive NFAT-mediated transcription of a β-lactamase reporter gene, accumulation of InsPs in LiCl-treated cells, recruitment of β-arrestin to agonist-occupied receptors, and phosphorylation of the extracellular signal-regulated kinase ERK2), ropinirole was found to be "distinct from the seven known valvulopathic 5- HT2B receptor agonists [studied] in that it is much less potent, albeit not less efficacious, than the VHD-associated drugs in all but one of the 5-HT2B receptor functional assays employed." 66
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