Ropinirole

Source: Wikipedia, the free encyclopedia.

Ropinirole
Clinical data
Trade namesRequip, Repreve, Ronirol, others
AHFS/Drugs.comMonograph
MedlinePlusa698013
License data
By mouth
ATC code
Legal status
Legal status
  • BR: Class C1 (Other controlled substances)[1]
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability50%[2]
MetabolismLiver (CYP1A2)[2]
Elimination half-life5-6 hours[2]
Identifiers
  • 4-[2-(Dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one
JSmol)
  • O=C2Nc1cccc(c1C2)CCN(CCC)CCC
  • InChI=1S/C16H24N2O/c1-3-9-18(10-4-2)11-8-13-6-5-7-15-14(13)12-16(19)17-15/h5-7H,3-4,8-12H2,1-2H3,(H,17,19) checkY
  • Key:UHSKFQJFRQCDBE-UHFFFAOYSA-N checkY
  (verify)

Ropinirole, sold under the brand name Requip among others, is a

by mouth.[4]

Common side effects include sleepiness, vomiting, and dizziness.

dopamine D2 receptors.[4]

It was approved for medical use in the United States in 1997.

generic medication.[3] In 2021, it was the 142nd most commonly prescribed medication in the United States, with more than 4 million prescriptions.[6][7]

Medical uses

Ropinirole is prescribed for mainly

SSRIs[8]
or antipsychotics.

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,

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]

Pharmacology

Ropinirole acts as a

cardiac valvulopathy.[14][15]

Ropinirole is metabolized primarily by

metabolites; SK&F-104557 and SK&F-89124, both of which are renally excreted,[16] and at doses higher than clinical, is also metabolized by CYP3A4. At doses greater than 24 mg, CYP2D6 may be inhibited, although this has been tested only in vitro.[2]

Society and culture

It is manufactured by

drug repurposing.[17]

Lawsuits

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.[18]

References

  1. ^ Anvisa (31 March 2023). "RDC Nº 784 - Listas de Substâncias Entorpecentes, Psicotrópicas, Precursoras e Outras sob Controle Especial" [Collegiate Board Resolution No. 784 - Lists of Narcotic, Psychotropic, Precursor, and Other Substances under Special Control] (in Brazilian Portuguese). Diário Oficial da União (published 4 April 2023). Archived from the original on 3 August 2023. Retrieved 16 August 2023.
  2. ^
    PMID 18201581
    .
  3. ^
    ISBN 978-0-85711-338-2
    .
  4. ^ a b c d e "Ropinirole Hydrochloride Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 3 March 2019.
  5. ^ "Ropinirole Pregnancy and Breastfeeding Warnings". Drugs.com. Retrieved 3 March 2019.
  6. ^ "The Top 300 of 2021". ClinCalc. Archived from the original on 15 January 2024. Retrieved 14 January 2024.
  7. ^ "Ropinirole - Drug Usage Statistics". ClinCalc. Retrieved 14 January 2024.
  8. ^ Clinical trial number NCT00334048 at ClinicalTrials.gov - "Treating Sexual Dysfunction From SSRI Medication: a Study Comparing Requip CR to Placebo"
  9. PMID 18226947
    .
  10. PMID 19339647
    .
  11. ^ "What is Augmentation?" (PDF). Austin, Texas: Restless Legs Syndrome (RLS) Foundation. Archived from the original (PDF) on 9 May 2018. Retrieved 8 May 2018.
  12. PMID 19557097
    .
  13. S2CID 26842270
    .
  14. S2CID 260924858
    . 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
  15. PMID 19570945
    .
  16. ^ Tompson D, Hewens D, Earl N, Oliveira D, Taubel J, Swan S, et al. (7–11 June 2009). An open-label, parallel-group, repeat-dose study to investigate the effects of end-stage renal disease and haemodialysis on the pharmacokinetics of ropinirole] (PDF). 13th International Congress of Parkinson’s Disease and Movement Disorders. Paris, France. Archived from the original (PDF) on 17 March 2012.
  17. ^ Lipp E (1 August 2008). "Novel Approaches to Lead Optimization". Genetic Engineering & Biotechnology News. Vol. 28, no. 14. p. 20. Retrieved 28 September 2008.
  18. ^ Wong C (29 November 2012). "Court Rules Parkinson's Drug Turned Straight Patient Into A Gay Sex Addict". Huffington Post.
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