Trade names Requip MedlinePlus a698013 Routes of
administration Oral CAS ID 91374-21-9 Bioavailability 50% | AHFS/Drugs.com Monograph Pregnancy
category C ATC code N04BC04 (WHO) Molar mass 260.375 g/mol | |
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How to pronounce ropinirole requip memorizing pharmacology flashcard
Ropinirole (INN; trade names Requip, Repreve, Ronirol, Adartrel) is a dopamine agonist of the non-ergoline class of medications. It is manufactured by GlaxoSmithKline (GSK), Cipla, Dr. Reddy's Laboratories and Sun Pharmaceutical. It is used in the treatment of Parkinson's disease and restless legs syndrome (RLS). Ropinirole is one of three medications approved by the FDA to treat RLS, the other two being pramipexole (Mirapex) and gabapentin enacarbil (Horizant). The discovery of the drug's utility in RLS has been used as an example of successful drug repurposing.
Contents
- How to pronounce ropinirole requip memorizing pharmacology flashcard
- Medical uses
- Dosage
- Pharmacology
- Side effects
- Lawsuits
- References
Ropinirole's patent expired in May 2008, and the drug is now available in generic form.
Medical uses
Ropinirole is prescribed for mainly Parkinson's disease, RLS and extrapyramidal symptoms. It can also reduce the side effects caused by selective serotonin reuptake inhibitors, including Parkinsonism syndrome as well as sexual dysfunction and erectile dysfunction caused by either SSRIs or antipsychotics.
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 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 Parkinson's disease, the maximum recommended dose is 24 mg per day, taken in three separate doses spread throughout the day. The maximum dose recommendations of ropinirole for subjects with end stage renal disease (ESRD) should be reduced by 25% compared with those recommended for subjects with normal renal function. A 25% dose reduction represents a more straightforward dosage regimen in terms of available tablet strength, compared with a 30% dose reduction.
For 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.
Pharmacology
Ropinirole acts as a D2, D3, and D4 dopamine receptor agonist with highest affinity for D2. It is weakly active at the 5-HT2, and α2 receptors and is said to have virtually no affinity for the 5-HT1, GABA, mAChRs, α1, and β-adrenoreceptors.
Ropinirole is metabolized primarily by cytochrome P450 CYP1A2 to form two metabolites; SK&F-104557 and SK&F-89124, both of which are renally excreted, 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.
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.
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 Parkinson's treatment.