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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.
Ropinirole’s patent expired in May 2008, and the drug is now available in generic form.
1 Medical uses
2 Dosage
3 Pharmacology
4 Side effects
5 Lawsuits
6 See also
7 References
8 External links
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.
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.
Ropinirole acts as a D 2, D 3, and D 4 dopamine receptor agonist with highest affinity for D 2. It is weakly active at the 5-HT 2, and α 2 receptors and is said to have virtually no affinity for the 5-HT 1, GABA, mAChRs, α 1, 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,
Side effects
Ropinirole can cause nausea, dizziness, hallucinations, orthostatic hypotension, and sudden sleep attacks during the daytime. Unusual side effects specific to D 3 agonists such as ropinirole and pramipexole can include hypersexuality, punding and compulsive gambling, even in patients without a history of these behaviours.
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 RLS 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.
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.
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