Requip: profile and news






Are You Sure You're Feeling OK?  May 16, 2006
...first issued press releases about trials of its drug Requip for relief of restless legs syndrome, and 2005, when the US Food and Drug Administration (FDA ... - AlterNet,

Hey, You Don't Look So Good  May 2, 2006
In 2005, Glaxo's Requip, a treatment for Parkinson's disease, was approved for restless legs. At the same time the Restless Legs ... - BusinessWeek

Forget the news, the commercials have me worried  Apr 25, 2006
Another side of this medical marketing business is naming the drugs -- which in the case of restless legs syndrome is called "Requip" -- a drug first approved ... - Louisville Courier-Journal,

SkyePharma PLC - Preliminary Results Announcement for the Year ...  Apr 19, 2006
Requip Once-a-day In December 2005, SkyePharma's collaborator GlaxoSmithKline submitted Requip Once-a-day, a once-daily dosage formulation of Requip(R ... - PR Newswire (press release),

The Quest for Rest  May 2, 2006
Requip, a new drug for restless legs, works by stimulating dopamine receptors in the brain, an effect also used to treat Parkinson's disease. ... - Standard-Speaker,

Drug company Glaxosmithkline announce sales boost  Apr 27, 2006
Glaxo also reported a strong performance by recently launched drugs such as Requip for Parkinson's Disease and Restless Legs Syndrome, which saw sales rise by ... - Manchester Evening News,

Glaxo confident on drug pipeline as profits leap  Apr 27, 2006
Garnier said he was particularly encouraged by the contribution of restless leg drug Requip, Avodart for prostate enlargement and osteoporosis drug Boniva in ... - San Diego Union Tribune,

Experts See Need for Further Study of Insomnia and Sleep Aids like ...  Apr 24, 2006
Some of the more peculiar side effects have been: (1) compulsive gambling and other unhealthy addictions linked to Mirapex and Requip, which are used to treat ... - Newsinferno.com,

Healthcare: At a Glance - Pharma Firms Slammed for 'Disease ...  Apr 21, 2006
...depression. Indeed - GSK is behind a treatment called Requip (ropinirole), which it hopes to market as Adartrel in the UK. Clew ... - International News Service,


Other information


Indication
For the treatment of the signs and symptoms of idiopathic Parkinson's disease. Also used for the treatment of restless legs syndrome.

Pharmacology
Ropinirole is a nonergot dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is unknown. The mechanism of ropinirole-induced postural hypotension is presumed to be due to a D2 -mediated blunting of the noradrenergic response to standing and subsequent decrease in peripheral vascular resistance.

Mechanism Of Action
Ropinirole binds the dopamine receptors D3 and D2. Although the precise mechanism of action of ropinirole as a treatment for Parkinson's disease is unknown, it is believed to be related to its ability to stimulate these receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have demonstrated that ropinirole influences striatal neuronal firing rates via activation of dopamine receptors in the striatum and the substantia nigra, the site of neurons that send projections to the striatum.

Drug Category
Dopamine Agonists; Antiparkinson Agents; Antidyskinetics; Central Nervous System Agents; ATC:N04BC04

Brand Names/Synonyms
CHEMBANK1792; Requip; Ropinirol [Inn-Spanish]; Ropinirole; Ropinirole Hcl; Ropinirole Hydrochloride; Ropinirolum [Inn-Latin]

Dosage Forms
TABLET (0.25 mg, 0.5 mg, 1 mg, 2 mg, 4 mg or 5 mg)

Absorption
Absolute bioavailability is 55%, indicating a first pass effect. Food does not affect the extent of absorption.

Interactions
Interactions for Ropinirole:

P 450 Interaction:    In vitro metabolism studies showed that CYP1A2 was the major enzyme responsible for the metabolism of ropinirole. There is thus the potential for substrates or inhibitors of this enzyme when coadministered with ropinirole to alter its clearance. Therefore, if therapy with a drug known to be a potent inhibitor of CYP1A2 is stopped or started during treatment with Requip , adjustment of the Requip dose may be required.

L-dopa:   Co-administration of carbidopa + L-dopa (Sinemet® 10/100 mg b.i.d.) with ropinirole (2.0 mg t.i.d.) had no effect on the steady-state pharmacokinetics of ropinirole (n=28 patients). Oral administration of Requip 2.0 mg t.i.d. increased mean steady state C max of L-dopa by 20% but its AUC was unaffected (n=23 patients).

Digoxin:   Co-administration of Requip (2.0 mg t.i.d.) with digoxin (0.125-0.25 mg q.d.) did not alter the steady-state pharmacokinetics of digoxin in 10 patients.

Theophylline:    Administration of theophylline (300 mg b.i.d., a substrate of CYP1A2) did not alter the steady-state pharmacokinetics of ropinirole (2 mg t.i.d.) in 12 patients with Parkinson's disease. Ropinirole (2 mg t.i.d.) did not alter the pharmacokinetics of theophylline (5 mg/kg i.v.) in 12 patients with Parkinson's disease.

Ciprofloxacin:   Co-administration of ciprofloxacin (500 mg b.i.d.), an inhibitor of CYP1A2, with ropinirole (2 mg t.i.d.) increased ropinirole AUC by 84% on average, and C max by 60% (n=12 patients).

Estrogens:   Population pharmacokinetic analysis revealed that estrogens (mainly ethinylestradiol: intake 0.6-3 mg over 4-month to 23-year period) reduced the oral clearance of ropinirole by 36% in 16 patients. Dosage adjustment may not be needed for Requip in patients on estrogen therapy because patients must be carefully titrated with ropinirole to tolerance or adequate effect. However, if estrogen therapy is stopped or started during treatment with Requip , then adjustment of the Requip (ropinirole hydrochloride) dose may be required.

Dopamine Antagonists:   Since ropinirole is a dopamine agonist, it is possible that dopamine antagonists, such as neuroleptics (phenothiazines, butyrophenones, thioxanthenes) or metoclopramide, may diminish the effectiveness of Requip . Patients with major psychotic disorders, treated with neuroleptics, should only be treated with dopamine agonists if the potential benefits outweigh the risks.

Population analysis showed that commonly administered drugs, e.g., selegiline, amantadine, tricyclic antidepressants, benzodiazepines, ibuprofen, thiazides, antihistamines, and anticholinergics did not affect the oral clearance of ropinirole.



Chemical IUPAC Name
4-(2-dipropylaminoethyl)-1,3-dihydroindol-2-one

Chemical Formula
C16H24N2O

Half Life
6 hours

Drug Type
Approved Drug

# Accession No
APRD00302

CAS Registry Number
91374-21-9

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