title: Critical review of ropinirole and pramipexole - putative dopamine D(3)-receptor selective agonists - for the treatment of RLS.
abstract: Ropinirole hydrochloride (REQUIP, ADARTREL) and pramipexole dihydrochloride (MIRAPEX, SIFROL) are two putative dopamine D(3) receptor subtype-selective agonists recently approved by the FDA for the treatment of 'restless legs syndrome' (RLS). RLS is a difficult to define condition that is possibly more prevalent than previously thought. Direct-to-consumer advertising has raised public and professional awareness of RLS, but questions, even skepticism about the very existence of the condition, persist. The drugs have adverse effects that can negatively impact on quality of life and thus, as true for all drugs, require consideration of the benefit : risk ratio. We review the definition, diagnostic criteria, pathophysiology, and treatment of RLS, and assess the clinical and preclinical evidence for a pharmacologic rationale for D(3) agonism in general and of the claimed D(3) selectivity of ropinirole and pramipexole in particular.
authors.affiliation: Department of Pharmaceutical Sciences, Temple University School of Pharmacy, Philadelphia, PA, USA.
authors.forename: L I
authors.initials: LI
authors.lastname: Varga
authors.forename: N
authors.initials: N
authors.lastname: Ako-Agugua
authors.forename: J
authors.initials: J
authors.lastname: Colasante
authors.forename: L
authors.initials: L
authors.lastname: Hertweck
authors.forename: T
authors.initials: T
authors.lastname: Houser
authors.forename: J
authors.initials: J
authors.lastname: Smith
authors.forename: A A
authors.initials: AA
authors.lastname: Watty
authors.forename: S
authors.initials: S
authors.lastname: Nagar
authors.forename: R B
authors.initials: RB
authors.lastname: Raffa
mesh_terms: D000818:Animals; D052160:Benzothiazoles / Q000009:adverse effects / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D003937:Diagnosis, Differential; D004298:Dopamine / Q000502:physiology; D018491:Dopamine Agonists / Q000627:therapeutic use*; D006801:Humans; D007211:Indoles / Q000009:adverse effects / Q000627:therapeutic use*; D000077487:Pramipexole; D050637:Receptors, Dopamine D3 / Q000819:agonists* / Q000502:physiology; D012148:Restless Legs Syndrome / Q000175:diagnosis / Q000188:drug therapy* / Q000503:physiopathology
chemical_list: D052160:Benzothiazoles; D018491:Dopamine Agonists; D007211:Indoles; D050637:Receptors, Dopamine D3; C046649:ropinirole; D000077487:Pramipexole; D004298:Dopamine