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Nonergotoline Dopamine Agonists and Other Medications

Two nonergotoline dopamine agonists are effective in treating RLS, including ropinirole (Requip®) and pramipexole (Mirapex®). In May 2005, ropinirole was the first drug in the United States to receive approval from the FDA for labeling for the treatment of moderate to severe RLS. These medications are taken by mouth, with or without food, one to three hours before the time of day that the symptoms usually first appear. Although food does not affect the absorption of these drugs, taking them with food may help to reduce the risk of nausea. Other associated side effects may include fatigue, stiffness, nausea, a sudden onset of sleepiness, or dizziness. Orthostatic hypotension may also occur, but the incidence may be lower than with the nonergotoline drugs. Another undesirable effect that some people have experienced is swelling in the arms and legs (peripheral edema).

Pramipexole stimulates D2 and D3 receptors. Pramipexole is typically initiated at a low dose, such as 0.125 mg and then gradually increased to an appropriate effective level (e.g., an average of 0.3 mg).

Ropinirole works by stimulating the D3 receptors. Like pramipexole, ropinirole is usually started at a low dose and then gradually increased until the symptoms of RLS are relieved. The usual starting dose for ropinirole is 0.25 mg, and increases gradually to 3 mg daily.