Dopamine Agonists to Treat Restless Legs Syndrome

A group of drugs called dopamine agonists is among the few drugs approved by the U.S. Food and Drug Administration (FDA) to treat restless legs syndrome (RLS). In general, these drugs are taken daily and only prescribed for people with severe RLS when other treatments have not worked.^1,2

How do dopamine agonists work to treat RLS?

Dopamine agonists are a group of drugs that imitate the brain chemical dopamine. This makes the brain think it is getting enough dopamine. Low dopamine levels are thought to cause the restless, creepy, crawly feelings of RLS. Higher dopamine levels seem to reduce these symptoms.

Studies show that these drugs work well to reduce RLS symptoms, reduce periodic limb movement, increase time in bed, and improve reported sleep quality. In general, the drugs begin to work after 1 week.³

Types of dopamine agonists used to treat RLS include:¹

• Requip (ropinirole)
• Mirapex (pramipexole)
• Neupro (rotigotine)

Mirapex and Requip are pills that begin to work 90 to 120 minutes after taken. This means that the drugs should be taken 2 hours before RLS symptoms begin. When first prescribed, doses are usually increased slowly every 2 to 3 days until the minimum amount for relief is found.

Neupro is a patch worn on the skin. Doses are gradually increased just like other dopamine agonists.

Other dopamine agonists that were once prescribed off-label for RLS and include:

• Cabergoline
• Pergolide

Off-label means that the FDA has not officially approved a drug to be used for another condition, but doctors may try it anyway. This practice is permitted by the FDA. However, these drugs caused severe side effects and are no longer used.²

When are dopamine agonists prescribed?

Dopamine agonists are prescribed when alpha-2-delta calcium channel ligands, iron supplements, and lifestyle changes have not brought relief.¹

What are the possible side effects of dopamine agonists?

The most common side effects of dopamine agonists tend to be mild, such as:^1,3

• Nausea
• Lightheadedness
• Fatigue
• Headache

Nearly half of everyone using the Neupro patch reported a skin reaction.

Less common symptoms include nasal stuffiness, constipation, insomnia, and swelling of the legs. Some people develop impulse-control issues, such as excessive shopping, high-risk sexual activity, and gambling. Most side effects go away within 10 to 14 days, although impulse control may not improve until the drug is stopped.¹

People taking these drugs should see their doctor every 6 to 12 months to be monitored for side effects, especially augmentation.¹

These are not all the possible side effects of dopamine agonists. Talk to your doctor about what to expect when taking dopamine agonists. You also should call your doctor if you have any changes that concern you when taking dopamine agonists.

What is augmentation?

Augmentation is a serious side effect common to dopamine agonists. Augmentation is when RLS symptoms get worse instead of improving when the person is taking higher doses of the medicine. The drugs may work for shorter periods of time, or the symptoms may begin earlier in the day or spread to the arms. These symptoms are often worse than the original symptoms before drug treatment. Between 50 and 70 percent of people who take these drugs eventually experience augmentation within 10 years.^1,4

Things to know about dopamine agonists

Withdrawal symptoms can occur if a dopamine agonist is stopped too quickly.

Doctors usually prefer to prescribe dopamine agonists before levodopa/carbidopa due to the lower risk of complications.¹

These drugs may also be prescribed for Parkinson’s disease, though at much higher doses than for RLS.¹

Before beginning treatment for RLS, tell your doctor about all your health conditions and any other drugs, vitamins, or supplements you are taking. This includes over-the-counter drugs.