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Restless Legs Medication

Restless leg syndrome is mostly associated with low levels of dopamine and iron in the substantia nigra. The recommended treatment for this syndrome depends on the severity of its symptoms. Read on to find out the medications and supplements used in the treatment of restless leg syndrome.
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What is Restless Leg Syndrome?

Restless leg syndrome is a neurological disorder characterized by an irresistible urge to move to relieve uncomfortable, odd sensations. The sensations experienced can be pain, ache, itch, tickle or crawly.

These odd sensations interfere with normal daily activities and the urge to move usually strikes during periods of rest and wakefulness. Therefore, restless leg syndrome affects the quality of sleep and may even cause insomnia.

These sensations usually affect the legs but they can also affect the torso or the arms (and even phantom limbs in amputees).

Not all cases of restless leg syndrome is accompanied by sensations. In some patients, there is simply the pressing urge to move.

Restless leg syndrome is really a spectrum disease. This means that while some experience very minor symptoms which barely qualify as a separate disorder, others experience more profound symptoms which affects their quality of life.

There are specific criteria used to diagnose restless leg syndrome.

The 4 Basic Criteria for RLS Diagnosis
  • An urge to move the limbs; this may be caused by odd sensations or not
  • Temporary relief of the symptoms after some degree of activity in the affected limb
  • Worsening of symptoms at rest
  • Worsening of symptoms in the evening or night; and relief in the morning

Restless leg syndrome is classified into 2: primary or idiopathic restless leg syndrome and secondary restless leg syndrome.

Primary restless leg syndrome is usually diagnosed early (before 40 years of age); it may remain dormant for a while but it worsens with age. The cause of this type of the syndrome is unknown.

Secondary restless leg syndrome is diagnosed later in life and it is usually caused by an underlying disease or medications.

Iron deficiency is the most commonly associated nutritional deficiency with restless leg syndrome. Iron is linked to dopamine levels in the brain. Specifically, iron crosses the blood-brain barrier and is used in the synthesis of levodopa, a precursor of dopamine.

Iron and dopamine levels are usually low in the substantia nigra of patients diagnosed with restless leg syndrome. The substantia nigra is located in the midbrain and it is responsible for controlling movement and addiction.

Folate deficiency and magnesium deficiency are also known to worsen the syndrome.

Medical conditions associated with restless leg syndrome include autoimmune diseases such as celiac disease and rheumatoid arthritis; neurodegenerative diseases such as peripheral neuropathy and Parkinson’s disease; and other diseases such as sleep apnea, ADHD, diabetes, thyroid disease and fibromyalgia.

Certain drugs can also cause or worsen restless leg syndrome. These include anti-nausea drugs that block dopamine receptors, antihistamines found in OTC cold medications, antipsychotics, anticonvulsants and antidepressants.

Opioid withdrawal, chronic alcohol consumption and surgery can also contribute to this syndrome.

Restless leg syndrome has a strong genetic component. It is estimated that 60% of patients have other members of their families with the same condition.

There are multiple chromosomes and genes that predispose people to this syndrome.

Non-Medications for Restless Leg Syndrome

There are no established ways to prevent restless leg syndrome except to avoid or treat the underlying causes. This is especially true for secondary restless leg syndrome which is caused by some other disease or medications.

The most popular non-medication methods of relieving the symptoms of restless leg syndrome are exercise and bath.

Most sufferers experience relief simply by walking. Where walking is not possible, stretching and shaking the legs may also help.

However, this relief does not last long and sufferers soon regain the urge to move their limbs. Besides, rigorous exercise can tire the body and cause fatigue which worsens the syndrome.

Relaxation techniques such as massage and warm baths can also help relieve symptoms in the restless limb. Hot and cold showers have also been reported to provide relief. Another relaxation technique known to improve symptoms involve lying on one’s front on the floor for 30 minutes.

In addition, to reduce the symptoms of restless leg syndrome caffeine, alcohol and tobacco should be avoided. Also, heavy meals should not be eaten before bed times. Avoiding these can help reduce nighttime excitation which can cause insomnia and restlessness.

Restless leg syndrome can also be treated with monochromatic near-infrared light treatment.

Medications for Restless Leg Syndrome

Dopaminergic Drugs

The drugs in this class are usually the first ones used in the treatment of restless leg syndrome.

Dopaminergic drugs increase the availability and activity of dopamine in the brain. Since the dopaminergic system is responsible for regulation of movement, this action helps reduce the irresistible urges associated with restless leg syndrome.

Common side effects of dopaminergic drugs include nausea, daytime sleepiness, insomnia, headache, chest pain, rapid heartbeat and dizzy spells especially when standing up quickly.

When patients are taken off these drugs, they may experience severe withdrawal symptoms for a couple of days thereafter. The duration of these withdrawal period will depend on how long a patient has been taking the drugs.

Dopaminergic drugs can either be dopamine precursors or dopaminergic receptor agonists.

Dopamine Precursors

Dopamine precursors include levodopa and carbidopa. Levodopa is the direct precursor of dopamine in the brain.

While levodopa was the drug of choice for treating severe restless leg syndrome, physicians now prefer to prescribe it along with other dopamine precursors. Therefore, levodopa plus carbidopa (Sinemet) is the current drug of choice in this class.

By combining levodopa with carbidopa, the side effects of levodopa (especially nausea) is much reduced and the combination is well tolerated amongst patients. Even then care is taken when treating with this combination. Usually, prescribers start with a very low dose which is to be taken by the patient an hour before going to bed. This dose is then increased until the patient reports relief.

Levodopa works fast and patients report quick relief.

However, dopamine precursors (and even dopamine receptor agonists) can cause augmentation or rebound of restless leg syndrome.

Augmentation refers to relief of symptoms during the time of the day when they were normally worse but the worsening of these symptoms earlier in the day. Rebound refers to increase in severity of symptoms as the drug wears off or when the body develops tolerance to it.

Patients receiving high doses (more than 200 mg/day) of levodopa are most affected by these presentations. Therefore, it is advised that levodopa should be used intermittently and no more than 3 times per week.

Once augmentation occurs, levodopa should be stopped and patients switched over to dopamine receptor agonists.

Dopamine Receptor Agonists

Dopamine receptor agonists, or simply dopamine agonists, include cabergoline (derived from ergot); ropinirole and pramipexole (derived from non-ergot sources).

These drugs bind to dopamine receptors and by mimicking dopamine, they produce similar effects. They produce lesser side effects than levodopa and can be used daily because they have a lower tendency to cause augmentation and rebound.

However, augmentation still occurs in 1 in 3 patients receiving dopamine agonists. In addition, high doses and long-term use increases the risk of augmentation.

On the other hand, dopamine agonists are effective for most restless leg syndrome patients (70% - 90%).

Ropinirole is widely known under the brand name, Requip. It is the first drug approved for treating moderate to severe restless leg syndrome.

Pramipexole is commonly sold under the brand name, Mirapex.


Benzodiazepines are also sedative hypnotics. They are not prescribed to reduce the irresistible urge to move. Rather, they are given to treat insomnia and help patients sleep through their symptoms.

Examples of benzodiazepines prescribed for restless leg syndrome patients are clonazepam, diazepam, temazepam and loprazolam.

These drugs may cause daytime drowsiness. They are only intended for short-term therapy.

Benzodiazepines should not be prescribed for patients with sleep apnea to prevent aggravation of symptoms. They are also not recommended for pregnant women and lactating mothers.

Stopping benzodiazepines after prolonged use will cause withdrawal symptoms such as arrhythmia, sweating, gastrointestinal problems, hallucination and even rebound insomnia.


Anticonvulsants are drugs that prevent seizures. They do this by relaxing the blood vessels. Therefore, they can be used to relax restless limbs.

Examples of anticonvulsants used in the treatment of restless leg syndrome are gabapentin (Neurontin), valproic acid and carbamazepine (Tegretol).

Gabapentin is the most commonly prescribed drug in the class for the treatment of restless leg syndrome. Besides its anticonvulsant property, it also possesses analgesic properties.

A new molecule based on gabapentin, gabapentin enacarbil (Horizant), is now increasingly prescribed for this symptom. It is a prodrug that releases gabapentin in the intestines. In this way, it produces double the bioavailability of old formulations of gabapentin.

Gabapentin has fewer side effects than carbamazepine and valproic acid but all anticonvulsants have serious side effects including increased appetite, weight gain, irritability, hand tremor, hair loss and heartburn.

Gabapentin also causes sleepiness and dizziness.


Opioids are synthetic narcotic pain relievers related to opiates such as codeine and morphine.

But opiates and opioids are used in the treatment of restless leg syndrome especially when pain is a major manifestation. However, some studies have also shown that opioids help reduce the frequency of restless limbs.

Oxycodone is the most commonly prescribed opioid for severe restless leg syndrome.

Most people find opioid use for this syndrome controversial because of the addictive potential. For patients who prefer not to be placed on opioids, tramadol is an effective alternative. It has opioid-like activities and none of their addictive potential.

However, opioids and even tramadol may cause insomnia and restless leg syndrome.


Other medications have also been shown to be useful for restless leg syndrome.

Clonidine (Catapres), an alpha 2 agonist, is used to treat patients who have hypertension and restless leg syndrome because it is effective for both conditions.

Bupropion, an antidepressant, is also a new drug used to treat this syndrome. It acts by blocking the removal of dopamine from nerve endings. Therefore, it prolongs the action of dopamine in the brain.


Supplements are also sometimes used to treat restless leg syndrome especially in patients with nutritional deficiencies.

Iron supplement is the most important of these supplements because studies have shown that iron levels are low in the cerebrospinal fluids of restless leg syndrome patients. Besides, iron is taken up into the brain where it is required for the formation of levodopa, a precursor of dopamine.

Restless leg syndrome can also be caused by folate deficiency and magnesium deficiency. Therefore, supplementation with those nutrients can help treat the syndrome.

Other minerals such as calcium, vitamins such as vitamin B12, amino acids such as glycine and herbal extracts such as lemon balm and valerian roots have been shown to provide some benefits for patients of restless leg syndrome.

The best way to take these supplements is to take a combination of them.

Sedorum is an excellent example of natural supplements that are safe to use and effective in the treatment of restless leg syndrome. It contains vitamins, minerals, amino acids and herbs proven to improve symptoms of restless leg syndrome.





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