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Drugs for RLS

Updated on December 10, 2012

There are several drugs that are available today for the treatment of restless leg syndrome.

Requip is a drug used in to treat thyroid disorders. This has been used for the treatment of RLS due to its effectiveness and efficiency. Others have found 5 hydroxytryptophan useful in the treatment of RLS. Here you will read on to find how effectively you can use these drugs for RLS and why they are effective.

Restless leg syndrome is a health disorder that is characterized by feelings of discomfort on the legs. These feelings and sensations on the legs are dependent on particular individuals such that there are different feelings with different people. This means that some people will feel pain on the legs, others will feel itchy, twitchy among many other different feelings. The disorder is more severe towards the evening, during the night and early in the morning. The causes of the disorder are not very clear and there are several theories that seek to explain the same. Some of these theories range from those who associate it with heredity, use of medications, underlying medical factors, dietary deficiencies such as in iron, vitamins etc. however, it is good to note that the most common symptom of the disorder is the urge to keep walking, or moving the legs. It is also notable that the disorder also affects other parts of the body such as hands, and back.

RLS is not life-threatening but can be very disturbing. It causes sleeplessness and also untold suffering. In this way, it is very important to learn how to control it by use of the necessary treatment options that are available. Among these treatment options is the use of requip.

What is requip?

Manufactured by GlaxoSmithKline, requip is a very important treatment option for RLS. It is usually an oral type of ropinirole that is available in tablets. This drug is also available in two formulations of normal and extended release. In addition to containing hydrochloride salt, the tablets also contain inactive ingredients such as iron oxide, cellulose, lactose, titanium dioxide among others.

The drug is tasked with dopamine issues in the body and the brain and is usually a prescription drug for Parkinson disease as well as restless leg disorder. It is important to note that requip can be taken with food. This is especially recommended by the manufacturers due to the fact that it reduces some of the side effects associated with it and more so nausea feelings. It is also good to know that there is nothing wrong if you feel that you want to take it without necessary having to take food as well.

Among the most notable other side effects apart from nausea include;

· Sleeping during the day. This can happen suddenly and can be cause further injuries such as accidents. It is notable that you can sleep suddenly while you are talking, when eating and while doing any other normal day-time work. This is without mentioning that you can sleep suddenly while driving, or swimming.

· Sweating profusely

· Hallucinations

· Drowsiness

· Low blood pressure

It is also important to realize that requip just like all other drugs in this class is known to lead to reduced control of certain manners. These behaviors include inclinations and addiction to such issues as gambling and sexual feelings. However, this tendency is not very much related to requip but has been a source of controversy and debate.

Augmentation and rebound is a term used to refer to the shifting of symptoms from when they are normally experienced to other times that are not associated with the disorder. This is true with the use of requip. It is known that the symptoms of RLS set in towards the evening and the night. With the use of requip, the symptoms shift from the known time to earlier in the evening and later the next morning.

Those people who are allergic to ropinirole and all other inactive components in requip should not use the drug. The drug should also not be used with alcohol, antidepressants or any sedatives. This is because of its side effects.

Like all other prescription drugs that are taken by people, requip should be used with a lot of care. A qualified professional such as a physician should be consulted all the time before using the drug. This is especially so if the patient is also using other medications. Some drugs are known to interfere with its efficacy or interfere with the metabolism of ropinirole in the body.

The withdrawal of requip should be done over a period of seven days. Requip should not be withdrawn abruptly this can cause other symptoms related to the effects of the drug deficiency in the body.

What is ropinirole?

Ropinirole is one of the commonly used dopamine agonists. It was chiefly intended for treating Parkinson disease but today, it is used to treat in addition to Parkinson disease, restless leg syndrome. In the treatment of RLS, ropinirole has become very popular. It should be noted that the patent to ropinirole expired in 2008 and since then the drug has been manufactured using various brand names.

Among the most common brand names of ropinirole include requip, adartel and ropark. It is known that the drug is highly absorbed once it has been taken. It is then distributed in the body and it is notable that about 40% of the drug is bound on the proteins in the plasma. Once the drug is taken orally, its metabolism takes place in the liver. It has been discovered that about ten percent of the drug is eliminated from the body without being changed. The rest of the drug is urinated out of the body in metabolites of ropinirole.

The drug is known to bide itself on the dopamine receptors thereby producing its effects. These effects include both therapeutic and side effects. The drug’s biding with D3 receptors for example has been singled out as bringing the effects of high sexual urges and inclinations to gambling. This is because the drug is known to bide with dopamine and therefore bring about all these effects both good and bad.

Studies on requip and RLS

The efficacy of requip in the treatment of restless leg syndrome has been examined using quite a number of research undertakings. In this way, there have been very popular and published researches that were done in and out of the United States. The most common such researches are the three that are found on the requip brochure. These among the three researches, one was done in the United States; the other was done outside the US while the third was a multinational study that excluded the US. These researches are outlined below;

· The individuals recruited in the research had experienced at least 15 attacks of restless leg syndrome within the previous month.

· The selection of the recruits was done using random sampling method. The recruits were then administered with requip and others were given placebo.

· The symptoms were measured or evaluated using internationally recognized method called IRLS. The scores were also gotten using global improvement scores.

· Those factors that were measured included the severity of the symptoms that affected both sensory and motor effects, the sleep disturbances such as insomnia and sleeping during the day, the RLS impact on other daily chores of the patient as well as changes in mood as a result of RLS.

· The US study recruited 380 patients of which 187 were put on requip treatment while the rest were put on placebo. In the study that excluded the US, the total number of patients involved in the study was 284. Those who were put on requip treatment were 146 while the rest were given placebo. 267 recruits were involved in the multinational study that included the US. Those who were placed on requip treatment were 131. The rest were administered with a placebo.

· The starting requip was administered in 0.25 mg and they were later allowed to go up to 4 mg. however, the mean dose used for all the three studies that were done was 2 mg.

· Results were taken after 12 weeks that were used as the primary efficacy of the drug.

Results

· In all the three studies that were done, requip statistically registered very high performance scores compared to the placebo. The group that was given requip experienced a great reduction of symptoms compared to those who were administered with the placebo.

· Within 36 weeks, requip had shown that it was producing long-term efficacy and that it was preventing the reoccurrence of the restless leg syndrome to the patients.

Side effects

· All these studies registered side effects as a result of using requip. Most common of these were nausea, vomiting, dizziness and fatigue.

There have also been studies that have been done to test the efficacy of ropinirole in the treatment of RLS. The most popular is the one that was published in 2007 in the journal of Sleep Medicine.

This study is the longest that has ever been done to examine the safety of ropinirole in the treatment and management of restless leg syndrome. This study was done to specifically test the safety of the drug in the treatment of RLS and took 52 weeks.

In this study, patients were given 0.25 mg of ropinirole does and that they were also allowed a maximum of 4 mg. the mean dose of the drug was 1.9 mg. the drug was administered only once daily just a few hours before going to bed. The study included a total of 310 individuals who were suffering from restless leg syndrome.

Those who complained at least one side effect of the drug totaled 282. When the study was completed, it had only 251 individuals. The side effects registered were moderate or mild and the most common of them was nausea. 8.7 patients experienced too much side effects that they even discontinued the treatment.

The results of the study however showed that ropinirole is safe and can be used for long term treatment of RLS. Majority of the people are able to put up with the drug and manage side effects. Nausea was shown to be checked by taking the extended release formulation of the drug with food.

On the side of effectiveness, ropinirole was seen to be very highly effective in the treatment of RLS. The study showed that 87.7% of those patients involved in the study registered improvements in the symptoms. They were able to sleep better and enjoy better quality of life.

There are other drugs for RLS which are also effective in the treatment of the disorder. 5 HTP is one of the drugs that can also be used to treat restless leg syndrome.

5 HTP and antidepressants

5 HTP is an amino acid that is derived from L-tryptophan. These two essential amino acids have the property that allows them to cross the blood-brain barrier and therefore they can cross to the brain. 5 HTP crosses the blood-brain barrier better than tryptophan and therefore becomes more effective. In as much as 5 HTP is better in crossing over to the brain than the tryptophan, you cannot get it from the food sources that we usually take.

This leaves the body with no other alternative than to synthesize 5 HTP from the tryptophan that we get from meat, papaya, potatoes, banana, chicken pumpkins and vegetables. There are eight essential amino acids in the food sources that we consume. Tryptophan is available in the least amounts and therefore accounts for about one percent of the amino acids that we consume. This brings about a problem. Competition to cross the blood-brain barrier is uphill task for tryptophan. It has to compete with all these other amino acids and the chances of reaching the brain are therefore very minimal.

This therefore means that tryptophan in the food that we take or in form of supplement is a very poor source of serotonin that the brain requires. This leaves us with only one option; to take dietary supplements of 5 HTP. This one crosses to the brain better and will be available in the brain to aid in the production of serotonin. These dietary supplements are sourced from an African tree called Griffonia Simplicifolia. All the 5 HTP that is taken is transformed into serotonin and any effect of 5 HTP is normally as a result of serotonin.

Serotonin and 5 HTP

Serotonin is a neurotransmitter that is produced in the central nervous system. The majority of serotonin, over 905% is produced in the gastrointestinal cells. When produced outside the CNS, serotonin is stored on the blood platelets and used for various bodily functions. Serotonin is used as a vasoconstrictor, in healing the wounds and aiding in the clotting of blood in case of an injury. It also serves as a growth factor in the body, but when in the CNS, it serves as a neurotransmitter.

It is good to note that serotonin is responsible for the release of insulin as well as hormones. Serotonin receptors are the ones that are directly responsible for the production of hormones such as vasopressin, oxytocin, cortisol, substance p and others. Serotonin receptors are however classed from one to seven. These ones are 5 HT1, 5 HT2, 5 HT 3, 5 HT4, 5 HT5, 5 HT6, 5 HT7. All these classes are similar apart form 5 HT3.

The release of other neurotransmitters is also dependent on the serotonin receptors. Among these other neurotransmitters include dopamine, GABA, glutamate among others. This therefore means that the serotonin receptors can perform supporting and inhibitive functions.

The amount of appetite, sleep behavior and the mood that an individual gets is chiefly determined serotonin neurotransmitter in the brain. Memory and learning capabilities are also determined by serotonin. This therefore means that due to the fact that serotonin determines mood, serotonin drugs are used as antidepressants to improve mood.

It also follows that too low levels of serotonin may cause depression. It may also cause weight gain due to craving for food as well as sleep disorders. it should also be noted that very high levels of serotonin is also dangerous in the sense that it will cause serotonin syndrome that is characterized by toxicity reactions.

What are antidepressants?

These are medications that are taken to reduce the effects of low mood or too much anxiety. They are used to treat depression to those who are suffering from the disorder. Antidepressants are not only used in the treatment of depression alone. They are also used to treat a number of other disorders such as ADHD, OCD, chronic pain, eating disorders, snoring, anxiety, migraine, among other disorders.

Most of these drugs take a long time before the onset of positive signs. They usually take between four and six weeks for results to be visible. They are also known to lose their efficacies after being used for too long. Notable is the fact that according to statistics, between 30 and 50 percent chances of treating depression using antidepressants fails. This is without mentioning that these antidepressants have very many side effects such as nausea, headaches, erectile dysfunction, and loss of libido among many other serious side effects.

5 HTP as compared to antidepressants

Several studies have been done testing the efficacy of 5 HTP and antidepressants on the treatment of depression. These studies have supported the fact that 5 HTP is a better treatment method of depression compared to other conventional antidepressants. Studies have indicated that 5 HTP is well and in a better manner than antidepressants endured by the patients.

It is usually recommended that when using 5 HTP, you should not combine the same with antidepressants. This should only be done under the directions of a qualified professional such as a physician. This is especially because of the fact that 5 HTP increases the levels of serotonin in the CNS. Antidepressants are also known to do the same. In this sense, the patient will risk developing serotonin syndrome which is potentially fatal.

Serotonin syndrome

Serotonin syndrome is potentially lethal but sometimes it is manifests itself in a mild manner. In as much as there are dangers associated with low levels of serotonin, to high levels result in the toxicity reaction that is called serotonin syndrome.

The most common symptoms of serotonin syndrome include confusion, headache, and hallucinations. Other symptoms are usually high blood pressure, sweating, irregular heart-beats, and shivering. You may also experience tremors and twitching as well as overactive reflexes.

Taking serotonin drugs together with the antidepressants is usually the common cause of this syndrome. There is therefore a need to consult your doctor just in case there is a possibility of using the two together. Once you stop taking the drug that is causing this syndrome, it only takes less than 24 hours to subside. However, there are severe symptoms that may need urgent medical attention. In this way, you should always be sure to see a qualified professional who will diagnose and treat the syndrome.

Conclusion

There are several sources of drugs for RLS. However, special attention should be paid in the efforts of looking for the best drug for a particular case. There are also other alternative treatment methods that are available for the individuals suffering from restless leg syndrome to use. Some of these alternative methods are the use of dietary supplements. However, supplements are not good enough as they do not address a very vital point; crossing the blood-brain barrier. There are those non-dietary supplements such as 5 HTP supplements. However, there has been debate in the use of 5 HTP and antidepressants in the treatment of depression.

Among the most common drug that is used to treat RLS includes requip. This drug is available in normal and extended releases. The tablets are taken orally and are very effective.

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    • Peter Geekie profile image

      Peter Geekie 5 years ago from Sittingbourne

      Dear progressivehealth

      I started my pharma chemical career with The Wellcome Foundation, pre the days of GSK. They were a very ethical company but with the passing of time i'm not quite so convinced. Certainly the formulation seems workable and would be worth talking to your doctor about.

      Thank you for a detailed article.

      kind regards Peter

    • teresapelka profile image

      Teresa Pelka 5 years ago from Dublin, Ireland

      Let me add, I don't believe in psychic pain. If pain is physical or physiological, whichever would be the preferred term, there has to be a physical origin.

    • teresapelka profile image

      Teresa Pelka 5 years ago from Dublin, Ireland

      I'd be careful with dopamine; just like the dispute whether epinephrine is really adrenalin - I'm staying by the latter term - infusing your nervous system with medication of this sort means introducing antagonists of natural neurotransmitters. Recovery is usually about five years, as for receptor exchange.

      Potassium and magnesium, along with calcium, sure can help muscle and nerve tissue. You wouldn't have Glaxo selling tomato paste, peanuts, and milk - and these should be recommended, whether there would be medication or not.

    • kj force profile image

      kjforce 5 years ago from Florida

      progressivehealth...very interesting hub.. " RLS " is a very common ailment, which sometimes is brought on by too much caffeine, insufficent Magnesium,iron and even dehydration.( always check with physician before assuming it is RLS)...massage before bed often helps, also recommended drinking coconut water is beneficial..I opt to exhaust all natural treatments before using Rx drugs..very well researched hub..thank you for bringing attention to this often ignored disorder...