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Pharma Sticky

Posted: Sat May 06, 2006 7:07 am
by ViewsAskew
This is the pharma sticky. This will contain information and links regarding drugs, side effects, etc.

Drugs to avoid

Posted: Sat May 06, 2006 7:08 am
by ViewsAskew
Many drugs are known to worsen RLS. Here is a general overview. For more specific info including names of specific drugs, please go to the links provided in this post. You can read several pages of posts regarding what other have found about worsening their RLS.

Antidepressants can worsen RLS, but it's hard to determine which will for any individual. Some people can't take any, others can take some but not others. The older tryciclics seem to be worse, however even some patients have had success with those. Before taking them, know that they may not work and you may have to try several ADs before finding one that will work for you.

OTC antihistamines almost always worsen RLS, though the newer non-sedating ones that are available through prescription usually do not cause as many problems. The OTC ones are usually some form of dipenhydramine (brand name Benadryl in the US). This is often in cold formulas and night-time sleep or cold formulas. Always read the labels carefully.

Antinauseants can worsen RLS. Many of them are anti-dopaminergic drugs. There are some available that do not affect the dopaminergic system and these are the ones you should ask for.

Antipsychotics of all kinds should be avoided.

The bladder control drug Ditropan (US brand name) has been associated with increased RLS for some people.

This is an updated post regarding drugs to avoid:

Medical alert cards you can order from the San Antonio RLS Support Group:

Medical alert card you can print on your printer from the So Cal RLS Support group: (it is on the opening page, Table of Contents)

Dose specific information about Requip

Posted: Sat May 06, 2006 7:17 am
by ViewsAskew
This was announced in May, 2006 based on results from a long-term safety study or Requip (ropinerole):

Baseline IRLS score averaged 22.1 with a range of 0 to 40

Mean dose was 1.9 mg per day; about 12% of patients got the max of 4.0 mg per day

Most adverse events were reported during the up-titration phase

89% of patients reported at least 1 adverse event. The most frequent adverse events were:
-nausea (37.2%)
-headache (18.5%)
-joint pain (12.3%)
-Nasopharyngitis, back pain, dizziness, somnolence and vomiting each occurred in about 10% of patients
-Most adverse events were mild or moderate in intensity
-10% of patients reported serious adverse events

8.4% of patients withdrew from the 2 studies due to adverse events ... 650050EAE0


Posted: Wed May 10, 2006 5:35 am
by ViewsAskew
A lot has been written here about augmentation (admittedly, much of it by me 8) ). I suffered from it tremendously, so my life's mission is to prevent it from happening to others.

Augmentation is simply RLS that happens earlier or more severely than usual. It happens primarily with dopamine agonists, however some new evidence suggests it may also happen with Ultram (tramadol). Dopamine agonists (US names) include Mirapex, Permax, Requip, Sinemet, etc. Rebound is also a similar problem, but it is when the RLS is suddenly much worse as the medicine is wearing off.

Here are links to past posts on how to recognize it and what to do about it.

And here is an article by Gamaldo and Earley that discussed it:

Before I write about what I learned about it, let me say that many doctors do not understand much (or anything) about it and they may just want you to take more and more of the drug. That is OK the first time, but if it continues to escalate, you are running the risk of permanently increasing your RLS if you keep upping the dose over a long period.

Here is information I learned about augmentation at the RLS conference in 2005. Dr Allen talked about it in 2004, and in 2005. They are not sure, but they think it may be less with long 1/2 life drugs, such as Cabergoline. However, he said there was no hope that Cabergoline will be approved in the US for treating RLS. They also think the patch will have a lower augmentation rate; it is still in clinical trials, however.

In terms of Mirapex, the studies show augmentation rates of 30%. Rates have not yet been measured with Requip, but they expect it is about the same as with Mirapex. To their knowledge only DAs cause augmentation. The word augmentation is actually a word used only for RLS! This is not a common medical term - I was surprised to hear that.

There is a new rating scale for augmentation, but they didn't give it to us. I think it may not be published yet. If anyone finds it or hears of it, please post about it. Their definition of augmentation is that there is
A. A shorter time for provocation
B. Length of rest shortens before it will start
C. Earlier onset

the real problem is that there is not consensus as to what to do. First, I will explain what was said at the conference. At the end of that, I will explain what Dr Buchfurer told me.

Att eh conference, Dr Allen said that when higher doses are needed suddenly, it is usually augmentation. It appears that it is hard for the doctors to determine if its augmentation of a worsening of your RLS - they most often assume it is a worsening rather than augmentation. Because of this, Dr Allen suggested that anyone experiencing worsened symptoms who is taking a DA should go through withdrawal from the DA for a week or so. Then it could be determined if the cause of the worsened RLS is actually augmentation, or because the RLS itself has worsened. He didn't recommend switching to another drug immediately, or to a different DA, as I have heard other doctors recommend.

This makes sense, but would be terribly hard to go through. Stopping a DA that is causing augmentation is very difficult and many people will not go through it willingly. When you stop it, the RLS intensifies for several days to a few weeks before going back to regular levels. I talked privately to Dr Allen about this, and he seemed to think that it could even continue to decrease for a month or more after stopping it, but within a couple of months, the level would have evened out and you wouldn't see any more decrease.

They also had a formula. If there is a rapid progression of RLS, you should:
A. check for GI issues that could cause poor iron uptake (bleeding, celiac disease, etc.)
B. Ensure no antihistimines are being taken
C. If no to both, then assume it is augmentation

He also said something about meds, like some antihistimines or dopamine antagonists, that cross the blood/brain barrier. These types of meds often cause problems for people with RLS. He said to check with your doctor before taking any meds that cross the blood/brain barrier. That is why the newer antihistimines are unlikely to cause problems - they do not cross this barrier.

Because of augmentation, Sinemet should ONLY be prescribed PRN and taken no more than 3 times a week. PRN stands for as needed. So this drug should never be taken daily by anyone. This eliminates problems of augmentation, as rates are 50-80% (different studies have found different rates).

Months after the conference, I talked to Dr Buchfurer about this. He indicated that whenever it was obvious that the person has augmentation, he stops the use of the DA and uses a strong opioid, usually methadone, to help the person get the rough period when you stop the DA. Then, once that rough period is over and the RLS has gone back to its "normal" amount, you can decide how much drug to take.

The gaping hole is what to do if you have just a "little" augmentation. Currently, most doctors do prescribe more of the drug to "cover" the increased symptoms or time period. The problem I have with that is when do you stop? My doctor did just this, and it became a vicious circle. Soon I needed the DA 24/7.

So, my advice is to call your doctor as soon as you get any signs of increased RLS and you are taking any DA (Mirapex, Sinemet, Requip, Pergolide, etc.). If your doctor wants you to take more, try that one time. If the RLS gets worse a second time with a short time frame, explain to your doctor that you would prefer to stop the DAs completely for a time period. Use a stong opioid to stop the DAs and stay off for a month. At the end of the month, switch to a different DA (for example, from Sinemet to Mirapex or from Mirapex to Requip. If it works, great. If it doesn't, then stop the DAs completely and don't use them for a long time and use one of the other classes of meds, such as the opioids.

Edited by author to add additional citations

Some Factoids about the Drugs We Take

Posted: Wed May 10, 2006 5:46 am
by ViewsAskew
I was going through my notes from the 2004 conference and happened on Dr Rye's slides about drug treatments and some other information about drugs and RLS. Here are some of the new things I learned at that conference. (This was moved from the New to RLS sticky. Seems more appropriate here.)

1. 80% of RLSers taking Mirapex and Requip do NOT have any side effects or have minor ones that don't affect them taking the drugs. Of course, that means 20% do. Many of those 20% are posting on this and other RLS boards, the other 80% post once or not at all and then live happily ever after (so to speak )

2. Requip and Mirapex are the best choices for PLMD at this writing (2005). Even a low dose can have a dramatic effect.

3. Requip and Mirapex can be substituted for each other rate of around 3:1 Requip to Mirapex and without tapering or titrating. (Some doctors say 2:1, others 4:1, so you may need to experiment.) So, if your standard dose of Mirapex was .5 mg and you wanted to switch to Requip, the experts say you don't have to slowly stop the Mirapex and slowly increase the Requip. Just substitute 1-1.5 mg of Requip the next time you take it.

4. Mirapex and Requip are enough different that the side effect profiles have little in common. So, if you have side effects you can't tolerate with one, try the other and there is a good chance are you won't have the same problems.

5. If you have experienced augmenation on two DAs, you should not try any others and stop them permanently. This is based on the RLS Algorithm.

6. Methadone is one of the safest opioids to take (not my words, but Dr Buchfurer), but one of the hardest to get.

7. Opioids used once a day, as most RLS sufferers take them, even oxycodone, carry almost no risk of addiction.

Posted: Sat Jan 06, 2007 3:57 am
by Hos
Something to consider if you're currently taking Permax (pergolide) or Dostinex (cabergoline). ... ryid=15233

Opiate dosing information

Posted: Tue Jan 16, 2007 3:20 am
by ViewsAskew
Here is some opiate dosing information:

For this link, you have to scroll down a little on the page to find the chart. Or click on the Analgesics (3. in the Primary class of RLS Meds table of contents).
Opioid Dosing Chart

Here is conversion equasion:

Oral: 200 mg codeine= 30 mg hydroCODone (what's in vicodin) = 7.5 mg hydroMORPHone (dilaudid) = 5 mg METHadone = 30 mg MORPHine = 20 mg OXYcodone (what's in percocet).

Posted: Fri Mar 30, 2007 4:11 pm
by Hos
Another big update regarding Permax: ... ns/tb/5357

Chantix and RLS

Posted: Wed Apr 18, 2007 9:49 pm
by chefws
I am a life long sufferer of rls, and tried to use Chantix to stop smoking with terrible results, so I wanted to warn people of it's actions.
Most sufferers take domamine antagonists (hmm, no spell check) and Chantix actually blocks the receptors, so the da's don't work.
I had no idea what was happening until I was reduced to 1/2 hr of sleep one night. I researched the mechanisms of how Chantix works, and found out that it was the problem. It was preventing the Permax from working, so I quit it immediately.
That was 2 months ago, and I am still having problems with the Permax. Due to the recall, I am switching to Requip, although I'm not excited by what I have read here on other threads. I dread the next few weeks of transition.
Just a heads up because I haven't seen any posts to that effect.

Posted: Thu Jun 21, 2007 7:07 am
by ViewsAskew
Here is a great chart, listing all the drugs that are approved or in testing specifically for RLS. ... proval.htm

Posted: Sun Sep 02, 2007 1:05 am
by RLS83
Thank you for compiling all this information - it is very helpful. :)

Posted: Thu Mar 06, 2008 6:29 am
by ViewsAskew
Here is a pretty interesting algorithm (different from the one at the Mayo CLinic) that gives dosages and stuff, too.

Posted: Thu Mar 06, 2008 6:58 am
by ViewsAskew
I found this article several years ago, then couldn't find it again when I wanted it! I just happened across it.

This was based on the review of patients taking opioids for RLS.

Since Susan couldn't get in, I'll guess others can't either, so here is the text:

Mov Disord. 2001; 16(6):1105-9 (ISSN: 0885-3185)
Walters AS; Winkelmann J; Trenkwalder C; Fry JM; Kataria V; Wagner M; Sharma R; Hening W; Li L
New Jersey Neuroscience Institute at JFK Medical Center Edison, New Jersey 08818, USA.

The medical records of 493 patients with restless legs syndrome (RLS) from three major centers were studied to determine the number and outcome of patients who had been treated with opioids as a monotherapy. At one time or another 113 patients (51 men, 62 women; age range, 37-88 years) had been on opioid therapy either alone (36 patients) or with opioids added secondarily to other medications used to treat RLS (77 patients). Twenty-three of the 36 opioid monotherapy patients had failed dopaminergic and other therapeutic agents prior to the initiation of opioid monotherapy. Twenty of the 36 opioid monotherapy patients continue on monotherapy for an average of 5 years 11 months (range, 1-23 years), despite their knowledge of the availability of other therapies. Of the 16 patients who discontinued opioids as a sole therapy, the medication was discontinued in only one case because of problems related to addiction and tolerance. Polysomnography on seven patients performed after an average of 7 years 1 month of opioid monotherapy (range, 1-15 years) showed a tendency toward an improvement in all leg parameters and associated arousals (decrease in PLMS index, PLMS arousal index, and PLM while awake index) as well as all sleep parameters (increase in stages 3 and 4 and REM sleep, total sleep time, sleep efficiency, and decrease in sleep latency). Two of these seven patients developed sleep apnea and a third patient had worsening of preexisting apnea. Opioids seem to have long-term effectiveness in the treatment of RLS and PLMS, but patients on long-term opioid therapy should be clinically or polysomnographically monitored periodically for the development of sleep apnea.

Posted: Thu Mar 06, 2008 7:07 am
by SquirmingSusan
Ann, that link brought me to a log in page. Do we need to register to read the article?

Posted: Thu Mar 06, 2008 7:18 am
by ViewsAskew
Hmmm - not sure. Maybe I registered at some time and don't remember. I got to it from a Google search....