May 4th
2008
3:42 PM
I spent the weekend reading about the development of Singulair. The early studies recognized that the first phase of the acute asthma response bronco-constriction was probably not caused by leukotrienes. They identified histamines and prostaglandins as the probable sources. I don't think that changed because the Singulair literature states that it should not be considered as a treatment for that. Leukotrienes were a source of inflammation caused by eosinophils and mast cells present in greater numbers (than normal) in airway tissue. So, it was beneficial to find a way to decrease that.
The cysLT1 receptor was identified as source of the signals that tell the cells to produce leukotriene. The receptor, a gene, consist of 337 (they think) amino acids. They modified a compound that would bind to that receptor thus blocking the cells ability to produce leukotrienes. This compound is very specific. It was formulated to bind to the "model" receptor. This compound will not even bind to cysLT receptor sub-types. (That is the good thing.) There is an enormous amount of research that discusses the genetic variability of the chemical reactions that occur in the leukotriene (calling it this for simplicity) pathway. We are also seeing that a number of researchers would like to use gene profiles to predict whether patients will respond favorably to different asthma/allergy drugs. ALL PATIENTS HAVE A RIGHT TO KNOW IF IT IS INHERENT THAT SOME PEOPLE WILL NOT RESPOND TO SINGULAIR OR RESPOND ADVERSELY.
There are many studies from the 1998 era that conclude that montelukast is not effective for everyone. Those researchers stated that it can be predicted that those people who are going to respond favorably will do that within the first 14 days or so. That conclusion would be consistent with a genetic component for efficacy and safety of Singulair. Those doctors concluded that those who did not respond within that time frame should not take Singulair for fear of harming them. That makes good sense.
The Italian researchers wanted to know if there was more going on than blocking leukotrienes in the action of montelukast. They set up a "test tube" study regarding montelukast, the cysLT1 receptor, and some t-cells that they selected. Why? Researchers always have something on their minds. They observed the death of these particular t-cells.
Montelukast is a quinoline. We basically know of quinilines and quinolones as compounds that were invented as broad spectrum antibiotics. They work because they interference with bacterial DNA so they cannot replicate themselves. Montelukast is a quinoline modified to bind with the cysLT1 receptor (a gene) and prevent that gene from activating. That's consistent with what a quinoline/quinolone does.
So what does montelukast do in blood plasma if it does not bind to the receptor because of genetic mis-match? (If montelukast does bind, then a chemical reaction has occurred and the liver will break down the by-products. Montelukast metabolized in 10-12 hours.) What happens if it doesn't bind? How long before it breaks down? Does it produce toxic by-products?
I want to know what happens to lymphocytes such as t-cells just because montelukast is a quinoline. Maybe nothing but what's up with the Italians researchers? I want to know if montelukast has the capability to interfere with lymphocytes who can clone themselves. That could be a good thing under circumstances when these lymphocytes are causing inflammation. But it could be a bad thing in the case of normal individuals with no problems.
I want to know if the bad side effects are due to the fact that the body has to break down and metabolize a quinoline that did not bind to the receptor for which it was created. The side effects of Singulair are strangely similar to what is observed in the quinolones such as levaquin. I have not as yet been able to compare montelukast as a quinoline to levaquin as a quinolone. I am hoping to find something on these categories. There may be no reason to worry that they cause similar damage. But frankly, I think that there is. There is some terrible chit happening to some people. The scariest is the neurological damage.
All of these questions would be in the everybody pharma knows to ask category. I don't know where the answers are. I haven't found them as of yet. Maybe there are no answers. We have to remember that Singulair and Vioxx were released in the same year. They have continued to be drugs under the current executive management of Merck. If the Vioxx marketing promoters had their ghost writers, why not the Singulair marketing promoters. The genetic component appears to be widely accepted but we haven't heard one thing about even that.
I think that it is sad that maybe the marketing of Singulair as one stop shopping for asthma/allergies may have destroyed the original concept. I really think from reading the original work that they knew that they couldn't engineer a drug for one size fits all. Everybody gets harmed when information is withheld.
Shame on the allergist who yelled at the mother who wanted to discuss issues. Does he know exactly who is allergic to Singulair and who isn't? Get him a dunce hat. Just because Singulair is marketed for allergies does not mean that you cannot be allergic to it. See the power of Madison Avenue? The ad agencies focus group these drugs to death. The ad agencies cleverly craft the product information. A good piece of legislation would be to prohibit consumer drugs ads.
-- By concernedcitizen | Reply | (4) replies | Private Message me
April 2th
2008
10:58 AM
Update: My daughter has been off Singulair for 3 months and is doing so much better. She is not having anymore nightmares, heart racing, anxiety attacks. No more itching, headaches, stomach pains, depression. She is so much happier now. She is 7 years old and acting like a happy child now. I am so glad that I took her off it in December. She is not crying and upset like she used to be. We could tell that she improved within one week and is still improving. Hope everyone else improves like my daughter has.
-- By mary1974 | Reply | (1) replies | Private Message me
April 2th
2008
9:33 AM
Here is some perspective for you all. I take Singulair and do well on it and in ACTUAL studies it has one of the safest safety records. Understand that post marketing reporting does not mean there is a correlation between the event and the product. Throughout the life of a drug the companies must disclose any report of side effects reported to them REGARDLESS of causality. A popular antihistamine that is OVER THE COUNTER also has suicidal thinking/behavior listed in its post marketing section. However, just because patients who had reported having these thoughts while taking the product doesn't mean it was a result of the product! Maybe they had a depressive personality and were also on multiple other medicines to treat that. You must look at the "Adverse Reactions, Warnings and Precautions" sections of package inserts to see the side effects that were actually seen in studies. You can die from ulcers derived from over use of aspirin or ibuprofen. Decongestants can throw off your blood pressure and these events are documented in actual studies! Listen to your bodies when taking any med. If you feel differently report it to your doctor.
These are all drugs people, there are potential side effects. There are also side effects to those "natural" over the counter remedies that are not nearly as regulated by the FDA or studies by the drug companies.
To anyone out there who has experienced side effects to singulair timed to when you started it, talk to your doctor, stop taking it and see if it goes away. Same advice for any product prescription or over the counter medicine. Side effects can be a combination of many factors (what other meds are you taking?) But understand for many people this product is the safest and most effective treatment for them. The FDA and Merck are reviewing all information to see if there is any correlation to the reporting. But singulair been around for about 10 years and prescibed to billions of people and is known to be one of the safer medicines out there overall.
In between the legitimate posts on this site I get the sense there is a lot of ambulance chasing going on. People looking to cash in on this big drug companies. We want drugs, we want them cheap and with no side effects which is not a reality. Keep stepping up the regulation and make the companies hire more lawers to protect themselves and jump through even more hoops and see what happens to the price and access to new meds. Even better, see how regulation has impacted the development of new medicines around the world (here's a tip, it will dramatically decrease). Drug companies certainly aren't perfect but which industry is?
Please, when taking any medicine over the counter, prescription or herbal supplement listen to your bodies to see if the potential benefits of the product outway the risks or side effects. Report any changes to your doctor.
-- By bachaman | Reply | (15) replies | Private Message me
March 28th
2008
1:59 PM
I have been crying for almost 24 hours now. I cannot believe what I am reading and hearing about Singulair. My son has been to hell and back again and again. I cannot say for sure the Singulair is the culprit. But after reading all of the other stories on this website, I am convinced it is a strong possibility.
My son is 11 years old. He has severe allergies and asthma. He takes many, many medications for this including Singulair. He as been on Singulair for about 8 years now (my best guess because he has been on it for sooooo long.)
My son was diagnosed with ADHD in pre-school. He has taken many medications for the ADHD, but none have ever done any good at all. We thought some of the medications even made things worse. Now, I'm not so sure.
After exhausting all the ADHD medications, our pediatrician sent my son to a psychiatrist and a counselor. The psychiatrist put him on 2 different antipsychotic medications. Again, neither one did any good and seemed to make matters worse. The psychiatrist sent my son to a psychologist to be tested for Asperger's. For those of you who don't know Asperger's is a high functioning form of autism. The psychologist ruled out Asperger's by diagnosed ADHD and Anxiety Disorder. He did not prescribe any medication.
For some unknown reason, I've only given my son the Singulair off and on for the last year. My son had the best year in school ever. However, his pediatrician was still not satisfied. He sent him to see another psychiatrist at Children's Hospital in Pittsburgh. We were told he is believed to have more than one disability. He is believed to have ADHD, Aspergers, Teurettes and a possible 4th medical problem that has not yet come to light.
We are scheduled to see a neurologist at Children's Hospital on the 15th of April to rule out any medical reasons for his tics. We see the psychiatrist again on the 18th of April.
I am so tormented by this recent news. Has all of these problems been caused from him taking the Singulair for so long? Although he has had his best year in school yet, he still has a lot of problems. Are the side effects of the Singulair permanent.
The other side of the coin is this: It is also very scary to watch my son not be able to breath. Asthma can also be life threatening. What is a parent supposed to do.
Also, I now don't know whether to keep these appointments that are coming up. I hate so much to put him through more. He has endured enough doctors and tests to last him a lifetime. However, what if it is not the Singulair and there is help out there for him that I am not aware of.
Please if anyone else has had a similar experiences e-mail me. I would love to hear from you.
God Bless everyone who has been through this kind of hell.
-- By foxhlam | Reply | (4) replies | Private Message me
May 7th
2008
1:02 PM
Hi, njcukett posted 2 days ago asking if anyone is still having abdominal pain after being off singuliar awhile.My 7 yr.old (on singuliar at least 3 yrs.) is still having pain.She also had bladder issues for the past 2 yrs.(Frequent dripping and urgency to void).This went unexplained by doctors.Over the past 6 weeks since she stopped taking singuliar,I have noticed a complete change in her stools.While on singuliar they had become grayish in color.She would have 2-3 of these movements a day.The color of her stools are now normal,but the lower abdominal pain is still present.So I am wondering if the pain is coming from the bladder, not the stomach.I am going in(without my daughter) to discuss this with her pediatrician next week.Singuliar also made her very anxious,do not want to add to that,by discussing this in front of her.For the people having abdominal pain,did the stools change while on singuliar compared to when off?Just curious.
-- By dtrzaski | Reply | (3) replies | Private Message me