We have a lot of learn and should never be closed minded. We should always listen, observe, and think. We don’t know everything and never will.

This is the description of the patent for a chemical structure very close to montelukast.

” The compounds of formula I have a good activity on the 5-HT.sub.5A receptor. Therefore, the invention further provides methods for the treatment of depression (which term includes bipolar depression, unipolar depression, single or recurrent major depressive episodes with or without psychotic features, catatonic features, melancholic features, atypical features or postpartum onset, seasonal affective disorders and dysthymia, depressive disorders resulting from a general medical condition including, but not limited to, myocardial infarction, diabetes, miscarriage or abortion), anxiety disorders, (which includes generalized anxiety and social anxiety disorder, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, psychotic disorders (which includes schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and other psychoses involving paranoia and delusions), pain (particularly neuropathic pain), memory disorders (including dementia, amnesic disorders and age-associated memory impairment), disorders of eating behaviors (including nervosa and bulimia nervosa), sexual dysfunction, sleep disorders (including disturbances of circadian rhythm, dyssomnia, insomnia, sleep apnea and narcolepsy), withdrawal from abuse of drugs (such as of cocaine, ethanol, nicotine, benzodiazepines, alcohol, caffeine, phencyclidine and phencyclidine-like compounds, opiates such as cannabis, heroin, morphine, sedative hypnotic, amphetamine or amphetamine-related drugs), motor disorders such as Parkinson’s disease, dementia in Parkinson’s disease, neuroleptic-induced Parkinsonism and tardive dyskinesias, as well as other psychiatric disorders and gastrointestinal disorders such as irritable bowel syndrome (WO 2004/096771). ”

******

http://www.freshpatents.com/2-aminoquinoline-derivatives-dt20080403ptan20080081907.php

Jack2 - Thanks for your response, which was interesting and informative.

It’s a somewhat arcane point, but it raises a question related to our Michigan preemption law. One clause notes that preemption does not apply if the labeling of a drug in question is not in compliance with FDA regulations at the time of sale. Even if a Dear HCP had gone out, the backlog stock might well be misbranded in that sense.

More generally, I am assuming there is often a considerable amount of stock limited only by expiration dates. And thus, despite whatever is learned via detailers or other communications from the company, it sounds possible that months could go by in which misbranded drugs are dispensed.

For allergic rhinitis it is - at best - a third line drug. Intranasal steroids are recommended in most every set of guidelines as having the greatest efficacy for allergic rhinitis symptoms. If used properly - and there is a correct way to spray these into the nose - they are extremely well tolerated and highly effective. There are only a few patients/conditions in whom they you should not be used. After that, there are less-sedating antihistamines. Yes, there are histamine receptors in the brain too, but some products have minimal/negligble brain penetration (fexofenadine is probably the cleanest from the CNS perspective - it is also true that the original antipsychotics led to the first antihistamines).

You can “treat” allergies by avoidance, and minimize the symptoms with nasal saline sprays/irrigation - if you want to go all “whole-grain” on the issue. There is always immunontherapy - though there is not evidence for the “allergy drops” which some advocate.

For asthma, monetlukast’s role (accoring to the NIH-NHLBI National Asthma Education and Prevention Program’s Expert Panel) is pretty constrained as well. In this situation it may be an alternate treatment (categorized along with cromolyn, theophylline, etc.), but it is specifically not a preferred controller treatment for children or adults. It may be a useful adjunt treatment along with regular (daily) use of an inhaled steroid in children or adults. However, in adults the first adjunct treatment should be a long-acting beta agonist. (This makes Advair and Symbicort second-line agents. This is still true even if Advair has been very successfully marketed - it still is an asthma controller with a “black box” warning relating to the disease it is supposed to treat.) The data aren’t there to make recommendations in children on whether or not montelukast or an LABA should be used as the best adjunct.

Montelukast use alone as an asthma controller is associated with higher rates of asthma exacerbations as measured by rescue inhaler use, steroid use, etc. The studies I’ve seen show a higher financial and patient outcome cost with the use of montelukast compared to inhaled steroids.

Don’t missunderstand, there are still problems with getting paitents to use any asthma controller with regularity. Some argue that montelukast offers an advantage due to once daily oral dosing. In a study of adherence, there were in fact more missed doses of the twice daily steroid. However, when the data were examined for missed days of therapy, montelukast. So even with imperfect adherence, paitents with inhaled steroids still had more days receiving some controller treatment than did the montelukast patients.

I’m not really sure what to say about the exercise-induced asthma indication, except that generally if a patient with asthma needs a controller for exercise-induced symptoms, it is a good bet that there is some unappreciated persistent symptoms. If so, this would be better treated with an inhaled steroid.

So that just leaves a little niche for montelukast - It is good for the odd syndrome of nasal polyposis, aspirin/NSAID induced bronchospasm/sensitivity, and urticarial conditions (which also require the use of other agents). Oddly, the product does not have any indication of which I’m aware for any of these conditions.

You will note that montelukast is one of those products which proves my rule of DTC advertising. This is a rule I share with patients - If it is advertised on TV, it must not be that good. If it were that good, the company would not need to advertise it.

I’m not saying that montelukast doesn’t help some people. I’m also not saying that it is a bad drug. But I am saying that this drug is successful more for it’s marketing than it’s clinical benefit. Of course this is true of many drugs.

I will remain (as always) skeptical about this possible link, until there are more data available. But in truth, I don’t think even a definite link will have much effect on sales of montelukast. The marketing (or Kool-Aid) has been very good. As we used to say: “strong work” for Merck.

My original comment was also directed at Pauls “all drugs have side effects” comment.

Now, on the above quoted statement…how does that time period of testing in anyway convert to real life use? Singulair is prescribed for allergy seasons…much longer than 1 week, albeit at lower doses. Could it be that at the “recommended dose” over a normal use period allowed the brain barrier to be crossed, something that would not have shown in such a short term trial.

I guess that means that the antidepressants have been so perfectly studied that it is time to pull them from the market. After 20 years of no benefits and all risks. I also remember reading that the antihistamines are related to antipsychotics and antidepressants.

I guess it is too much to ask for some PhRMA sympathizer (apparently) like Paul to care if people die from a drug.

When I took Zoloft and complained of becoming homicidal and suicidal on the drug, I was told to take more of it, and then again more. Then Zyprexa. Luckily I kicked that killer drug and my shrink and OBGYN to the curb.

You can’t trust anything from PhRMA and nothing ever fails to surprise me. I don’t think up to this point that the drug label for Singulair said anything about causing suicide, so how were people supposed to read the label and know not to take it?

It’s all about running through a field of flowers without allergies, not about overcoming depression, so nobody would ever think “Gee, maybe my suicide attempt was because of the Singulair” up until the time at which people begin to realize that PhRMA is full of it and will not raise an eyebrow if a clinical trial results in a few deaths, or if they notice them in the MedWatch system either.

JIM: For the updated labels the company needs to send out the updated label practically immediately (a matter of days), but the pharmacy won’t get it until they need to reorder from the wholesaler, and the wholesaler will first need to deplete their stock with the existing old label. I also doubt the pharmacist will actually read the new label or notice the change.

Ironically, or at least in contrast to what people here might think, a label change that does not necessitate a dear doctor label, will probably get out fastest through a sales rep compared to any other channel.