imiquimod absorption into blood,  aldara absorption,  induced , metabolites, IQ Imidazoquinoline



Ordinarily, drug absorption issues relating to topically applied drugs would be of no great concern.  The  treating physician would be able to quickly understand the data surrounding the question and determine the possibilities for that drug reaching the systemic compartment of his patients body during applications.

But as this website clearly demonstrates, Aldara is not just another topically applied drug.  By 3M's own admission, Aldara/imiquimod is "UNLIKE ANY OTHER DRUG TO DATE" in that it's only mechanism of drug action  is one that  forces the immune system to induce a very dangerous family of 14-cytokines.  That's it!  Nothing more and nothing less.  3M calls it "ALTERING OR MODIFYING THE IMMUNE SYSTEM". 

Every time the patient applies Aldara to their body's, these 14-cytokines are produced.  According to 3M, each patient's immune system responds differently to Aldara and there is "NO WAY"  to predict the outcome for a  patients first time exposure to the drug.  Which means that while all 14-cytokines are induced, the quantity for each respective cytokine will in all likelihood never be the same in any two patients.  Some patients will have a mildly responsive immune response to Aldara presenting a potentially low level of induced cytokines while the more moderate and certainly the highly reactive immune response will present very high and unpredictable levels of induced cytokines. 

I believe that in some patients, such as myself,  their immune systems are so highly reactive to the drug action that the immune system is forced into uncontrollable  maximum production of many or all of these cytokines.   I have found 3M sponsored data that seems to certainly support this notion.

Where the "absorption issue" becomes so important is when we come to terms with how these cytokines, although induced and produced locally in and around the drug application site, begin to enter and travel freely throughout the body's blood circulatory system. 

There are basically two elements for concern taking place during Aldara treatment at this point. 

(1)  At application sites, cytokine production can reach high levels in the more reactive patients.  These cytokines can then easily and transparently migrate into the blood circulatory system where they impose their respective physiological influences on virtually every segment of the body, systemically.  This is when Mayo Clinic and others but not 3M declare that "OVERDOSE" occurs.  When these cytokines reach such levels to create "systemic side effects", such as but not limited to flu-like symptoms, the patient is experiencing an overdose of "drug action" which is much different than 3M's standard misleading policy statement which is that "overdose of Aldara is highly unlikely".  

Remember as we go through this discussion that although as misleading as 3M's policy statement may be, Aldara itself is not THE ROOT SUBSTANCE creating the problem at this point in treatments but rather the immune system is operating on MODIFIED OR ALTERED instructions as the result of Aldara drug mechanism.  Aldara itself is no longer needed nor required to sustain this "abnormal" production of cytokines at the treatment site.  As 3M states, "the immune system maintains this ALTERED OR MODIFIED state long after the Aldara is removed from the treatment site, something you probably did not know.  How long?  It depends again on the patients immune system and the degree of hypersensitivity reaction that occurs.

But remember that 3M ran "vaccine" studies which fundamentally rely upon the drugs ability to "program", if you will, the immune systems memory, permanently.  Otherwise, imiquimod would be absolutely useless in the context of developing a vaccine.  It only follows that given the known and admitted long term ability of imiquimod to permanently MODIFY OR ALTER the memory status of the immune system that some unfortunate users of Aldara, such as myself, WILL experience permanent and irreversible alterations of immune memory that sends them off into uncharted and heretofore unseen drug induced disorders many of which are autoimmune related making them very difficult to diagnose and treat.

(2)  Early on, I believe it was in the late '80's or early '90's, 3M was faced with the daunting task of how they would design the absorption features of Aldara to accommodate imiquimods inability as a single agent to absorb into skin tissue.  Of course, this is the first property any topically applied drug must posses before it can remotely be considered a viable candidate for efficacy or as a marketable product.  Ultimately, 3M discovered ways of using a special mechanical process coupled with an assorted use of non-active ingredients that turned Aldara as we know it today into an efficient highly absorptive drug.  At one point in time, 3M showed high concerns and reservations for the high absorption requirements for Aldara.   The hard durable surfaces of  genital warts, the first FDA approved use of the drug, called for Aldara to exhibit high abilities for absorption.  Unable to chemically control the absorption hazards for Aldara,  3M became increasingly concerned over the real possibilities for serious systemic side-effects and began to adjust the frequencies of applications in the recommended regimen for Aldara to control how long the drug remained on the patients body.   That time frame was determined to be 8 to 10 hours and wash it off. 

Unfortunately, few treating physicians adhere to this regimen because they simply do not understand Aldara drug mechanism and how dangerous it can be to step outside the recommendations on the use of this drug.

  According to their U.S. patent, 3M ultimately achieved 10% absorption and preferred that 15% of the active ingredient imiquimod be absorbed into skin tissue to achieve the desired efficacy for Aldara, in the treatment of genital warts. 

Today, 3M states that less than .9% (nine-tenths of one percent) of the imiquimod is actually absorbed during treatments with Aldara.  What they don't tell you is that this study was performed using ONE APPLICATION on "intact skin tissue" on the underneath  forearm,  on normal pristine skin tissue, of the college male test subjects.  Can you think of any possible use for Aldara on normal pristine skin tissue? 

Well, the facts are that Aldara will ultimately be applied largely into lesion type skin conditions where it will be in constant physical contact with blood.  BCC's for instance will always become open lesions sometime during treatment with Aldara, if not from the beginning of treatment.  I know this first hand.  Yet 3M admits in sworn testimony that NO TEST OR CLINICAL TRIAL was ever conducted on what clinically takes place when Aldara/imiquimod is placed in a human open lesion or wound such as BCC's.  It simply was never done or I think it may have been done and simply dropped from the reports due to what was learned.

Along with site induced cytokines migrating into the blood circulatory system as described in item (1) above, we also must consider the molecules of the active ingredient imiquimod which, too, will be migrating into blood circulation .  As this migration of molecules takes place, 3M documents reveal that when imiquimod is placed in normal samples of blood a much more abundant and robust induced cytokine activity takes place than they saw induced in skin tissue.  This is further supported by 3M's own pre-clinical trial data where the monkey achieved death by intravenous injection with an amount 1/30 of  the oral amount of imiquimod necessary to cause its death.   So, when these circulating IQ molecules and their metabolites begin contacting the highly reactive cytokine producing elements of the blood, systemically, an additional level of cytokine production can be added to the site induced levels and we now find a very alarming possibility for dangerous cumulative levels of 14-cytokines being constantly made available throughout the patients body to perform all sorts of unnatural and dangerous changes to the systemic wide systems.  3M tries in every conceivable way to prevent this knowledge from becoming freely available to the medical community and public.  After all, they have told the FDA,  and virtually all others that there is no reason for concern because very little absorption of the drug takes place during treatments and site the .9% absorption figure as their proof. 

Incidentally, 3M also states that this induced cytokine activity continues "LONG AFTER"  the imiquimod is gone or removed. I think this undeniably proves that this long term extended cytokine production in the absence of Aldara/imiquimod can only occur through imiquimods ability to artificially impose upon the immune system its ability to ALTER OR MODIFY the immune system memory both temporarily and possibly permanently, otherwise this 3M statement would have no meaning.


If item (1) and (2) above are allowed to persist long enough during treatments with Aldara some patients will, according to the experts, place themselves in the likely position of contracting autoimmune disorders in addition to other conditions.  I was told by my dermatologist to keep applying the drug into the open wound of my BCC treatment site regardless of how much pain or systemic side effects were taking place.  This is almost the standard for instructions in the field of Dermatology today.  In doing so, experts feel with certainty I crossed over the line of safety sometime during my 21-day treatment period and the results are what I have today some ten years later,  fibromyalgia, sjogrens syndrome, osteoarthritis, irritable bowel syndrome, celiac disease, deteriorating hearing loss, peripheral neuropathy, and Parkinson's, most of which share autoimmune characteristics.  I also have leukopenia (< 3,000) along with other strange CBC levels.  Every one of these conditions began within 10-days of going on treatment with Aldara and have become permanent conditions that I must now live out the rest of my life with, so states 3M.

To recap our discussion, I started out my use of Aldara on a nickel size BCC skin cancer near the hair line of my forehead and ended my treatment some 21 days later with everything in this list above.  Seems to me I traded a very non-life threatening condition for more than ten life-altering conditions that left me disabled at the age of 51, in the year 2000.