Over a year ago, I wrote an article called, Ibudilast Kicks Inflammation in the Ass. Since then, it has been one of the most popular articles to date on my website. I am going to summarize what I have learned since then, as well as share with my readers how to source this medication. I have received so many emails from desperate readers that are looking for this medication, that I no long have an interest in keeping it to my inner circle of subscribers. I originally offered links to a site that sold it once someone signed up for my newsletter. But I don’t want to continue doing that. If you’d like to know more about this medicine, why it’s being “fast-tracked” for diseases like ALS and Methamphetamine addiction, then please read on!
Back in May of 2015 I stumbled across a drug called Ibudilast. It is an anti-inflammatory drug mainly used in Japan to treat asthma. It is very selective towards PDE4 enzymes, but does display inhibitory effects at other PDE (phosphodiesterase) enzyme targets. Many people in America will know of one famous PDE5 inhibitor, known as Viagra. It came to the market because of its effect on bloodflow in smooth muscle tissue of the corpus cavernosum of the penis. It was originally developed as a blood pressure and angina (chest-pain) medication. Patients taking the drugs noted that they were having spontaneous erections. Drug companies saw these results and marketed the first erectile dysfunction drug and made a mint!
Varying PDE inhibitors have varying effects across the body. Many of them also cause nausea and emesis (vomiting), so their usefulness in daily medication was very limited. Ibdudilast worked very well as a somewhat selective PDE4 inhibitor that did not seem to cause nausea and emesis. But what’s more. Ibudilast reduces microglial activation in the brain, and because it crosses the BBB (blood-brain barrier) efficiently, and reduces microglial activation, it became a suitable drug to be tested for different ailments. What is microglial activation?
Microglia Cells Explained
Microglia are a type of glial cell located throughout the brain and spinal cord. Microglia account for 10–15% of all cells found within the brain. As the resident macrophage cells, they act as the first and main form of active immune defense in the central nervous system (CNS).
To put it simply. Microglia are immune system cells in the brain that can be overactivated sometimes. This microglial overactivation can causes people to feel sick, anxious, depressed, confused and demented. Microglia are the resident “innate” immune cells in the brain. When they get revved up, they cause a storm of quinolinic acid release. Quinolinic Acid activates NMDA receptors. These are excitatory nerve receptors and can, eventually, become so over-excited, that the cell dies.
So sometimes our immune system can get really ramped up, cause a spill-over of toxic excitation, and then ultimately cause the death of the cell. It sounds twisted, and it is. Our own immune system has been the culprit for many of the diseases we see today. In some instances, our immune system sees our own self as a target to be destroyed. I am putting this eloquently, and using a journalistic tone. A scientist might have arguments against it, and I will admit this is simply my best way of describing to the everyday reader, what happens sometimes when our own immune system goes haywire and attacks the very host it was designed to protect.
Many of the diseases we see today, such as Parkinsons, Alzheimers, ALS, and MS, are now thought to be caused by a disruption in the immune system. An alert message is sent, and soldiers are thrust onto the battlefield, and while they are shooting their guns, they cause damage in their wake. Think of it like this. Our immune system is still using shotguns to deal with intruders, when we wish they had lazer beams. And even then, sometimes we send the wrong message and the weapon of choice doesn’t matter. But for the simplicity of this discussion, I will present that at this time, our immune system possesses only the evolutionary equivalent of a 12 gauge shotgun. So if you send it into battle, it might kill the enemy, but it will also destroy other surrounding tissue in its attempt to eradicate the intruder. In many instances, this is acceptable. We can recover from the attack. Our bodies can rebuild, and sometimes replace the cells that were damaged. But eventually, with aging, and in some instances much quicker in certain disease states, our bodies can’t keep up with the damage that’s being done by our sheriff’s deputies.
That’s where drugs like ibudilast come in. They turn down the inflamed microglial activation.
And what else causes microglial activation? Methamphetamine use does, for one.
Methamphetamine is a popular addictive drug whose use is associated with multiple neuropsychiatric adverse events and toxic to the dopaminergic and serotonergic systems of the brain. Methamphetamine-induced neuropathology is associated with increased expression of microglial cells that are thought to participate in either pro-toxic or protective mechanisms in the brain. Although reactive microgliosis has been observed in animal models of methamphetamine neurotoxicity, no study has reported on the status of microglial activation in human methamphetamine abusers. The present study reports on 12 abstinent methamphetamine abusers and 12 age-, gender-, education-matched control subjects who underwent positron emission tomography using a radiotracer for activated microglia, [11C](R)-(1-[2-chlorophenyl]-N-methyl-N-[1-methylpropyl]-3-isoquinoline carboxamide) ([11C](R)-PK11195). Compartment analysis was used to estimate quantitative levels of binding potentials of [11C](R)-PK11195 in brain regions with dopaminergic and/or serotonergic innervation. The mean levels of [11C](R)-PK11195 binding were higher in methamphetamine abusers than those in control subjects in all brain regions (> 250% higher, p < 0.01 for all). In addition, the binding levels in the midbrain, striatum, thalamus, and orbitofrontal and insular cortices (p < 0.05) correlated inversely with the duration of methamphetamine abstinence. These results suggest that chronic self-administration of methamphetamine can cause reactive microgliosis in the brains of human methamphetamine abusers, a level of activation that appears to subside over longer periods of abstinence.
So methamphetamine causes this storm to erupt in the brain. In a way, a meth user is giving themselves a disease similar to MS of the brain. Eventually it causes such damage that cannot be restored and brain damage occurs, leading to psychosis, dementia and parkinson’s like disease states.
Ibudilast Puts Out the Fire.
Ibudilast, the asthma medication I first wrote about, puts out the fire caused by methamphetamine. So what happens when you give this drug to a meth addict? Well, hopefully, and some preliminary data suggests possibly, it cures the addict of their addiction. It’s currently being “fast-tracked” which means it’s being pushed quickly through FDA trials because it may save many lives of addicts, and may save thousands of families who are affected by the addictions wide-reaching damage.
So what I did was wrote a quick article, and during my investigation found a place that sells this medication online. A japanese online pharmacy, www.mimaki-family-japan.com.
They sell both “Ketas” and “Pinatos”. Ketas is the brand-name sold in Japan, whereas Pinatos is the brand sold in Korea. Both products are the same quality in my experience, and yet the price difference is noticeable. Also, customers are only allowed to export one box of the cheaper of the two. But I found that buying one box of each made my total high enough to qualify for free shipping. So I was able to get 200 pills shipped for a relatively cheap price compared to my usual supplement budget, which had grown out of control. I was curious about the effects of this drug though, because I felt often like I had a flu like feeling many days. A malaise of depression and anxiety that left me feeling “crappy” for lack of a better term. And it sounded like Ibudilast may help relieve me of this “sickness” type of feeling. So I pulled the trigger and ordered two boxes. It took quite a while to format my address properly to get the credit card payment to go through successfully. I also found that once it shipped, I really didn’t receive any updates. It just “showed up” about two weeks after purchasing. Not too bad, but it may throw some people off in America who are used to having constant updates, and quick shipping times.
But nevertheless, I wanted to share the above link with my readers who are looking for this medication, so they can order it for them, or their loved ones. As for me, well, I’m still on the fence about it. I really like the way it makes me feel. It relieves me of an inflammatory condition, which makes me feel rejuvenated during the day. Sometimes I would feel crappy and not want to do much. Fatigued and depressed, I would opt out on going out to the park or doing things with people. Ibudilast seemed to relieve my “allergic reaction to life” to put it simply. But it did also seem to cause some digestive issues. While research is being done to see if Ibudilast could be used to treat colitis and inflammatory diseases of the digestive tract, I seemed to find it irritated mine, gave me a bit of uneasiness over time. In short, the nausea and emesis that other PDE inhibitors were prone to cause, were starting to present to me. I felt a bit nauseaus after a while. I didn’t want to throw up, but felt like I was getting gassy and having digestion problems. So I stopped.
I have since reordered a few times. And it seems like it happens again and again. At first, I really appreciate the relief it gives me. I feel mentally and physically rejuvenated. But eventually I find it gives me some kind of digestive issue and I stop taking it. I am currently taking 40mg, which is split into two doses. I may back down to just one 10mg dose twice daily, or even just once daily, to see if I can get the benefits (perhaps a reduced benefit) without the side effects that made me stop taking it in the first place.
I have been writing Metabolic Alchemy for over ten years now. And very rarely did I ever get much feedback. For the most part, I would just write articles regularly, and every so often I would get a reply to one that wasn’t spam. But after writing my article about Ibudilast, I started getting comments and emails almost daily. My inner circle subscription was growing by the day. (sign up for the inner circle by filling in your email address at the top red bar on the site!) and most of the newcomers were mothers, lovers, partners, or people affected by methamphetamine addiction. I even had one person contact me who was one of the original participants in the methamphetamine study done in UCLA Berkley. I was quickly realizing that I had stumbled upon a drug that could help many people, and many people could not figure out how to get this medication while waiting for our FDA to catch up with the research that was showing it may be a cure for a disease that is so profound, no amount of side effects could eclipse the benefit of this drug.
So now I share with my readers a link to the site where I originally found it, and I hope that it helps anyone else who stumbles upon this article. You may not even be aware of how this drug could have helped you before finding it here. In any event, I hope people continue to respond in the comments on their experiences with this drug, and also share any relevant research they have discovered while looking into this medication. I look forward to hearing from you! Drop us a line and share the wealth of knowledge you have come across, or share your success (or failure) story with us so that we can all learn from others experiences!