My dosing theory for “scary” drugs (and a poke at the trashy values of the collective and how they affect me)

These drugs have two things in common; one is their incredible efficacy when used by rational, lucid people who want to live a full healthy life:

cocaine, amphetamine, methamphetamine, methylphenidate (narcolepsy, ADD, off-label depression)

morphine, heroin, codeine, oxy’s, opium, tramadol, buprenorphine (chronic pain, off-label depression, anxiety)

marijuana (sedation/stimulation, anxiety, pain relief, depression)

benzodiazepines, barbiturates (sedation, anxiety)

psilocybin (pain, depression)

The second thing they have in common is the difficulty getting a prescription for them because they are either illegal, or stupid people exist in the world; so instead of letting them voluntarily take themselves out of the gene pool like nature intended, the State, many moons ago, had taken upon its self the uninvited task of taking care of these dullards at the expense of my liberty and my right to procure the drug of my choice, in the name of some false “altruism” or “greater good” because maladroits get themselves into trouble with drugs (as if they wouldn’t without drugs); and somehow society would become a dangerous or less safe place otherwise, or some such nonsense.

It’s telling that, because we’re caught in this frame of nanny-statism and legalities, one of the main things drug researchers peel their eyes for, like hawks, are drugs that make us feel really good, too good, too soon. Fear of litigation is a reason we have “safe”, mediocre, usually inefficacious modern psychiatric drugs that have little value and crappy side-effects, yet are continually stuffed down the throats of trusting, half-witted souls, a few of whom actually get some benefit (bless you)… I wonder if visionary, progressive pdocs who have to dole out this junk feel any kind of guilt or frustration. I know that I would feel weary if I could not script, off-label, drugs like methamphetamine (desoxyn), laudanum (yes, it still exists in the pharm repertoire) or marijuana.

~But, I think there’s something else afoot here as well:

…”‘k, so you guys at MumsdrugCo have developed this drug that gets rid of depression. Right on; I could sure use it. Umm, can I try it? No? It makes volunteers in clinical studies too happy… so it’ll make me feel really good, and… we, don’t… want this… do we? ‘K, I guess you guys know what you’re doing… I suppose. Umm, I have to tell you though: all the antidepressants I’ve tried over the years have done nothing for me except make me feel worse. I felt better when I didn’t take them at all. I’ll tell you what did work very well, though; opium and dextroamphetamine; dextroamphetamine worked on an as-needed basis, maybe twice a week. Then I discovered that opium targeted as much of an extent what was wrong with me. Opium cycled on for a while, then cycled off for a month, then back on really does help me a lot.

“You say I shouldn’t do that? Why? I could get into trouble with it? Know something? I think you’re projecting; I think you could get into trouble with it because you would doubt yourselves in my situation. Know what else? I think, because you and the legislators who govern you don’t trust yourselves, you won’t let drugs through that could benefit so many smart people, and now we all have to suffer because of stupid people and your own self-doubt. And as usual, given the reigns of state authority, like any cop, doctor or politician, notwithstanding your fear of litigation, you feel free and qualified to impose your values upon me; and the things you value are more often than not, of little value.”

Jesus and John Galt wept.

~Certain patients who can’t take care of themselves or are not capable of thinking rationally or projecting plans for the future should follow the advice of their doctors only, and ignore the following…

…but for those of us who crave a happy productive life, “scary” drugs are, in my opinion, among the best for what ails rational people. Some get positive results from taking very small, scientific daily “lifting” doses, titrating up when necessary, then after a few months, tapering down and off for a period of time (maybe a month; maybe two); then starting again. I don’t think it’s in our interest to take any psych drug, pharm or not, continuously without cycling off (well, more serious cases like schizophrenia or bipolar might be a different story). The brain is plastic and in a state of constant homeostasis, and I think more harm than good results from a constant bombardment of exogenous chemicals… who do you want to be when you’re seventy?

…I would rather live a month or two with depression, knowing that I’m going to feel better again in a while when I resume dosing up, than take a chance that my personal chemistry hasn’t had a time of rest and a chance to get back to “normal”, as bad as “normal” might be (and who knows? maybe I’ll feel better drug-free for a while, or…?). I don’t want my neurons (at least) to be permanently twisted some day…

…so I think cycling on and off is the way to go if one doses every day. I’m in a cycling off period right now because, frankly, I think doctors are up their asses with daily scientific fixed dosing. I don’t buy into the theory that the body must take this smooth bombardment, on and on, even when the patient knows in their gut it’s time to taper off, at least for a while.

~So in one week I’ll be opiate-free, and will not take it for at least one month. I’ll keep you posted on how I feel during this time. It has not been hard to taper; I should say rather, it hasn’t been hard because I’ve had some great help from benzo’s for anxiety, trazodone to knock me for the night, and baclofen (an amazing wonder drug) for everything else; wow, this combo works well.

~Another dosing schedule is possible; if one prefers to not dose every day, dosing every three days, or twice a week can work too. It’s not “scientific”, in that the body doesn’t have a constant level of chemical within, but who can tell me that a doctor knows best what works for me if I achieve acceptable results taking a substance on an as-needed basis?… and besides, how do we know that it is not healthier to keep the body on alert and “guessing” what’s going to happen next, instead of on a predictable course of action that the body sees through, laughs at and compensates for?…

…so, when I start dosing again in about five weeks, I’m going to try this theory and let you know how it goes…

…I think we’re going to be pleasantly surprised.

~Now, if only these market products were available, unscripted, from legal vendors, would we finally be free to experiment openly and share our results with each other instead of having to skulk about on the net, like criminals. Imagine the added bonus of lower prices thanks to competition and no Organised Crime dictating cornered markets.

…oh well. I can dream for that day.

~Let me know what works for you. Feel free to talk about any drug used off-label for the last six months at least, and what your system is. I’m curious.

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Separation distress and the importance of valued people

I stumbled onto two interesting authors, Jaak Panksepp and Douglas Watt…

“‘Big Pharma,’ as big business, seeks antidepressants that may become billion-dollar blockbuster drugs. Accordingly, it may neglect drugs that are off-patent (e.g., buprenorphine) as well as those that only serve a small subset of the population. Many authors (ever since Valenstein, 1998) have argued that the pharmaceutical industry may be exercising an increasingly distorting influence on prescription and treatment landscapes for the whole of medicine in the United States. This may be particularly true in relationship to depression, where many depressed patients are never referred to psychotherapy and instead are only put on first-line antidepressant drug regimens under the simplistic aegis that depression is “just a chemical imbalance.” These trends take place despite evidence that pharmacology is often only partially effective in depression (see recent STAR*D reports: Rush, 2007; Rush, Trivedi, & Fava, 2003) and despite evidence that patients suffering from trauma-related depressions do quite poorly treated alone with psychopharmacology without psychotherapy”

 Far be it from me, an academically untrained but round-eyed acolyte of the big world, to feel at all qualified to take on the authors’ implication that depression may be the result of anything but “a chemical imbalance” though an initial “trauma” may have initiated the process, and the chemical imbalance following the trauma can’t be fixed wholly pharmacologically. But I’ll state modestly that some day soon, almost every state of depression, whatever the cause, will be cured chemically sans psychotherapy…

…psychotherapy definitely has a purpose… probably always will; intelligent people understand that they have subjective limitations regarding self-awareness, and some have an interest in resolving recurring, stunting issues, or simply gaining insight for the sake of growth with the help of trained facilitators. But some day drugs will blow away our depression, regardless, with remaining only a curious interest in why we do the things we do and think what we think, for the sake of treating ourselves and others better.

~But my little declaration is not the reason for this post. Jaak Panksepp and Douglas Watt really have their stuff goin’ on, and are speaking my language. My personal theory of depression (…depression not caused by an innate anomaly) involves three roots: an unsuitable industrial diet, inappropriate exercise (not enough and chronic cardio), and stressors, including modern stressors (pollution, lifestyle etc). In this piece, the authors deal with separation stressors leading to a “protective” state of depression (do I smell the pernicious stench of dynorphin again?).

Whether or not this thesis is correct, the thing that jumps out and reminds me is the importance of keeping one’s self as engaged and socially involved as possible. Clearly (if only for the production and cultivation of calming oxytocin, which is known to sustain opioid reward in the brain), the importance of maintaining and nurturing relationships with people we value and who give us value in return can’t be overstated in a world that increasingly creates and promotes options for insularity and “aloneness”.

Equally, one must have a healthy hierarchy of values…

…if not, being depressed and alone might actually be a better situation than being depressed with people who don’t elevate us… don’t challenge us to go higher, but erode our quality of life, sense of self-esteem and our quest for happiness. In this case, until one has redeveloped a healthy sense of worth through proper diet, appropriate exercise, a low-stress lifestyle, and insight perhaps helped by psychotherapy, I think sometimes we can wait until we are in a better state to nurture rewarding relationships with quality people…

…just relax, and be good to yourself first.

Refractory depression & kappa system over-activation?

Sometimes I wonder if Nature likes us much. She seems to hate to see nice people who deserve it in an unconditionally happy state. Sometimes I think that she thinks that we are still in the paleolithic, and really happy people are impractical idiots who don’t have the wit to perceive danger, so quickly weed themselves out of the gene pool before reproducing to their full potential… so she does something about it. She “helps” them…

…is happiness an anomaly? I know this question is beat to death and naive, and I’m being facetious. Considering modern hunter-gatherers, primitive localist cultures supposedly most in line with our “ideal emotional state”, one might believe that perfect emotional homeostasis is more prevalent per capita with them because they live in an environment with stressors more compatible with our evolution compared to industrial cultures, and maybe it is; but even with these Peoples, emotional states go crooked, and when they do, they don’t twist toward unbridled joy.

Our bodies have a disheartening way of efficiently maintaining a skewed emotional equilibrium that, for too many of us, leans away from euphoria. Euphoric people are rare, though we’ve all known that guy/girl who seems to be in a constant and enviable state of bliss, always living in a sunrise. Not much seems to trigger a bad mood in these people. I have to wonder if, woe not being within a normal state of equilibrium, this state of apparent irrational cheerfulness isn’t a defect as well, albeit a lucky and fortunate one (though the line between happy and manic might be thin; and how much of a cost in longevity might this state of chronic “up” incur? On the other hand, does depression produce as much or more longevity-sapping in a body?).

I’m looking at the role of kappa (κ) opioid receptors and dynorphin endogenous opioid peptides and the implications for depression from a faulty κ system. Have some refractory depressives been given the curse of an overactive κ system? If so… shit. But, if so, despite the overwhelming complexity and interaction of our amazing/intimidating biology, maybe this is a good enough place as any for a depressive to start looking for some long overdue answers.

There is a world to know and I’m not getting too much into κ agonism/dopamine; dynorphin links with/CREB/NMDA receptors; the fact that dynorphin is produced in different areas in the nervous system with various functions; other neurotransmitters; hormones like prolactin or enzyme connections yadayada and will mostly be ignored here. It all turns into an overwhelming mess and would just numb the mind of anyone who isn’t a geek. Hell, I’m feeling numb just writing this paragraph…

…I just want to know the kappa system’s role in depression and how to stop it.

κ receptor/dynorphin overactivity is implicated in depression. Apparently Nature in her often disappointing wisdom has forced us to prevent, in her opinion, an irrational and self-destructive state of elation (yay. thanks a lot). I don’t think we can cure an imbalance at this time, so I’d be happy enough to just control it… somehow. And since I believe that happiness is our birthright, I think it behooves me to search for a way out of this kappa mess and fight back any way I can… screw this

Dynorphin is a varying group of opioid peptides that act as neurotransmitters. Dynorphin has the strongest affinity, and is the primary peptide, for the κ receptor. It is also a very potent endogenous opioid pain-killer. Its other functions deal with learning and memory, emotional control and stress response. The problem is, unlike its relatives endorphin and enkephalin, it doesn’t make one feel good; Quite the opposite, actually. A protein called CREB activates a gene that makes dynorphin. CREB triggers this “down” by increasing dynorphin… …and stress/pain triggers the whole cascade; no stress=no dynorphin release/kappa receptor overactivity=no “down”.

Opioid peptides endorphin and enkephalin release dopamine by disinhibiting dopamine pathways and help to make us feel good. Dynorphin doesn’t like us to feel good, so inhibits dopamine release (as do kappa receptors). In fact, dynorphin inhibits dopamine more and more with repeated illicit drug use, so would rather we overdose on drugs than let us feel good.

…stupidjerkdynorphin.    ;(

So it seems that there is a mood balancing act between dynorphin and endorphin/enkephalin.

To be fair, maybe part of the role of the kappa system is involved in learning to avoid certain situations, as if to condition one what to not do, via unpleasant stimulus; [eg: rodent bites… “ouch”… kappa activation… “I feel depressed. I’m never doing that again.”] …Well, who knows? ‘Tis but a theory. And maybe κ activation makes one numb, pain-free and “down” as a survival mechanism; possibly as a way to force lucidity and introspection and help one deal with a problem in a bad situation. Speculation, I know.

So, it seems that a goal for some depressives may be to find a relatively safe method for blocking dynorphin (or whatever else may increase dynorphin activity; perhaps CREB, for example), and thus put to a stop its well-meaning but apparently misguided effects. Learned helplessness is another negative side effect of kappa overstimulation, no doubt partly because dopamine, our driving, motivating neurotransmitter, is inhibited; disinhibition would go a long way to fighting depression. Also, blocking dynorphin allows glutamate, an excitatory neurotransmitter involved in learning and memory, to be released and restore functional plasticity in the hippocampus, reversing the phenomenon of learned helplessness…

…as well, non-pharmaceutical ways to reduce stress cannot be stressed enough: relaxing enjoyable activities that produce a somewhat meditative state and help to take one out of one’s self for a while really do work. I’ve found that relaxation through the senses (charcoal burning resin like frankincense and myrrh for smell, low lighting and a warm atmosphere for sight, meditative music for hearing, caressing and sex for touch, slowly eating good whole food for taste) work well for the short-term, like at home after work. Absolutely worth it…

…but, for god’s sake, don’t start taking downers like benzo’s to try to control stress/kappa to achieve the desired effect. Jeez, the last thing we need is a dependency on these things, which are the worst, in terms of physical addiction complications… really, I would rather be hooked on opies than benzo’s any day.

~Thus, buprenorphine shines its beacon of hope once again. It is not only a partial agonist at the Mu (μ) receptor (which produces a much valued non-euphoric state for therapy), but is also a κ antagonist, which effectively blocks dynorphin from κ receptors and creates a non-depressive state. Bupe may not only be just the thing for some with endorphin deficiency syndrome, but may also help people with a skewed dynorphin/κ system or even, perhaps, general depression and dysthymia.

*****

Btw, if you think I’ve missed something, please feel free to comment for everyone’s benefit.

A strategy for EDS relief

‘K, so you took the “Do you have EDS” test, are pretty sure you need opiate therapy, have read the Recommended Posts, and are contemplating going to your doc looking for opiates. First of all, good luck with that, and if you’ve got a silver tongue and have managed to wheedle a long-term prescription, let me know; maybe you and I can go unicorn hunting some time and sell one to a zoo for some serious cash.

The only way you’ll legally get what you’re looking for, if you get it at all, is if you arm yourself with your own documented drug failure history and printed opinions from experts and primary studies from the web.

If you’re a virgin, you have to start from the start. The first thing to do is get yourself diagnosed. If you’re truly depressed the doctor will see it clearly as soon as you walk into his office and start talking. EDS sells its self, for sure.

Next, start going through the standard on-label antidepressants. Remember to give these meds a chance, and at the same time keep in mind that it can take months for meds to cease working, or adverse effects to develop, after a time of efficacy. But if you find a med that actually does the job, thank your particular magical sky fairy for your good fortune and get on with life. You probably don’t have EDS… …otherwise, other tactics must be employed.

Take the meds your doctor prescribes. Start keeping detailed records of types and efficacy. Make sure that they are clear and lucid, because if these drugs don’t work, you want to be taken seriously when eventually asking to go off-label for opiates. Sertraline (Zoloft) and fluoxetine (Prozac) are standard SSRIs and will probably be scripted first; so if the doc scripts these, try one or both. If they don’t work, go on to one or two SNRIs. Venlafaxine (Effexor) is standard and will probably be the first of these. Effexor has a unique profile in that it has somewhat of an opioid profile, though what that really means for us, I have no idea. Effexor has also some hellish side effects and withdrawal symptoms; I had a particularly nasty time with this drug (though I won’t go into my bad experience with the carnival ride of ADs. I don’t want to bias your perspective).

Bupropion (Wellbutrin), an NDRI, might be the next choice, then maybe something different like trazodone and on and on. Try to get through quite a few different types, and include some old-school ADs like the tricyclics and MAOIs. If these don’t work, perhaps suggest going off-label and trying something like lamotrigine or amphetamine. Again, if something works for you, breathe a sigh of relief and get on with the business of living. If not, at least you’ve kept meticulous records, eliminated possibilities and narrowed down your options and diagnoses… you can now make some choices and think about opiate therapy.

I recommend going to a doctor who will read your research and drug history and listen with interest and sincerity. You should be able to get a good read on his attitude right from the start; and if he isn’t into it or is an opiate dumdum, maybe tactfully ask him to refer you to someone less timid, or find someone yourself.

In my opinion, the first opiate used should be buprenorphine. It is a legal opiate with an interesting profile of action used in withdrawal therapy and is becoming relatively popular as an off-label antidepressant… if you can find a willing doc. Also, despite my reservations, low dose naltrexone (LDN) seems to be having a good effect on some depressives, though I wonder how much of this is placebo. Nevertheless, if bupe doesn’t do it or you can’t find a doc to prescribe, it can’t hurt to try it, and who knows? it might just be the ticket.

However, if everything has been done under the sun and you haven’t found relief, you might have to look for shade under the big guns. This is where the full agonist opiates/opioids come in, and where the adventure, for better or worse, begins. There are a few ways to procure opiates; some legal, some not so much, but one can with some effort find them (my blog gives some ideas). There doesn’t seem to be much difference in efficacy between opiates, though codeine doesn’t like me too much. As well, I have made it clear in this blog that when dosing, the object is to achieve relief without a shred of the nod(!). Again, if one goes into nod territory, one goes into drug abuse territory and the whole raison de plus gets shot to hell…

…don’t do this…

…just don’t.

I refuse to acquire a guilt trip because my good intentions get ignored and someone’s life goes down the tubes.

So just don’t do it. Don’t turn a potential gift into a curse.

~There is one fairly sure way to get what you’re looking for without riding the med-go-round; if you’re already addicted (and really, how many opiate abusers aren’t simply self-medicating depressives?) and don’t have the will to stay out of the nod, you can go into methadone or bupe therapy. This will help you get back on track and focus on life because you don’t have to worry about scoring and fixing, your jones is satisfied without the obsessive distraction of euphoria, and both bupe and ‘done have a fantastic anecdotal efficacy for depression; in fact, if going into ‘done therapy wasn’t such a pain in the ass, it would be my first choice above bupe, despite its troublesome half-life. And if you’re not addicted, you have to be pretty desperate for answers to try this approach and lie; but, well, who am I to judge; no one should be dictating what drugs an adult can take anyway… bloody patronising…

…which brings me to the downside of this approach. Titrating off these drugs can be more painful than heroin(!), and odds are, this therapy will become part of your medical records (which might create a different perception than scripting opiates simply for depression); also, methadone therapy requires a daily trip to the clinic which inconveniently cuts into one’s day.

Whatever you do, study and read, read and study, weigh the pros and cons and be honest with your motives. If you make your life your highest value, the choices you make should keep you on the right track.

Good luck to you…

Opiates: why do I come alive? Why do you fall asleep?

My dad is pretty much a down the line straight shooter. He’s fairly conservative, so a reliable source of uncoloured opinion. One evening we were visiting and he mentioned that he was in pain. I can’t recall exactly what it was, but I think it might have been either his shoulder or a pulled back.

At any rate, I offered him a cup of liquid joy to ease the pain, and he accepted with slight trepidation. He was cautiously curious to know what opium was about, and quaffed the vile draff in as few hoists as possible…

…I’d been immersed in some computer stuff and had forgotten about his situation for a while, until I glanced his way and noticed a very passive, inanimate face where, about three hours before, a lively one had been. I chuckled and asked how he was feeling. He replied without expression, “very loose”.

He was obviously pain-free…

The next day I asked him how he’d liked it. He didn’t, really. It made him tired and kind of out of it, and his motility had slowed right down. I had noticed the previous evening that he wasn’t really enjoying the experience. This is curious from my point of view because he is an indefatigably sanguine and optimistic guy. One would have thought that a dose of O would send him into an even more pleasant state. But this wasn’t the case at all.

~Modern doctors and researchers have been pondering this difference of effects between individuals for decades. The question revolves around why a disproportionate number of addicts and prescribed depressed users come to life when opiated, while most non-addicts, who seem to have a take-it-or-leave-it attitude toward opiates, just simply don’t. They, like my dad become either tired and fall asleep, or feel unwell.

There are theories about why this is, and EDS seems to fit in nicely. I know that I come alive with each daily dose. I feel motivated and engaged; I have a drive to produce and succeed, a trait shared with most normals, and one that disappears when I don’t dose (maybe the endorphin-dopamine connection that makes normals productive and engaged is mimicked in depressives when exorphins are taken in, thereby kicking otherwise latent (?) dopamine into action). From what I’ve read, many with a disinterested view of opiates, seemingly without endorphin deficiencies feel unproductive, warm and cocooned, detached and apathetic with a sense of lazy well-being, though sometimes depressed when using for pain by doctor’s order; in a kind of cloud, disengaged from others. It’s funny to me… I simply don’t have this experience aside from some nice warmth. Maybe I’m not interested enough in euphoric doses to reach this state, but the few times that I have experimented and gone on the nod and “knew” that I had taken more opiates than my body required, I simply fell asleep. Frankly it’s boring, a waste of time and product, feels unnatural, and I don’t bother.

All of this conspires to so far convince me that many if not most chronic opiate users specifically seek this drug for a reason. I think we EDSers are indeed feeding our brains as best as we can with our primitive flower chemicals and acquire effects that lead to the typical behaviour that normals experience. I think I know this objectively, because I connect, and fit in with others around me in a way that does not happen when I’m not opiated. Apparently people don’t have the impression that I’m “different” from them. As well, no one thinks I’m high because, essentially, I’m not…

…this is interesting too. An EDSer on O doesn’t seem inebriated compared to a normal. The reason seems obvious: while a normal is adding opiates to a brain with normal endogenous opioid function/levels, an EDSer seems to be “topping up” his dysfunctional/low levels. I have no idea if this is correct, but I’ll eat a bug if it isn’t.

~The web is filled with anecdotes from John/Jane Q regarding the energizing effects of opiates on depressives (the experience of people on this bupe site being a concentrated example). As usual, I hope for investment and research into this, because an educated self-medicator who is rationally hooked on O is in a much better position than otherwise…

…it’s long past time.

Buprenorphine: the first choice

If I had a choice, I would use buprenorphine. But because of the stupidity of the nanny state, and the fact that I live in Canada and can’t have access to it, I have no choice but to use less desirable opiates; opiates that, because of their very nature, provoke a euphoria that one doesn’t really get from bupe; a euphoria that induces a reward (I won’t say “craving” necessarily; I never crave) that can be an unwanted and unnecessary distraction from daily life.

Bupe is the first choice for a few reasons:

~Less reward. Although not nonexistent, the euphoria that druggies seek is much less with bupe, and largely disappears in a short time.

~Because there is less reward, bupe has a somewhat less potential for abuse.

~A patient can get a prescription, as with less governed drugs. Unlike methadone, and the daily clinic routine, there is much less hassle with bupe and governing of the individual by the system.

~Bupe is a legal opiate, so one can avoid the hassle of the underworld, buying poppy pods or script drugs without a script online, or growing flowers (unless of course one likes growing these incredibly beautiful flowers).

~Kappa receptor overactivation may be implicated in depression. Because it is a relatively potent antagonist at kappa, much more specific than regular opiates, bupe is in a unique position.

~Because it has partial agonist properties at mu, tolerance to the drug is built up very slowly, if at all.

These are compelling reasons for the state to legalise bupe as a legitimate antidepressant. This pisses me off, but perhaps one day I’ll be able to stop swilling my poppy powder and get some pharmaceutical-grade relief. Whether or not “society” has a paranoia regarding opiates doesn’t mean two shits to me. I am an individual. I am sovereign, and owe absolutely nothing to the collective if I’m not commiting violence or theft.

Yeah, I know this sounds like a libertarian rant, but when something is effective for what ails one, and the government won’t deign to allow the use of the effective agent, one can’t be blamed for shaking his head (and fist) at the no-win situation.

Oh well… maybe some day.