In my mind the term “chasing the dragon” conjures up images of addicts and opium dens of times past.
But metaphorically the term alludes to the feeling that the next ingested dosage of a drug will result in a nirvana that seems and feels imminent and conclusive, yet upon consumption never quite yields the promised experience— leading to the desire for the next dose that still promises the same—thus chasing the dragon but never catching it. -Source: Wikipedia
As any hard charger knows, there are no biological shortcuts and that ultimately Mother Nature has a funny way of evening the tables.
In the pursuit of higher performance there’s constantly a balancing act between pushing the edges for immediate gain vs. the long terms gains that can be had via taking the longer and steadier route, and often times tolerance and addiction are just opposite sides of a coin.
This timely article is from our friends over at Smarter Nootropics. The article offers some great advice around how to responsibly and most effectively supplement nootropics as to minimize the downside and maximize your upside.
I’d like to thank the team over at Smarter Nootropics for providing a great resource to the nootropics community, head on over there to check them out.
Now onto the post –
Tolerance. It’s a dreaded word in the nootropics community. The idea that a substance you’re consuming only works on a temporary basis and through a number of biological adaptations, the substance becomes less effective over time. Personally, I find tolerance rather disconcerting and try to avoid it at all costs. This article is intended to inform you of the basic principles of homeostasis and tolerance while advising you how best to avoid tolerance with common nootropics.
Homeostasis is an important principle for understanding any biological system. Literally translating from greek as homeo “similar” and stasis “standing still”, homeostasis is the property of a system to regulate variables and keep them constant, or within a range.
Put simply, homeostasis is the body’s thermostat and the body is very smartly heated. As with a thermostat in a house; open the windows, the heater kicks on, close the windows, the temperature rises too high and the heating shuts off.
Common homeostatic mechanisms include blood pressure regulation, fluid balance, temperature control, hunger/energy balance and specifically relating to nootropics: neurotransmitter balance.
Neurotransmitter homeostasis can occur through a variety of mechanisms, including receptor downregulation, an increase in degrading enzymes (such as MAO) or a decrease in release of neurotransmitter from a neuron. The end result is that continued use of a substance can result in it becoming less effective over time. Essentially: The brain adapts and neurons desensitize.
Tolerance Can Become Addiction
A fairly grim point, but valid nonetheless. Take caffeine for example: Constant use of caffeine eventually results in habituation to its acute effects. It no longer gives you that energy you so crave. But taken a step further, you may find that you’ll need caffeine to simply feel normal.
Consider caffeine’s mechanism of action as an adenosine antagonist. Caffeine binds to adenosine receptors in the brain and by doing so regulates wakefulness and makes us feel drowsy. Caffeine crosses the blood brain barrier and effectively takes the place of some adenosine but crucially doesn’t send the “drowsy” signal. Essentially, caffeine blocks adenosine from performing its job and subjectively you’ll feel awake, motivated and energetic.
Over a long enough period, the body gets wise to this and up regulates adenosine receptors to compensate.
Within a few weeks the body has caught up to the deficit in adenosine and has a normal amount of adenosine binding to receptors. The problem now is that when you stop caffeine consumption, excess adenosine will bind to receptors, making you feel drowsier.
The end result can be that you’re now in a situation where you require the caffeine simply to maintain normal levels of adenosine binding in the brain.
With that in mind, it’s perhaps no coincidence that tea and coffee are among the most widely consumed beverages in the world.
Avoiding Tolerance: 3 Key Principles
The following principles are to serve as practical advice and minimize tolerance, where possible.
Take Regular Breaks
This is crucial. Listed below are cycling plans for various common nootropics including anxiolytics, racetams, nutrients and stimulants.
Use The Minimum Effective Dose
This principle is particularly relevant to stimulant use, such as caffeine. There’s simply no good reason to consume more than required. Aside from vastly speeding up tolerance, there’s a valid school of thought that hyperstimulated states aren’t really productive at all. Gauge how you’re feeling on the day and dose accordingly.
Time It Right
An extension of the minimum effective dose protocol: Save the compound for when you really need it. A good example of this would be using a stimulant before a large work project. If caffeine typically takes 30 minutes to kick in for you and lasts 3-4 hours, then line your schedule up to make sure you’re getting the best bang for your buck. You want your time with the compound to be as productive as possible, minimizing the need to redose.
Getting Specific: Which Nootropics and How to Cycle
Different stimulants carry different tolerance profiles. Generally speaking, I’d limit stimulant use to 3-4 times a week. Anything more and expect tolerance to creep in. Specific compounds include caffeine, modafinil, phenylpiracetam, nicotine and theobromine.
Nutrients, including Choline
As previously mentioned, I see no reason to cycle vitamin d3, omega 3 fatty acids, choline, creatine, or minerals such as magnesium. I view these compounds as simply providing the body with what it requires to function optimally. Think of proper nutritional supplementation as oil in the engine, rather than rocket fuel.
It’s debatable if racetams (excluding phenylpiracetam) carry any tolerance. My own firsthand experience suggests that they probably do and mixed anecdotal reports suggest the same.
For piracetam and aniracetam, consider a 4:1 ratio of 4 months “on” and a continuous month “off”. Gauge the effects with your month off and notice if there’s any difference.
For more potent and fast acting racetams, such as oxiracetam, pramiracetam and noopept, I’d consider using 4-5 times in a 7 day period suitable, or a more prolonged 3-4 week “on”, 1 week “off” ratio.
I’ve previously written about my experiences with CILTEP. It’s something I continue to use on a weekday basis. I have attempted a continuous 4 week run with the formula, but noticed a decline in effectiveness past 2 weeks. I like to use CILTEP 4-5 times in over 7 day period in order to remain sensitive to its effects.
Anxiolytics work by a few different mechanisms, each with their own tolerance profile.
Phenibut – The “king” of tolerance forming nootropics. While being an exceptional anxioytic, it’s also exceptionally easy to become tolerant to phenibut. The internet is littered with tolerance stories. Use phenibut no more than twice per week in order for it remain effective.
Picamilon – GABAergic, like phenibut, but far weaker. Consider a 2:1 schedule of 2 weeks on, 1 week off, assess from there.
Theanine – Tolerance would appear to be minimal if present at all. Consider 5:2 “on to off” ratio. I like to take weekends off with theanine though there are anecdotal reports that consistent use is fine.
Bacopa – My own experience would suggest tolerance is minimal. Given that bacopa takes 4 weeks to reach peak effects, consider a 3-4 month “on” and 2-4 weeks off cycle.
Wrapping it All Up
Tolerance with nootropics is real. But careful and considered use minimizes the risks. Regular breaks and proper cycling can ensure that you remain sensitive to the effects and that the compound stays effective for you.