Paraxanthine

When it comes to drugs less is more

I’m a chronic insomniac. At times when my sleep schedule has gotten bad enough that I’m falling asleep at like 6am I’ve generally fixed it by shifting it to be 7am, then 8am, etc. until it wraps around the other way and I’m going to sleep nice and early. This is to say, insomnia sucks. From times in my life when I’ve been sleeping better it seems helpful things are: exercise constantly, take lots of walks outside during the day, and don’t sleep alone. These are all somewhat extreme lifestyle interventions which are easier said than done. A much easier low effort intervention is drugs.

Unfortunately the drugs to knock you out produce low quality sleep and are all-around nasty. I have occasionally used them to reset my sleep schedule from like 3am to more like 11pm by using them a few nights in a row, which they work great for but using them for more than that is dodgy. For me at least diphenhydramine works just as well for that as anything else.

Several years ago I decided to try keeping myself awake during the day so that I’m more tired at night and can hopefully sleep better as a result. As it happens I’m horribly sensitive to caffeine, so taking that in the morning keeps me up all day. This has been working reasonably well for me for several years, specifically making a single Nespresso every morning. The best tasting version in my opinion is using official Nespresso brand pods with an Opal machine, but that unfortunately seems to extract a bit too much caffeine for me.

Nothing particularly notable so far, this is roughly the same routine as about half the human race and if anything I’m in the minority only taking it first thing in the morning. The problem is that even doing things this way still doesn’t seem to completely wear off at night. So I’ve done some digging on possible alternatives and recently found one which has been working well for me.

Caffeine has a half-life of about 4 hours with some variation between people. It then mostly gets metabolized into paraxanthine which has a half-life of about 3 hours. The small fraction which doesn’t gets metabolized into other things with half lives of about 7 hours. All the immediate metabolites have similar effects to caffeine itself. The obvious question given this information is, if you want it to wear off faster, why not just take paraxanthine? This is what I’ve been doing recently, and it seems to be working great. I’m still waking up in the middle of the night sometimes, but less often and I’m falling back asleep more easily. My total rest time seems to be a better and I feel noticeably more awake during the day. The effects of paraxanthine are very similar to caffeine but a bit less jittery. Apparently it also has less health risks than caffeine does, but those are minimal to begin with. Paraxanthine isn’t regulated as a drug and is something you can just go buy.¹

You might be wondering if paraxanthine is so great why have you never heard of it before? It turns out that oddly enough it’s very difficult to produce and only came on the market a few years ago, and it seems at the moment there’s only one company actually producing it. As a result it’s still too expensive to put routinely into energy drinks and the like. Not coincidentally, caffeine is toxic to most animals. Our livers just happen to be able to make a super special enzyme which can demethylate it resulting in paraxanthine. I’m not clear on this is literally the case, but the current production method involves something along the lines of taking the gene for producing that enzyme out of a human, implanting it in a bacterium, and using that to make the enzyme which is then used on caffeine.

An unrelated chemistry hack I recently came up with involves simethicone, which I take regularly because it helps with the symptoms of lactose intolerance. Simethicone is borderline for what should be considered a drug: It’s an anti-foaming agent which helps the gas get out of your system sooner rather than later.² Seemingly unrelated to this when I’m reducing a sauce I like to do it at a higher rather than lower temperature to make it go faster. This requires you scrape the bottom of the pan every few minutes to keep it from burning but works great. The problem is that if you get the temperature too high it causes the sauce to bubble up (or water if you’re boiling that to make pasta) and then get out of the pan and make a mess. It turns out simethicone works great for this: Add a pill to the sauce before you start boiling it and it will get absorbed and prevent foaming. Works great.

1. When I say ‘drugs’ here I mean in pharmacological sense not in the legal sense. Like how when police refer to psychedelics as ‘narcotics’ they don’t mean it in the pharmacological or legal sense, they mean it in the war on drugs sense.

2. You can’t gases to reabsorb by holding it in long enough. That isn’t a thing. What’s considered the gold standard for testing for lactose intolerance is to ingest lactose and then see if that results in traces of hydrogen in one’s breath afterwards. That’s considerably less reliable than testing to see if you can light your farts on fire. Much more convenient than that is to listen for high pitched farts. Someone should make a mobile app which can record fart sounds and use AI to analyze it and make a proper diagnosis.