This is part three in the Caffeine as a Gateway Drug series where we explore how drugs work in the body by looking at caffeine.
I never envisaged that writing about caffeine would leave me feeling somewhat enraged.
I’ll admit, those who know me well would say it doesn’t take much for me to get up on my soapbox and have a good old rant. But this is caffeine we’re talking about- there’s nothing remotely controversial about that, surely?
The journey to outrage started out as mere curiosity.
As I was writing part two of this series and thinking through the various ways in which caffeine can make its way into the body, I was taken aback by just how many caffeine products I could find.
Here’s some insight into how the inner monologue evolved…
At first, it was amusing – oh wow, look at all these products for endurance athletes. Fair enough, a coffee wouldn’t feel too good sitting in your gut before a marathon. Geez, high concentration caffeine powder is a bit over the top isn’t it? That doesn’t seem very safe. Oh, that’s really not safe — one scoop is equivalent to how many cups of coffee?
Then it turned frustrated – I think it’s a bit rich calling this a dietary supplement when it’s clearly being used and marketed as a drug. How can they say their product will make you alert but won’t cause jitteriness or diuresis- this isn’t precision medicine we’re talking about. A transdermal caffeine patch to look like a butterfly tattoo, are you kidding me? Really, people want to hurt their lungs with a vape just to get caffeine, what’s the point?
Finally, after finding a snortable vial containing 500mg of white powdered caffeine called “gotta bump?” that came complete with fake rolled up $100 bills and was sold in a bulk pack of 30 vials, the outrage hit. I mean, I’ve often joked that caffeine was a gateway drug, but I think this might be a bit too far given its availability to teenagers. What’s the likelihood of anyone using this as a laugh carefully measuring out 1/10 of a vial like the label suggests? This seems like a pretty irresponsible product from both a personal and public health perspective. (I was very close to purchasing just for research’s sake, but couldn’t bring myself to pay $30 in international shipping).
This experience exposed me to the types of statements made in the marketing of caffeine products. Which is why I thought I’d take a closer look at three common claims that I consider to be myths, along with a surprising truth or two.
Myth 1: It’s not given orally so it must be better
In Part Two, we talked about all the weird and wonderful ways you can get drugs into the body, including caffeine. Of the non-injectable routes of administration, it looks like the only place in your body that doesn’t have a caffeine-related product made for it is the ear and the vagina. As I mentioned earlier, there’s even snortable nasal powder and disposable vapes.
I’m not so naïve that I think that these types of products are available because people want to get the caffeine into their bloodstream in the most efficient way possible. But I do want to take a moment to explain why for a drug like caffeine, exposing more delicate parts of your body is both unsafe and a waste of time. This is one of those ‘just because you can, doesn’t mean you should’ type scenarios.
Firstly, unless it’s specially formulated, putting something up your nose or into your lungs will cause irritation. For those more innocent amongst us, if you’ve ever had the embarrassing experience of laughing whilst having a mouthful of fizzy drink, you will know the discomfort that results. Well, the same goes for snorting other things that aren’t designed to be snorted. They can really stuff up your nasal passages (pun intended).
Same goes for inhaling things into your lungs. Sure, vapes may be ‘cleaner’ than cigarettes, but they still contain ingredients that hurt the lining of your airways. As far as I’m concerned, causing inflammation in your airways is not a good idea. Especially not for a drug that is so readily absorbed from other routes.
As explained in Part Two, caffeine is almost completely absorbed from the gut and isn’t really impacted by first pass metabolism. This means the amount of caffeine that ends up in your blood after you swallow it will be just the same (or potentially even more) as the amount you snort, inhale, or stick up your bum.
I will admit, nasal and inhaled administration will have a faster onset of action than oral, working within minutes. However, the same fast onset of action could be achieved by putting an oral strip or melt under the tongue (sublingual)- without the inflammation.
Myth 2: Caffeine is a dietary supplement
Ok, I’ll admit this one isn’t always a myth and requires a bit of explaining. But I think it’s worth taking the time to understand, as the same principles apply to other naturally occurring products that act like drugs.
There are lots of natural products that elicit drug like effects in the body, caffeine included. The line between where a product stops becoming a food product and starts becoming a drug is kind of fuzzy.
From user perspective, I think it comes down to what you’re using the product for. In the case of caffeine, is the main reason you’re consuming it to enjoy the food product or to feel its effects in your body? If it’s the latter, I don’t think there’s anything wrong with that — it just means you’re using it as a drug which means you need to pay attention to dose.
(Incidentally, you should still pay some attention to total daily dose if you’re consuming caffeine as a food product. Decaffeinated products still contain some amount of caffeine. Combine that with a bottle of coke and a chocolate bar and you might be getting more than you think!)
As we introduced in Part Two, the dose is the amount of drug you put into your body. For most drugs, the effect in the body is proportional to the dose. But please be aware this definitely doesn’t mean more is better! When it comes to dosing, we’ve got a Goldilocks situation- we’re aiming for ‘just right’.
If a dose is too small, the drug won’t produce the desired effect. But if the dose is too big, the drug will cause more toxic effects, which at some point may result in death.
When we use drugs we need to aim for the sweet spot, between the low dose that’s not effective and the high dose that’s not safe. The exact sweet spot depends on the person — what they’re using the medicine for and how sensitive they are to its effects.
The dose required to produce the desired effect will depend on what you consider desirable. When it comes to caffeine, there are generally two reasons it’s used. The first is for it’s effects on the brain — to make you feel alert and perhaps more focused. A moderate dose equivalent to a cup of coffee (~50 to 100mg) is enough to achieve this for most adults.
Caffeine can also be used to enhance physical performance, with a long history of use in endurance exercise. It can be used on its own or as part of a pre-workout cocktail of other ‘supplements’ that are also being used as drugs. In this case, the caffeine is being used for its effects on the muscles and fat cells (peripheral effects) in addition to its effects within the brain and nerves (central effects). For this use, a dose equivalent to two cups of coffee (~200mg) appears to be effective. Higher than that is unlikely to further improve performance but is likely to cause more side effects.
Of course, whether an effect is considered desirable or undesirable depends on the user. Someone taking a 200mg dose of caffeine at 8pm when they’re starting a night shift will welcome the alertness at 11pm. Another person taking it prior to their evening gym session may be quite unhappy feeling alert as they try and go to sleep a few hours later.
As stated earlier, more is definitely not better when comes to the dose of caffeine. The maximum recommended total dose of caffeine is 400mg per day for adults, and 200mg per day for those who are pregnant or breastfeeding.
Another important thing to note is that just because it’s natural, doesn’t make it safe. Excessive doses of caffeine can kill you. A dose of between 5g and 10g of caffeine is considered to be lethal to adults but there have been reports of death after a dose of 3g. This is what makes high potency caffeine products and bulk packs of caffeine powder particularly unsafe. As a result, many countries like Australia have banned the sale of high concentration caffeine powders. Even still, it can be hard to enforce these regulations in practice and these types of products can be available and marketed to younger people. So the best thing is to be a mindful consumer and teach kids to be the same.
Myth 3: You can get the effect you want with no annoying side effects
Aside from producing desired and undesired effects, there are two other broad types of drug effects in the body — local and system wide (or systemic).
Lots of medicines are used for local effect. Treatments applied directly to the skin for dermatological conditions. Puffers inhaled into the lungs for conditions like asthma. Intrauterine devices placed in the uterus for contraception. Ear, nose and eye preparations instilled into the respective body part to treat said body parts. Local anaesthetics injected into the gums before a dental procedure.
Some drugs have local effects within the gut when they’re taken orally. Like laxatives that work by pulling water into the bowel through osmosis or bulking out the bowel motion with fibre. Caffeine also has local effects on the gut. It increases the secretion of stomach acid, which is why people who suffer from dyspepsia and reflux are encouraged to avoid it.
Interesting side note — the reason coffee makes some people want to poop quickly after drinking it seems to be more to do with the coffee formulation than the caffeine itself. There’s something about the acids within coffee, whether its caffeinated or not, that releases the hormone gastrin. This stimulates the colon within minutes of coffee being in the stomach. Other forms of oral caffeine, like capsules and gels, may still cause some stomach acidity but are unlikely to result in an urgent pooping scenario.
When you’re using a drug for a local effect, that’s where you want it to stay. If the drug passes into the bloodstream, that’s when you get system wide effects.
Drugs like caffeine aren’t very sophisticated. If you’ve ever seen the classic piece of 80’s cinema that is Innerspace, you’ll understand that once a drug compound makes is in the bloodstream it’ll go wherever the blood vessels take it. With one exception — the brain.
To get to the brain a medicine needs to be able to pass through the blood brain barrier. It’s kind of like that part of Lord of the Rings where Gandalf protects the bridge with “You shall not pass!”.
In this case, the barrier sits between the blood vessels that supply the brain with oxygen and the brain cells and other bits of the central nervous system. Only medicines that are able to pass through this barrier have effects in the brain — these medicines are known as centrally acting medicines owing to the fact that they affect the central nervous system. The actions of medicines on parts of the body that are outside of the central nervous system are known as peripheral effects.
Caffeine is one of those substances that is able to get past the blood brain barrier, which is why it’s a good example to help understand just how broad reaching the effects of a single medicine can be throughout the body.
I’m going to save the finer details for how caffeine interacts with its targets (pharmacology) and elicit effects in the body for another day. For now, it’s enough to know that unless there’s some sort of precision medicine involved (hint, if you can afford to pay for it yourself, it’s not precision medicine), it’s simply not possible to get the effect you want without the annoying side effects. That’s a paradoxical statement.
If a caffeine product has less side effects, it’s most likely because of the specific formulation. As we talked about earlier, a caffeine product won’t make you poop like drinking coffee will but it could still increase your stomach acid if it’s taken orally. If, however, you used a melt placed under the tongue (sub-lingual) it would avoid this effect. The broad range of other systemic effects, however, would remain.
In part four we’ll look at what exactly the systemic effects of caffeine are, and how drugs work to elicit their pharmacological effects in the body.
If there’s something you’d like me to cover in a future article, please let me know in the comments.
And if you found this useful or entertaining, or just want to give me some encouragement, please feel free to like and share this with your friends.
Thanks for reading!
I’ll admit that the elimination system has been sluggish this week since I went off caffeine.
To go back to the Die Hard analogy, you never mentioned that limo driver entering by the back door as being similar to a suppository.