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Is Caffeine Safe: How to Overcome Withdrawal

How it Works and Tolerance

Caffeine is molecularly similar to that of adenosine, a molecule that builds up and causes you to feel tired – builds up throughout the day and is depleted during sleep; adenosine thus facilitates sleep and dilates the blood vessels, probably to ensure good oxygenation during sleep.

So when you ingest caffeine, the molecules bind to the receptors in the brain normally used by adenosine

Is an adenosine-receptor antagonist; meaning it binds to the same receptors, but does not slow down neural activity

In other words, once caffeine is locked to adenosine’s receptors, there’s no place for adenosine to accumulate – prevents it from building up and making you sleepy

All of the extra adenosine that’s floating around causes the adrenal glands to secrete adrenaline – so it increases your attention level and and boosts energy

Also increases the production of dopamine in the brain’s pleasure circuits, giving you that feel-good sensation

Caffeine is not a direct stimulant, but rather a stimulant enabler; lets our natural stimulants run amuck – usually lasts from 4-6 hours

The blocking of adenosine receptors by caffeine causes your brain to produce more and more receptors to make up for them – this means that you’ll have to keep upping your caffeine intake in order to bind to all the new receptors (1,2)

According to a study published in The Journal of Clinical Investigation, caffeine tolerance occurred after just 1-4 days among their study participants.

They measured this by noting the increased blood pressure, increased heart rate, and plasma epinephrine levels – After 1-4 days these levels were back to their baseline. (3)


Caffeine causes vasoconstriction, but when we go through a withdrawal, a re-widening of the vessels increases blood flow to the brain, leading to a withdrawal headache (4,6)

Reduce Withdrawals

Caffeine withdrawal symptoms typically begin within 12 to 24 hours after discontinuing caffeine, peaking during the first two days, and can last all the way up to day nine – however, those that consume incredibly high doses of caffeine can experience symptoms for longer

Cold Turkey

Going cold turkey can be effective, however, it can be crippling to many and is not the ideal way to reduce withdrawals

Slowly Reduce Intake

Slowing reducing caffeine intake day by day is the preferred method – the slow withdrawal of caffeine from the body will eventually result in the decrease of the extra adenosine receptors

Common Solutions

– Replace caffeinated beverages with herbal teas to soothe symptoms and counteract dehydration, which can worsen headaches and withdrawal symptoms.

– Get extra sleep to combat fatigue and grogginess.


Rutaecarpine is an extract from the herb known as Evodea and has been shown to help rid the body of caffeine

A study published in the Archives of Pharmacal Research looked at rutaecarpine’s effect on caffeine metabolism in rats
Since mice and humans metabolize caffeine very similarly, the effects of rutaecarpine in regards to human caffeine metabolism are likely the same

The study found that rutaecarpine increases the metabolism of caffeine, theophylline, theobromine, and paraxanthine by inducing CYP1A2 (metabolism of xenobiotics; substances foreign to the body) and CYP2E1 in rats

Rutaecarpine speeds up the rate at which caffeine is broken down and removed from the body – cleansing caffeine from the body eliminates the side effects of caffeine much quicker (5)


1) THE BRAIN FROM TOP TO BOTTOM. (n.d.). Retrieved from

2) How Does Coffee Affect Your Brain? – Business Insider. (n.d.). Retrieved from

3) Tolerance to the humoral and hemodynamic effects of caffeine in man. (n.d.). Retrieved from


5) Effects of rutaecarpine on the metabolism and urinary excretion of caffeine in rats | SpringerLink. (n.d.). Retrieved from

6) Caffeine Withdrawal Headache Explained: Your Brain On — And Off — Caffeine. (2009, May 9). Retrieved from

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