Theobromine Supplement Benefits and Side Effects: The Effects on The Brain and The Natural “High” People Rave About

What is Theobromine?

Chocolate - the decadent dessert that delivers a boost in mood for humans, yet poses a toxic risk in pets. It is Theobromine, a natural molecule found in the cacao bean and some other plants, that is thanks for both cacao’s health-promoting properties as well as its danger to dogs.

This apparent contradiction can be explained by how this compound is metabolized once consumed. In dogs and select other mammals, the half-life is so long that it can rapidly accumulate to dangerous levels.

Luckily for humans, our bodies are capable of metabolizing Theobromine much faster, allowing us to cash in on the delicious taste and impressive health benefits that chocolate has to offer.

It is theorized that cacao may produce similar positive health effects to caffeine without the side effects, such as insomnia and jitters, thanks to its large Theobromine content. This bitter-tasting compound that makes up 0.5%-2.7% of chocolate. (5)

Chemically, it’s an alkaloid with a similar structure to caffeine - both compounds are categorized as methylxanthines. As a supplement, many people use it for nootropic purposes thanks to its benefits on brain health and mood.

Is Theobromine a Stimulant?

Studies suggest that Theobromine is much less stimulating than caffeine, with a potency of about 1/10th that of this popular stimulant. (1) Even though it’s less stimulating, it is still classified as a central nervous system (CNS) stimulant, and has been demonstrated to increase heart rate at high dosages.

Theobromine vs Caffeine: What’s the Difference?

Even though both of these compounds are methylxanthines, they have noticeably different effects on humans.

Caffeine is a water-soluble compound with a much shorter half-life, which degrades quickly in the human body and is more able to cross over the blood-brain barrier. (1,2) Theobromine is a more stable, fat-soluble compound.

The main benefits of Theobromine come from its ability to dilate blood vessels, enhancing blood flow to the brain. It is a cardiac stimulator that has even been used to dilate coronary arteries. Caffeine, on the other hand, is a vasorestrictor. When it comes to their mechanisms of action, caffeine has a stronger affinity for adenosine receptors and acts as a more potent phosphodiesterase inhibitor. (1,2)

Theobromine is considered to have psychoactive actions different from those of caffeine. (2) While caffeine is a drug that will cause lots of stimulation, these effects are much less pronounced with Theobromine.

One study compared the effects of theobromine, caffeine, theobromine + caffeine, or placebo on 24 healthy female subjects. (8) Researchers found that Theobromine alone led to feelings of calm and lowered blood pressure, caffeine alone led to increased alertness and increased blood pressure, and the two combined led to increased alertness without an effect on blood pressure. This study suggests that these two compounds have differing effects on blood pressure and mood.

Mechanism of Action: Effects on the Brain

This nootropic works largely through the inhibition of phosphodiesterases, blockage of adenosine receptors, and as a vasodilator. (1,2,5)

Through its inhibition of phosphodiesterase, it leads to increases in intracellular cAMP, protein kinase A (PKA) activation, and inhibition of inflammatory mediators. It is through this pathway that it acts as a vasodilator, reduces inflammation, and provides stimulation. As a vasodilator, Theobromine helps to increase oxygen flow to the brain and lowers blood pressure.

Adenosine receptors are G-protein-coupled receptors that responds to adenosine, a hormone-like molecule involved in the regulation of the central nervous system (CNS). Through blocking these receptors, it acts to decrease the release of certain hormones, such as norepinephrine. Norepinephrine is known to increase blood pressure, so this is another way by which this compounds leads to a reduction in blood pressure.

Studies have also found this compound to be one of the many antioxidants found in cacao beans and tea. (15)

Health Benefits and Uses

Mental High

Some people report feeling an enjoyable, “high” feeling after eating chocolate. Theobromine, particularly in the Theobromine to caffeine ratio found in cacao, is known to help promote a positive mood. This proportion of Theobromine to caffeine is known to produce feelings of alertness and a positive mood. (2)

Anxiety

Theobromine has been found to exert calming effects. In a study of 24 healthy adult females, 700 mg led to increased feelings of calm when compared to placebo 3 hours post-consumption. (8)

Asthma

In those with asthma, methylxanthines are used in bronchodilators to help manage the condition. (2) Theobromine helps to open up the bronchioles, which are tubes in the lungs where oxygen exchange occurs. This effect was confirmed in a human study on 21 adults with asthma, which found that capsules of this drug increased bronchial diameter. (10)

Cough Suppressant

Evidence suggests that Theobromine may be able to help suppress coughing through inhibition of afferent nerve activation and reduction of inflammation. (2)

In a study these effects were examined on guinea pigs and in vitro human vagus nerve preparations. Researchers concluded that this compound helps to prevent citric-acid-provoked coughing in guinea-pigs as well as the effects of capsaicin (the compound in chili peppers that provokes coughing) in the in vitro human vagus nerve samples. (3)

In a human clinical trial testing the effect of Theobromine on persistent cough, the treatment group experienced improvements in coughing, however these results did not reach significance. (4)

Blood Pressure

Numerous human studies have linked supplementation with lowered blood pressure. (7) In a study on 84 healthy adults, 250-1,000 mg Theobromine was found to significantly lower blood pressure and increase heart rate.

Another study on 24 healthy adult females found that 700 mg led to lower blood pressure one hour after administration. (8)

Cacao beans naturally have both caffeine and theobromine, and the combination of these two drugs leads to improved mood, but no effect on blood pressure. (8) This suggests that, if you are looking for benefits for high blood pressure, supplementation would be a better option than dark chocolate or unsweetened cacao consumption.

These findings are supported with an additional study which found that natural cocoa did not change ambulatory or central systolic blood pressure when compared to placebo, but cocoa enriched with extra Theobromine lowered central systolic blood pressure. (9)

Stimulation

At higher doses, around 300 to 1,000 mg/day, this supplement has been found to increase heart rate, boost subject’s interest in study tasks, and increase feelings of alertness. (1) These doses are quite high and are often accompanied by negative side effects, making it not the ideal choice if you are looking for a stimulant.

Fights Inflammation

Theobromine is such a powerful anti-inflammatory agent that a synthetic derivative of it, Pentoxifylline, is used for inflammatory conditions in children and adults. (11) Additionally, the benefit of this drug on cough appears to be partly related to fighting inflammation. (2)

The anti-inflammatory effects are thought to be thanks to its action as a phosphodiesterase inhibitor. As such, it downregulates pro-inflammatory cytokines. (2)

Weight loss

Some human studies have found a correlation between chocolate consumption and body mass index (BMI): those who eat chocolate more frequently tend to have lower BMIs. (14) In a study on obese rats, consumption of cocoa powder was found to lead to improved weight loss when compared to control rats. (13)

If you look at the list of ingredients on herbal weight loss supplements, you will frequently find this Theobromine. It is hypothesized that it plays a part in this beneficial role of cocoa and weight through reducing hunger. (11)

Side Effects

Overall this compound is safe and well-tolerated in humans. The beneficial effects have been found to reverse at higher doses. While lower doses of around 200-400 mg/day produce a positive mood, higher doses have been found to negatively affect mood. When taken at higher doses, this compound may lead to:

  • Irritability
  • Headache
  • Heart palpitations

If you experience headaches or migraines when taking this drug, you may have a sensitivity or allergy to Theobromine. While this is rare, an allergy or sensitivity can even lead to agitation and panic attacks.

Toxicity: Theobromine Poisoning in Humans

Theobromine toxicity is common in domestic pets and other mammals, however the toxicity threshold of this compound is much higher in humans. (2) The reason for this is that it is metabolized much more slowly in some mammals, including dogs, than in humans. (5)

Sources and Foods that Contain Theobromine

Methylxanthines, such as caffeine and Theobromine, are found in tea leaves (including green, black, white, and yerba mate teas), coffee, and chocolate. Different foods will have varying concentrations of each methylxanthine.

Raw cacao powder or nibs are the foods that contain the highest amounts of Theobromine. Its content is much lower in white chocolate than in dark chocolate. If you are looking to increase your consumption of this compound through chocolate, look for dark chocolate of 70% or higher. At many grocery stores you can find Lindt dark chocolate and Godiva dark chocolate at this percentage.

Not all cocoa bean products will be high in Theobromine. Cocoa butter and white chocolate only have trace amounts of Theobromine.

Dosage

Theobromine has a long half-life of approximately ten hours, so you only need to supplement once per day. (2) Dosages varies widely, with a low dose around 200 - 400 mg/day and a high dose at 1,000 mg/day.

Start low and gradually increase until you find the best dose for you. Some studies have found negative side effects, including irritability, with higher doses.

It is best to take this supplement early in the day since it does act as a mild CNS stimulant.

User Experiences and Reviews

One Reddit user experienced a “subtle high” with benefits in mood, experiencing calm, not stimulating effects. This user reported problems taking the powder due to the bitter taste, and preferred capsules.

Another review on LongeCity was from someone who took a high dose of 1,100 mg/day, divided into two doses. This user experienced some of the negative effects reported with high doses, including increase heart rate and undesirable stimulation.

Where to Buy Theobromine Powder and Supplements

This supplement is typically sold in powder form, although you can find capsules. Amazon carries a wide variety of supplements to choose from. You will find premade nootropic stacks containing this compound through Pure Nootropics and Nootropics Depot, two trustworthy sources for nootropics online.

Pure Nootropics sells a supplement called 1-2-Go that contains a stack of L-Theanine, Theobromine, and caffeine, and Nootropics Depot sells a cocoa extract. If you are looking for a general health-boost, you can always simply add raw cacao powder or cacao nibs to a smoothie.

References:

Share
Tweet
Share
Pin
0 Shares