Guarana: benefits, dosage, contraindications

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Guarana is a woody vine with evergreen leaves, native to the Amazonian tropical forests. The fruits are colored from dark red to orange, even yellow. They are partially open, revealing 1 to 3 dark chestnut-colored seeds, the lower part of which is covered with a thick white membrane. Indigenous tribes of the Amazon region have a long history of traditional use of guarana seeds, generally in a beverage, for their stimulating and aphrodisiac properties. In traditional preparation, guarana seeds are roasted to facilitate the removal of the "testa" (seed coat or husk), which is discarded. The seeds are pounded into powder and mixed with water to form a paste; this is rolled and dried to produce hard bars (or "sticks"), from which the powder can be scraped as needed. The seed is the part of the plant used for medicinal purposes. The "testa" represents 15 to 20% of the seed weight and contains up to 4% caffeine (compared to 1-2% in coffee), tannins (3 to 5%), and other constituents. The main characteristic constituents of the seeds are caffeine (1 to 5.8%), and other methylxanthines like theobromine (0.01 to 0.17%) and theophylline (0.006 to 0.25%). Other constituents include tannins (5-16%), mainly proanthocyanidins, catechin (1.3-6%), and epicatechin (1.2-3.8%), fatty oils (2.2-3.7%) containing acylglycerols and cyanogenic lipids, a volatile fraction (0.4%) mainly composed of Carvacrol. Orally, guarana is used for cognitive functions, sports performance, against fatigue, obesity, to enhance libido, and as a tonic. It is also used orally to prevent malaria, as well as for diarrhea, fever, and cardiovascular diseases. The therapeutic interest of guarana is due to the interaction of its different compounds and not only its high caffeine content. The significant caffeine content does not cause strong excitement due to its bond with tannins. The presence of saponosides, lipids, and tannins would slow down the intestinal absorption of caffeine.
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Other name(s) 

Brazilian Cocoa

Scientific name(s)

Paullinia cupana

Family or group: 

Plants

Active ingredients:

Caffeine

Tannins

Flavonoids

Theophylline

Theobromine

Polysaccharides


Indications

Rating methodology

EFSA approval.

Several clinical trials (> 2) randomized controlled with double blind, including a significant number of patients (>100) with consistently positive outcomes for the indication.
Several clinical trials (> 2) randomized controlled with double blind, and including a significant number of patients (>100) with positive outcomes for the indication.
One or more randomized studies or multiple cohorts or epidemiological studies with positive outcomes for the indication.
Clinical studies exist but are uncontrolled, with conclusions that may be positive or contradictory.
Lack of clinical studies to date that can demonstrate the indication.


Fatigue
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Guarana has also been evaluated in patients with breast cancer experiencing fatigue during chemotherapy treatment. The randomized study involving 32 patients revealed that a daily dose of 50 mg of guarana taken over 21 days resulted in a significant reduction in fatigue during this period compared to placebo and was not associated with toxicity or adverse effects. The Brief Fatigue Inventory (BFI) improved significantly after treatment with a dry guarana extract (37.5 mg twice daily) administered one week after the start of chemotherapy. The study conducted with 40 individuals with solid tumors showed that BFI fatigue scores improved or stabilized in 36 out of 40 patients. Interestingly, the benefits persisted for several weeks after stopping guarana treatment. The ESCOP and EMA recommend guarana as a tonic in cases of fatigue, exhaustion, or convalescence.

Posologie

posologieOral: seed

posologie50 - 450 mg

duration21 - days

populationAdults

formulationpowder, dry extract


Emotional balance
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Anecdotal evidence suggests that guarana produces effects similar to those of caffeine on subjective feelings of well-being, energy, motivation, and self-confidence. Tests on animal models indicate that guarana exerts a mild antidepressant effect, confirming the observed effects on mood. Mood enhancement has been demonstrated in a recent multi-dose, double-blind, placebo-controlled clinical study involving 26 volunteers who tested a low-caffeine guarana extract. Four concentrations were studied (37.5 mg, 75 mg, 150 mg, and 300 mg). Treatment at each dosage level produced a significant mood effect. Given the low levels of caffeine measured in the guarana extract, the mood enhancement cannot be explained by caffeine content alone. Another clinical research shows that taking two tablets of a product containing hawthorn (10 mg), black horehound (10 mg), passionflower (40 mg), valerian (50 mg), cola nut (15 mg), and guarana (15 mg), three times a day for 28 days, can reduce the severity of anxiety in a higher percentage of patients with adjustment disorder with anxious mood, compared to a placebo.

Posologie

posologieOrally: seed

posologie222 - 450 mg

formulationpowder, dry extract


Synergies


Sports performance
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To enhance sports performance, it has been shown that caffeine might decrease perceived effort levels, allowing the athlete to feel less fatigued and improve performance. Caffeine may enhance anaerobic exercise performance. It appears to improve muscle metabolism and increase time to exhaustion and oxygen deficit, which can lead to better performance. A study shows that taking a single dose of a product containing 222 mg of guarana, B vitamins, vitamin C, and minerals slightly improves exertion tolerance in trained individuals by about 2% compared to a placebo. The dose contained 222.2 mg of guarana (standardized to 40 mg caffeine), 1.4 mg of vitamin B1, 1.6 mg of vitamin B2, 18 mg of vitamin B3, 6 mg of vitamin B5, 2 mg of vitamin B6, 150 mcg of biotin, 200 mcg of folic acid, 1 mcg of vitamin B12, 60 mg of vitamin C, 100 mg of calcium, 100 mg of magnesium, and 9.5 mg of zinc was used. It is noted that some studies were unable to confirm these effects. A recent study showed that taking a supplement containing only guarana and caffeine (total caffeine content of 300 mg) does not improve agility or jump height. The combination of guarana, vitamins and minerals might be more effective.

Posologie

posologieOrally: seed

posologie2222 - 450 mg

populationAdults

formulationstandardized extract


Synergies


Weight control
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Guarana is traditionally used as an adjuvant in slimming diets. A double-blind, randomized controlled trial testing a combination of yerba mate (leaves of Ilex paraguayensis), guarana (seeds of Paullinia cupana), and damiana (leaves of Turnera diffusa var. aphrodisiaca) showed that the preparation significantly delayed gastric emptying, reduced the time of perception of gastric fullness, and induced significant weight loss over 45 days in overweight patients. The same combination of plants was tested in an open study on 73 overweight health professionals for 6 weeks. The active treatment resulted in a significant reduction in self-reported weight and waist and hip circumference, as well as an increase in post-meal satiety. A significant weight loss was reported by 22% of the volunteers. Another study, double-blind, placebo-controlled, and randomized, tested a multi-component plant combination containing extracts of asparagus, green tea, black tea, guarana, mate, red beans, Garcinia cambogia, and chromium yeast. It found, over a 12-week period, a significant change in the improvement index of body composition and a reduction in body fat compared to a placebo. The formula was more effective for participants engaging in an exercise program compared to those remaining sedentary. These studies show that caffeine or guarana combined with other plants have significant effects on weight loss, and on energy expenditure in healthy subjects. Although encouraging, the effects of guarana as a standalone treatment need to be confirmed.

Posologie

posologieOrally: seed

posologie855 mg

duration45 - days

populationAdults, Men, Women

formulationpowder, dry extract


Synergies


Cognitive Performance
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Several clinical studies conducted on healthy adults show that standardized guarana extract in caffeine, alone or with vitamins and minerals, improves the speed of performing cognitive tasks, memory, reaction time, and alertness scores compared to a placebo. Higher doses were noted to have no more efficacy. The median dose was 222 mg and caffeine content from 4 to 100 mg.

Posologie

posologieOral route: seed

posologie37.5 - 500 mg

formulationpowder, dry extract


Properties


Neurological

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Although the effects of guarana on the central nervous system (CNS) have not been the subject of clinical studies, ample evidence shows that caffeine, the main constituent of guarana, stimulates the CNS. Possible mechanisms include blocking adenosine receptors and inhibiting phosphodiesterase. By blocking adenosine receptors, caffeine may increase the release of neurotransmitters such as dopamine. This could result in a reduction of the clinical expression of Parkinson's disease. It has also been proposed that caffeine may decrease GABA and serotonin signaling. Caffeine's stimulating effects on the CNS are thought to improve alertness and psychomotor performance. Caffeine increases plasma catecholamine levels, probably through adenosine receptor antagonism and a reduction in the extraneuronal uptake of catecholamines. In a small randomized, single-blind, placebo-controlled clinical study, 15 subjects (normal sleeper) received 250 ml of a guarana seed drink (500 mg of guarana seed powder in 100 ml) or a placebo. After a night of sleep limited to 4 hours, guarana seed improved psychomotor performance and produced positive trends on mood.

Usages associés

Emotional balance

Bioenergizing

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Caffeine, the main constituent of guarana, is considered responsible for the energy increase. However, some researchers think other compounds present in guarana may also play a role in the "energy-boosting" effect, potentially leading to heightened stimulant effects compared to caffeine alone. Guarana extract can induce a stimulant effect in a specific laboratory model using a caffeine-resistant organism. These results have been seen in humans as well.

Usages associés

Fatigue, Sports performance

Metabolic

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Caffeine, the main constituent of guarana, increases resting energy expenditure and cellular thermogenesis. It also leads to an increase in non-oxidative fatty acid turnover and lipid oxidation; however, the net effect on lipid oxidation is minor. The effects of caffeine on energy expenditure and lipid metabolism seem to be mediated by sympathetic and non-sympathetic mechanisms. Caffeine is often used in combination with ephedra for weight loss and seems to have additive pharmacodynamic effects. A single dose of ephedra in combination with caffeine can increase heart rate from 67 beats per minute to 82 beats per minute in young, healthy individuals. This combination also increases systolic blood pressure and, to a lesser degree, diastolic pressure. Caffeine combined with ephedra also increases oxygen consumption. A clinical study in healthy subjects showed that ingesting a single dose of 2.72g of guarana significantly increases the respiratory quotient (a reflection of lipid oxidation) and systolic blood pressure.

Usages associés

Weight management

Cognitive function

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Studies in animals have shown that administration of guarana improves cognitive and physical performance. Indeed, a positive action of guarana on physical abilities, particularly during periods of stress, and an improvement in memory capacities has been noted. In another phase II trial, the effects of different doses of guarana on cognitive abilities in humans were evaluated. The analysis was conducted as a double-blind, placebo-controlled test on 26 subjects over 6 days. Different doses of a standardized guarana extract were studied. The impact of this treatment on cognition and mood was measured using two scales: CDR's (Cognitive Drug Research) automated assessments and Bond and Lader mood scales. Guarana thus led to improvements in memory, alertness, and satisfaction. The authors suggest that caffeine is not the only active component responsible for the described effects. Other components of this plant may also be involved.

Usages associés

Cognitive performance

Hypoglycemic

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In vitro research suggests that polyphenols isolated from guarana powder inhibit the enzymes alpha-glucosidase and alpha-amylase, which could contribute to hypoglycemic effects. In vivo, it has been shown that an aqueous extract of guarana affects the glycemic response after exercise. Thus, 60 minutes post-exercise, mice pretreated with the extract maintained their blood sugar levels while these dropped in the control group. After 2 hours, the drop in blood sugar was less in mice pretreated with the guarana extract. The mechanism behind this action is thought to be due to an increase in glycogen breakdown, allowing the body to have a more substantial energy source.


Gastroprotective

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A study on rats pretreated with a guarana extract showed that guarana significantly reduced gastric lesions induced by ethanol or indomethacin. Caffeine is not believed to be the only constituent responsible for this protective action. Guarana could also increase gastric acid secretion and delay gastric emptying. This was demonstrated in a clinical study using a combination of plants known as YGD, which contains yerba mate (leaves of Ilex paraguayensis), guarana (seeds of Paullinia cupana), and damiana (leaves of Turnera diffusa var. aphrodisiaca).


Satiating

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A double-blind, placebo-controlled clinical study showed the influence of a guarana-based treatment on the intestinal transit of 13 healthy subjects. Researchers found that the guarana-based preparation slowed food progression in the stomach by 53% compared to placebo, thereby increasing the duration of the satiety period.

Usages associés

Weight control

Antibacterial

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In vitro data demonstrated the antibacterial and antioxidant effects of the ethanolic extract of guarana, believed to be due to phenolic compounds. Guarana was found to be effective against numerous digestive pathogens, including Escherichia coli, Salmonella typhimurium, and Staphylococcus aureus. This provides a theoretical basis for the traditional use of guarana against diarrhea. More recently, in vitro research demonstrated antibacterial activity against Streptococcus mutans, which could have applications in preventing dental plaque formation. The antimicrobial activity was confirmed in vitro by testing guarana seed extracts against fungi and food-borne bacteria.


Antioxidant

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In vitro, it has been shown that guarana powder reduces spontaneous lipid peroxidation. In another model, a hydro-alcoholic extract of guarana limited fibroblast mortality and pro-oxidant effects (lipid peroxidation, DNA damage, oxidative stress) induced by a chemical agent. Finally, a study in healthy elderly subjects showed that individuals who regularly consumed guarana (at least 5 times/week) had better protection of their LDL against an oxidizing agent (27% statistically significant reduction in LDL oxidation) compared to non-consumers.


Hormonal metabolism

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In human research, acute caffeine ingestion induces an increase in epinephrine and norepinephrine levels, leading to increased heart rate and providing more energy to the body. There is also evidence that caffeine may be associated with decreased testosterone levels and increased levels of estrone and sex hormone-binding globulin. These results could explain why some studies have reported associations between caffeine and hormone-dependent conditions such as fibrocystic disease, osteoporosis, breast cancer, and endometriosis.


Safety dosage

Adult from 16 year(s): 37.5 mg - 450 mg (powder, dry extract)

- Cognition, alertness, and mood: doses ranging from 37.5 to 222 mg standardized in caffeine are sufficient to provide effects for at least 6 hours. - For other indications, take the equivalent of 1 to 3 g of Guarana powder or 450 mg up to 5 times a day.


Interactions

Médicaments

Amphetamines: strong interaction

Theoretically, the caffeine in guarana could increase the risk of additive effects on the central nervous system.

Antiplatelets/Anticoagulant: moderate interaction

In vitro and animal research suggests that guarana extract could inhibit platelet aggregation. This effect could be due to caffeine, which is also known for its antiplatelet activity. Among antiplatelet agents, there are aspirin, clopidogrel (Plavix), dipyridamole (Persantine), ticlopidine (Ticlid), among others. Anticoagulant agents include heparin and warfarin (Coumadin).

Ephedrine: strong interaction

Using ephedrine with caffeine, a component of guarana, can increase the risk of adverse effects. There is evidence that using ephedrine with caffeine may increase the risk of hypertension, myocardial infarction, cerebrovascular accidents, and seizures. Guarana should not be taken with other stimulants.

Adenosine: moderate interaction

The caffeine contained in guarana is a competitive inhibitor of adenosine at the cellular level.

Cimetidine: moderate interaction

The concomitant use of cimetidine and guarana could increase the serum concentrations of caffeine, thus increasing the risk of adverse effects, due to the presence of caffeine in guarana.

Clozapine: moderate interaction

Theoretically, co-administration of clozapine and guarana could acutely exacerbate psychotic symptoms because of the caffeine in guarana. Indeed, caffeine is likely to increase the effects and toxicity of clozapine. Doses of caffeine ranging from 400 to 1000 mg per day may inhibit clozapine metabolism.

Oral contraceptives: weak interaction

Theoretically, the concurrent use of oral contraceptives and guarana could increase serum concentrations of caffeine, and consequently the risk of adverse effects, due to the caffeine in guarana. Oral contraceptives are known to reduce the clearance rate of caffeine by 40 to 65%.

Dipyridamole: moderate interaction

The caffeine present in guarana could inhibit the vasodilation induced by dipyridamole.

Sedatives: weak interaction

Antagonistic effects could theoretically occur due to the stimulating activity of guarana on the central nervous system (CNS). However, an in vivo study revealed no significant interaction with pentobarbital.


Precautions

Pregnant women: avoid

Not enough data to conclude.

Breastfeeding women: avoid

Not enough data to conclude.

Anxiety: use with caution

Caffeine could exacerbate anxiety disorders.


Contraindications

Child up to 16 year(s): prohibited

Guarana is not recommended for children under 16 years.

Hypertension: prohibited

Contraindicated in case of cardiovascular disorders such as hypertension and arrhythmias.

Gastric ulcer: prohibited

Contraindicated in case of gastric and duodenal ulcers.

Cardiac disorders: prohibited

Contraindicated in case of cardiovascular disorders such as hypertension and arrhythmias.