Guarana - Uses, Side Effects, and More

Guarana (Paullinia cupana) is a plant native to the Amazon. It is a common ingredient of energy drinks and can be unsafe in large amounts.

Guarana contains caffeine. Caffeine works by stimulating the central nervous system, heart, and muscles. Guarana also contains theophylline and theobromine, which are chemicals similar to caffeine.

OVERVIEW

Introduction

Guarana is an extract of roasted and pulverized seeds of the plant Paullinia cupana which is indigenous to the Amazon Basin and whose major active components are caffeine and other xanthine alkaloids such as theophylline and theobromine. Guarana has been used as a stimulant and tonic to treat fatigue, decrease hunger and thirst and for headaches and dysmenorrhea. 

In conventional doses, guarana has few side effects and has not been linked to episodes of liver injury or jaundice.

Background

Guarana is derived from the seeds of the plant Paullinia cupana which is native to the Amazon Basin and is cultivated as a source of guarana and caffeine in South America.

 The P. cupana seeds contain a high concentration of caffeine (2% to 8%), far higher than in coffee beans (1% to 3%). 

The seeds are also rich in other xanthine alkaloids such as theophylline and theobromine as well as catechins, epicatechins and procyanidins. 

Guarana is produced by shelling and washing the seeds, followed by drying or roasting. 

The seeds are then pulverized into a powder that can be used as a food favoring, to prepare tea or as a component in energy drinks or multiingredient dietary supplements. 

Guarana has caffeine like effects on the heart, vasculature and central nervous system. 

In traditional medicine, guarana was used as a stimulant, mild diuretic and as a tonic to increase wakefulness, quell hunger and thirst, and to treat headaches, dysmenorrhea and digestive disorders. 

More recently, guarana has been purported to have beneficial effects on energy and endurance, as a weight loss agent, and for cognitive enhancement to increase concentration and memory. 

While guarana may have a mild effect on energy levels, cognition and satiety, these are generally short-lived and have minimal lasting clinical effects.

 In high doses, guarana can cause tremor, jitteriness, agitation, confusion, hypertension and dehydration.

 Most of its beneficial effects as well as its side effects can be explained by its caffeine content. 

Guarana is available in tablets and capsules, as liquid and in multiple commercial multiingredient supplements, particularly weight loss products and energy drinks. 

Daily doses range from 200 to 1000 mg daily. The use of multiple herbal products containing guarana and other sources of caffeine can result in caffeine toxicity.

Clinical Overview

Use

Guarana has traditionally been used as a natural energizer and cognitive stimulant, as flavoring in beverages, and as a component in natural weight loss products; however, 

clinical data do not support use as a natural energizer or weight loss aid. Limited clinical trials have been conducted with guarana alone, with some evidence for use in chemotherapy-related fatigue.

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Dosing

Doses ranging from 75 mg to 1,000 mg daily were administered in limited clinical trials.

Contraindications

Guarana is contraindicated in pregnancy and lactation.

Pregnancy/Lactation

Use is contraindicated. Low birthweight, birth defects, and premature birth have been documented with guarana use.

Interactions

Caffeine, a principal constituent of guarana, is unsafe as a food additive when combined with alcohol (ie, alcoholic beverages with added caffeine).

Adverse Reactions

Excessive nervousness, insomnia, and other health risks in patients sensitive to caffeine have been reported.

Toxicology

Research reveals little or no information regarding severe toxicity with the use of guarana. Because of its high tannin content, excessive use may lead to an increased risk of cancer of the oropharynx.

Scientific Family

• Sapindaceae (Soapberry)

Chemistry

In 1840, caffeine was identified as guarana's principal constituent, with levels ranging from 3% to greater than 5% by dry weight.

Schimpl 2013 By comparison, coffee beans contain approximately 1% to 2% of caffeine and the content in dried tea leaves varies from 1% to 4%.

Burke 2011 The related alkaloids theophylline and theobromine have also been identified in guarana. Guarana is high in tannins (primarily catechutannic acid and catechol), which are present in concentrations of 5% to 6% dry weight; these impart an astringent taste.Burke 2011

Other uses

Some researchers suggest that the revitalizing effects of guarana result partly from its antioxidant action.

Guarana's potential appetite suppressant and energy-inducing effects are likely related to its caffeine content. Numerous investigational studies have shown the sympathetic stimulant ephedrine, 

when combined with caffeine, demonstrates a synergistic effect on increasing metabolic rates, with subsequent increased energy expenditure (thermogenesis), as well as lipolytic actions.

These effects resulted in statistically significant weight loss when guarana was combined with diet in short-term animal and clinical trials. 

However, a review reports a lack of unequivocal benefits of guarana over water or sports drinks.(Higgins 2010)

A study in rats with diet-induced hypercholesterolemia demonstrated reductions from baseline levels in total cholesterol and low-density lipoprotein cholesterol with guarana doses of 12.5, 25, or 50 mg/day for 4 weeks.(Ruchel 2016)

The effects of a guarana extract (12.24 mg/g of caffeine) on 7 chemotherapeutic drugs used in the treatment of breast cancer were tested in vitro in a breast cancer cell line. 

Cell proliferation decreased about 20% to 25% with the extract alone, but guarana extract plus cyclophosphamide resulted in an 80% decrease in cancer cell population compared to the control group after 72 hours. 

Guarana added to the other 6 agents resulted in decreases in cell proliferation of 40% to 50%.(Hertz 2015)

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Dosing

Doses ranging from 75 mg to 1,000 mg daily have been used in limited clinical trials evaluating stimulant effects.

A group of researchers in Brazil evaluated the effect of guarana on chemotherapy-related fatigue and reported favorable outcomes with doses of 37.5 mg to 75 mg orally twice daily.

Interactions

The Food and Drug Administration (FDA) has ruled that caffeine is unsafe as a food additive when combined with alcohol (ie, alcoholic beverages with added caffeine).

FDA 2010, Marczinski 2014 In vitro, guarana extract inhibited aggregation of platelets, possibly due to inhibition of platelet thromboxane synthesis.

Based on the caffeine content of guarana, interactions with clozapine, lithium, anxiolytic agents, pseudoephedrine, and antihypertensive agents are theoretically possible