Paullinia cupana

Paullinia cupana

Synonyms

No documentation

Vernacular Name

Guarana gum, guarana seed, zoom cocoa, Brazilian cocoa.

Description

Paullinia cupana extracts are most commonly used in Western culture for the caffeine content, and are commonly included in dietary supplements and as a drink additive. In traditional use, its applications included that of tonic, stimulant and as a component of beverages.

P. cupana is a climbing plant found in the Amazon basin and is a member of the Sapindaceae family. It can grow to 12m in height and is a climbing or creeping shrub. The leaves are large and it produces small bright red fruits which contain a single black seed in the center, which becomes visible as the fruit ripens.

Origin / Habitat

P. cupana is indigenous to the Amazonian rainforests throughout Brazil and Venezuela. This climbing plant grows deep in the thick of the forests, thriving on humidity, warmth and nutritive soil from the Amazon River.

Chemical Constituents

Caffeine 2.5-7.0%; P. cupana seeds contain approximately 2-4.5% caffeine compared to coffee beans (approximately 1–2%).[1] Theophylline and theobromine; tannins (including catechols); saponins 

Plant Part Used

Seed

Medicinal Uses

General

Cognitive enhancement
Stimulant, anti-fatigue
Appetite suppressant; weight loss
Mood enhancement

Most Frequently Reported Uses

Cognitive enhancement
Stimulant, anti-fatigue
Appetite suppressant; weight loss

Other Reported Uses

Mood enhancement

Dosage

Dosage Range 

Tablets/Capsules: 200-900mg standardized P. cupana extract, before breakfast or lunch; not to exceed 3g daily.

Beverages: The average daily total of caffeine in the average adult is considered safe between 600-700mg. Check the label.

Most Common Dosage

500mg standardized extract twice per day

Standardization Dosage

P. cupana products should be standardized to contain between 5-22% caffeine per dose.

Pharmacology

Pre-clinical

The primary activity of P. cupana is due to its xanthine alkaloid content, including caffeine, theophylline and theobromine. Most traditional uses of P. cupana can be traced to its caffeine content. The activity of caffeine in the body includes central nervous system (CNS) stimulation, cardiac stimulation, diuresis, increase in blood pressure, erogenesis, neuroprotection, platelet aggregation inhibition, stimulation of skeletal muscle and hyperglycemic activity, all leading to uses in fatigue, athletic performance, weight loss and neurological conditions (such as Alzheimer’s disease).[2]

A laboratory animal study found that an extract of P. cupana seed inhibited an IgE-induced passive cutaneous anaphylaxis reaction and also inhibited the degranulation of basophilic cells.[3] The authors concluded that P. cupana seed extract may be a candidate for effective therapeutic material for allergic diseases.

In an in vitro study, an extract of P. cupana seed was found to have activity against Streptococcus mutans, the bacteria responsible for dental plaque.[4]

A laboratory study in mice found that P. cupana extract reduced gastric secretory volume and total acidity without affecting gastrointestinal transit time.[5] The authors concluded that P. cupana has a gastroprotective property that needs further study.

Clinical

A double-blind, randomized, placebo-controlled, parallel group study in 129 healthy individuals (ages 18-24) found that a supplement beverage containing vitamins, minerals, and P. cupana seed extract reducing mental fatigue and resulted in improved task performance, measured by an increase in speed and accuracy as compared to placebo.[6]

Another double-blind, counterbalanced, placebo-controlled study in 26 individuals assessed the acute mood and cognitive effects throughout the day of four different doses (37.5mg, 75mg, 150mg and 300mg) of a standardized P. cupana extract.[7] P. cupana improved secondary memory performance and increased alert and content mood ratings. Interestingly, the two lower doses produced more positive effects on cognition that the higher doses.

One randomized double-blind crossover trial of 36 breast cancer positive patients undergoing adjuvant radiation therapy compared P. cupana to placebo for effects on physical performance and mood.  Based on the 75mg daily dose, there was no apparent advantage with P. cupana over placebo for both fatigue and depressive symptoms.[8]

The clinical studies have reported dietary supplements that contain P. cupana in conjunction with other ingredients such as caffeine, bitter orange, green tea and garcinia, may improve weight loss in some individuals.[9],[10],[11]

Interaction and Depletions

Interaction with other Herbs

No documentation

Interaction with Drugs

Most of  potential of P. cupana drug interactions occur due to the caffeine content. Based on the pharmacology of caffeine, use P. cupana with caution when using the following medications:

  • Monoamine Oxidase Inhibitors (MAO-I): hypertensive crisis may occur when combining caffeine with MAO inhibitors
  • Adenosine: Caffeine may inhibit the hemodynamic effects of adenosine. P. cupana or caffeine should not be consumed for at least 12 hours prior to receiving adenosine.
  • Clozapine (Clozaril): Effects of clozapine may be altered.
  • Benzodiazepines, including alprazolam (Xanax) and diazepam (Valium): Sedative effects of benzodiazepines may be reduced by caffeine.
  • Lithium: Serum levels of lithium may be decreased by caffeine.
  • Aspirin: Absorption and bioavailability of aspirin may be increased by caffeine.
  • Oral contraceptives, cimetidine, verapamil, disulfiram, fluconazole, mexiletine, and quinolone antibiotics: Caffeine metabolism is inhibited.
  • Acetaminophen (Tylenol): Efficacy of acetaminophen may be increased, thereby reducing drug need.
  • Terbinafine (Lamisil): Terbinafine decreases the rate of caffeine clearance, potentially leading to side effects such as anxiety, insomnia and heart palpitations.
  • In a laboratory animal study, P. cupana altered the binding of technetium-99m-dimercaptosuccinic acid (99mTc-DMSA) to blood cells and plasma.[14] It is not recommended individuals undergoing technetium-99m scans, including blood cell labeling, to use P. cupana or beverages containing P. cupana before the diagnostic procedure.

Precautions and Contraindications

Side effects

P. cupana containing supplements, especially when used late in the evening, may alter sleep patterns in sensitive individuals. Discontinue if sleep disturbances occur.

Discontinue if anxiety or nervousness occurs.

Discontinue if allergy occurs.

Caution should be used in those individuals with bleeding disorders, as P. cupana has been reported to inhibit platelet aggregation in laboratory studies.[13]

P. cupana has been reported safe in recommended doses.

Pregnancy

Caution should be used in pregnancy and lactation.

Age limitation

No documentation

Adverse reaction

Based on pharmacology, use with caution in individuals with pre-existing heart conditions, including hypertension and arrhythmias.[12]

References 

  1. Bempong DK, Houghton PJ, Steadman K. The Xanthine Content of Guarana and Its Preparations. Pharmaceutical Biology; 1993:31(3):175-181.
  2. Tunnicliffe JM, Erdman KA, Reimer RA, Lun V, Shearer J. Consumption of dietary caffeine and coffee in physically active populations: physiological interactions. Appl Physiol Nutr Metab. Dec 2008;33(6):1301-1310.
  3. Jippo T, Kobayashi Y, Sato H, et al. Inhibitory effects of guarana seed extract on passive cutaneous anaphylaxis and mast cell degranulation. Biosci Biotechnol Biochem. Sep 2009;73(9):2110-2112.
  4. Yamaguti-Sasaki E, Ito LA, et al. Antioxidant capacity and in vitro prevention of dental plaque formation by extracts and condensed tannins of Paullinia cupana. Molecules. 20 Aug 2007;12(8):1950-1963.
  5. Campos AR, Barros AI, Santos FA, Rao VS. Guarana (Paullinia cupana Mart.) offers protection against gastric lesions induced by ethanol and indomethacin in rats. Phytother Res. Dec 2003;17(10):1199-1202.
  6. Kennedy DO, Haskell CF, Robertson B, Reay J, Brewster-Maund C, Luedemann J, Maggini S, Ruf M, Zangara A, Scholey AB. Improved cognitive performance and mental fatigue following a multi-vitamin and mineral supplement with added guaraná (Paullinia cupana). Appetite. Mar-May 2008;50(2-3):506-513.
  7. Haskell CF, Kennedy DO, Wesnes KA, Milne AL, Scholey AB. A double-blind, placebo-controlled, multi-dose evaluation of the acute behavioral effects of guaraná in humans. J Psychopharmacol. Jan 2007;21(1):65-70.
  8. Da Costa Miranda V, Trufelli DC, Santos J, et al. Effectiveness of guaraná (Paullinia cupana) for postradiation fatigue and depression: results of a pilot double-blind randomized study. J Altern Complement Med. Apr 2009;15(4):431-433.
  9. Opala T, Rzymski P, Pischel I, Wilczak M, Wozniak J. Efficacy of 12 weeks supplementation of a botanical extract-based weight loss formula on body weight, body composition and blood chemistry in healthy, overweight subjects--a randomised double-blind placebo-controlled clinical trial. Eur J Med Res. 30 Aug 2006;11(8):343-350.
  10. Bérubé-Parent S, Pelletier C, Doré J, Tremblay A. Effects of encapsulated green tea and Guarana extracts containing a mixture of epigallocatechin-3-gallate and caffeine on 24 h energy expenditure and fat oxidation in men. Br J Nutr. Sep 2005;94(3):432-436.
  11. Sale C, Harris RC, Delves S, Corbett J. Metabolic and physiological effects of ingesting extracts of bitter orange, green tea and guarana at rest and during treadmill walking in overweight males. Int J Obes (Lond). May 2006;30(5):764-773.
  12. Baghkhani L, Jafari M. Cardiovascular adverse reactions associated with Guarana: is there a causal effect? J Herb Pharmacother. 2002;2(1):57-61.
  13. Ravi Subbiah MT, Yunker R. Studies on the nature of anti-platelet aggregatory factors in the seeds of the Amazonian Herb Guarana (Paullinia cupana). Int J Vitam Nutr Res. Mar 2008;78(2):96-101.
  14. Freitas RS, Moreno SR, Lima-Filho GL, Fonseca AS, Bernardo-Filho M. Effect of a commercial extract of Paullinia cupana (guarana) on the binding of 99mTc-DMSA on blood constituents: An in vivo study. Appl Radiat Isot. May 2007;65(5):528-533.