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Wintergreen

Scientific Name(s): Gaultheria procumbens L.
Common Name(s): Boxberry, Canada tea, Checkerberry, Deerberry, Gaultheria oil, Mountain tea, Partridgeberry, Teaberry, Wintergreen

Clinical Overview

Use

In addition to being used as a flavoring, wintergreen and its oil have been used in topical analgesic and rubefacient preparations for the treatment of muscular and rheumatic pain. However, no clinical data support the use of wintergreen for any condition.

Dosing

Dosing recommendations for oral or topical administration of wintergreen oil are not available. Even small doses of oral wintergreen oil may cause toxicity.

One teaspoon (5 mL) of wintergreen oil is equivalent to approximately aspirin 7 g or 21.5 (325 mg) adult aspirin tablets.

Contraindications

Avoid oral or topical application in children. Avoid use in patients with known hypersensitivity to any components of wintergreen oil and in patients with known salicylate allergy, or GI irritation or inflammation.

Pregnancy/Lactation

Generally recognized as safe (GRAS) when used as food. Avoid dosages higher than found in food because safety and efficacy are unproven.

Interactions

Monitor for potentiation of warfarin anticoagulation in patients using methyl salicylate or topical wintergreen oil.

Adverse Reactions

Wintergreen may cause hypersensitivity reactions. Topical administration of methyl salicylate may cause redness and irritation; second- and third-degree burns have been reported rarely with menthol-methyl salicylate formulations.

Toxicology

When ingested, highly concentrated liquid methyl salicylate in the form of wintergreen oil, as with other volatile oils, can induce vomiting and cause severe, often fatal, poisonings.

Botany

Wintergreen is a perennial evergreen shrub with thin, creeping stems and leathery leaves with toothed, bristly margins. It is a low-growing plant native to eastern North America and usually found in woodland and exposed mountainous areas. Its small, waxy, white or pale pink flowers bloom in late summer, developing a scarlet fruit. The aromatic leaves and fruits are edible.Chevallier 1996, Simon 1984

History

American Indians reportedly used wintergreen for treating back pain, rheumatism, fever, headaches, and sore throats.Chevallier 1996 The plant and its oil have been used in traditional medicine as an anodyne, analgesic, carminative, astringent, and topical rubefacient. Wintergreen tea has been used to relieve cold symptoms and muscle aches.Dobelis 1986

Wintergreen oil is obtained by steam distillation of the warmed, water-macerated leaves. It is used interchangeably with sweet birch oil or methyl salicylate (typically no more than 0.04%) for flavoring foods and candy.

Wintergreen berries have been used to make pies.Duke 1985 A tea made from the leaves was used as a substitute for Camellia sinensis tea during the Revolutionary War.Chevallier 1996

Chemistry

Wintergreen oil is an extremely potent liquid form of methyl salicylate (98% methyl salicylate w/w).Chyka 2007 It is produced by macerating wintergreen leaves in warm water, followed by steam distillation.Khan 2010 During the process, gaultherin is enzymatically hydrolyzed to methyl salicylate.Howrie 1985, Simon 1984, Spoerke 1980 The yield of wintergreen oil from the leaves ranges from 0.5% to 0.8%.Khan 2010 Production of wintergreen oil by distillation from the natural product has been largely replaced by synthetic production of methyl salicylate.Bone 2013 Wintergreen oil has a distinct sweet aromatic odor and is either colorless or has a red or yellow tinge.Burdock 2010

Uses and Pharmacology

Small oral doses of wintergreen oil have been reported to stimulate digestion and gastric secretions.Duke 1985 Extreme caution is advised with this usage because dosing had not been determined and ingestion of even small amounts of wintergreen oil can cause toxicity.Chyka 2007

Topical wintergreen oil is a counterirritant that may offer some analgesic effect because of the structural similarity of methyl salicylate to aspirin. The US Food and Drug Administration lists OTC topical formulations of methyl salicylate (10% to 60%) as safe and effective for temporary relief of mild to moderate aches and pains. These formulations may also contain menthol and/or camphor and are available as gels, creams, ointments, and sprays.Olenak 2012

Animal data

Research reveals no animal data regarding the use of wintergreen.

Clinical data

Research reveals no clinical data regarding the efficacy of wintergreen for any condition.

Methyl salicylate is rapidly absorbed after oral administration of wintergreen oil.Howrie 1985 An open-label of 4 adult volunteers found that the bioavailability of methyl salicylate was greater after oral administration than after the use of methyl salicylate cream.Wolowich 2003

Topical administration of methyl salicylate results in systemic salicylate exposure.Morra 1996 Methyl salicylate also inhibits platelet aggregation, as measured in a randomized, blinded, crossover trial after administration of single doses of oral aspirin 162 mg and topical methyl salicylate 5 mg. Both treatments significantly decreased platelet aggregation compared to baseline, with no significant difference in the degree of platelet aggregation between them.Tanen 2008

Dosing

Dosing recommendations for oral or topical administration of wintergreen oil are not available. Wintergreen oil is 98% methyl salicylate. One milliliter of wintergreen oil is equivalent to 1.4 g of aspirin. One teaspoon (5 mL) of wintergreen oil 1 tsp (5 mL) is equivalent to approximately 7 g of salicylate 7 g of aspirin or the equivalent of 21.5 (325 mg) adult aspirin tablets. Even small doses of oral wintergreen oil may cause toxicity.Chyka 2007

Pregnancy / Lactation

GRAS when used as food. Avoid dosages higher than those found in food because safety and efficacy are unproven.

Interactions

Topical administration of methyl salicylate has been reported to increase the international normalized ratio (INR) with warfarin in case reports and case series, resulting in bruising, retroperitoneal bleeding, GI bleeding, and INR increases as high as 12.2. Patients using methyl salicylate or wintergreen oil should be monitored for potentiation of warfarin anticoagulation.Chan 2009, Joss 2000, Yip 1990

Adverse Reactions

One case report documents a potential hypersensitivity reaction in a nonsmoking, 21-year-old woman with a history of asthma who complained of wheezing, dry cough, and bronchial pain after using a tartar-control toothpaste flavored with wintergreen.McCarthy 1992, Toothpaste 1991 Another case report documents the development of laryngeal edema in a patient after accidental ingestion of wintergreen oil.Botma 2001 Because wintergreen oil is absorbed and converted to salicylic acid after both oral and topical administration, it should be used with caution in people with nonallergic aspirin sensitivity.Howrie 1985, Morra 1996, Olenak 2012

Wintergreen oil may cause hypersensitivity reactions, with topical administration of methyl salicylate causing redness and irritation.Olenak 2012 Second- and third-degree burns have been reported rarely with topical products containing menthol alone or menthol and methyl salicylate in concentrations greater than 3% and 10%, respectively. Most reactions occurred with 24 hours of initial application.FDA 2012

Toxicology

When ingested, the highly concentrated liquid methyl salicylate, in the form of wintergreen oil, as with other volatile oils, can induce vomiting and cause severe, often fatal, salicylate poisoning.Duke 1985, Howrie 1985

The oil may be particularly toxic to children, who may associate the pleasant odor of wintergreen oil with "candy." Wintergreen oil 5 mL is equivalent to aspirin 7 g, the same amount in 21.5 adult aspirin tablets (325 mg) (wintergreen oil 1 mL is equivalent to aspirin 1.4 g).Chyka 2007

Ingestion of as little as 4 mL in a child and 6 mL in an adult has been fatal.Chyka 2007, Dreisbach 1987, Tyler 1988 Because of this potential for toxicity, official labeling requirements have been changed so that no drug product may contain more than methyl salicylate 5%.FDA 2015 No deaths have been reported from ingestion of the plant itself.Simon 1984 The American Association of Poison Control Centers recommends emergency department referral for ingestion of more than a lick or taste of wintergreen oil (98% methyl salicylate) in a child younger than 6 years of age.Chyka 2007 Referral is also recommended for ingestion of more than wintergreen oil 4 mL in people 6 years of age and older.

Because the essential oil and its components can be absorbed through the skin, salicylate, intoxications can occur following topical application of methyl salicylate or wintergreen oil. Due to a structural similarity between methyl salicylate and acetylsalicylic acid (aspirin), a toxic syndrome similar to that seen in salicylism and characterized by tinnitus, nausea, and vomiting has been observed in people who have ingested wintergreen for prolonged periods of time.Duke 1985

A 40-year-old man became acutely ill within 1 hour after an herbalist applied an herbal skin cream containing an unknown amount of wintergreen oil for the treatment of psoriasis. Salicylate absorption may have been increased by use of an occlusive dressing. The patient developed tinnitus followed by hyperpnea, vomiting, diaphoresis, fever, and CNS disturbance (wintergreen oil in liquid form is a highly lipid soluble).Bell 2002

A 70-year-old woman, seeking relief for chronic knee pain, developed fatal clinical manifestations of methyl salicylate poisoning (eg, acid-base disturbance, endocrine abnormalities, fluid and electrolyte imbalances, CNS toxicity) after ingesting topical Koong Yick Hung Fa Oil 60 mL, which contains salicylic acid 56.2 g (the equivalent of 173 regular-strength, adult aspirin tablets).Hofman 1998

References

Bell AJ, Duggin G. Acute methyl salicylate toxicity complicating herbal skin treatment for psoriasis. Emerg Med (Fremantle). 2002;14(2):188-190.12147116
Bone K, Mills S. Principles and Practice of Phytotherapy: Modern Herbal Medicine. 2nd ed. New York, NY: Churchill Livingstone Elsevier; 2013:17-82.
Botma M, Colquhoun-Flannery W, Leighton S. Laryngeal oedema caused by accidental ingestion of Oil of Wintergreen. Int J Pediatr Otorhinolaryngol. 2001;58(3):229-232.11335011
Burdock GA. Fenaroli’s Handbook of Flavor Ingredients. 6th ed. Boca Raton, FL: CRC Press/Taylor & Francis Group; 2010.
Chan TY. Life-threatening retroperitoneal bleeding due to warfarin-drug interactions. Pharmacoepidemiol Drug Saf. 2009;18(5):420-422.19283775
Chevallier A. The Encyclopedia of Medicinal Plants. New York, NY: DK Publishing Inc; 1996.
Chyka PA, Erdman AR, Christianson G, et al. Salicylate poisoning: an evidence-based consensus guideline for out-of-hospital management. Clin Toxicol (Phila). 2007;45(2):95-131.17364628
Dobelis IN, ed. Magic and Medicine of Plants. Pleasantville, NY: Reader's Digest Association, Inc; 1986.
Dreisbach RH, Robertson WO. Handbook of Poisoning. 12th ed. Norwalk, CT: Appleton & Lange; 1987.
Duke JA, Ducellier J, Bogunschutz-Godwin MJ. Handbook of Medicinal Herbs. Boca Raton, FL: CRC Press; 1985.
Hofman M, Diaz JE, Martella C. Oil of wintergreen overdose. Ann Emerg Med. 1998;31(6):793-794.9624330
Howrie DL, Moriarty R, Breit R. Candy flavoring as a source of salicylate poisoning. Pediatrics. 1985;75:869-871.3991273
Joss JD, LeBlond RF. Potentiation of warfarin anticoagulation associated with topical methyl salicylate. Ann Pharmacother. 2000;34(6):729-733.10860133
Khan IA, Abourashed EA. Leung’s Encyclopedia of Common Natural Ingredients Used in Food, Drugs, and Cosmetics. 3rd ed. Hoboken, NJ: Wiley; 2010.
McCarthy P. Asthma-flavored toothpaste. Omni. 1992;14:36.
Morra P, Bartle WR, Walker SE, Lee SN, Bowles SK, Reeves RA. Serum concentrations of salicylic acid following topically applied salicylate derivatives. Ann Pharmacother. 1996;30(9):935-940.8876850
Olenak JL. Musculoskeletal injuries and disorders. In: Krinsky DL, Berardi RR, Ferreri SP, et al, eds. Handbook of Nonprescription Drugs: An Interactive Approach to Self-Care. 17th ed. Washington, DC: American Pharmacists Association; 2012:101-118.
Simon JE. Herbs: An Indexed Bibliography, 1971-1980. Hamden, CT: Shoe String Press; 1984.
Spoerke DG, Jr. Herbal Medications. Santa Barbara, CA: Woodbridge Press; 1980.
Tanen DA, Danish DC, Reardon JM, Chisholm CB, Matteucci MJ, Riffenburgh RH. Comparison of oral aspirin versus topical applied methyl salicylate for platelet inhibition. Ann Pharmacother. 2008;42(10):1396-1401.18698012
Toothpaste can cause allergic reaction. Nutri Health Rev. 1991;58:18.
Tyler VE, Brady LR, Robbers JE. Pharmacognosy. 9th ed. Philadelphia, PA: Lea & Febiger; 1988.
US Food and Drug Administration. CFR - Code of Federal Regulations Title 21. Food and Drugs. Labeling of drug preparations containing significant proportions of wintergreen oil. 21CFR201.303. Revised April 1, 2015.
US Food and Drug Administration. FDA Drug Safety Communication: Rare cases of serious burns with the use of over-the-counter topical muscle and joint pain relievers. http://www.fda.gov/Drugs/DrugSafety/ucm318858.htm. September 3, 2012. Accessed September 9, 2015.
Wolowich WR, Hadley CM, Kelley MT, Walson PD, Casavant MJ. Plasma salicylate from methyl salicylate cream compared to oil of wintergreen. J Toxicol Clin Toxicol. 2003;41(4):355-358.12870876
Yip AS, Chow WH, Tai YT, Cheung KL. Adverse effect of topical methylsalicylate ointment on warfarin anticoagulation: an unrecognized potential hazard. Postgrad Med J. 1990;66(775):367-369.2371186

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This information relates to an herbal, vitamin, mineral or other dietary supplement. This product has not been reviewed by the FDA to determine whether it is safe or effective and is not subject to the quality standards and safety information collection standards that are applicable to most prescription drugs. This information should not be used to decide whether or not to take this product. This information does not endorse this product as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this product. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this product. This information is not specific medical advice and does not replace information you receive from your health care provider. You should talk with your health care provider for complete information about the risks and benefits of using this product.

This product may adversely interact with certain health and medical conditions, other prescription and over-the-counter drugs, foods, or other dietary supplements. This product may be unsafe when used before surgery or other medical procedures. It is important to fully inform your doctor about the herbal, vitamins, mineral or any other supplements you are taking before any kind of surgery or medical procedure. With the exception of certain products that are generally recognized as safe in normal quantities, including use of folic acid and prenatal vitamins during pregnancy, this product has not been sufficiently studied to determine whether it is safe to use during pregnancy or nursing or by persons younger than 2 years of age.

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