Wintergreen

Generic name: Gaultheria Procumbens L.
Brand names: Boxberry, Canada Tea, Checkerberry, Deerberry, Gaultheria Oil, Mountain Tea, Partridgeberry, Teaberry, Wintergreen

Usage of Wintergreen

Salicylates, along with Capsaicin, menthol, and camphor, are a counterirritant class of topical analgesics. These compounds produce analgesia by activating and then desensitizing epidermal nociceptors.(Barkin 2013)

Topical wintergreen oil is a counterirritant that offers some analgesic effect because of the structural similarity of methyl salicylate to aspirin. Methyl salicylate formulations may also contain menthol and/or camphor and are available as gels, creams, ointments, and sprays.(Olenak 2012) Typically, these products contain from 10% to 40% methyl salicylate (United States Pharmacopeia) and are used in the treatment of painful muscles or joints.

Methyl salicylate is also used as a pesticide, fragrance ingredient, and flavoring agent. More recently, wintergreen oil has been used as a flavoring agent in tobacco products.(Greene 2017)

Analgesic effects

Research reveals no clinical data regarding the efficacy of wintergreen oil (alone) for any condition. However, the pain relief capabilities of methyl salicylate are better established and a multitude of over-the-counter products are available.(Anderson 2017)

Clinical data

In a randomized, double-blind, parallel-group, placebo-controlled, multicenter study of 208 patients with pain associated with mild to moderate muscle strain, a patch containing methyl salicylate and l-menthol provided significantly greater pain relief after 8 hours compared with the placebo group (P=0.005).(Higashi 2010)

Antiplatelet effects

Clinical data

Topical administration of methyl salicylate results in systemic salicylate exposure.(Morra 1996) In a small randomized, blinded, crossover trial, 9 healthy men received either a single oral dose (162 mg) of aspirin (a mainstay of chronic antiplatelet therapy in patients at risk for acute coronary syndrome) or 5 g of a topical methyl salicylate 30% preparation administered to the anterior thighs. Both treatments decreased platelet aggregation compared with baseline.(Tanen 2008)

Insecticidal effects

Animal and in vitro data

Insecticidal activity of wintergreen oil was demonstrated against Paederus fuscipes in both in vitro and in vivo experiments. P. fuscipes is a major predator of several agricultural pests but can cause dermatitis linearis in humans. The mechanism of action was related to inhibition of acetylcholinesterase in adult insects that was not significantly different from the positive control (chlopyrifos).(Liu 2018)

Wintergreen side effects

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 oil.McCarthy 1992 Another case report documents the development of laryngeal edema in an individual 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 individuals 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 reported reactions occurred within 24 hours of initial application.FDA 2012

Before taking Wintergreen

Wintergreen has GRAS status when used as food flavoring. Avoid doSages higher than those found in food because safety has not been established.

How to use Wintergreen

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

Warnings

Wintergreen has GRAS status when used as food flavoring. Several regulatory agencies have established an acceptable daily intake of 0.5 mg/kg/day for methyl salicylate.Greene 2017

Wintergreen oil is highly concentrated and lipid soluble; therefore, it poses a threat of severe, rapid-onset salicylate poisoning. The toxic potential of topical medicaments containing methyl salicylate or wintergreen oil should be fully appreciated.Chan 1996 Salicylate toxicity following intentional ingestion of a plant-based insecticide with wintergreen oil as a minor ingredient has been reported in a suicide attempt by a 74-year-old woman.Moss 2020

Typical symptoms of salicylate toxicity (eg, hematemesis, tachypnea, hyperpnea, dyspnea, tinnitus, deafness, lethargy, seizures, unexplained lethargy, confusion) warrant referral to an emergency department for evaluation.Chyka 2007

When ingested, the highly concentrated liquid methyl salicylate, in the form of wintergreen oil, 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 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 In the United States between 1990 and 2000, there were 3 acute drug ingestion fatalities in children 2 years or younger.Koren 2019

Because of the potential for toxicity, official labeling requirements have been changed for drug products containing more than 5% methyl salicylate.FDA 2015 In these cases, labelling must warn that the product may be dangerous and that it should be kept out of reach of children to prevent accidental poisoning. The American Association of Poison Control Centers recommends emergency department referral for ingestion of more than a lick or taste of wintergreen oil (methyl salicylate 98%) in a child younger than 6 years.Chyka 2007 No deaths have been reported from ingestion of the plant itself.Simon 1984

In the case of overdose, do not induce emesis for ingestions of salicylates or wintergreen oil. If immediately available and no contraindications are present, consider out-of-hospital administration of activated Charcoal for acute ingestion of a toxic dose of methyl salicylate.Chyka 2007 Salicylate poisoning is usually treated with activated charcoal and alkaline diuresis or hemodialysis.

Because the essential oil and its components can be absorbed through the skin, salicylate intoxication 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 individuals ingesting 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.Bell 2002

Case reports involving accidental methyl salicylate poisoning are common.Seneviratne 2015 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

In a review assessing toxicity from oral exposure to methyl salicylate, dose-response modeling showed changes in the reproductive/development end points after exposure to 500 mg/kg/day of methyl salicylate in male and female mice.Greene 2017

What other drugs will affect Wintergreen

In case reports and case series, topical administration of methyl salicylate has been reported to cause increases in international normalized ratio (INR) (as high as 12.2) when coadministered with Warfarin, resulting in bruising, retroperitoneal bleeding, and GI bleeding. Individuals using methyl salicylate or wintergreen oil should be monitored for increased warfarin effects.Chan 2009, Joss 2000, Yip 1990

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