For NASAL ALLERGIES, Butterbur Extract is a highly effective remedy for reducing nasal congestion, mucus, and itching of nasal passages and eyes, especially during allergy season, because of its significant anti-inflammatory and antihistamine properties.

Allergic rhinitis, or hay fever, is caused by the immune system over-reacting, leading to the release of mediators including histamines and leukotrienes from specific types of white blood cells including eosinophils and mast cells. These biological mediators can cause inflammation of the nasal linings, leading to sneezing, runny nose, post-nasal drainage, and red and irritated eyes. Research confirms that butterbur blocks leukotriene receptors, and thus can prevent or curtail allergic reactions.

How butterbur works

Butterbur extract can be as effective as some conventional antihistamines, but without the common side effect of drowsiness. The beneficial effects of butterbur extract come from its active constituents, a group of bitter-tasting compounds called petasins. These compounds belong to a class of natural molecules called sesquiterpenes that provide butterbur with its pharmacological activity, including pain-relieving and anti-inflammatory effects. S-petasin, the main sesquiterpene, and its isoform, iso-S-petasin, are the effective ingredients in butterbur, especially for the relief of nasal allergies.

Petasins work by blocking the production of leukotrienes. During an allergic reaction, your body releases inflammatory mediators like histamines and leukotrienes. These mediators cause inflammation of the nasal lining, leading to common allergy symptoms like sneezing, congestion, and runny nose. By stopping leukotrienes, petasins calm the allergic response in the nasal passages, helping to relieve or prevent irritation and swelling. Butterbur extract, therefore, acts as a leukotriene (LT) inhibitor, preventing or relieving allergic reactions much like the drug montelukast (Singulair). While montelukast is a standard treatment for nasal allergies, studies suggest that butterbur extract is an equally effective LT inhibitor and a much safer alternative, as montelukast has been associated with severe mental health side effects.

What is butterbur?

Butterbur is a perennial shrub that grows well in the marshy terrain of Europe, Asia, and North America. The variant Petasites hydridus is found in colder, northerly regions of Russia and Europe. An equally effective medicinal species called Petasites frigidus is found in the northern United States and Canada.

With its large, parasol-like leaves, Butterbur’s botanical name Petasites is thought to derive from the Greek word “petasos,” referring to the Thessalian sun hat worn by the ancient Greeks. Its common name may also stem from its use to wrap butter; the large heart-shaped leaves helping to prevent butter from melting in warm weather.

Butterbur has a long history of traditional use stretching back at least 2,000 years where it was used to relieve asthma attacks and nasal symptoms, soothe headaches, and ease digestion. Butterbur’s medicinal use was recorded by the famous Greek physician, pharmacologist, botanist, and author Dioscorides in 65 A.D. In the Middle Ages butterbur root was a traditional remedy for nasal congestion, headaches, coughs, and asthma, noted in Nicholas Culpeper’s book “The English Physician” in 1652.

The active constituents of butterbur root extract are called petasins which give butterbur its pharmacologic activity, including pain-relieving and anti-inflammatory actions. Petasins are a group of bitter-tasting compounds in a class of natural molecules called sesquiterpenes. For relieving nasal allergies, the main effective ingredients are S-petasin, the main sesquiterpene, and its isoform, iso-S-petasin.

Research confirms that butterbur helps nasal allergies

Researchers have investigated butterbur’s mechanism in human eosinophils — specialized white blood cells often elevated in people with allergies or inflammation. In a study of these cells, it was confirmed that petasin was the primary component with the highest leukotriene inhibitor activity. This indicates that petasin is directly responsible for disrupting the allergic signaling pathway, thereby inhibiting the inflammatory process.

Traditional antihistamines work by directly blocking histamine from binding to its receptor (the H1 receptor) on cells. This prevents the cascade of symptoms that histamine would normally cause like nasal congestion and sneezing. It is a direct action, single-target approach, but it is less effective for nasal congestion and may cause sedation and drowsiness. Butterbur’s action is broader and involves multiple pathways. One piece of evidence that highlights this distinction comes from a study where butterbur did not significantly reduce the skin wheal and flare response to histamine, while the traditional antihistamine fexofenadine (Allegra) did. This suggests that butterbur’s primary action is not through direct histamine receptor blockage.

A randomized trial of butterbur extract and a commonly used non-sedating antihistamine cetirizine (Zyrtec) compared the effectiveness of these two treatments. After two weeks, butterbur’s effects were comparable with the pharmaceutical remedy but produced fewer sedating effects.¹

A study in The Journal of Allergy and Clinical Immunology found that a butterbur extract was more effective than a placebo and just as effective as the antihistamine fexofenadine (Allegra) at relieving nasal congestion. Researchers concluded that butterbur’s effects likely stem from its ability to regulate inflammatory processes, like the synthesis of leukotrienes.²

Another human study showed that butterbur significantly improved allergy symptoms after one week. Within 5 days of treatment, there were smaller quantities of the allergy-producing substances leukotriene and histamines in the test subjects’ bodies.³

Other clinical trials found that butterbur extract reduced leukotriene and histamine levels in the nasal fluids of allergic rhinitis patients, while they enjoyed reduced day and nighttime nasal symptoms and registered better quality-of-life scores.⁴ Additionally, butterbur can speed the clearing of nasal obstruction after exposure to allergens like grass pollen.⁵

Nutrients that support butterbur’s action

Several other nutrients magnify the benefits of butterbur extract and are also helpful in their own right for nasal allergies. The action of butterbur is magnified by combining it with the following nutrients and botanicals:

  • Vitamin B2 (riboflavin): Studies show that the intake of B2 correlates with a lower risk of developing an allergy.⁶
  • Magnesium: Chronic magnesium deficiency may provoke a higher allergic reaction. It has been found that magnesium deficiency can cause an increase in histamine levels in the blood after being exposed to allergens. Conversely, taking magnesium can reduce levels in the body of irritant biochemical mediators.⁷
  • Ginger: Ginger works as a natural antihistamine, potent antiviral agent, and immune booster easing the symptoms of allergic rhinitis.⁸
  • Feverfew: Feverfew has a long history of use in traditional and folk medicine and has been noted for its anti-inflammatory and anti-allergic effects especially through the inhibition of histamine release. The herb contains vitamin B3 (niacin), iron, vitamin A, and vitamin C (ascorbic acid) and inhibits the formation of prostaglandins in the body, which are natural chemicals that play a role in inflammation.⁹
  • 5-Hydroxytryptophan: Encourages optimal neurotransmitter levels and healthy brain chemistry. 5-HTP raises serotonin levels in the brain, and several studies have found 5-HTP to be effective at reducing leukocyte recruitment and allergic inflammation, identifying a novel potential target for intervention in allergies.¹⁰

In our clinic, we have found that our patients with hay fever and nasal allergies often report major improvements using butterbur extract, ideally with synergistic vitamin B2 (riboflavin), magnesium, the botanicals ginger and feverfew, and the amino acid 5-hydroxytryptophan. Especially taking these treatments for 2 to 3 months during peak allergy seasons, patients tell us that nasal mucus is reduced, sneezing and congestion are eased, breathing becomes easier, postnasal drip is reduced, and they have less itching of nasal passages and eyes. After having one good season, people often become proactive about starting butterbur extract in the following year before their vulnerable months.

Recommendation: Butterbur extract 50–100 mg daily. To meet our specifications, a butterbur formula must be a correctly standardized extract of butterbur root, certified free of unhelpful pyrrolizidine alkaloids (PAs). Butterbur is best taken between meals for optimal absorption, or as directed by your healthcare practitioner.

References

  1. Blosa M, Uricher J, Nebel S, Zahner C, Butterweck V, Drewe J. Treatment of Early Allergic and Late Inflammatory Symptoms of Allergic Rhinitis with Petasites hybridus Leaf Extract (Ze 339): Results of a Noninterventional Observational Study in Switzerland. Pharmaceuticals (Basel). 2021 Feb 24;14(3):180. doi: 10.3390/ph14030180. PMID: 33668395; PMCID: PMC7996175.
  2. Schapowal A; Petasites Study Group. Randomised controlled trial of butterbur and cetirizine for treating seasonal allergic rhinitis. BMJ. 2002 Jan 19;324(7330):144–6. doi: 10.1136/bmj.324.7330.144. PMID: 11799030; PMCID: PMC64514.
  3. Thomet OA, Wiesmann UN, Blaser K, Simon HU. Differential inhibition of inflammatory effector functions by petasin, isopetasin and neopetasin in human eosinophils. Clin Exp Allergy. 2001 Aug;31(8):1310–20. doi: 10.1046/j.1365-2222.2001.01158.x. PMID: 11529903.
  4. Thomet OAR, et al. “Anti-inflammatory activity of an extract of Petasites hybridus in allergic rhinitis.” International Immunopharmacology 2.7 (2002): 997–1006.
  5. Dumitru AF, et al. “Petasol butenoate complex (Ze 339) relieves allergic rhinitis–induced nasal obstruction more effectively than desloratadine.” Journal of Allergy and Clinical Immunology 127.6 (2011): 1515–1521.
  6. Sharma S, et al. “Asthma, allergy, and responses to methyl donor supplements and nutrients.” Journal of Allergy and Clinical Immunology 133.5 (2014): 1246–1254.
  7. Werbach MR. “Nutrients to Reduce Allergic Symptoms.” Townsend Letter for Doctors and Patients 215 (2001): 158.
  8. Yamprasert R, et al. “Ginger extract versus Loratadine in the treatment of allergic rhinitis: a randomized controlled trial.” BMC Complementary Medicine and Therapies 20 (2020): 1–11.
  9. Pareek A, et al. “Feverfew (Tanacetum parthenium L.): A systematic review.” Pharmacognosy Reviews 5.9 (2011): 103.
  10. Abdala-Valencia H, et al. “Inhibition of allergic inflammation by supplementation with 5-hydroxytryptophan.” American Journal of Physiology-Lung Cellular and Molecular Physiology 303.8 (2012): L642–L660.