Wise Mind Herbs

The information on this page has been prepared with reference to published scientific literature, not by a medically qualified expert. It is not medical advice. Any decision to use a supplement or herb-based product is your responsibility. Consult a suitably qualified medical professional, especially if you have underlying conditions. Remember, nothing is for everyone, and not everything sold is what it claims to be. Some things work for some people, some of the time.

Butterbur (Petasites hybridus)

Butterbur refers to plants in the genus Petasites (family Asteraceae), with the most commonly studied species for medicinal use being Petasites hybridus. Other species include Petasites japonicus and Petasites frigidus. Common names include common butterbur, sweet coltsfoot, pestilence wort, and bog rhubarb. It's important to note that butterbur should not be confused with coltsfoot (Tussilago farfara), which is a different plant in the same family with some similar properties but different chemical composition and safety profile.

Image source and license:https://commons.wikimedia.org/wiki/File:Petasites_hybridus_plants.jpg.
Modified by Peter Jorgensen.

Primary Active Components

The therapeutic effects of butterbur are primarily attributed to sesquiterpene esters called petasins (including petasin, isopetasin, and neopetasin). These compounds have demonstrated anti-inflammatory, anti-spasmodic, and analgesic properties. However, unprocessed butterbur also contains pyrrolizidine alkaloids (PAs), which are hepatotoxic and potentially carcinogenic. For this reason, commercially available preparations are typically PA-free extracts.

Evidence-Based Health Benefits

Scientific research has investigated butterbur's efficacy for several conditions, with varying levels of evidence:

• Migraine prophylaxis: The strongest evidence supports butterbur's use in preventing migraines. Multiple randomized controlled trials and meta-analyses have shown that standardized butterbur extract can reduce migraine frequency by 50-60% in responsive patients
• Allergic rhinitis: Several clinical trials indicate butterbur extract is comparable to conventional antihistamines in reducing symptoms of hay fever without causing drowsiness
• Asthma: Limited evidence suggests butterbur may help reduce asthma symptoms by relaxing bronchial smooth muscles, though studies are preliminary
• Urinary tract disorders: Some research indicates butterbur may help with urinary tract spasms due to its antispasmodic effects

Dosage Recommendations

Clinical studies have used the following doses for standardized, PA-free butterbur extracts:

• Migraine prevention: 50-75 mg twice daily of an extract standardized to contain 15% petasins.
• Allergic rhinitis: 50 mg twice daily of extract standardized to contain 7.5 mg of petasin per tablet.
• Children (age 6-17) for migraine: Reduced dosages of 25-50 mg twice daily based on weight have been used in pediatric studies.

Most clinical trials have not evaluated doses significantly above these ranges. Limited pharmacokinetic studies suggest a plateau effect may occur at higher doses, but there are significant knowledge gaps regarding optimal dosing, particularly for long-term use. No studies have systematically evaluated doses more than double these recommendations.

Side Effects and Safety Concerns

Properly processed butterbur extracts that are certified PA-free have demonstrated a relatively good safety profile in clinical trials, but several concerns exist:

• Gastrointestinal effects: The most common adverse effects include mild nausea, eructation (belching), and gastric discomfort.
• Liver toxicity: This is primarily a concern with preparations containing pyrrolizidine alkaloids. Several cases of severe hepatotoxicity have been reported with butterbur products, particularly those without proper PA removal or testing.
• Allergic reactions: As a member of the Asteraceae family, butterbur may cause allergic reactions in individuals sensitive to plants in this family (including ragweed, chrysanthemums, and daisies).
• Headache, drowsiness, fatigue, and itchy eyes have been reported in some patients.

Due to safety concerns, health authorities in some countries have restricted or removed butterbur products from the market. The UK's Medicines and Healthcare products Regulatory Agency (MHRA) suspended butterbur product licenses in 2012 due to concerns about PA content. Similarly, Health Canada has issued warnings about potential liver toxicity.

Contraindications

• Pregnancy and breastfeeding: Butterbur is contraindicated due to insufficient safety data and theoretical risks from remaining alkaloids.
• Liver disease: Individuals with liver impairment should avoid butterbur.
• Children under 6 years: Limited safety data exists for young children.
• Allergies to Asteraceae family plants.

Commercial Pharmaceutical Products

• Petadolex®: A proprietary PA-free extract standardized to contain 15% petasins, manufactured by Weber & Weber. It has been used in multiple clinical trials for migraines.
• Tesalin®: A standardized extract used primarily in Europe for allergic rhinitis.

Currently, no synthetic homologues based on petasins have reached the pharmaceutical market, though research into potential derivatives continues.

Knowledge Gaps and Research Needs

Despite promising results, several important knowledge gaps remain:

• Long-term safety: Most studies have lasted 4-6 months, with limited data on safety beyond this period.
• Standardization issues: Variable preparation methods and inconsistent standardization make comparing studies difficult.
• Mechanism of action: While anti-inflammatory effects are documented, the precise mechanisms for migraine prevention remain incompletely understood.
• Drug interactions: Limited data exists on potential interactions with common medications.

Conclusion

Butterbur extract, specifically PA-free preparations standardized for petasin content, shows promising evidence for migraine prophylaxis and allergic rhinitis. However, concerns about product quality, potential hepatotoxicity, and limited long-term safety data warrant caution. Patients should only use certified PA-free products under healthcare provider supervision and should be aware of the varying regulatory status across different countries.

References

Apostolova, S., Oreshkova, T., Uzunova, V., Georgieva, I., Maslenkova, L., & Tzoneva, R. (2023). A standardized extract of Petasites hybridus L., containing the active ingredients petasins, acts as a pro-oxidant and triggers apoptosis through elevating of NF-κB in a highly invasive human breast cancer cell line. Frontiers in Bioscience-Landmark, 28(6), 111.

Blosa, M., Uricher, J., Nebel, S., Zahner, C., Butterweck, V., & Drewe, J. (2021). 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, 14(3), 180.

Borlak, J., Diener, H. C., Kleeberg-Hartmann, J., Messlinger, K., & Silberstein, S. (2022). Petasites for migraine prevention: new data on mode of action, pharmacology and safety. A narrative review. Frontiers in neurology, 13, 864689.

Coşkun, Z. Ö., Muluk, N. B., Cosan, D. T., & Cingi, C. E. M. A. L. (2023). Efficacy of butterbur in allergic rhinitis: a cell culture study. European Review for Medical & Pharmacological Sciences, 27.

Kleeberg-Hartmann, J., Vogler, B., & Messlinger, K. (2021). Petasin and isopetasin reduce CGRP release from trigeminal afferents indicating an inhibitory effect on TRPA1 and TRPV1 receptor channels. The Journal of Headache and Pain, 22, 1-14.

Kulinowski, Ł., Luca, S. V., Minceva, M., & Skalicka-Woźniak, K. (2022). A review on the ethnobotany, phytochemistry, pharmacology and toxicology of butterbur species (Petasites L.). Journal of Ethnopharmacology, 293, 115263.