Butterbur supplement extract, side effects, herb used for allergy and migraine, review of research studies, how well does it work? by Ray Sahelian, M.D.
December 20 2014

The butterbur plant (Petasites hybridus) is a shrub found throughout Europe as well as parts of Asia and North America. Butterbur that has been used medicinally for centuries to treat cough, asthma, and inflammatory diseases. The butterbur plant can grow to a height of three feet and is usually found in wet, marshy ground, in damp forests, and adjacent to rivers or streams.

Active ingredients in butterbur extract
Petasin, a kind of sesquiterpene ester, appears to be a major active compound of
butterbur extract. It has inhibitory activities on leukotriene generation in eosinophils and neutrophils. This indicates that it may have anti-inflammatory and anti-allergy properties although butterbur does not seem to be effective in blocking histamine release. Butterbur also helps reduce smooth muscle spasm.

Petadolex Buy Butterbur extract 60 Softgels - Enzymatic Therapy

Petadolex contains the patented extract of
Petasites hybridus, that supports healthy blood vessel tone in the brain, as well as normal blood flow in the brain. Butterbur has been the subject of several placebo-controlled clinical studies.

Petadolex is standardized to contain 15% of butterbur's key ingredient, petasin. It's also guaranteed to be pyrrolizidine alkaloid free, so you can use it with confidence. Pyrrolizidine alkaloids are toxic compounds that can harm the liver. Studies demonstrate patented Petadolex is safe and well tolerated.


Buy Butterbur supplement extract
Supplement Facts:
Purple Butterbur (Petasites hybridus) 50 mg pill
    (Petadolex brand) Root Extract standardized to contain 7.5 mg petasins

Recommendations: One butterbur softgel three times daily, or 2 softgels 2 times daily for the first four weeks. Thereafter, one softgel twice daily.

Butterbur safety and side effects, risks, toxicity
Butterbur has not been studied extensively enough to determine its side effects or toxicity profile, but there appears to be some early concerns that would cautions me from recommending its use for more than 2 weeks at a time without a break.

Safety of a patented special butterbur root extract for migraine prevention.
Headache. 2003.
To report on the safety of a patented special butterbur root extract used for migraine prevention. Two placebo-controlled clinical trials have been conducted supporting the beneficial use in humans. The patented special butterbur root extract is safe for treatment in humans.

Q. I have been doing some of my own research on Butterbur (Petasites hybridus). I have also come across numerous warnings from websites in the UK that butterbur can seriously harm your liver and even cause cancer. Since 2012 the UK has warned people not to take it. Even when the PA ( dangerous ingredient) has been taken out the report says :"Butterbur products have been associated with cases of liver toxicity; 40 cases have been reported in the literature. Of these cases, nine were of acute hepatitis and two of the nine cases resulted in liver failure requiring transplantation. The cases of liver toxicity appear to have occurred with extracts of butterbur where the PAs had been removed and only small amounts remained. There is some evidence that other constituents found in butterbur such as the sesquiterpene constituents for example petasin may be implicated in the liver toxicity. This is what it says, "Butterbur contains pyrrolizidine alkaloids (PAs) which studies have shown can result in serious liver damage and organ failure. PAs have also been shown to lead to cancer in animals. Butterbur is most commonly used to treat migraine and hayfever. Butterbur products have been associated with cases of liver toxicity; 40 cases have been reported in the literature. Of these cases, nine were of acute hepatitis and two of the nine cases resulted in liver failure requiring transplantation. The cases of liver toxicity appear to have occurred with extracts of butterbur where the PAs had been removed and only small amounts remained. There is some evidence that other constituents found in butterbur such as the sesquiterpene constituents for example petasin may be implicated in the liver toxicity."
   A. There have been such reports in the medical literature.

Forsch Komplementarmed Klass Naturheilkd. 2003. The common butterbur (Petasites hybridus)--portrait of a medicinal herb]. For hundreds of years butterbur (Petasites hybridus) has been used against many diseases. Modern indications are the prophylaxis of migraine, tension headache, spasms of the urogenital tract, gastro-intestinal tract and bile duct and hopefully hay fever and asthma in the near future. The petasines, the main components of butterbur, inhibit the synthesis of leucotrienes and decrease the intracellular concentration of calcium which explains the anti-inflammatory and spasmolytic properties of extracts of butterbur. Thanks to extraction with supercritical CO(2) the concentrations of the potentially hepatotoxic and carcinogenic pyrrolizidine alkaloids lie below the detection limits. Until now four cases of a reversible cholestatic hepatitis have been probably associated with long-term administration of butterbur (incidence of 1:175.000). It is unknown which components of butterbur are responsible for the long-term hepatotoxicity. Further side effects involve the gastrointestinal tract and are usually mild.

Butterbur Dosage and recommended use
Typically, extracts are standardized to contain a minimum of 7.5 mg of petasin and isopetasin. The adult dosage ranges from 50-100 mg twice daily with meals.

Medical uses

Allergies and Allergic Rhinitis

may be helpful for allergic rhinitis although the research thus far with butterbur leading to relief of allergies has not been consistent. Most, but not all, studies support the use of butterbur for allergic rhinitis. See allergy for more information.

Butterbur was found to be no more effective than placebo at relieving symptoms of intermittent allergic rhinitis, more commonly known as hay fever. However, lead author Dr. Brian J. Lipworth of the University of Dundee in Scotland found that the herb was more effective than placebo and as effective as the allergy drug Allegra (fexofenadine) at treating year-round allergic rhinitis. Petasin has been shown to block leukotrienes, substances that are thought to play a role in lung inflammation. Petasin has also been shown to inhibit compounds called histamines that are released by the immune system during allergic reactions. Dr. Brian Lipworth compared butterbur to placebo in 35 men and women with seasonal allergies to grass pollen for 2 weeks. Symptoms did not improve significantly in people taking butterbur or the placebo. There were also no significant differences in quality of life or nasal air flow. Despite the lack of a significant effect, the researchers did detect signs that butterbur may have been more helpful than placebo for people with the most severe symptoms. Lipworth's team speculates that the herb may have real benefits for people with severe allergy symptoms. Neither treatment caused serious side effects. Annals of Allergy, Asthma and Immunology, 2004.

Treating intermittent allergic rhinitis: a prospective, randomized, placebo and antihistamine-controlled study of Butterbur extract Ze 339.
Phytotherapy Research. 2005.
Butterbur extract (Ze 339; 8 mg total petasine; one tablet thrice-daily), fexofenadine (Telfast 180, one tablet once-daily) and placebo was given to 330 patients. Both active treatments were individually significantly superior to placebo in improving symptoms of allergic rhinitis, while there were no differences between the two active treatments. Butterbur and Fexofenadine are comparably efficacious relative to placebo.

Butterbur Ze339 for the treatment of intermittent allergic rhinitis: dose-dependent efficacy in a prospective, randomized, double-blind, placebo-controlled study.
Arch Otolaryngol Head Neck Surg. 2004.
One hundred eighty-six patients were randomized (Butterbur Ze339 high dose, 60; low dose, 65; and placebo, 61 patients). Established diagnostic criteria for intermittent allergic rhinitis were confirmed by skin allergy tests in all patients. High-dose butterbur group, 1 tablet 3 times daily; low-dose group, 1 tablet twice daily; or matching placebo. All groups were treated for 2 consecutive weeks. Butterbur Ze339 is an effective treatment for intermittent allergic rhinitis symptoms and is well tolerated.

Effects of butterbur treatment in intermittent allergic rhinitis: a placebo-controlled evaluation.
Ann Allergy Asthma Immunol. 2004.
Petasites hybridus contains the active ingredient petasin, which exhibits antileukotriene and antihistamine activity. Previous studies of intermittent allergic rhinitis have demonstrated a comparable response to butterbur compared with a histamine H1-receptor antagonist on the 36-Item Short-Form Health Survey quality-of-life score. In our study, there was no significant clinical efficacy of butterbur use vs placebo use on objective and subjective outcomes in intermittent allergic rhinitis. Further studies are now indicated to investigate the use of butterbur in persistent allergic rhinitis.

A placebo-controlled evaluation of butterbur and fexofenadine on objective and subjective outcomes in perennial allergic rhinitis.
Clinical Exp Allergy. 2004.
Sixteen patients with perennial allergic rhinitis and house dust mite sensitization were randomized in double-blind cross-over fashion to receive for 1 week either
Butterbur 50 mg twice daily, FEX 180 mg once daily and placebo once daily, or placebo twice daily. Butterbur and FEX, in comparison to placebo, were equally effective in attenuating the nasal response to AMP and in improving nasal symptoms, highlighting a potential role for butterbur in the treatment of allergic rhinitis.

Asthma / bronchitis
Various parts of the
butterbur plant have been used for centuries to treat bronchial asthma and whooping cough. Butterbur's possible effectiveness in treating respiratory disorders such as asthma and bronchitis is attributed to the antispasmodic and anti-inflammatory properties of the petasin constituent.

Petasites hybridus root extract in the treatment of asthma - an open trial.
Danesch UC. Alternative Medicine Reviews. 2004.
The efficacy and tolerability of a butterbur root extract (Petadolex) for the treatment of asthma was analyzed. Subjects included 64 adults and 16 children / adolescents treated for two months with the extract, followed by two months during which the intake of the extract was optional. Concomitant asthma medication was permitted. The number, duration, and severity of asthma attacks decreased, while peak flow, forced expiratory volume (FEV1), and all measured symptoms improved during therapy. In addition, more than 40 percent of patients using asthma medications at baseline reduced intake of these medications by the end of the study.

Asthma benefit
Butterbur, a herbal remedy, confers complementary anti-inflammatory activity in asthmatic patients receiving inhaled corticosteroids.
Clin Exp Allergy. 2004.
We evaluated the effects of butterbur, given as add-on therapy patients with asthma maintained on inhaled corticosteroids, assessing adenosine monophosphate  bronchoprovocation along with other surrogate inflammatory markers such as serum eosinophil cationic protein and peripheral blood eosinophil count. Chronic dosing conferred complementary anti-inflammatory activity in atopic asthmatic patients maintained on inhaled corticosteroids.

Migraine Headache
Complement Ther Clin Pract. February 2014. Butterbur extract: Prophylactic treatment for childhood migraines. In order to decrease the impact of the condition on the child and the family, prophylactic treatment is recommended if the child is experiencing disabling migraines. The medications currently prescribed for the prevention of pediatric migraines often have significant side effects and are of questionable therapeutic value. For those patients and parents who are interested in alternative therapies and natural remedies for preventive treatment of pediatric migraines, butterbur extract derived from the butterbur plant, Petasites hybridus, has emerged as a promising treatment.

Two clinical studies using 50 mg and 75 mg of a standardized butterbur extract twice daily for 12 weeks demonstrated its effectiveness as a prophylactic treatment for migraines. When used to treat migraines, administration is prophylactic and supplementation should be carried out daily for a few weeks and then tapered until migraine incidence begins to increase. Butterbur may work by preventing peptidoleukotriene biosynthesis.

An article published in the December 2004 issue of Neurology reports a study that compared butterbur with an inactive placebo. Researchers compared the effectiveness of two different doses of butterbur extract in about 230 migraine patients who had experienced two to six attacks per month for the 3 months prior to the study. The number of migraine headache attacks per month was reduced by 45 percent in the group that took 75 milligrams of butterbur twice daily, compared with a reduction of 28 percent in the placebo group during the 16-week trial. A group that took 50 milligrams of butterbur twice daily experienced a 32 percent decrease, not significantly different from placebo. The butterbur extract was well tolerated, the team reports, with burping as the only adverse event occurring more frequently in the active treatment groups. There were no changes in blood pressure, heart rate, or routine laboratory tests.
    My comments: As with many herbs and medicines, it is likely that some users will find butterbur reduces the severity or frequency of their migraine headache, whereas others may not find it to be helpful. How butterbur interacts with standard pharmaceutical medicines -- such as beta blockers or triptans -- used for prevention or treatment of migraines is currently not known.

Petasites hybridus root is an effective preventive treatment for migraine.
Neurology. 2004.
This is a three-arm, parallel-group, randomized trial comparing butterbur extract 75 mg bid, 50 mg bid, or placebo bid in 245 patients with migraine. Eligible patients met International Headache Over 4 months of treatment, migraine attack frequency was reduced by 48% for butterbur extract 75 mg bid, 36% for 50 mg bid, and 26% for the placebo group. The most frequently reported adverse reactions considered possibly related to treatment were mild gastrointestinal events, predominantly burping. Butterbur 50 mg PO bid was not significantly more effective than placebo on the primary study endpoints.

Dr. Sahelian, I would like to thank you. I was having migraines several times a month, some lasting days, and nothing I took helped substantially, including feverfew, 5HTP, and Imitrex. I have now been taking butterbur for two months, and I had had only two mild headaches in the first month (I don't think either lasted more than 1 or 2 hours) and none in the last month. I am going to taper my dose a bit, as is recommended, since I've been taking the highest dose. It has been a lifesaver. I am taking Solaray, Butterbur Extract, 50 mg, 60 Veggie Caps.

Gastrointestinal Disorders
A German study found extracts of
butterbur blocked ethanol-induced gastric damage and reduced ulcerations of the small intestine caused by indomethacin, an anti-inflammatory drug used to treat arthritic conditions. The results of this study were attributed to inhibition of lipoxygenase activity and leukotriene biosynthesis.

Interactions with medications
Could you tell me if butterbur pills interfere with warfarin also known as Coumadin used for blood thinning?
    I have not seen such combination studies, so I don't know. Warfarin is a potentially dangerous medication and one has to be careful when combining it with other medications and supplements.