Butterbur

• How It Works

  Butterbur extracts have been shown effective in the treatment of migraines and allergies.

  Butterbur is an herb native to Europe, Southwestern Asia, and North Africa. It has been used to treat allergies, asthma, headache, and muscle spasms. Butterbur was shown in clinical studies to be effective for migraines, allergic rhinitis (inflammation of the mucus membranes of nose marked by runny nose, congestion, itching, and sneezing) and asthma.

• Purported Uses
  • Allergic rhinitis
    Butterbur was shown to have benefits for allergic rhinitis.
  • Migraine
    Current evidence indicates that butterbur extract is effective against migraine.
  • Asthma
    A few studies showed that butterbur may benefit those with asthma.
• Do Not Take If
  • You are hypersensitive to butterbur.
  • You have liver disease or dysfunction because some compounds present in butterbur can be damaging to the liver.
• Brand Name

  ZE 339 (a standardized carbon dioxide extract of butterbur that contains 8mg petasine, Petadolex

• Scientific Name

  Petasites hybridus

• Clinical Summary

  Butterbur is an herb native to Europe, Southwestern Asia, and North Africa, the leaf and root extracts of which have been used to treat allergies, bronchial asthma, headache, pain, and muscle and urinary tract spasms. Petasins, the sesquiterpene compounds found in butterbur, are thought to be the active constituents ^{(1) (2) (3)}.

  Leaf and root extracts of butterbur are effective in controlling migraines in adults and in children ^{(4) (5) (6) (17) (19)}, and asthma ⁽⁷⁾. Butterbur extract may also be effective against somatoform disorders ⁽²⁰⁾.
  But results from studies on allergic diseases are mixed. Some studies suggest that the efficacy of butterbur extract for allergic rhinitis is comparable to standard antihistamine drugs ^{(8) (9) (10)}, but conflicting data indicate that it is no better than placebo for intermittent rhinitis ⁽¹¹⁾ or for allergic skin disease ⁽¹²⁾. A systematic review of trials suggests the need for more rigorous studies before recommending use of butterbur ⁽¹³⁾.

  Raw butterbur extracts may contain excessive pyrrolizidine alkaloids that can cause hepatotoxicity ⁽¹⁴⁾.

• Purported Uses
  • Allergic rhinitis
  • Asthma
  • Migraine
• Mechanism of Action

  Sesquiterpene petasin inhibits leukotriene and histamine activities, and is thought responsible for butterbur’s anti-inflammatory and antiallergic effects ⁽¹⁵⁾. Petasins were also shown to have calcium channel blocking effects ⁽¹⁸⁾ making them effective for migraine prophylaxis ⁽¹⁾. The vasorelaxation effects of petasin may be via direct Ca(2+) antagonism of L-type voltage-dependent Ca(2+) channel (VDCC) in vascular smooth muscle ⁽²¹⁾.

  In another study, a butterbur extract showed dose-dependent inhibition effect on cyclooxygenase (COX2) and prostaglandin E2 in vitro that was not correlated to the petasin content ⁽¹⁶⁾.

• Contraindications
  • Hypersensitivity to butterbur
  • Patients with liver disease or dysfunction should avoid raw butterbur extract with pyrrolizidine alkaloids due to potential for hepatotoxicity ⁽¹⁴⁾.
• References

  1. Thomet OA. Wiesmann UN, Schapowal A, et al. Role of petasin in the potential anti-inflammatory activity of a plant extract of petasites hybridus. Biochem Pharmacol 2001;61(8):1041-7.

  2. Thomet OA, Simon HU. Petasins in the treatment of allergic diseases: results of preclinical and clinical studies. Int Arch Allergy Immunol 2002;129(2):108-12.

  3. Saritas Y, von Reuss SH, Konig WA. Sesquiterpene constituents in Petasites hybridus. Phytochemistry 2002;59(8):795-803.

  4. Diener HC, Rahlfs VW, Danesch U, The first placebo-controlled trial of a special butterbur root extract for the prevention of migraine: reanalysis of efficacy criteria. Eur Neurol 2004;51(2):89-97.

  5. Grossman W, Schmidramsl H. An extract of Petasites hybridus is effective in the prophylaxis of migraine. Altern Med Rev 2001;6(3):303-10.

  6. Lipton RB, Gobel H, Einhaupl KM, et al. Petasites hybridus root (butterbur) is an effective preventive treatment for migraine. Neurology 2004;63(12):2240-4.

  7. Danesch UC. Petasites hybridus (Butterbur root) extract in the treatment of asthma—an open trial. Altern Med Rev 2004;9(1):54-62.

  8. Schapowal A: Petasites Study Group. Randomised controlled trial of butterbur and cetirizine for treating seasonal allergic rhinitis. BMJ 2002;324(7330):144-6.

  9. Schapowal A. 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. Dec 2004;130(12):1381-1386.

  10. Schapowal A: A Study Group. Treating intermittent allergic rhinitis: a prospective, randomized, placebo and antihistamine-controlled study of Butterbur extract Ze 339. Phytother Res 2005;19(6):530-7.

  11. Gray RD, Haggart K, Lee DK, Cull S, Lipworth BJ. Effects of butterbur treatment in intermittent allergic rhinitis: a placebo-controlled evaluation. Ann Allergy Asthma Immunol. Jul 2004;93(1):56-60.

  12. Jackson CM, Lee DK, Lipworth BJ. The effects of butterbur on the histamine and allergen cutaneous response. Ann Allergy Asthma Immunol. Feb 2004;92(2):250-254.

  13. Agosti R, Duke RK, Chrubasik JE, Chrubasik S. Effectiveness of Petasites hybridus preparations in the prophylaxis of migraine: a systematic review. Phytomedicine. Nov 2006;13(9-10):743-746.

  14. Wildi E, Langer T, Schaffner W, Buter KB. Quantitative analysis of petasin and pyrrolizidine alkaloids in leaves and rhizomes of in situ grown Petasites hybridus plants. Planta Med. Apr 1998;64(3):264-267.

  15. Thomet OA, Schapowal A, Heinisch IV, Wiesmann UN, Simon HU. Anti-inflammatory activity of an extract of Petasites hybridus in allergic rhinitis. Int Immunopharmacol. Jun 2002;2(7):997-1006.

  16. Fiebich BL, Grozdeva M, Hess S, et al. Petasites hybridus extracts in vitro inhibit COX-2 and PGE2 release by direct interaction with the enzyme and by preventing p42/44 MAP kinase activation in rat primary microglial cells. Planta Med. Jan 2005;71(1):12-19.

  17. Sun-Edelstein C, Mauskop A. Foods and supplements in the management of migraine headaches. Clin J Pain. 2009 Jun;25(5):446-52. Review.

  18. Sheykhzade M, Smajilovic S, Issa A, et al. S-petasin and butterbur lactones dilate vessels through blockage of voltage gated calcium channels and block DNA synthesis. Eur J Pharmacol. 2008 Sep 28;593(1-3):79-86.

  19. Oelkers-Ax R, Leins A, Parzer P, et al. Butterbur root extract and music therapy in the prevention of childhood migraine: an explorative study. Eur J Pain. 2008 Apr;12(3):301-13.

  20. Melzer J, Schrader E, Brattström A, Schellenberg R, Saller R. Fixed herbal drug combination with and without butterbur (Ze 185) for the treatment of patients with somatoform disorders: randomized, placebo-controlled pharmaco-clinical trial. Phytother Res. 2009 Sep;23(9):1303-8.

  21. Wang GJ, Lin YL, Chen CH, et al. Cellular calcium regulatory machinery of vasorelaxation elicited by petasin. Clin Exp Pharmacol Physiol. 2010 Mar;37(3):309-15.

  22. Aydın AA, Letzel T. Simultaneous investigation of sesquiterpenes, pyrrolizidine alkaloids and N-oxides in Butterbur (Petasites hybridus) with an offline 2D-combination of HPLC-UV and LC-MMI-ToF-MS. J Pharm Biomed Anal. 2013 Jun 28;85C:74-82.