Rhizome
The underground stem, preferably fresh; root extracts are favored.
Rhizome
Petasites hybridus (L.) Gaertn. (Asteraceae) — a plant of European stream banks whose rhizome extract, stripped of its toxic pyrrolizidine alkaloids, is studied for migraine prevention and allergic rhinitis. Its petasins are the active compounds, and the unprocessed plant is a genuine liver hazard.
At flowering, butterbur stands 20 to 50 cm tall, with brown-bracted flower heads and reddish tubular flowers that smell faintly of vanilla. After flowering it grows to about 1 m, with very large heart-shaped basal leaves, toothed, hairy underneath, on a foul-smelling stalk. It grows on stream banks and in wet, marshy ground.
The genus name comes from the Greek petasos, a broad-brimmed felt hat, for the plant's huge leaves. Those leaves were used to wrap butter, which gave butterbur its English name.
European herbalists relied on it for centuries: in the Middle Ages against plague and fever, and in the 17th century for cough, asthma and skin wounds. Its traditional uses rest mainly on its antispasmodic action.
Modern research turned to a standardized root extract, with placebo-controlled trials in migraine prevention and a head-to-head trial in hay fever. 5239
⚠ Alkaloid-Free Extracts Only
The raw plant contains liver-toxic pyrrolizidine alkaloids. Only extracts processed to remove them are appropriate for use. 15
The eremophilane sesquiterpene esters behind butterbur's activity, and the alkaloids that must be removed.
Angelic-acid esters of petasol. Petasin is the best-known compound of the root, and the extract is standardized to it. 1
The antimigraine component of butterbur. It activates TRPA1 channels on pain-sensing nerves and then desensitizes them. 6
The S-methylacrylic acid esters: S-petasine, neo-S-petasine and iso-S-petasine, alongside fukinone and bakkenolide.
Senecionine, integerrimine and senkirkine occur in traces, but they are hepatotoxic and genotoxic, and are removed from medicinal extracts. 15
The rhizome is used, and only as a standardized extract free of pyrrolizidine alkaloids.
The underground stem, preferably fresh; root extracts are favored.
Rhizome
Rhizome extract standardized to petasin and isopetasin, with the pyrrolizidine alkaloids removed.
Standardized Extract
Extracts must contain less than 1 microgram of pyrrolizidine alkaloids per daily dose.
Alkaloid-Free
Teinture-mère of the whole plant, for which root extracts are preferred.
Liquid Extract
Butterbur is taken as an alkaloid-free standardized extract, twice a day with meals.
Sesquiterpene esters carry the pharmacology, and traces of toxic alkaloids set the safety limits.
Relaxes smooth muscle, and the effect is stronger than that of papaverine.
Probably inhibits leukotriene synthesis and both COX-1 and COX-2. 1
A special root extract at 50 to 75 mg twice daily reduced migraine in trials. 235
Isopetasin activates TRPA1 on peptidergic nociceptors and then desensitizes them. 6
The extract blocks cyclooxygenases, lipoxygenases and phospholipase A2, acts on TRPA1 and TRPV1, and lowers CGRP release from meningeal nerves. 7
Inhibits vasoconstrictive leukotrienes without affecting cyclooxygenase; isopetasin shows this activity and petasin does not. 8
Helps loosen bronchial secretions in cough and hoarseness.
Increases urine output and sweating.
Soothes pain and tension in functional neurodystonia.
An open study with a special root extract covered children and adolescents. 4
Pyrrolizidine alkaloids damage the liver and act through genotoxic mechanisms. 15
Butterbur extract is studied mainly for migraine prevention and allergic rhinitis, with a long traditional use for spasms.
Butterbur's petasins act on pain-sensing nerves and on leukotriene pathways.
Isopetasin activates TRPA1 channels, which first excites neuropeptide-containing nociceptors and is then followed by their desensitization. 6
The extract inhibits cyclooxygenases, lipoxygenases and phospholipase A2, acts on TRPA1 and TRPV1, and reduces CGRP release from meningeal afferents during attacks. 7
Isopetasin inhibits vasoconstrictive leukotrienes without touching cyclooxygenase, giving the gastroprotective effect. 8
Petasin takes part in the anti-inflammatory activity of the extract, probably through leukotriene and COX inhibition. 1
Unprocessed butterbur can injure the liver, so only alkaloid-free extracts are used, and never in pregnancy.