PETASITES FOR PAIN AND INFLAMMATION

PETASITES FOR PAIN AND INFLAMMATION
© Dr Jillian Stansbury

There are between 15 and 20 species in the Petasites genus and all have been used for pain, inflammation, and allergic hyperreactivity. Petasites species are large-leaved, moisture-loving woodland plants native to temperate woodlands of northern Asia, Europe, and North America. Petasites species are sometimes referred to with the general name Sweet Coltsfoot, because of similarity to Tussilago. Petasites are in the Senecioneae Tribe of the Asteraceae family. Petasites hybridus, the most common Petasites species in the US goes by the common name Butterbur, reportedly as the large leaves were convenient to wrap and preserve fresh butter in root cellars of pioneer farms. Petasites japonica is found in Asia goes by the name Fuki in Japan, and Giant Butterbur and Bog Rhubarb in English speaking locales where it has become introduced. Petasites frigidus occurs in seasonal stream beds of the Pacific NW.

I have chosen to feature Petasites as it is often overlooked for its pain relieving effects. In the modern era, medical conferences devoted entirely to Petasites have taken place in Switzerland (such as one in Mar of 1996) for scientists to share their research on the plant. I first started employing Petasites for difficult types of pain such as for terminal cancer patients and for bone metastasis as suggested as such by RF Weiss in his book Herbal Medication. Anecdotally, I have found that Petasites helpful in reducing the need for other pharmaceuticals and sedatives, that in many cases may cause terminal patients to spend their last months’ heavily sedated, if not asleep and unable to spend time with their families. While you will not find published studies on Petasites for cancer or general pain, you will find numerous studies on the plant’s anti-inflammatory, anti-allergy, and anti-spasmodic effects, all possible contributors to an anodyne action. Petasites appears most specific for pain of the vasculature and for other smooth muscle spasms in hollow organs such as the bronchi, and to a lesser extent the ureters and possibly bladder.

ETYMOLOGY AND ETHNOBOTONICAL HISTORY
The word Petasites may derive from the Greek “petasos” referring to a hat of the variety that the Greek God Mercury is usually pictured wearing. Because of the large, almost umbrella-like leaves, Petasites indeed may have come in handy as a hat.
Both the leaves and the roots of Petasites species are used as medicines, with the roots reported to have stronger antispasmodic effects. Petasites has been used as a general anodyne in both European and Asian folklore and is reported as useful for asthma, allergies, hypertension, chest pain, migraine and vascular pain, and pain due to ulcers. Petasites was reportedly used during the middle ages for symptoms of the Plague. Petasites is used as a vegetable in Japan where folklore credits it’s consumption with anti-allergy and anti-inflammatory effects. The young spring stalks and growth are soaked in ashes or baking soda water to reduce the astringency, and then sliced and stir-fried with miso and spices to prepare a condiment to serve with soups and rice.

PETASITES CONSTITUENTS
Sesquiterpene lactones: Including Petasin, S-petasin, petasalbin, furanopetasin, petasinolides A and B, and furoeremophilone. Petasin is credited with an ability to affect calcium ion channels and promote vasodilation/relaxation. This action may lend Petasites a hypotensive and antispasmodic action. The ability to affect hemodynamics may also be another mechanism whereby Petasites can reduce migraines. Petasin and Isopetasin are isomers of one another and shown to have antispasmodic activity on smooth muscle, including vascular and bronchial wall muscle fibers. These constituents may also inhibit inflammatory leukotriene activity by affecting the metabolism of arachidonic acid. Anti-ulcer effects may be due to this mechanism, as well as inhibition of inflammatory vasoconstriction. The group of petasins and isopetasins found in Petasites include sulphur containing, and non-sulphur containing members. One of the most studied is S-petasin, a sulphur containing petasin. Petasin also inhibits DNA synthesis in cardiac and vascular smooth muscle.

OTHER PETASITES CONSTITUENTS

  • Eremophilan lactones are another group of compounds found in Petasites hybridus roots which, along with petasin, are credited with vasodilating effects. These compounds may also block calcium gated channels.
  • Pyrrolizidine alkaloids (PAs): Including senecionine, integerrimine, senkirkine, petasitine, and neopetasitine. The German Health Department recommends no more than 1 mcg per day of PAs. PA free preparations, such as “Petadolex” are available.
  • Caffeoylquinic acids of several types are found in many Petasites species. Caffeoyl moiety has a strong free radical scavenging and antioxidant capacity.
  • Fukinolic acid is the main holyphenolic compound found in Petasites named after the common name for P. japonicus, Fuki.
  • Essential oils extracted from Petasites albus include Euparin credited with moderate antioxidant action.
  • Bakkenolide, a constituent identified in Petasites tatewakianus is credited with neuroprotective activity and an ability to protect glucose and oxygen deprived cells from oxidative damage.

FOLKLORIC INDICATIONS
The folkloric literature appears to emphasize Petasites for tightness and spasm.
General Pain, muscle spasm
Asthma, bronchial spasm, Whooping Cough
Upper respiratory infections with spastic cough
Asthmatic Cough and Wheezing
Respiratory infections with fever
Urinary infections and irritations, urinary spasm
Biliary spasm, digestive and intestinal spasm
Uterine spasms and menstrual cramps
Migraines
Spinal Pain (“severe obstinate neuralgia in the small of the back” Maude Greive)
Ulcers and Ulcer Pain (the root “cureth all naughty filthy ulcers” Gerard, “when associated with vegative dystonia” RF Weiss.)
Cardiotonic – (“It is a great strengthener of the heart” Culpepper)

ANODYNE MECHANISMS OF ACTION
The Butterbur plant, Petasites hybridus has been used for centuries for all manner of painful and inflammatory conditions, and has also been found to be an anti-inflammatory by numerous mechanisms. Petasites inhibits cycooxygenase and inflammatory prostaglandin and may inhibit the formation of inflammatory leukotrienes. In particular the formation of peptido-leukotrienes released from macrophages has been noted from Petasites administration. Animal models of asthma have shown Petasites japonicus to inhibit the release of interleukins and tumor necrosis factor without evidence of cytotoxicity. Petasites has also been shown to have effects on mast cells. 1000 mg/kg are reported to reduce the release of histamine and leukotrienes from mast cells in animal studies as well as has been shown to reduce airway constriction typically induced by these substances.
It has been proposed that Petasites may reduce general oxidative stress in the body by normalizing blood lipids and upregulating liver detoxification pathways. Petasites has been shown to support the antioxidant enzyme systems of the liver including glutathione reductase, peroxidase, and transferases. Furthermore, Petasites has been shown to reduce total cholesterol and LDL and help normalize blood lipid profiles. By helping to reduce oxidative stress, Petasites can have neuroprotective and anti-seizural effects.

 
Petasites hybridus has a long history of use for migraine headaches and current research shows that Petasites may reduce inappropriate vasoconstriction via a mechanism that involves blocking calcium gated channels in the vasculature.  Petasites may also relax bronchoconstriction via activity at muscarinic sites. , and may reduce corticosterone release from the adrenal gland and inhibit cAMP driven enzyme activation, serving to deter contraction of smooth muscles. Animal studies have shown Petasites to reduce excessive contractility in heart muscle fibers due to the effects of S-petasin on intracellular calcium. In effect, Petasites could be said to be a negative chronotropic and inotroptic agent, as opposed to cardiac glycosides which are positive inotropic and chronotropic agents. Where cardiac glycosides such as Digitalis and Convallaria are indicated for heart failure, Petasites might be considered for hypertension, excessive vasoconstriction, and tachyarrhythmias and excitability. Asthma is improved by a similar mechanism, relaxing the smooth muscle of the airways via calcium channel inhibition. This also suggests that Petasites may be contraindicated in patients with cardiomyopathy, however, some of the folkloric literature suggests the plant to be a cardiotonic and no adverse side effects on the heart have been reported in the modern clinical trials.

PETASITES FOR MIGRAINES AND CHRONIC HEADACHES
Several reviews of nearly 300 research studies on various alternative non-steroidal therapies for migraine, place Petasites at top of the list as an effective natural option for reducing the frequency and severity of migraine headaches.  Several human clinical trials have demonstrated Petasites’ efficacy for migraine prevention. One randomized placebo controlled trial showed Petasites root extracts dosed at 25 mg twice daily to reduce migraine frequency by 45% in 4 weeks for those receiving the verum and by 15% in those receiving placebo. A similar study on adults with chronic headaches reported a 48% reduction in headaches with a 75 mg twice daily dosage of Petasites root in 4 months’ time. Another study on children and adolescents suffering with chronic headaches has been showed symptom improvement under the influence of Petasites. 91% of participants showed some improvements in frequency and severity of headaches and 77% demonstrated a 50% reduction in headaches . The most common side effect reported was eructations and no serious side effects or adverse events were reported.

PETASITES AND ALLERGIC AIRWAY DISEASES
Petasites has numerous anti-allergy effects explaining the folkloric use of the plants for asthma, spastic cough, and airway reactivity. Leukotriene synthesis in eosinophils and neutrophils is inhibited while elevated eosinophil and bloods nitric oxide levels are reduced. Petasites also inhibits cycloxygenase, an enzyme involve with the synthesis of inflammatory prostaglandins. Petasites japonicas is reported to reduce leukotriene and histamine-induced bronchoconstriction.
One clinical trial reported that Petasites alleviated symptoms of allergic rhinitis in a manner equal to anti-histamine pharmaceuticals , and another clinical trial showed a statistically significant reduction in symptoms of allergic rhinitis compared to placebo in as little as 7 days. Another human And yet another human clinical study showed that 50 mg of Petasites for just one week reduced the symptoms of allergic rhinitis equal to the prescription medicine fexofenadine.
One small human clinical trial on asthmatics reported Petasites hybridus root extracts to reduce the severity and frequency and duration of asthma attacks. In those using asthma medications and inhalers, 40% of study participants required less medication at the end of the 2 month study compared to baseline and improved spirometry readings could be demonstrated. A review of clinical trials on Petasites suggest efficacy for allergy and asthma that warrants further investigation.

PETASITES, PA’S AND HEPATOTOXICITY
There have been reports that Petasites hybridus may have hepatotoxic effects, as is the case with other plants noted to contain pyrollizidine alkaloids (PAs). Many plants of the Senecio tribe of the Asteraceae family are noted to contain PAs. PAs are highest in the stalks and rhizomes and lowest in the leaves. Products prepared by quality lab are recommended to insure that the PAs do not become abnormally elevated.
One study showed to signs of hepatocellular toxicity at blood levels of 69 nanograms per ml serum, a typical blood level with normal dosing. At 200 times this dosage, transient elevations in liver bilirubin and transaminases can be observed, which then returns to normal when the overdosing is withdrawn. Any potential liver irritation has been credited to petasin which is presently proposed to impair bile acid transport and liver and protein metabolism, but only at significantly above normal therapeutic dosages.

EXAMPLES OF THE TYPES OF PAIN THAT MAY RESPOND TO PETASITES

Formula for Migraine and Chronic Head Pain
A formula such as this one should be used several times a day for months to reduce the frequency and severity of chronic headaches.
Petasites 25 ml
Tanacetum 15 ml
Curcuma 10 ml
Hypericum 10 ml

Formula for Vascular Spasm Due to Inflammation
A formula such as this one may help allay pain due to tumors and vascular inflammation.
Petasites 15 ml
Aesculus 15 ml
Angelica 15 ml
Salvia miltiorrhiza 15 ml

Formula for Acute Anginal Coronary Spasm
Note that Petasites may be helpful for acute and episodic use in the treatment of angina, but that circulatory enhancing agents and cardiac glycosides, such as Convallaria, may be superior for long term trophorestorative and supportive therapy for heart failure patients.
Petasites 20 ml
Lobelia 20 ml
Gingko 10 ml
Allium 8 ml
Mentha EO 2 ml
2 tsp every 5 minutes, reducing as symptoms improve

Acute Chest Pain and Tightness
Wheezing and a tight heavy sensation in the chest will often respond to this formula. This is best used acutely with a separate protocol in place to help reduce allergic hyper-reactivity via diet, antioxidant supplements and long term herbal therapies.
Lobelia 18 ml
Petasites 18 ml
Angelica 10 ml
Gingko 10 ml
Eucalyptus essential oil 4 ml

Acute Spastic Cough
For cough variant asthma and for spastic coughing due to infections and bronchitis, this formula can be taken hourly, reducing as symptoms improve.
Petasites 15 ml
Lobelia 15 ml
Tussilago 10 ml
Thymus 10 ml
Foeniculum 8 ml
Eucalyptus EO 2 ml



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