butterbur

Action and Spectrum

Actions and Spectrum: 

butterbur (Petasites hybridus) is a perennial shrub native to Europe and Asia, used for centuries for various medicinal purposes. butterbur extract is made from the plant’s roots, leaves, and stems and has been studied for potential therapeutic benefits. 

Action: butterbur extract is thought to have several actions, including anti-inflammatory, antispasmodic, and anti-allergic properties. It has been used to treat various conditions, including migraines, hay fever, asthma, and allergies. butterbur is believed to work by inhibiting the production of inflammatory chemicals called leukotrienes and histamines, which are involved in allergic reactions. 

Spectrum: butterbur has been studied for its effectiveness in treating various conditions, including: 

• Migraines: Several studies have shown that butterbur extract can reduce the frequency and severity of migraines. 
• Hay fever: butterbur extract has been shown to reduce hay fever symptoms, including sneezing, runny nose, and itchy eyes. 
• Asthma: butterbur extract may help to reduce inflammation in the airways and improve lung function in people with asthma. 
• Allergies: butterbur extract may help to reduce symptoms of allergic rhinitis, including sneezing, runny nose, and itchy eyes. 

Drug Interaction

Adverse Reaction

Black Box Warning

Black Box Warning: 

butterbur extract has been associated with liver toxicity in rare cases, which has led to the issuance of a black box warning by the United States Food and Drug Administration (FDA).  

The black box warning for butterbur extract states that it has been associated with cases of liver injury, including hepatitis and liver failure, in some people. The warning advises healthcare providers to monitor liver function in people taking butterbur extract and to discontinue use if signs of liver damage occur. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

butterbur extract has several contraindications that should be considered before use: 

• Pregnancy and breastfeeding: There is not enough information about the safety of butterbur extract during pregnancy and breastfeeding. Therefore, it should not be used by pregnant or breastfeeding women. 
• Allergy to ragweed, marigolds, daisies, or related plants: butterbur extract may cause an allergic reaction in people allergic to these plants. 
• Liver disease: butterbur extract has been associated with rare cases of liver toxicity, and therefore, it should be avoided in people with liver disease. 
• Medications that affect liver function: butterbur extract may interact with medications that affect liver function, such as acetaminophen, and therefore, it should be used with caution in people taking these medications. 
• Children: The safety of butterbur extract in children has yet to be established, and therefore, it should be avoided in children. 
• Surgery: butterbur extract may increase the risk of bleeding during and after surgery, and therefore, it should be stopped at least two weeks before surgery. 

Caution 

butterbur extract has several cautions that should be considered before use: 

• Side effects: butterbur extract may cause side effects such as upset stomach, headache, and drowsiness in some people. If you experience these side effects, stop using butterbur extract and talk to your healthcare provider. 
• Quality control: The quality of butterbur extract supplements may vary; some supplements may contain contaminants or other harmful substances. Therefore, it is crucial to choose a reputable brand that has been third-party tested for quality and purity. 
• Dosing: The optimal dose of butterbur extract has yet to be established. Therefore, following the dosing instructions on the supplement label or as a healthcare provider recommends is essential. 
• Duration of use: The safety of long-term use of butterbur extract has yet to be established, and therefore, it should be used for short-term treatment of symptoms. 
• Interactions with medications: butterbur extract may interact with blood thinners, antihistamines, and chemotherapy drugs. Therefore, you must talk to your healthcare provider before taking butterbur extract if you are taking any medications. 
• Allergies: Although butterbur extract effectively reduces allergy symptoms, it may cause an allergic reaction in some people. Therefore, it is crucial to stop using butterbur extract and talk to your healthcare provider if you experience any symptoms of an allergic reaction. 

Pregnancy / Lactation

Pregnancy consideration:  

Pregnancy Category: N/A 

Lactation: N/A 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/later trimester.        
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women        
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.       
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.        
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.        
• Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

The pharmacology of butterbur has yet to be fully understood, but it is thought to be related to its active compounds, which include petasin and isopetasin. These compounds are believed to have anti-inflammatory, antioxidant, and antispasmodic effects. 

butterbur extract has been shown to inhibit the production of inflammatory cytokines, such as TNF-alpha and interleukin-6, and to reduce the activation of inflammatory cells, such as mast cells and eosinophils. These effects may contribute to the anti-inflammatory and anti-allergic properties of butterbur extract. 

butterbur extract has also been shown to have calcium channel-blocking properties, which may contribute to its ability to reduce migraine headaches and relieve smooth muscle spasms in the respiratory and urinary tracts. 

Pharmacodynamics: 

Mechanism of action: The action of this substance is attributed to its component Petasin, a sesquiterpene ester that exhibits leukotriene inhibitory function. Clinical studies have demonstrated that it is effective in alleviating hay fever symptoms, with similar efficacy to fexofenadine. Moreover, it is more effective than a placebo in preventing migraine attacks. 

Pharmacokinetics: 

Absorption 

It is believed that butterbur extract is absorbed in the small intestine, but the exact mechanisms of absorption still need to be better understood. 

Distribution 

It is not clear where butterbur extract is distributed in the body, but it has been detected in the brain and liver of rats. 

Metabolism 

butterbur extract is metabolized in the liver by enzymes such as cytochrome P450. The active compounds petasin and isopetasin are metabolized into their respective hydroxylated metabolites. 

Elimination and Excretion 

The excretion of butterbur extract and its metabolites is primarily through fecal elimination. In rats, most of the administered dose was eliminated in the feces within 48 hours. 

Adminstartion

Administration: 

butterbur extract is available in various forms, including capsules, tablets, and liquid extracts. The dosing and administration of butterbur extract may vary depending on the product and treated condition. 

• Dosage: The optimal dose of butterbur extract has yet to be established. Therefore, following the dosing instructions on the supplement label or as a healthcare provider recommends is crucial. The typical dose for adults is 50 to 150 milligrams of standardized butterbur extract two to three times per day. 
• Timing: butterbur extract may be taken with or without food, depending on the product. It is essential to follow the instructions on the product label or as a healthcare provider recommends. 
• Duration of treatment: The duration of treatment with butterbur extract may vary depending on the specific condition. It is essential to follow the instructions on the product label or as a healthcare provider recommends. 
• Quality control: Choosing a reputable brand that has been third-party tested for quality and purity is crucial. 
• Interactions with medications: butterbur extract may interact with blood thinners, antihistamines, and chemotherapy drugs. Therefore, you must talk to your healthcare provider before taking butterbur extract if you are taking any medications. 
• Allergies: Although butterbur extract effectively reduces allergy symptoms, it may cause an allergic reaction in some people. Therefore, it is crucial to stop using butterbur extract and talk to your healthcare provider if you experience any symptoms of an allergic reaction. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: butterbur 

Why do we use butterbur? 

butterbur extract has been used for a variety of purposes, including: 

• Migraine prevention: butterbur extract effectively reduces the frequency and severity of migraine headaches. 
• Allergy relief: butterbur extract may reduce allergy symptoms such as sneezing, runny nose, and itchy eyes. 
• Asthma: butterbur extract may improve lung function and reduce asthma symptoms. 
• Stomach ulcers: butterbur extract may help reduce the formation of stomach ulcers. 
• Urinary tract symptoms: butterbur extract may help reduce urinary frequency and urgency in people with urinary tract symptoms. 
• Anxiety: butterbur extract may have mild anti-anxiety effects. 
• Pain relief: butterbur extract may help reduce pain in osteoarthritis and menstrual cramps. 

It is key to note that the effectiveness of butterbur extract for these uses is not well established, and more research is needed to confirm its benefits. As with any supplement/medication, it is key to talk to a healthcare provider before taking butterbur extract, especially if you have any underlying medical conditions or are taking any medications.