phytosterols

Action and Spectrum

Actions and Spectrum: 

• Cholesterol-lowering: phytosterols have been shown to help lower LDL cholesterol levels by blocking the absorption of cholesterol in the intestine. They compete with cholesterol for absorption into the bloodstream, which can lead to lower overall cholesterol levels. 
• Anti-inflammatory: phytosterols have been shown to have anti-inflammatory properties, which may help reduce the risk of chronic diseases such as heart disease, diabetes, and cancer. 
• Immune system support: phytosterols have been shown to help support the immune system by enhancing the activity of certain immune cells. 
• Antioxidant: phytosterols have antioxidant properties, which can help protect against oxidative damage and reduce the risk of chronic diseases. 
• Skin health: phytosterols have been shown to have moisturizing and anti-inflammatory properties, which can help improve skin health and reduce the symptoms of conditions such as eczema and psoriasis. 

Drug Interaction

Adverse Reaction

Black Box Warning

Black Box Warning: 

The black box warning on phytosterol supplements states that they may increase the risk of coronary heart disease, particularly in individuals with a history of heart disease or high levels of LDL cholesterol. 

Contraindication / Caution

Contraindication/Caution: 

While phytosterols are generally considered safe and well-tolerated, there are some contraindications and cautions to be aware of:  

• Sitosterolemia: phytosterols may not be suitable for people with a rare genetic condition called sitosterolemia, which causes excessive absorption and accumulation of phytosterols in the body. In such cases, phytosterols may actually increase the risk of cardiovascular disease.  
• Liver disease: phytosterols may not be suitable for people with liver disease, as excessive intake may exacerbate liver damage.  
• Pregnancy and breastfeeding: There is not enough research to determine the safety of phytosterol supplements during pregnancy and breastfeeding, so it is best to err on the side of caution and avoid them.  
• Interactions with medication: phytosterols may interact with certain medications, including cholesterol-lowering drugs, and reduce their effectiveness. Therefore, it is important to consult with a healthcare provider before taking phytosterol supplements if you are taking any medications.  
• High intake: High intake of phytosterols may lead to gastrointestinal side effects, such as diarrhea and flatulence. It is important to follow the recommended dosage and not exceed the tolerable upper intake level.  

Pregnancy / Lactation

Pregnancy warnings:     

Pregnancy category: N/A 

Lactation: Excreted into human milk is unknown 

Pregnancy Categories:         

Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester. 

Category B: There were lack of studies on pregnant women and no evidence of risk to the foetus in animal experiments.   

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 available 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 phytosterols is primarily related to their ability to compete with cholesterol for absorption in the small intestine. When consumed in sufficient quantities, phytosterols can block the absorption of cholesterol, reducing the amount of cholesterol that enters the bloodstream.  

Pharmacodynamics: 

This mechanism of action is thought to be mediated by the transport protein Niemann-Pick C1-like 1 (NPC1L1), which is responsible for the uptake of both cholesterol and phytosterols in the small intestine. 

In addition to their cholesterol-lowering effects, phytosterols have also been shown to have anti-inflammatory and antioxidant properties.  

Pharmacokinetics: 

Absorption  

phytosterols are poorly absorbed by the human body, and their absorption rate is estimated to be less than 5%. However, the absorption rate can be increased when phytosterols are consumed in combination with fats, such as those found in dairy products or fatty fish.  

Distribution  

phytosterols that are absorbed into the bloodstream are transported to various tissues, including the liver and the intestine.  

Metabolism  

phytosterols are metabolized in the liver, where they are converted into different metabolites, such as plant sterol esters and plant sterol glucuronides. These metabolites are then excreted in the bile and eliminated from the body.  

Elimination and Excretion  

phytosterols and their metabolites are eliminated from the body primarily via the feces, with a small amount excreted in the urine.

Adminstartion

Administration:  

Here are some general guidelines for the administration of phytosterols:  

The recommended daily dosage of phytosterols varies depending on the individual’s age, gender, and health status, as well as the product and the concentration of phytosterols. The National Cholesterol Education Program recommends a daily intake of 2 grams of phytosterols for individuals with high cholesterol levels.

It is important to follow the manufacturer’s instructions or consult with a healthcare provider to determine the appropriate dosage.  phytosterols can be taken with or without food, although taking them with a meal can help improve their absorption.  

phytosterol supplementation is typically recommended as a long-term strategy for managing high cholesterol levels. It is important to consult with a healthcare provider to determine the appropriate duration of treatment. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: phytosterol 

Why do we use phytosterol? 

phytosterols are used primarily to help lower cholesterol levels, particularly low-density lipoprotein (LDL) cholesterol, which is often referred to as “bad” cholesterol.

phytosterols work by blocking the absorption of cholesterol in the intestine, which can lead to a reduction in LDL cholesterol levels in the bloodstream.