ENLIP CAPSULES (Each capsule contains Natural Phytosterols 95% 200mg / B. Sitosterol 90mg)

Indications

• Pain relief
• Inflammatory conditions
• Dental applications
• Antifungal treatments
• Antioxidant support

Dosage

Children: Refer to specific product guidelines for pediatric dosing as it may vary based on formulation and intended use.

Adults: Refer to specific product guidelines as dosing may vary based on formulation and intended use.

Mechanism of action

The exact mechanism of action of eugenol is not fully understood. However, it has been shown to interrupt action potentials, contributing to its analgesic properties. Eugenol exhibits anti-inflammatory effects by modulating the activity of polymorphonuclear leukocytes, which release inflammatory mediators. Additionally, eugenol has demonstrated antioxidant activity, protecting cells from oxidative stress. It has been observed to inhibit the formation of malondialdehyde in irradiated thymocytes, suggesting a protective role against oxidative damage.

Pharmacodynamics

Eugenol exhibits several pharmacological properties, including analgesic, anti-inflammatory, antipyretic, neuroprotective, antifungal, and antioxidant effects. Its ability to inhibit reactive oxygen species generation and modulate inflammatory mediators contributes to its therapeutic potential in managing pain and inflammation. The dose-dependent effects of eugenol on respiratory inhibition of mitochondria highlight its impact on cellular energy metabolism, further extending its pharmacodynamic profile.

Pharmacokinetics

Eugenol is rapidly absorbed and distributed throughout the body following administration. It undergoes extensive metabolism in the liver, with various metabolic pathways including conjugation and oxidation. The elimination half-life and specific pharmacokinetic parameters can be influenced by the route of administration and individual patient factors. The exact pharmacokinetics of eugenol in humans require further elucidation through clinical studies.

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Skin irritation
• Allergic reactions

Precautions

• Use with caution in individuals with liver disease or gastrointestinal disorders.
• Caution is advised in patients who are pregnant or breastfeeding.

Pregnancy

Eugenol should be used with caution during pregnancy due to insufficient data on safety.

Breast-feeding

Eugenol is excreted in breast milk; caution is advised when administering to breastfeeding mothers.

Storage

Store in a tightly closed container, in a cool, dry place away from light.

Formulations

• Essential oil
• Topical preparations

Indications

• Hypercholesterolemia
• High LDL cholesterol levels
• Cardiovascular disease prevention

Dosage

Children: Refer to the BNF for Children for appropriate dosing in paediatric patients.

Adults: Typically, a daily intake of 2 to 3 grams of phytosterols is recommended for cholesterol-lowering effects, often achieved through fortified foods or supplements.

Mechanism of action

Phytosterols function by competing with cholesterol for absorption in the gastrointestinal tract. They inhibit the intestinal absorption of cholesterol, leading to a reduction in serum cholesterol levels. This mechanism is primarily mediated through the inhibition of the Niemann-Pick C1-like 1 (NPC1L1) protein, which is essential for cholesterol uptake in enterocytes.

Pharmacodynamics

The pharmacodynamic effects of phytosterols include lowering low-density lipoprotein (LDL) cholesterol levels and potentially having anti-inflammatory and antioxidant properties. Regular consumption of phytosterols has been associated with a modest reduction in total cholesterol and LDL cholesterol levels, which are risk factors for cardiovascular diseases.

Pharmacokinetics

Phytosterols are not significantly absorbed in the gastrointestinal tract, with less than 5% of ingested phytosterols reaching systemic circulation. The bioavailability of phytosterols can be affected by factors such as dietary fat content and the presence of other nutrients. Since they are poorly absorbed, their effects are primarily local within the gastrointestinal tract, where they exert their cholesterol-lowering effects. The elimination half-life of phytosterols is not well-defined due to their limited absorption.

Adverse effects

• Gastrointestinal discomfort
• Diarrhea
• Nausea
• Bloating

Interactions

• May reduce absorption of fat-soluble vitamins (A, D, E, K)
• May interact with cholesterol-lowering medications

Precautions

• Use with caution in individuals with a history of gastrointestinal disorders
• Monitor for potential vitamin deficiencies with high intake

Pregnancy

Phytosterols are generally considered safe during pregnancy, but it is recommended to consult a healthcare provider.

Breast-feeding

Phytosterols are likely safe during breastfeeding; however, consult a healthcare provider for personalized advice.

Storage

Store in a cool, dry place away from direct sunlight.

Formulations

• Capsules
• Tablets
• Powder
• Functional foods (e.g., margarine, yogurt)

Indications

• Hypercholesterolemia
• Dietary management of cholesterol levels
• Potential adjunct in cardiovascular disease risk reduction

Dosage

Children: Refer to BNF for Children for appropriate pediatric dosing guidelines.

Adults: Refer to BNF for specific dosing recommendations, as doses can vary based on the formulation and clinical guidelines.

Mechanism of action

Sitosterol acts primarily by inhibiting the absorption of dietary cholesterol in the intestines. It competes with cholesterol for incorporation into micelles, which are necessary for cholesterol absorption. This competition leads to a reduction in the amount of cholesterol that enters the bloodstream and results in lower plasma cholesterol levels. Additionally, sitosterol may influence cholesterol metabolism and synthesis within the liver.

Pharmacodynamics

The pharmacodynamic effects of sitosterol include a reduction in total cholesterol and low-density lipoprotein (LDL) cholesterol levels. It may also have anti-inflammatory properties and can modulate immune responses. The overall impact on lipid profiles can contribute to a decreased risk of cardiovascular diseases associated with high cholesterol levels.

Pharmacokinetics

Sitosterol is poorly absorbed in the gastrointestinal tract, with only a small fraction of ingested amounts entering systemic circulation. It is primarily metabolized in the liver and may be excreted in bile. The bioavailability of sitosterol is influenced by dietary fat intake, as fats can enhance its absorption. The elimination half-life of sitosterol in the body is not well-defined, but it is generally believed to have a prolonged presence due to its incorporation into cell membranes.

Pregnancy

There is limited information available on the use of sitosterol during pregnancy. Consult a healthcare professional before use.

Breast-feeding

Limited data are available on the secretion of sitosterol in breast milk. Consult a healthcare professional before use.

Storage

Store in a cool, dry place away from direct sunlight.

Mechanism of action

The exact mechanism of action of eugenol is unknown. However, eugenol has been shown to interrupt action potentials, which may be involved in its anti-pain activity. Research has also shown eugenol to have anti-inflammatory, neuroprotective, antipyretic, antioxidant, antifungal and analgesic properties. ... Thymocyte suspension was irradiated by gamma-rays, and the malondialdehyde (MDA) formation was measured with the thiobarbituric acid reactive species (TBARS) method. The results showed an increase in MDA in irradiated (2 Gy) thymocytes, which was inhibited in samples treated with increasing concentrations of eugenol (10-200 uM) prior to irradiation. The concentration of eugenol required to inhibit half of the MDA formation (IC(50)) in irradiated thymocytes was 100 uM. A dose-dependent increase in the generation of ROS was observed in irradiated thymocytes (0.5-200 cGy) as measured by 2,7-dichlorodihydro fluorescein diacetate (DCH-FDA), which was inhibited by eugenol administered before irradiation. Respiratory inhibition of isolated rat liver mitochondria by eugenol was dose related and uncoupled oxidative phosphorylation from electron transfer. Polymorphonuclear leukocytes (PMNL) play an important role in the modulation of inflammatory conditions in humans. PMNL cells recruited at the site of inflammation, release inflammatory mediators such as leukotrienes, proteolytic enzymes and reactive oxygen species. Among these, leukotrienes are implicated in pathophysiology of allergic and inflammatory disorders like asthma, allergic rhinitis, arthritis, inflammatory bowel disease and psoriasis. 5-lipoxygenase (5-LO) is the key enzyme in biosynthetic pathway of leukotrienes. Our earlier studies showed that spice phenolic active principles significantly inhibit 5-LO enzyme in human PMNLs. In this study we have further characterized the inhibitory mechanism of eugenol, the active principle of spice-clove on 5-LO enzyme and also its effect on leukotriene C((4)) (LTC(4)). Substrate dependent enzyme kinetics showed that the inhibitory effect of eugenol on 5-LO was of a non-competitive nature. Further, eugenol was found to significantly inhibit the formation of LTC(4) in calcium ionophore A23187 and arachidonic acid (AA) stimulated PMNL cells. These data clearly suggest that eugenol inhibits 5-LO by non-competitive mechanism and also inhibits formation of LTC(4) in human PMNL cells and thus may have beneficial role in modulating 5-LO pathway in human PMNL cells. The Ca(2+)-activated Cl(-) channel TMEM16A is involved in epithelial fluid secretion, smooth muscle contraction and neurosensory signaling. We identified a Thai herbal antidiarrheal formulation that inhibited TMEM16A Cl(-) conductance. C18-reversed-phase HPLC fractionation of the herbal formulation revealed >98% of TMEM16A inhibition activity in one out of approximately 20 distinct peaks. The purified, active compound was identified as eugenol (4-allyl-2-methoxyphenol), the major component of clove oil. Eugenol fully inhibited TMEM16A Cl(-) conductance with single-site IC(50)~150 uM. Eugenol inhibition of TMEM16A in interstitial cells of Cajal produced strong inhibition of intestinal contraction in mouse ileal segments. TMEM16A Cl(-) channel inhibition adds to the list of eugenol molecular targets and may account for some of its biological activities. For more Mechanism of Action (Complete) data for EUGENOL (21 total), please visit the HSDB record page.