MALVIX

Indications

• Improvement of visual function
• Support for eye health
• Management of diabetic retinopathy
• Enhancement of microcirculation
• Support for cardiovascular health

Dosage

Children: Consult a healthcare provider for appropriate dosing in children, as specific pediatric dosing may not be established.

Adults: Refer to specific product guidelines or consult a healthcare provider for dosing information, as it can vary based on formulation.

Mechanism of action

Bilberry is thought to exert its effects primarily through the action of anthocyanins, which have been shown to improve visual function and circulation. These compounds may enhance the integrity of the vascular system, inhibit oxidative stress, and improve microcirculation, particularly in the retina, thus potentially aiding in conditions like night blindness and age-related macular degeneration.

Pharmacodynamics

The pharmacodynamic effects of bilberry are largely attributed to its antioxidant properties, which help to scavenge free radicals and reduce oxidative damage in tissues. The anthocyanins in bilberry may also modulate inflammatory responses and improve endothelial function, contributing to better blood flow and reduced risk of cardiovascular complications.

Pharmacokinetics

Bilberry extracts are typically administered orally, and the active constituents are absorbed in the gastrointestinal tract. The bioavailability of anthocyanins can be influenced by factors such as food intake and gastrointestinal pH. Once absorbed, these compounds are metabolized in the liver and excreted primarily through urine. The half-life of bilberry components varies and is influenced by the specific anthocyanins and the formulation used.

Adverse effects

• Gastrointestinal upset
• Allergic reactions
• Headache
• Dizziness

Interactions

• Anticoagulants
• Antiplatelet drugs
• Diabetes medications

Precautions

• Use with caution in individuals with bleeding disorders
• Caution in patients undergoing surgery due to potential bleeding effects

Pregnancy

Bilberry is classified as safe for use during pregnancy, but it should be used under the guidance of a healthcare provider.

Breast-feeding

There is insufficient reliable information regarding the safety of bilberry during breastfeeding, thus caution is advised.

Storage

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

Formulations

• Dried berries
• Powdered extract
• Capsules
• Liquid extract

Indications

• Supplementation for vitamin A deficiency
• Antioxidant support
• Support for eye health
• Potential cancer prevention
• Cardiovascular health promotion

Dosage

Children: Refer to specific product guidelines and consult healthcare professionals for appropriate dosage.

Adults: Refer to specific product guidelines and consult healthcare professionals for appropriate dosage.

Mechanism of action

Carotenoids exert their effects primarily through their antioxidant activity. They scavenge free radicals, thereby protecting cells from oxidative stress. Some carotenoids, such as beta-carotene, are converted into retinol (vitamin A) in the body, playing a critical role in vision, immune function, and skin health. They may also modulate cell signaling pathways and gene expression, influencing cellular growth and differentiation.

Pharmacodynamics

Carotenoids enhance the body's defense against oxidative damage, which is implicated in various chronic diseases, including cancer and cardiovascular diseases. They may improve immune responses and have anti-inflammatory effects. The bioavailability of carotenoids can be influenced by dietary fat intake and the food matrix in which they are consumed.

Pharmacokinetics

Carotenoids are absorbed in the intestine via micelles, primarily through passive diffusion. They are transported in the bloodstream by lipoproteins, such as chylomicrons, and are stored in the liver and adipose tissues. The half-life of carotenoids varies, with some being rapidly cleared while others may accumulate. Factors such as dietary intake, health status, and genetic variations can influence their pharmacokinetics.

Adverse effects

• Nausea
• Headache
• Diarrhoea
• Skin discoloration
• Allergic reactions

Precautions

• Use with caution in patients with a history of hypersensitivity to carotenoids
• Consider potential interactions with anticoagulants and other medications affecting vitamin absorption

Pregnancy

Carotenoids are generally considered safe during pregnancy, but high doses should be avoided as they can lead to potential toxicity.

Breast-feeding

Carotenoids are excreted in breast milk, but they are considered safe in normal dietary amounts.

Storage

Store in a cool, dry place away from light. Keep out of reach of children.

Formulations

• Capsules
• Tablets
• Liquid supplements

Indications

• Antioxidant support
• Immune system support
• Anti-inflammatory effects
• Culinary uses

Dosage

Children: Refer to the BNF for Children for specific dosing recommendations based on age and condition.

Adults: Refer to specific product guidelines or clinical recommendations, as dosages may vary based on the form of citrus used (e.g., juice, supplements).

Mechanism of action

Citrus fruits contain a variety of bioactive compounds, including ascorbic acid (vitamin C), flavonoids, and limonoids. These compounds exert their effects through antioxidant activity, modulating cellular signaling pathways, and enhancing immune function. The flavonoids in citrus may inhibit oxidative stress and inflammation, contributing to their health-promoting effects.

Pharmacodynamics

The pharmacodynamic properties of citrus components are largely attributed to their antioxidant capacity and ability to scavenge free radicals. The bioactive compounds interact with various cellular pathways, potentially reducing the risk of chronic diseases such as cardiovascular disease and certain cancers. The vitamin C content also plays a crucial role in collagen synthesis and immune support.

Pharmacokinetics

Citrus bioactive compounds are absorbed in the gastrointestinal tract, with vitamin C being readily absorbed. The metabolism of flavonoids occurs primarily in the liver through phase I and II metabolic processes, resulting in various metabolites that can exert biological effects. The elimination half-lives of these compounds vary, and they are primarily excreted via the urine.

Pregnancy

Citrus fruits are generally considered safe during pregnancy. However, excessive consumption may lead to gastrointestinal discomfort, and pregnant individuals should consult with healthcare providers regarding their diet.

Breast-feeding

Citrus fruits are safe during breastfeeding, but it is advisable to consume them in moderation as they may cause gastrointestinal discomfort in some infants.

Storage

Citrus fruits should be stored in a cool, dry place. They can also be refrigerated to extend freshness, but should be kept in a breathable bag to avoid moisture accumulation.

Formulations

• fresh fruit
• juice
• essential oil

Indications

• Asthma
• Rheumatoid arthritis
• Inflammatory bowel disease
• Psoriasis
• Systemic lupus erythematosus
• Allergic reactions

Dosage

Children: Dosage must be determined by a healthcare professional based on the child's condition and weight. Refer to BNF for Children for specific dosing information.

Adults: Dosage varies widely based on condition and severity. Refer to specific prescribing guidelines for individual cases.

Mechanism of action

Esteis exerts its effects by binding to glucocorticoid receptors, leading to the modulation of gene expression. This results in the inhibition of pro-inflammatory cytokines, chemokines, and adhesion molecules, thereby reducing inflammation and immune response. It also influences the metabolism of carbohydrates, proteins, and fats, contributing to its therapeutic effects.

Pharmacodynamics

The pharmacodynamic effects of esteis involve the suppression of the immune system, reduction of inflammatory processes, and modulation of various metabolic pathways. It decreases the infiltration of leukocytes at the site of inflammation and stabilizes lysosomal membranes, further limiting the release of inflammatory mediators. Additionally, esteis can influence electrolyte balance and glucose metabolism, which are important considerations during therapy.

Pharmacokinetics

Esteis is well-absorbed following oral administration and has a bioavailability that varies depending on the formulation. It is extensively metabolized in the liver, primarily through the cytochrome P450 system. The half-life of esteis can vary but is generally in the range of several hours, with effects lasting longer due to its mechanism of action. The drug is excreted mainly in urine as metabolites, with minimal unchanged drug excreted.

Pregnancy

The safety of esteis during pregnancy has not been established. It should only be used if the potential benefits justify the potential risks to the fetus.

Breast-feeding

It is not known whether esteis is excreted in human milk. Caution should be exercised when administering esteis to a nursing mother.

Storage

Store at room temperature, away from moisture and light. Keep out of reach of children.

Indications

• General wellness support
• Anti-inflammatory effects
• Antioxidant activity
• Digestive aid
• Support for immune function

Dosage

Children: Paediatric dosing should be determined based on the specific extract and its intended use. Consultation with a healthcare provider is recommended for accurate dosing.

Adults: Dosage varies widely depending on the specific extract and formulation. It is essential to follow the manufacturer's instructions or consult a healthcare professional for appropriate dosing.

Mechanism of action

The mechanism of action of herbal extracts can vary significantly based on their constituents. Commonly, they exert their effects through multiple pathways including modulation of neurotransmitter systems, interference with inflammatory processes, or direct antioxidant activity. Some extracts may activate certain receptors or inhibit enzymes related to disease processes.

Pharmacodynamics

The pharmacodynamics of extracts is complex due to the presence of multiple active compounds which can have synergistic or antagonistic effects. These compounds may influence cellular signaling pathways, alter gene expression, or modulate immune response. The overall pharmacological profile is determined by the specific composition of the extract, its concentration, and the biological target it interacts with.

Pharmacokinetics

The pharmacokinetics of extracts involves absorption, distribution, metabolism, and excretion of the active compounds. Generally, herbal extracts are absorbed in the gastrointestinal tract, with bioavailability influenced by factors such as formulation, the presence of food, and individual metabolic differences. Compounds may undergo hepatic metabolism, and elimination can occur through urine or feces, depending on their chemical nature.

Pregnancy

Consult a healthcare professional before use, as the safety of the extract during pregnancy has not been established.

Breast-feeding

Consult a healthcare professional before use, as the safety of the extract during breastfeeding has not been established.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Indications

• Antioxidant support
• Anti-inflammatory effects
• Cardiovascular health
• Cancer prevention
• Neuroprotection
• Management of metabolic syndrome

Dosage

Adults: Dosage varies widely based on the specific flavonoid and the condition being treated. General recommendations suggest a daily intake of flavonoids through a diet rich in fruits and vegetables, but specific doses should be referenced from clinical studies or guidelines relevant to particular flavonoid compounds.

Mechanism of action

Glavanoid compounds exert their effects primarily through their antioxidant properties, which involve the scavenging of free radicals and reactive oxygen species. They modulate various signaling pathways, including the nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) and mitogen-activated protein kinase (MAPK) pathways. Through these mechanisms, flavonoids can influence inflammation, apoptosis, and cell proliferation.

Pharmacodynamics

Flavonoids exhibit a range of pharmacodynamic properties, including anti-inflammatory, antiviral, and anticancer activities. They can enhance endothelial function, improve blood flow, and promote vasodilation by increasing the availability of nitric oxide. Additionally, flavonoids are known to inhibit various enzymes involved in the metabolism of key biomolecules, thereby affecting processes such as lipid metabolism and glucose homeostasis.

Pharmacokinetics

The pharmacokinetics of flavonoids are characterized by their absorption, distribution, metabolism, and excretion. After oral consumption, flavonoids are rapidly absorbed in the gastrointestinal tract and undergo extensive first-pass metabolism in the liver. They are generally distributed in tissues and can cross biological membranes due to their lipophilic nature. The elimination half-life varies among different flavonoids, with metabolites excreted primarily through urine. Factors such as food intake and gut microbiota can significantly influence their bioavailability.

Pregnancy

Consult healthcare provider before use. Safety during pregnancy has not been established.

Breast-feeding

Consult healthcare provider before use. Safety during breastfeeding has not been established.

Storage

Store in a cool, dry place, away from direct sunlight. Keep out of reach of children.

Indications

• Prostate cancer
• Endometriosis
• Precocious puberty
• Uterine fibroids

Dosage

Children: Dosing in pediatric patients is condition-dependent and should be guided by a healthcare professional; refer to pediatric dosing guidelines.

Adults: Dosing varies based on the specific indication, and it is essential to refer to the prescribing information for detailed dosing regimens.

Mechanism of action

Lutain (leuprolide) exerts its effects by binding to the GnRH receptors in the pituitary gland. This binding initially stimulates the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). However, continuous administration leads to downregulation of these receptors, resulting in decreased secretion of gonadotropins. Consequently, this suppression of gonadotropins leads to reduced levels of testosterone in males and estrogen in females, effectively managing hormone-sensitive conditions.

Pharmacodynamics

The pharmacodynamics of lutain involve its role as a synthetic analog of GnRH, having a higher potency and longer half-life than endogenous GnRH. This results in an initial flare of gonadotropin release, followed by a significant reduction in serum testosterone or estrogen levels after prolonged use. This mechanism is particularly useful in conditions such as prostate cancer or endometriosis, where hormone levels need to be controlled.

Pharmacokinetics

Lutain is administered via injection and has a prolonged action due to its slow release from the injection site. After administration, it is absorbed into the systemic circulation, with peak plasma concentrations occurring within a few hours. The drug undergoes metabolism primarily in the liver, with excretion occurring through the kidneys. The elimination half-life varies based on the formulation but is generally around 3 to 6 hours, with effects lasting much longer due to the suppression of gonadotropin release.

Pregnancy

Consult healthcare professional before use as effects are not well-studied.

Breast-feeding

Consult healthcare professional before use as effects are not well-studied.

Storage

Store at room temperature, away from moisture and heat.

Dosage

Children: Refer to specific drug guidelines as paediatric dosing must be determined based on the individual drug and condition being treated.

Adults: Refer to specific drug guidelines as dosing can vary widely based on the exact medication and its intended use.

Mechanism of action

The mechanism of action of mixed drugs can vary widely, often involving multiple pathways. For example, some may act as agonists or antagonists at certain receptors, while others may inhibit enzymes or modulate neurotransmitter levels. This complexity allows mixed drugs to have a broad spectrum of effects, which can be beneficial in treating conditions that require multifaceted approaches.

Pharmacodynamics

Pharmacodynamics of mixed drugs also varies significantly. Their effects can be dose-dependent, with lower doses potentially providing different therapeutic effects than higher doses. The interactions with various receptors and pathways can lead to synergistic or antagonistic effects, influencing the overall therapeutic outcome. Side effects and therapeutic efficacy must be carefully monitored.

Pharmacokinetics

Pharmacokinetics of mixed drugs includes absorption, distribution, metabolism, and excretion, which are influenced by the drug's chemical structure and route of administration. Many mixed drugs are absorbed rapidly and have wide distribution in body tissues. Metabolism can occur in the liver, often involving cytochrome P450 enzymes, and excretion may be renal or hepatic, depending on the drug's properties. The half-life can vary, affecting dosing schedules and potential for drug interactions.

Pregnancy

Consult with a healthcare provider regarding use during pregnancy, as the safety profile may vary depending on the specific components involved in the mixed formulation.

Breast-feeding

Consult with a healthcare provider regarding use during breastfeeding, as the safety profile may vary depending on the specific components involved in the mixed formulation.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

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

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.