VITAMIN C

Indications

• Vitamin C deficiency
• Scurvy
• Adjunct therapy in iron overload conditions

Dosage

Children: Child 1 month–3 years: 125–250 mg daily in 1–2 divided doses; Child 4–11 years: 250–500 mg daily in 1–2 divided doses; Child 12–17 years: 0.5–1 g daily in 1–2 divided doses.

Adults: 500 mg daily, taken in 1-2 divided doses, depending on the clinical condition and dietary needs.

Mechanism of action

Ascorbic acid functions primarily as a reducing agent, facilitating enzymatic reactions in the body, including the hydroxylation of proline and lysine in collagen synthesis. It also plays a role in the absorption of iron from the gastrointestinal tract and enhances the immune response.

Pharmacodynamics

Ascorbic acid is crucial for the maintenance of connective tissue and is involved in the metabolism of several amino acids. Its antioxidant properties help to mitigate oxidative stress and may play a role in reducing the risk of chronic diseases.

Pharmacokinetics

Ascorbic acid is absorbed in the intestines and is widely distributed throughout the body. The renal clearance of ascorbic acid is dose-dependent, with higher doses leading to increased excretion. The half-life varies but is generally around 15 to 30 minutes in healthy individuals, with tissue saturation levels influencing its retention.

Contra-indications

• Hypercalcaemia
• Hyperoxaluria
• Patients with cardiac dysfunction

Adverse effects

• Abdominal pain
• Headache
• Nausea
• Vomiting
• Diarrhoea
• Constipation
• Weight loss
• Polyuria
• Sweating
• Thirst
• Vertigo

Interactions

• Increases risk of cardiovascular adverse effects with iron chelators
• Increases risk of cardiovascular adverse effects with deferiprone
• Increases risk of cardiovascular adverse effects with desferrioxamine

Precautions

• Use with caution in patients with iron overload
• Monitor for symptoms of overdose

Pregnancy

High doses teratogenic in animals but therapeutic doses unlikely to be harmful.

Storage

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

Formulations

• Ascorbic acid 50 mg tablets
• Ascorbic acid 100 mg tablets
• Ascorbic acid 200 mg tablets
• Ascorbic acid 250 mg tablets
• Ascorbic acid 500 mg capsules

Indications

• Vitamin C deficiency
• Support for immune function
• Antioxidant therapy
• Collagen synthesis support
• Skin health improvement

Dosage

Children: For children, dietary recommendations for vitamin C intake range from 15 to 75 mg daily, depending on age. Specific dosing should be determined based on dietary sources and individual health needs.

Adults: General recommendations for vitamin C intake vary, but it is typically suggested to consume 65-90 mg daily for adults from dietary sources. Higher doses may be beneficial for specific health conditions, but specific dosing should refer to established guidelines.

Mechanism of action

The primary mechanism of action of acerola is attributed to its high levels of ascorbic acid (vitamin C), which is a potent antioxidant. It scavenges free radicals, reducing oxidative stress and inflammation. Additionally, vitamin C plays a crucial role in collagen synthesis, enhancing skin integrity, and supporting the immune system by promoting the function of various immune cells.

Pharmacodynamics

The pharmacodynamics of acerola is largely influenced by its vitamin C content. As an antioxidant, it protects cells from oxidative damage. It enhances the absorption of non-heme iron from plant-based foods, contributes to the regeneration of other antioxidants such as vitamin E, and plays a role in various enzymatic reactions essential for metabolic processes. Its effects on immune function help in improving resistance to infections.

Pharmacokinetics

Vitamin C is rapidly absorbed in the gastrointestinal tract, with peak plasma concentrations occurring within 2-4 hours after ingestion. It is distributed throughout the body and can cross the blood-brain barrier. The metabolism of vitamin C involves its conversion to dehydroascorbic acid, which can be reduced back to ascorbic acid. Vitamin C is excreted primarily through the kidneys, and excess amounts are eliminated in urine, indicating a well-regulated homeostatic mechanism.

Adverse effects

• Gastrointestinal upset
• Diarrhea
• Nausea
• Stomach cramps

Precautions

• Use with caution in individuals with a history of allergies to fruits or other dietary supplements.

Pregnancy

Acerola is generally considered safe during pregnancy due to its natural origins, but it is advisable to consult a healthcare provider before use.

Breast-feeding

Acerola is likely safe during breastfeeding, but consult a healthcare provider for personalized advice.

Storage

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

Formulations

• Acerola powder
• Acerola capsules
• Acerola juice
• Acerola tablets

Indications

• Cardiovascular diseases
• Chronic inflammation
• Oxidative stress-related conditions

Dosage

Children: Refer to the BNF for Children for appropriate paediatric dosing recommendations.

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

Mechanism of action

Bioflavonoids, such as Rutin, exhibit antioxidant effects by enhancing the activity of antioxidant enzymes, activating the Nrf2/HO-1 pathway, increasing glutathione levels, and reducing malondialdehyde. Their anti-inflammatory actions involve the inhibition of pro-inflammatory cytokines and enzymes, while their antiapoptotic effects include the inhibition of free radicals and various caspases, as well as the elevation of antiapoptotic proteins.

Pharmacodynamics

Bioflavonoids demonstrate a wide range of pharmacological effects, including antioxidant, anti-inflammatory, and cytoprotective actions. The modulation of intracellular signaling pathways contributes to the reduction of oxidative stress and inflammation, which may help in preventing chronic diseases such as cardiovascular diseases and cancer.

Pharmacokinetics

The pharmacokinetics of bioflavonoids depend on their solubility and absorption characteristics. They are generally well-absorbed in the gastrointestinal tract, and their bioavailability can be influenced by food intake. Metabolism primarily occurs in the liver, with conjugation to glucuronides and sulfates, and they are excreted via urine. The half-life varies among different bioflavonoids.

Pregnancy

There is insufficient evidence to establish the safety of bioflavonoids during pregnancy. Consult a healthcare provider for advice.

Breast-feeding

Limited data is available on the excretion of bioflavonoids in human milk. Caution is advised when administering to breastfeeding women.

Storage

Store in a cool, dry place, away from light and moisture.

Formulations

• Rutin
• Quercetin
• Hesperidin

Indications

• Anti-inflammatory support
• Muscle soreness relief
• Management of gout
• Sleep aid
• Antioxidant supplementation

Dosage

Children: Refer to specific product guidelines, as doses can vary based on formulation and intended use.

Adults: Refer to specific product guidelines, as doses can vary based on formulation and intended use.

Mechanism of action

The beneficial effects of cherries are attributed to their high content of anthocyanins and phenolic compounds, which exert antioxidant effects by scavenging free radicals. These compounds may also modulate inflammatory pathways by inhibiting pro-inflammatory cytokines and enzymes, thus contributing to their anti-inflammatory properties.

Pharmacodynamics

Cherries may help reduce muscle soreness after exercise, lower uric acid levels, and improve joint health in conditions like gout and arthritis. The anti-inflammatory effects are beneficial in managing symptoms associated with chronic inflammatory diseases. Additionally, the presence of melatonin may support sleep quality by regulating circadian rhythms.

Pharmacokinetics

The bioavailability of cherry compounds varies; anthocyanins are absorbed in the gastrointestinal tract and may be metabolized into various forms. Peak plasma concentrations typically occur within a few hours after consumption. The elimination half-life of cherry metabolites can vary, and factors like individual metabolism, the form of cherry consumed, and the presence of other dietary components can influence pharmacokinetics.

Pregnancy

Cherries are generally considered safe to consume during pregnancy. They provide beneficial nutrients but should be eaten in moderation.

Breast-feeding

Cherries are also safe during breastfeeding and can provide essential vitamins and antioxidants.

Storage

Store cherries in a cool, dry place. Refrigeration can extend their freshness, ideally in a perforated plastic bag.

Formulations

• Fresh cherries
• Dried cherries
• Cherry juice
• Cherry extract

Dosage

Children: Refer to specific drug guidelines or BNF for Children for accurate dosing information.

Adults: Refer to specific drug guidelines or BNF for accurate dosing information.

Mechanism of action

The mechanism of action of complex drugs can vary widely depending on their composition. Generally, these agents may act by modulating receptor activity, inhibiting enzyme pathways, or altering cellular signaling pathways. For instance, they may function as agonists or antagonists at specific receptors, influencing physiological responses such as neurotransmission or inflammation.

Pharmacodynamics

The pharmacodynamics of complex drugs involves understanding how they affect the body over time, including their potency, efficacy, and duration of action. These drugs may exhibit dose-dependent effects, where higher doses lead to increased therapeutic actions or side effects. Additionally, the interactions between the components of a complex formulation can result in synergistic or antagonistic effects, impacting the overall therapeutic outcome.

Pharmacokinetics

Pharmacokinetics of complex drugs encompasses the absorption, distribution, metabolism, and excretion (ADME) of the drug components. Absorption can be influenced by the formulation, while distribution may vary based on the lipophilicity and protein binding of each component. Metabolism often occurs in the liver, with various enzymes involved, and excretion typically takes place via renal or biliary pathways. The half-life of complex drugs can vary significantly based on their individual components.

Pregnancy

Consult healthcare provider. Risk-benefit assessment is essential before use.

Breast-feeding

Consult healthcare provider. Monitor for potential effects on the infant.

Storage

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

Indications

• Chronic venous insufficiency
• Hemorrhoids
• Varicose veins
• Hypertension
• Antioxidant support

Dosage

Children: Refer to BNF for Children for specific dosing guidance.

Adults: Refer to BNF for specific dosing guidance.

Mechanism of action

Hesperidin exerts its effects through various mechanisms, including the modulation of nitric oxide synthesis, which leads to vasodilation and improved blood circulation. It also possesses anti-inflammatory properties and can inhibit the activity of certain enzymes involved in oxidative stress, contributing to its antioxidant effects.

Pharmacodynamics

Hesperidin has been shown to enhance capillary resistance and reduce permeability, which can aid in the management of conditions like chronic venous insufficiency. Its antioxidant effects help to neutralize free radicals, thereby protecting cells from oxidative damage. Additionally, hesperidin may have a role in lipid metabolism and lowering cholesterol levels.

Pharmacokinetics

After oral administration, hesperidin is rapidly absorbed, with peak plasma concentrations occurring within a few hours. It undergoes extensive metabolism in the liver to yield various metabolites. The elimination half-life is variable but generally ranges from several hours to a day. Hesperidin and its metabolites are primarily excreted via urine.

Pregnancy

There is insufficient reliable information regarding the safety of hesperidin during pregnancy. Consult a healthcare provider for guidance.

Breast-feeding

Limited data is available on the excretion of hesperidin in breast milk. Caution is advised, and a healthcare provider should be consulted before use.

Storage

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

Indications

• Scurvy prevention
• Digestive aid
• Immune system support
• Skin health
• Antimicrobial applications

Dosage

Children: There is no specific paediatric dosage for lemon; it can be given to children in moderate amounts as part of a balanced diet.

Adults: There is no specific adult dosage for lemon; it can be consumed in various forms such as fresh fruit, juice, or as part of food and beverages.

Mechanism of action

Lemon contains compounds such as citric acid, flavonoids, and essential oils. Citric acid may enhance the absorption of minerals and has a role in the Krebs cycle, promoting energy metabolism. Flavonoids possess antioxidant properties, which help combat oxidative stress and inflammation, while essential oils can exhibit antimicrobial and anti-inflammatory effects.

Pharmacodynamics

The pharmacodynamic effects of lemon are primarily attributed to its antioxidant properties, which help neutralize free radicals, reduce oxidative stress, and support overall health. The citric acid in lemon may also aid in alkalizing the body, improving metabolic processes, and supporting digestion.

Pharmacokinetics

The bioavailability of lemon compounds can vary based on the form of consumption (whole fruit, juice, or extract). Vitamin C is rapidly absorbed in the gastrointestinal tract and distributed throughout the body. The metabolism of flavonoids occurs primarily in the liver, and they may have a variable half-life depending on individual metabolism.

Adverse effects

• Allergic reactions in sensitive individuals
• Gastrointestinal discomfort
• Tooth enamel erosion with excessive use

Precautions

• Caution in individuals with citrus allergies
• May cause skin irritation if applied topically in concentrated forms

Pregnancy

Lemon is generally considered safe during pregnancy, but excessive intake should be avoided.

Breast-feeding

Lemon is safe during breastfeeding when consumed in normal dietary amounts.

Storage

Store in a cool, dry place. Fresh lemons should be kept in the refrigerator to maintain freshness.

Formulations

• Fresh lemon
• Lemon juice
• Lemon essential oil
• Lemon zest

Indications

• Osteoarthritis
• Rheumatoid arthritis
• Joint pain
• Inflammation
• Vitamin C deficiency
• Antioxidant support

Dosage

Children: There is no specific paediatric dosage established; refer to product-specific guidelines or consult a healthcare professional for appropriate dosing.

Adults: There is no specific adult dosage established; refer to product-specific guidelines or consult a healthcare professional for appropriate dosing.

Mechanism of action

The exact mechanism of action of rosehips is not fully understood. However, they are believed to exert anti-inflammatory effects primarily due to their high content of vitamin C, flavonoids, and other antioxidants. These compounds may inhibit the production of pro-inflammatory cytokines and reduce oxidative stress, contributing to their therapeutic effects.

Pharmacodynamics

Rosehips have been observed to have anti-inflammatory, antioxidant, and immune-boosting properties. The vitamin C content supports collagen synthesis and may contribute to the maintenance of healthy connective tissues. Additionally, the phenolic compounds present in rosehips may modulate inflammatory pathways, providing potential benefits in conditions such as osteoarthritis and rheumatoid arthritis.

Pharmacokinetics

The pharmacokinetics of rosehips are not well-studied, but the bioavailability of vitamin C and other soluble compounds is generally high when ingested. Absorption occurs in the gastrointestinal tract, with peak plasma concentrations typically reached within a few hours. The metabolites are likely excreted primarily through the kidneys. The pharmacokinetics of rosehip extracts can vary depending on the formulation and preparation method.

Adverse effects

• Gastrointestinal upset
• Diarrhea
• Nausea
• Allergic reactions

Precautions

• Use with caution in individuals with a history of allergies to rose family plants
• Consult a healthcare provider before use in patients with chronic medical conditions or those taking other medications

Pregnancy

Limited information is available on the safety of rosehips during pregnancy. Consult a healthcare provider before use.

Breast-feeding

Limited information is available on the safety of rosehips during breastfeeding. Consult a healthcare provider before use.

Storage

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

Formulations

• Dried fruit
• Powder
• Capsules
• Teas
• Extracts

Indications

• Antioxidant support
• Anti-inflammatory therapy
• Supportive treatment in cardiovascular diseases
• Hepatoprotective agent
• Nephroprotective agent

Dosage

Children: Refer to the BNF for Children for appropriate paediatric dosing guidelines.

Adults: Refer to the BNF for specific adult dosing recommendations as they may vary based on the condition being treated.

Mechanism of action

Rutin exerts its protective effects through several mechanisms, including enhancement of antioxidant enzymes and activation of the Nrf2/HO-1 pathway, leading to increased levels of glutathione (GSH) and reduced malondialdehyde (MDA). It also exhibits anti-inflammatory actions by inhibiting pro-inflammatory cytokines such as IL-1β, IL-6, and TGF-β1, as well as enzymes like COX-2 and iNOS. Furthermore, rutin has antiapoptotic effects by inhibiting free radicals and various caspases, while promoting the expression of the antiapoptotic protein Bcl-2.

Pharmacodynamics

Rutin demonstrates various pharmacodynamic effects, particularly its ability to modulate oxidative stress and inflammation. It enhances the body's endogenous antioxidant defenses, contributing to cellular protection against oxidative damage. Additionally, the anti-inflammatory properties of rutin help in reducing tissue inflammation, which may be beneficial in conditions characterized by excessive inflammatory responses.

Pharmacokinetics

The pharmacokinetics of rutin are characterized by its absorption in the gastrointestinal tract, followed by metabolism primarily in the liver, where it is converted into various metabolites. These metabolites are then excreted mainly via the urine. The bioavailability of rutin can be influenced by factors such as food intake and individual metabolic variations.

Pregnancy

Rutin is generally considered safe in pregnancy, but consult a healthcare provider for specific recommendations.

Breast-feeding

Rutin is likely safe during breastfeeding, yet it is advisable to discuss with a healthcare professional.

Storage

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

Mechanism of action

A 2022 review of Rutin focused on its protective effects on the heart, liver, and kidneys against various chemical and natural toxins. The antioxidant effects involve enhancement of various antioxidant enzymes, Nrf2/HO-1 pathway activation, Glutathione (GSH) elevation, and malondialdehyde (MDA) reduction. The anti-inflammatory effects involve inhibition of IL-1β, IL-6, TGF-β1, COX-2, iNOS, TLR4, and XO. The antiapoptotic effects involve inhibition of free radicals, caspase-3/-7/-9, hsp70, HMGB1, and p53, and elevation of antiapoptotic protein Bcl-2.

Mechanism of action

A 2022 review of Rutin focused on its protective effects on the heart, liver, and kidneys against various chemical and natural toxins. The antioxidant effects involve enhancement of various antioxidant enzymes, Nrf2/HO-1 pathway activation, Glutathione (GSH) elevation, and malondialdehyde (MDA) reduction. The anti-inflammatory effects involve inhibition of IL-1β, IL-6, TGF-β1, COX-2, iNOS, TLR4, and XO. The antiapoptotic effects involve inhibition of free radicals, caspase-3/-7/-9, hsp70, HMGB1, and p53, and elevation of antiapoptotic protein Bcl-2.