Coxiwin 5.0%

Indications

• Constipation
• Softening of impacted feces
• Bowel cleansing prior to medical procedures

Dosage

Children: For children aged 2-11 years: 12.5 to 25 mg 3 times a day, adjusted according to response. For children aged 12-17 years: 120 mg for 1 dose.

Adults: For oral use: 50 to 500 mg daily in divided doses, adjusted according to response. For rectal use: 120 mg as a single dose.

Mechanism of action

Docusate sodium acts as a stool softener by increasing the wetting efficiency of the intestinal fluid, facilitating the mixing of aqueous and fatty substances, which leads to a reduction in stool hardness. It also promotes the secretion of intestinal fluids, which aids in the overall ease of bowel movements.

Pharmacodynamics

Docusate sodium works by altering the surface tension of the stool, making it easier for water to mix with the stool, thus softening it. Its effects are generally observed within 1 to 3 days of oral administration, while rectal administration can lead to a quicker response, typically within 20 minutes.

Pharmacokinetics

Docusate sodium is absorbed in the gastrointestinal tract, with a peak plasma concentration occurring approximately 1 to 2 hours after administration. The elimination half-life is not well-characterized, but the drug is excreted mainly in the urine. The onset of action varies depending on the route of administration; oral doses typically take 1-3 days to have an effect, whereas rectal doses have a faster onset.

Contra-indications

• Inflammatory bowel disease (except under medical supervision)
• Intestinal obstruction
• Hypersensitivity to soya
• History of hypersensitivity to arachis oil or peanuts

Adverse effects

• Anal irritation
• Contact dermatitis
• Granuloma pneumonia
• Lipoid pneumonia
• Rectal discharge

Interactions

• Avoid concurrent use with liquid paraffin
• Excessive use of stimulant laxatives may cause diarrhea and related effects such as hypokalemia

Precautions

• Prolonged use should be avoided
• Administered at night for optimal effect
• Rectal preparations not indicated if hemorrhoids or anal fissure are present

Pregnancy

Manufacturer advises caution; consult a healthcare professional before use during pregnancy.

Breast-feeding

Manufacturer advises caution; present in small amounts in milk following oral administration.

Storage

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

Formulations

• Docusate sodium 2.5 mg per 1 ml oral solution
• Docusate sodium 10 mg per 1 ml oral solution
• Docusate sodium 12.5 mg/5 ml oral solution
• Docusate sodium 100 mg capsules
• Docusate sodium 120 mg enema

Indications

• Gastrointestinal disturbances
• Toxin adsorption in cases of poisoning
• Diarrhea
• Gastroenteritis

Dosage

Children: Refer to the specific product guidelines or consult clinical resources for dosing recommendations.

Adults: Refer to the specific product guidelines or consult clinical resources for dosing recommendations.

Mechanism of action

Bentonite works by adsorbing toxins and pathogens in the gastrointestinal tract. The high surface area and negative charge of bentonite particles attract positively charged ions, allowing it to bind to various substances, including bacteria and toxins, thereby facilitating their removal from the body.

Pharmacodynamics

Bentonite's pharmacodynamic properties are largely attributed to its adsorptive capacity. It can effectively bind to various drugs and toxins, reducing their bioavailability. This property makes it useful in treating cases of poisoning or overdose, as it can prevent the absorption of harmful substances in the intestines.

Pharmacokinetics

Bentonite is not absorbed systemically. After oral administration, it remains in the gastrointestinal tract where it exerts its effects. The clay is eventually excreted in the feces. The onset of action can vary depending on the formulation and the presence of other substances in the gastrointestinal tract.

Adverse effects

• Constipation
• Abdominal discomfort
• Nausea

Interactions

• May reduce the absorption of other medications when taken concurrently

Precautions

• Use with caution in patients with gastrointestinal obstructions
• Ensure adequate hydration to prevent constipation

Pregnancy

Bentonite is generally considered safe during pregnancy; however, clinical data is limited.

Breast-feeding

Bentonite is likely safe during breastfeeding, but consult a healthcare professional for personalized advice.

Storage

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

Formulations

• Powder
• Capsules
• Suspension

Indications

• Food preservative
• Treatment of urea cycle disorders
• Metabolic disorders involving benzoyl-CoA

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines based on condition.

Adults: Refer to the BNF for specific dosing guidelines based on condition.

Mechanism of action

Benzoate acts mainly by inhibiting the growth of bacteria and fungi through its ability to lower the pH, creating an environment that is less favorable for microbial growth. It is also involved in metabolic pathways where it helps in the conjugation of toxic substances, facilitating their excretion from the body.

Pharmacodynamics

Benzoate is known for its antimicrobial properties, which are particularly effective against a wide range of fungi and bacteria. Its efficacy as a preservative is due to its ability to penetrate microbial cell membranes and disrupt their metabolic processes. Additionally, it has been observed to modulate various metabolic pathways, particularly those associated with aromatic compound degradation.

Pharmacokinetics

After ingestion, benzoate is rapidly absorbed in the gastrointestinal tract. It is metabolized primarily in the liver, where it undergoes conjugation with glycine to form hippurate, which is then excreted in the urine. The half-life of benzoate varies depending on individual metabolic rates but is generally short due to its efficient conversion and excretion.

Pregnancy

There is limited data on the use of benzoate in pregnancy. Consultation with healthcare professionals is advised before use.

Breast-feeding

Limited data is available on the excretion of benzoate in breast milk. Caution is recommended when administering to nursing mothers.

Storage

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

Indications

• Acidulant in food and beverages
• Preservative in pharmaceutical formulations
• pH adjuster in various chemical preparations

Dosage

Children: Refer to product-specific guidelines for appropriate dosing based on formulation and indication.

Adults: Refer to product-specific guidelines for appropriate dosing based on formulation and indication.

Mechanism of action

Citric acid acts by chelating metal ions, which can enhance the solubility of certain compounds and improve their bioavailability. It also contributes to the acidity of the environment, which can influence enzymatic activity and metabolic pathways, particularly in the degradation of citronellol.

Pharmacodynamics

Citric acid exhibits mild pharmacological effects primarily attributed to its role in metabolic processes. It aids in the regulation of pH levels, which can impact enzymatic reactions and biochemical pathways. The acid's chelating properties may help to reduce the toxicity of certain metal ions in biological systems.

Pharmacokinetics

Citric acid is rapidly absorbed after oral administration and is metabolized in the liver. It undergoes conversion to various metabolites in the citric acid cycle, contributing to energy production. The elimination primarily occurs through urine, with minimal accumulation in the body.

Pregnancy

Citric acid is generally regarded as safe during pregnancy when used in food amounts. However, consult a healthcare provider for advice on medicinal use.

Breast-feeding

Citric acid is considered safe during breastfeeding when consumed in food amounts. For medicinal use, consult a healthcare provider.

Storage

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

Indications

• Constipation
• Prevention of straining during bowel movements
• Management of conditions such as hemorrhoids or anal fissures

Dosage

Children: Refer to the BNF for Children for appropriate dosing in children.

Adults: The usual oral dosage is 50 to 500 mg daily in divided doses, or 100 to 250 mg taken once daily. Rectal administration can involve 283 to 566 mg as a single dose.

Mechanism of action

Docusate exerts its effects primarily through its surfactant properties in the intestines. It allows for the incorporation of fat and water into the feces, which softens the stool. Studies have shown that docusate increases the secretion of water, sodium, chloride, and potassium while decreasing the absorption of glucose and bicarbonate. This mechanism may involve an increase in intracellular cyclic AMP, either directly by docusate or through E series prostaglandins.

Pharmacodynamics

As an anionic detergent and laxative, docusate promotes stool softening by reducing surface tension. Its onset of action varies, with oral administration taking 6 to 72 hours and rectal administration acting within 2 to 15 minutes. The effects are localized in the jejunum, aiding in the passage of feces.

Pharmacokinetics

Docusate is absorbed in the gastrointestinal tract, but its specific absorption and elimination characteristics are not well-documented. It is primarily metabolized in the intestines, and the active metabolites facilitate the stool softening effect. The pharmacokinetic profile indicates that its action can vary based on the route of administration and individual patient factors.

Adverse effects

• Abdominal cramping
• Diarrhea
• Nausea
• Throat irritation

Precautions

• Use with caution in patients with intestinal obstruction or abdominal pain of unknown origin
• Not recommended for long-term use

Pregnancy

Docusate is generally considered safe to use during pregnancy, but it is advisable to consult a healthcare provider before use.

Breast-feeding

Docusate is excreted in breast milk; however, it is considered safe to use while breastfeeding.

Storage

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

Formulations

• Oral capsules
• Oral liquid
• Rectal suppositories

Indications

• Nutritional support in patients unable to consume food orally
• Parenteral nutrition
• Drug delivery for lipophilic medications
• Topical applications for skin conditions

Dosage

Children: Refer to specific product guidelines and clinical protocols for paediatric dosing.

Adults: Refer to specific product guidelines and clinical protocols for adult dosing.

Mechanism of action

Emulsions work by reducing the surface tension between the oil and water phases, allowing for the formation of stable droplets. This process is mediated by emulsifying agents, which can be surfactants or natural polymers that stabilize the emulsion and prevent phase separation. The absorption and bioavailability of drugs within the emulsion can be enhanced due to the increased surface area for absorption.

Pharmacodynamics

The pharmacodynamics of emulsions vary based on their composition and formulation. The presence of emulsifying agents can influence the release profile of the active ingredients, allowing for controlled or sustained release. Emulsions can also enhance the solubility of poorly water-soluble drugs, improving their therapeutic effects and minimizing side effects related to high concentrations of active ingredients.

Pharmacokinetics

The pharmacokinetics of emulsions depend on their route of administration and the specific properties of the drug contained within the emulsion. After administration, emulsions can be rapidly absorbed due to their small droplet size, leading to quicker onset of action. The distribution, metabolism, and excretion of the drug will follow the pharmacokinetic principles applicable to the active ingredients, influenced by their solubility and the emulsion's formulation.

Pregnancy

The safety of emulsions during pregnancy depends on the specific type and formulation. Consult relevant guidelines and specific product information.

Breast-feeding

Emulsions may be used while breastfeeding, but specific product information should be consulted to ensure safety.

Storage

Store at room temperature, away from light and moisture. Specific formulations may have unique storage requirements.

Indications

• Solvent in pharmaceutical formulations
• Moisturizer and humectant in topical applications
• Potential use in the management of drug solubility issues

Dosage

Children: Refer to specific formulations and clinical guidelines, as dosing varies widely based on the application and formulation.

Adults: Refer to specific formulations and clinical guidelines, as dosing varies widely based on the application and formulation.

Mechanism of action

Glycols, particularly propylene glycol, act as humectants, which help to retain moisture in formulations. They can also enhance the solubility of drugs, aiding in their absorption when used as excipients. Propylene glycol is metabolized in the liver to lactate and subsequently to glucose, providing a source of energy when utilized in metabolic pathways.

Pharmacodynamics

The pharmacodynamics of glycols involve their ability to modulate the viscosity of solutions and enhance the solubility of other compounds. Propylene glycol can also facilitate the absorption of other drugs when used in formulations. It exhibits a low toxicity profile when used appropriately, but excessive systemic exposure can lead to metabolic acidosis and other adverse effects.

Pharmacokinetics

Glycols are rapidly absorbed when administered intravenously or orally. Propylene glycol is metabolized primarily in the liver, with a half-life varying based on the dose and individual metabolism. Renal excretion plays a role in the elimination of metabolites. Accumulation can occur in individuals with impaired liver or kidney function, necessitating careful monitoring of dosing in such populations.

Pregnancy

The safety of glycol in pregnancy is not well established. Consult healthcare professionals before use.

Breast-feeding

Glycol's effects during breastfeeding are not well characterized. Caution is advised.

Storage

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

Indications

• Plant growth regulation
• Agricultural applications as a growth inhibitor

Dosage

Children: Not applicable.

Adults: Refer to the relevant agricultural guidelines for specific applications.

Mechanism of action

In an in vitro study, propylene acts as a plant growth inhibitor by inhibiting the oxidation of indole-3-acetic acid by peroxidase in the presence of superoxide anion radicals. This inhibition is linked to the activation of an iron complex (compound III) shuttle, which enhances the reaction rate between superoxide and peroxidase, ultimately affecting plant growth processes. Propylene is a less effective inhibitor compared to ethylene.

Pharmacodynamics

The pharmacodynamic effects of propylene are primarily observed in its role as a growth inhibitor in plants. By modulating the oxidation of phytohormones like indole-3-acetic acid, propylene can influence various growth responses in plants, potentially affecting processes such as cell elongation and division.

Pharmacokinetics

Information on the pharmacokinetics of propylene in humans is not well-documented, as its primary uses are industrial and agricultural. Its metabolism may be influenced by environmental factors, and its effects are primarily studied in the context of plant biology rather than human pharmacology.

Dosage

Children: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Adults: Refer to specific drug formulations and product labels as purified substances can vary widely in their use and dosing.

Mechanism of action

The mechanism of action for purified compounds varies widely depending on the specific substance. Generally, purified drugs exert their effects by interacting with specific biological targets, such as receptors, enzymes, or ion channels, leading to a desired therapeutic effect. This interaction can involve binding to receptors to activate or inhibit signaling pathways, modulating enzymatic activity, or altering physiological processes.

Pharmacodynamics

Pharmacodynamics describes the effects of a drug on the body and the relationship between drug concentration and effect. For purified drugs, this can involve dose-response relationships and the time course of their action. The purified form often enhances potency and reduces variability in response among patients, which can lead to more predictable therapeutic outcomes. The overall effect is determined by the drug's affinity for its target, the efficacy of the drug-receptor interaction, and the downstream signaling pathways activated as a result of this interaction.

Pharmacokinetics

Pharmacokinetics involves the absorption, distribution, metabolism, and excretion (ADME) of a drug. For purified substances, absorption can be more efficient due to the absence of impurities that may affect solubility or stability. Distribution may also be enhanced, leading to higher bioavailability. Metabolism can be influenced by the structure of the purified compound, as it may be metabolized more readily by liver enzymes. Excretion typically occurs through the kidneys or liver, depending on the molecular characteristics of the purified drug.

Pregnancy

Consult with a healthcare professional, as the safety of purified forms of medications during pregnancy may vary depending on the specific substance.

Breast-feeding

Consult with a healthcare professional, as the safety of purified forms of medications during breastfeeding may vary depending on the specific substance.

Storage

Store in a cool, dry place, away from light and moisture, and keep out of reach of children.

Indications

• Flatulence
• Bloating
• Gastroesophageal reflux disease
• Functional dyspepsia

Dosage

Children: For children, refer to the BNF for Children for specific dosing recommendations.

Adults: The usual adult dose is 40 to 125 mg taken after meals and at bedtime, as needed.

Mechanism of action

Simethicone is a surfactant that decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. It acts by forming a film of low surface tension that promotes the coalescence of mucus-surrounded gas bubbles, allowing for easier passage of gas.

Pharmacodynamics

Simethicone decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. Its effects are generally short-lived, as it is typically administered as needed. The therapeutic index is wide since it is not absorbed systemically, making it safe for use in various patient populations.

Pharmacokinetics

Simethicone is not systemically absorbed following oral administration, which contributes to its safety profile. Due to its lack of systemic absorption, specific pharmacokinetic parameters such as half-life, clearance, and volume of distribution are not applicable.

Pregnancy

Simethicone can be used during pregnancy as there are no known risks associated with its use.

Breast-feeding

Simethicone is considered safe to use during breastfeeding, as it is not absorbed systemically.

Storage

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

Formulations

• Oral suspension
• Chewable tablets
• Soft gels

Indications

• Coccidiosis
• Protozoan infections

Dosage

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

Adults: Refer to the BNF for specific dosing guidelines.

Mechanism of action

Toltrazuril acts by inhibiting the mitochondrial respiratory chain of protozoa, leading to a disruption of ATP synthesis. This mechanism results in the inhibition of the growth and reproduction of coccidia, particularly Eimeria species, by impairing their energy metabolism.

Pharmacodynamics

Toltrazuril exhibits its effects through selective targeting of the protozoan parasites' mitochondrial functions. The disruption of ATP synthesis results in reduced energy availability for cellular processes, ultimately leading to the death of the parasite. It has a high efficacy against various stages of the coccidian life cycle.

Pharmacokinetics

Toltrazuril is well absorbed after oral administration, with peak plasma concentrations occurring within a few hours. It is extensively metabolized in the liver, with metabolites contributing to its pharmacological activity. The elimination half-life allows for sustained effects against parasitic infections. The drug is primarily excreted via feces.

Pregnancy

There is limited data on the use of toltrazuril in pregnancy. It should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether toltrazuril is excreted in human milk. Caution should be exercised when administering toltrazuril to nursing women.

Storage

Store below 30°C. Protect from light and moisture.

Indications

• Thickening agent in food products
• Stabilizer in pharmaceutical formulations
• Emulsifier in cosmetic products
• Dietary fiber supplement

Dosage

Children: Dosage should be determined based on specific formulations and medical advice. Refer to the BNF for Children for detailed guidance.

Adults: Dosage depends on the specific formulation and purpose. Refer to product-specific guidelines or consult the BNF.

Mechanism of action

Xanthan gum works by forming a viscous gel in the presence of water. This gelling property is due to its unique molecular structure, which consists of a repeating unit of glucose, mannose, and glucuronic acid. When hydrated, xanthan gum can create a three-dimensional network that traps water, thus increasing the viscosity of the solution. This ability to enhance the texture and stability of various formulations is what makes xanthan gum a valuable ingredient in many products.

Pharmacodynamics

The pharmacodynamic properties of xanthan gum are primarily related to its thickening and stabilizing effects. It does not possess any pharmacological activity in the traditional sense, as it is not absorbed into the systemic circulation. Instead, its primary function is to modify the rheological properties of the formulations it is included in, affecting how they flow and interact with other ingredients.

Pharmacokinetics

Xanthan gum is not metabolized by the body and is considered safe for consumption. It is largely excreted unchanged in the feces. The gastrointestinal absorption of xanthan gum is minimal, which means it does not exert systemic effects. Upon ingestion, it may contribute to dietary fiber intake, promoting digestive health. Its viscosity can also influence gastrointestinal transit time, potentially providing a feeling of fullness.

Adverse effects

• Gastrointestinal discomfort
• Flatulence
• Diarrhea
• Bloating
• Allergic reactions (rare)

Precautions

• Use with caution in individuals with gastrointestinal disorders
• Monitor for allergic reactions in sensitive individuals

Pregnancy

Xanthan gum is generally considered safe for use during pregnancy as it is a food additive and not absorbed in significant amounts.

Breast-feeding

Xanthan gum is considered safe during breastfeeding as it is not absorbed systemically.

Storage

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

Formulations

• Powder
• Gel
• Liquid
• Capsules

Mechanism of action

Recent studies suggest that docusate's mechanism of action is due largely to it's surfactant effect in the intestines, which allow fat and water into the feces to soften the stool. Docusate’s mechanism of action was investigated in 1985 on healthy patients. Docusate was added directly to the jejunum based on calculated concentrations of docusate in the jejunum. At this concentration, there was an increase in secretion of water, sodium, chloride, and potassium as well as a decrease in absorption of glucose and bicarbonate. Based on in vitro data, the authors suggested this effect was due to an increase in intracellular cyclic AMP either directly through docusate or E series prostaglandins.

Pharmacodynamics

Docusate sodium is a laxative and an anionic detergent that supposedly promotes incorporation of water and fats into stool through a reduction in surface tension, resulting in softer fecal mass. Docusate's onset of action is 6-72 hours orally and 2-15 minutes rectally. The effects of docusate are thought to be exerted locally in the jejunum.

Mechanism of action

In an in vitro study of the mechanism of action of ethylene as a plant growth inhibitor, the effects of ethylene and some of its analogs, including propylene, on the oxidation of indole-3-acetic acid were examined. Ethylene and its analogs inhibited the oxidation of indole-3-acetic acid by peroxidase under conditions where the iron complex (compound III, an oxy-ferrous complex of peroxidase) shuttle was activated. Inhibition occurred only in the presence of the superoxide anion radical 02(-). Spectral and kinetic data indicated that ethylene and its analogs enhanced the rate of reaction of 02(-) with peroxidase; ie, the iron complex (compound III) shuttle, resulting in the formation of compound III. Propylene was a less effective inhibitor than ethylene.

Mechanism of action

Simethicone is a surfactant that decreases the surface tension of gas bubbles in the gastrointestinal tract, more easily allowing gas to exit the body. The clinical use of simethicone is based on its antifoam properties. Silicone antifoams spread on the surface of aqueous liquids, forming a film of low surface tension and thus causing collapse of foam bubbles. Simethicone reportedly allows mucus-surrounded gas bubbles in the GI tract to coalesce and be expelled.

Pharmacodynamics

Simethicone decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. It has a short duration of action as it is generally given as needed, and a wide therapeutic index as it is not systemically absorbed.