SEDAFOL

Indications

• Constipation
• Bowel cleansing

Dosage

Children: Child 1–11 months: 1 g as required, Child 1–11 years: 2 g as required, Child 12–17 years: 4 g as required.

Adults: 4 g as required, usually administered rectally.

Mechanism of action

When administered rectally, glycerol exerts a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexively stimulating evacuation. It decreases intraocular pressure by creating an osmotic gradient between the blood and intraocular fluid, causing fluid to move from the aqueous and vitreous humors into the bloodstream. Glycerol is classified as a hyperosmotic laxative and may also have lubricating and fecal softening effects.

Pharmacodynamics

Glycerol is commonly classified as an osmotic laxative, acting through its local irritant effects and possibly having lubricating and fecal softening actions. Glycerol suppositories usually produce effects within 15 to 30 minutes, providing quick relief from constipation.

Pharmacokinetics

Glycerol is rapidly absorbed through the gastrointestinal tract. It is metabolized in the liver and other tissues, with a half-life that varies depending on the route of administration. Following rectal administration, glycerol is primarily excreted in urine. The pharmacokinetics may vary based on dosage forms and individual patient factors.

Contra-indications

• Acute abdominal conditions
• Acute inflammatory bowel disease
• Intestinal obstruction
• Severe dehydration

Adverse effects

• Abdominal cramps
• Asthenia
• Gastrointestinal disorders
• Hypermagnesaemia
• Skin reactions
• Urine discolouration

Precautions

• Avoid prolonged contact with skin, especially in incontinent patients or infants wearing nappies due to the risk of irritation and excoriation.
• Excessive use may cause diarrhea and related effects such as hypokalaemia.

Pregnancy

Manufacturers advise avoidance due to limited information available.

Breast-feeding

Manufacturers advise avoidance as there is no information available.

Storage

Store at room temperature, away from direct sunlight.

Formulations

• Glycerol 1g suppositories
• Glycerol 2g suppositories
• Glycerol 4g suppositories
• Glycerol oral suspension

Indications

• Induction of general anesthesia
• Maintenance of general anesthesia
• Sedation for procedures

Dosage

Children: For children aged 1 month to 16 years, the usual dose for induction of anesthesia is 2.5–4 mg/kg, adjusted according to age, body weight, and response.

Adults: For induction of anesthesia, the usual adult dose is 1.5–2.5 mg/kg administered by slow intravenous injection. For maintenance, a continuous infusion of 4–12 mg/kg/hour may be used.

Mechanism of action

Propofol exerts its anesthetic effects by positively modulating the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) at GABA-A receptors, leading to increased inhibitory neurotransmission and resulting in sedation and anesthesia.

Pharmacodynamics

As a sedative-hypnotic agent, propofol rapidly induces hypnosis with minimal excitation, typically within 40 seconds after intravenous administration. This rapid action is due to its high lipid solubility, allowing for quick distribution to the central nervous system. The drug also has a favorable recovery profile, with patients often regaining consciousness shortly after cessation of the infusion.

Pharmacokinetics

Propofol is highly lipophilic, leading to rapid distribution and a short half-life. It is primarily metabolized in the liver via conjugation and oxidation, and excreted in urine, mainly as metabolites. The drug has a volume of distribution of around 4 liters per kilogram, and its clearance is approximately 1.5 liters per minute, which results in a short duration of action.

Contra-indications

• Hypersensitivity to propofol or any of its components
• Severe respiratory depression
• Acute porphyrias
• Acute circulatory failure (shock)
• Adrenal insufficiency

Adverse effects

• Apnea
• Hypotension
• Nausea
• Respiratory disorders
• Skin reactions
• Vascular pain
• Vomiting
• Arrhythmias
• Cough
• Hiccups
• Hypertension
• Muscle rigidity
• Neuromuscular dysfunction
• Nystagmus
• Procedural complications

Interactions

• Valproate may increase propofol concentration
• Active component of sacituzumab govitecan may increase exposure to propofol

Precautions

• Careful monitoring of fluids and electrolytes
• Use with caution in patients with cardiovascular disease
• Elderly patients may require dose adjustment
• Avoid in patients with fixed cardiac output, hypovolaemia, or severe hypotension

Pregnancy

Propofol should be used during pregnancy only if clearly needed and after careful consideration of risks and benefits.

Breast-feeding

Propofol is excreted in breast milk; caution should be exercised when administered to breastfeeding women.

Storage

Store at room temperature, protect from light, and do not freeze.

Formulations

• Emulsion for injection
• 0.5% or 1% injection solution

Dosage

Children: There are no established pediatric dosing guidelines for Been, as it is not approved for use in children. Further research is needed to determine safe and effective dosages.

Adults: Specific dosing guidelines for adults are not yet established due to the drug's experimental status. Clinicians are advised to refer to ongoing clinical trial protocols for dosing information.

Mechanism of action

The exact mechanism of action of Been is not fully elucidated, but it is thought to engage specific biological pathways that modulate cellular functions. Preliminary studies suggest it may influence neurotransmitter systems or target receptors involved in signaling pathways.

Pharmacodynamics

Been's pharmacodynamics are still being characterized as research continues. Initial findings imply it may have effects on various physiological systems, potentially altering metabolic processes, immune responses, or neurochemistry, depending on the targeted indications.

Pharmacokinetics

The pharmacokinetic profile of Been, including absorption, distribution, metabolism, and excretion, has not been thoroughly studied. Ongoing clinical trials aim to provide clear data regarding its bioavailability, half-life, and elimination pathways.

Indications

• Electrolyte replacement
• Volume expansion in hypovolemic patients
• Management of hyponatremia
• Support in intravenous fluid therapy

Dosage

Children: Refer to the BNF for Children for appropriate dosing in paediatric patients, as dosages may vary based on the formulation and clinical condition.

Adults: Refer to specific product information or clinical guidelines for dosage recommendations, as disodium is often part of combination products.

Mechanism of action

Disodium compounds often function by providing sodium ions that are essential for various physiological processes. Sodium ions play a critical role in maintaining osmotic balance, nerve impulse transmission, and muscle contraction. In the context of intravenous solutions, disodium helps to restore electrolyte balance in patients.

Pharmacodynamics

The pharmacodynamics of disodium is primarily related to its role in electrolyte balance and fluid homeostasis. Sodium ions are vital for the function of excitable tissues, including neurons and muscle cells. Changes in sodium levels can affect blood pressure, hydration status, and overall cellular function.

Pharmacokinetics

The pharmacokinetics of disodium compounds depend on their specific formulation and route of administration. When administered intravenously, disodium is rapidly distributed in the extracellular fluid, where it helps to maintain osmotic pressure. Sodium is primarily excreted by the kidneys, and its levels can be influenced by fluid intake, dietary sodium, and renal function.

Pregnancy

Use with caution. Consult a healthcare provider for specific guidance.

Breast-feeding

Use with caution. Consult a healthcare provider for specific guidance.

Storage

Store at room temperature, away from moisture and direct sunlight.

Indications

• Lead poisoning
• Mercury poisoning
• Calcium overload
• Certain diagnostic procedures involving heavy metals

Dosage

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

Adults: Refer to the BNF for specific dosing guidelines based on the condition being treated, considering factors such as the severity of metal poisoning and renal function.

Mechanism of action

Edetate functions by forming stable complexes with divalent and trivalent metal ions, including lead and calcium, through its multiple carboxylate and amine groups. This chelation renders the metals more soluble and promotes their renal excretion, thereby reducing their toxic effects in the body.

Pharmacodynamics

The chelation of metals by edetate decreases the free metal concentration in the bloodstream, which mitigates the toxic effects associated with heavy metal accumulation. The efficacy of edetate in removing metals such as lead has been well documented, and its ability to bind calcium can influence calcium homeostasis in certain clinical scenarios.

Pharmacokinetics

Edetate is administered intravenously, with rapid distribution throughout the extracellular fluid. It is primarily excreted unchanged by the kidneys. The onset of action occurs quickly after administration, and the duration depends on the dose and the patient's renal function. The elimination half-life is approximately 1 hour but may vary based on renal clearance.

Contra-indications

• Hypersensitivity to edetate or any component of the formulation
• Severe renal impairment
• Active bleeding disorders

Adverse effects

• Hypocalcemia
• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Headache
• Rash
• Fever

Interactions

• May enhance the effects of anticoagulants
• Concurrent use with calcium supplements may reduce effectiveness
• May interfere with the absorption of certain medications due to changes in gastrointestinal motility

Precautions

• Use with caution in patients with renal impairment
• Monitor electrolyte levels, particularly calcium, during treatment
• Assess the patient's hydration status before administration

Pregnancy

Limited data on the use of edetate in pregnancy. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution is advised as it is not known whether edetate is excreted in human milk. Weigh the risks and benefits before use.

Storage

Store in a cool, dry place, protected from light. Do not freeze.

Formulations

• Edetate disodium injection
• Edetate calcium disodium injection

Dosage

Children: Refer to specific guidelines for pediatric dosing; consult the BNF for Children for accurate dosage information.

Adults: Refer to specific guidelines for use; dosage may vary based on the context of use.

Mechanism of action

Hydroxide ions act primarily as bases, neutralizing acids to form water and salts. They participate in various biochemical pathways, including selenium metabolism and the degradation of reactive oxygen species. Hydroxide can influence enzyme activity and stability by altering the pH of the environment, thereby affecting metabolic reactions.

Pharmacodynamics

Hydroxide ions can impact biological processes by changing the local pH, which influences enzyme activity, ion transport, and the solubility of other compounds. Their ability to neutralize acids can help regulate physiological pH, contributing to homeostasis in living organisms.

Pharmacokinetics

As an inorganic ion, hydroxide does not undergo traditional pharmacokinetic processes like absorption, distribution, metabolism, or excretion. Instead, it is rapidly equilibrated in biological fluids and participates in acid-base reactions, having immediate effects on the local environment.

Pregnancy

There is limited information regarding the use of hydroxide during pregnancy. Consult a healthcare professional for advice.

Breast-feeding

Limited data is available on the excretion of hydroxide in breast milk. Consult a healthcare professional before use.

Storage

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

Indications

• Cholesterol management
• Cognitive support
• Liver health
• Emulsification in food products

Dosage

Children: Refer to the BNF for Children for specific dosing information as it may vary based on the formulation and indication.

Adults: Refer to the BNF for specific dosing information as it may vary based on the formulation and indication.

Mechanism of action

Lecithin serves as a source of phosphatidylcholine, a key component of cell membranes. It facilitates the transport of fats and cholesterol in the body, enhancing lipid metabolism. Additionally, phosphatidylcholine is involved in the synthesis of acetylcholine, a neurotransmitter important for memory and muscle function.

Pharmacodynamics

Lecithin has been shown to influence lipid metabolism, potentially lowering serum cholesterol levels and improving liver function. By serving as an emulsifying agent, it helps to increase the bioavailability of fat-soluble vitamins and other nutrients. Its role in cell membrane integrity supports overall cellular function and health.

Pharmacokinetics

Lecithin is absorbed in the gastrointestinal tract and metabolized in the liver. It is distributed throughout the body, where it is incorporated into cell membranes. The half-life of lecithin is not well-defined due to its nature as a dietary compound, but its components, such as phosphatidylcholine, are rapidly utilized by the body.

Pregnancy

Lecithin may be used during pregnancy, but it is essential to consult a healthcare provider before use.

Breast-feeding

Lecithin is generally considered safe while breastfeeding; however, it is advisable to seek medical advice.

Storage

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

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.

Dosage

Children: Refer to specific product guidelines for dosing information.

Adults: Refer to specific product guidelines for dosing information.

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Abdominal pain
• Headache
• Dizziness
• Fatigue

Precautions

• Use with caution in patients with a history of gastrointestinal disorders.
• Monitor for signs of allergic reactions.

Pregnancy

Safety in pregnancy has not been established, use only if clearly needed.

Breast-feeding

Consult a healthcare provider before use while breastfeeding.

Storage

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

Indications

• Management of menopausal symptoms
• Cardiovascular health improvement
• Cholesterol reduction
• Dietary protein source
• Potential role in cancer prevention

Dosage

Children: Refer to specific dietary guidelines and recommendations for children, as soya products can be part of a balanced diet.

Adults: Refer to specific dietary guidelines as soya is primarily consumed as a food source rather than a pharmacological agent.

Mechanism of action

Soya exerts its effects primarily through its isoflavones, which are phytoestrogens that can bind to estrogen receptors in the body. This action can modulate estrogen activity, leading to various physiological effects, such as alleviating menopausal symptoms and influencing lipid metabolism. Additionally, the protein in soya can help lower cholesterol levels and improve cardiovascular health by enhancing endothelial function and reducing inflammation.

Pharmacodynamics

The pharmacodynamics of soya is largely attributed to its isoflavone content, including genistein and daidzein. These compounds can mimic estrogen and may exert both estrogenic and anti-estrogenic effects depending on the tissue type. The consumption of soya has been associated with improvements in lipid profiles, reductions in blood pressure, and potential protective effects against certain cancers, particularly hormone-dependent cancers.

Pharmacokinetics

The bioavailability of isoflavones from soya varies but is generally well-absorbed following consumption. After ingestion, isoflavones undergo extensive metabolism in the liver and intestines, leading to the formation of various metabolites that can be detected in the plasma. The elimination half-life of these metabolites varies, but they are typically cleared from the body within hours to a few days, depending on individual metabolism and the amount consumed.

Contra-indications

• Hypersensitivity to soya or any of its components
• Severe soy allergy

Adverse effects

• Gastrointestinal discomfort
• Nausea
• Diarrhea
• Allergic reactions, including rash and itching
• Headache
• Fatigue

Interactions

• May interact with anticoagulants, increasing bleeding risk
• Potential interaction with thyroid medications, affecting thyroid hormone levels

Precautions

• Use with caution in individuals with a history of allergic reactions to legumes
• Monitor for possible hormonal effects in individuals with hormone-sensitive conditions

Pregnancy

Soya is generally considered safe in moderation during pregnancy, but high doses should be avoided due to potential hormonal effects.

Breast-feeding

Soya is usually considered safe during breastfeeding, but excessive consumption should be avoided as effects on infants are not fully understood.

Storage

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

Formulations

• Soybeans (whole or processed)
• Soy milk
• Soy protein isolate
• Soy flour
• Soy lecithin

Indications

• Nutritional supplement
• Source of essential fatty acids
• Support for eye health
• Potential cardiovascular health benefits

Dosage

Children: Refer to established dietary guidelines for children. Egg yolk can be introduced as part of a balanced diet, usually around 6 months of age, depending on individual dietary recommendations.

Adults: Refer to established dietary guidelines for egg consumption. Generally, 1 to 2 whole eggs per day is considered safe for most adults.

Mechanism of action

Egg yolk contains several bioactive compounds, including phospholipids and sterols, which may contribute to its health benefits. The cholesterol in egg yolk is crucial for the synthesis of various hormones and cellular membranes. Lutein and zeaxanthin, carotenoids found in the yolk, are known to accumulate in the retina and may help protect against age-related macular degeneration by filtering harmful blue light and acting as antioxidants.

Pharmacodynamics

The bioactive components of egg yolk, such as phospholipids and carotenoids, exhibit various pharmacodynamic effects. Lutein and zeaxanthin are antioxidants that help to reduce oxidative stress, which is associated with various chronic conditions. The presence of healthy fats in egg yolk can also influence lipid metabolism and improve the absorption of fat-soluble vitamins.

Pharmacokinetics

Nutrient absorption from egg yolk occurs primarily in the small intestine, where fats are emulsified by bile salts and digested by enzymes. The lipids and fat-soluble vitamins are then absorbed into the lymphatic system before entering the bloodstream. The bioavailability of nutrients from egg yolk can be influenced by several factors, including the overall diet and cooking methods. For example, cooking eggs can enhance the absorption of certain nutrients.

Pregnancy

Yolk is generally considered safe during pregnancy as it is a natural food source rich in essential nutrients. However, it is advisable to consume it in moderation and ensure it is properly cooked to avoid the risk of salmonella.

Breast-feeding

Yolk can be consumed while breastfeeding, as it provides beneficial nutrients. However, it should be introduced in moderation as part of a balanced diet.

Storage

Yolk should be stored in the refrigerator at or below 4°C. It is best used fresh and should be consumed or cooked promptly after separation from the egg.

Formulations

• Raw egg yolk
• Cooked egg yolk

Mechanism of action

When administered rectally, glycerin exerts a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexively stimulating evacuation. Glycerin decreases intraocular pressure by creating an osmotic gradient between the blood and intraocular fluid, causing fluid to move out of the aqueous and vitreous humors into the bloodstream. Glycerin (glycerol) and sorbitol are hyperosmotic laxatives. When administered rectally, glycerin and sorbitol exert a hygroscopic and/or local irritant action, drawing water from the tissues into the feces and reflexly stimulating evacuation. The extent to which the simple physical distention of the rectum and the hygroscopic and/or local irritant actions are responsible for the laxative effects of some of these drugs is not known. Only extremely high oral doses of sorbitol (25 g daily) or glycerin exert laxative action. /Glycerin/ decreases intraocular pressure by creating an osmotic gradient between the blood and intraocular fluid, causing fluid to move out of the aqueous and vitreous humors into the bloodstream. The physicochemical effects of a series of alkanols, alkanediols and glycerol on erythrocyte shape and hemolysis at 4 and 20 degrees C were examined. We calculated the dielectric constant of the incubation medium, Ds, and the dielectric constant of the erythrocyte membrane Dm in the presence of organic solutes. The ratio Ds/Dm = -38.48 at 20 degrees C defines the normal biconcave shape in a medium without hemolytic agents. A decrease in Ds/Dm favors externalization or internalization with consequent hemolysis. Alkanols and alkanediols convert biconcave erythrocytes into echinocytes, which is accompanied by an increase in the projected surface area. Glycerol converts biconcave erythrocytes into stomatocytes, which was accompanied by a marginal decrease in the projected surface area. Progressive externalization in alkanols and alkanediols or internalization in glycerol resulted in a decrease in the projected surface area and the formation of smooth spheres. The degree of shape change induced was related to the degree of hemolysis and the ratio Ds/Dm. A decrease in temperature reduced both the degree of shape change and hemolysis. .../Thus/ physicochemical toxicity may be a result of a temperature dependent hydrophobic interaction between the organic solutes and the membrane and is best interpreted by the ability of the solutes to change Ds and Dm.

Pharmacodynamics

Glycerin is commonly classified as an osmotic laxative but may act additionally or alternatively through its local irritant effects; it may also have lubricating and fecal softening actions. Glycerin suppositories usually work within 15 to 30 minutes.

Mechanism of action

The action of propofol involves a positive modulation of the inhibitory function of the neurotransmitter gama-aminobutyric acid (GABA) through GABA-A receptors.

Pharmacodynamics

Propofol is a sedative-hypnotic agent for use in the induction and maintenance of anesthesia or sedation. Intravenous injection of a therapeutic dose of propofol produces hypnosis rapidly with minimal excitation, usually within 40 seconds from the start of an injection (the time for one arm-brain circulation).