Esomac 10 mg Granules

Indications

• Gastroesophageal reflux disease (GERD)
• Erosive esophagitis
• Peptic ulcers
• Helicobacter pylori eradication
• Zollinger-Ellison syndrome

Dosage

Adults: The usual oral dose

Mechanism of action

Esomeprazole exerts its stomach acid-suppressing effects by covalently binding to cysteine residues on the H+/K+-ATPase enzyme at the secretory surface of gastric parietal cells. This action inhibits both basal and stimulated gastric acid secretion irreversibly, requiring the synthesis of new enzyme to restore acid production. By blocking the final step of gastric acid production, esomeprazole reduces gastric acidity in a dose-dependent manner.

Pharmacodynamics

Esomeprazole is a substituted benzimidazole that inhibits gastric acid secretion without exhibiting anticholinergic or H2 receptor antagonistic properties. It is indicated for the treatment of GERD, healing of erosive esophagitis, and eradication of H. pylori to reduce duodenal ulcer recurrence. The suppression of gastric acid secretion is dose-related and effective against various stimuli that promote acid secretion.

Pharmacokinetics

Esomeprazole is rapidly absorbed after oral administration, with peak plasma concentrations typically occurring within 1-2 hours. It undergoes extensive hepatic metabolism primarily by the cytochrome P450 system, especially CYP2C19, resulting in several metabolites. The elimination half-life is approximately 1-2 hours, though its antisecretory effects last longer. It is excreted predominantly in the urine. Dose adjustments may be necessary in patients with hepatic impairment.

Contra-indications

• Hypersensitivity to esomeprazole or any of its components
• Concomitant use with rilpivirine-containing products

Adverse effects

• Abdominal pain
• Constipation
• Diarrhea
• Dizziness
• Dry mouth
• Headache
• Insomnia
• Nausea
• Skin reactions
• Vomiting
• Bone fractures
• Confusion
• Depression
• Drowsiness
• Leucopenia
• Malaise
• Myalgia
• Paraesthesia
• Peripheral edema
• Thrombocytopenia
• Vertigo
• Vision disorders
• Agranulocytosis
• Alopecia
• Gynaecomastia
• Hallucination
• Hepatic disorders
• Hyperhidrosis
• Hyponatraemia
• Nephritis
• Tubulointerstitial nephritis
• Pancytopenia
• Photosensitivity reaction
• Severe cutaneous adverse reactions (SCARs)
• Stomatitis
• Taste altered
• Hypomagnesaemia

Interactions

• Esomeprazole may increase the exposure to cannabidiol
• Esomeprazole may increase the exposure to cilostazol

Precautions

• Increased risk of fractures, particularly in the elderly and when used at high doses for over a year
• Caution in patients at risk of osteoporosis; adequate intake of calcium and vitamin D is recommended
• May increase the risk of gastrointestinal infections, including Clostridioides difficile
• Symptoms of gastric cancer should be ruled out before treatment
• Use with caution in patients with hepatic impairment

Pregnancy

Use with caution. The manufacturer advises avoiding use unless necessary since the effects on the fetus are not fully known.

Breast-feeding

Manufacturer advises avoiding use as esomeprazole is present in breast milk and may cause diarrhea in nursing infants. However, amounts are probably too small to be harmful.

Storage

Store in a cool, dry place below 25°C. Keep out of

Dosage

Children: Refer to specific guidelines or consult the BNF for appropriate dosage.

Adults: Refer to specific guidelines or consult the BNF for appropriate dosage.

Mechanism of action

Acrylate acts as a reactive compound that can participate in various biochemical reactions. It may undergo conjugation with glutathione and other biomolecules, leading to detoxification or metabolic transformation. The involvement of acrylate in the metabolism of seleno-compounds suggests a role in the detoxification pathways, where it may facilitate the elimination of harmful substances from the body.

Pharmacodynamics

Acrylate does not have established pharmacodynamic effects as a therapeutic agent, as it is primarily recognized for its industrial applications. However, its interactions with biological macromolecules can lead to cytotoxic effects, especially at high concentrations. It is known to be a skin and respiratory irritant, and prolonged exposure may result in a range of toxicological effects.

Pharmacokinetics

The pharmacokinetics of acrylate in humans have not been extensively studied, but it is known to be rapidly absorbed through the skin and respiratory tract. Once in the body, acrylate can undergo biotransformation primarily through conjugation with glutathione, leading to more water-soluble metabolites that can be excreted via urine. The compound's half-life and distribution in human tissues are not well-characterized.

Pregnancy

The safety of acrylate during pregnancy has not been fully established. It is advisable to avoid use unless deemed absolutely necessary by a healthcare professional.

Breast-feeding

Limited data exist on the use of acrylate during breastfeeding. Caution is advised, and it should only be used if the benefits outweigh potential risks.

Storage

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

Indications

• Constipation
• Dietary fiber supplementation
• Irritable bowel syndrome
• Diverticular disease
• Weight management

Dosage

Children: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.

Adults: Refer to appropriate guidelines for specific dosage; generally taken with adequate fluid intake.

Mechanism of action

Cellulose acts primarily as a bulk-forming laxative. It absorbs water in the intestines, which increases stool bulk and stimulates peristalsis, thus facilitating bowel movements. Additionally, cellulose is not digestible by human enzymes, leading to fermentation by gut bacteria, which may enhance gut health and alter gut microbiota composition.

Pharmacodynamics

Cellulose increases stool weight and frequency of bowel movements. It works by retaining water in the intestines, leading to softer stools and improved passage through the gastrointestinal tract. The bulking effect of cellulose can help alleviate constipation and promote overall digestive health. It may also play a role in cholesterol reduction and glycemic control through its effects on digestion and absorption of nutrients.

Pharmacokinetics

Cellulose is not absorbed into the bloodstream due to its indigestible nature. Instead, it passes through the gastrointestinal tract, where it adds bulk to the stool. Its fermentation by colonic bacteria produces short-chain fatty acids, which may have beneficial effects on colon health. The onset of action for cellulose as a laxative can vary but is generally within 24 to 72 hours after ingestion.

Adverse effects

• Bloating
• Flatulence
• Diarrhea
• Abdominal discomfort

Precautions

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

Pregnancy

Cellulose is generally considered safe during pregnancy as it is a non-toxic, indigestible fiber.

Breast-feeding

Cellulose is also considered safe during breastfeeding; it is excreted in breast milk in negligible amounts.

Storage

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

Formulations

• Powder
• Capsules
• Tablets
• Granules

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

• Drug delivery systems
• Biodegradable implants
• Controlled release formulations
• Tissue engineering
• Medical device coatings

Dosage

Children: As with adult dosing, paediatric dosing of copolymers is specific to the formulation and application. Consult relevant pediatric pharmacology resources for detailed dosing recommendations.

Adults: Dosing of copolymers is highly variable and dependent on the specific drug formulation and intended use. For precise dosing information, refer to established pharmacological guidelines or product-specific resources.

Mechanism of action

Copolymers can function as drug delivery vehicles, allowing for controlled release of therapeutic agents. They can encapsulate drugs and release them in a sustained manner, depending on environmental triggers such as pH or temperature. This mechanism enhances the efficacy of drugs while minimizing side effects.

Pharmacodynamics

The pharmacodynamic properties of copolymers depend on their composition and structure, influencing their interaction with biological systems. They can modify drug release profiles and enhance the therapeutic effects of co-administered agents, facilitating targeted delivery to specific tissues or cells.

Pharmacokinetics

The pharmacokinetics of copolymers vary based on their molecular weight, structure, and the drugs they carry. Factors such as absorption, distribution, metabolism, and excretion will depend on the formulation and the specific application. Generally, copolymers can improve drug stability and prolong circulation time in the body.

Pregnancy

The safety of copolymer use during pregnancy has not been established. Non-essential use should be avoided.

Breast-feeding

The excretion of copolymers in human milk is unknown. Caution is advised when administering to nursing mothers.

Storage

Store in a cool, dry place away from direct light. Check specific product storage requirements as they may vary.

Indications

• Used as an excipient in solid dosage forms
• Facilitates drug disintegration and dissolution

Dosage

Children: Refer to specific product formulation guidelines as crospovidone is used as an excipient and does not have a direct dosage.

Adults: Refer to specific product formulation guidelines as crospovidone is used as an excipient and does not have a direct dosage.

Mechanism of action

Crospovidone acts by rapidly absorbing water and swelling upon contact with moisture. This action leads to the disintegration of solid dosage forms, thus increasing the surface area of the active ingredients and promoting their dissolution and subsequent absorption in the gastrointestinal tract. It does not affect the pH of the formulation, ensuring that the active ingredients remain stable.

Pharmacodynamics

Crospovidone exhibits properties that enhance the bioavailability of active ingredients in pharmaceutical formulations. Its ability to rapidly disintegrate tablets and capsules leads to quicker release and absorption of the drug into systemic circulation. As a disintegrant, it aids in the effective delivery of drugs that may otherwise be poorly soluble.

Pharmacokinetics

Crospovidone itself is not absorbed systemically when administered orally. It remains in the gastrointestinal tract, where it performs its function as a disintegrant. The pharmacokinetic profile of drugs formulated with crospovidone may be influenced by the enhanced dissolution and absorption rates provided by this excipient.

Pregnancy

Crospovidone is considered to have low toxicity and is generally regarded as safe for use during pregnancy, but specific studies are limited.

Breast-feeding

There is insufficient data on the excretion of crospovidone in human milk, but it is deemed safe for use during breastfeeding.

Storage

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

Formulations

• Powder
• Tablets

Indications

• Hypoglycemia
• Caloric supplementation in patients unable to eat
• Fluid replacement therapy
• Parenteral nutrition

Dosage

Children: Paediatric doses must be determined based on clinical condition and specific needs. Refer to the BNF for Children for appropriate dosing information.

Adults: The dosage of dextrose in adults varies based on clinical condition and route of administration. For hypoglycemia, intravenous dextrose 50% (D50W) is commonly administered. Refer to the BNF for specific dosing guidelines.

Mechanism of action

Dextrose supplies energy to tissues by generating ATP and NADH through glycolysis, where glucose is phosphorylated by hexokinase to form glucose 6-phosphate. This activates glucose for breakdown, ultimately converting glucose into energy molecules. Dextrose also plays a role in gene transcription, enzyme activity, and hormone secretion, regulating glucose homeostasis and cellular metabolic integrity.

Pharmacodynamics

Blood glucose acts as a crucial energy source for cellular activities and functions as a signaling molecule. It is oxidized into carbon dioxide and water, producing energy through glycolysis, the citric cycle, and oxidative phosphorylation. Dextrose can be converted into fat for energy storage and is stored as glycogen in the liver and muscles. Its administration, particularly orally, enhances insulin secretion due to stimulation of incretin hormones.

Pharmacokinetics

Dextrose is rapidly absorbed in the gastrointestinal tract, leading to a quick elevation of blood glucose levels. It is distributed throughout the body and can be utilized by various tissues for energy. The metabolism of dextrose primarily occurs in the liver, where it can be stored as glycogen or converted into fat. Renal excretion may occur when blood glucose levels are excessively high.

Adverse effects

• Hyperglycemia
• Fluid overload
• Hypokalemia
• Thrombophlebitis at injection site

Interactions

• Corticosteroids may increase blood glucose levels
• Beta-blockers may mask symptoms of hypoglycemia
• Diuretics may cause electrolyte imbalances

Precautions

• Use with caution in patients with diabetes mellitus
• Monitor blood glucose levels regularly
• Use cautiously in patients with renal impairment or heart failure

Pregnancy

Dextrose is generally considered safe for use during pregnancy when clinically indicated, but should be used with caution.

Breast-feeding

Dextrose can be used during breastfeeding as it is a natural sugar found in breast milk.

Storage

Store at room temperature, away from direct sunlight, and protect from freezing.

Formulations

• Dextrose 5% solution for infusion
• Dextrose 10% solution for infusion
• Dextrose 50% solution for injection
• Oral dextrose tablets

Indications

• Oral medications for improved solubility
• Topical applications for enhanced delivery of active ingredients
• Parenteral formulations for intravenous administration
• Vaccines delivered as emulsions for enhanced immune response

Dosage

Children: Refer to specific product information for dosage guidelines, as this varies by formulation and intended use.

Adults: Refer to specific product information for dosage guidelines, as this varies by formulation and intended use.

Mechanism of action

The mechanism of action of a dispersion often involves the physical distribution of active pharmaceutical ingredients in a medium, which can lead to increased surface area and improved interaction with biological membranes. For example, in emulsions, the dispersion of oil in water can enhance the absorption of lipid-soluble drugs.

Pharmacodynamics

Pharmacodynamics of dispersions relates to how the dispersed formulation affects the body. The presence of surfactants or emulsifying agents can modify drug release rates, enhance absorption, and improve therapeutic effects. The effectiveness of a dispersion is influenced by particle size, viscosity, and the nature of the dispersing medium.

Pharmacokinetics

The pharmacokinetics of dispersions depend on the formulation type and the route of administration. Key factors include the rate of dispersion breakdown, absorption through biological membranes, distribution within the body, metabolism, and excretion of the active ingredients. Dispersions can alter the onset of action and duration of effect based on their formulation characteristics.

Pregnancy

Consult with a healthcare provider before use. Safety in pregnancy is not established for all formulations.

Breast-feeding

Consult with a healthcare provider before use. Safety during breastfeeding may vary depending on the formulation.

Storage

Store in a cool, dry place away from direct sunlight. Follow specific storage instructions provided by the manufacturer.

Indications

• Alcohol use disorder
• Anxiety disorders
• Sedation
• Muscle relaxation

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines in paediatric populations.

Adults: Refer to the specific BNF guidelines for dosing related to alcohol use disorder and other indications.

Mechanism of action

Ethyl groups serve primarily as substituents in organic chemistry, influencing the properties and reactivity of the parent molecules. In the context of ethanol, which contains an ethyl group, its mechanism of action involves the enhancement of gamma-aminobutyric acid (GABA) receptor activity, leading to increased inhibitory neurotransmission. This results in its sedative, anxiolytic, and muscle relaxant effects.

Pharmacodynamics

The pharmacodynamics of compounds containing the ethyl group, particularly ethanol, include its effects on the central nervous system, where it acts as a depressant. Ethanol enhances the effects of GABA, resulting in sedation, impaired motor function, and decreased anxiety. It can also affect the dopaminergic pathways, leading to the release of dopamine, which contributes to its reinforcing properties.

Pharmacokinetics

Ethanol is rapidly absorbed from the gastrointestinal tract, with peak blood concentrations typically reached within 30 to 90 minutes after consumption. It is metabolized primarily in the liver by alcohol dehydrogenase and aldehyde dehydrogenase, with a first-order elimination kinetics, typically at a rate of 10 to 15 mL of pure alcohol per hour. Ethanol is also known to exhibit a volume of distribution of approximately 0.5 to 0.7 L/kg in adults.

Indications

• Iron deficiency anemia
• Chronic blood loss
• Nutritional iron deficiency
• Pregnancy-related anemia

Dosage

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

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

Mechanism of action

Ferric ions participate in various biological processes, including oxygen transport and electron transfer. They facilitate the formation of hemoglobin in red blood cells, allowing for efficient oxygen delivery throughout the body. Ferric compounds can also promote the absorption of iron from the gastrointestinal tract by providing a more bioavailable form of iron.

Pharmacodynamics

Ferric compounds exhibit their effects primarily through the restoration of iron levels in the body. This leads to improved synthesis of hemoglobin and overall enhancement of oxygen-carrying capacity. The pharmacological action is dose-dependent, with higher doses leading to more pronounced effects on hemoglobin levels and erythropoiesis. Additionally, ferric ions can influence various metabolic pathways involved in cellular respiration and energy production.

Pharmacokinetics

Ferric is absorbed in the gastrointestinal tract, with absorption rates influenced by dietary factors and the presence of other substances in the gut. Once absorbed, ferric ions are transported in the bloodstream bound to transferrin, a transport protein. The body regulates iron levels primarily through absorption rather than excretion, and excess iron can be stored in the liver, spleen, and bone marrow. The elimination of ferric compounds is generally slow, as they are incorporated into various biological systems or stored for future use.

Contra-indications

• Hypersensitivity to ferric compounds
• Iron overload conditions such as haemochromatosis or haemosiderosis
• Chronic liver disease
• Active peptic ulcer disease

Adverse effects

• Gastrointestinal disturbances including nausea, vomiting, and constipation
• Diarrhea
• Abdominal pain
• Black stools
• Allergic reactions including rashes and anaphylaxis
• Staining of teeth (with oral formulations)

Interactions

• Antacids may reduce the absorption of oral ferric preparations
• Tetracyclines and quinolone antibiotics may have reduced absorption when taken with iron
• Ascorbic acid may enhance the absorption of iron

Precautions

• Caution in patients with a history of gastrointestinal disease
• Monitor for signs of iron overload in patients receiving repeated doses
• Use with caution in patients with renal impairment

Pregnancy

Ferric compounds are generally considered safe in pregnancy when used as directed to treat iron deficiency, but should be used under medical supervision.

Breast-feeding

Ferric compounds are excreted in breast milk in small amounts, usually considered safe but should be used under medical supervision.

Storage

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

Formulations

• Oral tablets
• Oral solution
• Intravenous injection

Indications

• Anxiety disorders
• Nausea and vomiting
• Allergic conditions
• Preoperative sedation
• Pruritus

Dosage

Children: Refer to the BNF for Children for appropriate dosing recommendations based on age and weight.

Adults: Refer to the BNF for specific dosing guidelines based on the indication and patient characteristics.

Mechanism of action

Hydroxyzine works by antagonizing the H1 histamine receptors, leading to a reduction in the effects of histamine in the body. This action helps alleviate symptoms of allergic reactions and promotes sedation. Additionally, it may exert effects on serotonin and adrenergic receptors, which could contribute to its anxiolytic properties. Hydroxyzine is also involved in various metabolic pathways, including selenium metabolism and the degradation of reactive oxygen species.

Pharmacodynamics

The pharmacodynamic effects of hydroxyzine include sedation, anxiolysis, and reduction of allergic symptoms. Its sedative effects can make it useful in managing anxiety and inducing sleep, while its antihistaminic properties help to relieve symptoms such as itching and rashes associated with allergic reactions. The onset of action is typically within 15 to 30 minutes when taken orally, with peak effects occurring within 1 to 2 hours.

Pharmacokinetics

Hydroxyzine is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring approximately 2 hours after oral administration. It is extensively metabolized in the liver, with metabolites, including cetirizine, possessing their own therapeutic effects. Hydroxyzine has a half-life of approximately 20 hours, allowing for once or twice daily dosing. It is primarily excreted in the urine, with less than 1% of the unchanged drug found in urine.

Interactions

• hydroxyzine+antiepileptics: Severe (increases risk of overheating and dehydration)
• hydroxyzine+zonisamide: Severe (increases risk of overheating and dehydration)
• hydroxychloroquine+penicillamine: Severe (increases risk of haematological toxicity)
• hydroxychloroquine+agalsidase alfa: Unknown (decreases effects)
• hydroxychloroquine+agalsidase beta: Unknown (decreases exposure)
• hydroxychloroquine+oral cholera vaccine: Unknown (decreases efficacy)
• live vaccines+hydroxy carbamide: Unknown (increases risk of generalised infection (possibly life-threatening))
• lanthanum+hydroxychloroquine: Unknown (decreases absorption)
• macrolides+hydroxychloroquine: Unknown (increases risk of serious cardiovascular adverse effects)
• hydroxychloroquine+remdesivir: Unknown (decreases effects)

Pregnancy

Safety in pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Use with caution. Hydroxychloroquine is excreted in breast milk, and effects on the infant are unknown.

Storage

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

Formulations

• Tablets
• Oral solution

Dosage

Children: Refer to product-specific guidelines or literature for dosing information, as methacrylic acid is primarily used in industrial and medical applications rather than as a direct therapeutic agent.

Adults: Refer to product-specific guidelines or literature for dosing information, as methacrylic acid is primarily used in industrial and medical applications rather than as a direct therapeutic agent.

Mechanism of action

Methacrylic acid functions primarily as a monomer that undergoes polymerization to form methacrylate-based polymers. The polymerization process can be initiated by thermal, chemical, or photoinitiated methods, resulting in the formation of cross-linked networks that provide structural integrity and durability to the final product. It interacts with radical initiators to form reactive free radicals that propagate the polymer chain growth.

Pharmacodynamics

Methacrylic acid and its derivatives exhibit good mechanical properties and biocompatibility, making them suitable for use in medical and dental applications. The polymers formed from methacrylic acid demonstrate resistance to wear, chemical degradation, and UV light, which enhances their stability and longevity in various environments. The biocompatibility of methacrylate polymers is essential for their application in medical devices, ensuring minimal adverse reactions upon implantation.

Pharmacokinetics

The pharmacokinetics of methacrylic acid is not extensively characterized due to its primary use as a polymer precursor rather than a therapeutic agent. However, when released in vivo, it is assumed to undergo rapid metabolism. The compound is likely to be absorbed through various routes, but specific absorption, distribution, metabolism, and excretion (ADME) data are limited. As a low molecular weight organic acid, it may be subject to conjugation and subsequent elimination through renal pathways.

Pregnancy

Methacrylic acid and its derivatives should be used with caution during pregnancy, as there is limited data on their safety. It is advisable to avoid use unless the potential benefits outweigh the risks.

Breast-feeding

There is insufficient information regarding the excretion of methacrylic acid into human milk. Caution is advised when administered to breastfeeding women.

Storage

Store in a cool, dry place away from direct sunlight. Keep containers tightly closed when not in use.

Indications

• Allergic conditions
• Autoimmune diseases
• Asthma and chronic obstructive pulmonary disease (COPD)
• Certain cancers (e.g., leukemia, lymphoma)
• Skin conditions (e.g., dermatitis)
• Inflammatory bowel disease
• Multiple sclerosis exacerbations
• Severe infections requiring immunosuppression

Dosage

Children: Refer to BNF for Children for specific dosing; doses vary significantly based on the child's age, weight, and condition being treated.

Adults: Refer to BNF for specific dosing; typically, initial doses range from 4 to 48 mg depending on the severity of the condition.

Mechanism of action

Methylprednisolone exerts its effects by binding to glucocorticoid receptors, leading to the modulation of gene expression. This interaction influences the transcription of anti-inflammatory proteins while suppressing the expression of pro-inflammatory genes, ultimately resulting in reduced inflammation and immune response.

Pharmacodynamics

The pharmacodynamic effects of methylprednisolone are characterized by its ability to decrease inflammation, suppress the immune response, and affect carbohydrate metabolism. Therapeutic doses lead to various systemic effects, including modification of leukocyte distribution and inhibition of cytokine production.

Pharmacokinetics

Methylprednisolone is well absorbed after oral administration, with a bioavailability of approximately 50%. It has a volume of distribution that reflects extensive tissue binding. The drug is metabolized primarily in the liver through conjugation and reduction, and its metabolites are excreted in urine. The half-life varies based on the route of administration but is generally around 18 to 36 hours.

Adverse effects

• Increased blood pressure
• Hyperglycemia
• Weight gain
• Mood changes
• Insomnia
• Gastrointestinal disturbances
• Increased susceptibility to infections

Interactions

• methylphenidate+apraclonidine: Severe (decreases effects)
• methylthioninium chloride+bupropion: Severe (increases risk of severe hypertension)
• methylphenidate+linezolid: Severe (increases risk of elevated blood pressure)
• rasagiline+methylphenidate: Severe (increases risk of a hypertensive crisis)
• mao-inhibitors+methylphenidate: Severe (increases risk of a hypertensive crisis)
• dronedarone+methylprednisolone: Moderate (increases exposure)
• miconazole+methylprednisolone: Moderate (increases concentration)
• antifungals, azoles+methylprednisolone: Moderate (increases exposure)
• crizotinib+methylprednisolone: Moderate (increases exposure)

Precautions

• Use with caution in patients with hypertension
• Monitor blood glucose levels in diabetic patients
• Consider potential for infection risk due to immunosuppression
• Evaluate for psychiatric effects in susceptible individuals

Pregnancy

Corticosteroids may be used during pregnancy if the potential benefit justifies the risk to the fetus. Careful monitoring is advised.

Breast-feeding

Corticosteroids are excreted in breast milk; caution is advised. Monitor the infant for potential effects.

Storage

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

Formulations

• Tablets
• Injectable solutions
• Topical preparations

Mechanism of action

Methylsulphate functions as a methylating agent, transferring a methyl group to nucleophiles. This process involves the formation of a sulfonium ion, which is highly reactive and can readily react with nucleophilic sites on various substrates, leading to methylation reactions.

Pharmacodynamics

The pharmacodynamics of methylsulphate is primarily related to its role as a methylating agent in biochemical reactions. It can alter the structure and function of biological molecules, potentially affecting cellular processes and signaling pathways. However, detailed pharmacodynamic studies specific to therapeutic use are limited.

Pharmacokinetics

There is limited information on the pharmacokinetics of methylsulphate, given its typical use as a reagent in laboratory settings rather than a clinical drug. When used in chemical reactions, its reactivity and transformation into other compounds would dictate its pharmacokinetic profile, which could vary significantly based on the specific context of use.

Pregnancy

There is limited data on the use of methylsulphate in pregnancy. Consult relevant guidelines.

Breast-feeding

Data on the excretion of methylsulphate in human milk is not available. Caution is advised.

Storage

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

Mechanism of action

Oxides do not have a single mechanism of action as they are a broad category of compounds. However, in general, metal oxides can exhibit catalytic properties, while non-metal oxides may participate in biochemical reactions by forming acids or bases upon dissolution in water.

Pharmacodynamics

The pharmacodynamics of oxides depend on the specific type of oxide and its interaction with biological systems. For instance, metal oxides may have antimicrobial properties, while certain non-metal oxides can influence metabolic pathways through their acid-base chemistry. The effects vary widely, necessitating specific studies for each oxide's role in therapeutic contexts.

Pharmacokinetics

The pharmacokinetics of oxides are also variable. Many metal oxides are poorly soluble and thus have limited absorption when ingested. Non-metal oxides, such as carbon dioxide, can be readily absorbed and utilized in metabolic processes. The distribution, metabolism, and excretion of oxides depend on their chemical form and the biological system in which they are involved.

Pregnancy

Not applicable as oxide is not a drug but a class of chemical compounds.

Breast-feeding

Not applicable as oxide is not a drug but a class of chemical compounds.

Storage

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

Indications

• Emulsifying agent in drug formulations
• Stabilizer for parenteral preparations
• Solubilizer for hydrophobic drug compounds
• Ingredient in topical formulations

Dosage

Children: Refer to specific product guidelines, as dosing varies based on formulation and intended use.

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

Mechanism of action

Polysorbate functions primarily as an emulsifying agent. It reduces the surface tension between immiscible liquids, allowing them to mix more easily. This property is particularly useful in stabilizing emulsions and suspensions, facilitating the delivery of active pharmaceutical ingredients in various formulations.

Pharmacodynamics

Polysorbate does not exert pharmacological effects in the traditional sense, as it does not bind to specific receptors to elicit a physiological response. Instead, it plays a crucial role in modifying the physical properties of drug formulations, thereby enhancing drug delivery and absorption. Its ability to solubilize drugs enhances their bioavailability, particularly for poorly soluble compounds.

Pharmacokinetics

Polysorbate is generally considered to be non-toxic and is not absorbed to a significant extent when administered orally. It is metabolized by the liver and excreted primarily through the gastrointestinal tract. The pharmacokinetic profile may vary depending on the route of administration and the specific formulation in which it is used.

Adverse effects

• Allergic reactions
• Skin irritation
• Gastrointestinal disturbances

Precautions

• Use cautiously in patients with known allergies to polysorbates or related compounds
• Monitor for allergic reactions in susceptible individuals

Pregnancy

Polysorbate is generally considered safe for use during pregnancy, but consult with a healthcare provider for specific cases.

Breast-feeding

Polysorbate is considered safe during breastfeeding, but consult with a healthcare provider for individual advice.

Storage

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

Formulations

• Polysorbate 20
• Polysorbate 80

Indications

• Hyperthyroidism
• Graves' disease
• Thyroid storm

Dosage

Children: Refer to the BNF

Adults: The usual initial dose of propylthiouracil in adults is 300 mg per day, divided into 3 doses. The maintenance dose is typically 100-150 mg per day, adjusted based on thyroid function tests.

Mechanism of action

Propylthiouracil acts by inhibiting the enzyme thyroid peroxidase, which is involved in the iodination of tyrosine residues in thyroglobulin, a precursor of thyroid hormones. By blocking this enzyme, PTU reduces the production of thyroxine (T4) and triiodothyronine (T3), leading to decreased thyroid hormone levels in circulation. Additionally, PTU inhibits the conversion of T4 to T3 in peripheral tissues, further contributing to its antithyroid effects.

Pharmacodynamics

The pharmacodynamic effects of propylthiouracil are primarily centered around its ability to lower thyroid hormone levels, which helps alleviate symptoms of hyperthyroidism such as increased heart rate, weight loss, and anxiety. The onset of action can vary, but therapeutic effects may be observed within several weeks of initiation. Monitoring thyroid function tests is essential to assess the efficacy and adjust dosing as needed.

Pharmacokinetics

Propylthiouracil is well absorbed from the gastrointestinal tract, though its bioavailability can be affected by factors such as food intake. The drug is extensively metabolized in the liver, and its elimination half-life averages around 1-2 hours. Most of the drug is excreted in urine as metabolites. It is important to note that due to its rapid metabolism, multiple daily doses may be required to maintain therapeutic levels.

Interactions

• propylthiouracil+metyrapone: Severe (decreases effects)

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

• Controlled drug delivery
• Targeted therapy
• Improvement of bioavailability of poorly soluble drugs

Dosage

Children: For pediatric dosing information, refer to guidelines specific to the drug being administered.

Adults: Dosage should be individualized based on the specific drug being delivered and the therapeutic goals. Refer to specific drug guidelines for accurate dosing information.

Mechanism of action

The mechanism of action of spheres primarily involves the encapsulation of active pharmaceutical ingredients (APIs) within a spherical matrix. Upon administration, the spheres can release the drug through diffusion, degradation of the matrix, or a combination of both processes. This allows for sustained or targeted delivery of the drug to specific sites within the body, improving treatment efficacy.

Pharmacodynamics

The pharmacodynamic properties of spheres depend on the drug they encapsulate and the design of the delivery system. Generally, spheres can enhance drug solubility and stability, allowing for improved bioavailability. The release profile can be tailored to achieve desired therapeutic concentrations over time, which can lead to improved patient adherence and reduced toxicity.

Pharmacokinetics

Pharmacokinetics of spheres is influenced by factors such as the size of the spheres, the material used for their construction, and the method of drug release. After administration, the spheres can be distributed through the bloodstream, and their release rates can vary based on their composition and the physiological conditions of the body. The elimination of the spheres and the encapsulated drug typically occurs via metabolic pathways and renal or hepatic clearance.

Pregnancy

Safety during pregnancy has not been established. Use only if potential benefits justify the risks to the fetus.

Breast-feeding

It is unknown whether spheres are excreted in human milk. Caution should be exercised when administered to a nursing woman.

Storage

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

Indications

• Providing energy in dietary supplementation
• Enhancing flavor in food products
• Replacement of carbohydrates in certain medical nutrition therapies

Dosage

Children: Refer to general dietary guidelines for carbohydrate intake in children. No specific dosing guidelines provided.

Adults: Refer to general dietary guidelines for carbohydrate intake. No specific dosing guidelines provided.

Mechanism of action

Sugar is metabolized in the body to provide energy. Upon ingestion, sucrose is broken down by the enzyme sucrase into its constituent monosaccharides, glucose and fructose, which are then absorbed into the bloodstream. These monosaccharides can be utilized by cells for energy or stored as glycogen in the liver and muscles.

Pharmacodynamics

As a simple carbohydrate, sugar elevates blood glucose levels rapidly after consumption, leading to increased insulin secretion from the pancreas. This insulin facilitates the uptake of glucose by tissues, promoting energy production. The rapid increase in blood sugar can provide quick energy but may also lead to potential negative effects on metabolism and weight if consumed in excess.

Pharmacokinetics

After oral administration, sugar is quickly hydrolyzed in the gastrointestinal tract. Peak plasma glucose concentrations typically occur within 30 minutes to 2 hours post-ingestion, depending on the amount consumed and individual metabolism. The half-life of glucose in the bloodstream is relatively short, as it is rapidly taken up by tissues or converted into glycogen.

Pregnancy

Sugar is generally considered safe for use during pregnancy, but excessive intake should be avoided to prevent gestational diabetes and excessive weight gain.

Breast-feeding

Sugar is safe during breastfeeding; however, excessive consumption should be avoided.

Storage

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

Formulations

• Granulated sugar
• Brown sugar
• Powdered sugar
• Liquid sugar

Indications

• Used as an excipient in drug formulations
• Pleurodesis for the management of recurrent pleural effusions

Dosage

Children: Refer to specific guidelines for paediatric use, as dosing may differ based on age and clinical condition.

Adults: Refer to specific guidelines for the appropriate dosage in pleurodesis and other applications, as it may vary based on clinical context.

Mechanism of action

Talc exhibits very good absorptive properties, allowing it to absorb moisture and other substances effectively. This characteristic is particularly useful in pharmaceutical formulations, where it may enhance the stability and texture of the drug product.

Pharmacodynamics

Talc's primary pharmacodynamic effect is its ability to act as an inert filler and bulking agent in pharmaceutical preparations. It does not have any intrinsic pharmacological activity but serves to improve the physical properties of formulations, such as flowability and compressibility.

Pharmacokinetics

Talc is not absorbed systemically when used as an excipient or in medical procedures. Its effects are local, and it remains in the site of application, where it functions primarily as a mechanical agent. The pharmacokinetics of talc in the context of its use in pleurodesis involves its ability to promote adhesion of the pleural surfaces, thereby preventing fluid accumulation.

Pregnancy

Talc is classified as a substance with minimal systemic absorption, but safety during pregnancy has not been well established. Consult relevant guidelines.

Breast-feeding

Talc is not expected to be absorbed in significant amounts; however, caution is advised and consult guidelines.

Storage

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

Indications

• Used as a thickening agent in food products
• Utilized in pharmaceutical formulations as a stabilizer
• Employed in cosmetics for texture improvement
• Applied in industrial products for its viscosity properties

Dosage

Children: Refer to specific product guidelines for appropriate use. Xanthan is used in formulations as a thickener or stabilizer, and dosage should be evaluated based on the specific product and formulation.

Adults: Refer to specific product guidelines for appropriate use. Xanthan is typically used in small quantities as a thickener or stabilizer in food and pharmaceutical products.

Mechanism of action

Xanthan functions primarily as a thickener and stabilizer. It acts by interacting with water molecules to form a gel-like consistency, which enhances the texture and stability of products. Its unique rheological properties allow it to maintain viscosity under varying conditions, which is beneficial in food and pharmaceutical applications.

Pharmacodynamics

Xanthan's action is primarily physical rather than pharmacological. It does not exert a direct therapeutic effect but influences the delivery and stability of active ingredients in formulations. The gel formation and viscosity changes help ensure the uniform distribution of substances in liquid formulations, which can improve the effectiveness of the drug delivery.

Pharmacokinetics

As xanthan is a polysaccharide, it is not absorbed in the gastrointestinal tract when ingested. It passes through the digestive system largely unchanged. In terms of metabolism, xanthan is broken down by colonic bacteria, resulting in short-chain fatty acids. Its pharmacokinetic profile indicates that it has a low bioavailability due to its large molecular size and structure.

Pregnancy

There is insufficient data on the use of xanthan during pregnancy. Consult a healthcare professional before use.

Breast-feeding

There is insufficient data on the excretion of xanthan in human milk. Consult a healthcare professional before use.

Storage

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

Formulations

• Xanthan gum powder

Pregnancy

No specific data available, consult a healthcare professional.

Breast-feeding

No specific data available, consult a healthcare professional.

Storage

Store in a cool, dry place away from light.

Mechanism of action

Esomeprazole exerts its stomach acid-suppressing effects by preventing the final step in gastric acid production by covalently binding to sulfhydryl groups of cysteines found on the (H+, K+)-ATPase enzyme at the secretory surface of gastric parietal cells. This effect leads to inhibition of both basal and stimulated gastric acid secretion, irrespective of the stimulus. As the binding of esomeprazole to the (H+, K+)-ATPase enzyme is irreversible and new enzyme needs to be expressed in order to resume acid secretion, esomeprazole's duration of antisecretory effect that persists longer than 24 hours. Esomeprazole is a proton pump inhibitor that suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. The S- and R-isomers of omeprazole are protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphenamide. By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity. This effect is dose-related up to a daily dose of 20 to 40 mg and leads to inhibition of gastric acid secretion.

Pharmacodynamics

Esomeprazole is a compound that inhibits gastric acid secretion and is indicated in the treatment of gastroesophageal reflux disease (GERD), the healing of erosive esophagitis, and <i>H. pylori</i> eradication to reduce the risk of duodenal ulcer recurrence. Esomeprazole belongs to a new class of antisecretory compounds, the substituted benzimidazoles, that do not exhibit anticholinergic or H2 histamine antagonistic properties, but that suppress gastric acid secretion by specific inhibition of the H⁺/K⁺ ATPase at the secretory surface of the gastric parietal cell. By doing so, it inhibits acid secretion into the gsatric lumen. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus. Esomeprazole is the s-isomer of [DB00338], which is a racemate of the S- and R-enantiomer. Esomeprazole has been shown to inhibit acid secretion to a similar extent as [DB00338], without any significant differences between the two compounds _in vitro_. PPIs such as esomeprazole have also been shown to inhibit the activity of dimethylarginine dimethylaminohydrolase (DDAH), an enzyme necessary for cardiovascular health. DDAH inhibition causes a consequent accumulation of the nitric oxide synthase inhibitor asymmetric dimethylarginie (ADMA), which is thought to cause the association of PPIs with increased risk of cardiovascular events in patients with unstable coronary syndromes. Due to their good safety profile and as several PPIs are available over the counter without a prescription, their current use in North America is widespread. Long term use of PPIs such as esomeprazole has been associated with possible adverse effects, however, including increased susceptibility to bacterial infections (including gastrointestinal _C. difficile_), reduced absorption of micronutrients including iron and B12, and an increased risk of developing hypomagnesemia and hypocalcemia which may contribute to osteoporosis and bone fractures later in life.

Mechanism of action

Glucose supplies most of the energy to all tissues by generating energy molecules ATP and NADH during a series of metabolism reactions called glycolysis. Glycolysis can be divided into two main phases where the preparatory phase is initiated by the phosphorylation of glucose by hexokinase to form glucose 6-phosphate. The addition of the high-energy phosphate group activates glucose for the subsequent breakdown in later steps of glycolysis and is the rate-limiting step. Products end up as substrates for following reactions, to ultimately convert C6 glucose molecule into two C3 sugar molecules. These products enter the energy-releasing phase where the total of 4ATP and 2NADH molecules are generated per one glucose molecule. The total aerobic metabolism of glucose can produce up to 36 ATP molecules. These energy-producing reactions of glucose are limited to D-glucose as L-glucose cannot be phosphorylated by hexokinase. Glucose can act as precursors to generate other biomolecules such as vitamin C. It plays a role as a signaling molecule to control glucose and energy homeostasis. Glucose can regulate gene transcription, enzyme activity, hormone secretion, and the activity of glucoregulatory neurons. The types, number, and kinetics of glucose transporters expressed depends on the tissues and fine-tunes glucose uptake, metabolism, and signal generation to preserve cellular and whole body metabolic integrity. Vascular calcification is a hallmark of type 2 diabetes. Glucose stimulates calcification in culture of vascular smooth muscle cells (VSMCs) but the underlying mechanisms remain obscure. We observed that high glucose levels stimulated mouse and human VSMC trans-differentiation into chondrocytes, with increased levels of Sox9, type II collagen, glycosaminoglycan and Runx2 expression, and increased alkaline phosphatase activity and mineralization. These effects were associated with increased expression of IL-1beta, which stimulated alkaline phosphatase and calcification, suggesting that glucose induces chondrocyte differentiation of VSMCs, possibly through IL-1beta activation.

Pharmacodynamics

Blood glucose is an obligatory energy source for humans involved in various cellular activities, and it also acts as a signaling molecule for diverse glucose-sensing molecules and proteins. Glucose undergoes oxidation into carbon dioxide, water, and yields energy molecules in the process of glycolysis and subsequent citric cycle and oxidative phosphorylation. Glucose is readily converted into fat in the body which can be used as a source of energy as required. Under a similar conversion into storage of energy, glucose is stored in the liver and muscles as glycogen. Glucose stores are mobilized in a regulated manner, depending on the tissues' metabolic demands. Oral glucose tablets or injections serve to increase the supply of glucose and oral glucose administration is more effective in stimulating insulin secretion because it stimulates the incretin hormones from the gut, which promotes insulin secretion.

Mechanism of action

It has very good absorptive properties.