LORICOR SYRUP

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

• Seasonal allergic rhinitis
• Chronic idiopathic urticaria

Dosage

Children: Child 6–11 years: 30 mg twice daily. Child 12–17 years: 120 mg once daily for seasonal allergic rhinitis or 180 mg once daily for chronic idiopathic urticaria.

Adults: 120 mg once daily for seasonal allergic rhinitis or chronic idiopathic urticaria. Alternatively, 180 mg once daily may be prescribed depending on clinical judgement.

Mechanism of action

Loratadine exerts its effects by binding to H1 histamine receptors, which are found on various cell types, including epithelial, endothelial, and smooth muscle cells. It acts as an 'inverse agonist', stabilizing the inactive form of the H1 receptor and thereby preventing the actions of histamine, which is a key mediator in allergic responses. This mechanism effectively reduces the severity of symptoms associated with allergies.

Pharmacodynamics

Loratadine is selective for peripheral H1 receptors and does not significantly penetrate the central nervous system, resulting in minimal sedation and CNS depression. This pharmacodynamic profile helps to avoid common side effects associated with first-generation antihistamines, such as drowsiness and impaired psychomotor function.

Pharmacokinetics

Loratadine is well-absorbed after oral administration and undergoes extensive hepatic metabolism, primarily via cytochrome P450 enzymes. It has a long half-life, allowing for once-daily dosing. The drug is mainly excreted through urine and bile, with a small percentage eliminated unchanged. Dose adjustments may be necessary in individuals with renal impairment.

Contra-indications

• Acute porphyrias

Adverse effects

• Dizziness
• Drowsiness
• Headache
• Nausea
• Fatigue
• Abdominal pain
• Aggression
• Agitation
• Angioedema
• Appetite increased
• Arthralgia
• Depression
• Dyspnoea
• Hallucination
• Hepatitis
• Myalgia
• Oedema
• Palpitations
• Paraesthesia
• Seizure
• Skin reactions
• Suicidal ideation
• Syncope
• Tachycardia
• Taste altered
• Tremor
• Urinary disorders
• Vertigo
• Vision disorders
• Vomiting
• Weight increased

Interactions

• Other antihistamines

Precautions

• Patients and their carers should be advised that drowsiness can occur and may affect performance of skilled tasks such as cycling or driving.
• Avoid in patients with renal impairment if eGFR is less than 10 mL/minute/1.73 m2.

Pregnancy

Most manufacturers of antihistamines advise avoiding their use during pregnancy; however, there is no evidence of teratogenicity.

Breast-feeding

Most antihistamines are present in breast milk in varying amounts; although not known to be harmful, most manufacturers advise avoiding their use in mothers who are breast-feeding.

Storage

Store at room temperature, away from excessive heat and moisture.

Formulations

• Oral suspension
• Oral solution
• Tablet

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

• Food coloring agent
• Pharmaceutical coloring agent
• Diagnostic agent in certain imaging procedures

Dosage

Children: Refer to specific preparations for paediatric dosing as it may vary widely depending on the formulation and intended use.

Adults: Refer to specific preparations for adult dosing as it may vary widely depending on the formulation and intended use.

Mechanism of action

Erythrosine acts as a fluorescent dye, absorbing light in the visible spectrum and emitting it at a different wavelength. It binds to proteins and nucleic acids, which can affect biological processes such as cell division and apoptosis. Erythrosine's mechanism also involves interaction with cellular membranes, potentially influencing membrane integrity and function.

Pharmacodynamics

Erythrosine exhibits properties as a photosensitizer, with its efficacy increasing under light exposure. It can impact cellular activity by generating reactive oxygen species when activated by light, leading to oxidative stress in cells. This mechanism is utilized in certain therapeutic applications, although it is primarily recognized for its colorant properties.

Pharmacokinetics

Erythrosine is absorbed from the gastrointestinal tract when ingested, with peak plasma concentrations occurring shortly after administration. It is distributed throughout the body and is known to cross biological membranes. The compound is primarily excreted via urine, with some metabolites detected, indicating hepatic metabolism. The elimination half-life of erythrosine is variable and influenced by individual physiology and dosage.

Contra-indications

• Hypersensitivity to erythrosine or any of its components
• Thyroid disorders
• Patients with iodine allergy

Adverse effects

• Hypersensitivity reactions
• Thyroid dysfunction
• Nausea
• Vomiting
• Diarrhea
• Skin rashes

Interactions

• May interact with thyroid function tests, leading to false results
• Potential for interactions with other iodine-containing compounds

Precautions

• Use with caution in patients with a history of thyroid disease
• Monitor thyroid function in patients receiving long-term therapy
• Assess for allergic reactions prior to administration

Pregnancy

Erythrosine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult healthcare professional for advice.

Breast-feeding

It is not known whether erythrosine is excreted in human milk. Use with caution, considering the benefits and risks.

Storage

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

Formulations

• Oral suspension
• Injectable solution

Indications

• Nutritional support
• Prevention of chronic diseases
• Support for digestive health
• Antioxidant support
• Hydration

Dosage

Children: In children, the recommendation for fruit intake varies by age, with guidelines typically suggesting 1 to 2 servings per day, depending on age and dietary requirements.

Adults: Fruits are generally consumed as part of a balanced diet, with recommendations often suggesting 5 portions of fruits and vegetables per day, though specific amounts may vary based on individual dietary needs.

Mechanism of action

Fruits contain various bioactive compounds, including vitamins (such as vitamin C and folate), minerals (like potassium), dietary fiber, and phytochemicals (such as flavonoids and carotenoids). These components contribute to their health benefits through various mechanisms, including antioxidant activity, modulation of inflammation, and enhancement of immune function.

Pharmacodynamics

The pharmacodynamic effects of fruits are largely attributed to their phytochemical content, which can influence metabolic pathways, reduce oxidative stress, and improve cardiovascular health. The fiber content aids in digestion and can contribute to maintaining healthy cholesterol levels. The vitamins and minerals support various physiological functions, including immune response and cellular repair.

Pharmacokinetics

The bioavailability of nutrients from fruits can vary based on the composition of the fruit and the individual's digestive health. Vitamins and antioxidants are typically absorbed in the small intestine, while dietary fiber is fermented in the colon. The metabolism of fruit-derived nutrients occurs through various pathways, with some compounds undergoing conjugation and excretion via the kidneys.

Pregnancy

Fruits are generally safe to consume during pregnancy and provide essential nutrients. However, certain fruits may need to be limited due to sugar content or potential allergies.

Breast-feeding

Fruits are safe to consume while breastfeeding and can contribute to the nutritional needs of both the mother and the infant. Some fruits may help with lactation.

Storage

Fruits should be stored in a cool, dry place, and refrigeration can help prolong freshness. Some fruits may require specific storage conditions to maintain quality.

Formulations

• whole fruit
• dried fruit
• fruit juice
• fruit puree
• fruit smoothie

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

• Adjustment of pH in pharmaceutical formulations
• Facilitation of drug absorption
• Used in sterile preparations

Dosage

Children: Refer to specific product guidelines for dosing information, as hydrochloric acid is typically used in a controlled setting based on formulation requirements.

Adults: Refer to specific product guidelines for dosing information, as hydrochloric acid is typically used in a controlled setting based on formulation requirements.

Mechanism of action

Hydrochloric acid dissociates in aqueous solution to release hydrogen ions (H+), leading to a decrease in pH. This acidic environment promotes the activation of pepsinogen to pepsin, an enzyme essential for protein digestion. Additionally, the acidity aids in the absorption of certain minerals and drugs that require an acidic environment for optimal bioavailability.

Pharmacodynamics

The primary pharmacodynamic action of hydrochloric acid is the maintenance of gastric acidity, which is essential for normal digestive processes. The acidic environment helps in denaturing proteins, activating digestive enzymes, and providing a barrier against pathogenic microorganisms. Its effects can influence the absorption and efficacy of various medications, particularly those that are pH-dependent.

Pharmacokinetics

Hydrochloric acid does not undergo significant systemic absorption when used in its normal contexts, as it acts locally within the gastrointestinal tract. The amount of hydrochloric acid produced by the stomach varies with food intake and physiological needs. It is secreted by parietal cells in the gastric mucosa, and its secretion is regulated by neural, hormonal, and local factors. The half-life of hydrochloric acid is not applicable as it is continuously produced and neutralized within the gastrointestinal tract.

Contra-indications

• Hypersensitivity to hydrochloric acid or any of its components
• Severe renal impairment
• Active gastrointestinal bleeding

Adverse effects

• Abdominal pain
• Diarrhea
• Nausea
• Vomiting
• Esophageal irritation
• Gastric mucosal irritation
• Electrolyte imbalances

Interactions

• May interact with alkaline substances, potentially neutralizing hydrochloric acid
• Caution with antacids as they may affect the efficacy of hydrochloric acid

Precautions

• Use with caution in patients with a history of gastritis or gastric ulcers
• Monitor electrolytes in prolonged use
• Use cautiously in patients with respiratory conditions due to potential aspiration risks

Pregnancy

Hydrochloric acid is classified as a category C drug. Use during pregnancy only if clearly needed and the potential benefits justify the risks to the fetus.

Breast-feeding

There is limited data on the excretion of hydrochloric acid in human milk. Use with caution during breastfeeding.

Storage

Store in a cool, dry place away from direct sunlight and heat. Ensure the container is tightly closed.

Formulations

• Oral solutions
• Injectable forms
• Tablets

Indications

• Use as a preservative in pharmaceutical formulations
• Antimicrobial agent in cosmetic and food products
• Potential use in the management of inflammatory conditions due to salicylate biosynthesis

Dosage

Children: Refer to the BNF for Children for appropriate dosing information.

Adults: Refer to the specific product guidelines and BNF for appropriate dosing information.

Mechanism of action

Hydroxybenzoate functions primarily as a preservative by inhibiting the growth of microorganisms. It exerts its effects through the disruption of microbial cell metabolism, thereby preventing spoilage and degradation. The compound is involved in various biosynthetic pathways, including the production of salicylates, which possess anti-inflammatory properties.

Pharmacodynamics

Hydroxybenzoate displays antimicrobial activity against a range of bacteria and fungi. Its efficacy is influenced by factors such as pH and concentration, with higher concentrations generally leading to greater antimicrobial effects. The compound may also exhibit antioxidant properties, contributing to its protective effects in various formulations.

Pharmacokinetics

The pharmacokinetics of hydroxybenzoate involves its absorption, distribution, metabolism, and excretion. It is readily absorbed when applied topically or ingested. Once in the system, it is metabolized primarily in the liver, with metabolites excreted through the urine. The elimination half-life may vary based on the formulation and route of administration.

Pregnancy

There is limited information available regarding the safety of hydroxybenzoate during pregnancy. Consult a healthcare provider for advice.

Breast-feeding

It is unclear if hydroxybenzoate is excreted in human milk. Consult a healthcare provider before use.

Storage

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

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.

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)

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

• Sweetening agent in food and beverages
• Ingredient in pharmaceutical formulations
• Source of quick energy

Dosage

Children: Refer to specific formulations and clinical guidelines for dosing, as sucrose does not have a standardized dosage. Typically used as needed for sweetening.

Adults: Refer to specific formulations and clinical guidelines for dosing, as sucrose does not have a standardized dosage. Typically used as needed for sweetening.

Mechanism of action

Sucrose is metabolized in the body to glucose and fructose, which are then used as energy sources. It does not have a specific pharmacological mechanism of action but contributes to energy metabolism via the glycolytic and citric acid pathways.

Pharmacodynamics

Upon ingestion, sucrose is hydrolyzed by the enzyme sucrase into its constituent monosaccharides, glucose and fructose. These monosaccharides are absorbed in the small intestine and enter the bloodstream, leading to a rise in blood glucose levels. This process provides a quick source of energy for cellular functions.

Pharmacokinetics

Sucrose is rapidly absorbed in the gastrointestinal tract after hydrolysis. Its absorption depends on the presence of sucrase in the intestine. Once in the bloodstream, glucose can be utilized by cells or stored as glycogen in the liver and muscles. The elimination half-life of sucrose itself is not well-defined as it is quickly broken down and utilized.

Pregnancy

Sucrose is generally regarded as safe during pregnancy when consumed in moderation as part of a balanced diet.

Breast-feeding

Sucrose is considered safe during breastfeeding when consumed in normal dietary amounts.

Storage

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

Formulations

• Oral solution
• Granules
• Tablets

Indications

• Magnetic resonance imaging (MRI) contrast enhancement
• Drug delivery systems
• Potential therapeutic applications in oncology

Dosage

Children: Refer to the BNF for Children for appropriate pediatric dosing information.

Adults: Refer to the specific guidelines for dosage as per BNF and clinical protocols.

Mechanism of action

The principal uptake mechanism for superparamagnetic iron oxide nanoparticles involves clathrin-mediated endocytosis that is dependent on scavenger receptor A. This process allows phagocytic cells, particularly macrophages, to internalize the nanoparticles effectively. The interaction of these nanoparticles with macrophages is critical for their application in imaging and potential therapeutic interventions.

Pharmacodynamics

Superparamagnetic iron oxide nanoparticles exhibit properties that enhance the visibility of tissues during imaging procedures. Their magnetic properties allow for a significant increase in contrast during MRI scans. Additionally, they may have implications in therapeutic contexts, such as in the targeting of cancer cells, where their uptake by macrophages could facilitate localized drug delivery.

Pharmacokinetics

The pharmacokinetics of superparamagnetic iron oxide nanoparticles are characterized by rapid uptake by phagocytic cells, particularly in the liver and spleen. Following systemic administration, these nanoparticles are primarily cleared by macrophages through endocytosis. The particles tend to accumulate in the reticuloendothelial system, which can influence their distribution and elimination from the body.

Pregnancy

There is limited data on the safety of iron oxide nanoparticles during pregnancy. Caution is advised.

Breast-feeding

Limited data is available regarding the excretion of iron oxide nanoparticles in breast milk. Caution is advised.

Storage

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

Formulations

• Carboxydextran-coated superparamagnetic iron oxide nanoparticles

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

Histamine release is a key mediator in allergic rhinitis and urticaria. As a result, loratadine exerts it's effect by targeting H1 histamine receptors. Loratadine binds to H1 histamine receptors found on the surface of epithelial cells, endothelial cells, eosinophils, neutrophils, airway cells, and vascular smooth muscle cells among others. H1 histamine receptors fall under the wider umbrella of G-protein coupled receptors, and exist in a state of equilibrium between the active and inactive forms. Histamine binding to the H1-receptor facilitates cross linking between transmembrane domains III and V, stabilizing the active form of the receptor. On the other hand, antihistamines bind to a different site on the H1 receptor favouring the inactive form. Hence, loratadine can more accurately be classified as an "inverse agonist" as opposed to a "histamine antagonist", and can prevent or reduce the severity of histamine mediated symptoms. All of the available H1 receptor antagonists are reversible, competitive inhibitors of the interaction of histamine with H1 receptors. /H1 Receptor Antagonists/ H1 antagonists inhibit most responses of smooth muscle to histamine. /H1 Antagonists Receptors/ Within the vascular tree, the H1 antagonists inhibit both the vasoconstrictor effects of histamine and, to a degree, the more rapid vasodilator effects that are mediated by H1 receptors on endothelial cells. /H1 Receptor Antagonists/ H1 antagonists strongly block the action of histamine that results in increased capillary permeability and formation of edema and wheal. /H1 Receptor Antagonists/ For more Mechanism of Action (Complete) data for LORATADINE (6 total), please visit the HSDB record page.

Pharmacodynamics

Like other 2nd generation antihistamines, loratadine is selective for peripheral H1 receptors. Loratadine does not penetrate effectively into the central nervous system and has poor affinity for CNS H1-receptors. These qualities result in a lack of CNS depressant effects such as drowsiness, sedation, and impaired psychomotor function.

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

Although systemically applied nanoparticles are quickly taken up by phagocytic cells, mainly macrophages, the interactions between engineered nanoparticles and macrophages are still not well defined. ...Therefore ... the uptake of diagnostically used carboxydextran-coated superparamagnetic iron oxide nanoparticles of 60 nm (SPIO) and 20 nm (USPIO) by human macrophages /was analyzed/. By pharmacological and in vitro knockdown approaches, the principal uptake mechanism for both particles was identified as clathrin-mediated, scavenger receptor A-dependent endocytosis... /Iron oxide nanoparticles/ ... /It has been/ suggested that ferric oxide serves as a carcinogenic cofactor either by retarding the clearance of inhaled carcinogens or by inducing cytopathological changes which make the cells of the respiratory tract more prone to develop cancer when exposed to carcinogenic substances.