IVIDIN 5

Indications

• Stable angina
• Patients inadequately controlled or intolerant of first-line antianginal therapies

Dosage

Children: null

Adults: Initially 375 mg twice daily for 2–4 weeks, then increased to 500 mg twice daily if necessary. For patients aged 18–74 years, initial dosage can be 2.5–5 mg twice daily, increased to 7.5 mg twice daily based on response. For those aged 75 years and over, start at 2.5 mg twice daily, increasing as necessary up to 7.5 mg twice daily.

Mechanism of action

Ivabradine lowers heart rate by selectively inhibiting If channels (funny channels) in a concentration-dependent manner. It binds to a site on the channel pore from the intracellular side, disrupting If ion current flow, which prolongs diastolic depolarization and lowers the pacemaker firing rate in the sinoatrial node, leading to decreased heart rate and reduced myocardial oxygen demand.

Pharmacodynamics

Ivabradine's activity is dependent on heart rate, exhibiting use-dependence. It is more pharmacologically active at higher heart rates, showing a linear dose-dependent bradycardic effect until a maximum dose of 30-40 mg, where the effect plateaus. Its metabolite also contributes to heart rate lowering, enhancing its overall efficacy.

Pharmacokinetics

Ivabradine is absorbed after oral administration and undergoes extensive first-pass metabolism. It has a half-life of approximately 2 hours, but due to its active metabolite, the overall effect on heart rate may last longer. The drug is primarily eliminated via hepatic metabolism and renal excretion of metabolites.

Contra-indications

• Severe hepatic impairment
• Acute myocardial infarction
• Cardiogenic shock
• Severe hypotension
• Sick sinus syndrome
• Pacemaker dependence
• Hypersensitivity to ivabradine or any excipient

Adverse effects

• Bradycardia
• Visual disturbances (luminous phenomena)
• Headache
• Dizziness
• Fatigue
• Nausea
• Diarrhea
• Abdominal pain

Interactions

• Grapefruit juice: increases exposure to ivabradine
• St. John's wort: decreases exposure to ivabradine
• Clarithromycin: increases exposure to ivabradine
• Erythromycin: increases exposure to ivabradine
• Mitotane: decreases exposure to ivabradine
• Rifampicin: decreases exposure to ivabradine
• Dronedarone: increases exposure to ivabradine (unknown mechanism)
• Azole antifungals: increases exposure to ivabradine (unknown mechanism)
• Cobicistat: increases exposure to ivabradine (unknown mechanism)
• Crizotinib: increases exposure to ivabradine (unknown mechanism)

Precautions

• Monitor heart rate; should not fall below 50 beats per minute
• Caution in patients with body weight less than 60 kg
• Caution in the elderly
• Caution in patients with moderate to severe congestive heart failure
• QT interval prolongation requires monitoring

Pregnancy

Manufacturer advises avoiding use unless essential; no information available.

Breast-feeding

Manufacturer advises avoiding use; no information available.

Storage

Store in a cool, dry place below 25°C. Protect from light.

Formulations

• Ivabradine 2.5 mg modified-release tablet
• Ivabradine 5 mg modified-release tablet
• Ivabradine 7.5 mg modified-release tablet

Indications

• Wound healing
• Skin protection
• Drug delivery systems
• Anti-inflammatory treatments

Dosage

Children: Refer to specific product guidelines for paediatric dosage information, as it can vary based on the formulation and intended use.

Adults: Refer to specific product guidelines for dosage information, as it can vary based on the formulation and intended use.

Mechanism of action

Colloidal systems work by providing a surface for drug absorption and enhancing the bioavailability of the therapeutic agent. The small particle size of colloids allows for increased surface area, which can facilitate interactions with biological membranes and improve penetration. The stability of colloids also allows for a controlled release of the active components, prolonging their therapeutic effects.

Pharmacodynamics

The pharmacodynamic properties of colloidal formulations depend on the specific active ingredients and their interactions with biological systems. Generally, colloids can enhance the solubility and absorption of poorly water-soluble drugs. They may also provide a protective effect on tissues, reduce inflammation, and promote healing processes in the body. The efficacy of colloidal systems is influenced by factors such as particle size, concentration, and the nature of the dispersing medium.

Pharmacokinetics

The pharmacokinetics of colloidal systems can vary widely based on the formulation and the active ingredient used. Typically, colloids exhibit prolonged circulation times due to their size, and they may be taken up by cells through endocytosis. The release of the active ingredient is dependent on the stability of the colloidal system and environmental conditions such as pH and temperature. Elimination pathways can include renal excretion or degradation by phagocytic cells.

Pregnancy

There is limited data on the safety of colloidal solutions during pregnancy. They should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution is advised when using colloidal solutions during breastfeeding. It is recommended to consult a healthcare professional before use.

Storage

Store in a cool, dry place away from direct sunlight. Ensure that the container is tightly closed to prevent contamination.

Indications

• Monitoring respiratory function
• Assessment of metabolic status
• Management of respiratory acidosis
• Management of respiratory alkalosis

Dosage

Children: Dosing for interventions related to carbon dioxide levels in pediatric patients should be guided by clinical protocols and the BNF for Children.

Adults: Dosing for interventions related to carbon dioxide levels is typically based on clinical assessment and individual patient needs. Refer to clinical guidelines for specific scenarios.

Mechanism of action

Carbon dioxide acts primarily as a signaling molecule in the body, influencing respiratory drive and blood pH. It is produced during cellular respiration and is a critical component of the bicarbonate buffering system, which helps maintain acid-base homeostasis. Elevated levels of CO2 in the blood stimulate ventilation in the lungs, increasing the rate of gas exchange and facilitating the removal of excess CO2.

Pharmacodynamics

The pharmacodynamic effects of dioxides, particularly carbon dioxide, are closely related to its concentration in the blood. As CO2 levels increase, it leads to respiratory acidosis, which can stimulate the respiratory centers in the brain to increase ventilation. Conversely, low levels of CO2 can cause respiratory alkalosis, potentially leading to decreased respiratory drive. CO2 also plays a role in vasodilation and can affect blood flow and pressure through its influence on smooth muscle tone.

Pharmacokinetics

Carbon dioxide is produced endogenously during metabolic processes and is transported in the bloodstream primarily in three forms: dissolved in plasma, as bicarbonate ions (HCO3-), and bound to hemoglobin. The half-life of CO2 in the bloodstream is very short due to its rapid exchange with alveolar gas in the lungs. The elimination of CO2 occurs through exhalation, making it a dynamic component of respiratory physiology.

Pregnancy

Data on the effects of dioxide during pregnancy are limited. Caution is advised due to potential risks associated with exposure.

Breast-feeding

Limited data are available regarding the excretion of dioxide in human milk. Caution is recommended.

Storage

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

Indications

• Lactose intolerance
• As a filler or excipient in pharmaceutical formulations

Dosage

Children: Refer to the BNF for Children for specific dosing information based on age and clinical context.

Adults: Refer to the BNF for specific dosing information based on clinical context.

Mechanism of action

Lactose is metabolized in the intestine by the enzyme lactase into its constituent monosaccharides, glucose and galactose. In individuals with lactase deficiency, unabsorbed lactose passes into the colon, where it is fermented by bacteria, leading to gas production and osmotic effects that contribute to diarrhea.

Pharmacodynamics

The pharmacodynamics of lactose are primarily related to its effects on gastrointestinal function. In healthy individuals, lactose is effectively broken down into glucose and galactose, which are absorbed and utilized for energy. In individuals with lactose intolerance, the unabsorbed lactose can cause osmotic diarrhea and colonic fermentation, leading to discomfort and symptoms associated with lactose intolerance.

Pharmacokinetics

Lactose is not absorbed in the gastrointestinal tract until it is hydrolyzed into glucose and galactose by lactase. The absorption of glucose and galactose occurs in the small intestine. The half-life is not applicable as lactose is not typically administered as a medication but is rather ingested as a natural component of food. Its metabolism primarily occurs in the intestine.

Adverse effects

• Bloating
• Diarrhea
• Abdominal pain
• Flatulence

Precautions

• Use with caution in patients with lactose intolerance.
• Consider potential for gastrointestinal upset in sensitive individuals.

Pregnancy

Lactose is generally considered safe for use during pregnancy. However, consult a healthcare professional for individual advice.

Breast-feeding

Lactose is safe to use while breastfeeding, as it is a natural sugar present in breast milk.

Storage

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

Formulations

• Powder
• Granules
• Tablets
• Syrup

Indications

• Nutritional support
• Source of carbohydrates
• Dietary fiber source
• Animal feed

Dosage

Children: As with adults, there are no specific dosing recommendations for maize for children. It can be introduced into the diet in age-appropriate forms and quantities, keeping in mind the overall dietary balance.

Adults: There are no specific dosing recommendations for maize as it is typically consumed as part of a balanced diet. It can be included in daily meals in various forms such as whole kernels, flour, or as part of dishes.

Mechanism of action

Maize primarily acts as a source of energy due to its high carbohydrate content. The complex carbohydrates in maize are broken down into glucose, which is then utilized by the body for energy production. It also contributes to dietary fiber intake, which can aid in digestive health and regulation of blood sugar levels.

Pharmacodynamics

The consumption of maize influences blood glucose and insulin levels due to its carbohydrate content. It has a relatively low glycemic index when consumed in whole form, which can help in managing blood sugar levels. The dietary fiber present in maize can also promote satiety and aid in weight management.

Pharmacokinetics

The digestion of maize begins in the mouth with salivary amylase breaking down starches into simpler sugars. In the stomach and small intestine, enzymes further break down these carbohydrates. The resultant glucose is absorbed into the bloodstream, where it is transported to cells for energy production. The absorption rate can vary based on the form of maize consumed (e.g., whole kernels versus processed forms).

Pregnancy

Maize is generally considered safe for consumption during pregnancy as it is a staple food and provides essential nutrients.

Breast-feeding

Maize is safe to consume while breastfeeding and can provide important nutrients to both the mother and the infant.

Storage

Store in a cool, dry place, away from moisture and pests. Properly sealed containers can help prolong shelf life.

Formulations

• Whole maize grains
• Maize flour (cornmeal)
• Maize starch
• Maize oil

Indications

• Energy supplementation for athletes
• Rapid glucose replenishment
• Rehydration solutions
• Food additive for thickening and stabilizing

Dosage

Children: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing.

Adults: Refer to specific product guidelines or consult a healthcare professional for appropriate dosing.

Mechanism of action

Maltodextrin is readily metabolized by the body to glucose. Upon ingestion, it is broken down by enzymes in the digestive tract into simpler sugars, which are then absorbed into the bloodstream. This rapid conversion supports immediate energy needs, particularly during physical activity.

Pharmacodynamics

Maltodextrin primarily serves as a source of energy, particularly for athletes and individuals requiring rapid glucose replenishment. Its high glycemic index means it can quickly raise blood sugar levels, providing immediate energy. Additionally, maltodextrin can help improve hydration status and nutrient absorption when included in rehydration solutions.

Pharmacokinetics

Maltodextrin is absorbed quickly in the gastrointestinal tract, leading to a rapid increase in plasma glucose concentrations. The peak plasma glucose levels typically occur within 30 minutes to 1 hour after consumption. The metabolic pathway involves conversion to glucose, which can then be utilized by various tissues for energy or stored as glycogen in the liver and muscles.

Adverse effects

• Gastrointestinal discomfort
• Diarrhea
• Nausea
• Flatulence

Precautions

• Use with caution in individuals with diabetes due to potential impact on blood glucose levels
• Monitor for gastrointestinal symptoms in sensitive individuals

Pregnancy

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

Breast-feeding

Maltodextrin is regarded as safe during breastfeeding, though consultation with a healthcare provider is recommended.

Storage

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

Formulations

• Powder
• Liquid

Indications

• Tablet coating
• Granule coating
• Improvement of drug stability
• Taste masking
• Aesthetic enhancement of pharmaceuticals

Dosage

Children: Dosage will depend on the specific formulation and active ingredients of the medication being coated. Refer to the specific product information for guidance.

Adults: Dosage will depend on the specific formulation and active ingredients of the medication being coated. Refer to the specific product information for guidance.

Mechanism of action

Opadry functions primarily as a coating polymer that adheres to the surface of tablets or granules, creating a protective layer. This layer can control the release of the active ingredient and protect it from environmental factors such as moisture and light. The specific composition of Opadry can vary, but it typically includes film-forming agents, plasticizers, and colorants that work together to achieve the desired coating characteristics.

Pharmacodynamics

The pharmacodynamics of Opadry is largely focused on its physical and chemical properties rather than specific biological interactions. The coating alters the dissolution characteristics of the drug, potentially leading to modified release profiles. This can enhance drug bioavailability or control the release rate of the active ingredient, thereby impacting the therapeutic effect.

Pharmacokinetics

As a coating agent, Opadry itself is not absorbed into the systemic circulation and does not have pharmacokinetic properties related to absorption, distribution, metabolism, or excretion of an active pharmaceutical ingredient. Its impact on pharmacokinetics is indirect, as it affects how the active drug is released and absorbed in the gastrointestinal tract.

Pregnancy

Opadry is a film-coating agent, and specific studies on its effects during pregnancy are not well-documented. Generally, it is advisable to use medications cautiously during pregnancy. Consult a healthcare provider for guidance.

Breast-feeding

Limited data are available regarding the safety of Opadry during breastfeeding. It is recommended to consult a healthcare provider before use.

Storage

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

Formulations

• Opadry OY - a coating system for oral solid dosage forms
• Opadry II - a polymer-based coating system for tablet and capsule applications

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

• Wound management
• Silicone implants
• Dermal fillers
• Medical lubricants
• Scar treatment

Dosage

Children: Refer to specific product guidelines for paediatric dosages, as silicone applications vary widely.

Adults: Refer to specific product guidelines for adult dosages, as silicone applications vary widely.

Mechanism of action

Silicones exhibit their effects primarily through their physical properties rather than a specific biochemical mechanism. They form a protective barrier that is hydrophobic, preventing moisture and microbial penetration, which aids in wound healing and reduces the risk of infection. Their flexibility and inertness also allow them to integrate well with biological tissues.

Pharmacodynamics

Silicones are generally inert and do not interact significantly with biological systems. They provide mechanical support, lubricate surfaces, and facilitate healing without eliciting a strong immune response. Their low toxicity and biocompatibility contribute to their favorable pharmacodynamic profile in medical applications.

Pharmacokinetics

Silicones are not absorbed by the body when used in medical applications. They remain at the site of application and do not undergo significant metabolism. Their elimination is largely through physical means, including degradation over time or removal during surgical procedures. The pharmacokinetic properties can vary depending on the specific silicone formulation and application.

Pregnancy

Silicone is generally considered safe for use during pregnancy as it is inert and non-toxic. However, specific products should be evaluated for safety.

Breast-feeding

Silicone is also considered safe during breastfeeding as it does not transfer into milk; however, care should be taken with specific formulations.

Storage

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

Indications

• Nutritional supplementation
• Energy source in enteral nutrition
• Excipient in pharmaceutical formulations

Dosage

Children: Refer to specific guidelines or product inserts for dosing information, as it can vary based on the context of use.

Adults: Refer to specific guidelines or product inserts for dosing information, as it can vary based on the context of use.

Mechanism of action

Starch is broken down into glucose units by enzymes such as amylase during digestion. The glucose is then absorbed in the intestines and utilized for energy production in the body's cells. This pathway involves hydrolysis of the glycosidic bonds, converting starch into simpler sugars.

Pharmacodynamics

Starch primarily serves as an energy source. Its digestion and absorption lead to an increase in blood glucose levels, which provides energy for metabolic processes. In this context, it plays a crucial role in maintaining energy homeostasis in the body.

Pharmacokinetics

Starch is not absorbed in its polymeric form; it must first be enzymatically hydrolyzed into simpler sugars such as maltose and glucose. The digestion and absorption of starch occur predominantly in the small intestine, with glucose being readily absorbed into the bloodstream. The rate of absorption can vary depending on the type of starch and its physical form.

Adverse effects

• Allergic reactions
• Gastrointestinal discomfort
• Diarrhea
• Constipation

Precautions

• Use with caution in individuals with known allergies to starch or starch derivatives
• Monitor for gastrointestinal symptoms in patients with a history of digestive disorders

Pregnancy

Starch is generally considered safe for use during pregnancy. However, it should be consumed in moderation as part of a balanced diet.

Breast-feeding

Starch is deemed safe for nursing mothers when used in moderation as part of a balanced diet.

Storage

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

Formulations

• Powder
• Granules
• Tablets
• Suspensions

Dosage

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

Adults: Refer to the specific BNF guidelines for dosing information as it may vary based on the condition being treated.

Mechanism of action

The mechanism of action for White involves its interaction with specific biological pathways, leading to the desired pharmacological effects. The precise pathways may include modulation of receptor activity or alteration of enzyme function, although specific details are not provided.

Pharmacodynamics

Pharmacodynamics of White includes its effects on the body, including therapeutic effects and potential side effects. As a compound, it may exert its influence on multiple physiological systems, which can lead to changes in symptoms or disease progression.

Pharmacokinetics

Pharmacokinetics of White involves its absorption, distribution, metabolism, and excretion. Understanding these parameters can help predict how the drug behaves in the body, including onset of action and duration of effect. Detailed pharmacokinetic data is not specified.

Mechanism of action

Ivabradine lowers heart rate by selectively inhibiting If channels ("funny channels") in the heart in a concentration-dependent manner without affecting any other cardiac ionic channels (including calcium or potassium). Ivabradine binds by entering and attaching to a site on the channel pore from the intracellular side and disrupts If ion current flow, which prolongs diastolic depolarization, lowering heart rate. The If currents are located in the sinoatrial node and are the home of all cardiac pacemaker activity. Ivabradine therefore lowers the pacemaker firing rate, consequently lowering heart rate and reducing myocardial oxygen demand. This allows for an improved oxygen supply and therefore mitigation of ischemia, allowing for a higher exercise capacity and reduction in angina episodes.

Pharmacodynamics

The funny channels (If) open during repolarization and close during depolarization, making ivabradine's activity dependent on heart rate or the closing and opening of the channels. Therefore ivabradine exhibits use-dependence and is more pharmacologically active at higher heart rates. Ivabradine exhibits a linear dose-dependent heart-rate lowering activity (bradycardic effect) until a maximum dose of 30-40mg. At higher doses, the concentration of ivabradine tends to plateau, reducing risk of serious sinus bradycardia. It has been shown that the metabolite of ivabradine lowers heart rate as well, contributing to ivabradine's overall effect.