BESICOR 5

Indications

• Hypertension
• Angina pectoris
• Heart failure (adjunctive therapy)

Dosage

Children: Refer to BNF for Children for appropriate dosing information, as specific pediatric doses are not provided.

Adults: Initial dose: 5 mg once daily. Maintenance dose: may be increased to a maximum of 10 mg once daily depending on response and tolerability.

Mechanism of action

Bisoprolol fumarate selectively inhibits beta-1 adrenergic receptors located primarily in the heart. This results in a decrease in heart rate, myocardial contractility, and conduction velocity through the atrioventricular node, leading to reduced cardiac output and lower blood pressure. It does not significantly affect beta-2 adrenergic receptors, which are found in the lungs and vascular smooth muscle, resulting in a lower risk of bronchospasm in susceptible individuals.

Pharmacodynamics

The pharmacological effects of bisoprolol include a reduction in heart rate, myocardial oxygen demand, and blood pressure. The onset of action occurs within 1-2 hours after oral administration, with peak effects observed around 4-6 hours. The antihypertensive effect lasts for 24 hours, allowing for once-daily dosing. Bisoprolol also has a favorable safety profile compared to non-selective beta-blockers, particularly in patients with respiratory conditions.

Pharmacokinetics

Bisoprolol fumarate is well absorbed from the gastrointestinal tract, with a bioavailability of approximately 90%. It is primarily metabolized in the liver via cytochrome P450 enzymes, predominantly CYP2D6, and has a half-life of around 10-12 hours, allowing for once-daily dosing. Excretion occurs mainly through the kidneys, with approximately 50% of the drug eliminated unchanged in urine. Dosage adjustments may be necessary in patients with significant renal impairment.

Contra-indications

• Acute or decompensated heart failure requiring intravenous inotropes
• Sino-atrial block

Adverse effects

• Fatigue
• Dizziness
• Bradycardia
• Hypotension
• Cold extremities
• Depression
• Nausea
• Diarrhea
• Shortness of breath
• Sleep disturbances

Interactions

• Other beta-blockers
• Calcium channel blockers
• Antiarrhythmic agents
• CYP2D6 inhibitors
• Non-steroidal anti-inflammatory drugs (NSAIDs)
• Digoxin
• Insulin or oral antidiabetic agents

Precautions

• Caution in patients with a history of bronchospasm
• Careful monitoring in patients with renal impairment
• Caution in patients with hepatic impairment
• Gradual withdrawal recommended to avoid rebound hypertension
• Assess heart failure status before initiation and during titration

Pregnancy

Bisoprolol fumarate is not recommended during pregnancy unless the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Caution is advised as bisoprolol fumarate is excreted in breast milk; monitor the infant for adverse effects.

Storage

Store below 25 degrees Celsius in a dry place, away from light.

Formulations

• Bisoprolol fumarate 1.25 mg tablets
• Bisoprolol fumarate 2.5 mg tablets
• Bisoprolol fumarate 5 mg tablets
• Bisoprolol fumarate 7.5 mg tablets
• Bisoprolol fumarate solution for injection

Indications

• Hypertension
• Heart failure
• Angina pectoris
• Arrhythmias

Dosage

Children: Refer to BNF for Children for specific pediatric dosing.

Adults: Refer to BNF for specific dosing guidelines.

Mechanism of action

Though the precise mechanism of action of bisoprolol in hypertension is not fully understood, it is believed to primarily exert its therapeutic effects through the antagonism of β-1 adrenoceptors. This leads to a reduction in cardiac output by decreasing heart rate and myocardial contractility. Additionally, bisoprolol may lower renin output from the kidneys and exert some central nervous system effects that contribute to decreased sympathetic nervous system activity, further lowering blood pressure and heart rate.

Pharmacodynamics

Bisoprolol significantly decreases heart rate (chronotropy), reduces myocardial contractility (inotropy), and lowers blood pressure. Clinical studies have shown that bisoprolol can effectively reduce cardiovascular mortality and overall mortality in patients suffering from heart failure with reduced ejection fraction.

Pharmacokinetics

Bisoprolol is well absorbed from the gastrointestinal tract and has a bioavailability of approximately 80%. It is extensively metabolized in the liver, primarily by cytochrome P450 enzymes, and has an elimination half-life of about 10-12 hours, allowing for once-daily dosing. The drug is primarily excreted via the kidneys, with a small portion eliminated unchanged.

Contra-indications

• Severe bradycardia
• Second or third degree AV block
• Cardiogenic shock
• Uncontrolled heart failure
• Hypersensitivity to bisoprolol or any excipients

Adverse effects

• Fatigue
• Dizziness
• Bradycardia
• Hypotension
• Cold extremities
• Gastrointestinal disturbances
• Sleep disturbances
• Depression

Interactions

• Propafenone: Moderate (increases risk of cardiovascular adverse effects)
• Rifampicin: Unknown (decreases exposure)

Precautions

• Caution in patients with asthma or chronic obstructive pulmonary disease (COPD)
• Caution in patients with diabetes mellitus (may mask hypoglycemia)
• Caution in patients with peripheral vascular disease
• Monitor heart rate and blood pressure regularly

Pregnancy

Bisoprolol should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus. It may cause fetal bradycardia, hypotension, and neonatal withdrawal symptoms.

Breast-feeding

Bisoprolol is excreted in breast milk; caution is advised when administering to nursing mothers.

Storage

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

Formulations

• Oral tablets: 1.25 mg, 2.5 mg, 5 mg, 10 mg

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

• 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

• Skin irritation
• Minor cuts
• Abrasions
• Superficial skin lesions

Dosage

Children: Apply a thin layer to the affected area as needed, following the manufacturer's instructions.

Adults: Apply a thin layer to the affected area as needed, following the manufacturer's instructions.

Mechanism of action

The specific mechanism of action of Instacoat can vary depending on its active ingredients. Generally, topical formulations exhibit local effects by forming a protective layer over the skin, which can help in preventing infection and facilitating the natural healing process. Some ingredients may have anti-inflammatory properties that reduce redness and swelling, while others may promote cellular regeneration and wound healing.

Pharmacodynamics

Instacoat acts locally at the site of application, with minimal systemic absorption. The pharmacodynamic effects are mainly related to the ingredients used in the formulation. These effects can include enhancement of skin hydration, reduction of inflammation, and promotion of tissue regeneration. The overall outcome is improved skin integrity and faster healing of affected areas.

Pharmacokinetics

As a topical agent, Instacoat is primarily applied to the skin, resulting in localized effects. The pharmacokinetics would largely depend on the specific formulation and its active components. Typically, topical medications show limited systemic absorption, ensuring that the primary effects are exerted locally. The onset of action may occur within a few hours following application, with the duration of effect varying based on the formulation and skin characteristics.

Pregnancy

Data on the use of Instacoat during pregnancy is limited. Its use should be considered only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

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

Storage

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

Indications

• Used as an excipient in tablet formulations
• Used as a bulking agent in capsule formulations
• Used in food products as a thickener or stabilizer

Dosage

Children: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Adults: Refer to specific product guidelines as dosage will depend on the formulation and the active ingredients.

Mechanism of action

Microcrystalline cellulose acts as a non-digestible filler that enhances the flow properties of powders during the manufacturing of tablets and capsules. It does not have a direct pharmacological action on the body but ensures that the active ingredients are effectively delivered to the patient.

Pharmacodynamics

As a non-active ingredient, microcrystalline cellulose does not exert pharmacodynamic effects typical of active pharmaceutical ingredients. Its primary role is to provide a stable and consistent matrix for the drug, facilitating the release of the active compound once ingested.

Pharmacokinetics

Microcrystalline cellulose is not absorbed in the gastrointestinal tract; it passes through the digestive system largely unchanged. It adds bulk to the stool, which may aid in promoting regular bowel movements. The substance is excreted in feces, where it contributes to dietary fiber intake.

Pregnancy

Data regarding the use of microcrystalline cellulose during pregnancy is limited. It is advisable to consult with healthcare professionals before use.

Breast-feeding

Microcrystalline cellulose is considered safe during breastfeeding, as it is not absorbed systemically.

Storage

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

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

• Improvement of flow properties in powder formulations
• Preventing clumping in solid dosage forms
• Management of gastrointestinal disorders

Dosage

Children: Refer to specific formulation guidelines as silicified silica is typically used as an excipient and does not have a defined dosage.

Adults: Refer to specific formulation guidelines as silicified silica is typically used as an excipient and does not have a defined dosage.

Mechanism of action

Silicified silica acts by adsorbing moisture and preventing the clumping of powders. It also has the ability to absorb excess gastric acid, which can aid in the management of certain gastrointestinal conditions.

Pharmacodynamics

Silicified silica does not exert a direct pharmacological effect on body systems but improves the physical properties of pharmaceutical formulations. By promoting better flow and preventing caking, it enhances the bioavailability of active pharmaceutical ingredients (APIs).

Pharmacokinetics

Silica is not absorbed in the gastrointestinal tract and is excreted unchanged. Its pharmacokinetic profile is characterized by its inert nature and lack of systemic absorption, which allows it to function primarily at the site of administration.

Pregnancy

There is limited data on the use of silicified in pregnancy. Consult a healthcare provider before use.

Breast-feeding

It is unknown whether silicified is excreted in human milk. Caution is advised when administering to breastfeeding mothers.

Storage

Store in a tightly closed container, protected from moisture and light.

Dosage

Children: Refer to specific product formulations for guidelines, as dosing can vary based on the formulation and therapeutic context.

Adults: Refer to specific product formulations for guidelines, as dosing can vary based on the formulation and therapeutic context.

Mechanism of action

Stearates, such as magnesium stearate, function primarily by reducing friction during tablet manufacturing and enhancing the flow properties of powders. They do not exert a therapeutic pharmacological action in the body but facilitate the delivery of other active substances.

Pharmacodynamics

Given that stearates are primarily excipients, they do not exhibit traditional pharmacodynamic properties as active drugs do. Their role is to optimize the formulation of drugs, enhancing physical characteristics such as texture and consistency, which indirectly affect the performance of the active ingredients.

Pharmacokinetics

Stearates are poorly absorbed in the gastrointestinal tract due to their lipid nature. When ingested, they may pass through the digestive system with minimal systemic absorption. Their primary action occurs at the site of formulation, where they assist in the dispersion and release of active ingredients rather than being metabolized or exerting effects in the body.

Pregnancy

The safety of sterate during pregnancy has not been established. It should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

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

Storage

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

Dosage

Children: Refer to specific product information for paediatric dosing, as it will depend on the formulation and indication.

Adults: Refer to specific product information for dosing guidance, as it will vary based on formulation and clinical use.

Mechanism of action

The mechanism of action for a universal drug would depend on its specific formulation and intended targets. Generally, such drugs might act on multiple receptors or pathways, potentially modulating immune responses, inflammatory processes, or neurotransmitter systems. The aim would be to exert a beneficial effect across different physiological systems.

Pharmacodynamics

Pharmacodynamics of a universal drug would involve its effects on the body, including the relationship between drug concentration and therapeutic effect. A universal drug may exhibit dose-dependent responses, with efficacy influenced by receptor affinity, intrinsic activity, and the presence of other competing endogenous substances. Side effects may also vary based on the specific biological pathways affected.

Pharmacokinetics

Pharmacokinetics refers to how a drug is absorbed, distributed, metabolized, and excreted in the body. For a universal drug, this could involve varied absorption rates depending on the route of administration, extensive distribution to various tissues, metabolism by liver enzymes, and renal or biliary excretion. Factors such as age, sex, genetic polymorphisms, and comorbid conditions could influence its pharmacokinetic profile.

Pregnancy

Consult with a healthcare provider to evaluate risks versus benefits.

Breast-feeding

Consult with a healthcare provider to evaluate risks versus benefits.

Storage

Store at room temperature, away from moisture and heat.

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

Though the mechanism of action of bisoprolol has not been fully elucidated in hypertension, it is thought that therapeutic effects are achieved through the antagonism of β-1adrenoceptors to result in lower cardiac output. Bisoprolol is a competitive, cardioselective β1-adrenergic antagonist. When β1-receptors (located mainly in the heart) are activated by adrenergic neurotransmitters such as epinephrine, both the blood pressure and heart rate increase, leading to greater cardiovascular work, increasing the demand for oxygen. Bisoprolol reduces cardiac workload by decreasing contractility and the need for oxygen through competitive inhibition of β1-adrenergic receptors. Bisoprolol is also thought to reduce the output of renin in the kidneys, which normally increases blood pressure. Additionally, some central nervous system effects of bisoprolol may include diminishing sympathetic nervous system output from the brain, decreasing blood pressure and heart rate.

Pharmacodynamics

Bisoprolol decreases heart rate (chronotropy), decreases contractility (inotropy), and reduces blood pressure. The results of various clinical studies indicate that bisoprolol reduces cardiovascular mortality and all-cause mortality in patients with heart failure and decreased cardiac ejection fraction (EF).