APIBAN 5

Indications

• Prophylaxis of venous thromboembolism following knee replacement surgery
• Prophylaxis of venous thromboembolism following hip replacement surgery
• Treatment of deep vein thrombosis
• Treatment of pulmonary embolism
• Prophylaxis of recurrent deep vein thrombosis
• Prophylaxis of recurrent pulmonary embolism
• Prevention of stroke and systemic embolism in patients with non-valvular atrial fibrillation

Dosage

Adults: Initially 10 mg twice daily for 7 days, then maintenance 5 mg twice daily. For the prophylaxis of venous thromboembolism following hip or knee replacement surgery, the recommended dose is 2.5 mg twice daily, to be started 12-24 hours after surgery.

Mechanism of action

Apixaban selectively inhibits factor Xa in both its free and bound forms, independently of antithrombin III. This inhibition prevents the conversion of prothrombin to thrombin, thereby inhibiting thrombus formation.

Pharmacodynamics

The pharmacodynamic effects of apixaban are characterized by its ability to inhibit factor Xa, which plays a crucial role in the coagulation cascade. This leads to decreased thrombin generation, resulting in reduced clot formation. Its anticoagulant effect can be monitored by measuring anti-factor Xa activity.

Pharmacokinetics

Apixaban is rapidly absorbed after oral administration, with peak plasma concentrations reached within 3 to 4 hours. It has a bioavailability of approximately 50% and is primarily metabolized in the liver via cytochrome P450 enzymes, particularly CYP3A4. The elimination half-life ranges from 8 to 15 hours, and the drug is eliminated through both renal and fecal pathways, with about 25% excreted unchanged in urine.

Contra-indications

• Active bleeding
• Severe uncontrolled hypertension
• History of bleeding diathesis
• Significant risk of major bleeding

Adverse effects

• Bleeding complications
• Nausea
• Headache
• Dizziness
• Diarrhea
• Myalgia
• Skin reactions

Interactions

• St. John's Wort (moderate decrease in exposure)
• Antifungals (azoles - potential increased risk of bleeding)
• Calcium channel blockers (unknown effect on exposure)
• Ciclosporin (unknown effect on exposure)
• HIV protease inhibitors boosted with ritonavir or cobicistat (unknown effect on exposure)
• Idelalisib (unknown effect on exposure)
• Lapatinib (unknown effect on exposure)
• Mitotane (unknown decrease in exposure)
• Neratinib (unknown effect on exposure)

Precautions

• Use with caution in the elderly
• Monitor renal function
• Assess risk factors for bleeding before initiation

Pregnancy

Not known to be harmful, but caution is advised.

Breast-feeding

Use only if essential, as small amounts are present in milk.

Storage

Store in the original container with desiccant, discard any remaining capsules 6 weeks after opening.

Formulations

• Tablets: 2.5 mg, 5 mg, and 10 mg
• Modified-release capsules

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 a disintegrant in tablet formulations
• Improves dissolution of active pharmaceutical ingredients
• Facilitates the breakdown of solid dosage forms

Dosage

Children: Refer to specific product information for dosing guidelines, as croscarmelose is used as an excipient and not dosed independently.

Adults: Refer to specific product information for dosing guidelines, as croscarmelose is used as an excipient and not dosed independently.

Mechanism of action

Croscarmelose functions by rapidly absorbing water and swelling upon hydration. This swelling action creates pressure within the tablet, leading to disintegration into smaller particles. The increased surface area of the drug particles enhances dissolution and absorption in the gastrointestinal tract, ultimately improving the pharmacokinetic profile of the active ingredients.

Pharmacodynamics

As a disintegrant, croscarmelose does not exert a pharmacological effect on its own but plays a critical role in the formulation of oral solid dosage forms. Its pharmacodynamic properties are primarily related to its ability to facilitate the release of active ingredients from their dosage forms, thereby influencing the onset and duration of action of the administered medication.

Pharmacokinetics

Croscarmelose is not absorbed systemically when ingested, as it functions primarily within the gastrointestinal tract. It is excreted unchanged in the feces following its role in aiding the dissolution and disintegration of solid dosage forms. Its safety profile is well-established, and it is considered non-toxic, with minimal adverse effects when used in recommended amounts.

Pregnancy

Croscarmelose is generally considered safe for use during pregnancy as it is an inert substance and does not have systemic effects.

Breast-feeding

Croscarmelose is not absorbed systemically and is considered safe for use during breastfeeding.

Storage

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

Formulations

• Tablet
• Capsule
• Powder

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

• Cleansing agent in topical formulations
• Emulsifying agent in cosmetic products
• Foaming agent in shampoos and body washes

Dosage

Children: Refer to specific product formulations for appropriate concentrations and application methods.

Adults: Refer to specific product formulations for appropriate concentrations and application methods.

Mechanism of action

Lauryl sulfate functions as an anionic surfactant. It reduces the surface tension between different substances, allowing for better spreading and wetting. In the context of cleansing, it facilitates the removal of dirt and oils from the skin and hair by emulsifying these substances, thus making them easier to rinse away with water.

Pharmacodynamics

As a surfactant, lauryl sulfate displays properties that can disrupt cellular membranes and alter permeability. This mechanism is beneficial in enhancing the penetration of other therapeutic agents in topical formulations. However, its irritant potential on skin and mucous membranes should be noted, as it can lead to dryness and irritation with prolonged exposure.

Pharmacokinetics

Lauryl sulfate is primarily applied topically and is not intended for systemic absorption. When used in formulations, it acts locally at the site of application. Its absorption through the skin is minimal, and any systemic exposure is limited. Metabolism and excretion pathways are not well-defined for topical applications, as it is largely washed away after use.

Pregnancy

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

Breast-feeding

Unknown whether lauryl 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.

Dosage

Children: Paediatric fluid requirements should be calculated based on age, weight, and clinical condition. Refer to the guidelines in the BNF for Children for detailed recommendations.

Adults: Dosage in litres may vary depending on clinical circumstances, such as fluid resuscitation needs, maintenance fluid requirements, or medication delivery. Refer to clinical guidelines for specific scenarios.

Mechanism of action

Litres do not have a pharmacological mechanism of action as they are a unit of measurement rather than a drug. However, the administration of fluids measured in litres can influence various physiological processes, including hydration status, electrolyte balance, and overall fluid homeostasis in the body.

Pharmacodynamics

As a measurement unit, litres do not exhibit pharmacodynamics. However, the volume of fluid administered can impact the pharmacodynamics of medications that are diluted or delivered in fluid form, affecting the rate of absorption, distribution, metabolism, and excretion of drugs.

Pharmacokinetics

Litres as a unit of volume do not possess pharmacokinetic properties. The pharmacokinetics of a drug may be influenced by the volume of fluid in which it is administered, as this can affect the concentration of the drug in the bloodstream and its subsequent pharmacological effects.

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.

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

Mechanism of action

The exact mechanism of action for Pink is not detailed in the provided information. However, compounds with similar structures often function as antagonists or inhibitors at certain receptors or enzymes, which modulates physiological processes.

Pharmacodynamics

Pharmacodynamics details for Pink are not specified. Typically, the pharmacodynamics of similar compounds involve interactions with neurotransmitter systems, influencing both central and peripheral nervous system functions. This can lead to varying therapeutic effects depending on the target receptors.

Pharmacokinetics

The pharmacokinetics of Pink, including absorption, distribution, metabolism, and excretion, are not explicitly stated. However, compounds of this nature generally exhibit moderate to high oral bioavailability, with metabolism primarily occurring in the liver, followed by renal excretion of metabolites.

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.

Mechanism of action

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III. Apixaban also inhibits prothrominase. These effects prevent the formation of a thrombus.

Pharmacodynamics

Apixaban selectively inhibits factor Xa in its free and bound forms, independant of antithrombin III. Apixaban also inhibits prothrominase. These effects prevent the formation of a thrombus.