Seltavir 75

Indications

• Prevention of influenza
• Treatment of influenza

Dosage

Children: Child 1–11 months: 3 mg/kg once daily for 10 days for post-exposure prophylaxis; Child 1–12 years (body-weight up to 15 kg): 30 mg once daily for 10 days

Adults: 75 mg once daily for 10 days for post-exposure prophylaxis; for up to 6 weeks (or up to 12 weeks if immunocompromised) during an epidemic.

Mechanism of action

Oseltamivir phosphate is a pro-drug converted to its active form, oseltamivir carboxylate, which selectively inhibits the neuraminidase enzymes of influenza viruses. This inhibition prevents the release of new viral particles from infected cells and reduces viral shedding, thereby decreasing infectivity and limiting the spread of the virus. The drug is effective against both influenza A (including pandemic H1N1) and influenza B.

Pharmacodynamics

Postmarketing reports suggest that oseltamivir may be associated with neuropsychiatric events such as delirium and abnormal behavior, particularly in pediatric patients. These events can lead to self-injury or other serious outcomes. While the exact contribution of oseltamivir to these events is unclear, influenza itself can cause neurologic symptoms, and such incidents have been noted to occur rapidly but resolve quickly.

Pharmacokinetics

Following oral administration, oseltamivir is rapidly absorbed and converted to its active form, oseltamivir carboxylate, primarily in the liver. Peak plasma concentrations of the active metabolite are achieved within 2-3 hours. Oseltamivir has a half-life of approximately 6-10 hours, allowing for once or twice-daily dosing depending on the indication. The drug is eliminated through renal pathways, necessitating dose adjustments in patients with renal impairment.

Adverse effects

• Dizziness
• Gastrointestinal discomfort
• Nausea
• Sleep disorders
• Vertigo
• Vomiting
• Arrhythmia
• Impaired consciousness
• Seizure
• Skin reactions
• Angioedema
• Anxiety
• Abnormal behavior
• Confusion
• Delirium
• Delusions
• Hemorrhage
• Hallucination
• Hepatic disorders
• Self-injurious behavior
• Severe cutaneous adverse reactions (SCARs)
• Thrombocytopenia
• Visual impairment

Interactions

• Leflunomide: Unknown (increases exposure)
• Nitisinone: Unknown (increases exposure)
• Teriflunomide: Unknown (increases exposure)

Precautions

• Monitor for neuropsychiatric events, especially in pediatric patients
• Use with caution in patients with renal impairment
• Evaluate potential risks versus benefits in pregnant or breastfeeding women

Pregnancy

Although safety data are limited, oseltamivir can be used in pregnant women when the potential benefit outweighs the risk, especially during a pandemic.

Breast-feeding

Although safety data are limited, oseltamivir is the preferred drug for breastfeeding women when the potential benefit outweighs the risk, especially during an epidemic.

Storage

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

Formulations

• Tablets
• Capsules
• Oral suspension

Indications

• Hyperphosphatemia
• Chronic kidney disease
• Certain types of poisoning

Dosage

Children: Refer to specific product guidelines for pediatric dosing information, as it may vary based on the condition being treated and the specific binder used.

Adults: Refer to specific product guidelines for dosing information, as it may vary based on the condition being treated and the specific binder used.

Mechanism of action

Binders work by chemically or physically interacting with specific substances in the gastrointestinal tract, preventing their absorption. For example, phosphate binders such as calcium carbonate bind dietary phosphate, forming insoluble complexes that are excreted in the feces. This reduces the levels of phosphate in the bloodstream.

Pharmacodynamics

The pharmacodynamic effects of binders depend on their specific formulation and the substances they are designed to bind. In general, they reduce the absorption of targeted compounds, leading to decreased serum levels of those compounds. This can help to alleviate symptoms associated with their excess, such as bone pain in hyperphosphatemia.

Pharmacokinetics

Binders are not absorbed systemically; instead, they act locally in the gastrointestinal tract. Their onset of action may vary based on the formulation and the specific substance being targeted. The duration of action is typically until the binder is excreted in the feces.

Pregnancy

Safety during pregnancy is not well established. Use only if benefits outweigh risks.

Breast-feeding

Generally considered safe during breastfeeding, but consult a healthcare provider.

Storage

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

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

• Topical antiseptic for skin disinfection
• Surgical scrubs and hand sanitizers
• Wound care management
• Pharmaceutical excipient in solid and liquid formulations

Dosage

Children: Refer to specific product guidelines for pediatric dosing recommendations, as doses can vary based on formulation and intended use.

Adults: Refer to specific product guidelines for dosing recommendations, as doses can vary based on the formulation and intended use.

Mechanism of action

Povidone acts by forming a complex with iodine when used as an antiseptic, which releases iodine slowly to exert its antimicrobial effect. The iodine disrupts microbial cell walls and interferes with protein synthesis, leading to cell death. Additionally, as a polymer, povidone can enhance drug solubility and stability by forming a hydrophilic matrix.

Pharmacodynamics

Povidone has a broad spectrum of antimicrobial activity against bacteria, viruses, and fungi. Its antiseptic properties are primarily due to the release of iodine, which is effective in reducing microbial load and preventing infection. The polymer's ability to bind to various substances allows it to be utilized in formulations that require improved stability and solubility.

Pharmacokinetics

Povidone is not absorbed systemically when applied topically, as it remains localized at the site of application. Its pharmacokinetics are largely dependent on the formulation and route of administration, with the polymer being metabolized by hydrolysis and excreted in urine as low-molecular-weight compounds. The release and activity of iodine are influenced by the concentration of povidone and the presence of organic matter.

Adverse effects

• Local irritation
• Allergic reactions
• Skin rashes
• Hypersensitivity reactions

Precautions

• Use with caution in patients with known allergies to iodine or povidone-iodine
• Avoid use in deep puncture wounds or serious burns

Pregnancy

Povidone is generally considered safe for use during pregnancy, but it is advisable to consult a healthcare professional before use.

Breast-feeding

Povidone is considered safe during breastfeeding, but it is recommended to consult a healthcare professional.

Storage

Store at room temperature, away from moisture and heat. Keep the container tightly closed.

Formulations

• Topical solution
• Ointment
• Surgical scrub
• Gauze impregnated with povidone-iodine

Indications

• Used as a binder in tablet formulations
• Used as a disintegrant in capsules and tablets
• Used as a thickening agent in liquid formulations

Dosage

Children: Refer to specific formulation guidelines, as doses will vary based on the formulation and the active ingredients involved.

Adults: Refer to specific formulation guidelines, as doses will vary based on the formulation and the active ingredients involved.

Mechanism of action

Pregelatinised starch acts as a binder and disintegrant in pharmaceutical formulations. Upon contact with water, it swells and forms a gel-like consistency, facilitating the dissolution of active ingredients and enhancing the release of the drug in the gastrointestinal tract. This mechanism aids in the quick disintegration of tablets and capsules, leading to improved absorption.

Pharmacodynamics

The pharmacodynamics of pregelatinised starch is primarily related to its physical properties rather than any specific pharmacological effects. It enhances the disintegration and solubilization of drug particles, leading to increased bioavailability. Its ability to form a gel-like structure aids in the retention of moisture, which can be beneficial in maintaining the stability of moisture-sensitive compounds.

Pharmacokinetics

Pregelatinised starch is not absorbed in the gastrointestinal tract, as it is a polymer. Instead, it functions as a carrier and excipient, facilitating the delivery of active ingredients. It is metabolized by amylases in the digestive tract into simpler sugars, which are then absorbed. The rate of absorption of the active ingredients is influenced by the presence of pregelatinised starch due to its impact on the disintegration and dissolution processes.

Pregnancy

Pregelatinised starch is generally considered safe for use during pregnancy as it is a food-grade additive, but always consult a healthcare professional.

Breast-feeding

Pregelatinised starch is also considered safe during breastfeeding as it is commonly used in food products, but it is advisable to seek guidance from a healthcare provider.

Storage

Store in a cool, dry place away from direct sunlight. Keep containers tightly closed to prevent moisture absorption.

Formulations

• Pregelatinised starch powder
• Pregelatinised starch granules

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

Indications

• Dry skin conditions
• Cosmetic formulations
• Emollient in topical creams and lotions
• Emulsifying agent in pharmaceutical preparations

Dosage

Children: For pediatric use, refer to specific product formulations and guidelines, as dosing may vary based on the formulation and concentration.

Adults: Stearyl alcohol is used topically in various formulations. Specific dosing is typically determined by the formulation and intended use, refer to product guidelines for detailed instructions.

Mechanism of action

Stearyl alcohol functions primarily as an emollient and emulsifier. It aids in the formation of stable emulsions by reducing the surface tension between oil and water phases, allowing for the creation of creams and lotions. Its hydrophobic tail interacts with lipids, while the hydroxyl group can form hydrogen bonds with water, enhancing moisture retention in the skin.

Pharmacodynamics

Stearyl alcohol acts by providing a protective barrier on the skin, reducing transepidermal water loss and enhancing hydration. Its emollient properties make it effective in softening and smoothing the skin, which can alleviate dryness and improve the overall appearance of the skin. Additionally, it can enhance the delivery of other active ingredients in topical formulations.

Pharmacokinetics

Stearyl alcohol is not significantly absorbed systemically when applied topically. Its primary action is local to the site of application, where it exerts its emollient effects. The compound is metabolized in the body to various fatty acids and alcohols, and it is excreted primarily through the skin and gastrointestinal tract, with minimal systemic exposure.

Pregnancy

Stearyl is generally considered safe for use during pregnancy; however, specific formulations should be evaluated for their ingredients.

Breast-feeding

Stearyl can be used while breastfeeding, but it's recommended to consult a healthcare provider for specific concerns regarding topical applications.

Storage

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

Formulations

• Cream
• Ointment
• Lotion

Indications

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

Dosage

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

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

Mechanism of action

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

Pharmacodynamics

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

Pharmacokinetics

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

Pregnancy

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

Breast-feeding

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

Storage

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

Mechanism of action

Oseltamivir phosphate is a pro-drug of the active metabolite (oseltamivir carboxylate) which is a potent and selective inhibitor of influenza virus neuraminidase enzymes, which are glycoproteins found on the virion surface. Viral neuraminidase enzyme activity is important for viral entry into uninfected cells, for the release of recently formed virus particles from infected cells, and for the further spread of the infectious virus in the body. Oseltamivir activity reduces viral shedding and infectivity. Oseltamivir is effective agaisnt viral neuraminidases of influenza A (including pandemic H1N1) and influenza B. Oseltamivir is an ethyl ester prodrug requiring ester hydrolysis for conversion to the active form, oseltamivir carboxylate. The proposed mechanism of action of oseltamivir is inhibition of influenza virus neuraminidase with the possibility of alteration of virus particle aggregation and release.

Pharmacodynamics

There have been postmarketing reports of delirium and abnormal behavior leading to injury, and in some cases resulting in fatal outcomes, in patients with influenza who were receiving oseltamivir. Because these events were reported voluntarily during clinical practice, estimates of frequency cannot be made but they appear to be uncommon based on oseltamivir. These events were reported primarily among pediatric patients and often had an abrupt onset and rapid resolution. The contribution of oseltamivir to these events has not been established. Influenza can be associated with a variety of neurologic and behavioral symptoms that can include events such as hallucinations, delirium, and abnormal behavior, in some cases resulting in fatal outcomes. These events may occur in the setting of encephalitis or encephalopathy but can occur without obvious severe disease.

Mechanism of action

It has very good absorptive properties.