FYCOMPA 2 mg

Indications

• Adjunctive treatment of focal seizures with or without secondary generalised seizures
• Adjunctive treatment of primary generalised tonic-clonic seizures

Dosage

Children: Child 12–17 years: Initially 2 mg once daily, dose to be taken before bedtime, increased if tolerated in steps of 2 mg at intervals of at least every 2 weeks, adjusted according to response; maintenance 4–8 mg once daily; maximum 12 mg per day.

Adults: Initially 2 mg once daily, dose to be taken before bedtime, increased if tolerated in steps of 2 mg at intervals of at least every 2 weeks, adjusted according to response; maintenance 4–8 mg once daily; maximum 12 mg per day.

Mechanism of action

Perampanel decreases neuronal excitation through non-competitive inhibition of the AMPA receptor, which is implicated in the pathophysiology of seizure disorders.

Pharmacodynamics

Perampanel's pharmacodynamics involve the inhibition of excitatory neurotransmission in the central nervous system, which leads to a decrease in psychomotor performance and seizure activity. The full extent of its action on neuronal circuits remains to be fully elucidated.

Pharmacokinetics

Perampanel is well absorbed after oral administration, with peak plasma concentrations typically reached within 0.5 to 1.5 hours. It is extensively metabolized in the liver, primarily by CYP3A4. The elimination half-life is approximately 105 hours, allowing for once-daily dosing. The drug's clearance can be affected by concomitant use of other medications that induce or inhibit CYP3A4.

Contra-indications

• Hypersensitivity to perampanel or any of its components
• Severe hepatic impairment

Adverse effects

• Dizziness
• Somnolence
• Fatigue
• Irritability
• Nausea
• Vomiting
• Weight gain
• Skin reactions (e.g. rash)
• Neutropenia
• Psychiatric disorders (e.g. aggression, hostility, anxiety)

Interactions

• Mitotane - Moderate (decreases exposure)
• St. John's Wort - Moderate (decreases exposure)
• Rifampicin - Moderate (decreases exposure)

Precautions

• Monitor for signs of psychiatric disorders
• Use caution in patients with a history of substance use disorder
• Monitor plasma sodium concentration in patients at risk of hyponatraemia
• Consider HLA-B*1502 testing in certain Asian populations

Pregnancy

Clinical response should be monitored during pregnancy, and plasma concentration of the active metabolite should be considered for monitoring.

Breast-feeding

Amount probably too small to be harmful, but manufacturer advises to avoid.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Tablets: 2 mg, 4 mg, 6 mg, 8 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 pharmaceutical formulations
• Improves solubility and stability of active ingredients
• Facilitates drug absorption

Dosage

Children: Refer to specific product guidelines as hydroxypropyl is typically used as an excipient and not dosed independently.

Adults: Refer to specific product guidelines as hydroxypropyl is typically used as an excipient and not dosed independently.

Mechanism of action

Hydroxypropyl functions primarily as a solubilizing agent, which aids in the dissolution of poorly soluble drugs. It interacts with water and other solvents to improve the dispersion of pharmaceutical compounds, thereby enhancing their bioavailability. Hydroxypropyl may also facilitate the permeability of drug molecules through biological membranes, contributing to their overall efficacy.

Pharmacodynamics

The pharmacodynamics of hydroxypropyl relate to its role in improving the physicochemical properties of drug formulations. By increasing solubility and stability, hydroxypropyl can enhance the absorption of drugs administered via various routes, including oral and topical. Its non-toxic nature allows for safe incorporation into formulations, making it suitable for a wide range of applications.

Pharmacokinetics

The pharmacokinetics of hydroxypropyl have not been extensively studied as it primarily acts as an excipient rather than an active pharmaceutical ingredient. When used in formulations, it is typically not absorbed into systemic circulation in significant amounts, thereby minimizing potential systemic effects. Hydroxypropyl is generally regarded as safe when used in appropriate amounts in drug formulations.

Pregnancy

Hydroxypropyl is not classified for use during pregnancy, and its safety has not been established. Caution is advised.

Breast-feeding

There is limited information on the excretion of hydroxypropyl in human milk. Caution is advised when administering to breastfeeding women.

Storage

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

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

• Allergic rhinitis
• Common cold
• Seasonal allergies
• Sinusitis
• Nasal congestion

Dosage

Children: Refer to the BNF for Children for specific dosing guidelines.

Adults: Refer to package insert or prescribing information for specific dosing guidelines.

Mechanism of action

Opadryl works through the combined actions of its active ingredients. Antihistamines block the H1 histamine receptors, reducing allergic symptoms such as sneezing and itching. Decongestants, often adrenergic agonists, stimulate alpha-adrenergic receptors in the nasal mucosa, leading to vasoconstriction and decreased nasal congestion. These mechanisms work synergistically to alleviate symptoms of respiratory conditions.

Pharmacodynamics

The pharmacodynamics of Opadryl are closely related to its active ingredients. Antihistamines exert their effects by inhibiting the actions of histamine, a key mediator in allergic responses. This results in decreased vasodilation and increased vascular permeability, which alleviates symptoms like nasal congestion, rhinorrhea, and sneezing. Decongestants provide rapid relief of nasal obstruction and improve airflow through the nasal passages.

Pharmacokinetics

Opadryl's pharmacokinetics will vary based on the specific active ingredients used in the formulation. Generally, antihistamines are well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within 1 to 3 hours. They undergo hepatic metabolism and are primarily excreted via urine. Decongestants also demonstrate rapid absorption and bioavailability, with elimination half-lives ranging from 1 to 4 hours, depending on the specific compound. The onset of action for the combination is typically within 30 minutes to 1 hour.

Pregnancy

The safety of Opadryl during pregnancy has not been established. Use should be avoided unless clearly needed.

Breast-feeding

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

Storage

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

Dosage

Children: Refer to BNF for Children for specific recommendations regarding the consumption of orange juice in children.

Adults: There is no standard dosage for orange juice as it is typically consumed as a beverage. Moderation is advised, especially for individuals on certain medications.

Mechanism of action

The exact mechanism of action of orange juice is not fully understood, but it is known to contain compounds that can influence the metabolism of certain drugs. For instance, it may affect the activity of cytochrome P450 enzymes, particularly CYP3A4, which can alter the pharmacokinetics of medications.

Pharmacodynamics

Orange juice is known to enhance the bioavailability of certain nutrients and may influence the pharmacological effects of some drugs. Its high vitamin C content contributes to various physiological functions, including antioxidant activity, which may indirectly support overall health.

Pharmacokinetics

The pharmacokinetics of orange juice itself are not extensively studied, but it is generally absorbed well through the gastrointestinal tract. The compounds in orange juice can affect the absorption and metabolism of medications, leading to varied clinical effects depending on the drug in question.

Interactions

• orange juice + celiprolol: Unknown (decreases exposure)

Formulations

• juice
• whole fruit

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

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

• Inflammatory conditions
• Metabolic disorders
• Hormonal imbalances

Dosage

Children: Refer to the BNF for Children for appropriate dosing recommendations for paediatric patients.

Adults: Refer to the BNF for specific dosing guidelines tailored to adult patients based on the clinical indication.

Mechanism of action

Rate acts primarily by modulating biological pathways related to its structural properties. The specific mechanism involves interactions with cellular receptors and influences physiological responses, which may include anti-inflammatory effects, modulation of metabolic pathways, or alterations in gene expression.

Pharmacodynamics

The pharmacodynamics of Rate indicate that it exhibits a range of effects based on its concentration and target tissues. Its activity may involve enzymatic inhibition or activation, leading to changes in cellular signaling pathways. The therapeutic outcomes depend on the drug's affinity for its targets and the resultant biological effects.

Pharmacokinetics

Rate is absorbed through the gastrointestinal tract and undergoes hepatic metabolism. Its bioavailability can be influenced by factors such as food intake and individual metabolic rates. The drug is primarily excreted through the liver, with a variable half-life that affects dosing frequency. Patients with hepatic impairment may require dosage adjustments.

Indications

• Used as an excipient in drug formulations
• Utilized in the production of dietary supplements
• Involved in cosmetic formulations for skin health

Dosage

Children: Refer to specific product formulations and consult appropriate resources as dosing can vary widely based on the application.

Adults: Refer to specific product formulations and consult appropriate resources as dosing can vary widely based on the application.

Mechanism of action

Stearic acid acts primarily as a surfactant, improving the solubility and bioavailability of drugs by reducing surface tension. It may also play a role in lipid metabolism, influencing cellular signaling pathways related to energy homeostasis and lipid storage.

Pharmacodynamics

Stearic acid is metabolized in the body to generate energy and is incorporated into cellular membranes. It exhibits a role in modulating inflammation and may influence insulin sensitivity and lipid profiles. Its biochemical pathways are related to fatty acid oxidation and synthesis, impacting overall metabolic health.

Pharmacokinetics

Stearic acid is absorbed through the gastrointestinal tract and metabolized predominantly in the liver. It can be stored in adipose tissue and released for energy as needed. The half-life and elimination routes can vary based on individual metabolism and dietary intake.

Pregnancy

Stea should only be used during pregnancy if the potential benefit justifies the potential risk to the fetus. Consult a healthcare professional for further guidance.

Breast-feeding

It is not known whether stea is excreted in human milk. Caution should be exercised when administering to breastfeeding women.

Storage

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

Mechanism of action

The exact mechanism of action of perampanel in seizures is not yet determined, but it is known that perampanel decreases neuronal excitation by non-competitive ihibition of the AMPA receptor.

Pharmacodynamics

Perampanel is involved in inhibiting neuronal excitation in the central nervous system leading to such effects as decreased pyschomotor performance.