Unienzyme cMPS

Indications

• Papulopustular rosacea
• Inflammatory acne vulgaris

Dosage

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

Adults: For papulopustular rosacea, apply daily for up to 4 months. The treatment course may be repeated; discontinue if no improvement is observed after 3 months. For inflammatory acne vulgaris, apply twice daily, reduced to once daily or alternate days if irritation occurs.

Mechanism of action

Nicotinamide exhibits anti-inflammatory effects by inhibiting the release of pro-inflammatory cytokines and enhancing the barrier function of the skin. It is also involved in the NAD salvage pathway, which is essential for maintaining cellular energy levels and promoting cell repair mechanisms. Additionally, nicotinamide contributes to the synthesis of coenzymes involved in metabolic processes, including the conversion of niacin into NAD+.

Pharmacodynamics

Nicotinamide is known for its ability to improve skin hydration and reduce transepidermal water loss. It has been shown to decrease the appearance of acne lesions and rosacea by modulating inflammatory responses and accelerating cell turnover. Its antioxidant properties also help to protect the skin from oxidative stress and UV damage.

Pharmacokinetics

When applied topically, nicotinamide is absorbed through the skin layers, with minimal systemic absorption. Its peak plasma concentrations are generally low, and the drug has a half-life that varies depending on the route of administration. The metabolism of nicotinamide occurs primarily in the liver, where it is converted into its active forms, including NAD+. The elimination route is via the kidneys, with metabolites excreted in urine.

Contra-indications

• Pregnancy
• Severe acne involving large areas
• Severe skin reactions

Adverse effects

• Sunburn
• Skin reactions (common or very common)
• Cheilitis
• Eyelid oedema
• Flushing
• Dry skin
• Eye irritation
• Photosensitivity reactions
• Transient skin pigmentation changes

Interactions

• Clindamycin
• Topical retinoids
• Abrasive cleaners
• Comedogenic cosmetics

Precautions

• Avoid exposure to UV light, including sunlight and sunlamps
• Wash hands immediately after use
• Avoid contact with eyes and mucous membranes
• Use moisturizers to reduce the risk of skin irritation
• Discontinue treatment if severe irritation occurs

Pregnancy

Avoid use during pregnancy due to potential risks, as limited information is available regarding toxicity.

Breast-feeding

Amount of drug in milk after topical application is probably too small to be harmful; ensure infant does not come in contact with treated areas.

Storage

Store at room temperature away from moisture and light.

Formulations

• Cream
• Gel

Indications

• Acute poisoning
• Drug overdose
• Gastrointestinal decontamination

Dosage

Children: Refer to specific pediatric dosing recommendations based on the child's weight and the clinical situation.

Adults: Refer to specific guidelines depending on the type of poisoning and the clinical scenario.

Mechanism of action

Activated charcoal works through a process called adsorption, where toxins and drugs adhere to the surface of the charcoal particles due to electrostatic attractions and Van der Waals forces. This prevents the absorption of these substances in the gastrointestinal tract, allowing them to be excreted from the body.

Pharmacodynamics

The pharmacodynamic effects of activated charcoal are related to its ability to bind a wide range of substances. The efficacy of activated charcoal varies depending on the type and amount of the toxin or drug ingested, as well as the time elapsed since ingestion. Generally, activated charcoal is most effective when administered within one hour of ingestion of a toxic substance.

Pharmacokinetics

Activated charcoal is not absorbed by the gastrointestinal tract; instead, it remains in the gut, where it binds to ingested substances and promotes their elimination via feces. Its effects are dose-dependent, and it is typically administered as a single dose, although multiple doses may be considered in certain cases of severe poisoning.

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Constipation
• Abdominal pain
• Aspiration pneumonia (if inhaled)
• Electrolyte imbalances

Precautions

• Use with caution in patients with gastrointestinal obstruction
• Monitor for potential aspiration in patients with reduced consciousness
• Consider electrolyte levels in patients with significant diarrhea or vomiting

Pregnancy

Activated charcoal is generally considered safe for use in pregnancy, but consult a healthcare professional before use.

Breast-feeding

Activated charcoal is excreted in breast milk, use with caution and consult a healthcare professional.

Storage

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

Formulations

• Activated charcoal powder
• Activated charcoal capsules
• Activated charcoal tablets

Indications

• Acute poisoning
• Drug overdose
• Gastrointestinal decontamination
• Treatment of certain types of toxin ingestion

Dosage

Children: For children over 1 year of age, the recommended dosage of activated charcoal is 1 gram per kilogram of body weight, up to a maximum of 50 grams. For children under 1 year, consult the BNF for Children for specific dosing guidance.

Adults: The usual adult dosage for activated charcoal in the treatment of poisoning is 50 to 100 grams, administered orally or via a nasogastric tube. Repeat doses may be given in certain cases, depending on the toxin involved.

Mechanism of action

Activated charcoal works primarily by adsorbing toxins and drugs in the gastrointestinal tract, reducing their systemic absorption. The extensive surface area and porous structure of activated charcoal allow it to bind various substances through van der Waals forces and hydrogen bonding. This binding action helps to prevent the absorption of harmful substances into the bloodstream, facilitating their elimination from the body.

Pharmacodynamics

The efficacy of activated charcoal is related to its ability to adsorb a wide range of substances, including many pharmaceuticals and poisons. The effectiveness can vary depending on the specific substance, the timing of administration, and the dose of activated charcoal. It is generally most effective when administered soon after ingestion of the toxin.

Pharmacokinetics

Activated charcoal is not absorbed systemically; it acts locally within the gastrointestinal tract. After administration, it passes through the gastrointestinal system and is eventually excreted in the feces. The adsorption capacity of activated charcoal is influenced by factors such as the surface area, particle size, and the nature of the toxin to which it is exposed.

Contra-indications

• Intestinal obstruction
• Gastrointestinal perforation
• Severe constipation

Adverse effects

• Gastrointestinal disturbances such as nausea and vomiting
• Constipation
• Black stools
• Aspiration pneumonia if inhaled

Interactions

• May reduce the absorption of certain medications, including anticoagulants, anticonvulsants, and others
• Should not be given simultaneously with other oral medications

Precautions

• Use with caution in patients with a history of gastrointestinal disorders
• Ensure airway protection in unconscious or compromised patients to prevent aspiration
• Monitor for potential electrolyte imbalances

Pregnancy

Charcoal is generally considered safe during pregnancy, but should only be used when necessary and under medical supervision.

Breast-feeding

Charcoal is unlikely to adversely affect a nursing infant, but should be used with caution.

Storage

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

Formulations

• Activated charcoal tablets
• Activated charcoal powder
• Activated charcoal suspension

Indications

• Carbohydrate malabsorption
• Digestive disorders
• Pancreatic insufficiency
• Postprandial distress

Dosage

Children: Refer to BNF for Children for specific dosing recommendations based on age and weight.

Adults: Refer to BNF for specific dosing recommendations based on clinical condition.

Mechanism of action

Diastase works by hydrolyzing glycosidic bonds in starch and glycogen, converting them into simpler sugars such as maltose and glucose. This enzymatic reaction occurs in the small intestine, enhancing the overall efficiency of carbohydrate digestion and absorption.

Pharmacodynamics

The pharmacodynamics of diastase is characterized by its ability to improve the digestion of carbohydrates. By increasing the availability of monosaccharides, it aids in nutrient absorption and can alleviate symptoms associated with malabsorption syndromes. The onset of action typically occurs shortly after administration, depending on the formulation and presence of food in the gastrointestinal tract.

Pharmacokinetics

Diastase is not absorbed systemically, as it acts locally within the gastrointestinal lumen. Its activity is influenced by the pH of the intestinal environment, with optimal activity occurring in a slightly alkaline medium. The enzyme is excreted with the feces, and its half-life is not generally measured, as it is not a drug that circulates in the bloodstream.

Pregnancy

The safety of diastase during pregnancy has not been established. Use only if clearly needed and after assessing risks versus benefits.

Breast-feeding

There are no data on the excretion of diastase in human milk, and caution is recommended when administering to nursing mothers.

Storage

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

Indications

• Candidiasis
• Aspergillosis
• Cryptococcal meningitis
• Dermatophyte infections
• Histoplasmosis
• Blastomycosis
• Coccidioidomycosis

Dosage

Children: Refer to specific antif

Adults: Refer to specific antifungal agents for dosing information, as dosages vary widely by the type of infection and the antifungal being used.

Mechanism of action

Antifungal agents typically act by targeting the fungal cell membrane or cell wall, inhibiting synthesis of ergosterol, a key component of the membrane, or by disrupting cell wall integrity. This leads to cell death or inhibition of fungal growth. Different classes of antifungals, such as azoles, echinocandins, and polyenes, have specific mechanisms that exploit unique fungal structures.

Pharmacodynamics

Fungal cells have distinct biological pathways that differ from mammalian cells, allowing antifungal agents to selectively target fungal cells. For example, azoles inhibit the enzyme lanosterol demethylase, which is crucial in ergosterol synthesis, while echinocandins inhibit the synthesis of β(1,3)-D-glucan, an essential component of the fungal cell wall. The effect of antifungal therapy is influenced by the type of fungal organism, the site of infection, and the patient's immune status.

Pharmacokinetics

The pharmacokinetics of antifungal agents vary significantly among different classes. Generally, systemic antifungals are absorbed through the gastrointestinal tract, distributed to various body tissues, metabolized in the liver, and excreted via urine or feces. The half-life, volume of distribution, and clearance rates depend on the specific drug and its formulation. For example, some azoles have prolonged half-lives allowing for less frequent dosing, while others may require adjustments based on liver function.

Pregnancy

Consult relevant guidelines, as the safety of antifungal drugs during pregnancy varies by specific drug.

Breast-feeding

Consult relevant guidelines, as the safety of antifungal drugs during breastfeeding varies by specific drug.

Storage

Store in a cool, dry place away from direct sunlight. Specific storage conditions can vary by formulation.

Indications

• Digestive disorders
• Protein digestion aid
• Wound healing
• Anti-inflammatory treatment

Dosage

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

Adults: Refer to specific product guidelines or consult a healthcare professional for dosing recommendations, as doses can vary based on formulation and indication.

Mechanism of action

Papain works by hydrolyzing peptide bonds in proteins, which facilitates their digestion and absorption. It acts primarily in the gastrointestinal tract, where it helps convert complex proteins into simpler forms that can be easily absorbed. Papain's proteolytic action also contributes to its anti-inflammatory properties, as it can help reduce swelling and promote healing in tissues.

Pharmacodynamics

Papain exhibits its effects through its enzymatic activity on proteins. The breakdown of proteins into smaller peptides and amino acids aids in the digestive process. This enzymatic action is complemented by papain's ability to modulate inflammatory responses, which can be beneficial in treating conditions associated with tissue damage and inflammation.

Pharmacokinetics

Papain is typically administered orally or topically. When taken orally, it is subject to the acidic environment of the stomach, which may affect its stability and activity. However, it is generally well absorbed in the gastrointestinal tract. Topically applied papain is absorbed through the skin, where it can exert local effects. The half-life and specific metabolic pathways of papain are not well characterized due to its natural origin and the variability in formulations.

Contra-indications

• Hypersensitivity to papain or any of its components
• History of allergic reactions to other proteolytic enzymes

Adverse effects

• Allergic reactions including rash, itching, or swelling
• Gastrointestinal disturbances such as nausea, vomiting, or diarrhea
• Potential irritation or inflammation at the site of application

Precautions

• Use with caution in individuals with known allergies to other enzymes or related substances
• Consult a healthcare provider before use in patients with gastrointestinal disorders
• Not recommended for use in infants and young children without medical supervision

Pregnancy

Safety during pregnancy has not been established. Use only if clearly needed and prescribed by a healthcare professional.

Breast-feeding

There is insufficient data on the excretion of papain in human milk. Caution is advised when administering to nursing mothers.

Storage

Store at room temperature away from moisture and heat. Keep tightly closed in a cool, dry place.

Formulations

• Oral tablets
• Topical creams or ointments
• Powder for solution

Indications

• Flatulence
• Bloating
• Gastroesophageal reflux disease
• Functional dyspepsia

Dosage

Children: For children, refer to the BNF for Children for specific dosing recommendations.

Adults: The usual adult dose is 40 to 125 mg taken after meals and at bedtime, as needed.

Mechanism of action

Simethicone is a surfactant that decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. It acts by forming a film of low surface tension that promotes the coalescence of mucus-surrounded gas bubbles, allowing for easier passage of gas.

Pharmacodynamics

Simethicone decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. Its effects are generally short-lived, as it is typically administered as needed. The therapeutic index is wide since it is not absorbed systemically, making it safe for use in various patient populations.

Pharmacokinetics

Simethicone is not systemically absorbed following oral administration, which contributes to its safety profile. Due to its lack of systemic absorption, specific pharmacokinetic parameters such as half-life, clearance, and volume of distribution are not applicable.

Pregnancy

Simethicone can be used during pregnancy as there are no known risks associated with its use.

Breast-feeding

Simethicone is considered safe to use during breastfeeding, as it is not absorbed systemically.

Storage

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

Formulations

• Oral suspension
• Chewable tablets
• Soft gels

Mechanism of action

Simethicone is a surfactant that decreases the surface tension of gas bubbles in the gastrointestinal tract, more easily allowing gas to exit the body. The clinical use of simethicone is based on its antifoam properties. Silicone antifoams spread on the surface of aqueous liquids, forming a film of low surface tension and thus causing collapse of foam bubbles. Simethicone reportedly allows mucus-surrounded gas bubbles in the GI tract to coalesce and be expelled.

Pharmacodynamics

Simethicone decreases the surface tension of gas bubbles in the gastrointestinal tract, facilitating their expulsion. It has a short duration of action as it is generally given as needed, and a wide therapeutic index as it is not systemically absorbed.