LAZINE

Indications

• Seasonal allergic rhinitis
• Chronic idiopathic urticaria

Dosage

Children: For children aged 6 to 11 years, the dose is 30 mg twice daily. For children aged 12 to 17 years, the dose is 120 mg once daily.

Adults: For adults, the recommended dose is 180 mg once daily.

Mechanism of action

Levocetirizine is an active enantiomer of cetirizine and functions as a selective antagonist of the peripheral H1 receptor. By blocking the action of histamine, a key mediator in allergic responses, it reduces symptoms such as sneezing, itching, and runny nose. It also prevents the activation of sensory neurons, thereby mitigating pruritus and swelling associated with allergic reactions.

Pharmacodynamics

Levocetirizine exhibits antihistaminic effects with a rapid onset of action. Its affinity for peripheral H1 receptors allows it to effectively reduce the symptoms of allergic rhinitis and urticaria. While it is termed 'non-sedating', some degree of sedation may still occur in sensitive individuals, although this is generally minimal compared to first-generation antihistamines.

Pharmacokinetics

Levocetirizine is well absorbed after oral administration, with peak plasma concentrations typically reached within 0.9 hours. The drug has a volume of distribution of approximately 0.4 L/kg and is primarily excreted unchanged in urine. It has a half-life of about 8 hours, allowing for once-daily dosing. In patients with renal impairment, dose adjustments may be necessary due to altered drug clearance.

Contra-indications

• Acute porphyrias

Adverse effects

• Asthenia
• Constipation
• Drowsiness
• Dry mouth
• Abdominal pain
• Aggression
• Agitation
• Angioedema
• Appetite increased
• Arthralgia
• Depression
• Diarrhoea
• Dizziness
• Fatigue
• Hallucination
• Hepatitis
• Myalgia
• Nausea
• Oedema
• Palpitations
• Paraesthesia
• Seizure
• Skin reactions
• Sleep disorders
• Suicidal ideation
• Syncope
• Tachycardia
• Taste altered
• Tremor
• Urinary disorders
• Vertigo
• Vision disorders
• Vomiting
• Weight increased

Interactions

• Other antihistamines
• Alcohol (may increase sedation)
• CNS depressants

Precautions

• Caution in renal impairment
• Patients should be advised about potential drowsiness affecting driving and skilled tasks

Pregnancy

Most manufacturers of antihistamines advise avoiding their use during pregnancy; however, there is no evidence of teratogenicity.

Breast-feeding

Most antihistamines are present in breast milk in varying amounts; although not known to be harmful, most manufacturers advise avoiding their use in mothers who are breastfeeding.

Storage

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

Formulations

• Oral suspension
• Oral solution
• Tablets

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

• Hypovolemic shock
• Severe burns
• Postoperative fluid replacement
• Sepsis
• Trauma management

Dosage

Children: Refer to established guidelines for specific dosing, as it varies based on the type of colloidal solution used and the clinical condition being treated.

Adults: Refer to established guidelines for specific dosing, as it varies based on the type of colloidal solution used and the clinical condition being treated.

Mechanism of action

Colloidal solutions work by maintaining oncotic pressure in the blood, thus helping to retain fluid within the vascular system. This is primarily due to the large molecular weight of the colloidal particles, which cannot easily pass through capillary walls. The presence of colloids in the blood helps to draw water into the circulation, increasing blood volume and improving tissue perfusion.

Pharmacodynamics

The pharmacodynamics of colloidal solutions are centered on their ability to exert osmotic pressure, which helps maintain blood volume and pressure. This effect is particularly important in conditions such as hypovolemia and shock, where fluid replacement is necessary to restore hemodynamic stability. The efficacy of colloidal solutions can vary depending on the type of colloid used, as well as the underlying clinical condition being treated.

Pharmacokinetics

Colloidal solutions are typically administered intravenously and their pharmacokinetics can vary based on the specific formulation. Generally, colloids are distributed throughout the vascular compartment and have a longer duration of action compared to crystalloids, as they remain in circulation longer. The elimination of colloids is primarily through the reticuloendothelial system, where they are metabolized or eliminated by the liver and spleen. Factors such as particle size and composition can influence their distribution and clearance.

Adverse effects

• Allergic reactions
• Injection site reactions
• Nausea
• Vomiting
• Headache
• Fever

Precautions

• Use with caution in patients with known allergies to any component of the formulation
• Monitor for signs of hypersensitivity during administration
• Consider volume overload in patients with cardiac or renal impairment

Pregnancy

The safety of colloidal solutions during pregnancy has not been established. Use only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether colloidal solutions are excreted in human milk. Caution should be exercised when administering to breastfeeding mothers.

Storage

Store at room temperature, protect from light, and do not freeze. Keep out of reach of children.

Formulations

• Colloidal silver
• Colloidal gold
• Colloidal iron
• Other metal colloids

Dosage

Children: Refer to specific formulation guidelines, as inert substances do not have dosing recommendations.

Adults: Refer to specific formulation guidelines, as inert substances do not have dosing recommendations.

Mechanism of action

Inert substances do not have a mechanism of action as they do not interact with biological systems in a pharmacological manner. Their role is primarily to serve as carriers or stabilizers in drug formulations.

Pharmacodynamics

Pharmacodynamics is not applicable to inert substances since they do not produce a therapeutic effect or interact with biological systems. Their function is supportive rather than active.

Pharmacokinetics

Pharmacokinetics does not apply to inert substances as they are not metabolized or excreted in a manner similar to active drugs. They remain unchanged in the body and do not contribute to the pharmacological profile.

Pregnancy

Safety during pregnancy is not established. Consult a healthcare provider before use.

Breast-feeding

Safety during breastfeeding is not established. Consult a healthcare provider before use.

Storage

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

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
• Chronic urticaria

Dosage

Children: For children aged 6 to 11 years, the recommended dose is 5 mg once daily. For children aged 2 to 5 years, the dose is 1.25 mg once daily.

Adults: The usual dose for adults is 5 mg once daily.

Mechanism of action

Levocetirizine selectively inhibits histamine H1 receptors. This action prevents histamine from activating the receptor and causing effects such as smooth muscle contraction, increased permeability of vascular endothelium, histidine uptake in basophils, stimulation of cough receptors, and stimulation of flare responses in the nervous system.

Pharmacodynamics

As a second-generation histamine H1 antagonist, levocetirizine effectively reduces various allergic symptoms. It possesses a long duration of action, allowing for once-daily dosing. The therapeutic index is favorable, with studies showing that the maximal nonlethal dose is significantly higher than the therapeutic dose. Caution is advised for activities requiring full alertness and in patients predisposed to urinary retention.

Pharmacokinetics

Levocetirizine is well absorbed after oral administration, with peak plasma concentrations typically reached within approximately 1 hour. It has a volume of distribution of about 0.4 L/kg and is primarily excreted unchanged in the urine. The elimination half-life is approximately 8 to 9 hours, allowing for once-daily dosing.

Contra-indications

• Hypersensitivity to levocetirizine or any of its components
• Severe renal impairment

Adverse effects

• Drowsiness
• Fatigue
• Dry mouth
• Headache
• Gastrointestinal disturbances

Interactions

• CNS depressants may enhance sedative effects
• Alcohol may increase sedation

Precautions

• Caution in patients with a history of urinary retention
• Caution in patients with severe renal impairment
• Avoid operating machinery or driving until you know how levocetirizine affects you

Pregnancy

Levocetirizine should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

Levocetirizine is excreted in breast milk; caution should be exercised when administering to nursing mothers.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Tablets
• Oral solution

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

Indications

• Support of skin health
• Promotion of connective tissue strength
• Usage as an anti-caking agent in food and pharmaceutical preparations

Dosage

Children: Consult the BNF for Children for appropriate dosing information, as specific pediatric dosing recommendations for silica are not universally established.

Adults: Refer to specific product guidelines, as dosages can vary based on the formulation and intended use. General guidance suggests that silica supplements are often taken in doses ranging from 10 to 50 mg per day, but specific recommendations should be followed.

Mechanism of action

Silica is thought to play a role in the synthesis of collagen, which is essential for maintaining the structural integrity of various tissues, including skin, bones, and cartilage. It may aid in the absorption of essential nutrients and contribute to the overall strength and elasticity of connective tissues.

Pharmacodynamics

Silica is not absorbed significantly in the gastrointestinal tract when ingested. Its pharmacodynamic effects are largely attributed to its role in supporting connective tissue and enhancing the bioavailability of certain nutrients. Its presence in the body may also influence metabolic processes related to bone and skin health.

Pharmacokinetics

Silica is generally not absorbed systemically. When ingested, it passes through the gastrointestinal tract and is excreted in feces. Some studies suggest that silica can be incorporated into tissues, but the exact pharmacokinetic profile can vary based on the form and route of administration.

Pregnancy

There is limited data on the safety of silca during pregnancy. It should only be used if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is not known whether silca 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 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

Levocetirizine selectively inhibits histamine H₁ receptors. This action prevents histamine from activating this receptor and causing effects like smooth muscle contraction, increased permeability of vascular endothelium, histidine uptake in basophils, stimulation of cough receptors, and stimulation of flare responses in the nervous system.

Pharmacodynamics

Levocetirizine is a second generation histamine H₁ antagonist used to treat various allergic symptoms. It has a long duration of action as it is generally taken once daily, and a wide therapeutic window as animal studies show the maximal nonlethal dose is over 100x a normal dose. Patients are cautioned to avoid tasks that require complete alertness, avoid alertness, and use caution in patients with factors predisposing urinary retention.