IBICAR-250

Indications

• Prophylaxis of asthma
• Management of allergic rhinitis
• Treatment of nasal polyps

Dosage

Children: For children aged 2–11 years, the dose is 100–200 micrograms twice daily; for children aged 12–17 years, 200–400 micrograms twice daily, adjusted according to response.

Adults: For adults and children over 12 years with chronic asthma, the usual starting dose is 200-400 micrograms twice daily, which may be increased if necessary.

Mechanism of action

Beclometasone dipropionate acts by binding to glucocorticoid receptors in target cells, leading to the modulation of gene expression and the inhibition of pro-inflammatory cytokines, thereby reducing inflammation and hyperresponsiveness in the airways.

Pharmacodynamics

As a potent anti-inflammatory agent, beclometasone dipropionate decreases the infiltration of inflammatory cells into the airways, reduces mucus production, and enhances beta-adrenergic responsiveness. This results in improved airflow and reduced asthma symptoms.

Pharmacokinetics

Beclometasone dipropionate is administered via inhalation, where it undergoes extensive first-pass metabolism in the liver. Its systemic bioavailability is low due to significant hepatic metabolism. The drug has a long duration of action, with effects lasting for 12-24 hours, allowing for once or twice-daily dosing.

Contra-indications

• Hypersensitivity to beclometasone dipropionate or any of its excipients
• Hypersensitivity to atropine or its derivatives

Adverse effects

• Throat irritation
• Wheezing
• Nasal complaints
• Headache
• Nausea
• Stomatitis
• Gastrointestinal absorption may occur
• Corneal oedema
• Eye disorders
• Eye pain
• Palpitations

Precautions

• Monitor growth in children receiving prolonged treatment
• Consider systemic corticosteroid side effects with high doses or prolonged use

Pregnancy

Manufacturer advises only use if potential benefit outweighs the risk.

Breast-feeding

No information available-manufacturer advises only use if potential benefit outweighs risk.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Inhalation aerosol (Clenil Modulite®)
• Inhalation powder (Qvar®)

Indications

• Asthma
• Chronic obstructive pulmonary disease (COPD)
• Allergic rhinitis
• Topical treatment of inflammatory skin conditions

Dosage

Children: Dosing in children should be determined based on the BNF for Children. Refer to the BNF for specific paediatric dosing information.

Adults: The dosage for adults varies depending on the condition being treated. Refer to the BNF for specific dosing guidelines.

Mechanism of action

Beclometasone acts by binding to glucocorticoid receptors, leading to the modulation of gene expression. This results in the inhibition of pro-inflammatory cytokines and the promotion of anti-inflammatory proteins, thereby reducing inflammation and immune response.

Pharmacodynamics

As a corticosteroid, beclometasone exerts its effects by modulating various cellular functions. It decreases the migration of leukocytes to sites of inflammation, reduces capillary permeability, and inhibits the release of enzymes that contribute to the inflammatory response. The therapeutic effects are evident in conditions characterized by excessive inflammation.

Pharmacokinetics

Beclometasone is well-absorbed when administered by inhalation, and its bioavailability is significantly enhanced when delivered directly to the lungs. It undergoes extensive first-pass metabolism in the liver, which reduces systemic exposure. The half-life of beclometasone is approximately 15 hours, and it is primarily excreted via the urine as metabolites.

Contra-indications

• Hypersensitivity to beclometasone or any of its components
• Systemic fungal infections
• Active or latent tuberculosis

Adverse effects

• Local irritation
• Dryness of the throat
• Cough
• Dysphonia
• Oral candidiasis
• Adrenal suppression (with prolonged use)

Interactions

• cobicistat+beclometasone: Unknown (increases exposure)
• idelalisib+beclometasone: Unknown (increases exposure)
• clarithromycin+beclometasone: Unknown (increases exposure)

Precautions

• Use with caution in patients with active infections
• Monitor for signs of adrenal insufficiency in long-term therapy
• Consider alternate therapy in patients with a history of severe allergic reactions

Pregnancy

Beclometasone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Consult a healthcare provider.

Breast-feeding

Beclometasone is excreted in breast milk. Caution should be exercised when administering to nursing mothers.

Storage

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

Formulations

• Inhaler
• Nasal spray
• Topical cream
• Topical ointment

Indications

• Asthma
• Chronic Obstructive Pulmonary Disease (COPD)
• Allergic Rhinitis
• Cystic Fibrosis
• Pulmonary Hypertension

Dosage

Children: Refer to specific inhaled medication guidelines for paediatric dosing.

Adults: Refer to specific inhaled medication guidelines for adult dosing.

Mechanism of action

Inhaled medications can have various mechanisms of action depending on the specific drug. For example, beta-2 adrenergic agonists stimulate beta-2 receptors on bronchial smooth muscle, leading to bronchodilation. Corticosteroids inhibit the expression of inflammatory mediators and reduce airway inflammation, while anticholinergics block acetylcholine from binding to its receptors, resulting in decreased bronchoconstriction.

Pharmacodynamics

The pharmacodynamics of inhaled medications involve their interaction with specific receptors or pathways in the lungs. Bronchodilators cause relaxation of the bronchial smooth muscle, leading to increased airflow. Corticosteroids effectively reduce inflammation and mucus production in the airways, thereby improving respiratory function and reducing exacerbations of asthma and COPD. The rapid delivery of these drugs to the site of action enhances their efficacy.

Pharmacokinetics

Inhaled medications have distinct pharmacokinetic properties. The onset of action can be very rapid, often within minutes, due to direct delivery to the lungs. The bioavailability depends on factors such as particle size, inhalation technique, and the type of inhaler used. Systemic absorption is generally lower than with oral medications, which minimizes systemic side effects. The duration of action varies based on the specific drug class; for example, short-acting beta agonists provide quick relief, while long-acting agents offer prolonged effects.

Pregnancy

Consult healthcare provider for risk assessment and guidance, as safety data may vary depending on the specific inhalation formulation.

Breast-feeding

Consult healthcare provider, as some inhalation medications may be excreted in breast milk and could affect the infant.

Storage

Store in a cool, dry place away from direct sunlight. Check specific product guidelines for temperature and humidity requirements.

Indications

• Asthma
• Chronic Obstructive Pulmonary Disease (COPD)
• Allergic Rhinitis
• Acute Bronchospasm
• Exercise-Induced Bronchospasm

Dosage

Children: Refer to the BNF for Children for specific paediatric dosing information, as it varies by medication and condition.

Adults: Refer to the specific product information for adult dosing, as it varies by medication and condition.

Mechanism of action

Pressurized drug delivery systems, such as metered-dose inhalers (MDIs), utilize propellants to create an aerosolized mist of medication. The active pharmaceutical ingredient is usually a bronchodilator, corticosteroid, or a combination, which works by relaxing bronchial smooth muscles, reducing inflammation, and improving airflow in the lungs.

Pharmacodynamics

The pharmacodynamics of pressurized inhalation therapies depend on the specific drug used. For instance, beta-2 adrenergic agonists lead to bronchodilation by stimulating beta-2 receptors in the bronchial smooth muscle, while corticosteroids reduce inflammation by inhibiting various inflammatory processes and immune responses in the airways.

Pharmacokinetics

The pharmacokinetics of drugs delivered via pressurized systems varies widely depending on the active ingredient. Generally, the onset of action is rapid due to direct delivery to the lungs, with peak effects occurring within minutes to hours. Systemic absorption may occur, though this is often limited compared to oral or intravenous routes. The half-life, metabolism, and excretion depend on the specific drug component.

Pregnancy

Use during pregnancy only if clearly needed. Assess the risks and benefits with a healthcare provider.

Breast-feeding

Use with caution. Monitor the infant for potential side effects.

Storage

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