ADCO-LINCTOPENT

Indications

• Chronic bronchitis
• Asthma
• Bronchiectasis
• Pneumonia
• Respiratory tract infections with productive cough

Dosage

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

Adults: Refer to the BNF for specific dosing information.

Mechanism of action

Bromhexine aids in mucus clearance by reducing the viscosity of mucus and activating the ciliary epithelium, allowing secretions to be expelled from the respiratory tract. Additionally, bromhexine has been shown to inhibit the transmembrane serine protease 2 receptor (TMPRSS2), which plays a crucial role in viral respiratory diseases. This inhibition may help in preventing or treating various respiratory illnesses, including COVID-19, by blocking viral entry into cells.

Pharmacodynamics

Bromhexine thins airway secretions, thus improving breathing and alleviating discomfort associated with thick mucus in the airways. Its action is particularly beneficial in respiratory disorders where mucus obstruction is a significant issue.

Pharmacokinetics

Bromhexine is well absorbed after oral administration, with peak plasma concentrations typically reached within 1 to 2 hours. It is metabolized in the liver, primarily to ambroxol, which is its active metabolite. The elimination half-life of bromhexine is approximately 8 to 12 hours, and it is excreted mainly through urine. The pharmacokinetics can be influenced by factors such as liver function and concurrent medications.

Adverse effects

• Gastrointestinal disturbances
• Nausea
• Vomiting
• Diarrhea
• Allergic reactions

Precautions

• Use with caution in patients with peptic ulcer disease
• Monitor patients with asthma or bronchospastic conditions

Pregnancy

Bromhexine should be used during pregnancy only if clearly needed and after careful consideration of the potential benefits and risks.

Breast-feeding

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

Storage

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

Formulations

• Tablets
• Syrup
• Solution for inhalation

Indications

• Asthma
• Chronic obstructive pulmonary disease (COPD)
• Bronchospasm associated with reversible airway obstruction

Dosage

Children: Refer to specific guidelines or product information for dosing in children, as pediatric doses must be determined based on age, weight, and clinical condition.

Adults: Refer to specific guidelines or product information for dosing in adults, as doses can vary based on the preparation and clinical context.

Mechanism of action

Orcinoprenaline acts primarily on beta-2 adrenergic receptors located on the smooth muscle of the airways. Activation of these receptors stimulates adenylate cyclase, increasing intracellular levels of cyclic AMP (cAMP). Elevated cAMP levels lead to the activation of protein kinase A (PKA), which phosphorylates various proteins that result in smooth muscle relaxation and bronchodilation. Additionally, beta-2 agonists inhibit the release of bronchoconstrictor mediators from mast cells, contributing to their therapeutic effect.

Pharmacodynamics

The pharmacodynamic profile of orcinoprenaline includes rapid onset of action, typically within minutes of administration, and a duration of action that can last several hours. The drug's selectivity for beta-2 receptors minimizes cardiovascular side effects commonly associated with non-selective beta-adrenergic agonists. Side effects may include tremors, tachycardia, and hypokalemia, though these are generally less pronounced than with other agents.

Pharmacokinetics

Orcinoprenaline is rapidly absorbed following inhalation, with peak plasma concentrations achieved shortly after dosing. The drug undergoes hepatic metabolism, primarily through conjugation and oxidation pathways, with renal excretion of metabolites. The half-life of orcinoprenaline varies but is generally in the range of 3 to 6 hours, necessitating multiple doses throughout the day for sustained therapeutic effect.

Contra-indications

• Hypersensitivity to orcinoprenaline or any of its components
• Severe cardiovascular disorders
• Hyperthyroidism
• Pheochromocytoma
• Tachyarrhythmias

Adverse effects

• Tachycardia
• Palpitations
• Tremors
• Nervousness
• Headache
• Dizziness
• Hypertension
• Nausea
• Vomiting

Interactions

• Monoamine oxidase inhibitors (MAOIs) may enhance the pressor effects
• Beta-blockers may reduce the effectiveness of orcinoprenaline
• Other sympathomimetics may increase the risk of cardiovascular adverse effects

Precautions

• Use with caution in patients with diabetes mellitus due to potential hyperglycemia
• Monitor patients with pre-existing cardiovascular conditions closely
• Caution in patients with seizure disorders
• Assess risks versus benefits in the elderly or those with frail health

Pregnancy

Orcinoprenaline should only be used in pregnancy if the potential benefit justifies the risk to the fetus, as limited data are available on its safety during pregnancy.

Breast-feeding

It is not known whether orcinoprenaline is excreted in human milk. Caution is advised when administering to nursing mothers.

Storage

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

Formulations

• Inhalation aerosol
• Tablet
• Injection solution

Mechanism of action

Inflammation of the airways, increased mucus secretion, and altered mucociliary clearance are the hallmarks of various diseases of the respiratory tract. Mucus clearance is necessary for lung health; bromhexine aids in mucus clearance by reducing the viscosity of mucus and activating the ciliary epithelium, allowing secretions to be expelled from the respiratory tract. Recent have studies have demonstrated that bromhexine inhibits the transmembrane serine protease 2 receptor (TMPRSS2) in humans. Activation of TMPRSS2 plays an important role in viral respiratory diseases such as influenza A and Middle East Respiratory Syndrome (MERS). Inhibition of receptor activation and viral entry by bromhexine may be effective in preventing or treating various respiratory illnesses, including COVID-19. In vitro studies have suggested the action of ambroxol (a metabolite of bromhexine) on the angiogensin-converting enzyme receptor 2 (ACE2), prevents entry of the viral envelope-anchored spike glycoprotein of SARS-Cov-2 into alveolar cells or increases the secretion of surfactant, preventing viral entry.

Pharmacodynamics

Bromhexine thins airway secretions, improving breathing and discomfort associated with thick mucus in airways associated with a variety of respiratory conditions.