BRONKESE COMBINATION PRODUCT COUGH LINCTUS

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

• Bronchospasm
• Asthma
• Chronic obstructive pulmonary disease (COPD)

Dosage

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

Adults: Refer to the BNF for specific dosing guidelines.

Mechanism of action

Orciprenaline stimulates the β2-adrenergic receptors in the lungs, uterus, and vasculature supplying skeletal muscles, acting as a moderately selective agonist. Its actions are mediated through the intracellular signaling pathway involving cyclic adenosine monophosphate (cAMP), which is increased by the activation of adenylate cyclase, leading to relaxation of bronchial smooth muscles and inhibition of inflammatory mediator release from mast cells.

Pharmacodynamics

As a synthetic amine similar to isoproterenol, orciprenaline's pharmacological effects are primarily due to its action on beta-adrenergic receptors. The stimulation of these receptors results in the activation of adenylate cyclase, promoting the conversion of ATP to cAMP. Elevated cAMP levels induce relaxation of bronchial smooth muscles and suppress the release of inflammatory mediators, contributing to its efficacy as a bronchodilator.

Pharmacokinetics

Orciprenaline is administered via inhalation or orally. Its onset of action typically occurs within minutes when inhaled, and its effects can last for several hours. The drug is metabolized in the liver and excreted primarily through the urine. The half-life and specific metabolic pathways have not been detailed in the available data.

Adverse effects

• Tachycardia
• Palpitations
• Tremors
• Headache
• Nausea
• Dizziness
• Hypokalemia

Interactions

• Other sympathomimetics may potentiate the effect of orciprenaline
• Beta-blockers may reduce the effectiveness of orciprenaline
• Corticosteroids may enhance the effect of orciprenaline

Precautions

• Use with caution in patients with cardiovascular disorders
• Monitor potassium levels in patients at risk of hypokalemia
• Caution in patients with hyperthyroidism, diabetes mellitus, or seizure disorders

Pregnancy

Orciprenaline should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Breast-feeding

It is unknown whether orciprenaline is excreted in human milk. Caution should be exercised when administering to nursing mothers.

Storage

Store in a cool, dry place away from light. Do not freeze.

Formulations

• Inhalation solution
• Metered dose inhaler

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.

Mechanism of action

Orciprenaline stimulates the β2-adrenergic receptor expressed in the lungs, uterus, and vasculature supplying skeletal muscles by acting as a moderately selective agonist. It exerts minimal or no effect on alpha-adrenergic receptors. Intracellularly, the actions of orciprenaline are mediated by cAMP, the production of which is augmented by beta stimulation. The drug is believed to work by activating adenylate cyclase, the enzyme responsible for producing the cellular mediator cAMP.

Pharmacodynamics

Orciprenaline (also known as metaproterenol), a synthetic amine, is structurally and pharmacologically similar to isoproterenol. Orciprenaline is used exclusively as a bronchodilator. The pharmacological effects of beta adrenergic agonist drugs, such as orciprenaline, are at least in part attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic- 3',5'- adenosine monophosphate (c-AMP). Increased cAMP levels lead to relaxation of bronchial smooth muscles and inhibition of the release of inalammatory mediators from mast cells that are involved in promoting immediate hypersensitivity .