levocetirizine/montelukast/ambroxol

Action and Spectrum

Actions and Spectrum: 

levocetirizine: 

Action: levocetirizine is an antihistamine drug commonly used to relieve allergy symptoms.  

Spectrum: levocetirizine is primarily used to treat symptoms like runny nose, sneezing, itchy or watery eyes, and itching of the throat or nose. It is often used to manage seasonal allergies (hay fever) and chronic idiopathic urticaria (hives of unknown cause). 

montelukast: 

Action: montelukast is a typically leukotriene receptor antagonist. It generally works by blocking the action of the leukotrienes, which are inflammatory mediators that may cause constriction of airways, inflammation, and other allergic responses in the body. 

Spectrum: montelukast is mainly used to treat asthma and allergic rhinitis. It can help prevent asthma attacks and improve symptoms of allergic rhinitis, like sneezing, runny or stuffy nose, and itching. 

ambroxol: 

Action: ambroxol is a mucolytic and expectorant drug. It works by thinning and also loosening mucus in the airways, making it more easier to cough up and also clear from the respiratory tract. It also has some anti-inflammatory properties. 

Spectrum: ambroxol relieves symptoms associated with respiratory conditions characterized by excessive mucus production, such as acute and chronic bronchitis, chronic obstructive pulmonary disease, and respiratory infections. It can help make coughs more productive and lessen the discomfort caused by thick and sticky mucus.

Drug Interaction

Adverse Reaction

Frequency not defined 

Diarrhea 

Influenza 

Constipation 

Abdominal pain 

Headache 

Otitis media 

Dryness in mouth 

Allergic reaction 

Vomiting 

Sleepiness 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindication 

levocetirizine:  

• Hypersensitivity or allergy to levocetirizine or other antihistamines. 
• Severe kidney impairment (requires dose adjustment). 

montelukast:  

• Hypersensitivity or allergy to montelukast or other leukotriene receptor antagonists. 
• Active liver disease. 
• Phenylketonuria (PKU) – Some formulations may contain phenylalanine. 
• Children under six for specific indications (e.g., exercise-induced bronchoconstriction). 

ambroxol:  

• Hypersensitivity or allergy to ambroxol or related compounds. 
• Certain rare hereditary conditions like fructose intolerance, glucose-galactose malabsorption, or sucrase-isomaltase deficiency (some formulations may contain sugar alcohols). 
• Severe liver impairment. 

Caution 

levocetirizine: 

• Impaired Kidney Function: levocetirizine should be used cautiously in individuals with moderate-severe kidney impairment.  
• Central Nervous System (CNS) Depression: levocetirizine can cause drowsiness in some individuals.  

montelukast: 

• Neuropsychiatric Events: montelukast has been associated with neuropsychiatric events such as agitation, aggression, mood changes, and suicidal thoughts in some individuals, particularly children and adolescents. Patients, especially children, should be monitored for these symptoms, and the drug should be discontinued if they occur. 
• Churg-Strauss Syndrome: montelukast should be used with caution in patients with a history of Churg-Strauss syndrome, as it has been reported to exacerbate this condition in rare cases. 

ambroxol: 

• Gastric Ulcers: ambroxol should be used cautiously in individuals with a history of gastric/duodenal ulcers because it may cause gastric irritation. 
• Liver Impairment: Patients with liver impairment should use ambroxol cautiously, as the drug’s metabolism may be altered. Dose adjustments may be necessary. 
• Pregnancy and Breastfeeding: While ambroxol is generally considered safe during pregnancy and breastfeeding, caution should still be exercised, and it should only be used if the potential benefits outweigh the risks. Consultation with a healthcare provider is recommended in such cases. 
• Asthma and Chronic Obstructive Pulmonary Disease (COPD): ambroxol is commonly used in these respiratory conditions. However, it should be used cautiously in patients with a history of bronchial asthma, as it may cause bronchospasms in some cases. 

Pregnancy / Lactation

Pregnancy consideration:  

US FDA pregnancy category: Not assigned. 

Lactation:   

Excreted into human milk: Not known. 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence, these categories of drugs need to be avoided by pregnant women.    
• Category N: There is no data available for the drug under this category. 

Pharmacology

Pharmacology: 

levocetirizine is a second-generation antihistamine that selectively antagonizes the H1 histamine receptor, effectively blocking histamine-mediated allergic responses, thereby alleviating symptoms like runny nose and itching. montelukast, a leukotriene receptor antagonist, inhibits the actions of leukotrienes, inflammatory mediators involved in allergic and asthmatic reactions, thus reducing bronchoconstriction and inflammation in conditions like asthma and allergic rhinitis.

ambroxol acts as a mucolytic and expectorant by breaking down and thinning mucus in the respiratory tract, making it easier to clear, which aids in the management of conditions characterized by excessive mucus production and coughs, such as bronchitis and chronic obstructive pulmonary disease (COPD). When used in combination, these drugs can target various aspects of respiratory conditions, relieving allergic and mucus-related symptoms. 

Pharmacodynamics: 

Mechanism of action: The mechanism of action of levocetirizine, montelukast, and ambroxol involves their interactions with specific receptors and biochemical pathways in the body, and they serve different purposes: 

levocetirizine: 

levocetirizine is a second-generation antihistamine. It works by selectively blocking the action of histamine at the H1 histamine receptors. Histamine is the chemical released during allergic reactions, and it binds to these receptors, leading to symptoms like itching, sneezing, runny nose, and watery eyes. By antagonizing the H1 receptors, levocetirizine effectively inhibits the histamine-mediated allergic response, relieving these allergy symptoms. 

montelukast: 

Mechanism of Action: montelukast is a leukotriene receptor antagonist. It works by blocking the action of the leukotrienes, which are inflammatory mediators involved in allergic and asthmatic reactions. Leukotrienes can cause bronchoconstriction, inflammation, and mucus production in the airways. By inhibiting the action of leukotrienes, montelukast helps prevent bronchoconstriction and reduces inflammation, making it an effective medication for asthma and allergic rhinitis. 

ambroxol: 

ambroxol is a mucolytic and expectorant agent. It typically works by thinning and loosening mucus in the respiratory tract. It does this by increasing the production of pulmonary surfactant, which helps break down the structure of mucus, making it less dense and easier to clear from the airways. ambroxol also stimulates the ciliary activity in the respiratory tract, which further aids in moving mucus out of the lungs. These actions make it worthwhile for conditions characterized by excessive mucus production, such as bronchitis and chronic obstructive pulmonary disease (COPD). 

Pharmacokinetics: 

Absorption 

levocetirizine is well-absorbed from the gastrointestinal tract after oral administration. It reaches peak blood levels within 1 to 2 hours. 

montelukast is well-absorbed from the gastrointestinal tract after oral administration and can be taken with/without food. Peak blood levels are usually reached within several hours. 

ambroxol is rapidly absorbed from the gastrointestinal tract following oral administration. Peak plasma concentrations are typically reached within 1 to 3 hours. 

Distribution 

It is distributed throughout the body, with a relatively high affinity for H1 histamine receptors in target tissues. 

It is extensively distributed throughout the body and primarily binds to proteins in the plasma. 

It is distributed widely in the body, including the lungs and respiratory tract, where it exerts its mucolytic and expectorant effects. 

Metabolism 

levocetirizine undergoes minimal metabolism in the liver, primarily by enzymatic processes, and is mainly excreted unchanged. 

montelukast is extensively metabolized in the liver by cytochrome P450 enzymes, primarily CYP2C8 and CYP3A4, forming inactive or inactive metabolites. 

ambroxol undergoes hepatic metabolism, with some metabolites having mild pharmacological activity. 

Elimination and Excretion 

Most levocetirizine is excreted unchanged in the urine, with a half-life of approximately 7 to 10 hours. 

Most montelukast and its metabolites are excreted in the bile and feces, with a terminal half-life of about 3 to 6 hours. 

The primary route of excretion is through the urine, with a half-life of around 7 to 12 hours. 

Adminstartion

Administration: 

levocetirizine: levocetirizine is typically available in tablet or syrup form. 

Tablets: Usually taken orally with a glass of water.  

Syrup: If prescribed as a syrup, measure the prescribed dose using the provided measuring device or a syringe. Shake the bottle well before use. Please take it as directed by your healthcare provider. 

montelukast: montelukast is commonly available in tablet or chewable tablet form. 

Tablets: montelukast tablets are typically taken orally with a glass of water. Your healthcare provider will typically determine the dosage and frequency.  

Chewable Tablets: These are designed to be chewed before swallowing. Follow the prescribed dosage and administration instructions. 

ambroxol: ambroxol is available in various forms, including tablets, capsules, syrups, and inhalation solutions. 

Tablets/Capsules: Swallow the tablet or capsule whole with a glass of water. Do not crush or chew unless directed by your healthcare provider. Follow the recommended dosage and frequency. 

Syrups: Measure the prescribed dose using the provided measuring device or a syringe. Shake the bottle well before use. Please take it as directed by your healthcare provider. 

Inhalation Solutions: If using ambroxol for inhalation, follow the instructions provided with the nebulizer or inhalation device. Using the correct dosage and following your healthcare provider’s guidance is essential. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: levocetirizine/montelukast/ambroxol 

Why do we use levocetirizine/montelukast/ambroxol? 

The combination of levocetirizine, montelukast, and ambroxol is used in some formulations to manage various respiratory conditions. Each component of this combination serves a specific purpose: 

levocetirizine: levocetirizine is an antihistamine primarily used to relieve allergy symptoms like runny nose, sneezing, itchy or watery eyes, and itching of the throat or nose.  

montelukast: montelukast is a leukotriene receptor antagonist typically used to treat asthma and allergic rhinitis. It helps prevent asthma symptoms and can improve symptoms of allergic rhinitis, like sneezing, runny or stuffy nose, and itching. It works by blocking the action of leukotrienes, which are inflammatory mediators that can contribute to these conditions. 

ambroxol: ambroxol is a mucolytic and expectorant drug that thins and also loosens mucus in the respiratory tract, making it more easier to cough up and clear from the airways. It is commonly used to alleviate the symptoms associated with excessive mucus production, like acute and chronic bronchitis, chronic obstructive pulmonary disease, and respiratory infections.