Usage
Acebrophylline + Montelukast is prescribed for the treatment and prevention of respiratory conditions such as:
- Asthma: A chronic inflammatory disease of the airways characterized by variable and recurring symptoms, reversible airflow obstruction, and bronchospasm. This combination medication helps prevent asthma attacks, including exercise-induced bronchospasm.
- Chronic Obstructive Pulmonary Disease (COPD): A group of progressive lung diseases characterized by airflow limitation. This combination may help manage symptoms like coughing, wheezing, and shortness of breath.
- Allergic Rhinitis: Inflammation of the nasal mucosa due to exposure to allergens, commonly known as hay fever. This combination helps alleviate symptoms such as sneezing, runny nose, and nasal congestion.
- Bronchitis: Inflammation of the bronchial tubes. This combination can help in reducing inflammation and mucus production, thereby improving breathing.
- Emphysema: A lung condition that causes shortness of breath. While not a primary treatment, it can be used in combination with other medications.
Pharmacological Classification:
- Acebrophylline: Bronchodilator, Mucolytic, Anti-inflammatory agent
- Montelukast: Leukotriene Receptor Antagonist
Mechanism of Action:
Acebrophylline acts as a bronchodilator, relaxing the muscles in the airways to widen them. It also possesses anti-inflammatory and mucolytic properties, reducing inflammation and thinning mucus, which aids in easier breathing. Montelukast blocks the action of leukotrienes, substances released by the body during an allergic reaction that cause inflammation and bronchoconstriction. The combination addresses both bronchodilation and the underlying inflammatory component of these respiratory conditions.
Alternate Names
This fixed-dose combination generally does not have alternate generic names. It is often referred to by its constituent drugs. However, international or regional variations may exist.
Brand Names: Several brands are available. Please refer to the local pharmaceutical market for specific brand names used in India.
How It Works
Pharmacodynamics:
Acebrophylline relaxes bronchial smooth muscles, widening the airways. It inhibits phosphodiesterase, leading to increased intracellular cyclic AMP, which contributes to bronchodilation. It also exerts anti-inflammatory effects and reduces mucus viscosity, facilitating expectoration. Montelukast selectively blocks the CysLT1 receptor, preventing leukotriene D4 from binding and triggering inflammatory responses and bronchoconstriction.
Pharmacokinetics:
- Absorption: Both drugs are orally absorbed. Acebrophylline sustained-release formulations provide prolonged action. Montelukast absorption is not affected by food.
- Metabolism: Acebrophylline is metabolized in the liver. Montelukast undergoes hepatic metabolism primarily through CYP3A4 and CYP2C9 enzymes.
- Elimination: Both drugs are primarily eliminated through hepatic routes. Acebrophylline metabolites are excreted in urine. Montelukast is excreted primarily in bile.
Receptor Binding/Enzyme Inhibition:
- Acebrophylline: Inhibits phosphodiesterase.
- Montelukast: CysLT1 receptor antagonist.
Elimination Pathways:
- Acebrophylline: Hepatic metabolism, renal excretion of metabolites.
- Montelukast: Hepatic metabolism, biliary excretion.
Dosage
Standard Dosage
Adults: One tablet of Acebrophylline 200 mg + Montelukast 10 mg once daily, usually in the evening.
Children: Dosage varies based on age and weight. It is essential to consult a pediatrician for appropriate dosage.
- 6 months to 5 years: Montelukast 4 mg once daily (granules or chewable tablet for children over 2 years).
- 6 to 14 years: Montelukast 5 mg chewable tablet once daily.
- 15 years and older: Adult dose (Acebrophylline 200 mg + Montelukast 10 mg) once daily.
Special Cases:
- Elderly Patients: Dosage adjustment may be necessary depending on renal and hepatic function.
- Patients with Renal Impairment: Dosage adjustment may be required based on creatinine clearance.
- Patients with Hepatic Dysfunction: Use with caution and monitor liver function tests. Dosage adjustment may be needed.
- Patients with Comorbid Conditions: Consider potential drug interactions and adjust dosage accordingly.
Clinical Use Cases
This combination is generally not used in acute situations like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations like status epilepticus or cardiac arrest. It is intended for long-term management and prevention of chronic respiratory conditions. It’s crucial to use rescue medications for acute exacerbations.
Dosage Adjustments
Adjustments should be based on patient’s response to therapy, renal/hepatic function, and co-administered medications. Regular monitoring of liver function tests is recommended.
Side Effects
Common Side Effects
- Headache
- Nausea, vomiting, diarrhea
- Abdominal pain, discomfort
- Dizziness, drowsiness
- Skin rash, itching
- Upper respiratory tract infection
- Flu-like symptoms
Rare but Serious Side Effects
- Hepatic dysfunction
- Neuropsychiatric events (agitation, aggression, anxiety, depression, hallucinations, suicidal thoughts)
- Allergic reactions (angioedema, urticaria)
- Churg-Strauss Syndrome (rare systemic vasculitis)
Long-Term Effects
Long-term use may increase the risk of neuropsychiatric effects. Regular monitoring is essential.
Adverse Drug Reactions (ADR)
Serious ADRs require immediate discontinuation of the drug and prompt medical attention.
Contraindications
- Hypersensitivity to acebrophylline, montelukast, or any component of the formulation.
- Active liver disease or unexplained persistent elevations of serum transaminases.
- Acute asthma attacks.
Drug Interactions
- CYP450 interactions: Montelukast is metabolized by CYP3A4 and CYP2C9. Concomitant use with inhibitors or inducers of these enzymes may require dosage adjustment.
- Other drug interactions: Theophylline, phenobarbital, phenytoin, rifampicin, gemfibrozil, certain antibiotics (e.g., erythromycin, ciprofloxacin), and other medications may interact with this combination. A thorough medication review is essential.
Pregnancy and Breastfeeding
Consult with a physician before using during pregnancy or breastfeeding. Use only if the potential benefits outweigh the potential risks to the fetus or neonate. Data regarding safety during pregnancy and lactation are limited.
Drug Profile Summary
- Mechanism of Action: Bronchodilation, mucolytic action, leukotriene receptor antagonism.
- Side Effects: Headache, nausea, dizziness, skin rash, neuropsychiatric events (rare).
- Contraindications: Hypersensitivity, active liver disease, acute asthma attacks.
- Drug Interactions: CYP3A4/CYP2C9 inhibitors/inducers, theophylline, certain antibiotics.
- Pregnancy & Breastfeeding: Use with caution; consult a physician.
- Dosage: Adults: 200 mg/10 mg once daily. Pediatric dosage varies.
- Monitoring Parameters: Liver function tests, pulmonary function tests, monitor for neuropsychiatric symptoms.
Popular Combinations
This combination itself is a popular combination. However, additional medications like inhaled corticosteroids may be added depending on the severity of the condition.
Precautions
- Pre-existing medical conditions, especially liver and kidney diseases, should be evaluated before starting treatment.
- Monitor for allergic reactions and neuropsychiatric symptoms.
- Patients with phenylketonuria should use the chewable tablets with caution as they may contain phenylalanine.
- Patients with a history of seizures, depression, or thyroid problems should be carefully monitored.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Acebrophylline + Montelukast?
A: Adults: One tablet of Acebrophylline 200 mg + Montelukast 10 mg once daily, usually in the evening. Pediatric dosage should be determined by a pediatrician based on age and weight.
Q2: Can this medication be used during an acute asthma attack?
A: No, this medication is not intended for the relief of acute asthma attacks. Rescue medications like short-acting beta-agonists should be used for acute exacerbations.
Q3: Are there any significant drug interactions I should be aware of?
A: Yes, montelukast can interact with certain medications metabolized by CYP3A4 and CYP2C9 enzymes. It’s crucial to inform your doctor about all other medications you are taking, including over-the-counter drugs and supplements.
Q4: What are the common side effects of this combination?
A: Common side effects include headache, gastrointestinal upset, dizziness, and skin rash.
Q5: Is it safe to use during pregnancy and breastfeeding?
A: Consult with a physician before use during pregnancy or while breastfeeding. Safety data are limited.
Q6: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember. If it is close to the time for your next dose, skip the missed dose and take your next dose at the regular time. Do not double the dose.
Q7: Can this combination be used in children?
A: Yes, but the dosage varies depending on age and weight. A pediatrician should determine the appropriate dosage for children.
Q8: How long should I take this medication?
A: Take this medication for as long as prescribed by your physician. Do not discontinue use without consulting your doctor, even if your symptoms improve.
Q9: Should this combination be taken with food?
A: It can be taken with or without food, typically in the evening. Follow your doctor’s instructions regarding timing.
Q10: Are there any specific lifestyle recommendations while taking this medication?
A: Patients should avoid triggers that worsen their respiratory condition, like allergens and irritants such as smoke. Regular exercise and deep breathing exercises can also be beneficial for lung health. It’s essential to discuss any lifestyle changes with your doctor.
