Usage
This combination medication is primarily prescribed for the treatment of asthma and chronic obstructive pulmonary disease (COPD) associated with allergic rhinitis. It addresses both bronchoconstriction and allergic inflammation.
Pharmacological Classification:
- Doxofylline: Bronchodilator (Xanthine derivative)
- Levocetirizine: Antihistamine (second-generation)
- Montelukast: Leukotriene receptor antagonist
Mechanism of Action: Doxofylline relaxes the airway muscles, leading to bronchodilation. Levocetirizine blocks histamine, reducing allergic symptoms. Montelukast inhibits leukotrienes, further decreasing inflammation and bronchoconstriction.
Alternate Names
While there isn’t a universally recognized alternate name for this specific combination, it may be referred to by different brand names depending on the manufacturer. Some examples of brand names available in the market for this drug include DYSMA LM and Draplin-M.
How It Works
Pharmacodynamics: Doxofylline inhibits phosphodiesterases, increasing intracellular cyclic AMP, leading to smooth muscle relaxation in the airways. Levocetirizine antagonizes the H1 histamine receptor, reducing vascular permeability and other allergic manifestations. Montelukast selectively and competitively blocks the cysteinyl leukotriene receptor CysLT1.
Pharmacokinetics: Doxofylline is well-absorbed orally. Levocetirizine is rapidly absorbed with peak plasma levels in about an hour. Montelukast is also absorbed orally and metabolized mainly by CYP3A4 and CYP2C9. All three drugs are primarily eliminated through hepatic metabolism, with doxofylline also having some renal excretion.
Receptor binding, enzyme inhibition, or neurotransmitter modulation:
- Doxofylline: Phosphodiesterase inhibition
- Levocetirizine: H1 receptor antagonism
- Montelukast: CysLT1 receptor antagonism
Elimination pathways: Primarily hepatic metabolism for all three components, with some renal excretion of doxofylline.
Dosage
Standard Dosage
Adults:
One tablet containing Doxofylline 400mg, Levocetirizine 5mg, and Montelukast 10mg once daily.
Children:
Dosage must be carefully adjusted based on age and weight.
- 2-5 years: Levocetirizine 2.5mg and Montelukast 4mg once daily.
- 6-14 years: Levocetirizine 5mg and Montelukast 5mg once daily.
- 15 years and older: Adult dose.
Special Cases:
- Elderly Patients: Dosage adjustments based on renal function are often necessary.
- Patients with Renal Impairment: Reduce the dose according to creatinine clearance. Use cautiously in severe renal impairment.
- Patients with Hepatic Dysfunction: Use cautiously. Dosage adjustments may be necessary.
- Patients with Comorbid Conditions: Assess potential interactions with medications for conditions like diabetes and cardiovascular disease.
Clinical Use Cases
This fixed-dose combination isn’t typically used in acute scenarios like intubation, surgical procedures, mechanical ventilation, ICU care, status epilepticus, or cardiac arrest. The individual components might be used independently in specific situations. Refer to specialist guidelines for acute care management.
Dosage Adjustments
Renal or hepatic impairment necessitates dosage reductions. Metabolic disorders or genetic polymorphisms influencing drug metabolism should be taken into account.
Side Effects
Common Side Effects
Nausea, vomiting, headache, diarrhea, skin rash, flu-like symptoms, insomnia, dizziness, fatigue, dry mouth, abdominal pain.
Rare but Serious Side Effects
Hepatotoxicity, neuropsychiatric events (mood swings, suicidal thoughts), severe allergic reactions (angioedema, anaphylaxis).
Long-Term Effects
Limited data exists on long-term adverse effects. Watch for new or worsening symptoms with extended use.
Adverse Drug Reactions (ADR)
Severe allergic reactions, liver dysfunction, and neuropsychiatric issues mandate immediate medical attention.
Contraindications
Hypersensitivity to any component, severe renal or hepatic impairment. Pregnancy and lactation.
Drug Interactions
May interact with xanthines (theophylline, aminophylline), H2 receptor antagonists (cimetidine, ranitidine), antibiotics (erythromycin, clarithromycin), allopurinol, phenytoin, salbutamol, and influenza vaccine. Alcohol should be avoided.
Pregnancy and Breastfeeding
Contraindicated in pregnancy and breastfeeding. Consult a doctor for safer alternatives.
Drug Profile Summary
- Mechanism of Action: Doxofylline: bronchodilator; Levocetirizine: antihistamine; Montelukast: leukotriene inhibitor.
- Side Effects: Nausea, headache, insomnia, dizziness, hepatotoxicity, neuropsychiatric events, allergic reactions.
- Contraindications: Hypersensitivity, severe renal/hepatic impairment, pregnancy, breastfeeding.
- Drug Interactions: Xanthines, H2 antagonists, antibiotics, allopurinol, phenytoin, alcohol.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: Doxofylline 400mg/Levocetirizine 5mg/Montelukast 10mg once daily. Pediatric dosages need adjustments.
- Monitoring Parameters: Pulmonary function tests, liver function tests, neuropsychiatric symptoms.
Popular Combinations
May be combined with inhaled corticosteroids for severe asthma or COPD under specialist supervision.
Precautions
Assess for allergies, renal/hepatic dysfunction. Smoking cessation advised. Caution during pregnancy, breastfeeding, and in children and the elderly. Avoid alcohol. May affect mental alertness.
FAQs
Q1: What is the recommended dosage for Doxofylline + Levocetirizine + Montelukast?
A: Adults: One tablet of Doxofylline 400mg, Levocetirizine 5mg, and Montelukast 10mg once daily. Pediatric and special populations need adjustments.
Q2: Can this combination be used in acute asthma attacks?
A: No, it’s for long-term management, not acute exacerbations.
Q3: Are there any serious side effects?
A: Yes, though rare, they can include hepatotoxicity, neuropsychiatric events, and severe allergic reactions.
Q4: What are the common side effects?
A: Nausea, headache, insomnia, dizziness, and gastrointestinal upset.
Q5: Can pregnant or breastfeeding women take this medication?
A: No, it’s contraindicated.
Q6: Does this medication interact with other drugs?
A: Yes, it can interact with several drugs, including xanthines, some antibiotics, and alcohol.
Q7: Should any specific monitoring be done during treatment?
A: Yes, monitor liver function, pulmonary function, and watch for neuropsychiatric symptoms.
Q8: What are the key precautions for this combination?
A: Evaluate for allergies, renal/hepatic function. Smoking cessation is advised. Exercise caution in pregnancy, breastfeeding, and special populations. Avoid alcohol. May impair mental alertness.
Q9: What conditions is this combination used for?
A: Asthma and COPD associated with allergic rhinitis.
