Drug Interactions of Ascoril LS Syrup
Ascoril LS syrup, containing levosalbutamol (a beta-2 agonist bronchodilator), has several clinically significant drug interactions that require careful monitoring, particularly with beta-blockers, diuretics, digoxin, MAO inhibitors, and tricyclic antidepressants. 1
Critical Contraindications and High-Risk Interactions
Beta-Blockers
- Beta-adrenergic blocking agents are contraindicated in asthmatic patients taking levosalbutamol as they not only block the pulmonary effects but may produce severe bronchospasm 1
- If beta-blockers are absolutely necessary (e.g., post-myocardial infarction prophylaxis), only cardioselective beta-blockers should be considered and administered with extreme caution 1
MAO Inhibitors and Tricyclic Antidepressants
- Levosalbutamol must be administered with extreme caution in patients taking MAO inhibitors or tricyclic antidepressants, or within 2 weeks of discontinuing these agents 1
- The vascular effects of levosalbutamol may be significantly potentiated through these interactions 1
- Consider alternative bronchodilator therapy in patients requiring these psychiatric medications 1
Cardiovascular Drug Interactions
Digoxin
- Levosalbutamol can decrease serum digoxin levels by 16-22% based on studies with racemic albuterol 1
- Carefully evaluate and monitor serum digoxin levels in patients receiving chronic digoxin therapy when initiating levosalbutamol 1
- Dose adjustments of digoxin may be necessary to maintain therapeutic levels 1
Diuretics (Non-Potassium-Sparing)
- Loop and thiazide diuretics can cause ECG changes and hypokalemia that are acutely worsened by beta-agonists, especially when recommended doses are exceeded 1
- Monitor potassium levels regularly when co-administering levosalbutamol with non-potassium-sparing diuretics 1
- The clinical significance increases when beta-agonist doses exceed recommendations 1
Other Bronchodilator Interactions
Short-Acting Sympathomimetics
- Avoid concomitant use of other short-acting sympathomimetic bronchodilators or epinephrine with levosalbutamol 1
- If additional adrenergic drugs must be administered by any route, use with extreme caution to avoid deleterious cardiovascular effects 1
- This includes over-the-counter decongestants and cold preparations containing sympathomimetics 1
Metabolic and Pharmacokinetic Considerations
Metabolism Profile
- Levosalbutamol is metabolized almost exclusively by sulphotransferase (SULT) 1A3 to inactive metabolites 2
- The R-enantiomer (levosalbutamol) is metabolized up to 12 times faster than the S-enantiomer 2
- Genetic polymorphisms in SULT1A3 and beta-2 adrenoceptors can affect drug disposition and response, explaining interindividual variations in pharmacokinetic-pharmacodynamic relationships 2
Cardiovascular Effects Monitoring
- Mean heart rate increases of 0.8-10.9 bpm have been documented 30 minutes after dosing in pediatric patients 1
- Heart rate typically returns to baseline within 60 minutes and shows no significant elevation after 21 days of treatment 1
- In COPD patients with concurrent coronary heart disease, heart rate increased from 64.4 to 72.7 beats/min at 20 minutes but returned to baseline by 60 minutes, with no cumulative effect after 7 days 3
Common Pitfalls and Clinical Caveats
- Do not assume all beta-agonists are interchangeable: Levosalbutamol has distinct pharmacokinetic properties compared to racemic salbutamol 2, 4
- Avoid overlooking over-the-counter medications: Many cold preparations contain sympathomimetics that can interact 1
- Monitor for cumulative effects: While acute heart rate changes resolve quickly, patients with cardiovascular disease require closer monitoring 3
- Consider timing of gastric pH: Approximately 6% of levosalbutamol undergoes acid-catalyzed racemization in the stomach, though this is generally not clinically significant 2
Special Population Considerations
Patients with Cardiovascular Disease
- In patients with COPD concurrent with coronary heart disease, levosalbutamol demonstrated no sustained negative cardiovascular effects over 7 days of treatment 3
- However, initial heart rate monitoring is essential, particularly in the first hour after administration 3