Position of Levodropropizine in Cough Therapy

Introduction

Various antitussives with different mechanisms of action are used in cough treatment. Some are typically poorly tolerated due to their effects on the central nervous system. Therefore, attention and a detailed comparison of the safety and efficacy of established antitussives with levodropropizine, a peripherally acting antitussive that also has antiallergic effects and relieves bronchial smooth muscle spasms, are warranted. Compared to centrally acting antitussives, it shows a lower risk of sedative effects while maintaining comparable efficacy. Unlike medicinal products containing codeine, which are contraindicated in patients younger than 12 years, levodropropizine can be used by children aged 2 years and older.

Pharmacological Characteristics

Levodropropizine is a non-opioid antitussive that does not suppress respiratory functions. Medicinal products containing levodropropizine are used for symptomatic treatment of non-productive cough in adults and children. The mechanism of action is described as antitussive action by reducing the activation of vagal C-fibers. Levodropropizine also acts against bronchospasm induced by histamine, serotonin, or bradykinin. The drug is characterized by rapid absorption and distribution in the body. The maximum plasma concentration is reached 40–60 minutes after administration. Pharmacokinetic properties and bioavailability are the same for drops and syrup, and the drug is also available in tablet form. Its efficacy has been proven for coughs of various origins, such as upper and lower respiratory tract infections, tuberculosis, or non-productive coughs accompanying lung cancer.

Results of Clinical Studies

The efficacy and good tolerance of levodropropizine have been confirmed by numerous clinical studies. A meta-analysis of 7 studies involving 1178 patients showed that levodropropizine is an effective antitussive for both pediatric and adult populations and significantly reduces the intensity and frequency of coughing. Compared to centrally acting antitussives, it also reduces the number of night awakenings due to coughing. 

The results of 6 controlled double-blind studies with 174 hospitalized patients with coughs of various origins showed that levodropropizine treatment was effective in 80% of patients and was generally well tolerated. A double-blind randomized study comparing the results of treating non-productive cough in adult patients using levodropropizine and dextromethorphan in syrup form demonstrated that cough intensity decreased more rapidly with levodropropizine than with dextromethorphan. Adverse events were reported by 3.6% of patients in the levodropropizine group and 12.1% of patients taking dextromethorphan.

The efficacy and good tolerance are also confirmed by a survey conducted among doctors. Efficacy was rated as excellent or good in 93% of patients, and tolerance was excellent or good in 98% of cases.

Conclusion

The good tolerance and safety profile of levodropropizine are attributed to the absence of its effects on the central nervous system. Among the antitussives currently used, it has a unique position due to its mechanism of action and minimal adverse effects. Therefore, levodropropizine plays an important role in the treatment of coughs of various types and origins in patients of all age groups.

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Source: Birring S., de Blasio F., Dicpinigaitis P. V. et al. Antitussive therapy: a role for levodropropizine. Pulm Pharmacol Ther 2019 Jun; 56: 79−85, doi: 10.1016/j.pupt.2019.03.003.