Therapeutic Use of Levocloperastine as an Antitussive Agent

P. Aliprandi, L. Cima, M. Carrara


Clin Drug Invest. 2002;22(4) 

In This Article

Abstract and Introduction

Cough associated with acute and chronic respiratory conditions is common in patients of all ages. Levocloperastine is a novel antitussive with a pharmacological profile distinct from that of the racemic DL-cloperastine. Levocloperastine with its dual mechanism of action acts on both the central bulbar cough centre and on peripheral receptors in the tracheobronchial tree. In preclinical studies, levocloperastine demonstrated antitussive effects similar to those observed with codeine. In acute and repeated-dose toxicity studies, levocloperastine was well tolerated in rodents and dogs, with no clinically significant cardiovascular or gastrointestinal adverse events. The pharmacokinetic behaviour of levocloperastine, best described by a two-compartmental model with absorption phase, is similar to that of the racemic compound DL-cloperastine. In clinical trials, levocloperastine had a faster onset of action and produced greater reductions in the intensity and frequency of cough compared with DL-cloperastine, codeine and levodropropizine. The antitussive effects (reduction in intensity and frequency of cough) of levocloperastine were observed after the first day of treatment in patients of all ages. In children, levocloperastine reduced night-time awakenings and irritability; in adults, it was also effective in treating ACEinhibitor cough. Levocloperastine was generally well tolerated. There was no evidence of clinically significant central adverse events, whereas drowsiness, dry mouth and nausea were reported with comparator agents (levodropropizine, codeine, DL-cloperastine). Levocloperastine represents an effective alternative to currently used antitussive agents with the added advantage of faster onset of action and improved tolerability in all patient groups.

Cough, a reflex phenomenon occurring when sensitive receptors located in the larynx and upper airways are activated, is one of the most common symptoms for which patients consult primary care physicians and pneumologists.[1] Coughing serves a number of functions, including acting as an indicator of an underlying illness and as an important defence mechanism to clear the airways. If it becomes ineffective, excessive or persistent it can profoundly and adversely affect a patient's quality of life.[2] Treatment of cough depends on the function the cough is serving. When cough indicates an underlying illness, the aim of therapy is to cure such illness, but treatment should also attempt to control, prevent or eliminate cough using antitussive agents.[3]

Levocloperastine (Privituss®;1 Aesculapius Farmaceutici), the levorotatory isomer of DLcloperastine, is a centrally active, non-opioid antitussive agent with a chemical structure and pharmacological profile distinct from that of the racemate. It is devoid of central antinociceptive activities, does not cause addiction or dependence phenomena, and does not interfere with cardiovascular or gastrointestinal functions.[4,5] The therapeutic efficacy of DL-cloperastine in reducing the intensity and frequency of cough is well established, with efficacy similar to that of codeine and superior to that of dextromethorphan.[6,7,8,9] In this overview, we examine the pharmacological profile of levocloperastine and its clinical efficacy and tolerability in the treatment of cough associated with a range of respiratory conditions in patients of all ages.


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