title: A clinical and microbiological study on the enantiomers of delmopinol.
abstract: Objective The clinical part of this study aimed to investigate whether the racemate of delmopinol [(±)-delmopinol] is equivalent to its two enantiomers [(+)-delmopinol and (-)-delmopinol] with respect to efficiency and to determine and compare their pharmacokinetic properties. The purpose of the pre-clinical part was to elucidate possible differences in antimicrobial efficiency. Materials and methods The compounds were tested clinically in a double-blind, randomized, cross-over study comprising three treatment periods of 4 days each. The antimicrobial efficacy of the enantiomers was compared in vitro with respect to planktonic and biofilm bacteria of different species. Results No statistically significant differences in prevention of plaque formation were observed. Except for a somewhat higher systemic exposure in terms of AUC and Cmax indicated for (-)-delmopinol compared to (+)-delmopinol, the pharmacokinetic properties were similar. The most common adverse event was a transient anaesthetic feeling in the mouth. This event was reported with the same frequency for all three test solutions. The enantiomers showed similar antimicrobial effects on planktonic bacteria and their biofilms. Conclusions The enantiomers were found to be equally effective with respect to inhibition of plaque development and only minor differences were observed with respect to their pharmacokinetic properties. No differences could be observed in the adverse events reports. There is, therefore, no reason to use one of the enantiomers of delmopinol instead of the racemate. This was further supported by the antimicrobial tests. It is suggested that the combined action of cationic and neutral delmopinol is important for its effect on biofilms.
authors.affiliation: a Department of Oral Biology, Faculty of Odontology , Malmö University , Malmö , Sweden ;
authors.forename: Torgny
authors.initials: T
authors.lastname: Sjödin
authors.affiliation: b Department of Prosthodontics, Faculty of Odontology , Malmö University , Malmö , Sweden ;
authors.forename: Krister
authors.initials: K
authors.lastname: Nilner
authors.affiliation: c Active Biotech AB , Lund , Sweden ;
authors.forename: Birgitta
authors.initials: B
authors.lastname: Sparre
authors.affiliation: d Kineticon AB , Uppsala , Sweden ;
authors.forename: Catarina
authors.initials: C
authors.lastname: Bernet
authors.affiliation: e StatCons , Malmö , Sweden.
authors.forename: Mikael
authors.initials: M
authors.lastname: Åström
mesh_terms: D000293:Adolescent; D000328:Adult; D000900:Anti-Bacterial Agents / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use*; D018441:Biofilms / Q000187:drug effects; D018592:Cross-Over Studies; D003773:Dental Plaque / Q000382:microbiology / Q000517:prevention & control; D004311:Double-Blind Method; D004926:Escherichia coli / Q000187:drug effects; D005260:Female; D005891:Gingivitis / Q000517:prevention & control; D006801:Humans; D008297:Male; D008826:Microbial Sensitivity Tests; D008875:Middle Aged; D009025:Morpholines / Q000097:blood / Q000493:pharmacokinetics / Q000627:therapeutic use*; D009067:Mouthwashes / Q000493:pharmacokinetics / Q000627:therapeutic use*; D042808:Neisseria sicca / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013212:Staphylococcus epidermidis / Q000187:drug effects; D013237:Stereoisomerism; D054773:Streptococcus gordonii / Q000187:drug effects; D055815:Young Adult
chemical_list: D000900:Anti-Bacterial Agents; D009025:Morpholines; D009067:Mouthwashes; C073738:delmopinol
keywords: Antibacterial effects; biofilm; clinical effect; dental plaque; pharmacokinetics