Bisbiguanides

Chlorhexidine is a symmetrical cationic molecule that is most stable as a salt; the highly water-soluble diglu-conate is the most commonly used preparation. Because of its cationic properties, it binds strongly to hy-droxyapatite (the mineral component of tooth enamel), the organic pellicle on the tooth surface, salivary proteins, and bacteria. Much of the chlorhexidine binding in the mouth occurs on the mucous membranes, such as the alveolar and gingival mucosa, from which sites it is slowly released in active form.

Pharmacokinetics

The rate of clearance of chlorhexidine from the mouth after one mouth rinse with 10 mL of a 0.2% aqueous solution follows approximately first-order kinetics, with a half-life of 60 minutes. This means that following application of a single rinse with a 0.2% chlorhexidine solution, the concentration of the compound exceeds the minimum inhibitory concentration (MIC) for oral streptococci (5 mg/mL) for almost 5 hours. The pronounced substantivity, along with the relative susceptibility of oral streptococci, may account for the great effectiveness of chlorhexidine in inhibiting supragingival plaque formation.

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