Drug Groups

approved

Description

A disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque. [PubChem]

Indication

For reduction of pocket depth in patients with adult periodontitis, used as an adjunct to scaling and root planing procedures. Also for prevention of dental caries, oropharyngeal decontamination in critically ill patients, hand hygiene in health-care personnel, general skin cleanser, and catheter site preparation and care.

Pharmacology

Chlorhexidine, a topical antimicrobial agent, is bactericidal. Because of its positive charge, the chlorhexidine molecule reacts with the microbial cell surface to destroy the integrity of the cell membrane. This novel mechanism of action makes it highly unlikely for the development of bacterial resistance.

Toxicity

LD₅₀= 2g/kg (human, oral); LD₅₀= 3 g/kg (rat, oral); LD₅₀= 2.5 g/kg (mice, oral); LD₅₀= 21 mg/kg (male rat, IV); LD₅₀= 23 mg/kg (female rat, IV); LD₅₀= 25 mg/kg (male mice, IV); LD₅₀= 24 mg/kg (female mice, IV); LD₅₀= 1g/kg (rat, subcutaneous); LD₅₀= 637 mg/kg (male mice, subcutaneous); LD₅₀= 632 mg/kg (female mice, subcutaneous)

Affected Organisms

Absorption

Absorption of chlorhexidine from the gastrointestinal tract is very poor. Additionally, an in vivo study in 18 adult patients found no detectable plasma or urine chlorhexidine concentrations following insertion of four periodontal implants under clinical conditions.

Protein Binding

87%

Elimination

Excretion of chlorhexidine gluconate occurred primarily through the feces (~90%). Less than 1% of the chlorhexidine gluconate ingested by these subjects was excreted in the urine.

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