Chemical formula: C₂₁H₄₅N₃ Molecular mass: 339.602 g/mol PubChem compound: 3607
Hexetidine is a broad spectrum antimicrobial. It is active both in vivo and in vitro, against gram positive and negative bacterium, as well as yeasts (Candida albicans) and fungi.
It competes with vitamin B1 (thiamine), a substance essential for microbial growth. Its high affinity for proteins and polymers containing electronegative sites (peptidoglycans) can explain the association of hexetid with microbes and can at least to some extent associate its effect with its accumulation in specific regions. This chemical affinity also explains its association with dental plaque and dental plaque action.
The rapid action of hexetidine has been demonstrated in vitro and in vivo, and this is of particular importance for this formulation where the contact time with the microorganism is short-term.
Hexetidine also has healing, haemostatic and local anesthetic properties in the mouth and throat.
Hexetidine specifically inhibits enzyme systems, especially succinyl-dehydrogenase. It has also been shown that, at least with respect to E. coli, its inhibition of growth induced by hexetidine is somewhat inhibited by the addition of thiamine to the culture; whereas, in Bacillus cereus spores, hexetidine inhibits the oxidation of pyruvate, is also inhibited by thiamine. The antagonistic activity of thiamine may explain the antagonism of hexetidin-coenzyme A.
Additionally, zinc has been shown to inhibit the effect of hexetidine on the bisphosphorydyl nucleotide, while copper enhances this activity. These data support the view that its mechanism of action is also the connection with metal ions.
Specific pharmacokinetic studies for hexetidine have not been conducted in humans.
Retention of hexetidine has been observed in the mouth, mucous membrane and dental plaque.
In studies using radiolabeled hexetidine, retention in oral tissues has been shown to last from 8 to 10 hours after a single mouthwash and in some cases hexetidine has been detected in oral tissue over 65 hours after recovery.
No specific studies of hepestin have been performed with respect to liver failure.
No special studies of hexetidine have been performed in the elderly.
Based on the studies on acute, subchronic and chronic toxicity in various animal species, preclinical data show no particular risk for hexetidine for humans if used in accordance with the instructions.
Hexetine did not cause a significant increase in mutation when studied in vitro using the Ames test.
No specific studies of hexetidine have been performed.
No teratogenic effects were observed in white New Zealand white rabbits receiving 5, 10 and 20 mg of hepizidin/kg/day from the 6th to the 18th day of pregnancy.
A small number of these died as a result of the toxic side effects of hexetidine, but no other clinical symptom or change in behavior was observed during the study.
Hexetine was considered to be embryotoxic as evidenced by a small number of abortions. A significant increase in the number of losses on resorption and after implantation was observed in a group receiving 10 and 20 mg hexetidine/kg/day and a significant decrease in fetal weight in a group receiving 20 mg/kg/day.
Hexetine was orally given to New Zealand white rabbits after mating for reproduction and showed no apparent fertility side effect with respect to the control group.
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