Difflam-C Solution Mechanism of Action

Pharmacology: Benzydamine is an anti-inflammatory analgesic agent structurally unrelated to the steroid group. Benzydamine differs chemically from other non-steroidal anti-inflammatory agents in that it is a base rather than an acid. Animal models show that when administered systemically, benzydamine is effective against pain and oedema due to inflammatory conditions. It also inhibits granuloma formation. At concentrations used for topical treatment, benzydamine possesses local anaesthetic action. Benzydamine does not cause erosion of the gastric mucosa when given orally to rats at doses of up to 100mg/kg. The analgesic activity of benzydamine was more pronounced in models involving an experimental inflammation rather than in non-inflammatory pain. In common with the aspirin like drugs, benzydamine possesses an antipyretic activity. Peripheral reflexes were transiently inhibited after intravenous administration to cats. Chlorhexidine is a bisbiguanide antiseptic and helps to reduce the development of plaque and gingivitis when usual oral hygiene measures are interrupted. It is a strong base, with affinity for oral structures including hydroxyapatite of tooth enamel, pellicle of tooth surface, bacteria and salivary proteins. Chlorhexidine reduces dental plaque deposition and associated gingivitis as characterised by redness, swelling or bleeding of the gingiva. It also increases the number of days between aphthous ulcers and increases the rate of healing following periodontal surgery.
Mode of Action: The mechanism of anti-inflammatory action of benzydamine is not related to stimulation of the pituitary adrenal axis. Like other non-steroidal anti-inflammatory agents, benzydamine inhibits the biosynthesis of prostaglandins under certain conditions, but its properties in this respect have not been fully elucidated. The stabilising effect on cellular membranes may also be involved in the mechanism of action.
Following normal topical application of Difflam-C Solution chlorhexidine produces an immediate bacteriocidal effect, followed by a prolonged bacteriostatic action. Chlorhexidine is active against a wide range of micro-organisms, including Gram-positive bacteria and Gram-negative bacteria, yeast and some fungi and viruses. Chlorhexidine appears to delay bacterial growth by delayed surface action. It is attracted to and absorbed onto microbial cell walls and causes membrane leakage.
Pharmacokinetics: Absorption: Benzydamine is well absorbed following oral administration. Following topical administration of Difflam solutions and spray, benzydamine is well absorbed into the inflamed oral mucosa where it exerts anti-inflammatory and local anaesthetic actions. Plasma benzydamine levels following use of Difflam solutions are low and parallel the amount actually ingested. Chlorhexidine gluconate is poorly absorbed from the gastrointestinal tract. No detectable blood levels have been found in humans following oral use, and percutaneous absorption, if it occurs at all is insignificant.
Excretion: Benzydamine and its metabolites are excreted largely in the urine. Metabolism is largely by oxidative pathways although dealkylation can be shown.
Benzydamine has been detected in blood and urine following gargling with Difflam solutions. Most of the absorbed dose was eliminated in the first 24 hours. Repeated administration for 7 days did not result in accumulation of benzydamine in plasma.
Approximately 30% of the applied chlorhexidine gluconate is retained into the oral cavity, and it is slowly released in the oral fluids for up to 24 hours. Chlorhexidine is poorly absorbed from the gastrointestinal tract, and is primarily excreted in the faeces.