Difflam/Difflam Solution/Difflam-C/Difflam Forte

Difflam/Difflam Solution/Difflam-C/Difflam Forte

benzydamine

Manufacturer:

iNova

Distributor:

Metro Drug
Full Prescribing Info
Contents
Difflam Mint/Difflam Solution/Difflam Forte: Benzydamine hydrochloride.
Difflam/Difflam Eucalyptus & Menthol/Difflam Orange: Benzydamine hydrochloride, cetylpyridinium chloride.
Difflam-C: Benzydamine hydrochloride, chlorhexidine gluconate.
Description
Difflam Solution contains benzydamine HCl 0.15% w/v.
Each spray of Difflam Forte delivers approximately 0.51 mg of benzydamine HCl. It also contains the following ingredients: Ethanol, saccharin sodium and methylhydroxybenzoate. Difflam Forte does not contain gluten, lactose, sugar or coloring agents.
Difflam Orange/Difflam Eucalyptus & Menthol contains benzydamine HCl 3 mg and cetylpyridinium chloride 1.33 mg.
Each 15-mL solution of Difflam-C contains benzydamine HCl 22.5 mg (0.15% w/v) and chlorhexidine gluconate 18 mg (0.12% w/v).
Benzydamine is 1-benzyl-3-(3-dimethylaminopropoxy)-1H-indazole. Benzydamine HCl is a white, odorless, crystalline powder with a bitter taste, soluble in water, ethanol, methanol and chloroform. It is sparingly soluble in ether and petroleum ether.
Cetylpyridinium chloride is 1-hexadecylpyridinium chloride monohydrate. It is a white unctuous powder with a slight characteristic odor, very soluble in alcohol and chloroform and very slightly soluble in ether.
Chlorhexidine is 1,1-hexamethylenebis[5-(4-chlorophenyl)biguanide].
Action
Pharmacology: Benzydamine is an anti-inflammatory and analgesic agent structurally unrelated to the steroid group. Benzydamine differs chemically from other nonsteroidal 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 edema due to inflammatory conditions. It also inhibits granuloma formation. At concentrations used for topical treatment, benzydamine possesses local anesthetic action. It does not cause erosion of the gastric mucosa when given orally to rats at doses of up to 100 mg/kg.
The analgesic activity of benzydamine was more pronounced in models involving an experimental inflammation rather than in noninflammatory pain. As with the aspirin-like drugs, benzydamine possesses an antipyretic activity. Peripheral reflexes were transiently inhibited after IV administration to cats.
Isomalt is a sugar substitute. It is a disaccharide alcohol and is approximately equimolar mixture of glucose-mannitol and glucose-sorbitol. Isomalt produces no measurable changes in blood glucose levels.
Chlorhexidine is a bisbiguanide antiseptic that 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 characterized 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.
Pharmacodynamics: The mechanism of anti-inflammatory action of benzydamine is not related to stimulation of the pituitary-adrenal axis. Like other nonsteroidal anti-inflammatory agents, benzydamine inhibits the biosynthesis of prostaglandins under certain conditions, but its properties in this respect have not been fully elucidated. The stabilizing effect on cellular membranes may also be involved in the mechanism of action.
Following normal topical application of Difflam-C, chlorhexidine produces an immediate bactericidal effect, followed by a prolonged bacteriostatic action. Chlorhexidine is active against a wide range of microorganisms including gram-positive and gram-negative bacteria, yeast, some fungi and viruses. Chlorhexidine appears to delay bacterial growth by a 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 benzydamine HCl solution and spray, benzydamine is well-absorbed into the inflamed oral mucosa where it exerts anti-inflammatory and local anesthetic actions. Plasma benzydamine levels following use of benzydamine orally are low and parallel to the amount actually ingested.
Chlorhexidine gluconate is poorly absorbed from the gastrointestinal tract (GIT). 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 hrs. Repeated administration for 7 days did not result in accumulation of benzydamine in plasma.
Approximately 30% of the applied chlorhexidine gluconate is retained in the oral cavity and it is slowly released into the oral fluids for up to 24 hrs. Chlorhexidine is poorly absorbed from the GIT and is primarily excreted in the feces.
Indications/Uses
Temporary relief of painful conditions of the oral cavity including: Tonsillitis, sore throat, pharyngitis, mouth ulcers eg, aphthous ulcer, radiation mucositis, post-orosurgical and periodontal procedures, swelling, redness and inflammatory conditions.
Chlorhexidine in Difflam-C helps reduce the development of plaque and gingivitis during the period of treatment when the usual oral hygiene measures are interrupted.
Dosage/Direction for Use
Lozenges: 1 lozenge slowly sucked every 1-2 hrs as required up to a maximum of 12 lozenge/day. Uninterrupted treatment should not exceed 7 days.
Solution: Adults: 15 mL (approximately 1 tbsp) which should be gargled for at least 30 sec at 1½- to 3-hr intervals, as needed.
Rinse for Oral Lesions: 15 mL (approximately 1 tbsp) which should be held in the mouth and swirled for at least 30 sec, with repeat use every 1½-3 hrs throughout the day.
Alternative to Usual Oral Hygiene Procedures: Swirled around the mouth for at least 1 min.
Children 6-12 years: 5-15 mL as a gargle if able to do so, or as an oral rinse.
Uninterrupted treatment should not exceed 7 days.
Spray: Adults and Children >12 years: 2-4 sprays (1-2 mg) directly onto the sore/inflamed area and swallow gently. Repeat every 1½-3 hrs as necessary.
Children 6-12 years: 2 sprays (1 mg) directly onto the sore/inflamed area and swallow gently. Repeat every 1½-3 hrs as necessary.
Uninterrupted treatment should not exceed 7 days, unless under medical supervision.
Administration: Lozenges: Lozenges should not be chewed and should be slowly dissolved in the mouth.
Solution: Difflam solution is indicated for use as a rinse or gargle. It should not be swallowed but rather should be expectorated after each use.
Difflam Solution should generally be used undiluted, but if stinging occurs, it may be diluted with water. The solution should be expelled from the mouth after use.
Difflam-C is best used after brushing the teeth to minimize chlorhexidine-induced discoloration.
Overdosage
There are no known cases of overdosage with Difflam lozenges and throat spray. Adverse central nervous system (CNS) effects have been reported following overdosage with high doses of Difflam solution. Difflam is unlikely to cause adverse systemic effects, even if accidental ingestion should occur.
There is no specific antidote for benzydamine and should excessive quantities be ingested, the treatment should be symptomatic. Excess consumption of products containing isomalt may have a laxative effect.
Contraindications
Patients with known hypersensitivity to benzydamine HCl, cetylpyridinium chloride, chlorhexidine gluconate or to any of the components of Difflam.
Special Precautions
If a sore throat is either caused or complicated by a bacterial infection, appropriate antibacterial therapy should be considered in addition to the use of Difflam.
The clinical efficacy of an antibacterial agent in lozenges and an antiseptic agent in oral solutions in reducing the severity or duration of throat infections have not been clinically established.
Difflam Solution contains methylhydroxybenzoate as a preservative. This has been known to cause sensitization. Hypersensitivity reactions due to Difflam Solution or any of its components may occur in susceptible individuals.
Excess consumption of products containing isomalt may have a laxative effect.
Difflam-C is not intended for prolonged use except under dental or medical supervision.
Patients with Renal Impairment: Since absorbed benzydamine and its metabolites are excreted in the urine, the possibility of systemic effects should be considered in patients with severe renal impairment.
Patients with Hepatic Impairment: Since absorbed benzydamine is highly metabolized in the liver, the possibility of systemic effects should be considered in patients with severe hepatic impairment.
Use in pregnancy: Category B2. Studies in animals are inadequate or may be lacking, but available data showed no evidence of an increased occurrence of fetal damage. The safety of benzydamine HCl has not been established in pregnant patients. Risk to benefit ratio should be established if Difflam is to be used in these patients.
Use in children: Because of the lack of sufficient clinical experience, Difflam is not recommended in children <6 years.
Adverse Reactions
Difflam is generally well-tolerated and adverse effects are minor. The following adverse reactions have been reported after use of benzydamine HCl in solution form:
Local Adverse Reactions: The most commonly reported reaction is oral numbness (2.6%). Occasional burning or stinging sensation may occur and has been reported in 1.4% of treated cases. Other local adverse effects were less common and included dryness or thirst (0.2%), tingling (0.2%), warm feeling in mouth and altered sense of taste (<0.1%).
Systemic Adverse Reactions: These were very uncommon and never of a serious nature. They consisted mainly of nausea, vomiting, retching, gastrointestinal disorders (0.4%), dizziness (0.1%), headache and drowsiness (<0.1%).
Hypersensitivity reactions occur very rarely, but may be associated with pruritus, rash, urticaria, photodermatitis and occasionally, laryngospasm and bronchospasm.
The most common adverse reactions associated with chlorhexidine gluconate oral rinses are increased staining of teeth and other oral surfaces, increase in calculus formation and alteration in taste perception. Chlorhexidine tooth staining is harmless and can be minimized by thorough brushing of teeth before administration. No serious systemic adverse reactions associated with its use have been observed in clinical testing.
Drug Interactions
There are no known drug interactions with benzydamine.
Caution For Usage
Cleaning Instructions: Spray: After use, wipe the nozzle with a clean tissue to prevent blockage.
Storage
Lozenges: Store at temperatures not exceeding 30°C.
Solution: Store below 30°C. Protect from light. Shelf-Life: 3 years.
Spray: Store at temperatures not exceeding 25°C. Protect from light. Shelf-Life: 4 years.
MIMS Class
Preparations for Oral Ulceration & Inflammation
ATC Classification
A01AD02 - benzydamine ; Belongs to the class of other agents for local oral treatment.
R02AX - Other throat preparations ; Used in throat preparations.
R02AA - Antiseptics ; Used in throat preparations.
Presentation/Packing
Difflam Mint: Loz 3 mg (mint-fresh flavor) x 2's, 8's, 160's.
Difflam: Loz (honey & lemon flavor) 2's, 4's, 8's. (raspberry flavor) 2's, 4's, 8's. (strawberry flavor) 2's, 8's.
Difflam Eucalyptus & Menthol: Loz (eucalyptus and menthol flavor) 8's, 16's.
Difflam Orange: Loz (orange flavor) 8's, 16's.
Difflam Solution: Soln 1.5 mg/mL (clear, green, pleasant-tasting) x 100 mL, 200 mL, 500 mL.
Difflam-C: Soln (clear, pink, pleasant-tasting) 100 mL, 200 mL, 500 mL.
Difflam Forte: Throat spray 3 mg/mL (clear soln) x 15 mL.
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