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 Difflam
anti-inflammatory lozenges
COMPOSITION
Actives: Benzydamine hydrochloride 3 mg
Inactive: Isomalt, saccharin sodium
DESCRIPTION
Benzydamine is 1-Benzyl-3-(3-dimethyl-aminopropoxy)-1H-indazole. Benzydamine
hydrochloride is a white, odourless, crystalline powder with a bitter taste,
soluble in water, ethanol, methanol and chloroform. It is sparingly soluble
in ether and petroleum ether.
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
100 mg/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.
Isomalt is a sugar-substitute. It is a dissaccharide alcohol and is an
approximately equimolar mixture of glucose-mannitol and glucose-sorbitol.
Isomalt produces no measurable changes in blood glucose levels.
Pharmacodynamics
The mechanism of anti-inflammatory action 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 stabilising effect on cellular membranes may also be
involved in the mechanism of action.
Absorption
Benzydamine is well absorbed following oral administration. Following
topical administration of benzydamine hydrochloride in solution form,
benzydamine is well absorbed into the inflamed oral mucosa where it exerts
anti-inflammatory and local anaesthetic actions. Plasma benzydamine levels
following use of benzydamine orally are low and parallel the amount actually
ingested.
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.
INDICATIONS
For the temporary relief of painful conditions of the oral cavity including
tonsillitis, sore throat, radiation mucositis, aphthous ulcers, post-orosurgical
and periodontal procedures, pharyngitis, swelling, redness and inflammatory
conditions.
CONTRAINDICATIONS
Patients with known hypersensitivity to benzydamine or to any of the
components of the vehicle.
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 Anti-inflammatory Lozenges. For use in patients with hepatic
or renal impairment see Dosage and Administration section.
Excess consumption of products containing isomalt may have a laxative
effect.
Use in Pregnancy
Studies in animals are inadequate or may be lacking, but available data show
no evidence of an increased occurrence
of foetal damage. The safety of benzydamine hydrochloride has not been
established in pregnant patients. Risk to benefit ratio should be
established if Difflam Anti-inflammatory Lozenges are to be used in these
patients.
Use in Children
Because of the lack of sufficient clinical experience, Difflam
Antiinflammatory Lozenges are not recommended in children under 6 years of
age.
Drug Interactions
There are no known drug interactions with benzydamine.
ADVERSE REACTIONS
Difflam in topical oral preparations is generally well tolerated and
side-effects are minor. The following adverse reactions have been reported
after use of benzydamine hydrochloride 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,
gastro-intestinal disorders (0.4%), dizziness (0.1%), headache and
drowsiness (<0.1%).
Hypersensitivity reactions occur very rarely but may be associated with
pruritis, rash, urticaria, photodermatitis and occasionally laryngospasm or
bronchospasm.
DOSAGE AND ADMINISTRATION
Difflam Anti, inflammatory Lozenges should not be chewed. They should be
slowly dissolved in the mouth. One lozenge should be sucked slowly every one
to two hours as required up to a maximum of 12 lozenges per day.
Uninterrupted treatment should not exceed seven days.
With Impaired Renal Function
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.
With Impaired Liver Function
Since absorbed benzydamine is highly metabolised in the liver the
possibility of systemic effects should be considered in patients with severe
hepatic impairment.
OVERDOSAGE
There are no known cases of overdosage with Difflam Anti-inflammatory
Lozenges. Adverse CNS effects have been reported following overdosage with
high doses of benzydamine hydrochloride in solution form. 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.
PRESENTATION
Mint Fresh Flavour lozenges (green) blister pack,16's.
STORAGE
Store below 30°C.
SHELF LIFE
3 Years |
