Benzyuanine

Uses

Benzyuanine Hydrochloride mouthwash is used to treat many painful conditions affecting the throat or mouth including: Sore throat, Sore tongue or gums, Mouth ulcers, Discomfort caused by dentures, Pain after dental surgery etc.

Benzyuanine is also used to associated treatment for these conditions: Acute Sore Throat, Gingivitis, Inflammation of Mouth, Laryngitis, Mouth irritation, Mucositis of the oro-pharyngeal, Orofacial Pain, Pain, Pharyngitis, Sore gums, Throat irritation, Traumatic Injuries caused by Dental Prosthesis, Gum irritation, Oral Hygiene, Tooth Extractions, Oral antisepsis

How Benzyuanine works

Despite being categorized as a non-steroidal anti-inflammatory drug (NSAID), benzydamine demonstrates various mechanisms of action that differ from those of traditional aspirin-like NSAIDs. In particular, benzydamine predominantly acts by inhibiting the synthesis of pro inflammatory cytokines like tumour necrosis factor-alpha (TNF-α) and interleukin-1β (IL-1β) without largely affecting other pro inflammatory cytokines (ie. such as IL-6 and IL-8) or anti-inflammatory cytokines (ie. like IL-10 or IL-1 receptor antagonist).

Moreover, benzydamine is largely a weak inhibitor of prostaglandin synthesis as it has been shown to effectively inhibit cyclooxygenase (COX) and lipoxygenase enzyme activity only at concentrations of 1mM or greater. Considering most contemporary usages of benzydamine are topical applications that are generally not well absorbed through the skin and/or non-specialized mucosae, benzydamine does not often achieve the kind of absorption or blood concentrations necessary to cause any extraneous distant systemic effects or COX inhibition, allowing it to localize its action.

Additionally, it is also hypothesized that benzydamine is capable of inhibiting the oxidative burst of neutrophils and membrane stabilization. These actions are exhibited by the substance’s ability to inhibit the release of granules from neutrophils and to stabilize lysosomes.

Furthermore, benzydamine is capable of a local anaesthetic effect that may be related to its capability for inhibiting the release of inflammatory mediators like substance P and calcitonin gene related peptide from sensory nerve endings. Since substance P is capable of causing the release of histamine from mast cells, benzydamine’s prevention of substance P release further contributes to an anti-inflammatory effect.

Benzyuanine also demonstrates a non-specific antibacterial activity against various bacterial strains that are resistant to broad-spectrum antibiotics such as ampicillin, chloramphenicol, and tetracycline at concentrations of about 3 mmol/L. Combinatorial use of benzydamine and other antibiotics like tetracycline and chloramphenicol are also synergistic against antibiotic resistant strains of Staphylococcus aureus and Pseudomonas aeruginosa.

Dosage

Benzyuanine dosage

15 ml of Benzyuanine mouthwash should be rinsed or gargled every 1.5-3 hours or as required, for 20-30 seconds. If stinging occurs, it can be diluted with an equal volume of water.

Side Effects

Benzyuanine Hydrochloride mouthwash can cause side effects, although not everybody gets them. Side effects are generally minor.

• Severe allergic reaction which may include a red and lumpy skin rash, difficulty breathing, swelling of face, mouth, lips or eyelids, unexplained high temperature (fever) and feeling faint. If the swelling affects throat and makes breathing difficult and swallowing difficult, patients should be hospitalized
• Itchy rash, sometimes with pale, raised areas of skin with red edges (urticaria).
• A feeling of numbness in mouth.
• A stinging feeling in mouth- the mouthwash may be diluted with water if you experience stinging. This should help to reduce the stinging effect.

Toxicity

A possible adverse reaction associated with the use of the mouthwash or oromucosal spray formulations of benzymadine is potential numbness and/or stinging in the mouth and/or throat .

Some possible adverse reactions that tend to be associated more with topical cream formulations of benzymadine include increased sensitivity to sunlight, and localized itching, skin rash, redness, or swelling .

The prescribing information for all formulations of benzymadine however, warn against the possibility of severe allergic reaction (anaphylaxis) associated with swelling of the throat and mouth, difficulty in swallowing, speaking, and breathing, or wheezing .

As benzydamine is a non-steroidal anti-inflammatory drug (NSAID), it is necessary to determine if a patient is allergic to NSAIDs before considering its use .

Intoxication is expected as a consequence of accidental ingestion of large quantities of benzydamine (over 300 mg ingestion). Other symptoms associated with overdose of ingested benzydamine include gastrointestinal and central nervous system symptoms like nausea, vomiting, abdominal pain, oesophageal irritation, dizziness, hallucinations, agitation, anxiety, and irritability .

The official prescribing information for benzydamine generally suggest that benzydamine mouthwashes and sprays should not be used in pregnancy . Similarly, the official prescribing information for benzydamine also generally suggest that benzydamine mouthwashes and sprays should not be used during lactation unless considered essential by a physician .

The prescribing information for topical cream formulations of benzydamine note that benzydamine cream should not be used in pregnancy or lactation unless considered necessary by the physician .

Overall, non-clinical data reveal no special hazards for humans based on conventional studies of safety pharmacology, repeated toxicity, genotoxicity, cardiogenic potential, and toxicity to reproduction . Additionally, there is no evidence of teratogenic effects in animal studies .

Food Interaction

Volume of Distribution

The volume of distribution of benzydamine is 10 L .

Elimination Route

Oral doses of benzydamine are well absorbed and plasma drug concentrations reach a peak fairly rapidly and then decline with a half-life of approximately 13 hours. When applied topically, although the local drug concentrations are relatively large, the systemic absorption of topically applied benzydamine is relatively low compared to oral doses. This low topical absorption contributes to a decreased potential for any systemic drug side-effects when benzydamine is administered in this way.

Half Life

Approximately 13 h after oral administration , with a terminal half life of about 7.7 h .

Clearance

Benzyuanine demonstrateas a systemic clearance of 170 ml/min .

Elimination Route

The relatively high lipid solubility of the weak base benzydamine is thought to be associated with considerable passive resorption within the renal tubule, which suggests that only approximately 5% of benzydamine is excreted unchanged in the urine . At the same time however, other studies have suggested that considerably larger amounts (50-65%) of the drug is excreted unchanged in urine .

While several inactive oxidized metabolites of benzydamine are excreted in urine, the benzydamine N-oxide metabolite can remain in plasma and demonstrate a half-life that is longer than the parent benzydamine compound .

Nevertheless, it is generally believed that excretion occurs mainly through urine and is mostly in the form of inactive metabolites or conjugation products .

Pregnancy & Breastfeeding use

The safety of Benzyuanine has not been established in pregnant patients. Risk to benefit ratio should be established if this drug is to be used in these patients.

Contraindication

Patients allergic (hypersensitive) to Benzyuanine or other component of mouthwash should not use the preparation. Contact with eye should be avoided. If accidentally get into eyes, they should be immediately washed with cold water.

Storage Condition

Keep away from light, store in cool and dry place under 30º C. Keep out of reach of children.

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