Benzyuanine

Benzyuanine Uses, Dosage, Side Effects, Food Interaction and all others data.

Each ml mouthwash contains 1.5 mg Benzyuanine Hydrochloride (w/v)Benzyuanine Hydrochloride mouthwash is a Non-Steroidal Anti-Inflammatory Drug (NSAID) with analgesic and local anesthetic properties. The clinical pharmacology of Benzyuanine mouthwash is well known. Benzyuanine is poorly absorbed in the blood, thereby limiting systemic exposure to the drug when applied topically but ensures high concentration at the site of injury in mouth or throat. Therefore, it provides excellent oropharyngeal pain relief with minimal side effects. Although Benzyuanine is a Non-Steroidal Anti-Inflammatory agent, it possesses a different mechanism of action that distinguishes it from conventional NSAIDs. Benzyuanine mouthwash shows analgesic & anti-inflammatory action by inhibiting pro-inflammatory cytokines & reducing vascular permeability. Moreover, Benzyuanine mouthwash shows local anesthetic property which provides an immediate effect on pain.

Benzyuanine is a non-steroidal anti-inflammatory drug (NSAID) designed to elicit local anesthetic and analgesic effects mainly for the mouth and throat. It specifically acts on the local mechanisms of inflammation such as pain, oedema, or granuloma. Typically applied topically, the drug demonstrates anti-inflammatory activity reducing oedema as well as exudate and granuloma formation. Moreover, benzydamine exhibits analgesic properties and local anaesthetic activity if pain is caused by an inflammatory condition. Benzyuanine can be absorbed into the oral mucosa and intact skin. Once absorbed in the local area of pain or inflammation, benzydamine binds selectively to local inflamed tissues, usually allowing it to act with few adverse systemic effects. On average a period of 2 to 4 hours is necessary for the substance to reach peak plasma concentration.

Benzyuanine can be synthesized with the reaction of the N-benzyl derivative from methyl anthranilate with nitrous acid to give N-nitoso derivative. This is next reduced by sodium thiosulfate to give transient hydrazine. This hydrazine can then undergo spontaneous internal hydrazide formation. Treating this resultant enolate with 3-chloro-1-dimethylamkino propane ultimately yields benzydamine.

Trade Name Benzyuanine
Generic Benzydamine
Benzydamine Other Names Bencidamina, Benzydamine, Benzydaminum
Type
Formula C19H23N3O
Weight Average: 309.413
Monoisotopic: 309.184112373
Protein binding

Benzydamine exhibits < 20% plasma protein binding after oral administration .

Groups Approved
Therapeutic Class Topical anti-inflammatory preparations
Manufacturer
Available Country Taiwan
Last Updated: September 19, 2023 at 7:00 am
Benzyuanine
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

No interactions found.

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.

Innovators Monograph

You find simplified version here Benzyuanine

Benzyuanine contains Benzydamine see full prescribing information from innovator Benzyuanine Monograph, Benzyuanine MSDS, Benzyuanine FDA label

*** Taking medicines without doctor's advice can cause long-term problems.
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