Benzydamine Hydrochloride

Approved Indications:

• Oropharyngeal Inflammation: Treatment of pain and inflammation associated with sore throat, tonsillitis, pharyngitis, laryngitis, gingivitis, stomatitis, aphthous ulcers, and post-dental procedures.
• Postoperative Oral Care: Used after oral surgeries such as tonsillectomy, dental extraction, or periodontal surgery to reduce inflammation and discomfort.
• Radiotherapy-induced Oral Mucositis: Used to relieve symptoms of oral mucositis caused by cancer treatment, especially radiotherapy.
• Musculoskeletal Disorders (Topical): Relief of localized pain and inflammation in soft tissues (e.g., sprains, strains, contusions).

Off-Label or Clinically Accepted Uses:

• Prevention of Oral Mucositis in Chemotherapy: In some clinical settings, Benzydamine mouthwash is used prophylactically to prevent mucositis during chemotherapy.

Adults and Elderly:

• Mouthwash (0.15%): Rinse or gargle with 15 ml (undiluted) every 1.5 to 3 hours as needed. Spit out after use; do not swallow.
• Spray (0.15%): 4 to 8 puffs to the affected area every 1.5 to 3 hours.
• Topical Cream/Gel (3%): Apply 2–4 times daily to the affected area with light massaging. Do not apply on open wounds.

Pediatric:

• Children ≥6 years: Mouthwash 15 ml diluted 1:1 with water. Gargle or rinse every 3 hours. Must be used under adult supervision.
• Children <6 years: Not recommended due to risk of swallowing.

Special Populations:

• Renal/Hepatic Impairment: No specific dose adjustment needed; minimal systemic absorption.
• Route of Administration: Oral mucosal (rinse/gargle/spray), topical cutaneous.

Benzydamine hydrochloride is a non-steroidal anti-inflammatory drug (NSAID) with distinct local anesthetic and analgesic properties. It inhibits pro-inflammatory cytokines and stabilizes cell membranes by reducing the production of prostaglandins and thromboxanes through partial inhibition of cyclooxygenase (COX). Additionally, it inhibits TNF-alpha and IL-1β without systemic immunosuppression. It also has local anesthetic effects by modulating sodium channels in nerve fibers, leading to a reduction in pain sensation at the site of application.

• Absorption: Minimal systemic absorption when applied topically or as a rinse. However, it is absorbed through the mucosa in small amounts.
• Distribution: Localized at the site of application; low plasma levels detected.
• Metabolism: Metabolized mainly in the liver via hydroxylation and conjugation.
• Elimination: Primarily excreted via the kidneys in urine, mostly as metabolites.
• Half-life: Approximately 13 hours after systemic administration (rarely relevant in topical/oral mucosal use).
• Bioavailability: Low when used topically or orally; therapeutic effects are primarily local.

• Pregnancy: Not classified by the FDA into a formal category. Available data suggest minimal systemic absorption and low risk, but use should be limited to situations where clearly needed.
• Lactation: Not known to be excreted in human milk. Due to low systemic absorption, the risk to a breastfeeding infant is low. Use with caution and avoid direct contact with the breast area.
• General Advice: Avoid prolonged or high-dose use during pregnancy and lactation due to limited human data.

• Primary Class: Non-steroidal Anti-inflammatory Drug (NSAID)
• Sub-class: Topical/oral NSAID with local anesthetic properties

• Known hypersensitivity to Benzydamine or any excipients in the formulation
• Patients with a history of allergic reactions to other NSAIDs
• Application to open wounds or ulcerated skin in topical formulations

• Allergic Reactions: May cause local allergic reactions including contact dermatitis, especially in prolonged use.
• Systemic Absorption: Minimal, but caution in patients with severe renal impairment.
• Pediatric Use: Supervision required to avoid swallowing.
• Asthma Patients: Rare risk of bronchospasm; use with caution.
• Long-term Use: Not recommended for extended durations unless under medical supervision.
• Monitoring: Clinical monitoring for irritation, allergic reactions, or signs of superinfection is advised.

Common (≥1%):

• Oral burning or stinging sensation
• Dry mouth
• Numbness or tingling at the site of application
• Local irritation or redness (topical)

Uncommon to Rare (<1%):

• Rash, pruritus
• Photosensitivity (topical)
• Hypersensitivity reactions (urticaria, angioedema)
• Anaphylactic reaction (extremely rare)

Severe (very rare):

• Bronchospasm
• Severe allergic reaction

Onset is typically within minutes to hours of application; side effects are usually dose-dependent and reversible upon discontinuation.

• Topical/Local Formulation: Clinically significant interactions are unlikely due to limited systemic absorption.
• No Known Major CYP450 Interactions: Not metabolized via cytochrome P450 enzymes.
• Concurrent Use of Other Oral Antiseptics or NSAIDs: May increase local irritation or enhance sensitivity; caution advised.
• Alcohol-Based Mouthwashes: Avoid concurrent use to prevent excessive mucosal dryness or irritation.

• Supportive Use in Oncology (2023): Recognized in several oncology supportive care guidelines for prophylaxis and management of radiotherapy-induced oral mucositis.
• Pediatric Dosing Cautions (2022): Updated recommendations emphasize strict supervision in children under 12 years due to risk of accidental ingestion.
• EMA Safety Review (2021): Reaffirmed safety in topical and oral mucosal use when applied correctly and not ingested.

• Oral Rinse/Spray: Store below 25°C. Do not refrigerate or freeze. Protect from direct sunlight. Keep container tightly closed.
• Topical Gel/Cream: Store at room temperature (15°C to 30°C). Avoid high humidity. Do not apply to broken skin.
• Shelf-life: Typically 24 to 36 months depending on formulation; refer to manufacturer labeling.
• Handling: Shake oral rinse bottle gently before use. Do not dilute unless directed.