Benzoxonium Chloride (2.5mg/5ml) + Lidocaine (2.5mg/5ml)

Clinical Pharmacologist's Monograph

⚠️ Prescription Only: This medicine is Schedule H/H1. Do not self-medicate.

1. Clinical Overview

A topical oral solution combining the antiseptic and disinfectant properties of Benzoxonium Chloride with the local anesthetic action of Lidocaine. Primarily used for symptomatic relief of pain and inflammation associated with various oropharyngeal conditions. Benzoxonium Chloride is a quaternary ammonium compound effective against a broad spectrum of Gram-positive and Gram-negative bacteria, fungi, and some viruses. Lidocaine provides rapid-onset, short-duration anesthesia of the mucous membranes.

OnsetDurationBioavailability
Lidocaine: 2-5 minutes; Benzoxonium Chloride: Antimicrobial action begins immediately upon contact.Lidocaine: 30-60 minutes; Benzoxonium Chloride: Residual antiseptic effect may last for several hours.Topical (oral mucosal): Lidocaine systemic absorption is low and variable (<10%). Benzoxonium Chloride is minimally absorbed from intact oral mucosa.

2. Mechanism of Action

The combination provides dual action: Lidocaine reversibly blocks voltage-gated sodium channels in neuronal membranes, inhibiting the initiation and conduction of nerve impulses, leading to local anesthesia. Benzoxonium Chloride disrupts microbial cell membranes through its cationic surfactant properties, leading to leakage of cytoplasmic constituents and cell death.

3. Indications & Uses

  • Symptomatic relief of sore throat (pharyngitis)
  • Pain relief in aphthous ulcers (canker sores)
  • Pain and discomfort due to gingivitis and stomatitis
  • Post-tonsillectomy pain management

4. Dosage & Administration

Adult Dosage: Gargle or rinse with 5-10 ml (1-2 teaspoonfuls) for about 30 seconds, 3-4 times daily, preferably after meals and at bedtime. Do not swallow.

Administration: Use undiluted. Measure the dose. Gargle thoroughly, ensuring contact with the throat, or rinse around the mouth. Spit out completely after use. Avoid eating or drinking for at least 15-30 minutes after application to allow the medicine to work. Do not use for more than 7 days without medical advice.

5. Side Effects

Common side effects may include:

  • Transient local burning or stinging sensation
  • Temporary numbness of tongue and mouth (desired effect)
  • Altered taste perception (dysgeusia)
  • Mild irritation or dryness of oral mucosa

6. Drug Interactions

DrugEffectSeverity
Other Local AnestheticsAdditive systemic toxicity risk if used concurrently on large areas.Moderate
Antiarrhythmics (e.g., Amiodarone, Mexiletine)Increased risk of cardiac adverse effects (bradycardia, arrhythmias).Moderate
CYP1A2 & CYP3A4 Inhibitors (e.g., Ciprofloxacin, Fluconazole, Erythromycin)May increase systemic Lidocaine levels, increasing toxicity risk.Moderate
Beta-blockers (e.g., Propranolol)May reduce hepatic blood flow, increasing Lidocaine levels.Moderate
SuccinylcholineBenzoxonium Chloride, as a quaternary ammonium compound, may potentiate neuromuscular blockade.Theoretical/Low

7. Patient Counselling

  • DO gargle or rinse for the full 30 seconds.
  • DO spit out the solution completely after use.
  • DO wait at least 30 minutes before eating or drinking.
  • DO use a measuring spoon for accurate dose.
  • DO NOT swallow the solution.
  • DO NOT use for more than 7 days unless directed by a doctor.
  • DO NOT use in children without proper supervision.
  • DO NOT apply to large open wounds in the mouth.

8. Toxicology & Storage

Overdose: Primarily due to Lidocaine systemic toxicity: CNS - Lightheadedness, drowsiness, tinnitus, blurred vision, tremors, convulsions, respiratory arrest. Cardiovascular - Bradycardia, hypotension, arrhythmias, cardiac arrest. Benzoxonium Chloride: Ingestion may cause GI irritation, nausea, vomiting.

Storage: Store below 30°C. Protect from light. Keep the bottle tightly closed. Keep out of reach of children. Do not freeze.