Benzydamine

Benzydamine is a non-steroidal anti-inflammatory drug (NSAID) with local anesthetic and analgesic properties, primarily used topically or as an oromucosal formulation to relieve inflammation and pain in the mouth, throat, vagina, and musculoskeletal tissues. It is structurally related to indazole derivatives and is known for minimal systemic absorption, making it favorable for localized inflammatory conditions.

---

Brand Names

Benzydamine is marketed under various brand names internationally. Some of the most recognized include:

• Tantum Verde (mouth/throat sprays, lozenges)

• Difflam (lozenges, oral rinse, throat spray, topical cream/gel)

• Tantum Rosa (vaginal douche)

• Benzydamine Hydrochloride (generic name in many products)

• Oropivalone-Benzydamine (in combination)

Available in the form of:

• Mouthwash (0.15%)

• Throat spray (0.15%)

• Lozenges (3 mg)

• Topical cream or gel (3% or 5%)

• Vaginal douche powder sachets (0.5 g)

---

Mechanism of Action

Benzydamine exerts its effects through multiple mechanisms:

1. Anti-inflammatory Action:

• Inhibits pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6.

• Unlike classical NSAIDs, it does not significantly inhibit cyclooxygenase (COX-1 or COX-2) at therapeutic doses.

2. Local Anesthetic Action:

• Stabilizes neuronal membranes and inhibits sodium channels, producing a mild numbing effect.

3. Antimicrobial Activity:

• Exhibits bacteriostatic and fungistatic properties, particularly effective against Candida albicans, Streptococcus, and Staphylococcus species.

---

Therapeutic Uses

Benzydamine is indicated for symptomatic relief in a range of local inflammatory conditions:

Oromucosal Uses:

• Pharyngitis and tonsillitis (infective or viral)

• Mucositis (especially chemotherapy- or radiotherapy-induced)

• Post-dental surgery inflammation

• Stomatitis, gingivitis, aphthous ulcers

• Sore throat associated with cold/flu

• Laryngeal irritation (e.g. in vocal overuse or intubation)

Topical Uses:

• Musculoskeletal pain: Sprains, strains, contusions

• Soft tissue trauma

• Tendinitis, bursitis, periarthritis

Gynecological Uses:

• Inflammatory vaginal conditions (e.g. vaginitis, vulvovaginitis)

• Postpartum vulvoperineal inflammation

• Post-episiotomy recovery

• Vaginal hygiene (e.g., in elderly, diabetics)

---

Dosage and Administration

Oral Rinse (0.15%):

• 15 mL undiluted rinse, gargled or swished in mouth, every 1.5–3 hours.

• Spit out after 30 seconds; do not swallow.

Throat Spray (0.15%):

• 4–8 puffs every 1.5–3 hours, depending on severity and age.

• Each puff delivers approximately 0.255 mg benzydamine hydrochloride.

Lozenges (3 mg):

• 1 lozenge, slowly dissolved in the mouth every 2–3 hours.

• Max: 8 lozenges/day (adults).

Topical Cream/Gel (3–5%):

• Apply 2–4 times daily on affected area.

• Gently massaged into the skin until absorbed.

Vaginal Douche (0.5 g powder):

• Dissolve sachet in 500 mL lukewarm water.

• Use 1–2 times daily.

---

Contraindications

• Known hypersensitivity to benzydamine or any formulation excipients.

• Children <6 years for certain forms (e.g., spray or lozenge) due to choking risk.

• Avoid vaginal douche in presence of active pelvic infection unless prescribed.

---

Precautions

• Avoid long-term or repeated use without medical advice.

• Caution in patients with bronchial asthma or NSAID hypersensitivity.

• Not for systemic infections—should not replace antibiotics when needed.

• Avoid contact with eyes; rinse with water immediately if it occurs.

---

Side Effects

Local (common):

• Mouth or throat numbness

• Tingling or burning sensation

• Dry mouth

• Oral mucosa irritation

• Sore tongue or altered taste

Allergic Reactions (rare):

• Rash, pruritus

• Anaphylactic reactions, angioedema

• Bronchospasm, especially in asthmatics

Systemic (very rare):

• Hallucinations, agitation, insomnia (mainly with overuse or accidental ingestion)

• Gastrointestinal upset if swallowed in large quantities

---

Drug Interactions

Benzydamine has minimal systemic absorption; clinically significant drug interactions are rare. However:

• NSAIDs or aspirin: Additive risk of allergy in sensitive individuals.

• Oral antiseptics: Simultaneous use may alter oral flora; space applications if both are required.

• No notable interactions with antibiotics, antifungals, or local anesthetics.

---

Use in Special Populations

Pregnancy:

• Category B (varies by country): Animal studies show no harm, but limited human data.

• Use only if clearly needed, especially with vaginal use or long-term oral use.

Lactation:

• Unknown if excreted in breast milk.

• Avoid swallowing; minimal systemic exposure when used correctly.

Children:

• Safe for use in children ≥6 years for most oromucosal forms.

• Always supervise younger children with sprays or lozenges to prevent choking.

---

Pharmacokinetics

• Absorption: Minimal with topical and oromucosal use; designed for local action.

• Distribution: High local tissue concentration at site of application.

• Metabolism: Rapid hepatic metabolism if swallowed.

• Elimination: Renal excretion of metabolites.

---

Storage and Stability

• Store below 25°C, protected from heat and direct sunlight.

• Do not freeze sprays or rinses.

• Lozenges should be kept in original blister packaging to protect from moisture.

---

Patient Counseling Information

• Use exactly as directed; do not swallow oral rinse or spray.

• Spit out after gargling; avoid eating or drinking for 15–30 minutes post-application.

• For vaginal use: Use freshly prepared solution; discard unused portion.

• Do not use on open wounds or ulcerated skin unless advised.

• Stop use and consult a doctor if:

  • Symptoms worsen or persist beyond 7 days

  • Signs of hypersensitivity appear

• Keep all products out of reach of children, especially lozenges.

---

Clinical Evidence and Efficacy

Oral Mucositis (Oncology patients):

• Proven efficacy in reducing pain and severity of radiation- or chemotherapy-induced mucositis.

• Recommended in MASCC/ISOO guidelines as a palliative intervention.

Sore Throat & Upper Respiratory Tract Infections:

• Effective in symptomatic relief of sore throat, hoarseness, and odynophagia.

• Faster relief compared to placebo in RCTs.

Postoperative Oral/Dental Surgery:

• Reduces pain, swelling, and trismus post-extraction or other oral procedures.

Vaginal Use:

• Demonstrated efficacy in relieving burning, itching, and discharge in inflammatory vulvovaginitis.

• Often used as adjunctive care with antimicrobials.

---

Comparative Considerations

Benzydamine	Chlorhexidine	Lidocaine (topical)
NSAID + anesthetic	Antiseptic only	Anesthetic only
Anti-inflammatory + pain relief	Broad-spectrum antibacterial	Rapid local numbing
Good for mucositis, sore throat	Used for gingivitis, surgical rinse	Good for oral ulcers, hemorrhoids
Minimal systemic absorption	May cause tooth staining	Shorter duration of action

Regulatory Status

• Available OTC in many countries (EU, Australia, MENA).

• Prescription-only in some formulations or markets.

• Not FDA-approved in the US as of 2025; however, available internationally under multiple brands