Benzydamine

Benzydamine is an anti-inflammatory, antipyretic and analgesic agent. Benzydamine belongs to the group of non-steroidal anti-inflammatory drugs.

Indications and use

Benzydamine is used exclusively superficially (topically). It is used for pain relief and anti-inflammatory treatment of the mouth, throat and musculoskeletal system. It is used as a gargle solution, spray or in the form of lozenges for the treatment of sore throats and other inflammatory conditions of the mouth and throat. As a cream or gel, it is used for the symptomatic treatment of blunt injuries such as bruises or for the treatment of inflammatory diseases of the bursa or joints. In addition, it can be used for the symptomatic treatment of inflammation of the vaginal mucosa in the form of a vaginal solution.

Systemically, benzydamine is no longer used in Europe, as agents with much more favorable properties and a better side effect profile (e.g., ibuprofen) are preferred. In other countries, benzydamine is available in tablet and capsule form for oral administration.

History

Benzydamine was developed in the 1960s by the Italian pharmaceutical company Angelini Pharma and was first marketed in 1967.

Pharmacodynamics and mechanism of action

Although benzydamine is classified as a nonsteroidal anti-inflammatory drug (NSAID), it exhibits mechanisms of action that differ from conventional members of this group. Specifically, benzydamine primarily inhibits the synthesis of proinflammatory cytokines such as tumor necrosis factor-alpha (TNF-α) and interleukin-1β (IL-1β) without affecting other cytokines (e.g., IL-6, IL-8, or IL-10). Benzydamine is also a weak inhibitor of prostaglandin synthesis. Like other members of the NSAIDs, it inhibits the enzyme activity of cyclooxygenase (COX) and lipoxygenase. However, because most current uses involve local application of benzydamine, benzydamine often does not reach the blood concentrations needed to produce this effect. In addition, benzydamine has a local anesthetic effect that may be related to its ability to inhibit the release of inflammatory mediators such as substance P and "calcitonin gene related peptide" from sensory nerve endings. This explains the rapid pain relief after the use of benzydamine. Benzydamine also shows non-specific antibacterial activity against various bacterial strains. The combined use of benzydamine and other antibiotics may be beneficial in infections with antibiotic-resistant bacteria.

Pharmacokinetics

Orally ingested benzydamine is well absorbed, reaching high plasma concentrations relatively quickly. Benzydamine has a plasma protein binding of < 20% after oral administration and is metabolized primarily by oxidation, dealkylation, and conjugation. It is generally believed that excretion occurs primarily in the urine, and to a large extent metabolites of benzydamine are eliminated. The elimination half-life is approximately 8-10 hours.

With topical application, although local drug concentrations are high, systemic absorption of benzydamine is extremely low and usually does not reach levels required for a systemic effect. As a result, systemic side effects after topical application are extremely rare.

Interactions

Since benzydamine is applied only locally, drug-drug interactions are not expected to occur.

Side effects

Side effects depend on the site of application.

Side effects when used in the mouth and throat:

• Hypersensitivity reaction
• Nausea and vomiting
• numbness in the mouth and throat
• Dry mouth
• Burning in the area of application

In rare cases, cramping of the vocal cords (glottis) may also occur or swelling may occur.

Application on the skin as cream/gel:

No side effects have been reported to date when used on the skin.

Application on the vaginal mucosa:

In rare cases, itching or burning may occur in the area of application.

Pregnancy and lactation

With proper use, local application is possible during pregnancy and lactation.

Misuse

Benzydamine may have a noise-producing effect when taken orally in particularly high doses. In some countries, benzydamine is therefore misused as an intoxicant.