What is the use of Benzonatate ( Tessalon), a cough suppressant?

From the Guidelines

Benzonatate (Tessalon) is used as a cough suppressant, specifically for the treatment of coughs associated with lung cancer that are unresponsive to other treatments.

Key Points

• Benzonatate is a peripherally acting antitussive, meaning it works locally in the lungs to suppress coughing, rather than acting on the central nervous system like opioid-based cough suppressants 1.
• It is suggested for use in adult patients with lung cancer experiencing opioid-resistant cough that does not respond to peripheral antitussives, as part of a comprehensive management approach that includes identifying and treating any co-existing causes of cough 1.
• The evidence for benzonatate's effectiveness in treating cough associated with lung cancer is based on small case series, with one study showing it effectively controlled cough in 80% of 21 patients with malignant pulmonary involvement 1.
• Benzonatate may be considered for patients with intractable cough due to lung cancer who have not responded to other treatments, including opioids, demulcents, and other pharmacological approaches 1.
• It is essential to note that the management of cough in lung cancer patients should be individualized, taking into account the patient's specific symptoms, medical history, and treatment goals, and that benzonatate should be used as part of a broader approach to managing cough and other symptoms associated with lung cancer 1.

From the FDA Drug Label

INDICATIONS AND USAGE BENZONATATE is indicated for the symptomatic relief of cough. CLINICAL PHARMACOLOGY BENZONATATE acts peripherally by anesthetizing the stretch receptors located in the respiratory passages, lungs, and pleura by dampening their activity and thereby reducing the cough reflex at its source.

The use of Benzonatate (Tessalon), a cough suppressant, is for the symptomatic relief of cough 2. It works by anesthetizing the stretch receptors in the respiratory passages, lungs, and pleura, thereby reducing the cough reflex 2.

• Key mechanism: anesthetizing stretch receptors
• Key effect: reducing cough reflex
• Onset of action: within 15 to 20 minutes
• Duration of action: 3 to 8 hours 2

From the Research

Use of Benzonatate (Tessalon) as a Cough Suppressant

• Benzonatate is an antitussive medication used to relieve cough symptoms 3, 4
• It is thought to work by anesthetizing vagal sensory nerve fibers that mediate cough, and has been shown to inhibit voltage-gated sodium channels, including Nav1.7 4
• Benzonatate has been extensively studied in the acute and chronic cough settings and has shown relatively high efficacy and safety profiles 3
• It is one of the few antitussives that have been specifically studied in cancer and advanced cancer cough, and has been shown to be effective and safe in recommended daily doses 3

Mechanism of Action

• Benzonatate's mechanism of action is thought to be related to its local anesthetic-like effects on voltage-gated sodium channels 4
• It has been shown to inhibit Nav1.7 voltage-gated sodium channels, which are highly expressed in vagal sensory neurons that mediate cough 4
• Benzonatate's inhibition of voltage-gated sodium channels is thought to be responsible for its cough suppressant effects 4

Safety and Toxicity

• Benzonatate overdose can cause life-threatening toxicity, including coma, seizures, hypotension, and cardiac arrest 5, 6, 7
• The risk of overdose is higher in children, and the US Food and Drug Administration (FDA) has issued warnings about the risks of benzonatate overdose in children under 10 years old 5, 7
• Adults can also experience severe adverse events from benzonatate overdose, including cardiac arrest and respiratory failure 6, 7