What is Tessalon (Benzonatate)?

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From the Guidelines

Tessalon (Benzonatate) is a peripherally acting antitussive medication.

Key Characteristics

  • It is used to control cough, particularly in patients with lung cancer or other pulmonary malignancies.
  • The medication works by acting on the peripheral nervous system, rather than the central nervous system, to suppress cough.
  • Benzonatate has been shown to be effective in controlling cough in patients with malignant pulmonary involvement, including those who are unresponsive to opioid treatment 1.

Clinical Use

  • The medication is often used when other treatments, such as opioids, have failed to provide relief from cough.
  • Benzonatate has been studied in small case series, with results showing that it can effectively control cough in up to 80% of patients with lung cancer 1.
  • While the evidence for Benzonatate is limited, it is considered a viable option for clinicians to use in an effort to relieve cough caused by lung cancer.

Important Considerations

  • The efficacy of Benzonatate may vary depending on the individual patient and the underlying cause of their cough.
  • As with any medication, Benzonatate should be used under the guidance of a healthcare professional and with careful monitoring of its effects.

From the FDA Drug Label

DESCRIPTION Benzonatate, a non-narcotic oral antitussive agent, is 2,5,8,11,14,17,20,23,26-nonaoxaoctacosan-28-yl p(butylamino) benzoate; with a molecular weight of 603.7. Each soft gelatin capsule, for oral administration, contains 200 mg benzonatate USP.

Tessalon (Benzonatate) is a non-narcotic oral antitussive agent used for oral administration, with each soft gelatin capsule containing 200 mg benzonatate USP 2.

From the Research

What is Tessalon (Benzonatate)?

Tessalon, also known as Benzonatate, is a peripherally acting oral antitussive used to relieve cough symptoms. It is one of the most widely prescribed nonnarcotic antitussives 3, 4, 5.

Mechanism of Action

The mechanism of action of Benzonatate is thought to be anesthesia of vagal sensory nerve fibers that mediate cough, by inhibiting voltage-gated sodium channels, specifically the Nav1.7 subtype 6.

Properties and Metabolism

Benzonatate undergoes rapid ester hydrolysis producing 4-(butylamino) benzoic acid (BBA) and methylated polyethylene glycol (MPG) metabolites, which are eliminated in urine and feces 7.

Safety and Efficacy

Benzonatate has been demonstrated to be effective and safe in recommended daily dose for cough, with a relatively high efficacy and safety profile 3. However, ingestion of Benzonatate may pose a risk to patients due to the potential for rapid development of life-threatening adverse events, such as cardiac arrest, and limited treatment options in the overdose setting 4, 5.

Genotoxicity

Studies have shown that Benzonatate and its major metabolite BBA are not mutagenic and do not cause numerical or structural chromosome alterations 7.

Important Considerations

Rational prescribing and patient education are needed to minimize the risks associated with Benzonatate overdose 4, 5. The selection of antitussives for prescription should take into account the patient's current medications, previous antitussive use, the availability of routes of administration, any history of drug abuse, and the presence of other symptoms 3.

References

Guideline

Guideline Directed Topic Overview

Dr.Oracle Medical Advisory Board & Editors, 2025

Research

Important drugs for cough in advanced cancer.

Supportive care in cancer : official journal of the Multinational Association of Supportive Care in Cancer, 2001

Research

Cardiac Arrest Due to Benzonatate Overdose.

The American journal of case reports, 2019

Research

Genotoxicity assessment of the novel antitussive agent Benzonatate and its major metabolite.

Mutation research. Genetic toxicology and environmental mutagenesis, 2018

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.

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