Benzonatate
Benzonatate Uses, Dosage, Side Effects, Food Interaction and all others data.
Benzonatate is an oral antitussive drug used in the relief and suppression of cough in patients older than ten years of age. Currently, benzonatate is the only non-narcotic antitussive available as a prescription drug. It works to reduce the activity of cough reflex by desensitizing the tissues of the lungs and pleura involved in the cough reflex. Benzonatate was approved by the FDA in 1958 under the market name Tessalon Perles. Because its chemical structure resembles that of the anesthetic agents in the para-amino-benzoic acid class (such as procaine and tetracaine), benzonatate exhibits anesthetic or numbing action. Although it not prone to drug misuse or abuse, benzonatate is associated with a risk for severe toxicity and overdose, especially in children.
Benzonatate suppresses cough associated with both acute and chronic respiratory conditions. Its works by desensitizing the pulmonary stretch receptors involved in the cough reflex. There are limited clinical trials of benzonatate; however, earlier studies demonstrated inhibition of experimentally-induced cough and subjectively-measured pathological cough by benzonatate.
Benzonatate has no inhibitory effects on the respiratory center in recommended dosage. Its onset of action is within 15 to 20 minutes following administration and its duration of effect is about 3 to 8 hours.
| Trade Name | Benzonatate |
| Availability | Prescription only |
| Generic | Benzonatate |
| Benzonatate Other Names | Benzonatat, Benzonatate, Benzonatato, Benzonatatum, Benzononatine |
| Related Drugs | diphenhydramine, Benadryl, guaifenesin, codeine, dextromethorphan, Mucinex |
| Type | |
| Formula | C30H53NO11 |
| Weight | Average: 603.7419 Monoisotopic: 603.361861543 |
| Protein binding | There is limited information on the protein binding profile of benzonatate. |
| Groups | Approved |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | United States |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Benzonatate is a non-narcotic oral antitussive drug used to suppress coughing.
Benzonatate is indicated for the symptomatic relief of cough.
Benzonatate is also used to associated treatment for these conditions: Cough
How Benzonatate works
Benzonatate is a local anesthetic drug that acts peripherally by anesthetizing and reducing the activity of vagal stretch receptors or nerve fibres located in the respiratory passages, lungs, and pleura. Once the stretch receptors are stimulated, they send impulses to the cough centre located in the medulla via an afferent pathway consisting of sensory nerve fibres or the vagus nerve. The efferent signal is then generated that sends impulses to the expiratory muscles to produce a cough. Anesthetizing these receptors by benzonatate results in the inhibition of the cough reflex activity and cough production. Benzonatate also inhibits the transmission of impulses of the cough reflex in the vagal nuclei of the medulla. There are several proposed mechanisms of benzonatate; it is also a potent voltage-gated sodium channel inhibitor.
Toxicity
The lowest published toxic dose (TDLo) from oral administration in man is 51 mg/kg. The oral LD50 is 400 mg/kg and the subcutaneous LD50 is 100 mg/kg in mice.
The signs and symptoms of overdose are typically observed within 15 to 20 minutes and can lead to neurological and cardiovascular toxicity, which is related to blocked sodium channels. Intentional and unintentional death from overdose may occur. The risk of overdose is highest in children and toxicity may result from the ingestion of 1 or 2 capsules in this age group. If capsules are chewed or dissolved in the mouth, oropharyngeal anesthesia will develop rapidly, which may cause choking and a compromised airway function. Symptoms arising from CNS stimulation include restlessness and tremors, which may lead to clonic convulsions followed by profound CNS depression. Within 1 hour following ingestion, convulsions, coma, cerebral edema and cardiac arrest leading to death have been reported.
Evacuation of gastric contents and administration of copious amounts of activated charcoal is advised. It is important to note that cough and gag reflexes may be significantly depressed even in conscious patients with overdose; special attention is needed to protect against aspiration of gastric contents. When intravenously administering short-acting barbiturates to treat convulsions, the dose should be carefully titrated for the smallest effective dose. Overdose should be managed with supportive care with continuous monitoring of neurologic and cardiovascular status. Intensive support of respiration and cardiovascular-renal function should be initiated for severe intoxication. Because benzonatate is structurally similar to local anesthetic agents, the use of intravenous lipid emulsion therapy in response to life-threatening cardiovascular collapse is also suggested.
Food Interaction
- Take with or without food. The absorption is unaffected by food.
Benzonatate Disease Interaction
Volume of Distribution
There is limited information on the volume of distribution of benzonatate.
Elimination Route
Following oral administration, benzonatate enters the systemic circulation via gastrointestinal absorption. The Cmax of benzonatate following oral administration of 100 mg in healthy Chinese volunteers was 1063 ± 460 ng/mL.
Half Life
The half life of benzonatate following oral administration of 100 mg in healthy Chinese volunteers was 1.01 ± 0.41 h.
Clearance
There is limited information on the clearance of benzonatate.
Elimination Route
There is limited information on the route of elimination of benzonatate.
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