Benzonatate | Uses, Dosage, Interactions & Side effects

Benzonatate belongs to the class of drugs called antitussives. It is a non-narcotic medication used to relieve cough. This article covers all the aspects about it.

What is Benzonatate?

Benzonatate is the ester that results from the formal condensation of 4-butylaminobenzoic acid and nonaethylene glycol monomethyl ether. It is similar to procaine and benzocaine in terms of its structural make-up. It is a non-narcotic cough medicine belonging to the class of medications called antitussives, which basically are the cough suppressants that help in relieving the cough reflex.

The FDA approved benzonatate in 1958 under the trade name Tessalon Perles. It was made available as a prescription medicine for the treatment of cough in individuals over the age of 10. At present, It is the only non-opioid antitussive available by prescription.

Chemical Structure & Properties

Chemical Structure of Benzonatate

PRODUCT SPECIFICATIONS
Name of Product Benzonatate
IUPAC Name 2-[2-[2-[2-[2-[2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl 4-(butylamino)benzoate
Synonyms Benzononatine; Tessalon; Benzononantin; Exangit; Ventussin; Benzonatato; Benzonatatum; Zonatuss
CAS No 104-31-4
Molecular Formula C30H53NO11
Molecular Weight 603.7 g/mol
Appearance (Form) Liquid
Appearance (Color) Colorless to faintly yellow oil
Solubility Soluble in most organic solvents except aliphatic hydrocarbons
LogP 2.45
Pubchem CID 7699
Pubchem SID 470087777

Uses

Uses of Benzonatate

Benzonatate is a medication that is prescribed to patients suffering from severe coughing that is brought on by a variety of respiratory conditions or infections. These conditions include bronchitis, asthma, pneumonia, pneumothorax, opiate-resistant cough in lung cancer, emphysema and the infectious common cold.

The usage of benzonatate in the treatment of hiccups has been demonstrated to be effective.

Because benzonatate is a local anaesthetic, the liquid that is contained within the capsule can be placed in the mouth to numb the oropharynx in preparation for awake intubation.

How does Benzonatate work as cough suppressant?

Benzonatate shares the chemistry and pharmacology of other local anaesthetic, such as tetracaine and procaine. It is a potent voltage-gated sodium channel inhibitor. After being absorbed and circulating to the respiratory tract, benzonatate acts as a local anaesthetic by reducing the sensitivity of vagal afferent fibres and stretch receptors in the bronchi, alveoli, and pleura in the lower airway and lung. This inhibits their activity and diminishes the cough reflex.

In addition, benzonatate possesses central antitussive activity, which makes it effective in treating coughs. It does this by blocking the transmission of impulses that are sent to the vagal nuclei of the medulla during the cough reflex. However, there is minimal inhibition of the respiratory center at a therapeutic dosage.

Benzonatate and COVID

The infection by SARS-CoV-2 virus in Coronavirus disease (COVID-19) is accompanied by chronic cough. According to an article published on GoodRx, the use of benzonatate has been shown to be beneficial in reducing coughing in a number of the patients. Owing to its sedative action, it numbs the throat and helps reduce the reflex to cough.

Dosage and Route of Administration

Though the medicine comes in oral capsule form that you take by mouth in the whole content, but it not to be break, chewed, sucked or cut. The quantity depends on the age, treatment condition, other ongoing medical conditions, reaction with the first dose, etc. It comes in 100mg, 150mg and 200mg strength.

  • For adults: It is prescribed as 100-200 mg three times a day which means a maximum of 600mg per day.
  • For children: The age group of 11-17 years is prescribed the same maximum of 600mg per day.
  • For children (under the age of 10): It is not recommended for children below the age group of 10 years, due to the side effects.

Overdosage

According to reports, the margin of safety for using benzonatate seems to be rather low, despite the fact that it has a long history of usage that has always been safe and suitable. In approximately 15 to 20 minutes, benzonatate overdose symptoms can be identified.

If capsules are chewed or dissolved in the mouth, fast oropharyngeal anesthesia will develop, which may lead to choking and airway obstruction. Restlessness, tremors, seizures, trembling or shaking of the hands or feet, abnormal heart rhythms (cardiac arrhythmia), cerebral edema, absent breathing (apnea), and tachycardia are the observed symptoms of benzonatate overdosage. Coma and cardiac arrest leading to death can also occur in severe cases. Children are at an increased risk for toxicity.

The treatment focuses on gastric content removal and symptoms management.

Interactions

There is a possibility that benzonatate will react negatively with other pharmaceuticals or dietary supplements.

If you take benzonatate with other medicines that cause drowsiness, the impact may become even more pronounced. Thus, before taking any opioid medication, sleeping pills, muscle relaxants, or medication for anxiety or seizures, make sure to consult with your primary care physician.

Certain drugs like Ambenonium, Aprotinin, Betaine, Capsaicin, Chlorpromazine, Cinchocaine and Cisplatin may increase the neuromuscular blocking activities of Benzonatate when taken together.

Other medications, such as those available both with and without a doctor’s prescription, as well as vitamins and herbal supplements, may also have an adverse reaction when combined with benzonatate. Therefore, your doctor should be aware of all the other medications you are taking.

Side effects

The following are some of the common benzonatate side effects-

  • Headache, drowsiness, dizziness
  • Nausea, upset stomach, constipation
  • Itching, rash
  • Stuffy nose
  • Feeling chilly
  • Irritation in the eyes

Some serious side effects that may be associated with the use of Benzonatate are as follows-

  • Tightening of the throat, a choking feeling
  • Difficulty breathing or swallowing
  • Numbness of the chest
  • Hallucinations
  • Rash or hives
  • Heart and blood vessel problems

Individuals may experience additional adverse effects not listed. Consult your physician for advice regarding side effects.

Precautions/Warnings

  • People who are allergic to benzonatate should avoid this medicine
  • Chewing of the medicine is not allowed as it can numb the throat and may cause serious side effects
  • Choking, chest pain or numbness, confusion, etc. are serious side effects
  • Strictly prohibited for children younger than 10 years, it can prove to be fatal
  • Medicine can also cause visual hallucinations if taken with other medicines
  • It is not good for the women who are breastfeeding as it may pass to the child

FAQs

Q. Is Benzonatate a steroid?

Benzonatate is a non-narcotic drug that is used to reduce coughing. It works by numbing the throat and the lungs, which makes the cough reflex less active.

Q. Is Benzonatate an antibiotic?

Benzonatate is an antitussive drug (cough suppressants).

Q. What drugs should not be taken with Benzonatate?

There is a possibility that benzonatate will interact negatively with other medicines, such as those used to treat coughs and colds, antihistamines, anti-seizure drugs, medicines intended to treat sleep disorders or anxiety, muscle relaxants, opioids, or psychiatric medications. Benzonatate may interact with Sudafed, Mucinex, Robitussin, Ibuprofen, Guaifensin, etc.

Q. Does Benzonatate make you sleepy?

With the use of Benzonatate, drowsiness and vertigo may occur.

Q. Can you take Benzonatate with Nyquil?

There is no evidence that NyQuil and benzonatate interact negatively with one another. However, because both medications have the potential to produce drowsiness, you should exercise extreme caution if you use them in combination.

Q. How long does Benzonatate stay in your system?

One pill of benzonatate helps in relieving coughing for three to eight hours. The half-life, or the time required for half of the drug to be eliminated from the body, is around one hour.

Q. Is Benzonatate a controlled substance?

Benzonatate is not a controlled substance.

Q. Can I take Benzonatate with Mucinex?

Both benzonatate and Mucinex treat cough, but in very different ways. Mucinex is an expectorant, which means that it works by loosening mucus and making it easier to cough up, whereas benzonatate is an anti-tussive drug, which means that it works by suppressing cough. For this reason, a doctor may prescribe a combination of the two medications.

Q. Can you take a Dayquil with Benzonatate?

There has been no interaction found between Dayquil and Benzonatate but both are cough medicine.

Q. Can you take Benzonatate while pregnant?

Benzonatate is a pregnancy category C medication. Animal studies indicate that the medication has harmful effects on the foetus when administered to pregnant mothers. Insufficient human research have been conducted to determine with certainty how the medicine may impact the foetus in humans.

Q. Can you take Benzonatate with Robitussin?

Robitussin is a cough medicine containing the active ingredient Dextromethorphan. There are no discovered interactions between benzonatate and dextromethorphan, however, one should consult their physician before using benzonatate and robitussin together.

Q. Is Benzonatate over the counter?

Benzonatate is not a medicine available over the counter. This medication is accessible only with a prescription from a physician.

Q. Can I take Ibuprofen with Benzonatate?

There are no observed interactions between Ibuprofen and benzonatate. However, this does not always imply that there are no interactions. Consult your healthcare provider at all times.

Disclaimer-

The information provided here is based on general knowledge, articles, research publications etc. and we do not claim the authenticity of any of the information provided above. We do not claim or suggest/advise any medical, therapeutic, health or nutritional benefits of Benzonatate. We do not supply or promote our Benzonatate product for the applications which are covered by valid patents and which are not approved by the FDA.

Macsen Labs is a manufacturer and supplier of high-quality Benzonatate.

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