Tessalon
Description
Tessalon, 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.
C30H53NO11
Each Tessalon Perle contains:
Benzonatate, USP 100 mg
Tessalon Perles (capsules) also contain: D&C Yellow 10,
gelatin, glycerin, methylparaben and propylparaben.
Physical Description
Liquid
Color/Form
Colorless to faintly yellow oil
Solubility
Soluble in most organic solvents except aliphatic hydrocarbons
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In water, 1.23 mg/L at 25 °C (est)
Vapor Pressure
4.22X10-14 mm Hg at 25 °C (est)
Octanol/Water Partition Coefficient
2.45 (LogP)
Dissociation Constants
pKa = 3.03 (est)
Experimental Properties
Hydroxyl radical reaction rate constant = 1.49X10-10 cu
cm/molec-sec at 25 °C (est)
Weight
Average: 603.7419
Monoisotopic: 603.361861543
Chemical Formula
C30H53NO11
Uses for Tessalon
Cough
Used for symptomatic relief of cough.100 101 106 108
May be effective in suppressing cough in acute respiratory
conditions such as pneumonia, bronchitis, pertussis, and the
common cold; and in chronic diseases such as pulmonary
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emphysema, bronchial asthma, tuberculosis, and pulmonary
tumor.b
Has been shown to be more effective than codeine in reducing
the frequency of experimentally induced cough,101 and may be
effective in providing symptomatic relief in patients with
opiate-resistant cough.108
Dosage Forms
Excipient information presented when available (limited,
particularly for generics); consult specific product labeling.
[DSC] = Discontinued product
Capsule, Oral:
Tessalon Perles: 100 mg
Zonatuss: 150 mg [DSC] [contains brilliant blue fcf (fd&c blue
#1)]
Generic: 100 mg, 150 mg, 200 mg
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Pharmacodynamics
Benzonatate, a non-narcotic antitussive agent chemically
related to tetracaine and other ester-type local anesthetics, is
used to suppress cough associated with both acute and chronic
respiratory conditions. The drug acts peripherally by
anesthetizing the stretch receptors located in the respiratory
passages, lungs, and pleura through the dampening of their
activity, which reduces the cough reflex.
Mechanism of action
Benzonatate acts peripherally, anesthetizing the stretch
receptors of vagal afferent fibers in the alveoli of the lungs,
bronchi, and pleura. Since these receptors are responsible for
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mediating the cough reflex, anesthetizing these receptors result
in the inhibiton of cough production. Benzonatate also
suppresses transmission of the cough reflex at the level of the
medulla where the afferent impulse is transmitted to the motor
nerves. When applied locally, Benzonatate binds within the
intracellular portion of voltage-gated sodium channels,
decreasing the rate of membrane depolarization and increasing
the threshold for electrical excitability.
Pharmacokinetics
Tetracaine congener with antitussive properties; suppresses
cough by topical anesthetic action on the respiratory stretch
receptors
Onset of Action
Therapeutic: 15 to 20 minutes
Duration of Action
3 to 8 hours
Use: Labeled Indications
Cough: Symptomatic relief of cough
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Contraindications
Hypersensitivity to benzonatate, related compounds, or any
component of the formulation
Side effects
Benzonatate may cause side effects. Tell your doctor if any of
these symptoms are severe or do not go away:
• nausea
• constipation
• drowsiness
• headache
• dizziness
• stuffy nose
• feeling chilly
• burning in the eyes
Some side effects can be serious. If you experience any of these
symptoms, call your doctor immediately:
• rash or hives
• itching
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Administration
100mg generic benzonatate capsules
Benzonatate is sold as yellow or blue 100 mg and 200 mg
softgel capsules. Initial dose is one 100 mg perle (gelcap) by
mouth, 3 times a day. Dosage may be increased as necessary,
up to a maximum of 600 mg per day.[14]
Due to its potency and potential toxicity, the capsules must be
swallowed intact in order to allow slower release of the
medication.
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References
https://pubchem.ncbi.nlm.nih.gov/compound/Benzonatate#sec
tion=Other-Experimental-Properties
https://www.drugs.com/monograph/tessalon.html
https://www.drugs.com/ppa/benzonatate.html
https://medlineplus.gov/druginfo/meds/a682640.html
