Tessalon Perles

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Tessalon Perles

Classes

Non-Opioid Antitussives

Administration
Oral Administration Oral Solid Formulations

Swallow whole. Do not break, chew, or dissolve in the mouth as this could cause temporary anesthesia of the mouth and throat and could cause choking.

Adverse Reactions
Severe

laryngospasm / Rapid / Incidence not known
anaphylactoid reactions / Rapid / Incidence not known
bronchospasm / Rapid / Incidence not known

Moderate

constipation / Delayed / Incidence not known
dysphagia / Delayed / Incidence not known
hypotension / Rapid / Incidence not known
confusion / Early / Incidence not known
hallucinations / Early / Incidence not known

Mild

nausea / Early / Incidence not known
rash / Early / Incidence not known
pruritus / Rapid / Incidence not known
drowsiness / Early / Incidence not known
dizziness / Early / Incidence not known
headache / Early / Incidence not known
ocular irritation / Rapid / Incidence not known
chills / Rapid / Incidence not known
nasal congestion / Early / Incidence not known

Common Brand Names

Tessalon Perles, Zonatuss

Dea Class

Rx

Description

Oral nonnarcotic antitussive agent; chemically related to the ester-type local anesthetics; effective in suppressing cough particularly in cases of chronic cough resistant to opiate agonists; off-label use includes topical application to the oropharynx to obliterate the gag reflex prior to intubation or endoscopy.

Dosage And Indications
For the symptomatic treatment of cough. Oral dosage Adults, Adolescents and Children 10 years and older

100 mg, 150 mg, or 200 mg PO 3 times daily is the normal dosage. Maximum dosage is 600 mg/day PO.

For the treatment of intractable singultus (hiccups)† unresponsive to standard therapies. Oral dosage Adults, Adolescents and Children 10 years and older

Anecdotal reports suggest a dosage of 100 mg PO as a single dose. May repeat in 4 hours if needed. Dose of 100 mg PO may be given up to every 4 hours; do not exceed 600 mg/day PO.

For topical anesthesia† of the oropharyngeal region prior to awake endotracheal intubation† or prior to endoscopy†.
NOTE: This route should only be used by health care professionals trained in anesthesia and intubation. Specialized references should be consulted for specific procedures and administration techniques. Resuscitative equipment and drugs used in the management of adverse reactions should be immediately available.
Oropharyngeal topical dosage† Adults

A dose of 200 mg applied topically to the oropharyngeal area, followed by 4% lidocaine translaryngeally has been used. This route should only be used by those trained in anesthesia and intubation. In 1 study, a shorter time period was required to obtain the loss of gag reflex in the benzonatate-treated group (i.e., roughly 1 minute) vs. the 5 to 6 minutes required in those patients receiving superior laryngeal nerve block with 1% lidocaine.

†Indicates off-label use

Dosing Considerations
Hepatic Impairment

Specific guidelines for dosage adjustments in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Renal Impairment

Specific guidelines for dosage adjustments in renal impairment are not available; it appears that no dosage adjustments are needed.

Drug Interactions

There are no drug interactions associated with Benzonatate products.

How Supplied

Benzonatate/Tessalon Perles/Zonatuss Oral Cap: 100mg, 150mg, 200mg

Maximum Dosage
Adults

600 mg/day PO.

Geriatric

600 mg/day PO.

Adolescents

600 mg/day PO.

Children

10 years and older: 600 mg/day PO.
9 years and younger: Safety and efficacy have not been established.

Infants

Safety and efficacy have not been established.

Neonates

Safety and efficacy have not been established.

Mechanism Of Action

Benzonatate acts peripherally by anesthetizing the stretch receptors of vagal afferent fibers located in the alveoli of the lungs, the bronchi, and the pleura. The drug may also act centrally by inhibiting the transmission of the cough reflex at the level of the medulla where the vagal afferent impulse is transmitted to the motor nerves. In patients with asthma, intravenously administered benzonatate increased minute ventilation, rate and depth of respiration. However, overall lung volume and expiratory flow rate were not altered. At recommended oral dosages, benzonatate has no inhibitory effect on the respiratory center; however, in overdosage, the pharmacology of benzonatate resembles that of other ester-type local anesthetics. Clinical effects include initial CNS stimulation, which is followed by CNS depression and respiratory compromise.
 
When applied locally, as in the oropharynx prior to intubation or endoscopy, benzonatate acts like other local anesthetics. The drug blocks the generation and conduction of nerve impulses at the level of the cell membrane. Local anesthetics bind directly within the intracellular portion of voltage-gated sodium channels. This decreases the rate of membrane depolarization, thereby increasing the threshold for electrical excitability. The blockade affects all nerve fibers in the following sequence: autonomic, sensory, and motor, with effects diminishing in reverse order. Loss of nerve function clinically is as follows: pain, temperature, touch, proprioception, and skeletal muscle tone. Direct nerve membrane penetration is necessary for effective anesthesia, which is achieved by applying benzonatate around the nerve trunks or ganglia supplying the area to be anesthetized. Benzonatate provides anesthesia in roughly 1—2 minutes after direct topical application to the oropharynx, noticeable clinically as the loss of the gag reflex.

Pharmacokinetics

Benzonatate is usually administered orally. The onset of action is 15 to 20 minutes, and antitussive effects last for approximately 3—8 hours. It is assumed that benzonatate, like other ester-type local anesthetics, is hydrolyzed to para-aminobenzoic acid (PABA) by plasma esterases. However, the absorption, distribution, metabolism and excretion of benzonatate are not well characterized.

Pregnancy And Lactation
Pregnancy

Animal reproduction studies have not been performed with benzonatate. Benzonatate is chemically related to anesthetic agents of the para-amino-benzoic acid class (e.g. procaine; tetracaine). It is not known whether benzonatate can cause fetal harm when administered during pregnancy or if the drug can affect reproduction capacity. Due to the lack of studies on safety of use during pregnancy, benzonatate should be given to a pregnant individual only if clearly needed.

It is not known if benzonatate is excreted in human milk, and caution is recommended if the drug is used during breast-feeding. The effects of benzonatate on a nursing infant are unknown. An alternate antitussive may be preferred, especially while nursing a newborn or premature infant. Despite the lack of published data, some experts consider dextromethorphan to be compatible with breast-feeding when usual adult doses are taken by the mother.