Benzonatate

Pronunciation

Class: Antitussives
ATC Class: R05DB01
VA Class: RE302
CAS Number: 104-31-4
Brands: Tessalon

Warning(s)

Special Alerts:

[Posted 12/14/2010] ISSUE: FDA is warning the public that accidental ingestion of benzonatate (Tessalon) by children under the age of 10 years can result in death from overdose. Overdose with benzonatate in children less than 2 years of age has been reported following accidental ingestion of as few as 1 or 2 capsules. Benzonatate may be attractive to children because of the drug’s appearance (it is a round-shaped liquid-filled gelatin capsule).

BACKGROUND: Benzonatate is a prescription drug approved for relief of cough in patients over 10 years of age. The safety and effectiveness of benzonatate in children under 10 years of age have not been established. Benzonatate is sold under the brand-name Tessalon and is also sold in generic preparations. Individuals who experience overdose of benzonatate may exhibit restlessness, tremors, convulsions, coma, and cardiac arrest. Signs and symptoms of overdose can occur rapidly after ingestion (within 15-20 minutes). Deaths in children have been reported within hours of the accidental ingestion.

RECOMMENDATION: Patients who are taking benzonatate should keep the medication in a child-resistant container and store it out of reach of children. If a child accidentally ingests benzonatate, seek medical attention immediately. Signs and symptoms of benzonatate overdose can occur rapidly after ingestion (within 15-20 minutes) and may include restlessness, tremors, convulsions, coma, and cardiac arrest. For more information visit the FDA website at: and .

Introduction

Local anesthetic antitussive agent.a b

Uses for Benzonatate

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

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 emphysema, bronchial asthma, tuberculosis, and pulmonary tumor.b

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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

Conscious Intubation

Has been applied locally in the oral cavity in adults by releasing the drug from the liquid-filled capsules (e.g., by chewing or dissolving two 100-mg liquid-filled capsules in the mouth) to provide sufficient oropharyngeal anesthesia for conscious intubation.107

Do not employ this method of administration when the drug is used as an antitussive because of the risk of potentially life-threatening complications resulting from local effects on the oropharyngeal tract.100 101 102 104 (See Sensitivity Reactions under Cautions and also Oral Administration under Dosage and Administration.)

Benzonatate Dosage and Administration

Administration

Oral Administration

Swallow the liquid-filled capsules whole.100 101 102

Do not chew or dissolve in the mouth when used as an antitussive, since temporary, potentially life-threatening local anesthesia of the oral mucosa, choking, or severe hypersensitivity reactions could occur; oropharyngeal anesthesia develops rapidly with such improper administration.100 101 102

Local administration (chewing the capsules or allowing to dissolve in mouth) can be employed to facilitate conscious intubation.103 107 (See Conscious Intubation under Uses.)

Dosage

Pediatric Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Cough
Oral

Children ≤10 years of age: 8 mg/kg daily in 3–6 divided doses,106 although safety and efficacy have not been established in this age group.100 (See Pediatric Use under Cautions.)

Children >10 years of age: 100 or 200 mg 3 times daily.100 101 106

Adults

Cough
Oral

100 or 200 mg 3 times daily;100 101 106 doses up to 600 mg daily may be given in divided doses if necessary.100 101 106

Prescribing Limits

Pediatric Patients

Cough
Oral

Children >10 years of age: Maximum 600 mg daily in divided doses.100 101 106

Adults

Cough
Oral

Maximum 600 mg daily in divided doses.100 101 106

Special Populations

Hepatic Impairment

No specific dosage recommendations for hepatic impairment.a b

Renal Impairment

No specific dosage recommendations for renal impairment.a b

Geriatric Patients

No specific geriatric dosage recommendations.a

Cautions for Benzonatate

Contraindications

  • Known hypersensitivity to the drug or related compounds.100

Warnings/Precautions

Sensitivity Reactions

Severe hypersensitivity reactions, including bronchospasm, laryngospasm, and cardiovascular collapse, have been reported with benzonatate.100 101 102

Such reactions may have resulted from local anesthesia secondary to sucking or chewing the liquid-filled capsules rather than swallowing them whole.100 101

Severe reactions have required medical intervention with vasopressor therapy and supportive measures.100

Major Toxicities

Overdosage

Deliberate or accidental overdosage of benzonatate can result in CNS stimulation which may lead to restlessness, tremors, and seizures; profound CNS depression and death can follow.100 103 104 105

Dizziness,104 disorientation,103 drunken feeling,104 unresponsiveness,104 pulmonary congestion,104 ventricular tachycardia,103 cardiac arrest,103 and nausea104 also have been reported with overdosage.

General Precautions

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

CNS Effects

Rarely, bizarre behavior, including mental confusion and visual hallucinations, when used concomitantly with certain other drugs.100

Possibility that adverse CNS effects associated with other p-aminobenzoic acid-derivative local anesthetics (e.g., procaine, tetracaine) could occur with benzonatate should be considered.100

Specific Populations

Pregnancy

Category C.a

Lactation

Not known whether benzonatate is distributed into milk.100 Caution if used in nursing women.100

Pediatric Use

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

Risk of overdosage and toxicity (including death) in children <2 years of age receiving OTC preparations containing antihistamines, cough suppressants, expectorants, and nasal decongestants alone or in combination for relief of symptoms of upper respiratory tract infection.109 110 Limited evidence of efficacy for these preparations in this age group; appropriate dosages not established.109 Therefore, FDA recommends not to use such preparations in children <2 years of age; safety and efficacy in older children currently under evaluation. Because children 2–3 years of age also are at increased risk of overdosage and toxicity, some manufacturers of oral nonprescription cough and cold preparations recently agreed to voluntarily revise the product labeling to state that such preparations should not be used in children <4 years of age. During the transition period, some preparations on pharmacy shelves will have the new recommendation (“do not use in children <4 years of age”), while others will have the previous recommendation (“do not use in children <2 years of age”). FDA recommends that parents and caregivers adhere to dosage instructions and warnings on the product labeling that accompanies the preparation and consult a clinician about any concerns. Clinicians should ask caregivers about use of OTC cough/cold preparations to avoid overdosage.

Common Adverse Effects

Generally well tolerated when the liquid-filled capsules are swallowed intact.100 101 106

Adverse effects may include sedation, headache, mild dizziness, bizarre behavior (e.g., mental confusion, visual hallucinations), nasal congestion, nausea, GI upset, constipation, sensation of burning in the eyes, a vague “chilly” sensation, pruritus and skin eruptions, numbness in the chest, and hypersensitivity (e.g., bronchospasm, laryngospasm, cardiovascular collapse, possibly related to local anesthesia from chewing or sucking the liquid-filled capsules).100 103 106 (See Sensitivity Reactions under Cautions.)

Benzonatate Pharmacokinetics

Absorption

Onset

Usually within 15–20 minutes after swallowing capsules intact.100 103 104 106

Oropharyngeal anesthesia: Develops rapidly when applied locally (e.g., by chewing or dissolving the liquid-filled capsules in the mouth),100 101 102 104 107 with complete anesthesia occurring within about 1 minute.107

Duration

Approximately 3–8 hours following a single oral dose.100 101 103 104 106

Stability

Storage

Oral

Liquid-filled Capsules

Tight, light-resistant containers at 15–30°C.100

Actions

  • Inhibits cough production by anesthetizing stretch receptors of vagal afferent fibers in the bronchi, alveoli, and pleura that mediate the cough reflex; also suppresses transmission of the cough reflex at the level of the medulla where the afferent impulse is transmitted to the motor nerves.b

  • Does not depress respiration at recommended dosages100 104 106 ; in patients with bronchial asthma, the drug has been reported to increase the rate and depth of respiration, minute volume, and vital capacity.b

Advice to Patients

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

  • Importance of warning patients using benzonatate as an antitussive to swallow the liquid-filled capsules whole without chewing or dissolving in the mouth because of risk of potentially life-threatening local anesthesia.b (See Oral Administration under Dosage and Administration and also Sensitivity Reactions under Cautions.)

  • Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs as well as any concomitant illnesses.

  • Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.100

  • Importance of informing patients of other important precautionary information.100 (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Pending revision, the material in this section should be considered in light of more recently available information in the MedWatch notification at the beginning of this monograph.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Benzonatate

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules, liquid-filled

100 mg*

Tessalon Perles (with parabens)

Forest

200 mg

Tessalon Capsules (with gelatin, glycerin, and parabens)

Forest

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 02/2014. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Benzonatate 100MG Capsules (ZYDUS PHARMACEUTICALS (USA)): 30/$20.99 or 60/$30.97

Benzonatate 200MG Capsules (ZYDUS PHARMACEUTICALS (USA)): 30/$33.99 or 90/$89.98

Tessalon Perles 100MG Capsules (PFIZER U.S.): 30/$49.99 or 90/$139.97

AHFS DI Essentials. © Copyright, 2004-2014, Selected Revisions January 1, 2011. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

100. Forest Pharmaceuticals. Tessalon (benzonatate) prescribing information (dated 1999 Aug). In: Physicians’ desk reference. 55th ed. Montvale, NJ: Medical Economics Company Inc; 2001:1270.

101. Food and Drug Administration. Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use; tentative final monograph for OTC antitussive drug products. Proposed rule. [21 CFR Part 341] Fed Regist. 1983; 48:48576-95. (lDIS 176844)

102. Food and Drug Administration. Cold, cough, allergy, bronchodilator, and antiasthmatic drug products for over-the-counter human use; tentative final monograph for OTC antitussive drug products. Final rule. [21 CFR Part 310,341,369] Fed Regist. 1987; 52:30042-7. (lDIS 232963)

103. Crouch BI, Knick KA, Crouch DJ et al. Benzonatate overdose associated with seizures and arrhythmias. J Toxicol Clin Toxicol. 1998; 36:713-8. [IDIS 420898] [PubMed 9865240]

104. Cohan JA, Conradi SE. Two fatalities resulting from Tessalon (benzonatate). Vet Human Toxicol. 1986; 28:543-4.

105. Sheen S, Osterhoudt K, Birenbaum D. Seizures in a toddler associated with benzonatate ingestion. J Toxicol Clin Toxicol. 1997; 35:493.

106. Anon. Benzonatate. In: Osol A, Pratt R, eds. The United States dispensatory. Philadelphia: JB Lippincott Company; 1973:187-8.

107. Mongan PD, Culling RD. Rapid oral anesthesia for awake intubation. J Clin Anesth. 1992; 4:101-5. [PubMed 1562332]

108. Doona M, Walsh D. Benzonatate for opioid-resistant cough in advanced cancer. Palliat Med. 1998; 12:55-8. [PubMed 9616460]

109. Srinivasan A, Budnitz D, Shehab N et al. Infant deaths associated with cough and cold medications—two states, 2005. MMWR Morb Mortal Wkly Rep. 2007; 56:1-4. [PubMed 17218934]

110. Food and Drug Administration. Cough and cold medications in children less than two years of age. Rockville, MD; 2007 Jan 12. From FDA website.

a. Forest Pharmaceuticals, Inc. Tessalon (benzonatate, USP) prescribing information. Schaumburg, IL: 2000 Sep.

b. AHFS drug information 2004. McEvoy GK, ed. Benzonatate. Bethesda, MD: American Society of Health-System Pharmacists; 2004:2596.

pdh. Schilling McCann JA, Publisher. Pharmacists drug handbook. 2nd ed. Philadelphia, PA: Lippincott Williams and Wilkins and American Society of Health-System Pharmacists; 2003.

HID. Trissel LA. Handbook on injectable drugs. 12th ed. Bethesda, MD: American Society of Health-System Pharmacists; 2003:175-80.

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