Benzonatate

Benzonatate
Clinical data
Trade namesTessalon, others
Other namesBenzononatine; Egyt-13; KM-65[1]
AHFS/Drugs.comMonograph
MedlinePlusa682640
License data
Routes of
administration		By mouth
Drug classAntitussives; Local anesthetics; Sodium channel blockers
ATC code
Legal status
Legal status
Pharmacokinetic data
Onset of action15–20 minutes[3][5]
Elimination half-life1 hour[6][unreliable medical source?]
Duration of action3–8 hours[3][5]
Identifiers
  • 2,5,8,11,14,17,20,23,26-Nonaoxaoctacosan-28-yl 4-(butylamino)benzoate
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.002.904 Edit this at Wikidata
Chemical and physical data
FormulaC30H53NO11
Molar mass603.750 g·mol−1
3D model (JSmol)
  • O=C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOC)c1ccc(NCCCC)cc1
  • InChI=1S/C30H53NO11/c1-3-4-9-31-29-7-5-28(6-8-29)30(32)42-27-26-41-25-24-40-23-22-39-21-20-38-19-18-37-17-16-36-15-14-35-13-12-34-11-10-33-2/h5-8,31H,3-4,9-27H2,1-2H3 checkY
  • Key:MAFMQEKGGFWBAB-UHFFFAOYSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Benzonatate, sold under the brand name Tessalon among others, is a medication that is used for the symptomatic relief of cough.[7][8] A 2023 systematic review found that there is inadequate evidence to support the effectiveness and safety of benzonatate for cough and highlighted rising safety concerns.[9] Benzonatate is taken by mouth.[7][5] Effects generally begin within 20 minutes and last 3 to 8 hours.[7][3]

Side effects include sleepiness, dizziness, headache, upset stomach, skin rash, hallucinations, and allergic reactions.[7] Overdosage can result in serious adverse effects including seizures, irregular heartbeat, cardiac arrest, and death.[10][11] Overdose of only a small number of capsules can be fatal.[11] Chewing or sucking on the capsule, releasing the drug into the mouth, can also lead to laryngospasm, bronchospasm, and circulatory collapse.[7] It is unclear if use in pregnancy or breastfeeding is safe.[12] Benzonatate is a local anesthetic and voltage-gated sodium channel blocker.[6][unreliable medical source?] It is theorized to work by inhibiting stretch receptors in the lungs, in turn suppressing the cough reflex in the brain.[6][unreliable medical source?][7] Benzonatate is structurally related to other local anesthetics like procaine and tetracaine.[13][6][unreliable medical source?]

Benzonatate was discovered in 1956 and was approved for medical use in the United States in 1958.[5][7] It is available as a generic medication.[10] Availability worldwide is limited, with the drug remaining marketed only in the United States and Mexico.[14][13][15] In 2022, it was the 130th most commonly prescribed medication in the United States, with more than 4 million prescriptions.[16][17]

  1. ^ Cite error: The named reference Elks2014 was invoked but never defined (see the help page).
  2. ^ "FDA-sourced list of all drugs with black box warnings (Use Download Full Results and View Query links.)". nctr-crs.fda.gov. FDA. Retrieved 22 October 2023.
  3. ^ a b c d Cite error: The named reference Tessalon label was invoked but never defined (see the help page).
  4. ^ "Benzonatate capsule". DailyMed. 3 January 2024. Retrieved 20 February 2024.
  5. ^ a b c d Cite error: The named reference Homsi2001 was invoked but never defined (see the help page).
  6. ^ a b c d "Benzonatate".
  7. ^ a b c d e f g "Benzonatate Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Retrieved 23 March 2019.
  8. ^ Becker DE (2010). "Nausea, vomiting, and hiccups: a review of mechanisms and treatment". Anesthesia Progress. 57 (4): 150–6, quiz 157. doi:10.2344/0003-3006-57.4.150. PMC 3006663. PMID 21174569.
  9. ^ Costantino RC, Leonard J, Gorman EF, Ventura D, Baltz A, Gressler LE (October 2023). "Benzonatate Safety and Effectiveness: A Systematic Review of the Literature". Annals of Pharmacotherapy. 57 (10): 1221–1236. doi:10.1177/10600280221135750. PMID 36688284. S2CID 256102939.
  10. ^ a b "Drugs for cough". The Medical Letter on Drugs and Therapeutics. 60 (1562): 206–208. December 2018. PMID 30625123.
  11. ^ a b Minhaj FS, Leonard JB (December 2021). "A description of the clinical course of severe benzonatate poisonings reported in the literature and to NPDS: A systematic review supplemented with NPDS cases". Hum Exp Toxicol. 40 (12_suppl): S39–S48. Bibcode:2021HETox..40S..39M. doi:10.1177/09603271211030560. PMID 34219543. S2CID 235735410.
  12. ^ "Benzonatate Use During Pregnancy". Drugs.com. 10 October 2019. Retrieved 20 February 2020.
  13. ^ a b Cite error: The named reference pmid18771744 was invoked but never defined (see the help page).
  14. ^ Walsh TD, Caraceni AT, Fainsinger R, Foley KM, Glare P, Goh C, et al. (2008). Palliative Medicine E-Book. Elsevier Health Sciences. p. 751. ISBN 9781437721942.
  15. ^ Cite error: The named reference SchweizerischerApotheker-Verein2000 was invoked but never defined (see the help page).
  16. ^ "The Top 300 of 2022". ClinCalc. Archived from the original on 30 August 2024. Retrieved 30 August 2024.
  17. ^ "Benzonatate Drug Usage Statistics, United States, 2013 - 2022". ClinCalc. Retrieved 30 August 2024.