Peringatan Keamanan

The lowest published toxic dose (TDLo) from oral administration in man is 51 mg/kg. The oral LD50 is 400 mg/kg and the subcutaneous LD50 is 100 mg/kg in mice.L11196

The signs and symptoms of overdose are typically observed within 15 to 20 minutes and can lead to neurological and cardiovascular toxicity, which is related to blocked sodium channels. Intentional and unintentional death from overdose may occur. The risk of overdose is highest in children and toxicity may result from the ingestion of 1 or 2 capsules in this age group.A5790 If capsules are chewed or dissolved in the mouth, oropharyngeal anesthesia will develop rapidly, which may cause choking and a compromised airway function. Symptoms arising from CNS stimulation include restlessness and tremors, which may lead to clonic convulsions followed by profound CNS depression. Within 1 hour following ingestion, convulsions, coma, cerebral edema and cardiac arrest leading to death have been reported.L11193

Evacuation of gastric contents and administration of copious amounts of activated charcoal is advised. It is important to note that cough and gag reflexes may be significantly depressed even in conscious patients with overdose; special attention is needed to protect against aspiration of gastric contents. When intravenously administering short-acting barbiturates to treat convulsions, the dose should be carefully titrated for the smallest effective dose. Overdose should be managed with supportive care with continuous monitoring of neurologic and cardiovascular status. Intensive support of respiration and cardiovascular-renal function should be initiated for severe intoxication.L11193 Because benzonatate is structurally similar to local anesthetic agents, the use of intravenous lipid emulsion therapy in response to life-threatening cardiovascular collapse is also suggested.A5790

Benzonatate

DB00868

small molecule approved

Deskripsi

Benzonatate is an oral antitussive drug used in the relief and suppression of cough in patients older than ten years of age.A5790 Currently, benzonatate is the only non-narcotic antitussive available as a prescription drug.A189519 It works to reduce the activity of cough reflex by desensitizing the tissues of the lungs and pleura involved in the cough reflex. Benzonatate was approved by the FDA in 1958 under the market name Tessalon Perles.A5790 Because its chemical structure resembles that of the anesthetic agents in the para-amino-benzoic acid class (such as procaine and tetracaine), benzonatate exhibits anesthetic or numbing action.L11193 Although it not prone to drug misuse or abuse, benzonatate is associated with a risk for severe toxicity and overdose, especially in children.A189513

Struktur Molekul 2D

Berat 603.7419
Wujud liquid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of benzonatate following oral administration of 100 mg in healthy Chinese volunteers was 1.01 ± 0.41 h.[A190267]
Volume Distribusi There is limited information on the volume of distribution of benzonatate.
Klirens (Clearance) There is limited information on the clearance of benzonatate.

Absorpsi

Following oral administration, benzonatate enters the systemic circulation via gastrointestinal absorption.A5790 The Cmax of benzonatate following oral administration of 100 mg in healthy Chinese volunteers was 1063 ± 460 ng/mL.A190267

Metabolisme

Benzonatate is hydrolyzed to the major metabolite 4-(butylamino)benzoic acid (BABA) by plasma butyrylcholinesterase (BChE).A189519

Rute Eliminasi

There is limited information on the route of elimination of benzonatate.

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

75 Data
Pegvisomant Pegvisomant may increase the neuromuscular blocking activities of Benzonatate.
Mefloquine Mefloquine may increase the neuromuscular blocking activities of Benzonatate.
Tacrine Tacrine may increase the neuromuscular blocking activities of Benzonatate.
Sulpiride Sulpiride may increase the neuromuscular blocking activities of Benzonatate.
Profenamine Profenamine may increase the neuromuscular blocking activities of Benzonatate.
Chlorpromazine Chlorpromazine may increase the neuromuscular blocking activities of Benzonatate.
Gallamine triethiodide Gallamine triethiodide may increase the neuromuscular blocking activities of Benzonatate.
Triflupromazine Triflupromazine may increase the neuromuscular blocking activities of Benzonatate.
Cisplatin Cisplatin may increase the neuromuscular blocking activities of Benzonatate.
Cinchocaine Cinchocaine may increase the neuromuscular blocking activities of Benzonatate.
Pyridostigmine Pyridostigmine may increase the neuromuscular blocking activities of Benzonatate.
Nizatidine Nizatidine may increase the neuromuscular blocking activities of Benzonatate.
Galantamine Galantamine may increase the neuromuscular blocking activities of Benzonatate.
Isoflurophate Isoflurophate may increase the neuromuscular blocking activities of Benzonatate.
Diethylcarbamazine Diethylcarbamazine may increase the neuromuscular blocking activities of Benzonatate.
Procaine Procaine may increase the neuromuscular blocking activities of Benzonatate.
Minaprine Minaprine may increase the neuromuscular blocking activities of Benzonatate.
Donepezil Donepezil may increase the neuromuscular blocking activities of Benzonatate.
Terbutaline Terbutaline may increase the neuromuscular blocking activities of Benzonatate.
Mechlorethamine Mechlorethamine may increase the neuromuscular blocking activities of Benzonatate.
Hexafluronium Hexafluronium may increase the neuromuscular blocking activities of Benzonatate.
Demecarium Demecarium may increase the neuromuscular blocking activities of Benzonatate.
Physostigmine Physostigmine may increase the neuromuscular blocking activities of Benzonatate.
Rivastigmine Rivastigmine may increase the neuromuscular blocking activities of Benzonatate.
Edrophonium Edrophonium may increase the neuromuscular blocking activities of Benzonatate.
Procainamide Procainamide may increase the neuromuscular blocking activities of Benzonatate.
Memantine Memantine may increase the neuromuscular blocking activities of Benzonatate.
Ambenonium Ambenonium may increase the neuromuscular blocking activities of Benzonatate.
Tubocurarine Tubocurarine may increase the neuromuscular blocking activities of Benzonatate.
Ketamine Ketamine may increase the neuromuscular blocking activities of Benzonatate.
Metoclopramide Metoclopramide may increase the neuromuscular blocking activities of Benzonatate.
Decamethonium Decamethonium may increase the neuromuscular blocking activities of Benzonatate.
Pancuronium Pancuronium may increase the neuromuscular blocking activities of Benzonatate.
Pipecuronium Pipecuronium may increase the neuromuscular blocking activities of Benzonatate.
Ginkgo biloba Ginkgo biloba may increase the neuromuscular blocking activities of Benzonatate.
Neostigmine Neostigmine may increase the neuromuscular blocking activities of Benzonatate.
Bambuterol Bambuterol may increase the neuromuscular blocking activities of Benzonatate.
1,10-Phenanthroline 1,10-Phenanthroline may increase the neuromuscular blocking activities of Benzonatate.
Methylphosphinic Acid Methylphosphinic Acid may increase the neuromuscular blocking activities of Benzonatate.
Thiotepa Thiotepa may increase the neuromuscular blocking activities of Benzonatate.
Huperzine A Huperzine A may increase the neuromuscular blocking activities of Benzonatate.
Phenserine Phenserine may increase the neuromuscular blocking activities of Benzonatate.
Regramostim Regramostim may increase the neuromuscular blocking activities of Benzonatate.
Aprotinin Aprotinin may increase the neuromuscular blocking activities of Benzonatate.
Betaine Betaine may increase the neuromuscular blocking activities of Benzonatate.
Capsaicin Capsaicin may increase the neuromuscular blocking activities of Benzonatate.
Coumaphos Coumaphos may increase the neuromuscular blocking activities of Benzonatate.
Dichlorvos Dichlorvos may increase the neuromuscular blocking activities of Benzonatate.
Fenthion Fenthion may increase the neuromuscular blocking activities of Benzonatate.
Metrifonate Metrifonate may increase the neuromuscular blocking activities of Benzonatate.
Acotiamide Acotiamide may increase the neuromuscular blocking activities of Benzonatate.
Methanesulfonyl Fluoride Methanesulfonyl Fluoride may increase the neuromuscular blocking activities of Benzonatate.
Paraoxon Paraoxon may increase the neuromuscular blocking activities of Benzonatate.
Tyrothricin Tyrothricin may increase the neuromuscular blocking activities of Benzonatate.
Ipidacrine Ipidacrine may increase the neuromuscular blocking activities of Benzonatate.
Distigmine Distigmine may increase the neuromuscular blocking activities of Benzonatate.
Tretamine Tretamine may increase the neuromuscular blocking activities of Benzonatate.
Posiphen Posiphen may increase the neuromuscular blocking activities of Benzonatate.
Succinylcholine The serum concentration of Benzonatate can be increased when it is combined with Succinylcholine.
Oxybuprocaine The serum concentration of Oxybuprocaine can be increased when it is combined with Benzonatate.
Cocaine The serum concentration of Cocaine can be increased when it is combined with Benzonatate.
Trimethaphan The serum concentration of Trimethaphan can be increased when it is combined with Benzonatate.
Doxacurium The serum concentration of Doxacurium can be increased when it is combined with Benzonatate.
Chloroprocaine The serum concentration of Chloroprocaine can be increased when it is combined with Benzonatate.
Ephedrine The serum concentration of Ephedrine can be increased when it is combined with Benzonatate.
Butyrylthiocholine The serum concentration of Butyrylthiocholine can be increased when it is combined with Benzonatate.
Clevidipine The serum concentration of Clevidipine can be increased when it is combined with Benzonatate.
Sar9, Met (O2)11-Substance P The serum concentration of Sar9, Met (O2)11-Substance P can be increased when it is combined with Benzonatate.
Mirabegron The serum concentration of Mirabegron can be increased when it is combined with Benzonatate.
Aclidinium The serum concentration of Aclidinium can be increased when it is combined with Benzonatate.
Moxisylyte The serum concentration of Moxisylyte can be increased when it is combined with Benzonatate.
Propacetamol The serum concentration of Propacetamol can be increased when it is combined with Benzonatate.
Isoprenaline Isoprenaline may increase the neuromuscular blocking activities of Benzonatate.
Isavuconazonium The serum concentration of Isavuconazonium can be increased when it is combined with Benzonatate.
Benzgalantamine Benzgalantamine may increase the neuromuscular blocking activities of Benzonatate.

Target Protein

Sodium channel protein type 5 subunit alpha SCN5A

Referensi & Sumber

Synthesis reference: Matter, M.; U.S. Patent 2,714,608; August 2, 1955; assigned to Ciba Pharmaceutical Products, Inc.
Artikel (PubMed)
  • PMID: 19121573
    Dicpinigaitis PV, Gayle YE, Solomon G, Gilbert RD: Inhibition of cough-reflex sensitivity by benzonatate and guaifenesin in acute viral cough. Respir Med. 2009 Jun;103(6):902-6. doi: 10.1016/j.rmed.2008.12.008. Epub 2009 Jan 1.
  • PMID: 28334901
    Bishop-Freeman SC, Shonsey EM, Friederich LW, Beuhler MC, Winecker RE: Benzonatate Toxicity: Nothing to Cough At. J Anal Toxicol. 2017 Jun 1;41(5):461-463. doi: 10.1093/jat/bkx021.
  • PMID: 23258970
    Thimann DA, Huang CJ, Goto CS, Feng SY: Benzonatate toxicity in a teenager resulting in coma, seizures, and severe metabolic acidosis. J Pediatr Pharmacol Ther. 2012 Jul;17(3):270-3. doi: 10.5863/1551-6776-17.3.270.
  • PMID: 24648790
    Burns JM, Boyer EW: Antitussives and substance abuse. Subst Abuse Rehabil. 2013 Nov 6;4:75-82. doi: 10.2147/SAR.S36761. eCollection 2013.
  • PMID: 31129533
    Man J, Jiao F, Wang Y, Gu Y, Ding L, Shu C: Determination of benzonatate and its metabolite in human plasma by HPLC-MS/MS: A preliminary pharmacokinetic study in healthy Chinese volunteers after oral administration of benzonatate soft capsule. J Pharm Biomed Anal. 2019 Sep 5;173:134-143. doi: 10.1016/j.jpba.2019.05.030. Epub 2019 May 16.
  • PMID: 22958367
    Polverino M, Polverino F, Fasolino M, Ando F, Alfieri A, De Blasio F: Anatomy and neuro-pathophysiology of the cough reflex arc. Multidiscip Respir Med. 2012 Jun 18;7(1):5. doi: 10.1186/2049-6958-7-5.

Contoh Produk & Brand

Produk: 362 • International brands: 4
Produk
  • Benzonatate
    Capsule • 100 mg/1 • Oral • US • Approved
  • Benzonatate
    Capsule • 200 mg/1 • Oral • US • Approved
  • Benzonatate
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
  • Benzonatate
    Capsule • 200 mg/1 • Oral • US • Generic • Approved
  • Benzonatate
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
  • Benzonatate
    Capsule • 200 mg/1 • Oral • US • Generic • Approved
  • Benzonatate
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
  • Benzonatate
    Capsule • 100 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 362 produk.
International Brands
  • Exangit
  • Tesaperl — Novartis
  • Tessalon Perles
  • Ventussin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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