Peringatan Keamanan

The oral LD50 of bromhexine in rats is 6 g/kg.L33125 The observed symptoms of accidental overdose with bromhexine are consistent with the
known adverse effects of bromhexine, including headache, nausea, and vomiting, among other symptoms. Provide symptomatic treatment and contact poison control services if an overdose is confirmed or suspected.L33060

Bromhexine

DB09019

small molecule approved

Deskripsi

Bromhexine is mucolytic agent used for a variety of respiratory conditions associated with increased mucus secretion. It is derived from the Adhatoda vasica plant and aids in the clearance of excess mucus, improving breathing and reducing cough. It was introduced into the market in 1963, and is widely available as an over-the-counter drug in many countries.A233240 Recently, bromhexine and its metabolite ambroxol have garnered interest for the potential prevention and treatment of COVID-19 due to their interactions with cell receptors in the lungs.A233345,A233370

Struktur Molekul 2D

Berat 376.13
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following single oral doses ranging from 8 and 32 mg, the terminal half-life of bromhexine has been measured between 6.6 and 31.4 hours.[L33060]
Volume Distribusi After intravenous administration in a pharmacokinetic study, bromhexine was found to be widely distributed. Bromhexine is known to cross the blood-brain barrier; small concentrations may cross the placenta. The average volume of distribution of bromhexine was 1209 ± 206 L (19 L/kg). Lung tissue concentrations of bromhexine two hours after a dose were 1.5 to 3.2 times higher in bronchial tissues than plasma concentrations. Pulmonary parynchema concentrations were 3.4 to 5.9 times higher when compared to plasma concentrations.[L33060]
Klirens (Clearance) The clearance of bromhexine ranges from 843-1073 mL/min, within the range of the hepatic circulation.[L33060]

Absorpsi

After oral administration, bromhexine demonstrates linear pharmacokinetics when given in doses of 8-32 mg. Bromhexine is readily absorbed in the gastrointestinal tract at a rapid rate. This drug undergoes extensive first-pass effect in the range of 75-80%.A233285,L33060 The bioavailability is therefore reduced to approximately 22-27%.L33060

Metabolisme

Bromhexine is almost completely metabolized to a variety of hydroxylated metabolites in addition to dibromanthranilic acid. Ambroxol is a known metabolite of bromhexine.L33060 In one study of human plasma, (E)-4-hydroxydemethylbromhexine (E-4-HDMB) and (E)-3-hydroxydemethylbromhexine (E-3-HDMB) were quantified as major metabolites of ambroxol, and (Z)-4-hydroxydemethylbromhexine and (Z)-3-hydroxydemethylbromhexine were quantified as minor metabolites.A233340

Rute Eliminasi

After a dose of bromhexine was administered during a pharmacokinetic study, approximately 97% of the radiolabeled dose was detected in the urine; under 1% was detected as the parent drug.L33060

Interaksi Obat

0 Data
Tidak ada data.

Target Protein

Transmembrane protease serine 2 TMPRSS2
Angiotensin-converting enzyme 2 ACE2

Referensi & Sumber

Synthesis reference: ???????????. (2015). Production method of bromhexine hydrochloride(Worldwide CN2013103399540A ).https://patents.google.com/patent/CN103396323A/en
Artikel (PubMed)
  • PMID: 28331610
    Zanasi A, Mazzolini M, Kantar A: A reappraisal of the mucoactive activity and clinical efficacy of bromhexine. Multidiscip Respir Med. 2017 Mar 20;12:7. doi: 10.1186/s40248-017-0088-1. eCollection 2017.
  • PMID: 32983936
    Ansarin K, Tolouian R, Ardalan M, Taghizadieh A, Varshochi M, Teimouri S, Vaezi T, Valizadeh H, Saleh P, Safiri S, Chapman KR: Effect of bromhexine on clinical outcomes and mortality in COVID-19 patients: A randomized clinical trial. Bioimpacts. 2020;10(4):209-215. doi: 10.34172/bi.2020.27. Epub 2020 Jul 19.
  • PMID: 6897618
    Bechgaard E, Nielsen A: Bioavailability of bromhexine tablets and preliminary pharmacokinetics in humans. Biopharm Drug Dispos. 1982 Oct-Dec;3(4):337-44. doi: 10.1002/bdd.2510030407.
  • PMID: 20031363
    Liu J, Chen X, Hu Y, Cheng G, Zhong D: Quantification of the major metabolites of bromhexine in human plasma using RRLC-MS/MS and its application to pharmacokinetics. J Pharm Biomed Anal. 2010 Apr 6;51(5):1134-41. doi: 10.1016/j.jpba.2009.11.024. Epub 2009 Dec 1.
  • PMID: 32360584
    Habtemariam S, Nabavi SF, Ghavami S, Cismaru CA, Berindan-Neagoe I, Nabavi SM: Possible use of the mucolytic drug, bromhexine hydrochloride, as a prophylactic agent against SARS-CoV-2 infection based on its action on the Transmembrane Serine Protease 2. Pharmacol Res. 2020 Jul;157:104853. doi: 10.1016/j.phrs.2020.104853. Epub 2020 Apr 30.
  • PMID: 33045350
    Alkotaji M: Azithromycin and ambroxol as potential pharmacotherapy for SARS-CoV-2. Int J Antimicrob Agents. 2020 Dec;56(6):106192. doi: 10.1016/j.ijantimicag.2020.106192. Epub 2020 Oct 10.
  • PMID: 20616932
    Gupta PR: Ambroxol - Resurgence of an old molecule as an anti-inflammatory agent in chronic obstructive airway diseases. Lung India. 2010 Apr;27(2):46-8. doi: 10.4103/0970-2113.63603.
  • PMID: 581989
    Jauch R, Bozler G, Hammer R, Koss FW, Karlsson M, Vitek E, Haring I, Beschke K, Hadamovsky S, Maass D, Wollmann R: Ambroxol, studies of biotransformation in man and determination in biological samples (author's transl). Arzneimittelforschung. 1978;28(5a):904-11.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 1 • International brands: 5
Produk
  • Bromhexine Hydrochloride
    Powder • 1000 g/1000g • Not applicable • US
International Brands
  • Amiorel — Boehringer Ingelheim
  • Bisolmed — Boehringer Ingelheim
  • Bisolvon — Boehringer Ingelheim
  • Bisolvon Chesty — Boehringer Ingelheim
  • Fluibron

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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