Bromhexine: Difference between revisions

Bromhexine
Clinical data
AHFS/Drugs.com	International Drug Names
Pregnancy; category	A (Aus);
ATC code	R05CB02 (WHO) ;
Legal status
Legal status	In general: Over-the-counter (OTC);
Pharmacokinetic data
Bioavailability	75-80%
Elimination half-life	12 hr
Identifiers
	IUPAC name 2,4-Dibromo-6-{[cyclohexyl(methyl)amino]methyl}aniline;
CAS Number	3572-43-8 ;
PubChem CID	2442;
DrugBank	DB09019 ;
ChemSpider	2348 ;
UNII	Q1J152VB1P;
KEGG	D07542 ;
ChEBI	CHEBI:77032 ;
ChEMBL	ChEMBL253376 ;
CompTox Dashboard (EPA)	DTXSID6022686 ;
ECHA InfoCard	100.020.622
Chemical and physical data
Formula	C14H20Br2N2
Molar mass	376.136 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES Brc1cc(c(N)c(Br)c1)CN(C)C2CCCCC2;
	InChI InChI=1S/C14H20Br2N2/c1-18(12-5-3-2-4-6-12)9-10-7-11(15)8-13(16)14(10)17/h7-8,12H,2-6,9,17H2,1H3 ; Key:OJGDCBLYJGHCIH-UHFFFAOYSA-N ;
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Revision as of 23:19, 1 October 2020

Bromhexine is a mucolytic drug used in the treatment of respiratory disorders associated with viscid or excessive mucus.^[1]

It was patented in 1961 and came into medical use in 1966.^[2]

Function

Bromhexine is intended to support the body's mechanisms for clearing mucus from the respiratory tract. It is secretolytic, increasing the production of serous mucus in the respiratory tract, which makes the phlegm thinner and less viscous. This contributes to a secretomotoric effect, allowing the cilia to more easily transport the phlegm out of the lungs. For this reason it is often added to cough syrups.

It has been shown to increase the proportion of serous bronchial secretion, making it more easily expectorated. It is indicated as "secretolytic therapy in bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport".

Bromhexine is contained in various formulations, high and low strength syrups 8 mg/5 ml, 4 mg/5 ml, tablets and soluble tablets (both with 8 mg bromhexine) and solution for oral use 10 mg/5 ml, adapted to the need of the patients. The posology varies with the age and weight, but there are products for all age groups from infant on. Bromhexine is well established and tolerated.

Brand names

Broncholyte Elixir
Bisolvon
Paxirasol
Barkacin
Bromhexin
Vasican
Bisolex
Robitussin Chesty/Forte
Duro-Tuss Chesty/Forte
Benadryl Chesty/Forte
Movex
Bromex
Solvex
Mucolyte
Brofentol
Brofentol Plus
Dysolvon
Flegamina
Ventilate Forte (combination of bromhexine and salbutamol)
Cofdex

References

^ Morton, Ian; Hall, Judith (1999). Concise Dictionary of Pharmacological Agents. Springer. p. 55. ISBN 0-7514-0499-3. Retrieved 2009-06-03.
^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 544. ISBN 9783527607495.

[CDoPA-1] Morton, Ian; Hall, Judith (1999). Concise Dictionary of Pharmacological Agents. Springer. p. 55. ISBN 0-7514-0499-3. Retrieved 2009-06-03.

[Fis2006-2] Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 544. ISBN 9783527607495.

[1]

[2]

@@ Line 59: / Line 59: @@
 Bromhexine is contained in various formulations, high and low strength syrups 8&nbsp;mg/5&nbsp;ml, 4&nbsp;mg/5&nbsp;ml, tablets and soluble tablets (both with 8&nbsp;mg bromhexine) and solution for oral use 10&nbsp;mg/5&nbsp;ml, adapted to the need of the patients. The [[posology]] varies with the age and weight, but there are products for all age groups from infant on. Bromhexine is well established and tolerated.
-==Experimental Antiviral Use==
-Some [[coronaviruses]], e.g. both the [[SARS-CoV|SARS coronavirus of 2003]] and the [[SARS-CoV-2]] which causes [[COVID-19]], are activated by [[TMPRSS2]] and can thus be inhibited by TMPRSS2 inhibitors.<ref name="Hoffmann_2020" /> "[[SARS-CoV-2]] uses the SARS-CoV receptor [[ACE2]] for entry and the serine protease TMPRSS2 for S protein priming<ref>{{cite journal | vauthors = Rahman N, Basharat Z, Yousuf M, Castaldo G, Rastrelli L, Khan H | title = Virtual screening of natural products against type II transmembrane serine protease (TMPRSS2), the priming agent of Coronavirus 2 (SARS-CoV-2) | journal = Molecules | volume = 25 | issue = 10 | pages = 2271 | date = May 2020 | pmid = 32408547 | pmc = 7287752 | doi = 10.3390/molecules25102271 }}</ref>. A TMPRSS2 inhibitor approved for clinical use blocked entry and might constitute a treatment option."<ref name="Hoffmann_2020">{{cite journal | vauthors = Hoffmann M, Kleine-Weber H, Schroeder S, Krüger N, Herrler T, Erichsen S, Schiergens TS, Herrler G, Wu NH, Nitsche A, Müller MA, Drosten C, Pöhlmann S | display-authors = 6 | title = SARS-CoV-2 Cell Entry Depends on ACE2 and TMPRSS2 and Is Blocked by a Clinically Proven Protease Inhibitor | journal = Cell | date = March 2020 | volume = 181 | issue = 2 | pages = 271–280.e8 | pmid = 32142651 | doi = 10.1016/j.cell.2020.02.052 | pmc = 7102627 | lay-url = https://www.dpz.eu/en/home/single-view/news/die-vermehrung-von-sars-coronavirus-2-im-menschen-verhindern.html | lay-source = Deutsches Primatenzentrum GmbH | doi-access = free }}</ref>  Bromhexine is also one such experimental candidate as a TMPRSS2 inhibitor for potential use against both influenza and coronavirus infections in general, including those prior to the advent of [[COVID-19]]<ref name=Shen_2017>{{cite journal |last1=Shen |first1=Li Wen |last2=Mao |first2=Hui Juan |last3=Wu |first3=Yan Ling |last4=Tanaka |first4=Yoshimasa |last5=Zhang |first5=Wen |title=TMPRSS2: A potential target for treatment of influenza virus and coronavirus infections |journal=Biochimie |date=November 2017 |volume=142 |pages=1–10 |doi=10.1016/j.biochi.2017.07.016 |pmid=28778717 |pmc=7116903 }}</ref> as well as COVID-19 itself. <ref name=Depfenhart_2020>{{cite journal |last1=Depfenhart |first1=Markus |last2=de Villiers |first2=Danielle |last3=Lemperle |first3=Gottfried |last4=Meyer |first4=Markus |last5=Di Somma |first5=Salvatore |title=Potential new treatment strategies for COVID-19: is there a role for bromhexine as add-on therapy? |journal=Internal and Emergency Medicine |date=August 2020 |volume=15 |issue=5 |pages=801–812 |doi=10.1007/s11739-020-02383-3 |pmid=32458206 |s2cid=218877551 |doi-access=free }}</ref>
 ==Brand names==