Ambroxol Hydrochloride

Ambroxol Hydrochloride

Drug Nomenclature

Date of monograph revision: 13-Oct-1997; 23-Jun-1998; 07-Apr-2000; 01-Nov-2001; 01-Jul-2004; 05-Jul-2006
Synonyms: Ambroksolihydrokloridi; Ambroksolio hidrochloridas; Ambroxol hydrochlorid; Ambroxol, hidrocloruro de; Ambroxol-hidroklorid; Ambroxolhydroklorid; Ambroxoli Hydrochloridum; NA-872 (ambroxol)
BAN: Ambroxol Hydrochloride [BANM]
INN: Ambroxol Hydrochloride [rINNM (en)]
INN: Hidrocloruro de ambroxol [rINNM (es)]
INN: Ambroxol, Chlorhydrate d' [rINNM (fr)]
INN: Ambroxoli Hydrochloridum [rINNM (la)]
INN: Амброксола Гидрохлорид [rINNM (ru)]
Chemical name: trans-4-(2-Amino-3,5-dibromobenzylamino)cyclohexanol hydrochloride
Molecular formula: C13H18Br2N2O,HCl =414.6
CAS: 18683-91-5 (ambroxol); 15942-05-9 (ambroxol hydrochloride); 23828-92-4 (ambroxol hydrochloride)
ATC code: R05CB06
Chemical Structure of Ambroxol

Chemical Structure of Ambroxol

Pharmacopoeias:

In Chin. and Eur. (see Go to European Pharmacopoeia Convention Signatories).

Ph. Eur. 5.5 (Ambroxol Hydrochloride). A white or yellowish crystalline powder. Sparingly soluble in water; practically insoluble in dichloromethane; soluble in methyl alcohol. A 1% solution in water has a pH of 4.5 to 6.0. Protect from light.

Drug Profile

Ambroxol is a metabolite of bromhexine (Go to Bromhexine) and is used similarly as a mucolytic. It is given in a usual daily dose of 60 to 120 mg of the hydrochloride by mouth, in 2 or 3 divided doses. Ambroxol has also been given by inhalation, injection, or rectally.

Ambroxol acefyllinate (acebrofylline) has been used similarly.

Adverse effects.

Hypersensitivity.

A report1 of contact allergy to ambroxol, but not bromhexine.

  1. 1. Mancuso G, Berdondini RM. Contact allergy to ambroxol. Contact Dermatitis 1989; 20: 154. PubMed

Pharmacokinetics.

References to pharmacokinetic studies of ambroxol.

  1. 1. Hammer R, et al Speziesvergleich in Pharmakokinetik und Metabolismus von NA 872 Cl Ambroxol bei Ratte, Kaninchen, Hund und Mensch. Arzneimittelforschung 1978; 28: 899–903. PubMed
  2. 2. Jauch R, et al. Ambroxol, Untersuchungen zum Stoffwechsel beim Menschen und zum quantitativen Nachweis in biologischen Proben. Arzneimittelforschung 1978; 28: 904–11. PubMed
  3. 3. Vergin H, et al. Untersuchungen zur Pharmakokinetik und Bioäquivalenz unterscheidlicher Darreichungsformen von Ambroxol. Arzneimittelforschung 1985; 35: 1591–5. PubMed

Respiratory disorders.

Mixed results1-3 were obtained when ambroxol was used in chronic bronchitis (Go to Chronic obstructive pulmonary disease); in a randomised study, it was no better than placebo in preventing acute exacerbations of chronic obstructive pulmonary disease; however, in a subset of patients with more severe disease, ambroxol therapy reduced the number of exacerbations.4 It was ineffective5 when given to mothers for the prophylaxis of neonatal respiratory distress syndrome (Go to Neonatal respiratory distress syndrome), although it may be of modest benefit in the early treatment of established disease in infants.6,7

Inhalation of ambroxol aerosol has also produced beneficial effects in a patient with alveolar proteinosis who refused alveolar lavage.8

For the use of mucolytics in productive cough see Go to Cough.

  1. 1. Olivieri D, et al. Ambroxol for the prevention of chronic exacerbations: long-term multicenter trial: protective effect of ambroxol against winter semester exacerbations: a double-blind study versus placebo. Respiration 1987; 51 (suppl 1): 42–51. PubMed
  2. 2. Guyatt GH, et al. A controlled trial of ambroxol in chronic bronchitis. Chest 1987; 92: 618–20. PubMed
  3. 3. Alcozer G, et al. Prevention of chronic bronchitis exacerbations with ambroxol (Mucosolvan Retard): an open, long-term, multicenter study in 5,635 patients. Respiration 1989; 55 (suppl 1): 84–96. PubMed
  4. 4. Malerba M, et al. Effect of twelve-months therapy with oral ambroxol in preventing exacerbations in patients with COPD: double-blind, randomized, multicenter, placebo-controlled study (the AMETHIST Trial). Pulm Pharmacol Ther 2004; 17: 27–34. PubMed
  5. 5. Dani C, et al. Antenatal ambroxol treatment does not prevent the respiratory distress syndrome in premature infants. Eur J Pediatr 1997; 156: 392–3. PubMed
  6. 6. Wauer RR, et al. Randomized double blind trial of Ambroxol for the treatment of respiratory distress syndrome. Eur J Pediatr 1992; 151: 357–63. PubMed
  7. 7. Schmalisch G, et al. Changes in pulmonary function in preterm infants recovering from RDS following early treatment with ambroxol: results of a randomized trial. Pediatr Pulmonol 1999; 27: 104–12. PubMed
  8. 8. Diaz JP, et al. Response to surfactant activator (ambroxol) in alveolar proteinosis. Lancet 1984; i: 1023. PubMed

Uricosuric action.

A study1 was carried out in 48 young male healthy subjects to examine the uricosuric effect of ambroxol. The minimum effective dose for lowering plasma-uric acid concentrations was found to be between 250 and 500 mg daily given in 2 divided doses. Although these doses are much higher than those used to treat bronchopulmonary disease, doses as high as l g daily were well tolerated.

  1. 1. Oosterhuis B, et al. Dose-dependent uricosuric effect of ambroxol. Eur J Clin Pharmacol 1993; 44: 237–41. PubMed

Preparations

Single-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Argentina: Ambril; Apracur Expectorante¤; Cortos; Dogistin¤; Graneodin Expectorante¤; Mucomex¤; Mucosolvon; Tabcin Expectorante¤; Tavinex Expectorante; Tavinex Expectotabs; Austria: Ambrobene; Ambrohexal; Ambrolan; Ambrolos; Bisolangin; Bisolaryn; Broxol; Mucosolvan; Sekretovit¤; Belgium: Surbronc; Brazil: Ambrizol; Ambrol; Ambroten; Ambrox; Ambroxolvan¤; Anabron; Benatoss¤; Benetoss¤; Brismucol; Broncoflux; Brondilat; Bronxol; Cebronfilina; Expectuss; Filinar; Fluibron; Fluidin; Fluxol; Mucibron; Mucoclean; Mucolin; Mucosolvan; Mucoxolan; Neossolvan; Probec¤; Pulmosolvan; Surfactil; Teomuc; Chile: Bronchopront¤; Broncot; Fluibron; Fluomit; Milbron¤; Mintamox; Mucosolvan; Muxol; Tocalm; Czech Republic: Ambrobene; Ambrosan; Bronchopront; Dignobroxol; Dr Rentschler Hustenloser; Fervex; Halixol; Mucosin; Mucosolvan; Neo-Bronchol; Solvolan; France: Muxol; Surbronc; Germany: Ambril; Ambro-Puren; Ambro; Ambrobeta; Ambrodoc; Ambrohexal; Ambroinfant; Ambrolos; Ambropp¤; Antussan¤; Bisolvon AM¤; Bronchopront; Bronchowern; Contac Husten-Trunk¤; Dignobroxol¤; duramucal; Expit; Farmabroxol¤; Flavamed Hustentabletten, Husten-Heissgetrank, Hustensaft, Hustentropfen, and Husten-Retardkapseln¤; frenopect; Frubizin akut; Gelopol¤; Ilvico Hustenloser¤; Jenabroxol¤; Larylin Husten-Heissgetrank¤; Larylin Husten-Loser Pastillen; Larylin Husten-Loser Saft¤; Lindoxyl; Logomed Husten¤; Mibrox¤; Muco-Aspecton¤; Muco-Fips¤; Muco-Tablinen¤; Mucoangin; Mucobroxol¤; Mucoclear¤; Mucophlogat¤; Mucosolvan; Mucotablin¤; Mucovent¤; Neo-Bronchol¤; Nymix Mucolytikum¤; Padiamuc; Pect Hustenloser¤; Pulmonal S¤; Sigabroxol; stas-Hustenloser; Therapin Hustenloser¤; tuss; Tussipect A¤; tusso-basan¤; Tusso¤; Greece: Abrobion; Abrolen; Afrodor; Amboral; Ambrobion¤; Ambromyc; Anavix; Aprinol; Bunafon; Celibron; Ebertuss; Effercet; Erosil; Fluibrox; Grenovix; Hivotex; Kriolen; Lextarol; Mavixan; Mucolin; Mucosolvan; Mucovix; Nibren; Olbenorm; Provixen-N; Puntol; Respirol; Stefolant; Strubelin; Tevoril; Tosse; Tussefar; Zyrantol; Hong Kong: Amxol; Bronchopront; Max; Medovent¤; Mucosolvan; Hungary: Ambrobene; Ambrohexal; Bronchopront; Halixol; Solvolan; India: Acocontin; Acolyt; Ambrodil; Inhalex; Italy: Ambromucil; Ambrotus; Amobronc; Atus; Broncomnes; Broxol; Chinson¤; Fluibron; Fluixol; Lintos; Lisopulm¤; Muciclar; Mucoaricodil; Mucobron; Mucosolvan; Secretil; Surfactal; Surfolase; Tauxolo; Viscomucil; Japan: Mucosal; Mucosolvan; Malaysia: Amxol; Axol; Mucosolvan; Shinoxol; Mexico: Ambodil¤; Ambrofur; Ambrowel¤; Amocol; Balsibron; Bionoxol; Brismucol; Brogal; Bronolban; Brosolan; Broxaquim; Broxofar; Broxoffler; Broxol; Broxolan¤; Broxolim; Ebromin; Exabrol; Expeflen; Fantrodol¤; Ital-Ultra; Loexom; Minisol¤; Mucibron; Mucoangin; Mucosolvan; Mucovibrol T; Mucovibrol; Mucoxol; Musalten; Musvan; Muxol¤; Oxolvan; Oxoway¤; Prospec; Protitus; Randex; Rimoxol¤; Sekretovit; Septacin; Seraxol-S; Softixol¤; Solpat; Tobrin; Tradexol¤; Trimexine; Tunitol-BX; Tusibron; Viaxol; Weiscal; Netherlands: Mucoangin; Portugal: Benflux; Bromax; Bronchopront¤; Broncoliber; Drenoxol; Fluidox; Fluidrenol; Hipotosse; Mucodrenol; Mucosolvan; Surfolase; Tusolven; Russia: Ambrobene (Амбробене); Ambrohexal (Амброгексал); Ambrosan (Амбросан); Ambrosol (Амбросол); Bronchowern (Бронховерн); Halixol (Халиксол); Lasolvan (Лазолван); Medovent (Медовент); Singapore: Amxol; Axol¤; Bronchopront¤; Fluibron¤; Max; Mucosolvan; Shinoxol¤; Spain: Ambrolitic; Dinobroxol; Motosol; Mucibron; Mucosan; Naxpa; Switzerland: Abramen¤; Fluibron¤; Mucabrox; Mucoangin; Mucosolvon; Thailand: Ambrol; Ambrolytic¤; Ambrox; Ambroxan; Ampromed; Amtuss; Amxol; Bronchopront¤; Broncol; Broxol; Broxsa¤; Max; Medovent; Misovan; Movent¤; Mucodic; Mucolan; Mucolid; Mucomed; Mucopec; Mucosolvan; Mucoxine-F; Mucozan¤; Musocan; Nucobrox; Polibroxol; Posecus¤; Simusol; Strepsils Chesty Cough; United Arab Emirates: Mucum; Venezuela: Ambril; Ambromuco; Benflux; Brixilon; Brocantol; Bronilis; Litusix; Misulvan; Mucorama; Mucosolvan; Muxen;

Multi-ingredient Preparations

The symbol ¤ denotes a preparation which is discontinued or no longer actively marketed.

Argentina: Amoxi Respiratorio¤; Amoxidal Respiratorio Duo; Amoxidal Respiratorio; Amoxigrand Bronquial; Amoxipenil Bronquial; Amoxitenk Respiratorio¤; Aseptobron Respiratorio; Bronco Biotaer¤; Bronquisedan Mucolitico; Bronquisedan; Cefacar Mucolitico¤; Cefacilina Bronquial; Gentiabron¤; Letondal; Muco Cortos¤; Muco Dosodos Biotic; Muco Dosodos; Mucoprednibron; Mucosolvon Compositum; No-Tos Biotic; Nobactam Bronquial; Oxibron NF; Oximar Respiratorio; Toraxan; Trexirol NF¤; Austria: Mucospas; Mucotectan¤; Vibrabron¤; Brazil: Penetro¤; Chile: Ambrotos; Czech Republic: Doxycyclin Al Comp; Germany: Ambrodoxy; Ambroxol AL comp; Ambroxol comp; Amdox-Puren; Azudoxat comp¤; Broncho-Euphyllin; Doxam; Doximucol; Doxy Comp; Doxy Lindoxyl; Doxy Plus; Doxy-duramucal¤; Doxy-Wolff Mucolyt; Doxysolvat¤; Jenabroxol comp¤; Mibrox comp¤; Mucotectan¤; Sagittamuc¤; Sigamuc; Spasmo-Mucosolvan; Terelit; India: Ambrodil Plus; Ambrodil-S; Amcof; Amcold; Asthalin AX; Axalin; Kofarest; Mucaryl-AX; Novamox AX; Roxeptin-ME; Suprivent-A; Mexico: Acimox-Ex; Aeroflux; Alexing; Ambodil-C; Aminoefedrison; Balsibron-C; Bisincof; Bolbamox; Brogal Compositum; Brogal-T; Brominol-C; Bronolban-M; Broquixol; Brosolan-C; Broxofar Compuesto; Broxol Plus; Broxolim-AM; Broxolim-C; Brumax; Cefabroxil; Cibronal; Cobadex; Coricidin Expec; Dexol; Dofaxil; Ebromin-P; Epicol NF¤; Faribrox; Ferlex; Fludexol-CL; Fluxol; Gimabrol; Histiacil NF; Laritol Ex; Linfarden; Loexom FC; Loexom FS; Loxorol; Mucoflux; Mucosolvan Compositum; Mucovibrol Amoxi; Mucovibrol C; Musaldox; Neumyn-AS; Pentibroxil; Ravotaf; Rombox; Sekretovit Amoxi; Sekretovit Ex; Sensibit XP; Septacin Amoxi; Septacin Ex; Seraxol; Serbol; Sermoxol; Tadinar-C; Tavexyl; Tenalif; Torva; Toxol; Portugal: Clembroxol¤; Mucospas; Ventoliber; Russia: Coldact Broncho (Колдакт Бронхо); Venezuela: Aeroflux; Ambromuco Compositum; Arbixil; Clenbuxol; Litusix Compositum; Mucolin; Mucosolvan Compositum;



Your email address will not be published. Required fields are marked *

*

Comment