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- ambroxol hydrochloride
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/06/30 04:50:20」(JST)
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Ambroxol
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| Systematic (IUPAC) name |
| trans-4-(2-Amino-3,5-dibrombenzylamino)-cyclohexanol |
| Clinical data |
| AHFS/Drugs.com |
International Drug Names |
| Pregnancy cat. |
? |
| Legal status |
? |
| Identifiers |
| CAS number |
18683-91-5 N |
| ATC code |
R05CB06 |
| PubChem |
CID 2132 |
| ChemSpider |
10276826 Y |
| UNII |
200168S0CL Y |
| KEGG |
D07442 Y |
| ChEMBL |
CHEMBL153479 Y |
| Chemical data |
| Formula |
C13H18Br2N2O |
| Mol. mass |
378.10 |
SMILES
- O[C@H]2CC[C@H](NCc1cc(Br)cc(Br)c1N)CC2
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InChI
-
InChI=1S/C13H18Br2N2O/c14-9-5-8(13(16)12(15)6-9)7-17-10-1-3-11(18)4-2-10/h5-6,10-11,17-18H,1-4,7,16H2/t10-,11- Y
Key:JBDGDEWWOUBZPM-XYPYZODXSA-N Y
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N (what is this?) (verify)
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Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. It is the active ingredient of Mucosolvan, Mucobrox, Lasolvan, Mucoangin, Surbronc and Lysopain. The substance is a mucoactive drug with several properties including secretolytic and secretomotoric actions that restore the physiological clearance mechanisms of the respiratory tract, which play an important role in the body’s natural defence mechanisms. It stimulates synthesis and release of surfactant by type II pneumocytes. Surfactant acts as an anti-glue factor by reducing the adhesion of mucus to the bronchial wall, in improving its transport and in providing protection against infection and irritating agents.[1][2]
Ambroxol is indicated as "secretolytic therapy in bronchopulmonary diseases associated with abnormal mucus secretion and impaired mucus transport. It promotes mucus clearance, facilitates expectoration and eases productive cough, allowing patients to breathe freely and deeply".[3]
Ambroxol hydrochloride tablets in Japan
There are many different formulations developed since the first marketing authorisation in 1978. Ambroxol is available as syrup, tablets, pastilles, dry powder sachets, inhalation solution, drops and ampules as well as effervescent tablets.
Ambroxol also provides pain relief in acute sore throat. Pain in sore throat is the hallmark of acute pharyngitis.[4] Sore throat is usually caused by a viral infection. The infection is self limited and the patient recovers normally after a few days. What is most bothering for the patient is the continuous pain in the throat maximized when the patient is swallowing. The main goal of treatment is thus to reduce pain. The main property of Ambroxol for treating sore throat is the local anaesthetic effect, described first in the late 1970s,[5][6] but explained and confirmed in more recent work.
Ambroxol is a very potent inhibitor of the neuronal Na+ channels.[7] This property led to the development of a lozenge containing 20 mg of ambroxol. Many state-of-the-art clinical studies[4] have demonstrated the efficacy of Ambroxol in relieving pain in acute sore throat, with a fast onset of action and a long duration of effect of at least 3 hours. Additional anti-inflammatory properties of Ambroxol are of clinical relevance since treatment lead to a marked reduction of redness of the patient’s sore throat.
References[edit]
- ^ Sanderson RJ et al. (1976), "Morphological and physical basis for lung surfactant action.", Respir Phys 27 (3): 379–92, PMID 989610
- ^ Kido H et al. (Nov 2004), "Secretory leukoprotease inhibitor and pulmonary surfactant serve as principal defenses against influenza A virus infection in the airway and chemical agents up-regulating their levels may have therapeutic potential.", Biol Chem 385 (11): 1029–034, PMID 15576322
- ^ Malerba M, Ragnoli B. (Aug 2008), "Ambroxol in the 21st century: pharmacological and clinical update.", Expert Opin Drug Metab Toxicol. 4 (8): 1119–29, doi:10.1517/17425255.4.8.1119, PMID 18680446
- ^ a b de Mey C. et al. (2008), "Efficacy and safety of ambroxol lozenges in the treatment of acute uncomplicated sore throat.", Arzneimittelforschung 58 (11): 557–68, doi:10.1055/s-0031-1296557, PMID 19137906
- ^ Püschmann S, Engelhorn R. (1978), "Pharmakologische Untersuchungen des Bromhexin-Metaboliten Ambroxol. (Pharmacological study on the bromhexine-metabolite ambroxol)", Arzneimittelforschung 28 (5a): 889–98, PMID 581987
- ^ Klier KF, Papendick U. (1977), "Die lokalanaesthetische Wirkung von NA-872-haltigen Augentropfen. (The local anesthetic effect of NA872-containing eyedrops)", Med Monatsschr. 31 (12): 575–8, PMID 593223
- ^ Weiser T. (2006), "Comparison of the effects of four Na+ channel analgesics on TTX-resistant Na+ currents in rat sensory neurons and recombinant Nav1.2 channels.", Neurosci Lett. 395 (3): 179–184, doi:10.1016/j.neulet.2005.10.058, PMID 16293367
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Cough and cold preparations (R05)
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| Expectorants |
- Althea root
- Antimony pentasulfide
- Creosote
- Guaiacolsulfonate
- Guaifenesin
- Ipecacuanha (Syrup of ipecac)
- Levoverbenone
- Potassium iodide
- Senega
- Tyloxapol
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| Mucolytics |
- Acetylcysteine
- Ambroxol
- Bromhexine
- Carbocisteine
- Domiodol
- Dornase alfa
- Eprazinone
- Erdosteine
- Letosteine
- Mesna
- Neltenexine
- Sobrerol
- Stepronin
- Tiopronin
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|
| Cough suppressants |
Opium alkaloids,
opioids,
and derivatives |
- Acetyldihydrocodeine
- Benzylmorphine
- Codeine
- Dextromethorphan
- Diacetylmorphine
- Dihydrocodeine
- Dimemorfan
- Droxypropine
- Ethylmorphine
- Hydrocodone
- Hydromorphone
- Isoaminile
- Laudanum
- Levomethadone
- Levopropoxyphene
- Methadone
- Nicocodeine
- Nicodicodeine
- Normethadone
- Noscapine
- Pholcodine
- Thebacon
- Tipepidine
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Other
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- Benzonatate
- Benproperine
- Bibenzonium bromide
- Butamirate
- Clobutinol
- Clofedanol
- Cloperastine
- Diphenhydramine
- Dibunate
- Dimethoxanate
- Dropropizine
- Fedrilate
- Glaucine
- Levodropropizine
- Meprotixol
- Morclofone
- Nepinalone
- Oxolamine
- Oxeladin
- Pentoxyverine
- Pipazetate
- Prenoxdiazine
- Piperidione
- Zipeprol
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anat (n, x, l, c)/phys/devp
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noco (c, p)/cong/tumr, sysi/epon, injr
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proc, drug (R1/2/3/5/6/7)
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UpToDate Contents
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English Journal
- Effect of Ambroxol and Beclomethasone on Lipopolysaccharide-Induced Nitrosative Stress in Bronchial Epithelial Cells.
- Ricciardolo FL1, Sorbello V, Benedetto S, Paleari D.
- Respiration; international review of thoracic diseases.Respiration.2015 May 12. [Epub ahead of print]
- BACKGROUND: Nitrosative stress is involved in different airway diseases. Lipopolysaccharide (LPS) induces neutrophil-related cytokine release and nitrosative stress in human bronchial epithelial (BEAS-2B) cells alone or with human polymorphonuclear neutrophils (PMNs). Ambroxol protects against oxida
- PMID 25998443
- Marked improvement in autoimmune pulmonary alveolar proteinosis with severe hypoxemia in a patient treated with ambroxol: a case report.
- Oda N1, Tamai K2, Suzuki Y3, Yoshimatsu H4, Matsuoka H5, Matsumoto Y6, Okada N7.
- Journal of medical case reports.J Med Case Rep.2015 May 6;9(1):100. doi: 10.1186/s13256-015-0588-6.
- INTRODUCTION: Pulmonary alveolar proteinosis is characterized by accumulation of surfactant and phospholipids in the pulmonary alveoli. Whole lung lavage is considered the first-line therapy, which requires special techniques. To the best of our knowledge, there have only been limited reports that h
- PMID 25943363
- A novel inhaled multi-pronged attack against respiratory bacteria.
- Lee SH1, Teo J2, Heng D3, Zhao Y4, Ng WK5, Chan HK6, Tan LT5, Tan RB7.
- European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences.Eur J Pharm Sci.2015 Apr 5;70:37-44. doi: 10.1016/j.ejps.2015.01.005. Epub 2015 Jan 19.
- Airway mucus hypersecretion is a common clinical feature of many severe respiratory diseases, and when complicated by a recalcitrant bacterial infection, the whole treatment regimen thereby becomes more challenging and protracted. The accumulation of thickened mucus secretions in the lower airways p
- PMID 25612805
Japanese Journal
- 症例 超高齢者に発症した自己免疫性肺胞蛋白症の1例
- 沼田 岳士,大澤 翔,本間 祐樹 [他]
- 日本呼吸器学会誌 = Annals of the Japanese Respiratory Society 4(2), 181-184, 2015-03-10
- NAID 40020410540
- 経口メチルセルロース/アルギン酸液剤の物性に及ぼす薬物の影響
- 下山 哲哉,浦木 睦,高橋 彩,小林 正拓,高畑 雅臣,牧野 陽佑,伊藤 邦彦,小林 道也
- 薬剤学 74(1), 73-83, 2014
- … The present study aimed to determine how the addition of drugs (acetaminophen, mexiletine, metoprolol, ambroxol, loxoprofen, theophylline, ketotifen and salbutamol) affects the rheological and in vitro drug release characteristics of a 2% methylcellulose formulation and of a 2% methylcellulose/0.5% alginate formulation. … The gelation temperature of both formulations significantly increased with the addition of mexiletine and ambroxol, but it was still less than 37°C. …
- NAID 130003398001
- Factors Affecting the Bitterness Intensities of Ten Commercial Formulations of Ambroxol
- , , [他], ,
- Chemical and Pharmaceutical Bulletin 60(8), 949-954, 2012
- … The bitterness of 10 different products with ambroxol as active ingredient, the original and nine generics, were evaluated by human gustatory sensation tests in which the tablets were kept in the mouth, with water, at 20 and 37°C. … The bitterness threshold of ambroxol solution was found to increase when the temperature of the water with which the tablets were taken, was raised from 20 to 37°C. …
- NAID 130001852503
Related Links
- Ambroxol is a secretolytic agent used in the treatment of respiratory diseases associated with viscid or excessive mucus. It is the active ingredient of Mucosolvan, Mucobrox, Mucol, Lasolvan, Mucoangin, Surbronc, Ambolar, and ...
- アンブロキソール塩酸塩(Ambroxol hydrochloride)の検索ならお薬検索QLife（キューライフ）。お医者さんが処方する処方薬と、薬局で買える市販薬(OTC)、の効果と副作用、写真、添付文書、保管方法等を掲載。商品名だけでなく一般名や剤 ...
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