Salbutamol sulfat ( Martindale 28 hal 31) Nama lain : Albuterol sulfat Pemerian : serbuk putih atau hampir putih

Kelarutan : mudah larut dalam air, sukar larut dalam etanol, dalam kloroform dan dalam eter. Stabilitas : stabilitas salbutamol sulfat dalam larutan dapar fosfat berkurang dengan meninngkatnya pH diatas 6,9. Dosis : s.c / i.m 250-500g yang dapat diulang sesudah 4 jam. pH : 3,4 5 Khasiat : obat asma dan bronkhitis kronis. Penyimpanan : dalam wadah tertutup baik dan tidak tembus cahaya. Sterilisasi : Otoklaf Propilen Glikol ( Excipients hal. 407- 408, FI IV hal 712) Pemerian : Cairan kental, jernih, tidak berwarna; rasa khas; praktis tidak berbau; menyerap iar pada udara lembab. Kelarutan : Dapat bercampur dengan air, dengan aseton dan dalam kloroform; larut dalam eter dan dalam beberapa minyak esensial; tetapi tidak dapat bercampur dalam minyak lemak. Konsentrasi : 10-60 % Kegunaan : pengawet (anti mikroba), pelarut atau kosolven yang dapat bercampur dengan air OTT : Dengan bahan pengoksidasi seperti kalium permanganat Stabilitas : Stabil ketika bercampur dengan etanol 95%, dan air. stabil pada suhu sejuk dan dalam wadah tertutup rapat, tapi pada temperature tinggi dan terbuka dapat mengalami oksidasi. Stabil jika dicampurkan dengan etanol (95%), gliserin atau air

Sterilisasi : Dengan otoklaf Penyimpanan : Wadah tertutup rapat, terlindung dari cahaya, dan di tempat sejuk dan kering Aminophyllin (FI IV Hal 90 , Martindale ed.35 hal 1000-1001, Martindale edisi 31 hal1651, DI 2003 hal 3487) Pemerian : Butir atau serbuk putih atau agak kekuningan,bau ammonia lemah, rasa pahit. Kelarutan : Tidak larut dalam etanol dan dalam eter. Larut dalam air. Larutan 1 gram dalam 25ml air menghasilkan larutan jernih; larutan 1gram dalam 5ml air menghablur jika didiamkan dan larut kembali jika ditambah sedikit etilendiamin. PH : 8,6-9,0 (FI IV hal 92) Stabilitas : Stabil pada suhu kamar dan pada PH 3,5-8,6 selama 48 jam pada suhu 25 C. Jika dibiarkan di udara terbuka, perlahan kehilangan etilendiamin dan menyerap karbondioksida dengan melepaskan teofilin. Khasiat : Antiasma, diuretikum, bronkodilator. Wadah dan Penyimpanan : Dalam wadah dosis tunggal bebas karbondioksida dari kaca tipe 1, terlindungi dari cahaya. OTT : asam , klorpromazin HCl, clindamycin phospat, corcotrophin, dimenhidrinat, eritromicin gluceptate, hidralazin HCl, prokain HCl, prametazin HCl, vancomisin HCl. Sterilisasi : otoklaf/filtrasi Dosis : 25 mg/ml (Aminofilin mengandung 84,0 dan 87,4% teofilin dan 13,5 15,0% etilendiamin). (DI 2003 hal 3488, Martindale edisi 31 hal 1651) Rute : Intravena Teofilin (FI IV hal. 783) Pemerian : serbuk hablur putih, tidak berbau, rasa pahit.

Kelarutan sukar larut dalam larutan alkali dan ammonium hidroksida , agak sukar larut dalam etanol, dalam kloroform, dan dalam eter. Stabilitas : stabil di udara Sterilisasi : otoklaf

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Identification

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Identification Name Accession Number Type Salbutamol DB01001 (APRD00553) small molecule

Groups

approved

Description

Salbutamol is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma a selective for beta2 receptors than beta1 receptors giving it higher specificity for pulmonary beta receptors receptors located in the heart. Salbutamol is formulated as a racemic mixture of the R- and S-isomers. Th greater affinity for the beta2-receptor than the S-isomer and the S-isomer has been associated with toxicit of levalbuterol, the single R-isomer of salbutamol. However, the high cost of levalbuterol compared to sa spread use of this enantiomerically pure version of the drug. Salbutamol is generally used for acute episod bronchial asthma, chronic bronchitis and other chronic bronchopulmonary disorders such as chronic obstr (COPD). It is also used prophylactically for exercise-induced asthma.

Structure

Download: MOL | SDF | SMILES | InChI Display: 2D Structure | 3D Structure

Albuterol Albuterol Sulfate Albuterol Sulphate

Synonyms
Levalbuterol Salbutamol Sulfate Salbutamol Sulphate

Salts

Not Available
Name Accuneb Aerolin Airomir Asmaven

Comp

Brand names
Asmol Asthalin Asthavent Broncovaleas Buventol

Cetsim
10

Brand Name

Ingredients Ipratropium Bromide + Salbutamol Sulfate Ipratropium Bromide + Salbutamol Sulfate

Brand mixtures

Combivent Gen-Combo Sterinebs

Categories

Bronchodilator Agents Adrenergic beta-Agonists Tocolytic Agents

CAS number Weight Chemical Formula InChI Key InChI IUPAC Name SMILES Mass Spec Taxonomy Kingdom

18559-94-9 Average: 239.3107 Monoisotopic: 239.152143543 C13H21NO3 InChIKey=NDAUXUAQIAJITI-UHFFFAOYSA-N InChI=1S/C13H21NO3/c1-13(2,3)14-7-12(17)9-4-5-11(16)10(6-9)8-15/h4-6,12,14-17H,7-8H2,1-3H3

Plain Text

4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol CC(C)(C)NCC(O)C1=CC(CO)=C(O)C=C1
Plain Text

Not Available

Organic

Classes

Benzyl Alcohols and Derivatives Phenols and Derivatives Phenethylamines Hydroxy Compounds Benzyl Alcohols and Derivatives Aliphatic and Aryl Amines Phenols and Derivatives Benzene and Derivatives Alcohols and Polyols Amino Alcohols Phenethylamines Aromatic compounds Phenyl Esters

Substructures

Pharmacology

Indication

For symptomatic relief and prevention of bronchospasm due to bronchial asthma, chronic bronchitis, and bronchopulmonary disorders such as COPD.

Pharmacodynamics

Salbutamol (INN) or albuterol (USAN), a moderately selective beta(2)-receptor agonist similar in structu as a bronchodilator to manage asthma and other chronic obstructive airway diseases. The R-isomer, leval bronchodilation while the S-isomer increases bronchial reactivity. The R-enantiomer is sold in its pure fo manufacturer of levalbuterol, Sepracor, has implied (although not directly claimed) that the presence of o fewer side-effects.

Mechanism of action

Salbutamol is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic receptors. Binding of the lungs results in relaxation of bronchial smooth muscles. It is believed that salbutamol increases cAMP adenylate cyclase, and the actions of salbutamol are mediated by cAMP. Increased intracellular cyclic AM cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular lowered intracellular calcium concentration leads to a smooth muscle relaxation and bronchodilation. In a salbutamol inhibits the release of bronchoconstricting agents from mast cells, inhibits microvascular leak clearance. Systemic absorption is rapid following aerosol administration. Not Available Not Available

Absorption Volume of distribution Protein binding

Hydrolyzed by esterases in tissue and blood to the active compound colterol. The drug is also conjugativel O-sulfate. Metabolism

Important The metabolism module of DrugBank is currently in beta. Questions or suggestions? Please co

Substrate Salbutamol

Enzymes

Product Salbutamol 4-O-sulfate

Route of elimination Half life Clearance Toxicity Affected organisms Pathways Pharmacoeconomics

Approximately 72% of the inhaled dose is excreted in the urine within 24 hours, 28% as unchanged drug 1.6 hours Not Available LD50=1100 mg/kg (orally in mice)

Humans and other mammals

Not Available

Manufacturers

Armstrong pharmaceuticals inc Genpharm inc Ivax pharmaceuticals inc sub teva pharmaceuticals usa Pliva inc Schering corp sub schering plough corp Glaxosmithkline Teva global respiratory research llc 3m pharmaceuticals inc

Dey lp Actavis mid atlantic llc Apotex inc richmond hill Apotex inc Bausch and lomb inc Cobalt laboratories inc Copley pharmaceutical inc Hi tech pharmacal co inc Holopack international Landela pharmaceutical Nephron pharmaceuticals corp Nephron corp Novex pharma Roxane laboratories inc Teva parenteral medicines inc Watson laboratories inc Wockhardt eu operations (swiss) ag Amneal pharmaceuticals Mova pharmaceuticals corp Teva pharmaceuticals usa inc Vintage pharmaceuticals llc Vistapharm inc Mylan pharmaceuticals inc Muro pharmaceutical inc Dava pharmaceuticals inc American therapeutics inc Mutual pharmaceutical co inc Sandoz inc Ucb inc Warner chilcott div warner lambert co Breath ltd Sepracor inc Teva Pharmaceuticals 3M Health Care Actavis Group Advanced Pharmaceutical Services Inc. Amerisource Health Services Corp. Apotheca Inc. Apothecon Armstrong Pharmaceuticals Inc. A-S Medication Solutions LLC Aslung Pharmaceutical Lp Atlantic Biologicals Corporation Automatic Liquid Packaging Inc. Bausch & Lomb Inc. Bryant Ranch Prepack Cardinal Health Catalent Pharma Solutions Charter Laboratories Inc. Cipla Ltd.

Packagers

Cobalt Pharmaceuticals Inc. DAVA Pharmaceuticals Dey Pharma LP Direct Dispensing Inc. DispenseXpress Inc. Dispensing Solutions Diversified Healthcare Services Inc. GlaxoSmithKline Inc. H.J. Harkins Co. Inc. Heartland Repack Services LLC Hi Tech Pharmacal Co. Inc. Holopack International Corp. Ivax Pharmaceuticals Kaiser Foundation Hospital Lake Erie Medical and Surgical Supply Major Pharmaceuticals Murfreesboro Pharmaceutical Nursing Supply Mutual Pharmaceutical Co. Mylan Nephron Pharmaceuticals Corp. Novopharm Ltd. Nucare Pharmaceuticals Inc. Odyssey Pharmaceuticals Inc. Palmetto Pharmaceuticals Inc. Patient First Corp. PD-Rx Pharmaceuticals Inc. Pharmedix Physician Partners Ltd. Physicians Total Care Inc. Pliva Inc. Prasco Labs Preferred Pharmaceuticals Inc. Qualitest Quality Care Rebel Distributors Corp. Redpharm Drug Rx Elite Sandhills Packaging Inc. Schering Corp. Sepracor Pharmaceuticals Inc. Southwood Pharmaceuticals Stratus Pharmaceuticals Inc. Teva Pharmaceutical Industries Ltd. UDL Laboratories United Research Laboratories Inc. Vintage Pharmaceuticals Inc. Vistapharm Inc. Warrick Pharmaceuticals Corp. Watson Pharmaceuticals

Form Aerosol, metered Liquid Powder

Route Respiratory (inhalation) Oral Respiratory (inhalation) Intramuscular Intravenous Oral Respiratory (inhalation) Oral Unit description

Dosage forms

Solution Solution Solution Solution Tablet

Xopenex 0.63 mg/3 ml solution Proventil HFA 108 (90 Base)mcg/act Aerosol 6.7 gm Inhaler Xopenex HFA 45 mcg/act Aerosol 15 gm Inhaler AccuNeb 0.63 mg/3ml Neb. Solution 1 Box= 25 Vials AccuNeb 1.25 mg/3ml Neb. Solution 1 Box= 25 Vials

64.2

55.0

53.8

53.1

53.1

Prices

ProAir HFA 108 (90 Base)mcg/act Aerosol 8.5 gm Inhaler Ventolin HFA 108 (90 Base)mcg/act Aerosol 18 gm Inhaler Proair hfa 90 mcg inhaler Proventil hfa 90 mcg inhaler Xopenex hfa 45 mcg inhaler
10

45.9

39.9

12.6

8.07

6.12

DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.

Country United States

Patent Number 7500444 6352684 2125665 2125667

Approved 2005-07-04 1992-11-28 2001-06-12 2000-06-13

2025-07-

Patents

United States Canada Canada

2009-11-

2012-12-

2012-12-

Properties State Experimental solid

Property Value

Properties

melting point water solubility logP logS pKa Property water solubility logP logP logS pKa (strongest acidic) pKa (strongest basic) physiological charge hydrogen acceptor count hydrogen donor count polar surface area rotatable bond count refractivity polarizability

151 C 1.41E+004 mg/L 1.4 -1.22 10.3 Value 2.15e+00 g/l 0.44 0.34 -2 10.12 9.4 1 4 4 72.72 5 67.87 26.86

Y (2

Predicted Properties

References Synthesis Reference General Reference Not Available Not Available

Resource KEGG Drug PubChem Compound PubChem Substance ChemSpider BindingDB ChEBI ChEMBL Therapeutic Targets Database PharmGKB IUPHAR Guide to Pharmacology Drug Product Database RxList Link D02147 2083 46505312 1999 25769 2549 2549 DNC000873 PA448068 558 558 790419 http://www.rxlist.com/cgi/generic/duoneb.htm

External Links

Wikipedia

http://en.wikipedia.org/wiki/Salbutamol

ATC Codes

R03CC02 R03AC02 12:12.08.12 48:12.04.12

AHFS Codes PDB Entries FDA label MSDS Interactions

Not Available Not Available show (52.5 KB)

Drug Amitriptyline Amoxapine Atenolol Bisoprolol Carvedilol Clomipramine Desipramine Doxepin Esmolol Imipramine Isocarboxazid Labetalol

Interaction

The tricyclic antidepressant, amitriptyline, increases the sympathomime Antagonism Antagonism Antagonism

The tricyclic antidepressant, amoxapine, increases the sympathomimetic

The tricyclic antidepressant, clomipramine, increases the sympathomim

The tricyclic antidepressant, desipramine, increases the sympathomimet Antagonism Increased arterial pressure Antagonism Possible increase of arterial pressure Increased arterial pressure Antagonism Increased arterial pressure Moclobemide increases the sympathomimetic effect of salbutamol. Antagonism Antagonism Increased arterial pressure Antagonism Antagonism Increased arterial pressure Increased arterial pressure Antagonism

The tricyclic antidepressant, doxepin, increases the sympathomimetic ef

The tricyclic antidepressant, imipramine, increases the sympathomimeti

Drug Interactions

Linezolid Methyldopa Metoprolol Midodrine Moclobemide Nadolol Nortriptyline Oxprenolol Phenelzine Pindolol Propranolol Rasagiline Reserpine Timolol

The tricyclic antidepressant, nortriptyline, increases the sympathomimet

Food Interactions Targets

Not Available

1. Beta-2 adrenergic receptor Pharmacological action: yes Actions: agonist

Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. T binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine Organism class: human UniProt ID: P07550 Gene: ADRB2 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:

1.
2. 3. 4. 5.

6.

Brichetto L, Milanese M, Song P, Patrone M, Crimi E, Rehder K, Brusasco V: Beclomethasone rapidly ablates allergen-induced beta 2-adre human isolated bronchi. Am J Physiol Lung Cell Mol Physiol. 2003 Jan;284(1):L133-9. Epub 2002 Aug 16. Pubmed Chong LK, Suvarna K, Chess-Williams R, Peachell PT: Desensitization of beta2-adrenoceptor-mediated responses by short-acting beta2-adr mast cells. Br J Pharmacol. 2003 Feb;138(3):512-20. Pubmed Yamanishi T, Chapple CR, Yasuda K, Yoshida K, Chess-Williams R: Role of beta-adrenoceptor subtypes in mediating relaxation of the pig Neurourol Urodyn. 2003;22(4):338-42. Pubmed Brouri F, Hanoun N, Mediani O, Saurini F, Hamon M, Vanhoutte PM, Lechat P: Blockade of beta 1- and desensitization of beta 2-adrenocep cardiac fibrosis. Eur J Pharmacol. 2004 Feb 6;485(1-3):227-34. Pubmed Choudhry S, Ung N, Avila PC, Ziv E, Nazario S, Casal J, Torres A, Gorman JD, Salari K, Rodriguez-Santana JR, Toscano M, Sylvia JS, Al Gomez I, Fagan JK, Salas J, Clark S, Lilly C, Matallana H, Selman M, Chapela R, Sheppard D, Weiss ST, Ford JG, Boushey HA, Drazen JM EK, Burchard EG: Pharmacogenetic differences in response to albuterol between Puerto Ricans and Mexicans with asthma. Am J Respir Cri 15;171(6):563-70. Epub 2004 Nov 19. Pubmed Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Beta-1 adrenergic receptor Pharmacological action: unknown Actions: agonist

Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. T and norepinephrine with approximately equal affinity Organism class: human UniProt ID: P08588 Gene: ADRB1 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report

References:

1.

Baker JG: The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. Br J Pharmacol. 2005 Feb;14

Enzymes 1. Cytochrome P450 3A4 Actions: inhibitor Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide UniProt ID: P08684 Gene: CYP3A4 Protein Sequence: FASTA Gene Sequence: FASTA SNPs: SNPJam Report References:

1.

Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

Comments
Drug created on June 13, 2005 07:24 / Updated on February 08, 2013 16:19
This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.

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