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 250-500µg 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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targets (2) enzymes (1) Show Drugs w ith Similar Structures
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Identification
Name
Salbutamol
Accession Number
DB01001 (APRD00553)
Type
small molecule
drugs
Groups
approved
Description
Salbutamol is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma selective for beta2 receptors than beta1 receptors giving it higher specificity for pulmonary beta receptor 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 toxici of levalbuterol, the single R-isomer of salbutamol. However, the high cost of levalbuterol compared to s spread use of this enantiomerically pure version of the drug. Salbutamol is generally used for acute episo bronchial asthma, chronic bronchitis and other chronic bronchopulmonary disorders such as chronic obst (COPD). It is also used prophylactically for exercise-induced asthma.
Structure
Download: MOL | SDF | SMILES | InChI Display: 2D Structure | 3D Structure
Albuterol Albuterol Sulfate Synonyms
Albuterol Sulphate Levalbuterol Salbutamol Sulfate Salbutamol Sulphate
Salts
Not Available
Name Accuneb Aerolin Airomir Asmaven Brand names
Asmol Asthalin Asthavent Broncovaleas Buventol
Com
Cetsim 10
Brand Name Brand mixtures
Combivent
Ipratropium Bromide + Salbutamol Sulfate
Gen-Combo Sterinebs
Ipratropium Bromide + Salbutamol Sulfate
Categories
Ingredients
Bronchodilator Agents Adrenergic beta-Agonists Tocolytic Agents
CAS number
18559-94-9
Weight
Average: 239.3107 Monoisotopic: 239.152143543
Chemical Formula
C 13H21 NO3
InChI Key
InChIKey=NDAUXUAQIAJITI-UHFFFAOYSA-N
InChI
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
IUPAC Name
4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol
SMILES
CC(C)(C)NCC(O)C1=CC(CO)=C(O)C=C1
Mass Spec
Not Available
Plain Text
Plain Text
Taxonomy
Kingdom
Organic
Classes
Substructures
Pharmacology
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
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 o the lungs results in relaxation of bronchial smooth muscles. It is believed that salbutamol increases cAM adenylate cyclase, and the actions of salbutamol are mediated by cAMP. Increased intracellular cyclic A cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellula lowered intracellular calcium concentration leads to a smooth muscle relaxation and bronchodilation. In salbutamol inhibits the release of bronchoconstricting agents from mast cells, inhibits microvascular leak clearance.
Absorption
Systemic absorption is rapid following aerosol administration.
Volume of distribution
Not Available
Protein binding
Not Available Hydrolyzed by esterases in tissue and blood to the active compound colterol. The drug is also conjugative O-sulfate.
Metabolism
Important The metabolism module of DrugBank is currently in beta . Questions or suggestions? Please co
Substrate
Enzymes
Salbutamol
Product Salbutamol 4-O-sulfate
Route of elimination
Approximately 72% of the inhaled dose is excreted in the urine within 24 hours, 28% as unchanged drug
Half life
1.6 hours
Clearance
Not Available
Toxicity
LD 50=1100 mg/kg (orally in mice)
Affected organisms Pathways
Humans and other mammals
Not Available
Pharmacoeconomics
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
Packagers
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.
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
Dosage forms
Route
Aerosol, metered
Respiratory (inhalation)
Liquid
Oral
Powder
Respiratory (inhalation)
Solution
Intramuscular
Solution
Intravenous
Solution
Oral
Solution
Respiratory (inhalation)
Tablet
Oral Unit description
Prices
Xopenex 0.63 mg/3 ml solution
64.
Proventil HFA 108 (90 Base)mcg/act Aerosol 6.7 gm Inhaler
55.
Xopenex HFA 45 mcg/act Aerosol 15 gm Inhaler
53.
AccuNeb 0.63 mg/3ml Neb. Solution 1 Box= 25 Vials
53.
AccuNeb 1.25 mg/3ml Neb. Solution 1 Box= 25 Vials
53.
ProAir HFA 108 (90 Base)mcg/act Aerosol 8.5 gm Inhaler
45.
Ventolin HFA 108 (90 Base)mcg/act Aerosol 18 gm Inhaler
39.
Proair hfa 90 mcg inhaler
12.
Proventil hfa 90 mcg inhaler
8.0
Xopenex hfa 45 mcg inhaler
6.1 10
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Country
Patents
Patent Number
Approved
United States
7500444
2005-07-04
2025-07
United States
6352684
1992-11-28
2009-11
Canada
2125665
2001-06-12
2012-12
Canada
2125667
2000-06-13
2012-12
Properties
State
solid
Experimental
Property
Value
S
Properties
Predicted Properties
melting point
151 °C
water solubility
1.41E+004 mg/L
logP
1.4
logS
-1.22
pKa
10.3
Property
Value
water solubility
2.15e+00 g/l
logP
0.44
logP
0.34
logS
-2
pKa (strongest acidic)
10.12
pKa (strongest basic)
9.4
physiological charge
1
hydrogen acceptor count
4
hydrogen donor count
4
polar surface area
72.72
rotatable bond count
5
refractivity
67.87
polarizability
26.86
(
References
Synthesis Reference
Not Available
General Reference
Not Available
External Links
Resource
Link
KEGG Drug
D02147
PubChem Compound
2083
PubChem Substance
46505312
ChemSpider
1999
BindingDB
25769
ChEBI
2549
ChEMBL
2549
Therapeutic Targets Database
DNC000873
PharmGKB
PA448068
IUPHAR
558
Guide to Pharmacology
558
Drug Product Database
790419
RxList
http://www.rxlist.com/cgi/generic/duoneb.htm
Wikipedia
ATC Codes
AHFS Codes
http://en.wikipedia.org/wiki/Salbutamol
R03CC02 R03AC02
12:12.08.12 48:12.04.12
PDB Entries
Not Available
FDA label
Not Available
MSDS
show (52.5 KB)
Interactions
Drug Interactions
Drug
Interaction
Amitriptyline
The tricyclic antidepressant, amitriptyline, increases the sympathomim
Amoxapine
The tricyclic antidepressant, amoxapine, increases the sympathomimeti
Atenolol
Antagonism
Bisoprolol
Antagonism
Carvedilol
Antagonism
Clomipramine
The tricyclic antidepressant, clomipramine, increases the sympathomi
Desipramine
The tricyclic antidepressant, desipramine, increases the sympathomime
Doxepin
The tricyclic antidepressant, doxepin, increases the sympathomimetic e
Esmolol
Antagonism
Imipramine
The tricyclic antidepressant, imipramine, increases the sympathomimeti
Isocarboxazid
Increased arterial pressure
Labetalol
Antagonism
Linezolid
Possible increase of arterial pressure
Methyldopa
Increased arterial pressure
Metoprolol
Antagonism
Midodrine
Increased arterial pressure
Moclobemide
Moclobemide increases the sympathomimetic effect of salbutamol.
Nadolol
Antagonism
Nortriptyline
The tricyclic antidepressant, nortriptyline, increases the sympathomime
Oxprenolol
Antagonism
Phenelzine
Increased arterial pressure
Pindolol
Antagonism
Propranolol
Antagonism
Rasagiline
Increased arterial pressure
Reserpine
Increased arterial pressure
Timolol
Antagonism
Food Interactions
Not Available
Targets 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. 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 1 6.Pubmed Chong LK, Suvarna K, Chess-Williams R, Peachell PT: Desensitization of b eta2-adrenoceptor-mediated responses b y short-acting beta2-ad 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-adrenoce 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, Dr azen J EK, Burchard EG: Pharmacogenetic differences in response to albuterol between Puerto Ricans and Mexicans with asthma. Am J Respir Cr 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. 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;1
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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