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Home / Drugs / Starting with S / Salbutamol
 
Salbutamol
 

Salbutamol is a short-acting, selective beta2-adrenergic receptor agonist used in the treatment of asthma and COPD. It is 29 times more selective for beta2 receptors than beta1 receptors giving it higher specificity for pulmonary beta receptors versus beta1-adrenergic receptors located in the heart. Salbutamol is formulated as a racemic mixture of the R- and S-isomers. The R-isomer has 150 times greater affinity for the beta2-receptor than the S-isomer and the S-isomer has been associated with toxicity. This lead to the development of levalbuterol, the single R-isomer of salbutamol. However, the high cost of levalbuterol compared to salbutamol has deterred wide-spread use of this enantiomerically pure version of the drug. Salbutamol is generally used for acute episodes of bronchospasm caused by bronchial asthma, chronic bronchitis and other chronic bronchopulmonary disorders such as chronic obstructive pulmonary disorder (COPD). It is also used prophylactically for exercise-induced asthma.
BrandsAccuneb
Aerolin
Airomir
Asmaven
Asmol
Asthalin
Asthavent
Broncovaleas
Buventol
Cetsim
Cobutolin
Ecovent
Loftan
ProAir
ProAir HFA
Proventil
Proventil HFA
Rotahaler
Salamol
Salbulin
Salbutard
Salbutine
Salbuvent
Solbutamol
Sultanol
Venetlin
Ventalin Inhaler
Ventolin
Ventolin HFA
Ventolin Inhaler
Ventolin Rotacaps
Volma
Volmax
Xopenex
Xopenex HFA
CategoriesBronchodilator Agents
Adrenergic beta-Agonists
Tocolytic Agents
ManufacturersArmstrong 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
Packagers3M 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
SynonymsAlbuterol
Albuterol Sulfate
Albuterol Sulphate
Levalbuterol
Salbutamol Sulfate
Salbutamol Sulphate

indication

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

pharmacology

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

mechanism of action

Salbutamol is a beta(2)-adrenergic agonist and thus it stimulates beta(2)-adrenergic receptors. Binding of albuterol to beta(2)-receptors in the lungs results in relaxation of bronchial smooth muscles. It is believed that salbutamol increases cAMP production by activating adenylate cyclase, and the actions of salbutamol are mediated by cAMP. Increased intracellular cyclic AMP increases the activity of cAMP-dependent protein kinase A, which inhibits the phosphorylation of myosin and lowers intracellular calcium concentrations. A lowered intracellular calcium concentration leads to a smooth muscle relaxation and bronchodilation. In addition to bronchodilation, salbutamol inhibits the release of bronchoconstricting agents from mast cells, inhibits microvascular leakage, and enhances mucociliary clearance.

toxicity

LD50=1100 mg/kg (orally in mice)

biotransformation

Hydrolyzed by esterases in tissue and blood to the active compound colterol. The drug is also conjugatively metabolized to salbutamol 4'-O-sulfate.

absorption

Systemic absorption is rapid following aerosol administration.

half life

1.6 hours

route of elimination

Approximately 72% of the inhaled dose is excreted in the urine within 24 hours, 28% as unchanged drug and 44% as metabolite.

drug interactions

Amitriptyline: The tricyclic antidepressant, amitriptyline, increases the sympathomimetic effect of salbutamol.

Amoxapine: The tricyclic antidepressant, amoxapine, increases the sympathomimetic effect of salbutamol.

Atenolol: Antagonism

Bisoprolol: Antagonism

Carvedilol: Antagonism

Clomipramine: The tricyclic antidepressant, clomipramine, increases the sympathomimetic effect of salbutamol.

Desipramine: The tricyclic antidepressant, desipramine, increases the sympathomimetic effect of salbutamol.

Doxepin: The tricyclic antidepressant, doxepin, increases the sympathomimetic effect of salbutamol.

Esmolol: Antagonism

Imipramine: The tricyclic antidepressant, imipramine, increases the sympathomimetic effect of salbutamol.

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 sympathomimetic effect of salbutamol.

Oxprenolol: Antagonism

Phenelzine: Increased arterial pressure

Pindolol: Antagonism

Propranolol: Antagonism

Rasagiline: Increased arterial pressure

Reserpine: Increased arterial pressure

Timolol: Antagonism