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Encyclopedia > Montelukast
Montelukast
Systematic (IUPAC) name
2-[1-[[(1R)-1-[3-[2-(7-chloroquinolin-2-yl)ethenyl]
phenyl]-3-[2-(2-hydroxypropan-2-yl)phenyl]propyl]
sulfanylmethyl]cyclopropyl]acetic acid
Identifiers
CAS number 158966-92-8
ATC code R03DC03
PubChem 60951
DrugBank APRD00434
Chemical data
Formula C35H36ClNO3S 
Mol. mass 586.184 g/mol
Pharmacokinetic data
Bioavailability 63% to 73%
Protein binding 99%
Metabolism Hepatic (CYP3A4 and CYP2C9-mediated)
Half life 2.7-5.5 hours
Excretion Biliary
Therapeutic considerations
Pregnancy cat.

B (U.S.), B1 (Au) Image File history File links Singulair. ... IUPAC nomenclature is a system of naming chemical compounds and of describing the science of chemistry in general. ... CAS registry numbers are unique numerical identifiers for chemical compounds, polymers, biological sequences, mixtures and alloys. ... The Anatomical Therapeutic Chemical Classification System is used for the classification of drugs. ... A section of the Anatomical Therapeutic Chemical Classification System. ... PubChem is a database of chemical molecules. ... The DrugBank database available at the University of Alberta is a unique bioinformatics and cheminformatics resource that combines detailed drug (i. ... This article or section does not cite any references or sources. ... General Name, symbol, number carbon, C, 6 Chemical series nonmetals Group, period, block 14, 2, p Appearance black (graphite) colorless (diamond) Standard atomic weight 12. ... General Name, Symbol, Number hydrogen, H, 1 Chemical series nonmetals Group, Period, Block 1, 1, s Appearance colorless Atomic mass 1. ... General Name, symbol, number chlorine, Cl, 17 Chemical series halogens Group, period, block 17, 3, p Appearance yellowish green Standard atomic weight 35. ... General Name, symbol, number nitrogen, N, 7 Chemical series nonmetals Group, period, block 15, 2, p Appearance colorless gas Standard atomic weight 14. ... General Name, Symbol, Number oxygen, O, 8 Chemical series nonmetals, chalcogens Group, Period, Block 16, 2, p Appearance colorless (gas) very pale blue (liquid) Standard atomic weight 15. ... General Name, Symbol, Number sulfur, S, 16 Chemical series nonmetals Group, Period, Block 16, 3, p Appearance lemon yellow Standard atomic weight 32. ... The molecular mass (abbreviated Mr) of a substance, formerly also called molecular weight and abbreviated as MW, is the mass of one molecule of that substance, relative to the unified atomic mass unit u (equal to 1/12 the mass of one atom of carbon-12). ... BIC pen cap, about 1 gram. ... The mole (symbol: mol) is the SI base unit that measures an amount of substance. ... In pharmacology, bioavailability is used to describe the fraction of an administered dose of unchanged drug that reaches the systemic circulation, one of the principal pharmacokinetic properties of drugs. ... A drugs efficacy may be affected by the degree to which it binds to the proteins within blood plasma. ... Drug metabolism is the metabolism of drugs, their biochemical modification or degradation, usually through specialized enzymatic systems. ... The liver is an organ present in vertebrates and some other animals. ... Cytochrome P450 3A4 (abbreviated CYP3A4) (EC 1. ... Cytochrome P450 2C9 (abbreviated CYP2C9), a member of the cytochrome P450 mixed-function oxidase system, is involved in the metabolism of xenobiotics in the body. ... It has been suggested that Effective half-life be merged into this article or section. ... Excretion is the process of eliminating waste products of metabolism and other materials that are of no use. ... The pregnancy category of a pharmaceutical agent is an assessment of the risk of fetal injury due to the pharmaceutical, if it is used as directed by the mother during pregnancy. ... Motto: (Out Of Many, One) (traditional) In God We Trust (1956 to date) Anthem: The Star-Spangled Banner Capital Washington D.C. Largest city New York City None at federal level (English de facto) Government Federal constitutional republic  - President George Walker Bush (R)  - Vice President Dick Cheney (R) Independence from... For other uses, see Australia (disambiguation). ...

Legal status

℞-only (U.S.), POM (UK), S4 (Au) The regulation of therapeutic goods, that is drugs and therapeutic devices, varies by jurisdiction. ... A prescription drug is a licensed medicine that is regulated by legislation to require a prescription before it can be obtained. ...

Routes Oral

Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific locus of operation, it does not interact with other allergy medications such as theophylline. In pharmacology and toxicology, a route of administration is the path by which a drug, fluid, poison or other substance is brought into contact with the body 1. ... Leukotrienes are autocrine and paracrine eicosanoid lipid mediators derived from arachidonic acid by 5-lipoxygenase. ... An allergy is an abnormal, acquired sensitivity to a given substance, including pollen, drugs, or numerous environmental triggers. ... Leukotrienes are autocrine and paracrine eicosanoid lipid mediators derived from arachidonic acid by 5-lipoxygenase. ... Bronchoconstriction is the constriction of the airways in the lungs due to the tighting of surrounding smooth muscle, with consequent coughing, wheezing, and shortness of breath. ... Asthma is a chronic lung condition affecting populations around the world. ... Theophylline is a methylxanthine drug used in therapy for respiratory diseases such as COPD or asthma under a variety of brand names. ...


Montelukast is marketed in United States and many other countries by Merck & Co. with the brand name Singulair®. It is available as oral tablets, chewable tablets, and oral granules. In India and other countries, it is also marketed under the brand name Montair®, produced by Indian company Cipla. Merck & Co. ... This article does not cite any references or sources. ... An assortment of grains The word grain has a great many meanings, most being descriptive of a small piece or particle. ... Cipla is an Indian pharmaceutical company, best-known for manufacturing cheap anti-AIDS drugs. ...


Side effects

Side effects include gastrointestinal disturbances, hypersensitivity reactions, sleep disorders and increased bleeding tendency, aside from many other generic adverse reactions. Its use is associated with a higher incidence of Churg-Strauss syndrome (whether or not this drug is 'unmasking' subclinical Churg-Strauss is as yet uncertain). An adverse drug reaction (abbreviated ADR) is a term to describe the unwanted, negative consequences sometimes associated with the use of medications. ... Upper and Lower gastrointestinal tract The gastrointestinal tract (GI tract), also called the digestive tract, or the alimentary canal, is the system of organs within multicellular animals that takes in food, digests it to extract energy and nutrients, and expels the remaining waste. ... Hypersensitivity refers to undesirable (damaging, discomfort-producing and sometimes fatal) reactions produced by the normal immune system. ... This article does not cite any references or sources. ... Churg-Strauss syndrome is a necrotizing vasculitis characterized by eosinophilia. ...


References

  • Lipkowitz, Myron A. and Navarra, Tova (2001) The Encyclopedia of Allergies (2nd ed.) Facts on File, New York, p. 178, ISBN 0-8160-4404-X

External links

v • d • e
Drugs for obstructive airway diseases: asthma/COPD (R03)
Adrenergics, inhalants Short acting β2-agonists: Salbutamol/Levosalbutamol • Fenoterol • Terbutaline
Long acting β2-agonists (LABA): Bambuterol • Clenbuterol • Formoterol • Salmeterol
other: Epinephrine • Isoproterenol • Orciprenaline
Glucocorticoids Beclometasone • Budesonide • Ciclesonide • Fluticasone • Mometasone
Anticholinergics Ipratropium • Tiotropium
Mast cell stabilizers Cromoglicate • Nedocromil
Xanthines Aminophylline • Theobromine • Theophylline
Leukotriene antagonists Montelukast • Pranlukast • Zafirlukast
Combination products Budesonide/formoterol • Fluticasone/salmeterol • Ipratropium/salbutamol
 v • d • e Merck & Co., Inc.

Corporate Directors: Lawrence Bossidy | William Bowen | Richard Clark | Johnnetta Cole | William Harrison | William Kelley | Rochelle Lazarus | Thomas Shenk | Anne Tatlock | Samuel Thier | Wendell Weeks | Peter Wendell Chronic obstructive pulmonary disease (COPD), also known as chronic obstructive airway disease (COAD), is a group of diseases characterized by limitation of airflow in the airway that is not fully reversible. ... A section of the Anatomical Therapeutic Chemical Classification System. ... Beta2-adrenergic receptor agonists are a class of drugs used to treat asthma and other pulmonary disease states. ... Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and COPD. Salbutamol sulphate is usually given by the inhaled route for direct effect on bronchial smooth muscle. ... Levosalbutamol (INN) or levalbuterol (USAN), trade name Xopenex, is the R-enantiomer of the short-acting β2-adrenergic receptor agonist albuterol (salbutamol). ... Fenoterol is an asthma medication designed to open up the airways to the lungs. ... The drug Terbutaline (trade names Brethine, Bricanyl, or Brethaire) is a β2-adrenergic receptor agonist, used as a fast-acting bronchodilator and off-label to delay premature labour as a tocolytic. ... Long acting beta-adrenoceptor agonists include formoterol, salmeterol and are usually prescribed for moderate to severe persistent asthma patients or patients with COPD. They are designed to replace the shorter acting B2-agonists such as salbutamol, as they have a duration of action of approximately 12 hours in comparison with... Bambuterol (INN, marketed by AstraZeneca under the trade names Bambec® and Oxeol®) is a long acting beta-adrenoceptor agonist used in the treatment of asthma. ... Clenbuterol is a drug prescribed to sufferers of breathing disorders as a decongestant and bronchodilator. ... Formoterol belongs to the family of prescription-only medicines known as beta 2-agonists. ... Salmeterol is a long-acting beta2-adrenergic receptor agonist drug that is currently prescribed for the treatment of asthma and chronic obstructive pulmonary disease COPD. It is currently available in both dry-powder inhalers (DPIs) and pressurised metered dose inhalers (pMDIs). ... “Adrenaline” redirects here. ... Isoproterenol hydrochloride (Medihaler-Iso®) is a beta adrenergic receptor agonist medication, used as an inhaled aerosol to treat asthma. ... Orciprenaline (INN, also known as metaproterenol) is a bronchodilator used in the treatment of asthma. ... Glucocorticoids are a class of steroid hormones characterised by an ability to bind with the cortisol receptor and trigger similar effects. ... Beclometasone dipropionate (INN, Beclomethasone dipropionate (BAN) is a corticosteroid drug. ... Budesonide is a glucocorticoid steroid for the treatment of asthma, non-infectious rhinitis (including hay fever and other allergies), and for treatment and prevention of nasal polyposis. ... Ciclesonide is a glucocorticoid used to treat obstructive airway diseases. ... Fluticasone proprionate is a glucocorticoid often prescribed as treatment for asthma and allergic rhinitis. ... Mometasone furoate (also referred to as Mometasone) is a moderately potent glucocorticoid steroid used in the treatment of inflammatory skin disorders (such as eczema and psoriasis), allergic rhinitis (such as hayfever), and asthma for patients unresponsive to less potent corticosteroids. ... An anticholinergic agent is a member of a class of pharmaceutical compounds which serve to reduce the effects mediated by acetylcholine in the central nervous system and peripheral nervous system. ... Sources Brenner, G. M. (2000). ... Tiotropium (IPA: ) is a long-acting anticholinergic bronchodilator used in the management of chronic obstructive pulmonary disease (COPD). ... Mast cell stabilizers are medications used to prevent or control certain allergic disorders. ... Cromoglicate (INN) (also referred to as cromolyn (USAN) or cromoglycate (former BAN)) is traditionally described as a mast cell stabilizer, and is commonly marketed as the sodium salt sodium cromoglicate. ... The introduction to this article provides insufficient context for those unfamiliar with the subject matter. ... Xanthines are a group of alkaloids that are commonly used for their effects as mild stimulants and as bronchodilators, notably in treating the symptoms of asthma. ... Aminophylline is a drug combination that contains theophylline and ethylenediamine in 2:1 ratio. ... Theobromine, also known as xantheose,[1] is a bitter alkaloid of the cacao plant. ... Theophylline is a methylxanthine drug used in therapy for respiratory diseases such as COPD or asthma under a variety of brand names. ... A leukotriene antagonist is a hormone antagonist acting upon leukotrienes. ... Pranlukast is a cysteinyl leukotriene receptor-1 antagonist. ... Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma. ... Unopened Symbicort Turbuhaler (left) and opened (middle and right) Budesonide/formoterol is a combination formulation containing budesonide and formoterol used in the management of asthma and chronic obstructive pulmonary disease (COPD) in the EU. It is marketed by AstraZeneca under the trade name Symbicort. ... Fluticasone Propionate The Diskus device Inner Workings of Diskus The combination preparation fluticasone/salmeterol is a formulation containing fluticasone propionate and salmeterol xinafoate used in the management of asthma and chronic obstructive pulmonary disease (COPD). ... The combination preparation ipratropium/salbutamol is a formulation containing ipratropium bromide and salbutamol sulfate (albuterol sulfate) used in the management of chronic obstructive pulmonary disease (COPD) and asthma. ... Merck & Co. ... For other uses, see Corporation (disambiguation). ... In relation to a company, a director is an officer (that is, someone who works for the company) charged with the conduct and management of its affairs. ... Lawrence A. Bossidy (Larry) (born 1944?) is a businessman and author. ... William G. Bowen is the current president of the Andrew W. Mellon Foundation. ... For people of the same name, please see Richard Clark. ... Johnnetta B. Cole (born October 19, 1936) is an American academic who served as the first African American female president of Spelman College. ... William B. Harrison, Jr. ... William Donald Kelley, DDS, MS (b. ... Thomas Shenk is a professor of Molecular Biology at Princeton University, specializing in biochemistry, cell biology, genetics, genomics, and microbiology & virology. ...

Key products: Indinavir | Aprepitant | Alendronate | Rizatriptan | Finasteride | Montelukast | Rofecoxib | Ezetimibe/simvastatin | Ezetimibe | Simvastatin | The Merck Index | The Merck Manual Categories: Possible copyright violations ... Aprepitant (brand name: Emend™) is a medication, that is used in the treatment of chemotherapy induced nausea / emesis. ... Alendronate (Fosamax, Merck) is a bisphosphonate drug used for osteoporosis and several other bone diseases. ... Rizatriptan (Maxalt®) is a triptan drug developed by Merck & Co. ... Finasteride (marketed as Proscar, Propecia, Fincar, Finpecia, Finax, Finast, Finara, Finalo, Prosteride, Gefina, Finasterid IVAX) is an antiandrogen which acts by inhibiting type II 5-alpha reductase, the enzyme that converts testosterone to dihydrotestosterone (DHT). ... Rofecoxib (IPA: ) is a nonsteroidal anti-inflammatory drug (NSAID) developed by Merck & Co. ... Ezetimibe/simvastatin (IPA: ) is a drug combination used for the treatment of dyslipidemia. ... Ezetimibe (IPA: ) is an anti-hyperlipidemic medication which is used to lower cholesterol levels. ... Simvastatin (INN) (IPA: ) is a hypolipidemic drug belonging to the class of pharmaceuticals called statins. It is used to control hypercholesterolemia (elevated cholesterol levels) and to prevent cardiovascular disease. ... The Merck Index is an encyclopedia of chemicals, drugs and biologicals with over 10,000 monographs on single substances or groups of related compounds. ... The Merck Manual of Diagnosis and Therapy (often referred to simply as The Merck Manual) is one of the worlds most widely used medical textbooks. ...

Annual Revenue: $22.9 billion USD ( 2% FY 2004) | Employees: 63,000 | Stock Symbol: NYSE: MRK | Website: www.merck.com The United States dollar is the official currency of the United States. ... Image File history File links No higher resolution available. ... A fiscal year (or financial year or accounting reference date) is a 12-month period used for calculating annual (yearly) financial reports in businesses and other organizations. ... The New York Stock Exchange (NYSE), nicknamed the Big Board, is a New York City-based stock exchange. ...


  Results from FactBites:
 
Mosby's Drug Consult Top 200 (6819 words)
The efficacy of montelukast sodium in pediatric patients 6-14 years of age was demonstrated in one 8 week double-blind, placebo-controlled trial in 336 patients (201 treated with montelukast sodium and 135 treated with placebo) using an inhaled β-agonist on an “as-needed” basis.
The efficacy of montelukast sodium for the chronic treatment of asthma in pediatric patients 2-5 years of age was explored in a 12 week placebo-controlled safety and tolerability study in 689 patients, 461 of whom were treated with montelukast sodium.
Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in adults and pediatric patients 2 years of age and older.
West Virginia Center for Drug and Health Information (911 words)
Background: Montelukast is an effective therapy for the control of asthma exacerbations in adults and children with persistent asthma, which makes it a potential treatment modality for children with intermittent asthma.
Objective: The purpose of the study was to investigate the role of montelukast in the prevention of viral-induced asthma exacerbations in children aged 2 to 5 years with a history of intermittent asthma symptoms.
Montelukast reduces asthma exacerbations in 2- to 5-year-old children with intermittent asthma.
  More results at FactBites »


 

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