Montelukast drug data and news

Montelukast drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Montelukast
Brand Names/Synonyms Montelukast; Singulair; Singular
Indication For the treatment of asthma
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Description Not Available
Pharmacology Montelukast, like zafirlukast, is a leukotriene receptor antagonist used as an alternative to anti-inflammatory medications in the management and chronic treatment of asthma and exercise-induced bronchospasm (EIB). Unlike zafirlukast, montelukast does not inhibit CYP2C9 or CYP3A4 and is, therefore, not expected to affect the hepatic clearance of drugs metabolized by these enzymes.
Mechanism Of Action Montelukast selectively antagonizes leukotriene D4 (LTD4) at the cysteinyl leukotriene receptor, CysLT1, in the human airway. Montelukast inhibits the actions of LTD4 at the CysLT1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.
Montelukast News
(When available)

Weight May Influence Asthma Care  07 Mar 2006
Researchers say beclomethasone, an inhaled steroid, may be better for normal-weight people asthmatics, while a pill steroid called montelukast sodium (brand ... - Forbes

Over-the-counter drug works well for allergies  Mar 1, 2006
...pseudoephedrine controls nasal allergy symptoms just as well as the more expensive prescription drug Singulair, also known by its generic name, montelukast. ... - Reuters

No Difference Between Over-the-Counter Decongestant and ...  Mar 2, 2006
...indicates that there was no difference between an over-the-counter decongestant (pseudoephedrine) and a prescription medication (montelukast) in relieving ... - DG News

OTC allergy drug keeps pace with Singulair  Feb 20, 2006
...pseudophedrine -- taken in daily doses of 240 mg, works just as well in relieving the symptoms of hay fever as 10 mg daily of montelukast, which costs about ... - United Press International

Over-the-counter Decongestant Equals Prescription Drug In ...  Feb 24, 2006
...found that daily doses of 240 mg of pseudoephedrine hydrochloride (Sudafed® 24 Hour) were just as effective as 10 mg daily of montelukast sodium (Singulair ... - Science Daily (press release)

Prescription drug and OTC decongestant equally effective in ...  Feb 21, 2006
Thirty of them were given prescription decongestant montelukast sodium (Singulair) of 10 milligrams daily, the remainder took decongestant pseudoephedrine ... - Earthtimes.org

OTC Decongestant and Prescription Drug Found Equal for Allergic ...  Feb 20, 2006
20 - Over-the-counter pseudoephedrine and the prescription leukotriene receptor antagonist Singulair (montelukast) were found equally effective in combating ... - MedPage Today,

Asthma Control May Be Weighty Matter  Feb 23, 2006
23 - Obese patients with asthma who are taking oral leukotriene antagonists like Singulair (montelukast) tend to have better control while leaner patients may ... - MedPage Today,

Allergy Relief Can Come Cheaply  Feb 21, 2006
Thirty of the adults took 10 milligrams a day of the prescription decongestant montelukast sodium (Singulair), while the other 28 took 240 miiligrams a day of ... - ABC News

Singulair pill shows more promise for obese people  Feb 23, 2006
Golden says. Singulair is the brand name of montelukast sodium and is sold by Merck & Co., which funded this study. Researchers ... - News-Medical.net,

Don't sniff at cheaper allergy drugs  Feb 21, 2006
...dose of pseudoephedrine hydrochloride (sold over the counter under the brand name Sudafed 24 Hour) and a 10-mg dose of montelukast sodium (prescription brand ... - Globe and Mail,

Two hay fever drugs produce equal results  Feb 20, 2006
...doses of 240 mg of pseudoephedrine hydrochloride (Sudafed 24 Hour) were just as effective as 10 mg daily of prescription-only montelukast sodium (Singulair) at ... - Monsters and Critics.com,

OTC Decongestant Nothing To Sneeze At  Feb 21, 2006
The University of Chicago study included 30 hay fever sufferers who took 10-milligram doses of montelukast (Singulair) each morning for two weeks and 28 who ... - CBS News

OTC Allergy Medicine As Effective As Some Prescriptions  Feb 21, 2006
...reveals that daily doses of 240 mg of pseudoephedrine hydrochloride (Sudafed® 24 Hour) are just as effective as 10 mg daily of montelukast sodium (Singulair ... - All Headline News

OTC allergy drug found to rival Singulair  Feb 21, 2006
The 58-patient study compared the use of Pfizer's non-prescription Sudafed (pseudoephedrine hydrochloride) with Merck & Co's Singulair (montelukast sodium) in ... - Pharmaceutical Business Review

Over-the Counter Allergy Medication Found to Be As Effective As ...  Feb 22, 2006
240-mg dosage of pseudoephedrine) also experienced no more sleep problems or other side effects than people who took prescription Singulair (10-mg montelukast ... - Newsinferno.com,

Study to determine if asthma drugs can reduce need for steroids in ...  Mar 2, 2006
The 30-week trial, called MARS (Montelukast or Azithromycin for Reduction of Inhaled Corticosteroids in Childhood Asthma), is part of a national study ... - Washington University Record,

Testing: Generic Versus Prescription Ends in a Tie  Feb 27, 2006
In daily doses over two weeks, the first took 10 milligrams of Singulair (montelukast sodium), while the second took 240 milligrams of pseudoephedrine (Sudafed ... - New York Times,

Steroid puff best for kids with persistent asthma  Feb 10, 2006
...persistent asthma, treatment with fluticasone (Flovent), an inhaled steroid, was consistently more effective than treatment with montelukast (Singulair), an ... - Reuters.uk,

Body mass effects response to asthma medications  Feb 23, 2006
...her response to Singulair. Singulair is the brand name of montelukast sodium and is sold by Merck & Co., which funded this study. - Hindustan Times,

Drugs Relieve hay Fever Symptoms Equally  Feb 20, 2006
..."Our hypothesis was that montelukast (Singulair) would have additional benefits and pseudophedrine (Sudafed) would interfere with sleep, but when we compared ... - Ivanhoe,

Merck profits edge ahead in fourth quarter  Feb 1, 2006
...in at $1.1 billion, a little ahead of forecasts, on sales of $5.77 billion, helped by a 12% hike in revenues from asthma drug Singulair (montelukast) to $819 ... - Pharma Times (subscription),

Study targets better asthma treatments  Jan 17, 2006
Researchers administered an inhaled corticosteroid (fluticasone propionate) twice daily or an leukotriene receptor antagonist (montelukast) nightly to more ... - Webindia123,

Inhaled Corticosteroids Most Effective for Persistent Asthma in ...  Jan 10, 2006
Response Profiles to Fluticasone and Montelukast in Mild-to-Moderate Persistent Childhood Asthma is featured in the January 2006 issue of the Journal of ... - DG News

ICS Most Effective For Persistent Asthma In Children  Jan 11, 2006
Response Profiles to Fluticasone and Montelukast in Mild-to-Moderate Persistent Childhood Asthma is featured in the January 2006 issue of the Journal of ... - Science Daily (press release)

Inhaled Steroid Controls Asthma Better Than Oral Agent  Jan 12, 2006
Their study compared the inhaled corticosteroid Flovent (fluticasone) with the oral leukotriene receptor antagonist Singulair (montelukast) for asthma control ... - CNN

Study Compares Kids' Asthma Drugs  Jan 19, 2006
The children were divided into two groups. One group received an inhaled corticosteroid (fluticasone propionate) twice daily or an LTRA (montelukast) nightly. ... - Forbes

Merck profits edge ahead in fourth quarter  Feb 1, 2006
...in at $1.1 billion, a little ahead of forecasts, on sales of $5.77 billion, helped by a 12% hike in revenues from asthma drug Singulair (montelukast) to $819 ... - Pharma Times (subscription),

Dr. Reddy's Reports Q3 FY06 Revenue of Rs. 5,902 Million; YoY ...  Jan 24, 2006
Sales from Europe increase by 78% to Rs 384 million. This growth was primarily driven by sales of montelukast, terbinafine and omeprazole pellets. ... - Genetic Engineering News,

Expression of urocortin in rat lung and its effect on pulmonary ...  Jan 11, 2006
...the mast cell stabilizer cromolyn and histamine-1 (H 1 ) receptor antagonist azelastine respectively, but not by the leukotriene receptor antagonist montelukast ... - Journal of Endocrinology

Montelukast (Singulair) Added to Antihistamine or Corticosteroid ...  Nov 11, 2005
...to have similar efficacy to corticosteroid nasal sprays for poorly controlled seasonal allergic rhinitis when combined with montelukast (Singulair), according ... - DG News

No Additional Benefit from Adding Montelukast to Fluticasone ...  Nov 10, 2005
ANAHEIM, CA -- November 10, 2005 -- Adding montelukast (Singulair) to fluticasone propionate may not improve airway inflammation in patients with persistent ... - DG News

Merck Announces New Unisured Discount Program Targeted to More ...  Oct 7, 2005
FOSAMAX(R) (alendronate sodium), MAXALT(R) and MAXALT MLT(R) (rizatriptan benzoate), PROSCAR(R) (finasteride), SINGULAIR (R) (montelukast sodium), TRUSOPT(R ... - Hispanic PR Wire (press release),

Surgery Boosts Quality of Life for Child with Chronic Sinusitis  Sep 22, 2005
The parents reported that children had been given nasal steroids (64 percent), asthma inhalers (64 percent), antibiotics (55 percent), montelukast [Singulair? ... - Newswise (press release)

FDA Approvals: ProQuad, Ambien CR, Singulair  08 Sep 2005
...in children aged 12 months to 12 years; an extended-release formulation of zolpidem tartrate tablets for the treatment of insomnia; and montelukast sodium for ... - Medscape (subscription)

Singulair helpful for kids with asthma and allergies  Sep 7, 2005
NEW YORK (Reuters Health) - The asthma controller Singulair (generic name, montelukast) appears useful and economical for the treatment of children with asthma ... - Reuters.uk,

When an Asthma Drug Has an Inferiority Complex: A Noninferiority ...  Aug 14, 2005
Garcia and colleagues1 report a multicenter, double-blinded, active-control, randomized trial to compare the efficacy of oral montelukast and inhaled ... - RedNova.com,

FDA approves Singulair for perennial allergic rhinitis  Aug 26, 2005
Fda ( Food and Drug Administration ) has approved Singulair ( Montelukast ) for the relief of symptoms of perennial allergic rhinitis ( PAR ), or indoor ... - Xagena.it,

Indications for Singulair® Expand with FDA Approval for Perennial ...  Aug 27, 2005
Merck & Co, Inc announced today that the US Food and Drug Administration (FDA) has approved SINGULAIR® (montelukast sodium) for the relief of symptoms of ... - I-Newswire.com (press release)

Migraine in children  Aug 16, 2005
A Belgian study showed that although montelukast given to infants aged 6-12 months with RSV-positive bronchiolitis did not change the rate of hospitalisation ... - AustralianDoctor.com (subscription),

Indications for Merck's SINGULAIR(R) Expand with FDA Approval for ...  Aug 18, 2005
...announced today that the US Food and Drug Administration (FDA) has approved SINGULAIR(R) (montelukast sodium) for the relief of symptoms of perennial allergic ... - Business Wire (press release),

Asthma Drug Helps Kids with Sleep Apnea  Aug 5, 2005
5 (HealthDay News) -- The oral anti-inflammatory drug montelukast -- used to treat asthma and allergic rhinitis -- appears to be an effective alternative ... - Atlanta Journal Constitution (subscription)

Vitamin D low in hip patients  Aug 2, 2005
Singulair, known generically as montelukast, is usually prescribed for treating asthma and can be given to kids as a chewable tablet. ... - Ottawa Sun

New therapy avoids tonsilectomy  Aug 1, 2005
In a 16-week study involving 24 young people, researchers employed montelukast, an anti-inflammatory agent used in asthma and allergic rhinitis. ... - myDNA.com

American Thoracic Society Journal news tips for August 2005 (first ...  Aug 1, 2005
In a 16-week study involving 24 young people, researchers employed montelukast, an anti-inflammatory agent used in asthma and allergic rhinitis. ... - EurekAlert

Singulair eases sleep-disordered breathing in kids  Aug 1, 2005
Singulair, known generically as montelukast, is usuallyprescribed for treating asthma and can be given to kids as achewable tablet. ... - Leading The Charge

New Data Reinforces Use of Singulair(tm) in Asthma Patients with ...  Jul 9, 2005
Singulair(tm) (montelukast) significantly improved symptoms of both allergic rhinitis and asthma, compared to placebo, in asthma patients who also suffer from ... - I-Newswire.com (press release)

Dosage Forms Oral tablets
Drug_Category Antiarrhythmic Agents; Unclassified Therapeutic Agents (92:00.00); ATC:R03DC03
Absorption rapidly absorbed following oral administration (bioavailability is 64%)
Interactions -->Interactions for Montelukast:

Montelukast at a Dose of 10 mg Once Daily Dosed to Pharmacokinetic Steady State

  • did not cause clinically significant changes in the kinetics of a single intravenous dose of theophylline (predominantly a cytochrome P450 1A2 substrate).
  • did not change the pharmacokinetic profile of warfarin (a substrate of cytochromes P450 2A6 and 2C9) or influence the effect of a single 30-mg oral dose of warfarin on prothrombin time or the INR (International Normalized Ratio).
  • did not change the pharmacokinetic profile or urinary excretion of immunoreactive digoxin.
  • did not change the plasma concentration profile of terfenadine (a substrate of cytochrome P450 3A4) or fexofenadine, its carboxylated metabolite, and did not prolong the QTc interval following co-administration with terfenadine 60 mg twice daily.
Montelukast at Doses of ³100 mg Daily Dosed to Pharmacokinetic Steady State:
  • did not significantly alter the plasma concentrations of either component of an oral contraceptive containing norethindrone 1 mg/ethinyl estradiol 35 mcg.
  • did not cause any clinically significant change in plasma profiles of prednisone or prednisolone following administration of either oral prednisone or intravenous prednisolone.

Phenobarbital, which induces hepatic metabolism, decreased the AUC of montelukast approximately 40% following a single 10-mg dose of montelukast. No dosage adjustment for montelukast is recommended. It is reasonable to employ appropriate clinical monitoring when potent cytochrome P450 enzyme inducers, such as phenobarbital or rifampin, are co-administered with montelukast.

Montelukast has been administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma with no apparent increase in adverse reactions. In drug-interaction studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following drugs: theophylline, prednisone, prednisolone, oral contraceptives (norethindrone 1 mg/ethinyl estradiol 35 mcg), terfenadine, digoxin, and warfarin.

Although additional specific interaction studies were not performed, montelukast was used concomitantly with a wide range of commonly prescribed drugs in clinical studies without evidence of clinical adverse interactions. These medications included thyroid hormones, sedative hypnotics, non-steroidal anti-inflammatory agents, benzodiazepines, and decongestants.

Phenobarbital, which induces hepatic metabolism, decreased the AUC of montelukast approximately 40% following a single 10-mg dose of montelukast. No dosage adjustment for montelukast is recommended. It is reasonable to employ appropriate clinical monitoring when potent cytochrome P450 enzyme inducers, such as phenobarbital or rifampin, are co-administered with montelukast.

Toxicity Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness
Organisms Affected Humans and other mammals
Chemical IUPAC Name 2-[1-[[1-[3-[2-(7-chloroquinolin-2-yl)ethenyl]phenyl]-3-[2-(1-hydroxy-1-methyl-ethyl)phenyl]-propyl]sulfanylmethyl]cyclopropyl]ethanoicacid
Chemical Formula C35H36ClNO3S
Molecular Weight 586.184 g/mol
Smiles String CC(C)(C1=CC=CC=C1CCC(C2=CC=CC(=C2)C=CC3=NC4=C(C=CC(=C4)Cl)C=C3)SCC5(CC5)CC(=O)O)O
Melting Point Not Available
Water Solubility Not Available
State hygroscopic, optically active, white to off-white powder
LogP/Hphobicity 8.488
Isoelectric Point Not Available
Biotransformation Hepatic
Half Life 2.7-5.5 hours
Protein Binding [%] 99% (to plasma proteins)
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Montelukast.html
http://www.rxlist.com/cgi/generic3/monteluk.htm
Drug Type Approved Drug
Accession No APRD00434
CAS Registry Number 158966-92-8
KEGG Compound ID C07482
PubChem ID SID:65422
PharmGKB ID PA450546
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] 2243602

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