Singulair: profile and news






Glaxo to remain the asthma king  May 15, 2006
Analysts say that the Advair/Serevent franchise won't get blown away by Singulair or Symbicort. By Aaron Smith, CNNMoney.com staff writer. ... - CNNMoney.com

Merck Q1 Profit Rises On Strong US Zocor, Singulair Sales; Guides ...  Apr 20, 2006
Co., Inc. (MRK | charts | news | PowerRating) said first-quarter profit rose on strong US sales of Zocor and Singulair. This came ... - Trading Markets,

I WAS THE EPITOME OF HEALTH UNTIL MY LIFE BECAME A TOXIC HELL  May 14, 2006
...concluded. Miscanic now walks around with an inhaler and takes three drugs to help him breathe: Advair, Pulmicort and Singulair. ... - New York Post,

Professor develops asthma technology  May 4, 2006
Albuterol. Tangner said he also uses a steroid-based medication that reduces inflammation and Singulair, an allergy medication. ... - Oklahoma Daily,

Merck Announces Strong Financial Results for the First Quarter ...  Apr 20, 2006
..."Our first-quarter results were driven by the performance ofZOCOR, SINGULAIR and our vaccines, plus the strong performance of ourpartnerships and alliances. ... - Finanzen.net,

Merck, Lilly, Schering-Plough 1st-Qtr Profits Rise (Update3)  Apr 20, 2006
Merck's net income climbed 11 percent as tax benefits and sales of cholesterol drugs and the Singulair asthma pill offset the loss of the Vioxx painkiller. ... - Bloomberg

Merck 1st-Qtr Net Gains on Cholesterol, Allergy Pills (Update2)  Apr 20, 2006
April 20 (Bloomberg) -- Merck & Co. said first-quarter profit rose 11 percent on sales of the Zocor cholesterol drug, the Singulair allergy pill and vaccines. ... - Bloomberg

Merck Beats Estimates  Apr 20, 2006
...research - Cramer's Take) posted an 11% rise in first quarter earnings as sales inched higher, led by a 9% rise in sales of allergy treatment Singulair. ... - TheStreet.com

Merck posts profit improvement  Apr 20, 2006
...reported Thursday improved first-quarter earnings, due in part to contributions from medications Singulair and Zocor, as revenue nosed 1% higher. ... - MarketWatch

Relief from allergies is confusing  Apr 30, 2006
Another type of medication reduces inflammation although it contains no steroids. Singulair is a prescription medicine that blocks leukotrienes. ... - Houston Chronicle,

Merck Well-Positioned to Regain Industry-Leadership Position, CEO ...  Apr 25, 2006
The first-quarter results were driven by the performance of ZOCORand SINGULAIR in the United States and Merck's vaccines, plus thestrong performance of the ... - Finanzen.net,

Merck Says Follow-up Study Shows No Increased Risk After ...  May 11, 2006
...controversy and the court cases, the company performed well in the first quarter, posting exemplary results on the strength of its Zocor and Singulair products ... - Trading Markets,

Watson Pharmaceuticals Q1 EPS Declines On Lower Brand Product ...  May 9, 2006
...or $0.69 per share on revenues of $5.41 billion for the first quarter of 2006, on strong sales of its cholesterol drug Zocor and asthma treatment drug Singulair ... - Trading Markets,

Daily check-in, occasionally money related  May 12, 2006
I got some sort of nose spray and that works. I am taking the antibiotics and the singulair for allergies, and one of the cough meds. ... - SavingAdvice.com,

Merck Boosts 1Q Profit Despite Flat Sales  Apr 20, 2006
Revenues edged up less than 1 percent, to $5.41 billion from $5.36 billion, led by strong sales of Zocor, some Merck vaccines and Singulair for asthma and ... - Houston Chronicle,

Merck faces 11,500 lawsuits over Vioxx  Apr 20, 2006
Strong demand for Singulair, a treatment for asthma, and an aggressive cost-cutting campaign helped to lift net profits for the first three months of the year ... - Times Online,

DTC Takes a Back Seat  May 10, 2006
...with 2004. Merck & Co.’s Singulair slipped from No. 8 in 2004 to No. 9 in 2005, based on promotional expenditure. Merck spent ... - Med Ad News (subscription),

Earnings roundup: Merck's $1.5B profit beats analysts' estimates  Apr 20, 2006
Revenue rose just 1 percent, to $5.4 billion, although sales of the Singulair allergy pill and the Zocor cholesterol drug, which loses patent protection this ... - Newark Star Ledger,

Merck 1Q earnings up 11%  Apr 21, 2006
78¢ per share. The company said its results were boosted by its cholesterol drug, Zocor, and the Singulair allergy pill. Merck’s ... - newratings.com

Merck & Co Q1 Profit Up 11% - Quick Facts1  Apr 20, 2006
Richard Clark, chief executive officer and president commented, "Our first-quarter results were driven by the performance of ZOCOR, SINGULAIR and our vaccines ... - Trading Markets,

Kirby: Evil pollen is maulin' my sinuses  Apr 25, 2006
I have never been able to find a medication that completely alleviated my allergy symptoms. Claritin, Singulair, Flo-nase, I've tried them all. ... - Salt Lake Tribune,

Merck Q1 profits rise despite flat revenues  Apr 21, 2006
Sales of the oral asthma drug Singulair (montelukast) rose 9% to $801 million, and Merck forecast turnover of the product will rise at least 11% this year to ... - Pharma Times (subscription),

A Better Prognosis for Big Pharma  May 4, 2006
...unexpectedly lost Vioxx in 2004, and is set to lose patent protection on Zocor in 2006, on Fosamax in 2008, on Cozaar/Hyzaar in 2010, and on Singulair in 2012. ... - BusinessWeek

Sanofi-Aventis Q1 Profit Surges 54%, Boosted By Higher Vaccines ...  May 5, 2006
MRK | charts | news | PowerRating), a pharmaceutical company, on April 20, reported that first-quarter profit rose on strong US sales of Zocor and Singulair. ... - Trading Markets,

Allergies will grow on you, newcomers to the desert eventually ...  May 1, 2006
You should avoid these if you have high blood pressure or heart problems. Singulair, a newer prescription drug, inhibits the release of histamines. ... - Arizona Republic,

Dow Average Sets Six-Year High on Merck, GM Results, Oil's Drop  Apr 20, 2006
The company said first-quarter profit rose 11 percent to $1.52 billion on sales of the Zocor cholesterol drug, the Singulair allergy pill and vaccines. ... - Bloomberg

UPDATE 1-US Zocor sales help lift Merck quarterly profit  Apr 20, 2006
4 percent to $1.06 billion. Sales of asthma treatment Singulair rose 9 percent to $801 million. Sales of newer cholesterol treatments ... - Reuters

Cholesterol drugs boost Merck and Schering  Apr 20, 2006
Singulair, a respiratory drug, was the only one of its blockbuster drugs to post sales growth - 9 per cent - in the first quarter. ... - MSNBC

Business Briefing  Apr 20, 2006
Merck & Co., maker of cholesterol drugs, the Singulair allergy pill and vaccines, said first-quarter net income increased to $1.52 billion, or 69 cents a share ... - Seattle Post Intelligencer

AFX European summary - late  Apr 20, 2006
BOSTON (AFX) - Merck & Co reported improved first-quarter earnings, due in part to contributions from medications Singulair and Zocor, as revenue nosed 1 pct ... - Forbes

Drug Companies' Profit Up On Sales and Cost-Cutting  Apr 20, 2006
Merck's net income climbed 11 percent, exceeding analysts' expectations, as tax benefits and sales of the Zocor cholesterol drug and the Singulair asthma pill ... - New York Times,

Merck boosts profit, but sales flat  Apr 20, 2006
Revenue edged up less than 1%, to $5.41 billion, led by strong sales of Zocor, some Merck vaccines and Singulair for asthma and allergies. ... - USA Today

Wait for More Bad News on Merck  Apr 20, 2006
...drug franchises. Cozaar/Hyzaar, Fosamax, and Zocor were all down, while Singulair had a reasonably good performance. Barring an ... - Motley Fool

Schering-Plough, Merck impress, Lilly disappoints  Apr 20, 2006
...augmented by US demand for its Zocor cholesterol medicine, which loses patent protection in June, and a 9 percent rise in sales of its asthma drug Singulair. ... - Reuters

Legal woes cloud Merck gains  Apr 24, 2006
...'Our first-quarter results were driven by the performance of Zocor, Singulair and our vaccines, plus the strong performance of our partnerships and alliances ... - Monsters and Critics.com,

Profit rises at big drug companies  Apr 21, 2006
Merck said its net income rose 11 percent as tax benefits and sales of Zocor, a cholesterol drug, and Singulair, an asthma pill, offset the loss of Vioxx, the ... - International Herald Tribune,

Novartis Q1 Profit Climbs On Sales Growth, Acquisition; Announces ...  Apr 24, 2006
Pharmaceutical company Merck & Co., Inc. (MRK | charts | news | PowerRating) said first-quarter profit rose on strong US sales of Zocor and Singulair. ... - Trading Markets,

Earnings snapshots: GM logs sixth straight quarterly loss  Apr 20, 2006
Merck & Co. said first-quarter profit rose 11 percent on lower taxes and sales of cholesterol drugs, the Singulair allergy pill and vaccines. ... - Salt Lake Tribune,

Merck's strong quarter boosts year forecast  Apr 20, 2006
...in Whitehouse Station, NJ, said the strong profit was partly driven by sales from Zocor, a cholesterol-cutting blockbuster, as well as the asthma drug Singulair ... - CNNMoney.com

Time to break out the tissues  Apr 28, 2006
Other medications include cortisone nasal sprays, which do not have the negative side effects of taking cortisone orally, and Singulair, which blocks ... - Iowa City Press Citizen,

Strong results a mixed bag for drug stocks  Apr 20, 2006
...blockbusters going off patent: Zocor in 2006, osteoporosis treatment Fosamax in 2008, hypertension drug Cozaar in 2009, and asthma drug Singulair in 2010. ... - CNNMoney.com

Merck’s cost-cutting initiative costs dearly  Apr 26, 2006
Despite the company expecting sales of $3.3bn to $3.6bn in 2006 for its asthma treatment Singulair, and a strong performance from drugs such as its newer ... - In-PharmaTechnologist.com,

Spring Allergies  Apr 23, 2006
...needed on a regular basis. Singulair™ is another medication that can be used to treat children with allergies. It is available as ... - About - News & Issues,

Highlights of rising and falling US stocks  Apr 20, 2006
The Dow component said its first-quarter results were driven by the performance of its Zocor and Singulair products, its vaccines and partnerships and alliances ... - Investor's Business Daily (subscription)

Asthma Treatment -- A Safe, Effective Drug-free Alternative  Apr 20, 2006
Soon I was on the albuterol inhaler, the Advair inhaler and taking the singulair pills every day just to maintain my breathing. ... - Emediawire (press release),

GM, Altria, Nokia, Merck in the spotlight  Apr 20, 2006
The Dow component said results were driven by the performance of its Zocor and Singulair products, its vaccines and partnerships and alliances. ... - Investor's Business Daily (subscription)


Other information


Indication
For the treatment of asthma

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.

Drug Category
Antiarrhythmic Agents; Unclassified Therapeutic Agents (92:00.00); ATC:R03DC03

Brand Names/Synonyms
Montelukast; Singulair; Singular

Dosage Forms
Oral tablets

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.



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

Half Life
2.7-5.5 hours

Drug Type
Approved Drug

# Accession No
APRD00434

CAS Registry Number
158966-92-8

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