Montelukast - Singulair (1998) - Leukotriene Receptor Antagonists- Bronchodilators- (FDC- List )
Drug Interaction:
Phenobarbital which acts as a potent cytochrome P450) enzyme inducer, may decrease the AUC of montelukast by upto 40%. However this interaction is not significant. Other P450 inducers such as rifampicin or valproate, may also induce the metabolism of montelukast, but the clinical effects of these interactions are not well established
Indication:
Initial U.S. Approval: 1998
U.S.FDA APPROVED DRUGS FROM 01-01-08 TO 31-12-08
Drug name Indication Date of Approval
70. Montelukast 10mg 31-01-08
+ Levocetrizine 5mg film coated
tablets
For the treatment of allergic rhinitis only
201. Montelukast Suspension 5mg/ml 16-09-08
i. For the treatment of Prophylaxis & chronic
treatment of Asthma in Pediatrics Patients 12months
of age & older
ii. For relieving symptoms of seasonal allergic rhinitis
in Pediatric patients 2 years of age and older &
Perennial allegic rhinitis in Pediatric Patients
6 months of age & older
238. Montelukast 10-11-08
+ Desloratidine (10mg+5mg) FC tablets
For the treatment of allergic rhinitis in adults only
SINGULAIR® (montelukast sodium) Tablets, Chewable Tablets,
and Oral Granules
Initial U.S. Approval: 1998
RECENT MAJOR CHANGES
Indications and Usage Exercise-Induced Bronchoconstriction (EIB) (1.2) 03/2012
Dosage and Administration Exercise-Induced Bronchoconstriction (EIB) (2.2) 03/2012
Montelukast sodium chewable tablet 4mg/5mg and Montelukast sodium
film coated tablets
Indication-
As and add on therapy in mild to moderate asthma inadequately controlled
by inhaled corticosteroids and short active B2 agonist. excercise induced
bronchoconstriction
Approved by FDA on 26-02-2012 (Ref- FDA approved List- 2014)
Asthma
Patent Expiry Date of drugs (Ref - IDMA Publication)
Chemical Category Manufacturer/ US Patent
Ingredient- Marketer Expiration Date
Montelukast Respiratory Merck 15-10-2013
Sodium
Montelukast Respiratory Merck & C0 15-19-2013
Adverse Reaction:
Montelukast appears to be well tolerated in clinical trials . The most common adverse interactions reported are headache, rash, dizziness, and abdominal pain. Elevated liver transaminases have been reported with montelukast use, but not at a greater incidence than the placebo. A small percentage of pediatric patients have experienced diarrhea, sinusitis and otitis media during montelukast clinical trials.
Contra-Indications:
Hypersensitivity Pregnancy and lactation The drug has been shown to cross the placena of pregnant rats and rabbits., but there have been no reports of its use in pregnant women. Montelukast is also known to be excreted into breast milk, but only limited information is available. Caution to be excecised prior to initiating montelukast therapy in nursing mothers.
Special precautions:
Motelukast is not indicated for use in the reversal of bronchospasm in acute asthma attacks, including status asthmaticus. Motelukast should not be abruptly substituted for inhaled or oral cortiocosteroids.
Montelukast should be used as monotherapy for the tretment and management of excercise-induced bronchospasm.
Patients who have exacerbations of asthma after excercise should continue to use their usual regimen of inhaled beta agonists as prophylaxis and have for rescue a short acting beta agonist.
Patients with known aspirin sensitivity should continue avoidance of aspirin or non-steroidal anti-inflammatory agents while taking miontelukast.
Clinical monitoring is recommended when systemic coticosteroids reduction is considered in patients receiving montelukast.
Dosages/ Overdosage Etc:
Initial U.S. Approval: 1998
Indications:
Asthma
Dosage
Children 6 to 14 years of age- 5mg chewable tablet daily in the evening
Patients over 15 years of age- Usual dosage is 10mg daily in the evening.
Maximum dose is 10mg, although doses as high as 250mg have been found to be safe in clinical trials.
Patient Information:
PATIENT COUNSELING INFORMATION
See FDA-approved patient labeling (Patient Information).
Information for Patients
1.Patients should be advised to take SINGULAIR daily as prescribed, even when
they are asymptomatic, as well as during periods of worsening asthma,
and to contact their physicians if their asthma is not well controlled.
2. Patients should be advised that oral SINGULAIR is not for the treatment of
acute asthma attacks. They should have appropriate short-acting inhaled
beta]-agonist medication available to treat asthma exacerbations.
3.Patients who have exacerbations of asthma after exercise should be
instructed to have available for rescue a short-acting inhaled bet--agonist.
4.Daily administration of SINGULAIR for the chronic treatment of asthma has not
been established to prevent acute episodes of EIB.
5.Patients should be advised that, while using SINGULAIR, medical attention
should be sought if short-acting inhaled bronchodilators are needed more often
than usual, or if more than the maximum number of inhalations of short-acting
bronchodilator treatment prescribed for a 24-hour period are needed.
6. Patients receiving SINGULAIR should be instructed not to decrease the dose
or stop taking any other anti-asthma medications unless instructed by a physician.
7. Patients should be instructed to notify their physician if neuropsychiatric events
occur while using SINGULAIR. „h Patients with known aspirin sensitivity should
be advised to continue avoidance of aspirin or non-steroidal anti-inflammatory
agents while taking SINGULAIR.
8. Phenylketonuric patients should be informed that the 4-mg and 5-mg chewable
tablets contain phenylalanine (a component of aspartame).
Pharmacology/ Pharmacokinetics:
Pharmacology:
Montlukast is a competitive antagonist. It binds with affinity to the LTD4 receptor , inhibiting bronchoconstrition.
Pharmacokinetics:
Two-third of oral dose is rapidly absorbed from gastrointestinal tract following oral administration, reaching peak levels at 2 to 2.5 hrs after administration of 5mg tablet and 2 to 2.5hrs after administration of 10mg tablet. The 10mg tablet is approximately 64% bioavailable, regardless of whether it is administered with food. The 5mg tablet is 73% bioavailable in the fasting state, but bioavailability declines to 63% when it is taken with food.
Montelukast undergoes extensive metabolism in the liver. The mean plasma half life of the drug is 2.7 to 5.5hrs
Interaction with Food:
Bioavailability declines when it is taken with food.
Pregnancy and lactation:
USE IN SPECIFIC POPULATIONS
1. Pregnancy
Pregnancy Category B:
There are no adequate and well-controlled studies in pregnant women.
Because animal reproduction studies are not always predictive of human
response, SINGULAIR should be used during pregnancy only if clearly needed.
2. Nursing Mothers
Studies in rats have shown that montelukast is excreted in milk. It is not known if
montelukast is excreted in human milk. Because many drugs are excreted in
human milk, caution should be exercised when SINGULAIR is given to a nursing mother.
3.Pediatric Use
Safety and efficacy of SINGULAIR have been established in adequate and
well-controlled studies in pediatric patients with asthma 6 to 14 years of age.
Safety and efficacy profiles in this age group are similar to those seen in adults
4. Geriatric Use
Of the total number of subjects in clinical studies of montelukast, 3.5% were 65 years
of age and over, and 0.4% were 75 years of age and over.
No overall differences in safety or effectiveness were observed between these
subjects and younger subjects, and other reported clinical experience
has not identified differences in responses between the elderly and younger
patients, but greater sensitivity of some older individuals cannot be ruled out.
The pharmacokinetic profile and the oral bioavailability of a single 10-mg oral
dose of montelukast are similar in elderly and younger adults.
The plasma half-life of montelukast is slightly longer in the elderly.
No dosage adjustment in the elderly is required..
