What is montelukast, and how does it work (mechanism of action)?
Montelukast is an oral leukotriene receptor
antagonist that is used for the treatment of asthma and seasonal allergic
rhinitis (hay fever). Leukotrienes are a group of naturally occurring chemicals
in the body that promote inflammation in asthma and seasonal allergic rhinitis
and in other diseases in which inflammation is important (such as allergy). They
are formed by cells, released, and then bound to other cells that cause
inflammation. It is the binding to other cells that stimulates the cells to
cause inflammation. Montelukast works in a manner similar to zafirlukast (Accolate),
blocking the binding of some leukotrienes to the cells that cause inflammation.
Unlike zafirlukast, montelukast does not inhibit CYP2C9 or CYP3A4, two enzymes
in the liver that are important in breaking down and eliminating many drugs.
Therefore, unlike zafirlukast, montelukast is not expected to affect the
elimination of other drugs. The safety and effectiveness of montelukast has been
demonstrated in children as young as 6 months of age. It was approved by the FDA
in 1998.
What brand names are available for montelukast?
Singulair
Is montelukast available as a generic drug?
GENERIC AVAILABLE: Yes
Do I need a prescription for montelukast?
Yes
What are the side effects of montelukast?
The most common side effects with montelukast are:
- headache,
- dizziness,
- abdominal pain,
- sore throat, and
- rhinitis (inflammation of the inner lining of the nose).
Other important side effects include:
Elevated liver enzymes, suicidal behavior, fluid
retention, depression, and hallucinations have also been reported.
What is the dosage for montelukast?
The recommended dose of montelukast in adults is 10 mg daily
for treating asthma and allergic rhinitis and 10 mg two hours before exercising
for prevention of exercise induced bronchospasm. Montelukast should be taken in
the evening with or without food when used for asthma or allergic rhinitis. The
4 and 5 mg tablets are used in children.
Which drugs or supplements interact with montelukast?
Phenobarbital, rifampin, and carbamazepine
(Tegretol, Tegretol XR, Equertro, Carbatrol) may
decrease blood concentrations of montelukast. This may reduce the effect of
montelukast.
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Is montelukast safe to take if I’m pregnant or breastfeeding?
Montelukast crosses the placenta into the fetus following
oral administration to animals, but there have been no adequate studies in
pregnant women to determine the effects on the fetus. Physicians may prescribe zafirlukast during pregnancy if it is felt that its benefits outweigh the
potential but unknown risks to the fetus.
Studies in animals have shown that montelukast is
excreted in milk; however, it is not known if montelukast is secreted into
breast milk in humans.
What else should I know about montelukast?
What preparations of montelukast are available?
Tablets: 10 mg. Chewable tablets: 4 and 5 mg.
How should I keep montelukast stored?
Tablets should be stored at room temperature, 15 C – 30 C (59 F – 86
F).