Montelukast
An oral leukotriene receptor antagonist that prevents asthma and exercise-induced symptoms and eases allergic rhinitis.
Drug card
- How it works
- Blocking CysLT1 receptors so leukotrienes cannot narrow the airways
- Used for
- Preventing and controlling asthma
- Preventing exercise-induced bronchoconstriction
- Allergic rhinitis, when other drugs fail
- Long-lasting hives (chronic urticaria)
- Known for
- Agitation, aggression, depression or anxiety
- Its name
- -lukast means a leukotriene receptor antagonist
Study it as a flashcard, and it comes back before you forget it.
Mechanism of action
How does montelukast work?
An orally active, highly selective CysLT1 receptor antagonist: it blocks LTD4 at receptors on airway smooth muscle and inflammatory cells without any agonist effect, so bronchoconstriction, airway edema and eosinophil recruitment fall. It reaches the brain in animal studies; why it causes neuropsychiatric effects is not understood.
Uses
What is montelukast used for?
- Preventing and controlling asthma
- Preventing exercise-induced bronchoconstriction
- Allergic rhinitis, when other drugs fail
- Long-lasting hives (chronic urticaria)
Side effects
Side effects of montelukast
- Agitation, aggression, depression or anxietyKnown forSerious
- Suicidal thoughts and behaviorSerious
- Nightmares, sleepwalking or insomnia
- Stuttering, tics or tremor
- Headache
- Abdominal pain
- Diarrhea and nausea
- Fever and upper respiratory infections
- Eosinophilic vasculitis (Churg-Strauss syndrome)Serious
- Liver injury (rare)Serious
- Allergic reactions, including anaphylaxisSerious
- Seizures (rare)Serious
Known for marks what an exam expects you to know it for.
Watch for
Cautions and what sets it apart
- Boxed warning: serious neuropsychiatric events, including suicide; in rhinitis it is kept for when other drugs fail.
- It does not reverse bronchospasm in an acute attack.
- It is not swapped suddenly for steroids; cutting oral steroids can unmask Churg-Strauss vasculitis.
- In aspirin-sensitive asthma, aspirin and NSAIDs are still avoided.
Good to know: Usually an add-on controller in mild asthma; neuropsychiatric effects can appear in people with no psychiatric history and sometimes persist after stopping.
Remember it
A way to remember it
Clear airways, but mind the mood.
Blocking leukotrienes eases asthma and rhinitis, but the boxed warning is for neuropsychiatric events such as agitation, aggression, depression, sleep disturbance and suicidal thoughts.
Written for biofideX
Its name
-lukast means leukotriene receptor antagonist
Montelukast and zafirlukast block cysteinyl leukotriene receptors and are used for long-term control of asthma; montelukast also treats allergic rhinitis. WHO files -lukast under -ast.
- Every drug name stem
Its class
Leukotriene receptor antagonists
Mast cells and eosinophils release cysteinyl leukotrienes (LTC4, LTD4, LTE4), which act on CysLT1 receptors to tighten airway smooth muscle, swell the airway wall and draw in inflammatory cells. These drugs bind CysLT1 selectively and block LTD4 without any agonist effect, easing bronchoconstriction and allergic inflammation. Taken as tablets, they prevent symptoms but cannot reverse an acute attack.
Easily mixed up with inhaled corticosteroids, second-generation antihistamines and methylxanthines.
Sources
Checked against
Written for biofideX in plain words, after checking these references:
For learning pharmacology, not for treatment decisions: no doses are given, and a prescriber, pharmacist or the product's own label is the word on any one patient. Spotted a mistake? Tell us and we'll correct it.
Lungs and allergy
Montelukast is one of 16 drugs practiced together here: their classes, how they work, what they treat and what they're known for.
Start Practicing