Drug Profile Montelukast * Dr. Paul Samuel
Montelukast is a selective and orally active
Pharmacokinetics
leukotriene receptor antagonist that specifically
Montelukast is rapidly and nearly completely
inhibits the cysteinyl leukotriene CystLT1 receptor.
absorbed following oral administration. Monelukast
It is available as montelukast sodium.
is more than 99% bound to plasma proteins. Indications
Montelukast is extensively metabolized in liver andis excreted through bile. Phenobarbital, which
Prophylaxis and chronic treatment of asthma in
induces hepatic metabolism, decreases the AUC
adults and pediatric patients of 12 months age
(plasma concentration curve) of montelukast
approximately 40% following a single 10mg dose;no dosage adjustment is recommended.
Allergic rhinitis ( seasonal allergic rhinitis inadults and pediatric patients 2 years of age and
Pharmacodynamics
older, and perennial allergic rhinitis in adults and
Montelukast causes potent inhibition of airway
pediatric patients 6months of age and older
cysteinyl leukotriene receptors as demonstrated by
Mechanism of action
the ability to inhibit bronchoconstriction due toinhaled LTD4 in asthmatic patients. Dosage as low
The cysteinyl leukotrienes (cysLTs) are potent
as 5 mg causes substantial blockage of LTD4-
inflammatory mediators released by mast cells and
induced-bronchoconstriction. Montelukast causes
basophils on activation by antigen. They are
bronchodilation within 2 hours of administration;
synthesized from arachadonic acid through the action
these effects were additive to the bronchodilation
of the enzyme 5-OH-lipoxygenase. The terminal
active metabolites of this pathway are leukotriene
Dosage forms
C4, leukotrieneD4, and leukotriene E4. These agents
are potent inflammatory mediators and are major
agents involved in the late-phase allergic response.
antagonists work through binding to receptors ontarget cells at the end organ, interfering with the ability
of the cysLTs in binding and creating a physiologic
effect. Several of these agents have been developed
and are available in the United States for the
treatment of asthma. While both montelukast and
zafirlukast are FDA approved for the treatment of
asthma, only montelukast is approved for the
Drug Profile
efficacy to a mild non-sedating antihistamine, such
as loratadine, in the reduction of nasal symptoms,
although it is less effective than an intranasal
corticosteroid spray. Because montelukast is
age with perennial allergic rhinitis - One
effective in the treatment of both upper- and lower-
airway inflammation, it is an ideal medication to
Contraindications
consider in the treatment of patients with concurrent
allergic rhinitis and asthma. It can be used alone or
in combination with other medications for bothdiseases, and can also be considered as add-on
Adverse effects
therapy in patients with persistent symptoms despite
Usually none. In a 12 week placebo-controlled
clinical study, drug related headache and abdominal
Reference Literature review
treatment of allergic rhinitis: an evidence-based
Several studies have demonstrated the efficacy
of montelukast in the treatment of both seasonal and
John H. Krouse. Allergic Rhinitis-Current
perennial allergic rhinitis, and a recent review outlines
Pharmacotherapy. Otolaryngologic Clinics of
its benefits1. In general, montelukast has comparable
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