The active ingredient of Monocast tablet is Montelukast Sodium INN.
Montelukast is a selective and orally active leukotriene receptor antagonist
that inhibits the cysteinyl leukotriene CysLT1 receptor. The cysteinyl
leukotrienes (LTC4, LTD4, LTE4) are products of Arachidonic acid
metabolism and are released from various cells, including mast cells and
oeosinophils. These eicosanoids bind to cysteinyl leukotriene (CysLT)
receptors. The CysLT type-1 (CysLT1) receptor is found in the human
airway (including airway smooth muscle cells and airway macrophages)
and on other pro-inflammatory cells (including oeosinophils and certain
myeloid stem cells). CysLTs have been correlated with the
pathophysiology of asthma and allergic rhinitis. In asthma, leukotrienemediated effects include airway oedema, smooth muscle contraction, and
altered cellular activity associated with the inflammatory process. In
allergic rhinitis, CysLTs are released from the nasal mucosa after allergen
exposure during both early and late phase reactions and are associated
with symptoms of allergic rhinitis. Intranasal challenge with CysLTs has
been shown to increase nasal airway resistance and symptoms of nasal
Montelukast is an orally active compound that binds with high affinity
and selectivity to the CysLT1 receptor (in preference to other
pharmacologically important airway receptors, such as the prostanoid,
cholinergic, or b adrenergic receptors). Montelukast inhibits physiologic
actions of LTD4 at the CysLT1 receptor without any agonist activity.
Monocast is indicated for the prophylaxis and chronic treatment of
asthma in adults and paediatric patients 12 months of age and older.
Monocast is indicated for the relief of symptoms of seasonal allergic
rhinitis in adults and paediatric patients 2 years of age and older.
Dosage and Administration
General information : Monocast should be taken once daily. For asthma,
the dose should be taken in the evening. For seasonal allergic rhinitis, the
time of administration may be individualised to suit patients’ needs.
Patients with both asthma and seasonal allergic rhinitis should take only
one tablet daily in the evening.
Adults and adolescents 15 years of age and older with asthma or seasonal
allergic rhinitis : The dosage is one 10 mg tablet daily.
Paediatric patients 6 to 14 years of age with asthma or seasonal allergic
rhinitis : The dosage is one 5 mg chewable tablet daily. No dosage
adjustment within this age group is necessary.
Paediatric patients 2 to 5 years of age with asthma or seasonal allergic
rhinitis : The dosage is one 4 mg chewable tablet daily.
Paediatric patients 12 to 23 months of age with asthma : The dosage is
one 4 mg chewable tablet daily to be taken in the evening. Safety and
effectiveness in paediatric patients younger than 12 months of age have
not been established.
Hypersensitivity to any component of this product.
General : Montelukast is not indicated for use in the reversal of
bronchospasm in acute asthma attacks, including status asthmaticus.
Patients should be advised to have appropriate rescue medication
available. Therapy with Montelukast can be continued during acute
exacerbation of asthma. While the dose of inhaled corticosteroid may be
reduced gradually under medical supervision, montelukast should not be
abruptly substituted for inhaled or oral corticosteroids. Montelukast
should not be used as monotherapy for the treatment and management
of exercise induced bronchospasm. Patients who have exacerbation of
asthma after exercise should continue to use their usual regimen of
inhaled b agonist as prophylaxis and have available for rescue a short
acting inhaled b agonist. Patients with known Aspirin sensitivity should
continue avoidance of aspirin or non-steroidal anti-inflammatory
agents while taking Montelukast. Although montelukast is effective in
improving airway function in asthmatics with documented aspirin
sensitivity, it has not been shown to truncate bronchoconstrictor
response to aspirin and other non-steroidal anti-inflammatory drugs in
aspirin-sensitive asthmatic patients.
Eosinophilic Conditions : In rare cases, patients on therapy with
Montelukast may present with systemic eosinophilia, sometimes
presenting with clinical features of vasculitis consistent with Churg
Strauss syndrome, a condition which is often treated with systemic
corticosteroid therapy. These events usually, but not always, have been
associated with the reduction of oral corticosteroid therapy. Physicians
should be alert to eosinophilia, vasculitic rash, worsening pulmonary
symptoms, cardiac complications, and/or neuropathy presenting in their
patients. A causal association between montelukast and these underlying
conditions has not been established.
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, Prednisolone, oral contraceptives (Norethindrone 1
mg/Ethinyl Oestradiol 35 mg), 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 clinically evident adverse
interactions. These medications included thyroid hormones, sedative
hypnotic, non-steroidal anti-inflammatory agents, benzodiazepines, and
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.
Adolescents and Adults 15 years of age and older : In placebo-controlled
clinical trials, Montelukast has been evaluated for safety in approximately
2600 adolescent and adult patients of 15 years and older, the following
adverse experiences reported with Montelukast occurred in greater than
or equal to 1% of patients. General : Asthenia/fatigue, Fever, Pain;
Gastrointestinal : Dyspepsia, Gastroenteritis; Nervous System/Psychiatric :
Dizziness, Headache; Respiratory System : Congestion, Cough, Influenza;
Skin : Rash; Laboratory adverse experiences : ALT increase, AST increase,
Paediatric patients 6 to 14 years of age : In paediatric patients receiving
montelukast, the following events occurred with a frequency ³ 2% are
diarrhoea, laryngitis, pharyngitis, nausea, otitis, sinusitis, and viral
infection. With prolonged treatment, the adverse profile did not change
Use in Special Populations
Pregnancy : Montelukast crosses the placenta following oral dosing in rats
and rabbits. There are, however, no adequate and well controlled studies
in pregnant women. Because animal reproduction studies are not always
predictive of human response, Montelukast should be used during
pregnancy only if clearly needed.
Lactation : It is not known if Montelukast is excreted in human milk.
Because many drugs are excreted in human milk, caution should be
exercised when Montelukast is given to a nursing mother.
Paediatric use : Safety and efficacy of Montelukast has been established in
adequate and well controlled studies in paediatric patients with asthma
and allergic rhinitis between age 1 to 14 years. Long term trials evaluating
the effect of chronic administration of Montelukast on linear growth in
paediatric patients have not been conducted.
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. But greater
sensitivity of some older individuals cannot be ruled out.