FLOAID (Montelukast Sodium)

Floaid
(Montelukast Sodium)
10mg Tablets
5mg Chewable Tablets

4mg Paediatric Dry Powder Sachet

COMPOSITION
Floaid 10 mg tablets: Each film coated tablet contains 10.4 mg Montelukast
Sodium U.S.P. equivalent to 10 mg Montelukast Acid.
Floaid 5 mg chewable tablets: Each chewable tablet contains 5.2 mg Montelukast
Sodium U.S.P. equivalent to 5 mg Montelukast Acid.
Floaid 4 mg Paediatric Dry Powder sachet for Oral use: Each sachet of Floaid
contains 4.15 mg Montelukast Sodium U.S.P. equivalent to 4 mg Montelukast
Acid.

DESCRIPTION

a) Mode of Action:
Montelukast Sodium is a selective leukotriene receptor antagonist that specifically
inhibits the cysteinyl leukotriene CysLT1 receptor.
b) Pharmacokinetic properties
Absorption. Montelukast is rapidly absorbed following oral administration. For the 10-mg film-coated tablet, the mean peak plasma concentration (Cmax) is achieved
3 hours (Tmax) after administration in adults in the fasted state. The mean oral
bioavailability is 64%. The oral
bioavailability and Cmax are not influenced by a standard meal.
For the 5-mg chewable tablet, the Cmax is achieved in 2 hours after administration
in adults in the fasted state. The mean oral bioavailability is 73% and is decreased to
63% by a standard meal.
After administration of the 4-mg chewable tablet to paediatric patients 2 to 5 years
of age in the fasted state, Cmax is achieved 2 hours after administration. The mean
Cmax is 66% higher while mean Cmax is lower than in adults receiving a 10 mg
tablet.
Distribution. Montelukast is more than 99% bound to plasma proteins. The steady-
state volume of distribution of montelukast averages 8-11 litres.
Biotransformation. Montelukast is extensively metabolised in the liver. In studies
with therapeutic doses, plasma concentrations of metabolites of montelukast are
undetectable at steady state in adults and children.
Cytochrome P450 2C8 is the major enzyme in the metabolism of montelukast.
Additionally CYP 3A4 and 2C9 may have a minor contribution.
Elimination. The plasma clearance of montelukast averages 45 ml/min in healthy
adults. Montelukast and its metabolites are excreted almost exclusively via the bile.
Characteristics in patients. No dosage adjustment is necessary for the elderly or
mild to moderate hepatic insufficiency. There are no data on the pharmacokinetics
of montelukast in patients with severe hepatic insufficiency (Child-Pugh score>9).
With high doses of montelukast (20- and 60-fold the recommended adult dose), a
decrease in plasma theophylline concentration was observed. This effect was not seen at the recommended dose of 10 mg once daily.
Therapeutic Indications
1. Asthma: Floaid 4 mg dry powder / Floaid 5 mg chewable tablet is indicated in
the treatment of asthma as add-on therapy in those 2 to 5 year old patients with
mild to moderate persistent asthma who are inadequately controlled on inhaled
corticosteroids and in whom “as-needed” short-acting β-agonists provide
inadequate clinical control of asthma.
Floaid 4 mg dry powder may also be an alternative treatment option to low-dose
inhaled corticosteroids for 2 to 5 year old patients with mild persistent asthma who
do not have a recent history of serious asthma attacks that required oral
corticosteroid use, and who have demonstrated that they are not capable of using inhaled corticosteroids.
Floaid 4 mg dry powder is also indicated in the prophylaxis of asthma from 2 years of
age and older in which the predominant component is exercise-induced
bronchoconstriction.
1.1. Floaid 5 mg chewable tablet may also be an alternative treatment option to low-
dose inhaled corticosteroids for 6 to 14 year old patients with mild persistent
asthma who do not have a recent history of serious asthma attacks that required
oral corticosteroid use, and who have demonstrated that they are not capable of
using inhaled corticosteroids.
Floaid 5 mg chewable tablet is also indicated in the prophylaxis of asthma in
those 6 to 14 years old which the predominant component is exercise-induced
choconstriction.
1.2. Floaid 10 mg tablet is indicated in the treatment of asthma as add-on therapy in
patients 15 years and older with mild to moderate persistent asthma who are
inadequately controlled on inhaled corticosteroids and in whom “as needed”
short-acting β-agonists provide inadequate clinical control of asthma. In those
asthmatic patients in whom Floaid 10 mg tablet is indicated in asthma,
Floaid 10 mg tablet can also provide symptomatic relief of seasonal allergic
rhinitis.
Floaid 10 mg tablet is also indicated in the prophylaxis of asthma in which the
predominant component is exercise induced bronchoconstriction in patients 15
years and older.
2. Perennial Allergic Rhinitis (PAR):in patients 6 months of age and older
3. Acute prevention of exercise-induced bronchoconstriction (EIB): in patients 6
years of age and older.
4. Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in
patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients
6 months of age and older.

DOSAGE AND ADMINISTRATION

Floaid 4 mg Dry Powder:
The dosage for paediatric patients 2-5 years of age is one 4 mg dry powder sachet
daily. Floaid 4 mg dry powder can be administered either directly in the mouth, or mixed with a tablespoon of cold or room temperature soft food (e.g. applesauce, ice
cream and rice). The sachet should not be opened until ready to use. After opening
the sachet, the full dose of Floaid powder must be administered immediately (within
15 minutes). If mixed with food, Floaid powder must not be stored for future use.
Floaid powder is not intended to be dissolved in liquid for administration. However,
liquids may be taken subsequent to administration. Floaid powder can be
administered without regard to the timing of food ingestion.

Floaid 5 mg chewable tablet:

The dosage for paediatric patients 6-14 years of age is one 5 mg chewable tablet
daily to be taken in the evening. The tablets are to be chewed before swallowing. If
taken in connection with food, Floaid 5 mg chewable tablet should be taken 1 hour
before or 2 hours after food. No dosage adjustment within this age group is
necessary.

General recommendations:

The therapeutic effect of Floaid 5 mg chewable tablet on parameters of asthma
control occurs within one day. Patients should be advised to continue taking Floaid
5 mg chewable tablet even if their asthma is under control, as well as during periods
of worsening asthma.
No dosage adjustment is necessary for patients with renal insufficiency, or mild to
moderate hepatic impairment. There are no data on patients with severe hepatic
impairment. The dosage is the same for both male and female patients.
Floaid 5 mg chewable tablet as an alternative treatment option to low-dose
inhaled corticosteroids for mild persistent asthma.

Therapy with Floaid 5 mg chewable tablet in relation to other treatments for 
asthma:

When treatment with Floaid 5 mg chewable tablet is used as add-on therapy to
inhaled corticosteroids, Floaid 5 mg chewable tablet should not be abruptly
substituted for inhaled corticosteroids.

Floaid 10 mg tablet:

Floaid 10 mg film-coated tablets are available for adults and adolescents 15 years of age and older.
The dosage for adults and adolescents 15 years of age and older with asthma, or with
asthma and concomitant seasonal allergic rhinitis is one 10 mg tablet daily to be
taken in the evening.

General recommendations:

The therapeutic effect of Floaid 10 mg tablet on parameters of asthma control
occurs within one day. Floaid 10 mg tablet may be taken with or without food.
Patients should be advised to continue taking Floaid 10 mg tablet even if their
asthma is under control, as well as during periods of worsening asthma.
Floaid 10 mg tablet should not be used concomitantly with other products
containing the same active ingredient, montelukast.
No dosage adjustment is necessary for the elderly, or for patients with renal
insufficiency, or mild to moderate hepatic impairment. There are no data on
patients with severe hepatic impairment. The dosage is the same for both male and
female patients.

Therapy with Floaid 10 mg tablet in relation to other treatments for asthma:

Floaid 10 mg tablet can be added to a patient's existing treatment regimen.
Inhaled corticosteroids: Treatment with Floaid 10 mg tablet can be used as add-on
therapy in patients when inhaled corticosteroids plus "as needed" short acting β- agonists provides inadequate clinical control. Tradename should not be abruptly substituted for inhaled corticosteroids.
Contraindications Hypersensitivity to any component of this product.
Special warnings and precautions for use
Patients should be advised never to use oral montelukast to treat acute asthma
attacks and to keep their usual appropriate rescue medication for this purpose
readily available. If an acute attack occurs, a short-acting inhaled β-agonist should
be used. Patients should seek their doctor's advice as soon as possible if they need
more inhalations of short-acting β-agonists than usual.
Montelukast should not be abruptly substituted for inhaled or oral corticosteroids.
There are no data demonstrating that oral corticosteroids can be reduced when
montelukast is given concomitantly.
In rare cases, patients on therapy with anti-asthma agents including 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 cases usually, but not always,
have been associated with the reduction or withdrawal of oral corticosteroid
therapy. Although a causal relationship with leukotriene receptor antagonism has
not been established physicians should be alert to eosinophilia, vasculitic rash,
worsening pulmonary symptoms, cardiac complications and/or neuropathy
presenting in their patients. Patients who develop these symptoms should be
reassessed and their treatment regimens evaluated.
Treatment with montelukast does not alter the need for patients with aspirin-
sensitive asthma to avoid taking aspirin and other non-steroidal anti-inflammatory
drugs.
Patient and physician should be alert for neuropsychiatric events. Patients should
be instructed to notify their health care practitioner if any such changes occur.
Interaction with other medicinal products and other forms of interaction
Montelukast may be administered with other therapies routinely used in the
prophylaxis and chronic treatment of asthma. In drug-interactions studies, the
recommended clinical dose of montelukast did not have clinically important effects
on the pharmacokinetics of the following medicinal products: theophylline,
prednisone, prednisolone, oral contraceptives (ethinyl estradiol/ norethindrone
35/1), terfenadine, digoxin and warfarin.
The area under the plasma concentration curve (AUC) for montelukast was
decreased approximately 40% in subjects with co-administration of phenobarbital.
Since montelukast is metabolized by CYP 3A4, 2C8 and 2C9, caution should be
exercised, particularly in children, when montelukast is co-administered with
inducers of CYP 3A4, 2C8 and 2C9, such as phenytoin, phenobarbital and
rifampicin.
In vitro studies have shown that montelukast is a potent inhibitor of CYP 2C8.
However, data from a clinical drug-drug interaction study involving montelukast
and rosiglitazone (a probe substrate representative of medicinal products primarily
metabolized by CYP 2C8) demonstrated that montelukast does not inhibit CYP
2C8 in vivo. Therefore, montelukast is not anticipated to markedly alter the
metabolism of medicinal products metabolized by this enzyme (e.g. paclitaxel,
rosiglitazone and repaglinide).
In vitro studies have shown that montelukast is a substrate of CYP 2C8, and to a less
significant extent, of 2C9, and 3A4. In a clinical drug-drug interaction study
involving montelukast and gemfibrozil (an inhibitor of both CYP 2C8 and 2C9)
gemfibrozil increased the systemic exposure of montelukast by 4.4-fold. No
routine dosage adjustment of montelukast is required upon co-administration with
gemfibrozil or other potent inhibitors of CYP 2C8, but the physician should be
aware of the potential for an increase in adverse reactions.
Based on in vitro data, clinically important drug interactions with less potent
inhibitors of CYP 2C8 (e. g., trimethoprim) are not anticipated. Co-administration
of montelukast with itraconazole, a strong inhibitor of CYP 3A

OVERDOSE
No specific information is available on the treatment of overdose with montelukast.
STORAGEO
Store below 25 C and protect from light & moisture.

PRESENTATION
1. Floaid 10 mg tablets:Blister pack of 14 tablets.
2. Floaid 5 mg chewable tablets:Blister pack of 14 chewable tablets.
3. Floaid 4 mg Paediatric Dry Powder sachet for oral use:Carton of 14 sachets.
To be sold on the prescription of a registered medical practitioner only.
Keep all medicines out of the reach of children.