DRUG NAME DESCRIPTION
1. SINGULAIR Montelukast sodium, the active ingredient in SINGULAIR, is SINGULAIR should be taken once daily
(montelukast sodium) Tablets and a selective and orally active leukotriene receptor
Oral Granules antagonist that inhibits the cysteinyl leukotriene CysLT1
receptor.
Montelukast sodium is described chemically as [R-(E)]-1-
[[[1-[3-[2-(7-chloro-2-quinolinyl)ethenyl]phenyl]-3-[2-(1-
hydroxy-1-
methylethyl)phenyl]propyl]thio]methyl]cyclopropaneacetic
acid, monosodium salt.
Montelukast sodium is a hygroscopic, optically active,
white to off-white powder. Montelukast sodium is freely
soluble in ethanol, methanol, and water and practically
insoluble in acetonitrile.
Each 10-mg film-coated SINGULAIR tablet contains 10.4 mg
montelukast sodium, which is equivalent to 10 mg of
montelukast, and the following inactive ingredients:
microcrystalline cellulose, lactose monohydrate,
croscarmellose sodium, hydroxypropyl cellulose, and
magnesium stearate. The film coating consists of:
hydroxypropyl methylcellulose, hydroxypropyl cellulose,
titanium dioxide, red ferric oxide, yellow ferric oxide, and
carnauba wax.
Each 4-mg and 5-mg chewable SINGULAIR tablet contains
4.2 and 5.2 mg montelukast sodium, respectively, which
are equivalent to 4 and 5 mg of montelukast, respectively.
Both chewable tablets contain the following inactive
ingredients: mannitol, microcrystalline cellulose,
hydroxypropyl cellulose, red ferric oxide, croscarmellose
sodium, cherry flavor, aspartame, and magnesium
DOSE EFFECTS
The most common adverse
in the evening. The following doses are reactions (incidence 5% and
recommended: greater than placebo; listed in
descending order of frequency)
For adults and adolescents 15 years of in controlled clinical trials were:
age and older: one 10-mg tablet. upper respiratory infection,
fever, headache, pharyngitis,
For pediatric patients 6 to 14 years of cough, abdominal pain, diarrhea,
age: one 5-mg chewable tablet. otitis media, influenza,
rhinorrhea, sinusitis, otitis.
For pediatric patients 2 to 5 years of
age: one 4-mg chewable tablet or one
packet of 4-mg oral granules.
For pediatric patients 12 to 23 months
of age: one packet of 4-mg oral
granules.
Safety and effectiveness in pediatric
patients less than 12 months of age
with asthma have not been established.
There have been no clinical trials in
patients with asthma to evaluate the
relative efficacy of morning versus
evening dosing. The pharmacokinetics
of montelukast are similar whether
dosed in the morning or evening.
Efficacy has been demonstrated for
asthma when montelukast was
administered in the evening without
regard to time of food ingestion.
 stearate.
Each packet of SINGULAIR 4-mg oral granules contains 4.2
mg montelukast sodium, which is equivalent to 4 mg of
montelukast. The oral granule formulation contains the
following inactive ingredients: mannitol, hydroxypropyl
cellulose, and magnesium stearate.
2. ACCOLATE Zafirlukast is a synthetic, selective peptide leukotriene
(zafirlukast) Tablets receptor antagonist (LTRA), with the chemical name 4-(5-
cyclopentyloxy-carbonylamino-1-methyl-indol-3-ylmethyl)-
3-methoxy-N-otolylsulfonylbenzamide. The molecular
weight of zafirlukast is 575.7
afirlukast, a fine white to pale yellow amorphous powder,
is practically insoluble in water. It is slightly soluble in
methanol and freely soluble in tetrahydrofuran,
dimethylsulfoxide, and acetone.
ACCOLATE is supplied as 10 and 20 mg tablets for oral
administration.
Inactive Ingredients
Film-coated tablets containing croscarmellose sodium,
lactose, magnesium stearate, microcrystalline cellulose,
povidone, hypromellose, and titanium dioxide.
Because food can reduce the bioavailability of zafirlukast,
ACCOLATE should be taken at least 1 hour before or 2
hours after meals.
Adults and Children 12 years of age and
older
The recommended dose of ACCOLATE
in adults and children 12 years and
older is 20 mg twice daily.
Pediatric Patients 5 through 11 years of
age
The recommended dose of ACCOLATE
in children 5 through 11 years of age is
10 mg twice daily.
Elderly Patients
Based on cross-study comparisons, the
clearance of zafirlukast is reduced in
elderly patients (65 years of age and
older), such that Cmax and AUC are
approximately twice those of younger
adults. In clinical trials, a dose of 20 mg
twice daily was not associated with an
increase in the overall incidence of
adverse events or withdrawals because
of adverse events in elderly patients.
Neuropsychiatric adverse events,
including insomnia and
depression, have been reported
in association with ACCOLATE
therapy (see PRECAUTIONS,
Neuropsychiatric Events).
Hypersensitivity reactions,
including urticaria, angioedema
and rashes, with or without
blistering, have also been
reported in association with
ACCOLATE therapy. Additionally,
there have been reports of
patients experiencing
agranulocytosis, bleeding,
bruising, or edema, arthralgia,
myalgia, malaise, and pruritus in
association with ACCOLATE
therapy.
3. ZYFLO Zileuton is an orally active inhibitor of 5-lipoxygenase, the
(zileuton) tablets enzyme that catalyzes the formation of leukotrienes from
arachidonic acid. Zileuton has the chemical name ()-1(1-
Benzo[b]thien-2-ylethyl)-1-hydroxyurea
Zileuton has the molecular formula C11H12N2O2S and a
molecular weight of 236.29. It is a racemic mixture (50:50)
of R(+) and S(-) enantiomers. Zileuton is a practically
odorless, white, crystalline powder that is soluble in
methanol and ethanol, slightly soluble in acetonitrile, and
practically insoluble in water and hexane. The melting
point ranges from 144.2C to 145.2C. ZYFLO tablets for
oral administration are supplied in one dosage strength
containing 600 mg of zileuton.
Inactive Ingredients: crospovidone, hydroxypropyl
cellulose, hypromellose, magnesium stearate,
microcrystalline cellulose, pregelatinized starch, propylene
glycol, sodium starch glycolate, talc, and titanium dioxide.
The recommended dosage of ZYFLO for
the symptomatic treatment of patien ts
with asthma is one 600-mg tablet four
times a day for a total daily dose of
2400 mg. For ease of administration,
ZYFLO may be taken with meals and at
bedtime. Hepatic transaminases should
be evaluated prior to initiation of ZYFLO
and periodically during treatment (see
PRECAUTIONS, Hepatic).
pruritus, somnolence, urinary
HOW SUPPLIED
ZYFLO Tablets are available as 1 dosage
strength: 600-mg white to off white,
ovaloid, film coated tablets debossed
CT 1 on one side and bisect on the
other side. High-density polyethylene
bottles of:
Less common adverse events
occurring at a frequency of
greater than 1% and more
commonly in ZYFLO-treated
patients included: arthralgia,
chest pain, conjunctivitis,
constipation, dizziness, fever,
flatulence, hypertonia, insomnia,
lymphadenopathy, malaise, neck
pain/rigidity, nervousness,
tract infection, vaginitis, and
vomiting.

120
Tablets........................................NDC
10122-901-12

Recommended storage
Store tablets at controlled room
temperature between 20-25C, (68-
77F). See USP. Protect from light.