Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/2579
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BECONASE AQ (Spray)
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Adults and Children 12 Years of Age and Older: The usual dosage is 1 or 2 nasal inhalations (42 to 84 mcg)
in each nostril twice a day (total dose, 168 to 336 mcg/day).<br/>Children 6 to 12 Years of Age: Patients should be started with 1 nasal inhalation in each
nostril twice daily; patients not adequately responding to 168 mcg or
those with more severe symptoms may use 336 mcg (2 inhalations in each
nostril). Once adequate control is achieved, the dosage should be decreased
to 84 mcg (1 spray in each nostril) twice daily. BECONASE AQ Nasal Spray
is not recommended for children below
6 years of age. The maximum total daily dosage should
not exceed 2 sprays in each nostril twice daily (336 mcg/day). In
patients who respond to BECONASE AQ Nasal Spray, an improvement of the symptoms
of seasonal or perennial rhinitis usually becomes apparent within a few days
after the start of therapy with BECONASE AQ Nasal Spray. However, symptomatic
relief may not occur in some patients for as long as 2 weeks. BECONASE
AQ Nasal Spray should not be continued beyond 3 weeks in the absence
of significant symptomatic improvement. The therapeutic
effects of corticosteroids, unlike those of decongestants, are not immediate.
This should be explained to the patient in advance in order to ensure cooperation
and continuation of treatment with the prescribed dosage regimen. In
the presence of excessive nasal mucous secretion or edema of the nasal mucosa,
the drug may fail to reach the site of intended action. In such cases it is
advisable to use a nasal vasoconstrictor during the first 2 to 3 days
of therapy with BECONASE AQ Nasal Spray.<br/>Directions for Use: Illustrated Patient's Instructions for Use accompany each
package of BECONASE AQ Nasal Spray.
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Beclomethasone dipropionate, monohydrate, the active component
of BECONASE AQ Nasal Spray, is an anti-inflammatory steroid having the chemical
name 9-chloro-11��,17,21-trihydroxy-16��-methylpregna-1,4-diene-3,20-dione
17,21-dipropionate, monohydrate and the following chemical structure: Beclomethasone
17,21-dipropionate is a diester of beclomethasone, a synthetic halogenated
corticosteroid. Beclomethasone dipropionate, monohydrate is a white to creamy-white,
odorless powder with a molecular weight of 539.06. It is very slightly soluble
in water, very soluble in chloroform, and freely soluble in acetone and in
ethanol. BECONASE AQ Nasal Spray is a metered-dose,
manual pump spray unit containing a microcrystalline suspension of beclomethasone
dipropionate, monohydrate equivalent to 42 mcg of beclomethasone dipropionate,
calculated on the dried basis, in an aqueous medium containing microcrystalline
cellulose, carboxymethylcellulose sodium, dextrose, benzalkonium chloride,
polysorbate 80, and 0.25% v/w phenylethyl alcohol. The pH through expiry
is 5.0 to 6.8. After initial priming (6 actuations),
each actuation of the pump delivers from the nasal adapter 100 mg of
suspension containing beclomethasone dipropionate, monohydrate equivalent
to 42 mcg of beclomethasone dipropionate. If the pump is not used for
7 days, it should be primed until a fine spray appears. Each 25-g bottle
of BECONASE AQ Nasal Spray provides 180 metered sprays.
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Mechanism of Action: Following topical administration, beclomethasone dipropionate
produces anti-inflammatory and vasoconstrictor effects. The mechanisms responsible
for the anti-inflammatory action of beclomethasone dipropionate are unknown.
Corticosteroids have been shown to have a wide range of effects on multiple
cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, and lymphocytes)
and mediators (e.g., histamine, eicosanoids, leukotrienes, and cytokines)
involved in inflammation. The direct relationship of these findings to the
effects of beclomethasone dipropionate on allergic rhinitis symptoms is not
known. Biopsies of nasal mucosa obtained during clinical
studies showed no histopathologic changes when beclomethasone dipropionate
was administered intranasally. Beclomethasone dipropionate
is a pro-drug with weak glucocorticoid receptor binding affinity. It is hydrolyzed
via esterase enzymes to its active metabolite beclomethasone-17-monopropionate
(B-17-MP), which has high topical anti-inflammatory activity.<br/>Pharmacokinetics:<br/>Absorption: Beclomethasone
dipropionate is sparingly soluble in water. When given by nasal inhalation
in the form of an aqueous or aerosolized suspension, the drug is deposited
primarily in the nasal passages. The majority of the drug is eventually swallowed.
Following intranasal administration of aqueous beclomethasone dipropionate,
the systemic absorption was assessed by measuring the plasma concentrations
of its active metabolite B-17-MP, for which the absolute bioavailability following
intranasal administration is 44% (43% of the administered dose came from the
swallowed portion and only 1% of the total dose was bioavailable from the
nose). The absorptionof unchanged beclomethasone dipropionate following oral
and intranasal dosing was undetectable (plasma concentrations<50 pg/mL).<br/>Distribution: The tissue distribution at steady state for beclomethasone
dipropionate is moderate (20 L) but more extensive for B-17-MP (424 L).
There is no evidence of tissue storage of beclomethasone dipropionate or its
metabolites. Plasma protein binding is moderately high (87%).<br/>Metabolism: Beclomethasone dipropionate is cleared very rapidly from
the systemic circulation by metabolism mediated via esterase enzymes that
are found in most tissues. The main product of metabolism is the active metabolite
(B-17-MP). Minor inactive metabolites, beclomethasone-21-monopropionate (B-21-MP)
and beclomethasone (BOH), are also formed, but these contribute little to
systemic exposure.<br/>Elimination: The elimination of beclomethasone dipropionate and B-17-MP
after intravenous administration are characterized by high plasma clearance
(150 and 120 L/hour) with corresponding terminal elimination half-lives
of 0.5 and 2.7 hours. Following oral administration of tritiated beclomethasone
dipropionate, approximately 60% of the dose was excreted in the feces within
96 hours, mainly as free and conjugated polar metabolites. Approximately
12% of the dose was excreted as free and conjugated polar metabolites in the
urine. The renal clearance of beclomethasone dipropionate and its metabolites
is negligible.<br/>Pharmacodynamics: The effects of beclomethasone dipropionate on hypothalamic-pituitary-adrenal
(HPA) function have been evaluated in adult volunteers by other routes of
administration. Studies with beclomethasone dipropionate by the intranasal
route may demonstrate that there is more or that there is less absorption
by this route of administration. There was no suppression of early morning
plasma cortisol concentrations when beclomethasone dipropionate was administered
in a dose of 1,000 mcg/day for 1 month as an oral aerosol or for
3 days by intramuscular injection. However, partial suppression of plasma
cortisol concentrationswas observed when beclomethasone dipropionate was
administered in doses of 2,000 mcg/day either by oral aerosol or intramuscular
injection. Immediate suppression of plasma cortisol concentrations was observed
after single doses of 4,000 mcg of beclomethasone dipropionate. Suppression
of HPA function (reduction of early morning plasma cortisol levels) has been
reported in adult patients who received 1,600-mcg daily doses of oral beclomethasone
dipropionate for 1 month. In clinical studies using beclomethasone dipropionate
aerosol intranasally, there was no evidence of adrenal insufficiency. The
effect of BECONASE AQ Nasal Spray on HPA function was not evaluated but would
not be expected to differ from intranasal beclomethasone dipropionate aerosol. In
1 study in children with asthma, the administration of inhaled beclomethasone
at recommended daily doses for at least 1 year was associated with a
reduction in nocturnal cortisol secretion. The clinical significance of this
finding is not clear. It reinforces other evidence, however, that topical
beclomethasone may be absorbed in amounts that can have systemic effects and
that physicians should be alert for evidence of systemic effects, especially
in chronically treated patients (see PRECAUTIONS).
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Hypersensitivity to
any of the ingredients of this preparation contraindicates its use.
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BECONASE AQ Nasal Spray,
42 mcg is supplied in an amber glass bottle fitted with a metering atomizing
pump and nasal adapter in a box of 1 (NDC 0173-0388-79) with patient's
instructions for use. Each bottle contains 25 g of suspension and will
provide 180 metered sprays. The correct amount of medication
in each spray cannot be assured after 180 sprays even though the bottle is
not completely empty. The bottle should be discarded when the labeled number
of actuations has been used. Store
between 15��and 30��C (59��and 86��F). GlaxoSmithKline Research
Triangle Park, NC 27709 April 2005 RL-2182
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General: Intranasal corticosteroids may cause a reduction in growth
velocity when administered to pediatric patients (see PRECAUTIONS: Pediatric
Use). During withdrawal from oral corticosteroids,
some patients may experience symptoms of withdrawal, e.g., joint and/or muscular
pain, lassitude, and depression. Rarely, immediate
hypersensitivity reactions may occur after the intranasal administration of
beclomethasone (see ADVERSE REACTIONS). Rare instances
of nasal septum perforation have been spontaneously reported. Rare
instances of wheezing, cataracts, glaucoma, and increased intraocular pressure
have been reported following the intranasal use of beclomethasone dipropionate. In
clinical studies with beclomethasone dipropionate administered intranasally,
the development of localized infections of the nose and pharynx with Candida albicans has occurred only rarely. When
such an infection develops, it may require treatment with appropriate local
therapy and discontinuation of treatment with BECONASE AQ Nasal Spray. If
persistent nasopharyngeal irritation occurs, it may be an indication for stopping
BECONASE AQ Nasal Spray. Beclomethasone dipropionate
is absorbed into the circulation. Use of excessive doses of BECONASE AQ Nasal
Spray may suppress HPA function. Intranasal corticosteroids
should be used with caution, if at all, in patients with active or quiescent
tuberculous infections of the respiratory tract, untreated local or systemic
fungal or bacterial infections, systemic viral or parasitic infections, or
ocular herpes simplex. For BECONASE AQ Nasal Spray
to be effective in the treatment of nasal polyps, the spray must be able to
enter the nose. Therefore, treatment of nasal polyps with BECONASE AQ Nasal
Spray should be considered adjunctive therapy to surgical removal and/or the
use of other medications that will permit effective penetration of BECONASE
AQ Nasal Spray into the nose. Nasal polyps may recur after any form of treatment. As
with any long-term treatment, patients using BECONASE AQ Nasal Spray over
several months or longer should be examined periodically for possible changes
in the nasal mucosa. Because of the inhibitory effect
of corticosteroids on wound healing, patients who have experienced recent
nasal septal ulcers, nasal surgery, or nasal trauma should not use a nasal
corticosteroid until healing has occurred. Although
systemic effects have been minimal with recommended doses, this potential
increases with excessive doses. Therefore, larger than recommended doses should
be avoided.<br/>Information for Patients: Patients being treated with BECONASE AQ Nasal Spray should
receive the following information and instructions. This information is intended
to aid them in the safe and effective use of this medication. It is not a
disclosure of all possible adverse or intended effects. Patients
should use BECONASE AQ Nasal Spray at regular intervals since its effectiveness
depends on its regular use. The patient should take the medication as directed.
It is not acutely effective, and the prescribed dosage should not be increased.
Instead, nasal vasoconstrictors or oral antihistamines may be needed until
the effects of BECONASE AQ Nasal Spray are fully manifested. One to 2 weeks
may pass before full relief is obtained. The patient should contact the physician
if symptoms do not improve, if the condition worsens, or if sneezing or nasal
irritation occurs. For the proper use of BECONASE
AQ Nasal Spray and to attain maximum improvement, the patient should read
and follow carefully the patient's instructions accompanying the product. Persons
who are using immunosuppressant doses of corticosteroids should be warned
to avoid exposure to chickenpox or measles. Patients should also be advised
that if they are exposed, medical advice should be sought without delay.<br/>Carcinogenesis, Mutagenesis, Impairment of Fertility: The carcinogenicity of beclomethasone dipropionate was evaluated
in rats that were exposed for a total of 95 weeks, 13 weeks at inhalation
doses up to 0.4 mg/kg and the remaining 82 weeks at combined oral
and inhalation doses up to 2.4 mg/kg. There was no evidence of carcinogenicity
in this study at the highest dose, approximately 60 times the maximum recommended
daily intranasal dose in adults on a mg/mbasis or approximately
35 times the maximum recommended daily intranasal dose in children on
a mg/mbasis. Beclomethasone dipropionate
did not induce gene mutation in bacterial cells or mammalian Chinese hamster
ovary (CHO) cells in vitro. No significant clastogenic effect was seen in
cultured CHO cells in vitro or in the mouse micronucleus test in vivo. In
rats, beclomethasone dipropionate caused decreased conception rates at an
oral dose of 16 mg/kg (approximately 390 times the maximum recommended
daily intranasal dose in adults on a mg/mbasis). There was no
significant effect of beclomethasone dipropionate on fertility in rats at
oral doses of 1.6 mg/kg (approximately 40 times the maximum recommended
daily intranasal dose in adults on a mg/mbasis). Inhibition of
the estrous cycle in dogs was observed following oral dosing at 0.5 mg/kg
(approximately 40 times the maximum recommended daily intranasal dose in adults
on a mg/mbasis). No inhibition of the estrous cycle in dogs was
seen following 12 months' exposure at an estimated inhalation
dose of 0.33 mg/kg (approximately 25 times the maximum recommended daily
intranasal dose in adults on a mg/mbasis).<br/>Pregnancy:<br/>Teratogenic Effects: Pregnancy Category
C. Like other corticosteroids, beclomethasone dipropionate was teratogenic
and embryocidal in the mouse and rabbit at a subcutaneous dose of 0.1 mg/kg
in mice or 0.025 mg/kg in rabbits (approximately equal to the maximum
recommended daily intranasal dose in adults on a mg/mbasis).
No teratogenicity or embryocidal effects were seen in rats when exposed to
an inhalation dose of 0.1 mg/kg plus oral doses of up to 10 mg/kg
per day for a combined dose of 10.1 mg/kg (approximately 240 times the
maximum recommended daily intranasal dose in adults on a mg/mbasis). There
are no adequate and well-controlled studies in pregnant women. Beclomethasone
dipropionate should be used during pregnancy only if the potential benefit
justifies the potential risk to the fetus.<br/>Nonteratogenic Effects: Hypoadrenalism may occur in infants born of mothers receiving
corticosteroids during pregnancy. Such infants should be carefully observed.<br/>Nursing Mothers: It is not known whether beclomethasone dipropionate is excreted
in human milk. Because other corticosteroids are excreted in human milk, caution
should be exercised when BECONASE AQ Nasal Spray is administered to a nursing
woman.<br/>Pediatric Use: The safety and effectiveness of BECONASE AQ Nasal Spray
have been established in children aged 6 years and above through evidence
from extensive clinical use in adult and pediatric patients. The safety and
effectiveness of BECONASE AQ Nasal Spray in children below 6 years of
age have not been established. Controlled clinical
studies have shown that intranasal corticosteroids may cause a reduction in
growth velocity in pediatric patients. This effect has been observed in the
absence of laboratory evidence of HPA axis suppression, suggesting that growth
velocity is a more sensitive indicator of systemic corticosteroid exposure
in pediatric patients than some commonly used tests of HPA axis function.
The long-term effects of this reduction in growth velocity associated with
intranasal corticosteroids, including the impact on final adult height, are
unknown. The potential for���catch-up���growth following discontinuation
of treatment with intranasal corticosteroids has not been adequately studied.
The growth of pediatric patients receiving intranasal corticosteroids, including
BECONASE AQ Nasal Spray, should be monitored routinely (e.g., via stadiometry).
The potential growth effects of prolonged treatment should be weighed against
the clinical benefits obtained and the risks/benefits of treatment alternatives.
To minimize the systemic effects of intranasal corticosteroids, including
BECONASE AQ Nasal Spray, each patient should be titrated to the lowest dose
that effectively controls his/her symptoms. In a double-blind,
controlled trial, 100 children between the ages of 6 and 9��years
with allergic rhinitis were randomized to receive aqueous intranasal beclomethasone
dipropionate 168 mcg twice daily or placebo for 1 year. As measured
by stadiometry, children who received beclomethasone dipropionate grew more
slowly than those who received placebo. A difference in mean change in height
was observed within 1 month of drug initiation. At the end of 12 months,
the beclomethasone dipropionate-treated group had a growth velocity on average
of4.75 cm/year compared to 6.20 cm/year in the placebo group (p<0.01).
While the placebo group had an expected distribution of growth velocity, approximately
50% of the beclomethasone dipropionate-treated children grew below the 10percentile. In
children 7.3 years of age, the mean age of children in this study, the
range for expected growth velocity is: boys���3percentile
= 4.1 cm/year, 50percentile = 5.8 cm/year, and 97percentile
= 7.5 cm/year; girls���3percentile = 4.3 cm/year,
50percentile = 5.9 cm/year, and 97percentile
= 7.5 cm/year. The potential reversibility of the reduction in growth
velocity was not studied. No significant differences were observed between
the 2 groups for mean basal plasma cortisol or ACTH-stimulated plasma cortisol
levels.<br/>Geriatric Use: Clinical studies of BECONASE AQ Nasal Spray did not include
sufficient numbers of subjects aged 65 and over to determine whether they
respond differently from younger subjects. Other reported clinical experience
has not identified differences in responses between the elderly and younger
patients. In general, dose selection for an elderly patient should be cautious,
starting at the low end of the dosing range, reflecting the greater frequency
of decreased hepatic, renal, or cardiac function, and of concomitant disease
or other drug therapy.
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When used at excessive doses, systemic corticosteroid effects
such as hypercorticism and adrenal suppression may appear. If such changes
occur, BECONASE AQ Nasal Spray should be discontinued slowly consistent with
accepted procedures for discontinuing oral steroid therapy. No deaths occurred
when beclomethasone dipropionate was given as single oral doses of 3,000 mg/kg
to mice (approximately 36,000 times the maximum recommended daily intranasal
dose in adults on a mg/mbasis, or approximately 21,000 times
the maximum recommended daily intranasal dose in children on a mg/mbasis)
and 2,000 mg/kg to rats (approximately 48,000 times the maximum recommended
daily intranasal dose in adults or approximately 29,000 times the maximum
recommended daily intranasal dose in children on a mg/mbasis).
One bottle of BECONASE AQ Nasal Spray contains beclomethasone dipropionate,
monohydrate equivalent to 10.5 mg of beclomethasone dipropionate; therefore,
acute overdosage is unlikely.
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beclomethasone dipropionate monohydrate
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BECONASE AQ (Spray)
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In general, side effects in clinical studies have been primarily
associated with irritation of the nasal mucous membranes. Adverse
reactions reported in controlled clinical trials and open studies in patients
treated with BECONASE AQ Nasal Spray are described below. Mild
nasopharyngeal irritation following the use of beclomethasone aqueous nasal
spray has been reported in up to 24% of patients treated, including occasional
sneezing attacks (about 4%) occurring immediately following use of the spray.
In patients experiencing these symptoms, none had to discontinue treatment.
The incidence of transient irritation and sneezing was approximately the same
in the group of patients who received placebo in these studies, implying that
these complaints may be related to vehicle components of the formulation. Fewer
than 5 per 100 patients reported headache, nausea, or lightheadedness following
the use of BECONASE AQ Nasal Spray. Fewer than 3 per 100 patients reported
nasal stuffiness, nosebleeds, rhinorrhea, or tearing eyes. Rare
cases of ulceration of the nasal mucosa and instances of nasal septum perforation
have been spontaneously reported (see PRECAUTIONS). Reports
of dryness and irritation of the nose and throat and unpleasant taste and
smell have been received. There are rare reports of loss of taste and smell. Rare
instances of wheezing, cataracts, glaucoma, and increased intraocular pressure
have been reported following the use of intranasal beclomethasone dipropionate
(see PRECAUTIONS). Rare cases of immediate and delayed
hypersensitivity reactions, including anaphylactoid/anaphylactic reactions,
urticaria, angioedema, rash, and bronchospasm, have been reported following
the oral and intranasal inhalation of beclomethasone dipropionate. Cases
of growth suppression have been reported for intranasal corticosteroids, including
BECONASE AQ (see PRECAUTIONS: Pediatric Use).
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dailymed-instance:warning |
The replacement of a systemic corticosteroid with BECONASE
AQ Nasal Spray can be accompanied by signs of adrenal insufficiency. Careful
attention must be given when patients previously treated for prolonged periods
with systemic corticosteroids are transferred to BECONASE AQ Nasal Spray.
This is particularly important in those patients who have associated asthma
or other clinical conditions where too rapid a decrease in systemic corticosteroids
may cause a severe exacerbation of their symptoms. If
recommended doses of intranasal beclomethasone are exceeded or if individuals
are particularly sensitive or predisposed by virtue of recent systemic steroid
therapy, symptoms of hypercorticism may occur, including very rare cases of
menstrual irregularities, acneiform lesions, cataracts, and cushingoid features.
If such changes occur, BECONASE AQ Nasal Spray should be discontinued slowly
consistent with accepted procedures for discontinuing oral steroid therapy. Persons
who are using drugs that suppress the immune system are more susceptible to
infections than healthy individuals. Chickenpox and measles, for example,
can have a more serious or even fatal course in susceptible children or adults
using corticosteroids. In children or adults who have not had these diseases
or been properly immunized, particular care should be taken to avoid exposure.
How the dose, route, and duration of corticosteroid administration affect
the risk of developing a disseminated infection is not known. The contribution
of the underlying disease and/or prior corticosteroid treatment to the risk
is also not known. If exposed to chickenpox, prophylaxis with varicella zoster
immune globulin (VZIG) may be indicated. If exposed to measles, prophylaxis
with pooled intramuscular immunoglobulin (IG) may be indicated. (See the respective
package inserts for complete VZIG and IG prescribing information.) If chickenpox
develops, treatment with antiviral agents may be considered. Avoid
spraying in eyes.
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BECONASE AQ Nasal Spray is indicated for the relief of the
symptoms of seasonal or perennial allergic and nonallergic (vasomotor) rhinitis. Results
from 2 clinical trials have shown that significant symptomatic relief was
obtained within 3 days. However, symptomatic relief may not occur in
some patients for as long as 2 weeks. BECONASE AQ Nasal Spray should
not be continued beyond 3 weeks in the absence of significant symptomatic
improvement. BECONASE AQ Nasal Spray should not be used in the presence of
untreated localized infection involving the nasal mucosa. BECONASE
AQ Nasal Spray is also indicated for the prevention of recurrence of nasal
polyps following surgical removal. Clinical studies
have shown that treatment of the symptoms associated with nasal polyps may
have to be continued for several weeks or more before a therapeutic result
can be fully assessed. Recurrence of symptoms due to polyps can occur after
stopping treatment, depending on the severity of the disease.
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BECONASE AQ
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