INFORMATION FOR HEALTH PROFESSIONALS
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ATOMASE AQUEOUS: An aqueous white suspension filled into amber glass bottles fitted with a metered dose pump device delivering 50mcg beclomethasone dipropionate per dose.
ATOMASE FORTE AQUEOUS: An aqueous white suspension filled into amber glass bottles fitted with a metered dose pump device delivering 100mcg beclomethasone dipropionate per spray.
Beclomethasone dipropionate is a diester of beclomethasone, a synthetic corticosteroid chemically related to betamethasone. It differs from betamethasone in having a chlorine at the 9-alpha position in place of fluorine.
Beclomethasone dipropionate has potent anti-inflammatory activity, however, the mechanisms responsible are unknown. The precise mechanism of beclomethasone dipropionate's action in the nose is unknown since biopsies of nasal mucosa have shown no histopathological changes after nasal administration. Similarly, no adrenal insufficiency has been noted after nasal administration by aerosol and none is expected after use of the aqueous spray.
Beclomethasone dipropionate is sparingly soluble in water, however, systemic absorption occurs after all forms of administration. When given by nasal inhalation, it is primarily deposited in the nasal passages. A portion of the medicine is also swallowed.
Absorption occurs rapidly from all respiratory and gastrointestinal tissues. There is no evidence of tissue storage. Many tissues other than the liver have the ability to rapidly metabolise beclomethasone dipropionate, firstly to beclomethasone 17-monopropionate and subsequently to free beclomethasone.
The principal route of excretion of both unchanged medicine and metabolites is the faeces, irrespective of the route of administration. In humans, only 12-15% of a dose can be expected to appear in urine as both conjugated and free metabolites. The half-life of beclomethasone dipropionate in humans is approximately 15 hours. Plasma protein binding is approximately 87%.
ATOMASE AQUEOUS, and ATOMASE FORTE AQUEOUS nasal sprays are indicated for the relief of the symptoms of seasonal or perennial allergic and non-allergic (vasomotor) rhinitis.
Clinical trials have shown that significant symptomatic relief may be obtained within three days. However, symptomatic relief may not occur in some patients for as long as two weeks. Beclomethasone dipropionate aqueous nasal sprays should not be continued beyond three weeks in the absence of significant symptomatic improvement and should not be used in the presence of untreated localised infection involving the nasal mucosa.
ATOMASE AQUEOUS, and ATOMASE FORTE AQUEOUS nasal sprays are 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.
ADULTS AND CHILDREN 6 YEARS OF AGE AND OLDER: The usual dose is one to two inhalations into each nostril twice a day. The maximum recommended dose is 8 sprays (400mcg) per day. In patients who respond, an improvement in symptoms of seasonal or perennial rhinitis usually becomes apparent within a few days of initiation of therapy. Up to two weeks may, however, be required. The spray should not be continued beyond three weeks in the absence of significant symptomatic improvement. ATOMASE AQUEOUS nasal sprays are not recommended for children below 6 years of age.
ADULTS:
The usual dose is one inhalation into each nostril twice a day up to a maximum of 4 sprays (400mcg) per day. In patients who respond, an improvement in symptoms of seasonal or perennial rhinitis usually becomes apparent within a few days of initiation of therapy. Up to two weeks may, however, be required. The spray should not be continued beyond three weeks in the absence of significant symptomatic improvement. ATOMASE FORTE AQUEOUS nasal spray is not recommended for children.Hypersensitivity to beclomethasone dipropionate.
GENERAL: The replacement of a systemic corticosteroid with ATOMASE AQUEOUS, and ATOMASE FORTE AQUEOUS nasal sprays can be accompanied by signs of adrenal insufficiency.
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, acne-form lesions and cushingoid features. If such changes occur, ATOMASE AQUEOUS, and ATOMASE FORTE AQUEOUS nasal sprays should be discontinued slowly, consistent with accepted procedures for discontinuing oral steroid therapy.
Intranasal corticosteroids may cause a reduction in growth velocity when administered to paediatric patients (see Paediatric Use)
During withdrawal from oral steroids, some patients may experience symptoms of withdrawal, eg. joint and/or muscular pain, lassitude and depression. Rarely, immediate hypersensitivity reactions may occur with the intranasal administration of beclomethasone. Extremely rare instances of wheezing, nasal septum perforation, and increased intraocular pressure have been reported following the intranasal application of aerosolised corticosteroids.
Although these have not been observed in clinical trials with beclomethasone dipropionate nasal spray, vigilance should be maintained.
In clinical studies with beclomethasone dipropionate administered intranasally, the development of localised 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 or discontinuation of treatment with ATOMASE, ATOMASE AQUEOUS, or ATOMASE FORTE AQUEOUS nasal spray.
If persistent nasopharyngeal irritation occurs, it may be an indication for stopping ATOMASE, ATOMASE AQUEOUS, or ATOMASE FORTE AQUEOUS nasal spray. Beclomethasone dipropionate is absorbed into the circulation after both oral and nasal administration. Use of excessive doses of beclomethasone dipropionate may suppress HPA function.
Beclomethasone dipropionate aerosols should be used with caution, if at all, in patients with active or quiescent tuberculous infections of the respiratory tract; untreated fungal, bacterial or systemic viral infections; or ocular herpes simplex.
For ATOMASE AQUEOUS, or ATOMASE FORTE AQUEOUS nasal sprays to be effective in the treatment of nasal polyps, the spray must be able to enter the nose. Therefore, treatment of nasal polyps with ATOMASE AQUEOUS, or ATOMASE FORTE AQUEOUS nasal sprays should be considered adjunctive therapy to surgical removal and/or the use of other medications that will permit effective penetration of ATOMASE AQUEOUS, or ATOMASE FORTE AQUEOUS nasal sprays into the nose. Nasal polyps may recur after any form of treatment.
As with any long-term treatment, patients using ATOMASE AQUEOUS, or ATOMASE FORTE AQUEOUS nasal sprays 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 trauma should not use a nasal corticosteroid until healing has occurred.
The long-term effects of beclomethasone dipropionate in human subjects are still unknown. In particular the local effects on developmental or immunologic processes in the mouth, pharynx, nose, trachea and lung are unknown. There is also no information available about the possible long term systemic effects of inhaled beclomethasone dipropionate.
Although systemic effects have been minimal with recommended doses, this potential increases with excessive doses. Therefore, larger than recommended doses should be avoided.
INFORMATION FOR PATIENTS: Patients being treated with beclomethasone dipropionate aerosols should receive the following information and instructions. This information is intended to aid in the safe and effective use of medication. It is not a disclosure of all possible adverse or intended effects. Patients should use beclomethasone dipropionate aerosols at regular intervals since effectiveness depends on regular use. The patients should take the medication as directed.
Beclomethasone dipropionate is not acutely effective, and the prescribed dosage should not be increased. Instead, where beclomethasone dipropionate is to be administered intranasally, vasoconstrictors or oral anti-histamines may be needed until the effects of ATOMASE AQUEOUS, or ATOMASE FORTE AQUEOUS nasal spray is fully manifested. One to two weeks may pass before full relief is obtained. The patient should contact the doctor if symptoms do not improve, if the condition worsens, or if sneezing or nasal irritation occurs.
For the proper use of the aerosols and to attain maximum improvement, the patients should read and follow the accompanying patient instructions carefully.
CARCINOGENESIS, MUTAGENESIS, IMPAIRMENT OF FERTILITY: Treatment of rats for a total of 95 weeks, 13 weeks by inhalation and 82 weeks by the oral route, resulted in no evidence of carcinogenic activity. Mutagenic studies have not been performed. Impairment of fertility, as evidenced by inhibition of the estrous cycle in dogs, was observed following treatment by the oral route. No inhibition of the estrous cycles in dogs was seen following treatment with beclomethasone dipropionate by the inhalation route.
The oral LD50 of beclomethasone is > 1g/kg in rodents.
PREGNANCY: Like other corticosteroids, parenteral (subcutaneous) beclomethasone dipropionate has been shown to be teratogenic and embryocidal in the mouse and rabbit when given in doses approximately ten times the human dose. In these studies beclomethasone was found to produce foetal resorption, cleft palate, agnathia, microstomia, absence of tongue, delayed ossification, and agenesis of thymus.
No teratogenic or embryocidal effects have been seen in the rat when beclomethasone dipropionate was administered by inhalation at ten times the human dose or orally at 1,000 times the human dose. 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 foetus.
Hypoadrenalism may occur in infants born of mothers receiving corticosteroids during pregnancy. Such infants should be carefully observed.
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 beclomethasone dipropionate aerosols are administered to a nursing woman.
PAEDIATRIC USE: The safety and effectiveness in children below 6 years of age has not been established. Controlled clinical studies have shown that intranasal corticosteroids may cause a reduction in growth velocity in paediatric patients. This effect has been observed in the absence of laboratory evidence of hypothalamic-pituitary-adrenal (HPA) axis suppression, suggesting that growth velocity is a more sensitive indicator of systemic corticosteroid exposure in paediatric 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 paediatric patients receiving intranasal corticosteroids, should be monitored routinely (e.g. via stadiometry). The potential growth effects of prolonged treatment should be weighed against clinical benefits obtained and the availability of safe and effective non corticosteroid treatment alternatives. To minimize the systemic effects of intranasal corticosteroids, each patient should be titrated to his/her lowest effective dose.
Deaths due to adrenal insufficiency have occured in asthmatic patients during and after transfer from systemic corticosteroids to aerosol beclomethasone dipropionate. Suppression of HPA function (reduction of early morning plasma cortisol levels) has been reported in adult patients who received orally inhaled beclomethasone dipropionate at doses of 1600mcg daily for one month.
Localised infections with Candida albicans or Aspergillus niger have occurred. Some patients on oral therapy have complained of hoarseness or dry mouth. Rare cases of immediate or delayed hypersensitivity reactions, including urticaria, angioedema, rash and bronchospasm have been reported after the use of beclomethasone oral or nasal aerosols.
In general, side effects of nasal administration are primarily associated with irritation of the nasal mucous membranes.
Adverse reactions reported in controlled clinical trials and open studies are as follows: mild nasopharyngeal irritation in up to 24% of patients treated and occasional sneezing attacks in up to 4% occurring immediately following use.
No patient had to discontinue treatment and the incidence was similar to those patients receiving placebo. Other reactions have been: headache, nausea, light-headedness, nasal stuffiness, nosebleeds, rhinorrhea, and teary eyes. Rare instances of wheezing, nasal septum perforation and increased intraocular pressure have been reported.
The immediate activity of ATOMASE AQUEOUS, or ATOMASE FORTE AQUEOUS nasal sprays may be enhanced by use of a nasal vasoconstrictor in the early stages of treatment.
Excessive use may result in the development of systemic corticosteroid effects such as hypercorticism and adrenal suppression. If this occurs the spray should be discontinued slowly, consistent with accepted procedures for discontinuing oral steroid therapy. Acute overdosage is unlikely.
Keep all sprays out of reach of children. Store below 30°C. Protect from light.
Atomase Aqueous Nasal Spray (50mcg) - Pharmacist Medicine
Atomase Forte Aqueous Nasal Spray (100mcg) - Prescription Medicine.
200 doses.
Beclomethasone dipropionate is 9α-chloro-11β,17α,21-trihydroxy-16β-methylpregna-1,4-diene-3,20-dione17,21-dipropionate. Its molecular formula and weight are C28H37ClO7 and 521 respectively.
Other ingredients are: water, glycerine, dispersible cellulose and benzalkonium chloride.
Douglas Pharmaceuticals Ltd
PO Box 45-027
AUCKLAND 8
Ph: (09) 835-0660
Fax: (09) 835-0665
6 August 2001