INFORMATION FOR HEALTH PROFESSIONALS
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ATOMASE Aqueous Nasal Spray: An aqueous white suspension filled into amber glass bottles fitted with a metered dose pump device delivering 50mcg beclomethasone dipropionate per dose.
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 mechanisms 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 Nasal Spray is indicated for the short term treatment or prophylaxis of seasonal allergic rhinitis (hayfever) in children and adults over the age of 12 years.
Clinical trials have shown that significant symptomatic relief may be obtained within three days. Treatment with beclomethasone dipropionate aqueous nasal sprays should not be continued beyond seven days in the absence of significant symptomatic improvement and should not be used in the presence of untreated localised infection involving the nasal mucosa.
ADULTS AND CHILDREN 12 YEARS OF AGE AND OLDER: The usual dose is one to two sprays 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 rhinitis usually becomes apparent within a few days of initiation of therapy. ATOMASE Aqueous Nasal Spray should not be continued beyond seven days in the absence of significant symptomatic improvement.
The dose may be reduced to two sprays into each nostril once daily after the first few days of therapy.
ATOMASE Aqueous Nasal Spray is not recommended for children below 12 years of age.
Hypersensitivity to beclomethasone dipropionate.
GENERAL: The replacement of a systemic corticosteroid with ATOMASE Aqueous Nasal Spray 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 Nasal Spray should be discontinued slowly, consistent with accepted procedures for discontinuing oral steroid therapy.
Because of the possible risk of adrenal suppression, the use of ATOMASE Aqueous Nasal Spray currently with other corticosteroid products (eg. tablets, inhalers, nasal inhalers, eye/nose drops) is not recommened.
During withdrawal from oral steroids, some patients may experience symptoms of withdrawal, e.g. 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 clincial 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 Aqueous Nasal Spray.
Beclomethasone dipropionate 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. Treatement should be discontinued if signs or symptoms of nasal infection develop.
If persistent nasopharyngeal irritation occurs, it may be an indication for stopping ATOMASE 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.
As with any long-term treatment, patients using ATOMASE Aqueous Nasal Spray over several months or longer should be examined periodically for possible changes in the nasal mucosa. The use of ATOMASE Aqueous Nasal Spray for longer than 3-6 months without medical assessment is not recommended.
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.
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 aqueous nasal sprays, 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 aqueous nasal sprays 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 Nasal Spray are fully manifested. One to two weeks may pass before full relief is obtained. The patient should contact the doctor if symptoms do not improve, or if the condition worsens, or if sneezing or nasal irritation occurs.
For the proper use of ATOMASE Aqueous Nasal Spray 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 12 years of age has not been established.
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, lightheadedness, 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 Nasal Spray 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 out of reach of children. Store below 30°C. Protect from light.
ATOMASE Aqeuous Nasal Spray (50mcg) - Pharmacist Only Medicine
200 doses.
Beclomethasone dipropionate is 9a-chloro-11B,17a,21-trihydroxy-16B-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
3 December, 1998