Sodium Cromoglycate for Oral Inhalation. C23H14Na2O11 Mol Wt. 512.3 CAS No. [15826-37-6] Sodium cromoglycate is a white crystalline odourless powder. It is soluble in 20 parts water at 20oC. Chemically it is the disodium salt of 1, 3-bis (2 carboxychromon 5-yloxy) -2-hydroxypropane.
The active component of INTAL FORTE 5 mg CFC-free is sodium cromoglycate 3.521 w/w. Each canister provides at least 112 actuations each containing 5 mg of sodium cromoglycate. INTAL FORTE 5 mg CFC-free is presented as a metered dose inhaler containing sodium cromoglycate as a suspension in the new non - CFC propellant HFA-227, for inhalation.
INTAL FORTE 5 mg CFC-free is indicated for the preventive treatment of bronchial asthma (which may be due to allergy, exercise, cold air or chemical irritants) in adults and children.
INTAL FORTE 5 mg CFC-free therapy is preventative, it is therefore important that regular dosing should be maintained. The patient should be advised that because several doses may be needed to establish benefit, relief may not be apparent immediately, but may take some weeks to develop. The inhaler should be well shaken, the dust cap removed and after each actuation the aerosol inhaled slowly and deeply. To avoid condensation of moisture in the inhaler and blocking of the spray, exhalation through the inhaler should be avoided. The dust-cap should be replaced following use.
INTAL FORTE CFC-Free DS 1
#114317v1.0
Adults and children
The recommended dosage is 10 mg of sodium cromoglycate (as two 5 mg inhalations of the aerosol) four times daily. (The suggested dosage regimen is two inhalations at bedtime, and on waking in the morning, and at regular intervals of 3 to 6 hours during the day). The dose may be increased to two inhalations six or eight times daily in more severe cases or during periods of high antigen challenge. When the asthmatic condition is stabilised, it is sometimes possible to reduce the dosage, but this must be carefully assessed for each individual patient, to ensure adequate control of asthma. The addition of sodium cromoglycate in patients currently treated with oral or inhaled steroids, may allow reduction or discontinuation of the steroid dose. For protection against bronchospasm induced by exercise or other known trigger factors, INTAL FORTE 5 mg CFC-free should be used 15 - 30 minutes before exposure to the factor concerned. It is essential to instruct the patient how to use the Inhaler correctly. Patients with difficulty coordinating inhalation may find a spacer device or a holding chamber helpful.
INTAL FORTE 5 mg CFC-free is contraindicated in patients with known hypersensitivity to any of its constituents.
INTAL FORTE 5 mg CFC-free should not be used for the relief of an acute attack of bronchospasm. In those cases where reduction of steroid treatment is attempted in patients receiving sodium cromoglycate, the patient must be carefully supervised while the steroid dose is reduced in a stepwise fashion. If possible, peak flow monitoring should be continued during such reductions and patients should be given instructions about what action to take if deterioration of asthma symptoms occurs. If it is necessary to withdraw treatment, it should normally be done progressively over a period of one week. Symptoms of asthma may recur, following withdrawal of treatment. INTAL FORTE 5 mg CFC-free should be discontinued if an eosinophilic pneumonia appears.
Sodium cromoglycate has been used for the treatment of a variety of indications in man for many years and no interactions with other drugs have been reported, nor are expected for sodium cromoglycate, due to its pharmacokinetic properties(no metabolism, moderate plasma protein binding, low plasma concentrations and its high safety profile.
Category A: Cumulative post-marketing experience with sodium cromoglycate does not suggest an association between the drug and congenital defects. It should be used in pregnancy only if the benefit to the mother outweighs the potential risk to the fetus. It is unknown if this drug is excreted in human milk. Cumulative post-marketing experience with sodium cromoglycate used by nursing mothers does not suggest an adverse effect on the infant. It should be used in nursing mothers only if the benefit to the mother outweighs the potential risk to the infant.
INTAL FORTE CFC-Free DS 2
#114317v1.0
INTAL FORTE 5 mg CFC-free has no known effect on ability to drive or operate machinery.
Mild throat irritation, coughing and transient bronchospasm may occur. Hypersensitivity reactions, including angioedema, bronchospasm, hypotension and collapse, have been reported extremely rarely, in patients using inhaled sodium cromoglycate. Very rare cases of eosinophilic pneumonia have been reported. As with other inhalation therapy, paradoxical bronchospasm may occur immediately after administration: in such cases the product should be discontinued and alternative treatment instituted.
Animal studies have shown that sodium cromoglycate has a very low local or systemic toxicity and extended human studies have not revealed any safety hazard with products containing sodium cromoglycate. Overdosage is therefore unlikely to cause problems, but, if suspected, treatment should be supportive and directed to the control of the relevant symptoms.
Sodium cromoglycate inhibits the activation of many of the cell types involved in the development and progression of asthma. Thus, sodium cromoglycate inhibits the release of inflammatory mediators including cytokines from mast cells and reduces the chemotactic activity of eosinophils and neutrophils. Activation of and mediator release from monocytes and macrophages in vitro is also reduced by sodium cromoglycate. Sodium cromoglycate inhibits antigen-induced early and late phase airway obstruction in conscious animals and reduces the influx of inflammatory cells into the airways. The drug also inhibits sensory nerve (C fibre) activation in the dog lung and inflammatory responses induced by neuronal stimulation in the airways of animals. This diverse range of activities of the drug may be explained by the ability of sodium cromoglycate to block chloride channels in different cell types which are important in cell activation. In acute bronchial provocation tests in humans, sodium cromoglycate has been shown to inhibit or diminish the asthmatic reaction to antigen, exercise and to a range of non-specific triggers including cold air, sulphur dioxide, hypertonic saline and bradykinin. Antigen-induced increased bronchial hyperactivity to histamine is prevented and a reduction in bronchial mucus eosinophils and antigen-specific IgE occurs after 4 weeks treatment of asthmatic subjects with sodium cromoglycate.
After inhalation in man via a metered dose inhaler approximately 10% of a dose of sodium cromoglycate is absorbed from the respiratory tract. The remainder is either exhaled or deposited in the oropharynx, or swallowed and eliminated via the alimentary tract, as only a small amount (1%) of the dose is absorbed from the gastrointestinal tract. The rate of absorption of sodium cromoglycate from the respiratory tract is slower than the elimination rate (t1/2 of 1.5 - 2h). Hence, the drug remains effectively in the lungs to produce its local therapeutic effect and is then cleared rapidly from the systemic circulation. No substantial increase in plasma concentrations occurs during repeated dose therapy.
INTAL FORTE CFC-Free DS 3
#114317v1.0
Sodium cromoglycate is moderately and reversibly bound to plasma proteins ( [?] 65%) and is not metabolised in humans. It is excreted unchanged in both urine and bile in approximately equal proportions.
Sodium cromoglycate is not carcinogenic, mutagenic or teratogenic in animals. No evidence of impaired fertility was shown in laboratory animal reproduction studies. By inhalation, even in long-term studies, it proved impossible to achieve toxic dose levels of sodium cromoglycate in a range of mammalian species. Sodium cromoglycate is non-irritating to the eye and nasal mucosa in animal tests.
Polyvinylpyrrolidone (Povidone) K30, polyethylene glycol (PEG) 600, 1,1,1, 2, 3,3,3 heptafluoropropane (HFA 227 - a non ozone depleting propellant).
None known.
24 months
Store below 30degC, not in a refrigerator. As the aerosol inhaler canister is pressurised it should be protected from heat or direct sunlight and should not be punctured or incinerated even when empty. Store out of reach of children.
A metered dose of pressurised aerosol. The aluminium can is fitted with a metering valve which delivers 112 actuations (each containing 5 mg of sodium cromoglycate per shot), after initial priming. If the inhaler is new, it should be primed by actuating 4 times prior to inhalation. Re- priming of the inhaler is not required where periods of non-use are between zero and two days (ie. less than 48 hours). If there is a period of non-use of between 3 and 7 days, additional priming with 2 actuations is advised. If the inhaler is not used beyond seven days, additional priming with 4 actuations is advised. The cartoned pack consists of an aerosol canister and a plastic mouthpiece, with a dust cap. Each pack is individually supplied in a carton together with a patient information leaflet. An additional mouthpiece has been supplied to assist in the cleaning and maintenance of INTAL FORTE 5mg CFC-free.
Distributed by sanofi-aventis new zealand limited Level 8, James & Wells Tower 56 Cawley Street Ellerslie Auckland
INTAL FORTE CFC-Free DS 4
#114317v1.0
Phone: (09) 580 1810
18 July 2011
INTAL FORTE CFC-Free DS 5
#114317v1.0