Consumer medicine information

1. Why am I using Rilast Rapihaler?

Rilast Rapihaler contains two active ingredients in one inhaler: budesonide and formoterol fumarate dihydrate. Rilast Rapihaler is used for treatment of asthma in adults and adolescents (12 years and over) or Chronic Obstructive Pulmonary Disease (COPD) in adults (18 years and over).
For more information, see Section 1. Why am I using Rilast Rapihaler? in the full CMI.

2. What should I know before I use Rilast Rapihaler?

Do not use if you have ever had an allergic reaction to any medicine containing budesonide or formoterol, or any of the ingredients listed at the end of the CMI.
Talk to your doctor if you have any other medical conditions, take any other medicines, or are pregnant or plan to become pregnant or are breastfeeding.
For more information, see Section 2. What should I know before I use Rilast Rapihaler? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with Rilast Rapihaler and affect how it works. A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use Rilast Rapihaler?

• Rilast Rapihaler should be inhaled into your lungs through the mouth.

• Follow all directions given to you by your doctor or pharmacist.

5. What should I know while using Rilast Rapihaler?

6. Are there any side effects?

All medicines can have side effects. If you do experience any side effects, most of them are minor and temporary. These include sore, yellowish, raised patches in the mouth (thrush), hoarse voice, unpleasant taste in your mouth, pounding heart, headache, trembling or muscle cramps. However, some side effects may need medical attention. These include severe allergic reactions such as difficulty breathing, swelling of the face, lips or tongue, severe rash or pneumonia (lung infection), signs include fever or chills, increased phlegm or a change in colour, increased cough or difficulties breathing. Serious side effects are rare.
For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

1 Name of Medicine

Budesonide.
Formoterol fumarate dihydrate.

2 Qualitative and Quantitative Composition

Rilast Rapihaler is a pressurised metered dose inhaler (pMDI).
The following strengths are registered:
Rilast Rapihaler 100/3. Each delivered dose (the dose that leaves the mouthpiece) contains as active constituents: budesonide 80 microgram/inhalation and formoterol 2.25 microgram/inhalation.
Rilast Rapihaler 200/6. Each delivered dose (the dose that leaves the mouthpiece) contains as active constituents: budesonide 160 microgram/inhalation and formoterol 4.5 microgram/inhalation.
To avoid confusion, Rilast Rapihaler is labelled as metered dose like Rilast Turbuhaler. Table 1 gives the corresponding dose delivered to the patient.
https://stagingapi.mims.com/au/public/v2/images/fulltablegif/RILRAP01.gif For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Inhalation, pressurised.

4 Clinical Particulars

4.9 Overdose

An overdose of formoterol may lead to effects that are typical for β₂-adrenergic agonists: tremor, headache, palpitations, and tachycardia. Monitoring of serum potassium concentrations may be warranted. Hypotension, metabolic acidosis, hypokalaemia, and hyperglycaemia may also occur. Supportive and symptomatic treatment may be indicated. β-blockers should be used with care because of the possibility of inducing bronchospasm in sensitive individuals. A metered dose of 120 microgram administered during 3 hours in patients with acute bronchial obstruction raised no safety concerns.
Acute overdosage with budesonide, even in excessive doses, is not expected to be a clinical problem. However, the plasma cortisol level will decrease and number and percentage of circulating neutrophils will increase. The number and percentage of lymphocytes and eosinophils will decrease concurrently. When used chronically in excessive doses, systemic glucocorticosteroid effects, such as hypercorticism and adrenal suppression, may appear.
Withdrawing Rilast Rapihaler or decreasing the dose of budesonide will abolish these effects, although the normalisation of the HPA-axis may be a slow process.
For information on the management of overdose, contact the Poison Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Individually, budesonide and formoterol were not genotoxic in a series of assays for gene mutations (except for a slight increase in reverse mutation frequency in Salmonella typhimurium at high concentrations of formoterol), chromosomal damage and DNA repair. The combination of budesonide and formoterol has not been tested in genotoxicity assays.
Carcinogenicity. The carcinogenic potential of the budesonide/formoterol combination has not been investigated in animal studies.
In formoterol carcinogenicity studies performed by AstraZeneca, there was a dose dependent increase in the incidence of uterine leiomyomas in mice dosed orally at 0.1, 0.5, and 2.5 mg/kg/day for 2 years, and a mesovarian leiomyoma was observed in a female rat dosed by inhalation at 0.13 mg/kg/day for 2 years. The effects observed are expected findings with high-dose exposure to β₂-agonists.
Formoterol carcinogenicity studies performed by other companies used systemic exposure levels 800 to 4800-fold higher than those expected upon clinical use of formoterol (based on an 18 microgram daily dose).
Some carcinogenicity activity was observed in rats and mice. However, in view of the dose levels at which these effects were observed and the fact that formoterol is not mutagenic (except for very weak activity at high concentrations in one test system), it is concluded that the cancer risk in patients treated with formoterol fumarate is no greater than for other β₂-adrenoceptor agonists.
The carcinogenic potential of budesonide has been evaluated in the mouse and rat at oral doses up to 200 and 50 microgram/kg/day respectively. In male rats dosed with 10, 25, and 50 microgram budesonide/kg/day, those receiving 25 and 50 microgram/kg/day showed an increased incidence of primary hepatocellular tumours. In a repeat study, this effect was observed in a number of steroid groups (budesonide, prednisolone, triamcinolone acetonide), thus indicating a class effect of corticosteroids.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Chemical structure. Budesonide.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSBUDESO.gif Chemical name: 16α, 17α-22 R, S-propylmethylenedioxypregna-1, 4-diene-1β, 21-diol-3, 20-dione.
Formoterol fumarate dihydrate.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSFORFUD.gif Chemical name: (R*R*)-(±)-N-[2-hydroxy-5-[1-hydroxy-2-[[2-(4-methoxyphenyl)-1-methylethyl]amino]ethyl]phenyl]formamide, (E)-2-butendioate(2:1), dihydrate.
CAS number. Budesonide. 51333-22-3.
Formoterol fumarate dihydrate. 183814-30-4.

7 Medicine Schedule (Poisons Standard)

Prescription only medicine (Schedule 4).

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/RILRAPST.gif