CICLESONIDE: THE ANTI-DIVA BREATHER
BONUS: REMEMBER TO TAKE IT TWICE A DAY, MORNING AND EVENING.
Generic Name: ciclesonide
ORAL INHALATION CORTICOSTEROID:
INTRANASAL INHALATION CORTICOSTEROID:
1-
- Generic Name: ciclesonide
- Trade or Brand Name: Omnaris
2-
- Generic Name: ciclesonide
- Trade or Brand Name: Zetonna
Chemical Name and Structure
- A non-halogenated glucocorticoid having the chemical name pregna-1,4-diene-3,20-dione, 16,17-[[(R)-cyclohexylmethylene]bis(oxy)]-11-hydroxy-21(2-methyl-1-oxopropoxy)-,(11β,16α). The empirical formula is C32H44O7 and its molecular weight is 540.7.
- Ciclesonide is a white to yellow-white powder.
- It is soluble in dehydrated:
- alcohol
- acetone
- dichloromethane
- Chloroform
ALVESCO 80 mcg, Solution, Inhalation Aerosol/Actuation
- MDI oral inhalation only.
- Pressurised inhalation solution from plastic actuator
- Clear and colourless
ALVESCO 160 mcg, Solution, Inhalation Aerosol/Actuation
- MDI oral inhalation only.
- Pressurised inhalation solution from plastic actuator
- Clear and colourless
Omnaris 50 mcg Nasal Spray, Suspension
- Water-based formulation: Hypotonic suspension
- Nasal Spray for seasonal allergies
- perennial allergic rhinitis:
- Children: ≥ 6 years
- Adolescent andAdult : ≥ 12 years
- Clear and colourless
Zetonna 37 mcg /Actuation Metered-Dose Nasal Aerosol
- Deliver a pressurized ciclesonide from the actuator
- Zetonna is supplied in a 6.1g canister containing 60 doses
- Delivered in fine aerosol mist
- Nasal Spray for seasonal allergies
- perennial allergic rhinitis
- Adults and Adolescents 12 Years of Age only
- Clear and colourless
CLASSIFICATION
USE
- Ciclesonide is a man-made glucocorticoid used to treat and prevent difficulty breathing, chest tightness, wheezing, and coughing caused by asthma and allergic rhinitis
- It works by decreasing swelling and irritation in the airways to allow for easier breathing
- Maintenance treatment of asthma as prophylactic therapy in:
1- children patients 6 years old or older
2- adult and adolescent patients 12 years of age and older.
- NOT indicated for the relief of acute bronchospasm
- NOT a rescue inhaler and should not be used for relief of sudden symptoms of shortness of breath during an asthma attack
ROUTES/DOSAGES
*Prime with three (3) sprays on initial use
A- FOR ORAL INHALATION ONLY: ALVESCO 80 mcg and 160 mcg Inhalation Aerosol
Patients ≥ 12 years who received bronchodilators alone
1- Recommended Starting Dose
80 mcg twice daily
2- Recommended Highest Dose
160 mcg twice daily
Patients ≥ 12 years who received inhaled corticosteroids
1- Recommended Starting Dose
80 mcg twice daily
2- Recommended Highest Dose
320 mcg twice daily
Patients ≥ 12 years who received oral corticosteroids(such as PREDNISONE)
1- Recommended Starting Dose
320 mcg twice daily
2- Recommended Highest Dose
320 mcg twice daily
B- For NASAL SPRAY ONLY: Omnaris 50 mcg Nasal Spray
Patient Children: ≥ 6 years
Adolescent and Adult ≥ 12 years
1- Recommended Starting Dose
2 sprays per nostril once daily (200 mcg/day).
2- Recommended Highest Dose
Should not exceed 2 sprays in each nostril (200 mcg/day).
C- FOR NASAL AEROSOL METERED-DOSE: Zetonna 37 mcg/Actuation Metered-Dose Nasal Aerosol
Adolescent and Adult ≥ 12 years
1- Recommended Starting Dose
1 actuation per nostril once daily (37 mcg per actuation)
2- Recommended Highest Dose
1 actuation in each nostril daily (37 mcg per actuation)
WARNING SIGNS
Prednisone should be reduced gradually, no faster than 2.5 mg/day on a weekly basis, beginning after at least 1 week of therapy with ALVESCO. Patients should be carefully monitored for signs of asthma instability including:
- monitoring of serial objective measures of airflow (PEAK FLOW RATE MEASUREMENT)
- signs of adrenal insufficiency during steroid taper and following discontinuation of oral corticosteroid therapy.
Withdrawal symptoms
Ciclesonide deposition in the lung
The particle inhaled are very small (≤5µm), which penetrate rapidly and deeper in small airways (<2mm diameter), and reduce inflammation at these important sites.
Ciclesonide Graph of total regional distribution in the lung
Distributed throughout the airways
Ciclesonide Comparare to other ICS
Offers a total lung deposition of 52%, of which 55% is distributed to the small airways where it can act against underlying asthma inflammation.
PHARMACOKINETICS
Onset: Within 24-48 hours
Peak Effect: 1-5 weeks
Duration: Unknow
Metabolism: ciclesonide is metabolized by esterases in nasal mucosa and lungs
Elimination:
- Half-life is 0.71hour (ciclesonide) and 6-7 (des-ciclesonide)
- Excreted principally in feces (66%) ciclesonide
- A lesser extent (≤20%) in urine as des-ciclesonide
- Occurs at 1.04 hours inhalation of ciclesonide
Ciclesonide is NOT INDICATED for the relief of acute bronchospasm
Status Asthmaticus
ciclesonide is contraindicated in the primary treatment of status asthmaticus or other acute episodes of asthma where intensive measures are required.
Hypersensitivity
ciclesonide is contraindicated in patients with known hypersensitivity any of the ingredients.
Hypersensitivity reactions with manifestations such as:
angioedema with
swelling of the lips and tongue and pharynx.(Known as Quincke's edema, is the rapid swelling of the dermis, subcutaneous tissue, mucosa and submucosal tissues. It is very similar to hives.)
Oral candida or thrush
Nasal candida or thrush
Gram stain of candida or thrush
- Gram Stain positive = it is called budding yeast present because can look like a single yeast cell
- Pseudohyphae = yeast cell that continues to get longer.
ADVERSE REACTION/SIDE EFFECTS
Adverse reaction:
Systemic and local corticosteroid use may result in the following:
Candida albicans infection
Immunosupression
Hypercorticism and adrenal suppression
Growth effects
Glaucoma and cataracts
Side effects:
cough, nasal congestion, bronchospasms, headache, back pain, change of voice and/or hoarseness (dysphonia) as a result of inhaled steroid.
DRUG INTERACTION
- Interactions of corticosteroids more likely to occur with systemic (rather than inhaled) corticosteroids
- Increased serum glucose levels
- Risk for hypokalemia when using potassium-depleting diuretics like hydrochlorothiazide and furosemide
REFERENCES
- Integrated Cardiopulmonary Pharmacology 4th edition by Colbert, Bruce and Gonzales, Luis III.
- www.sunovion.com (Sunovion Pharmaceuticals: online resources for every medication brand for healthcare professional