Usage
Ciclesonide is prescribed for the prophylactic management of steroid-responsive bronchial asthma in adults and children 6 years of age and older. It is also used to treat symptoms of seasonal and perennial allergic rhinitis (hay fever) in adults and adolescents 12 years of age and older. It is classified as an inhaled corticosteroid (ICS). Ciclesonide acts by reducing inflammation in the airways, thereby preventing asthma attacks and alleviating allergy symptoms.
Alternate Names
Ciclesonide is also known as des-isobutyryl-ciclesonide (its active metabolite). Brand names include Alvesco and Omnaris.
How It Works
Pharmacodynamics: Ciclesonide is a prodrug that is converted to its active metabolite, des-isobutyryl-ciclesonide (des-ciclesonide), in the lungs. Des-ciclesonide binds to glucocorticoid receptors in the airways, leading to decreased inflammation. This includes reduced production and release of inflammatory mediators, decreased vascular permeability, and inhibition of inflammatory cell migration.
Pharmacokinetics: Following inhalation, ciclesonide is extensively metabolized in the lungs to des-ciclesonide. Systemic absorption is low, minimizing systemic side effects. Des-ciclesonide is further metabolized in the liver and eliminated primarily via hepatic excretion. The elimination half-life of des-ciclesonide is approximately 12 hours.
Dosage
Standard Dosage
Adults:
- Asthma: Initial dose is 80 mcg twice daily via oral inhalation, which may be increased to a maximum of 160 mcg twice daily. In some cases, especially for those transferring from oral corticosteroids, higher doses (up to 320 mcg twice daily) may be necessary.
- Allergic Rhinitis: One spray (37 mcg) in each nostril once daily is the recommended dose. The maximum dose should not exceed 74 mcg/day.
Children:
- Asthma (6-11 years): 80-160 mcg once daily via oral inhalation, preferably in the evening, though morning dosing is also effective. It can also be given as 80 mcg twice daily. Using a spacer is recommended.
- Allergic Rhinitis (12 years and older): Same as adult dosing.
Special Cases:
- Elderly Patients: Dose adjustment is generally not necessary.
- Patients with Renal Impairment: Dose adjustment is generally not necessary.
- Patients with Hepatic Dysfunction: Dose adjustment is not usually needed, although systemic exposure to the active metabolite may be increased.
- Patients with Comorbid Conditions: Close monitoring is recommended, especially in patients with diabetes, osteoporosis, or ocular herpes simplex.
Side Effects
Common Side Effects:
Headache, nasopharyngitis, sinusitis, pharyngolaryngeal pain, upper respiratory tract infection, arthralgia, nasal congestion, back pain, epistaxis (nosebleed). Candidiasis of the oropharynx can occur. Patients should rinse their mouth after inhalation to reduce this risk. Hoarseness, cough, and dry mouth are other potential side effects.
Rare but Serious Side Effects:
Bronchospasm (wheezing, chest tightness), allergic reactions (angioedema, rash, hives), adrenal suppression, worsening asthma symptoms. Growth retardation in children is possible with prolonged use. Vision changes such as blurred vision have also been rarely reported.
Long-Term Effects:
With prolonged use, there is a potential for decreased bone mineral density (osteoporosis), cataracts, glaucoma, and growth suppression in children. Regular monitoring is necessary. Immunosuppression may also occur with long-term high doses.
Contraindications
- Hypersensitivity to ciclesonide.
- Primary treatment of status asthmaticus or other acute episodes of asthma requiring intensive measures.
- Untreated active or latent tuberculosis, fungal, bacterial, or systemic viral infections.
Drug Interactions
- Ketoconazole: Increases ciclesonide levels.
- Strong CYP3A4 inhibitors (e.g., itraconazole, ritonavir): Can significantly increase ciclesonide levels and risk of adverse effects.
- CYP3A4 inducers (e.g., rifampin, phenytoin): May decrease ciclesonide efficacy.
Pregnancy and Breastfeeding
- Pregnancy: Ciclesonide is Pregnancy Category C. Use only if the benefit outweighs the risk to the fetus. Animal studies have shown potential adverse effects, though human studies are limited.
- Breastfeeding: It is unknown if ciclesonide passes into breast milk. Caution is advised.
Drug Profile Summary
- Mechanism of Action: Reduces airway inflammation through binding to glucocorticoid receptors.
- Side Effects: Common: Headache, nasopharyngitis, sinusitis. Serious: Bronchospasm, adrenal suppression.
- Contraindications: Hypersensitivity, acute asthma attacks, untreated infections.
- Drug Interactions: Ketoconazole, strong CYP3A4 inhibitors/inducers.
- Pregnancy & Breastfeeding: Use with caution; potential fetal risk.
- Dosage: Adults: 80-160 mcg twice daily (inhalation); Children (6-11 years): 80-160 mcg daily.
- Monitoring Parameters: Lung function tests (FEV1, peak flow), growth in children, signs of adrenal suppression, oral candidiasis.
Popular Combinations
Ciclesonide is often used in combination with long-acting beta-agonists (LABAs) such as formoterol or salmeterol for enhanced asthma control.
Precautions
- Monitor for oropharyngeal candidiasis, adrenal suppression, and changes in growth in children.
- Ensure proper inhaler technique.
- Avoid abrupt discontinuation, especially in patients on systemic corticosteroids.
- Caution in patients with osteoporosis, diabetes, glaucoma, and active infections.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ciclesonide?
A: Adults and adolescents 12 years and older: 80 mcg inhaled twice daily initially, which may be increased to 160 mcg twice daily for asthma. For allergic rhinitis, one spray (37 mcg) in each nostril once daily. Children 6-11 years of age: 80-160 mcg inhaled once daily for asthma.
Q2: What are the common side effects of Ciclesonide?
A: Common side effects include headache, nasopharyngitis, sinusitis, sore throat, and upper respiratory infection.
Q3: How does Ciclesonide work?
A: Ciclesonide is converted to its active form, des-ciclesonide, in the lungs. This active form reduces airway inflammation by binding to glucocorticoid receptors.
Q4: Is Ciclesonide safe during pregnancy?
A: Ciclesonide is Pregnancy Category C. Its use during pregnancy should be considered only if the benefits outweigh the potential risks to the fetus.
Q5: Can Ciclesonide interact with other medications?
A: Yes, Ciclesonide can interact with medications like ketoconazole, strong CYP3A4 inhibitors and inducers. Always inform your physician about all other medications you are taking.
Q6: What should patients do after inhaling Ciclesonide?
A: Patients should rinse their mouth with water and spit it out without swallowing to help reduce the risk of oral thrush (candidiasis).
Q7: Can Ciclesonide be used to treat acute asthma attacks?
A: No, Ciclesonide is not indicated for the relief of acute bronchospasm. It is a maintenance medication for prophylactic treatment of asthma.
Q8: What are the long-term side effects of Ciclesonide?
A: Potential long-term side effects, particularly with high doses, include decreased bone mineral density, cataracts, glaucoma, and growth suppression in children.
A: Contact your doctor if you experience worsening asthma symptoms, signs of an allergic reaction (rash, swelling), or any other unusual or severe side effects.
