Usage
Ciclesonide + Formoterol is prescribed for the long-term management of asthma and Chronic Obstructive Pulmonary Disease (COPD) in adults and children. It is a combination medication containing an inhaled corticosteroid (Ciclesonide) and a long-acting beta2-agonist (Formoterol). This combination belongs to the pharmacological class of respiratory stimulants, specifically, inhaled corticosteroids and bronchodilators. The mechanism of action involves reducing airway inflammation (Ciclesonide) and relaxing the airway muscles (Formoterol) to improve airflow.
Alternate Names
No alternate generic names were found in the provided sources. Brand names may vary depending on the region. One example found was Alvesco for Ciclesonide and Symbicort for the combination of Budesonide/Formoterol, which offers a similar action mechanism.
How It Works
Pharmacodynamics: Ciclesonide, a corticosteroid, exerts its anti-inflammatory effects by binding to glucocorticoid receptors in the airways. This binding activates anti-inflammatory pathways, reducing swelling, mucus production, and airway hyperresponsiveness. Formoterol, a long-acting beta2-agonist, relaxes bronchial smooth muscle by stimulating beta2-adrenergic receptors, leading to bronchodilation and increased airflow to the lungs.
Pharmacokinetics: Ciclesonide is a prodrug activated in the lungs to des-ciclesonide. It has low oral bioavailability due to extensive first-pass metabolism. Formoterol is rapidly absorbed after inhalation. Both drugs are metabolized, primarily in the liver (Ciclesonide) and by other processes such as glucuronidation (Formoterol), and are eliminated through various routes, including biliary excretion (Ciclesonide) and renal excretion (Formoterol).
Mode of Action: Ciclesonide’s mode of action involves reducing inflammation by inhibiting inflammatory cell migration and activation, blocking late-phase allergic reactions, and decreasing airway hyperresponsiveness. Formoterol, on the other hand, acts on beta2-adrenergic receptors in the airways, promoting bronchodilation by relaxing the smooth muscles and improving airflow. Specific receptor binding or enzyme inhibition details beyond what’s described above were not available within the given sources. Elimination pathways involve metabolism and excretion as mentioned above, but CYP enzyme specifics or hepatic/renal contributions’ details weren’t available in the provided texts.
Dosage
Standard Dosage
Adults:
The recommended starting dose and the highest recommended dose can vary based on previous therapies. For patients previously on bronchodilators alone, a starting dose of 80 mcg twice daily, up to a maximum of 160 mcg twice daily, is advised. Patients previously using inhaled corticosteroids can start at 80 mcg twice daily and go up to a maximum of 320 mcg twice daily.
Children:
Children aged 5 years and older can use 12 mcg (1 inhalation) every 12 hours using an aerolizer inhaler. The maximum dose is 24 mcg daily. For children between 6 and 16 years, 6 mcg or 12 mcg can be inhaled every 12 hours with a maximum dose of 24 mcg daily. Pediatric use should always be under strict medical supervision, as it can affect growth.
Special Cases:
- Elderly Patients: No specific dosing adjustments were mentioned in the sources for elderly patients, but caution should be exercised due to potential age-related physiological changes.
- Patients with Renal Impairment: Use with caution in patients with severe renal impairment.
- Patients with Hepatic Dysfunction: Dose adjustment might not be necessary in patients with liver impairment, but careful monitoring is recommended.
- Patients with Comorbid Conditions: Caution should be exercised in patients with cardiovascular disorders, diabetes, hypokalemia, glaucoma, osteoporosis, infections (like tuberculosis), seizure disorders, and adrenal insufficiency. Careful monitoring and potential dose modifications may be required.
Clinical Use Cases
The provided sources focused on asthma and COPD management and did not specify dosages for scenarios like intubation, surgical procedures, mechanical ventilation, ICU use, or emergency situations. The drug is not for the relief of acute bronchospasm or status asthmaticus, and therefore, isn’t suitable for acute episodes or emergencies.
Dosage Adjustments
Dosage adjustments should be patient-specific, considering factors like renal or hepatic dysfunction, metabolic disorders, genetic polymorphisms, and the presence of comorbid conditions. When reducing the dose, gradual adjustments (e.g., 25-50% reductions) are recommended to avoid destabilizing the condition. For specific adjustments, consultation with a pulmonologist or a respiratory specialist is crucial.
Side Effects
Common Side Effects:
Headache, nasopharyngitis, upper respiratory tract infection, sinusitis, throat pain, unpleasant taste in the mouth, dry mouth, burning or irritation in the mouth, runny or stuffy nose, sore throat, hoarse voice, mild itching or skin rash, joint pain, and back pain.
Rare but Serious Side Effects:
Severe allergic reactions (rash, itching, swelling, angioedema), chest pain, high blood pressure, rapid heartbeat, serious eye symptoms (sudden vision loss, blurred vision, eye pain or swelling), and severe heart problems (irregular heartbeats, shortness of breath, dizziness).
Long-Term Effects:
Chronic complications from prolonged use may include adrenal suppression, decreased bone mineral density (BMD), glaucoma, cataracts, and growth retardation in children.
Adverse Drug Reactions (ADR):
Clinically significant ADRs requiring urgent medical attention may include severe allergic reactions, cardiac arrhythmias, adrenal crisis, and worsening of glaucoma or cataracts.
Contraindications
Absolute contraindications include severe hypersensitivity to milk proteins or any component of the medicine and acute asthma attacks. Relative contraindications include active or untreated infections (e.g., tuberculosis, fungal, bacterial, or viral infections), cardiovascular disorders, convulsive disorders, thyrotoxicosis, diabetes mellitus, ketoacidosis, and hypokalemia.
Drug Interactions
Ciclesonide + Formoterol may interact with various medications, including antifungals (e.g., ketoconazole), beta-blockers (e.g., propranolol, metoprolol), diuretics (e.g., furosemide), bronchodilators (e.g., albuterol), steroids (e.g., prednisone), monoamine oxidase inhibitors (MAOIs), tricyclic antidepressants (TCAs), macrolide antibiotics (e.g., erythromycin), and some HIV medications. Concomitant use of adrenergic agents may potentiate sympathetic effects, while use with theophylline may increase the risk of hypokalemia and ECG changes. Consumption of grapefruit or grapefruit juice should be avoided, as it may interact with the medication.
Pregnancy and Breastfeeding
Ciclesonide is classified as Pregnancy Category C. Animal studies have shown adverse effects, but there are no adequate and well-controlled studies in pregnant women. Its use during pregnancy should be limited to situations where the potential benefit outweighs the risk. Formoterol’s effect on pregnancy is not well-established. While information on related medications suggests that inhaled formoterol may not pass into breast milk in significant amounts, it is essential to consult a doctor before using it during breastfeeding.
Drug Profile Summary
- Mechanism of Action: Ciclesonide: reduces airway inflammation; Formoterol: relaxes airway muscles.
- Side Effects: Common: headache, nasopharyngitis, upper respiratory tract infections; Serious: allergic reactions, cardiac effects, adrenal suppression.
- Contraindications: Hypersensitivity, acute asthma attacks, active infections.
- Drug Interactions: Antifungals, beta-blockers, diuretics, MAOIs, TCAs.
- Pregnancy & Breastfeeding: Consult a doctor; potential risks exist.
- Dosage: Adult: 80-320 mcg twice daily; Children: 12-24 mcg daily.
- Monitoring Parameters: Lung function tests, blood pressure, heart rate, potassium levels, growth in children, and symptoms.
Popular Combinations
Ciclesonide + Formoterol is itself a commonly used combination. Triple therapy, including tiotropium, may be considered for certain patients, particularly those with COPD.
Precautions
General precautions include pre-screening for allergies, metabolic disorders, organ dysfunction, and infections. Specific populations (pregnant women, breastfeeding mothers, children, elderly) require extra caution. Patients should be advised to avoid alcohol, smoking, and certain medications.
FAQs (Frequently Asked Questions)
A: The dosage varies based on individual patient characteristics and prior treatment. Adults typically start at 80 mcg twice daily and may increase to a maximum of 160-320 mcg twice daily, depending on previous therapy. Children 5 years or older may use 12 mcg twice daily, up to a maximum of 24 mcg daily.
A: Common side effects include headache, nasopharyngitis, upper respiratory infections, throat irritation, cough, and dry mouth.
A: It is important to consult with a healthcare professional regarding its use during pregnancy and breastfeeding, as potential risks exist.
A: No, it is not indicated for the relief of acute bronchospasm or status asthmaticus. A rescue inhaler should be used for acute episodes.
A: Formoterol provides rapid bronchodilation within minutes, whereas the anti-inflammatory effects of Ciclesonide may take several weeks for full effect.
Q6: Are there any drug interactions I should be aware of?
A: Yes, it can interact with various medications like antifungals, beta-blockers, and some HIV drugs. It’s crucial to inform your doctor about all concomitant medications.
Q7: Can this medication affect growth in children?
A: Yes, long-term use of inhaled corticosteroids, including Ciclesonide, may affect growth in children. Regular monitoring of growth is essential.
Q8: What should I do if I miss a dose?
A: Take the missed dose as soon as you remember unless it’s close to the next scheduled dose. Do not double the dose.
A: Potential long-term effects may include adrenal suppression, decreased bone mineral density, glaucoma, and cataracts. Regular monitoring is important.
A: The inhaler should be stored at room temperature, away from direct sunlight and moisture.
