Ciclex50 mcg/spray

Ciclex is an inhaled corticosteroid (prodrug) used for long-term maintenance and prophylactic treatment of two separate conditions, depending on the formulation used:

• Oral inhalation (metered-dose inhaler): Maintenance treatment of asthma as prophylactic (preventive) therapy in adults and pediatric patients 12 years of age and older who require regular use of an inhaled corticosteroid.
• Nasal spray: Treatment of nasal symptoms (sneezing, itching, congestion, rhinorrhea) of seasonal allergic rhinitis in adults and children 6 years and older, and of perennial (year-round) allergic rhinitis in adults and adolescents 12 years and older.

Important: Ciclex is not indicated for the relief of acute bronchospasm or status asthmaticus. It is a controller medicine, not a rescue inhaler, and must be used together with a separate fast-acting (rescue) bronchodilator for sudden asthma symptoms.

Ciclex has also been studied off-label for other allergic and inflammatory airway conditions, but such uses are not established by regulatory labeling and should only be undertaken under direct physician guidance.

Each dose of Ciclesonide inhalation aerosol or nasal spray contains Ciclesonide as the active pharmaceutical ingredient, formulated as a hydrofluoroalkane (HFA)-propelled solution aerosol (for oral inhalation) or as an aqueous suspension (for nasal spray). Strengths available include 80 mcg and 160 mcg per actuation for the oral inhaler, and 50 mcg per spray for the nasal formulation. Refer to the specific product label for the exact strength and inactive ingredients of the dispensed product.

Ciclex is a synthetic, non-halogenated inhaled corticosteroid (ICS) that acts as a prodrug. After deposition in the lung or nasal mucosa, it is enzymatically hydrolyzed by esterases to its pharmacologically active metabolite, des-Ciclex, which has potent local anti-inflammatory activity. Because activation occurs mainly at the site of delivery, Ciclex is designed to reduce oropharyngeal deposition of active drug and associated local side effects compared with some older inhaled steroids. It is available as a pressurized metered-dose inhaler for asthma and as an aqueous nasal spray for allergic rhinitis.

Ciclex belongs to the pharmacological class of inhaled corticosteroids (glucocorticoids), used as anti-inflammatory agents for chronic airway and nasal allergic disease. It is classified therapeutically as an anti-asthmatic / anti-allergic agent for local (topical) respiratory use.

Mechanism of Action

Ciclesonide is a prodrug that, upon deposition in lung or nasal tissue, is converted by esterase enzymes into its active metabolite, des-ciclesonide. Des-ciclesonide binds with high affinity to the glucocorticoid receptor (approximately 120 times greater affinity than the parent compound), suppressing multiple inflammatory cell types (mast cells, eosinophils, lymphocytes) and mediators involved in the allergic and asthmatic inflammatory cascade, thereby reducing airway/nasal mucosal inflammation, hyperresponsiveness, and symptoms.

Pharmacokinetics

• Absorption: Oral bioavailability of ciclesonide itself is negligible (<1%); absolute bioavailability of the parent drug is about 22%, with roughly 63% relative systemic exposure to des-ciclesonide after inhalation.
• Protein binding: Ciclesonide and des-ciclesonide are highly protein bound (≥99%).
• Metabolism: Hydrolyzed by esterases to des-ciclesonide; further metabolized primarily via CYP3A4 (and to a lesser extent CYP2D6).
• Elimination half-life: Approximately 0.7 hours for ciclesonide and 6-7 hours for des-ciclesonide.
• Excretion: Predominantly via bile/feces (~66%), with a smaller renal component (≤20%).

How to Use Ciclex

• Inhaler: For oral inhalation only. Shake gently and prime with 3 test sprays before first use or if not used for 10 days or longer. Exhale fully, place the mouthpiece in the mouth, inhale slowly and deeply while actuating, then hold the breath briefly. Rinse the mouth with water (without swallowing) after each use to reduce the risk of oral thrush.
• Nasal spray: Gently shake and prime before first use (or after 4 or more days without use) until a fine mist appears. Blow the nose gently, tilt the head slightly forward, insert the nozzle into one nostril pointing away from the nasal septum, and spray while breathing in gently. Repeat in the other nostril. Avoid spraying directly onto the nasal septum. Discard the nasal spray bottle after the labeled number of actuations or 4 months after opening, whichever comes first.

Do not swallow Ciclex and do not use it more often or in higher doses than prescribed. Ciclex must always be used together with a separate fast-acting rescue inhaler for sudden breathing difficulty; it does not relieve acute symptoms itself.

Ciclex (via its active metabolite, des-Ciclex) is metabolized mainly by the CYP3A4 enzyme system. Clinically significant interactions are limited but include:

• Strong CYP3A4 inhibitors (e.g., ketoconazole, ritonavir, itraconazole): Co-administration with Ciclex can substantially increase systemic exposure to des-Ciclex (approximately 3.6-fold with ketoconazole), raising the risk of systemic corticosteroid effects (e.g., adrenal suppression, Cushingoid features). Concurrent use should be avoided when possible, or the patient monitored closely.
• Other inhaled bronchodilators (e.g., albuterol, formoterol): No clinically significant pharmacokinetic interaction with Ciclex has been observed with concurrent use.

Inform the prescribing physician of all other medicines, including antifungals, protease inhibitors, and other corticosteroids, before starting Ciclex.

Common Side Effects

• Headache
• Nasopharyngitis (common cold-like symptoms)
• Sinusitis
• Pharyngolaryngeal pain / sore throat
• Upper respiratory tract infection
• Nasal congestion
• Epistaxis (nosebleed, more common with nasal spray)
• Back pain, joint pain (arthralgia)

Less Common but Important Side Effects

• Oral or nasal candidiasis (thrush) with Ciclex use - reduced risk compared with some other inhaled corticosteroids due to the prodrug design, but still possible; rinse the mouth after inhaler use as a precaution.
• Hypersensitivity reactions, including rash, urticaria, and rarely angioedema (swelling of lips, tongue, or throat) - seek urgent care if these occur.
• Nasal septal effects (rare nasal ulceration or perforation with nasal spray).

Systemic corticosteroid-related effects (adrenal suppression, reduced growth velocity in children, decreased bone mineral density, glaucoma/cataracts) are discussed under Precautions and Warnings, as they relate mainly to long-term or high-dose use of Ciclex rather than typical short-term adverse events.

Pregnancy

There are no adequate and well-controlled studies of Ciclex in pregnant women. As with other inhaled corticosteroids, Ciclex should be used during pregnancy only if the potential benefit to the mother (i.e., maintaining adequate control of asthma or allergic rhinitis) justifies the potential risk to the fetus. Uncontrolled asthma during pregnancy carries its own risks to mother and fetus, so Ciclex therapy should not be stopped without medical advice. Always consult a physician before using Ciclex during pregnancy.

Lactation

It is not known whether Ciclex or its active metabolite passes into human breast milk in clinically significant amounts. Because many corticosteroids are excreted in breast milk to some degree, caution is advised, and Ciclex should be used during breastfeeding only if clearly needed and under medical supervision, weighing the benefits of treatment against any possible risk to the nursing infant.

• Not a rescue medicine: Ciclex does not relieve acute bronchospasm; patients must have a separate fast-acting bronchodilator available for acute symptoms (see Contraindications).
• Local infections: Ciclex may cause oral or nasal candidiasis; rinse the mouth after inhaler use. Report persistent white patches, soreness, or nasal irritation to a physician.
• Adrenal suppression: Systemic corticosteroid effects, including hypothalamic-pituitary-adrenal (HPA) axis suppression, may occur with Ciclex, particularly at higher doses or with prolonged use. Use the lowest effective dose. Patients transferring from chronic systemic (oral) corticosteroids to Ciclex should do so gradually under medical supervision, as abrupt withdrawal of systemic steroids can be dangerous, and some patients may show signs of adrenal insufficiency during transition.
• Growth effects in children: Inhaled corticosteroids, including Ciclex, may cause a reduction in growth velocity in pediatric patients; growth should be monitored routinely, and the lowest effective dose used.
• Increased susceptibility to infections: Use Ciclex with caution in patients with active or quiescent untreated respiratory infections, including tuberculosis, and fungal, bacterial, viral, or parasitic infections, or ocular herpes simplex. Patients on immunosuppressive doses should avoid exposure to chickenpox or measles and seek medical advice promptly if exposed.
• Bone and eye effects: Long-term use of Ciclex has been associated with decreased bone mineral density and, rarely, glaucoma, increased intraocular pressure, or cataracts; patients with a history of these conditions should be monitored.
• Paradoxical bronchospasm: Rarely, wheezing may worsen immediately after a dose of Ciclex; if this occurs, discontinue and treat with a fast-acting bronchodilator, then seek medical advice.
• Hypersensitivity: Discontinue Ciclex immediately if signs of an allergic reaction occur (see Side Effects).

Acute overdose with Ciclex is unlikely to cause immediate danger given its topical mode of delivery and low oral bioavailability, but chronic overdosage or use of excessive doses of Ciclex over a prolonged period may lead to systemic corticosteroid effects (hypercorticism/Cushingoid features), including adrenal suppression. There is no specific antidote. If an overdose is suspected, or if a child has accidentally ingested or inhaled a large amount of Ciclex, seek immediate medical attention or contact a poison control center/emergency services rather than attempting home treatment. Long-term use of Ciclex at doses higher than prescribed should be avoided; adrenal function may need to be monitored after excessive or prolonged use.

Store Ciclex at room temperature (below 30°C), away from direct light, heat, and moisture. Do not freeze the nasal spray. Do not puncture, break, or incinerate the inhaler canister, and avoid exposure to temperatures above 49°C (120°F). Keep the cap on when not in use and discard nasal spray bottles after the labeled number of actuations or per the expiry indicated on the label. Keep out of reach and sight of children.

Pediatric Use

Safety and efficacy of the Ciclex oral inhaler have been established for asthma maintenance therapy in patients 12 years and older; it has not been established in children below 12 years of age. The Ciclex nasal spray is approved from 6 years of age for seasonal allergic rhinitis and from 12 years for perennial allergic rhinitis; safety and efficacy in younger children have not been established. Growth velocity should be monitored periodically in pediatric patients on long-term Ciclex therapy.

Geriatric Use

Clinical studies of Ciclex did not include sufficient numbers of patients aged 65 years and older to determine whether they respond differently from younger adults. Dose selection for an elderly patient should generally start at the lower end of the dosing range, reflecting the greater frequency of comorbidities and concomitant medication use in this population.

Renal and Hepatic Impairment

Specific dose adjustments for Ciclex have not been established for renal or hepatic impairment; because systemic exposure is low, clinically important effects are not expected, but Ciclex should be used with caution and under medical supervision in patients with significant hepatic impairment, given the drug's hepatic metabolism.

Ciclex is intended for regular, ongoing (maintenance) use rather than short-term or as-needed treatment. For asthma, Ciclex should be used daily even when symptoms are absent, as it works to prevent inflammation and flare-ups over time; noticeable improvement may take up to 4 weeks. For allergic rhinitis, Ciclex is typically used throughout the relevant allergy season or as long as year-round symptoms persist. The duration of Ciclex treatment should be determined by the prescribing physician based on symptom control, and therapy should not be stopped or the dose changed without medical advice, especially in patients who have been on higher doses for a prolonged period.

Inhaled Corticosteroid (Glucocorticoid); Anti-asthmatic and Anti-allergic (Nasal) agent.

Ciclesonide is a prodrug that undergoes activation by esterase enzymes in lung and nasal tissue to form its active metabolite, des-ciclesonide. Des-ciclesonide binds to the glucocorticoid receptor with high affinity, suppressing the transcription of pro-inflammatory genes and inflammatory cell activity (eosinophils, mast cells, lymphocytes, cytokines) in the airway or nasal mucosa. This reduces mucosal inflammation, edema, and mucus secretion, thereby controlling asthma symptoms and allergic rhinitis symptoms with continued regular use of Ciclesonide.

Ciclex oral inhaler is approved for asthma maintenance therapy in patients 12 years of age and older; safety and efficacy have not been established for asthma in children under 12. The Ciclex nasal spray is approved for seasonal allergic rhinitis in children 6 years and older, and for perennial allergic rhinitis from 12 years of age; it has not been shown effective for perennial rhinitis in children younger than 12, and safety/efficacy of Ciclex below the approved ages have not been established. As with other inhaled corticosteroids, growth velocity should be monitored periodically in children on long-term Ciclex therapy, and the lowest dose that controls symptoms should be used.