ciclesonide intranasal

Action and Spectrum

Actions and Spectrum:

The actions and spectrum of ciclesonide intranasal:

• Anti-inflammatory effects: ciclesonide reduces inflammation in the nasal tissues. It inhibits the release of inflammatory mediators such as cytokines and leukotrienes.
• Allergic rhinitis treatment: ciclesonide is used to treat the symptoms of allergic rhinitis, including nasal congestion, runny nose, sneezing, and itching.
• Preventative effects: ciclesonide can also be used as a preventative treatment to reduce the frequency and severity of allergic rhinitis symptoms.
• Safety and tolerability: ciclesonide is generally well-tolerated and has a good safety profile. It shows a low incidence of adverse effects.
• Once-daily dosing: ciclesonide is administered as a once-daily dose, making it a convenient and easy-to-use treatment option.
• ciclesonide has a fast onset of action, with some patients experiencing symptom relief within hours of the first dose.

Drug Interaction

Adverse Reaction

Frequency Defined

1-10%:

Headache (3.1-6.6%)

Nasopharyngitis (3.7%)

Epistaxis (2.9-6%)

Nasal discomfort (3.2%)

<1%:

Nasal congestion

Localized infections

Nasal ulcer

Dizziness

Black Box Warning

Contraindication / Caution

Contraindication/Caution:

• Hypersensitivity: ciclesonide intranasal is contraindicated in patients with a known hypersensitivity to ciclesonide or any of its ingredients.
• Active or latent tuberculosis: Patients with active or latent tuberculosis should be treated appropriately before starting ciclesonide intranasal.
• Viral infections: ciclesonide intranasal should be used with caution in patients with active or quiescent respiratory tract viral infections.
• Ocular herpes simplex: ciclesonide intranasal should be used with caution in patients with a history of ocular herpes simplex.
• Immunosuppression: ciclesonide intranasal may suppress the immune system, so caution should be exercised in patients with immunosuppression or receiving immunosuppressive therapy.
• Pediatric use: ciclesonide intranasal has not been studied extensively in pediatric patients under the age of 6 years, so caution should be exercised in this population.
• Pregnancy and breastfeeding: The safety of ciclesonide intranasal during pregnancy and breastfeeding has not been established, so caution should be exercised in these populations.

Pregnancy / Lactation

Pregnancy consideration:

Category C

Breastfeeding warnings:

It is unknown whether the drug is excreted in breast milk.

Pregnancy category:

• Category A: well-controlled and satisfactory studies do not show risk to the fetus in the first/later trimester.      
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women.
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
• Category D: adequate data available with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
• Category N: No data is available for the drug under this category.

Pharmacology

Pharmacology:

• Mechanism of action: ciclesonide is a prodrug activated by esterases in the nasal mucosa to form its active metabolite, desisobutyryl-ciclesonide. This active metabolite binds to and activates glucocorticoid receptors, leading to a reduction in inflammation and the inhibition of the production of various pro-inflammatory mediators.
• Anti-inflammatory activity: ciclesonide acts as a potent anti-inflammatory agent by reducing the production of pro-inflammatory cytokines, chemokines, and adhesion molecules. This results in a decrease in the infiltration of inflammatory cells, such as eosinophils and mast cells, into the nasal tissues.
• Onset and duration of action: ciclesonide has a fast onset of action, with some patients experiencing relief of nasal symptoms within hours of the first dose. ciclesonide’s therapeutic effect can last up to 24 hours, allowing for once-daily dosing.
• Metabolism and excretion: ciclesonide is metabolized in the liver to form its active metabolite, desisobutyryl-ciclesonide, which is then eliminated primarily through the kidneys.
• Drug interactions: ciclesonide is a substrate of the enzyme CYP3A4 and may interact with other medications that inhibit or induce this enzyme, such as ketoconazole and rifampin.

Pharmacodynamics:

Pharmacodynamic properties of ciclesonide:

• Anti-inflammatory effects: ciclesonide has potent anti-inflammatory effects, particularly in the respiratory system. It works by inhibiting the production of pro-inflammatory mediators, such as cytokines and chemokines, and reducing the infiltration of inflammatory cells into the airways.
• Glucocorticoid activity: ciclesonide is a glucocorticoid, which binds to and activates glucocorticoid receptors in cells throughout the body. This results in various physiological effects, including anti-inflammatory, anti-allergic, and immunosuppressive actions.
• Reduction of airway hyperresponsiveness: ciclesonide has been shown to reduce airway hyperresponsiveness in patients with asthma, which is a hallmark feature of the disease. This effect is likely due to the medication’s anti-inflammatory and immunosuppressive properties.
• Decreased mucus production: ciclesonide can also reduce the production of mucus in the airways, which is often a significant contributor to respiratory symptoms in patients with asthma and allergic rhinitis.
• Prevention of allergic reactions: By reducing inflammation and inhibiting the release of pro-inflammatory mediators, ciclesonide can help to prevent and alleviate allergic reactions in patients with asthma and allergic rhinitis.

Pharmacokinetics:

The pharmacokinetics of ciclesonide intranasal are as follows:

Absorption

The bioavailability of ciclesonide intranasal is negligible

Distribution

Protein-bound is more than 99%

The volume of distribution of 2.9 L/kg for the parent compound and 12.1 L/kg for the active metabolites

Metabolism

ciclesonide is metabolized hepatically into their active metabolites

Elimination

Excretion-

The drug is excreted in 66% of feces and 20% of urine

Adminstartion

Administration:

It is recommended to gently shake and prime a nasal spray before using it for the first time or after it has not been used for a certain period. It helps to ensure that the medication is mixed correctly and that the spray nozzle is clear of any blockages or debris.

Patient Information Leaflet

Patient information leaflet

Generic Name: ciclesonide

Pronounced: sik-le-SON-ide

Why do we use ciclesonide intranasal?

ciclesonide intranasal is a medication used to treat a variety of nasal symptoms like:

• Allergic rhinitis: ciclesonide intranasal is used to treat the symptoms of allergic rhinitis, including nasal congestion, sneezing, itching, and runny nose. It works by reducing inflammation in the nasal tissues, which can help to alleviate these symptoms.
• Other nasal symptoms: In addition to allergic rhinitis, ciclesonide intranasal may be used to treat other nasal symptoms, such as non-allergic rhinitis or sinusitis.
• Preventative treatment: ciclesonide intranasal can also be used as a preventative treatment for allergic rhinitis, helping to reduce the frequency and severity of symptoms.
• Fast-acting relief: ciclesonide intranasal has a fast onset of action, with some patients experiencing relief of symptoms within hours of the first dose.
• Once-daily dosing: ciclesonide intranasal is administered as a once-daily dose, making it a convenient and easy-to-use treatment option.