ciclesonide inhaled

Action and Spectrum

Ciclesonide is categorized under glucocorticoids and thus has functions such as reduction of leukocyte migration, inhibition of mediator release and immunosuppressive actions. They work via phospholipase A2 inhibitory proteins (lipocortins), which control the production of: other prostaglandins and leukotrienes. 

Drug Interaction

Adverse Reaction

Adverse drug reactions 

Frequency Defined  

>10%  

Nasopharyngitis  

Headache   

1-10%  

Ear pain  

Urticaria   

Oral Candidiasis  

Facial edema  

Back pain   

Upper respiratory infection  

Gastroenteritis  

Extremity pain  

Epistaxis  

Conjunctivitis

Black Box Warning

Contraindication / Caution

Contraindication/Caution 

Contraindication 

Hypersensitivity 

Caution 

Kaposi’s Sarcoma 

Impaired wound healing 

Candida infection 

Glaucoma 

Pregnancy / Lactation

Pregnancy/Lactation  

Pregnancy warnings:    No adequate evidence for a result in humans must take care of potential risks in pregnant women     

Pregnancy Category: C 

Lactation: Unknown if distributed into breast milk, avoid 

Pregnancy Categories:       

• Category A: Satisfactory and well-controlled studies show no risk to the fetus in the first or later trimester.       
• Category B: No evidence shown of risk to the fetus found in animal reproduction studies, and there are not enough studies on pregnant women       
• Category C: Adverse effects on the fetus found with evidence in animal reproduction studies and no adequate evidence for a result in humans 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: There is no data available for the drug under this category. 

Pharmacology

Pharmacology 

It is a prodrug that is hydrolyzed by esterases in the human body to its active metabolite, C21-desisobutyryl-ciclesonide (des-ciclesonide or RM1) following intranasal administration. Des-ciclesonide possesses anti-inflammatory effect and binds to the glucocorticoid receptor with a potency 120 times more than that of ciclesonide. The precise way through which ciclesonide reduces symptoms of allergic rhinitis is not well understood. However, corticosteroids are multi-potent and their effects involve multiple cell types such as the mast cells, eosinophils, neutrophils, macrophages and lymphocytes and multiple mediators of the inflammatory response. 

Pharmacodynamics 

Ciclesonide is categorized under glucocorticoids and thus has functions such as reduction of leukocyte migration, inhibition of mediator release and immunosuppressive actions. They work via phospholipase A2 inhibitory proteins (lipocortins), which control the production of: other prostaglandins and leukotrienes. This is due to specific moderation of inflammatory response through reduction of capillary leakage and dilation and decline in adhesion of leukocytes and macrophage besides downward regulation of secretion of vasoactive compounds.  

Pharmacokinetics 

Absorption 

Bioavailability: 63% (active metabolite) 

Absorption: 52% 

Distribution: 

Protein Bound: 99% (intravenously) 

Volume of Distribution (Vd): 

Ciclesonide: 2.9 L/kg (following intravenous administration) 

Des-ciclesonide: 12.1 L/kg (following intravenous administration) 

Metabolism: 

It is metabolized to the active metabolite des-ciclesonide by esterases. Further metabolism occurs in the liver primarily via CYP3A4, and to a lesser extent by CYP2D6 

Elimination/Excretion 

Following IV administration: 

Half-life: 

• Ciclesonide: 0.71 hours 

• Des-ciclesonide: 6-7 hours 

Clearance: 

• Ciclesonide: 152 L/L/hr 

• Des-ciclesonide: 228 L/L/hr 

Excretion: 

• Feces: 66% 

• Urine: 20% 

Adminstartion

Administration 

It is administered intra-nasally in the form of nasal spray. Do not use more than 2 nasal sprays in each nostril. 

Patient Information Leaflet

Patient Information Leaflet  

Generic Name: ciclesonide inhaled 

Why do we use ciclesonide inhaled? 

ciclesonide inhaled is a corticosteroid which is used to treat Prophylaxis Asthma. It is also used to relieve inflammation and nasal congestion.