Ciclesonide

Ciclesonide is an inhaled medication from the group of non-halogenated glucocorticoids. Glucocorticoids - including ciclesonide - are anti-inflammatory drugs. Ciclesonide is used for the long-term treatment of asthma.

In the USA, ciclesonide has also been used as a nasal spray to treat "runny nose" (allergic rhinitis) since 2012. Ciclesonide is a prodrug, which means that the active ingredient is supplied to the body in an inactive form and is only converted into the active form in the body through conversion processes. Due to this property, ciclesonide has a certain selectivity for the lower respiratory tract, meaning that it only works there.

However, ciclesonide is not suitable for acute respiratory distress. Chemically (structurally), ciclesonide is very similar to budesonide. Ciclesonide is considered to be "better tolerated" than oral glucocorticoids due to its inhaled application. However, this fact should be viewed critically, as systemic side effects cannot be ruled out and there are not enough conclusive studies on this. One advantage is that ciclesonide usually only needs to be used once a day.

Ciclesonide has an anti-inflammatory effect, helps to prevent asthma attacks, alleviates allergic symptoms and suppresses the immune system's response (immunosuppressive). Ciclesonide must be taken regularly for the full effect to unfold. This usually only happens after a few weeks.

Ciclesonide is converted by the body into desciclesonide (active form) and then binds to the glucocorticoid receptors. Ciclesonide influences phospholipase A2 proteins and lipocortin, which controls inflammatory mediators. Inflammatory mediators are substances that control inflammatory processes in the body. The anti-inflammatory reactions are regulated both by the dilation of the smallest blood vessels (capillaries) and by the permeability of fluids through the vessel walls. Ciclesonide acts by limiting both properties. After binding to the glucocorticoid receptors, the complex consisting of receptor and desciclesonide migrates into the cell nucleus, where it increases or decreases the release of inflammatory mediators such as interleukin-2 (IL2).

Ciclesonide is supplied to the body as a prodrug, i.e. in an inactive form, as a drug for inhalation (aerosol) and is only converted into the active form desciclesonide in the lungs by certain enzymes (esterases). Due to the high fat solubility (lipophilicity) of ciclesonide, it accumulates in the lungs. This property keeps possible side effects to a minimum. The remaining quantities that enter the bloodstream are broken down in the liver by the cytochrome P450 enzymes (CYP 3A4 and 2D6) and excreted via the bile.

Always take Ciclesonide exactly as described in the package leaflet or as advised by your doctor.

The usual recommended dose in adults is 160 mcg (micrograms) per day and can be reduced to 80 mcg (micrograms) per day if the patient responds well. Ciclesonide is usually used as an inhaler (metered dose inhaler). If ciclesonide is used as an inhaler, care should be taken to use it correctly. With the metered dose inhaler, 3 test sprays should be carried out into the ambient air after a longer period of non-use or if it has been newly prescribed. First exhale, then place the inhaler in your mouth via the mouthpiece and use your finger to deliver the dose and slowly inhale through your mouth. The air should then be held for a few seconds and finally exhaled slowly through the nose. To reduce the risk of mouth fungus, the inhaler should be used before eating or the mouth should be rinsed with water after use.

The following side effects may occur when taking ciclesonide:

• difficult breathing with coughing, shortness of breath, wheezing, tightness in the chest or increasing rales.
• waking up at night because of the symptoms
• No relief of symptoms with an on-demand spray
• Severe allergic reactions such as swelling of the tongue, lips or throat
• Coughing or wheezing that worsens after inhalation

If the above side effects occur, the medication should be discontinued immediately and a doctor contacted.

Occasionally:

• Hoarseness
• Fungal infection in the mouth (oral thrush)
• Headache
• Dry mouth or throat
• Nausea and/or vomiting

Rarely:

• Abdominal pain
• High blood pressure

Frequency not known:

• Sleep disturbances
• Depression or anxiety
• Restlessness or nervousness
• Irritability or overexcitability

The following side effects may occur with prolonged use:

• Growth disorders in adolescents
• Reduced bone density
• Blurred vision (cataracts)
• Loss of vision (glaucoma)
• Cushing's syndrome

The effect and side effects of ciclesonide may be increased if the following active substances are taken at the same time:

• Ketoconazole
• itraconazole
• ritonavir
• nelfinavir

Ciclesonide should not be taken by:

• Patients with severe asthma, as an acute asthma attack may occur
• Patients who are already taking cortisone tablets.
• Patients with liver or kidney disease.
• Patients with hypersensitivity to ciclesonide

Ciclesonide can lead to positive test results in doping tests.

Ciclesonide should only be used with caution in patients with active or dormant pulmonary tuberculosis, mycoses, viral infections or bacterial infections.

Ciclesonide is not approved for children under 12 years of age as there is a lack of experience reports. Prolonged use in children over 12 years of age may result in reduced growth.

Height should be checked by a doctor at regular intervals.

It is not recommended to use ciclesonide during pregnancy or breastfeeding as there is insufficient information on the use of ciclesonide. Medical advice should be sought and the risk-benefit profile discussed.

If mothers have received corticosteroids during pregnancy, the child's adrenal function should be carefully monitored.