Budesonide: Effects, Applications, Side Effects

How budesonide works

As a glucocorticoid, the active ingredient budesonide has an anti-allergic, anti-inflammatory and suppressive effect on the immune system (immunosuppressive). It is related to the body’s own stress hormone cortisol, which is also colloquially called cortisone (but “cortisone” actually stands for the inactivated form of the hormone).

The active ingredient budesonide is designed to be inactivated as soon as it enters the bloodstream. This keeps budesonide side effects to a minimum.

However, this also means that the active ingredient cannot reach the site of action via the bloodstream. It must therefore always be applied locally, for example as a budesonide nasal spray/drops, as an inhalation, in the form of enteric-coated capsules or as granules or rectal foam (the latter acts locally in the intestine).

Once budesonide enters the bloodstream, it is metabolized in the liver to degradation products with low glucocorticoid activity. After three to four hours, about half of the active substance is excreted in the stool (“half-life”).

When is budesonide used?

The active ingredient budesonide is used for:

  • bronchial asthma
  • chronic obstructive pulmonary disease (COPD)
  • allergic rhinitis (e.g. hay fever)
  • eosinophilic esophagitis (chronic inflammatory disease of the esophagus)

The duration of use is usually several weeks, but may be shorter or longer in individual cases.

How budesonide is used

After inhalation, you should always eat or drink something to prevent budesonide side effects in the mouth and throat (e.g. fungal infections).

There are also combination preparations for asthma patients that contain budesonide and a long-acting beta-sympathomimetic (e.g. formoterol). This additionally relieves asthmatic symptoms by widening the bronchi and thus helping to improve gas exchange in the lungs (“reliever”).

In chronic inflammatory bowel diseases, budesonide is often used in the form of enteric-coated capsules or granules. Gastro-resistant because stomach acid would decompose budesonide.

Especially if the descending part of the colon is affected by the inflammation, a rectal foam or a rectal suspension with budesonide is also suitable. This is usually applied once a day for a few weeks.

What are the side effects of budesonide?

Budesonide side effects depend partly on the way it is used.

With inhalation and nasal sprays, side effects such as fungal infections in the mouth/throat, hoarseness, cough, nosebleeds, and irritation of the mucous membranes of the throat and mouth occur frequently (i.e., in one in ten to one in one hundred people treated).

The side effects of the melting tablets correspond mainly to those of inhalation. In some cases, side effects also occur that are typical of budesonide dosage forms for use in the intestine.

What should be considered when taking budesonide?

If indicated, there are no contraindications. Caution is advised in case of hypersensitivity to the active ingredient or any of the other ingredients of the respective preparation.

Interactions

These include, for example, the antifungal agents ketoconazole and itraconazole, the immune inhibitor ciclosporin (for autoimmune diseases and after transplantation), ethinylestradiol and other estrogens (female sex hormones), and the antibiotic rifampicin. If the doctor is aware of the intake of such drugs, he can adjust the dosage of budesonide accordingly.

Age restriction

Medicinal products on the market containing budesonide are approved for children aged 6 years and older (nasal spray and inhalers) and adults aged 18 years and older (for inflammatory bowel disease and eosinophilic esophagitis).

The solution for nebulization is approved from the age of 6 months.

Pregnancy and lactation

Budesonide can also be used during breastfeeding. There are no reports of side effects in the breastfed infant.

How to obtain medicines containing budesonide

Any medicine containing the active ingredient budesonide requires a prescription in Germany, Austria, and Switzerland.

Not all dosage forms from Germany are also available in Austria or Switzerland. This applies in particular to rectal foams and nasal sprays containing budesonide.

Since when is budesonide known?

This also opened up the possibility of modifying the structure of the active ingredient in order to change and improve its properties. In the case of the active ingredient budesonide, a “predetermined breaking point” was deliberately added, which gives way as soon as the active ingredient leaves the site of action.