Budesonide

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Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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The active ingredient budesonide is used to treat asthma, COPD, allergic rhinitis and inflammatory bowel disease. Budesonide orodispersible tablets for the treatment of a certain form of esophagitis have also recently become available. Budesonide is used locally and is rapidly broken down once it enters the bloodstream. Here you can read everything you need to know about the effects and use of budesonide, side effects and interactions.

This is how budesonide works

As a so-called glucocorticoid, the active ingredient budesonide has an antiallergic, anti-inflammatory and dampening effect on the immune system (immunosuppressive). It is related to the body's own stress hormone cortisol, which is also known colloquially as cortisone (but actually "cortisone" stands for the inactivated form of the hormone).

Budesonide acts - just like cortisol - at certain docking points in the cell and changes the metabolic processes there in order to cope with stressful situations. It also suppresses inflammatory processes. It also increases the production of glucose and the breakdown of fat in the liver, which provides the body with more energy.

The active ingredient budesonide is designed to be inactivated as soon as it enters the bloodstream. In this way, the budesonide side effects can be kept 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 used locally, for example as a budesonide nasal spray / drop, as inhalation, in the form of gastric juice-resistant capsules or as granules or rectal foam (the latter acts locally in the intestine).

Breakdown and excretion

As soon as budesonide enters the bloodstream, it is metabolized in the liver to breakdown products with low glucocorticoid effects.After three to four hours, about half of the active ingredient is excreted in the stool ("half-life").

When is budesonide used?

The active ingredient budesonide is used in:

  • bronchial asthma
  • chronic obstructive pulmonary disease (COPD)
  • allergic rhinitis (e.g. hay fever)
  • inflammatory bowel disease (Crohn's disease, ulcerative colitis)
  • eosinophilic esophagitis (chronic inflammatory disease of the esophagus)

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

This is how budesonide is used

In the case of diseases of the respiratory tract (asthma, COPD), a budesonide spray or powder inhaler for inhalation or a solution for nebulization is used once or twice a day. The full effect only occurs after more than a week of consistent use. Budesonide is therefore not suitable for the relief of acute asthmatic complaints, but as a drug for basic therapy ("controller").

After inhaling 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 products for asthma patients that contain budesonide and a long-acting beta-sympathomimetic (e.g. formoterol). This also alleviates asthmatic complaints by expanding the bronchi and thus helping to improve gas exchange in the lungs ("reliever").

Budesonide nasal spray for allergic rhinitis must be shaken before use in order to distribute the active ingredient evenly. By default, one puff is usually given into each nostril twice a day.

In chronic inflammatory bowel diseases, budesonide is often used in the form of enteric capsules or granules. Resistant to the stomach because the stomach acid would break down 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. It is usually used once a day for a few weeks.

Budesonide orodispersible tablets that dissolve quickly in the mouth are available for the treatment of eosinophilic esophagitis. Then you are not allowed to eat or drink anything for at least 30 minutes.

What are the side effects of budesonide?

Budesonide side effects depend in part on the type of application.

Inhalation and nasal sprays often lead to side effects such as fungal infections in the mouth and throat, hoarseness, cough, nosebleeds and irritation of the pharynx and oral mucosa (i.e. every tenth to one hundredth person treated).

Common side effects of dosage forms for use in the intestine are digestive disorders, muscle cramps, heart stumbling, nervousness, mood swings, visual disturbances, skin reactions, low potassium blood levels, water retention in the tissue (edema) and fat distribution disorders.

The side effects of the orodispersible tablets are mainly the same as those of inhalation. In some cases, side effects also occur, as are typical for 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 the event of hypersensitivity to the active ingredient or to one of the other ingredients of the respective preparation.

Interactions

Budesonide is broken down in the liver by an enzyme system that also breaks down many other drugs (CYP3A4). Therefore, the combination with other active ingredients that inhibit or stimulate this enzyme can increase or decrease the effect of budesonide.

Said active ingredients include, for example, the antifungal agents ketoconazole and itraconazole, the immune inhibitor ciclosporin (for autoimmune diseases and after transplants), ethinylestradiol and other estrogens (female sex hormones) and the antibiotic rifampicin. If the doctor is familiar with the use of such drugs, he can adjust the budesonide dosage accordingly.

The breakdown of budesonide may be inhibited in patients with severe liver disease. The dose may therefore need to be reduced.

Age restriction

Medicinal products with budesonide on the market are approved for children from 6 years of age (nasal spray and inhalers) and for adults from 18 years of age (for inflammatory bowel diseases and eosinophilic esophagitis).

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

pregnancy and breast feeding period

Budesonide is considered safe to use during pregnancy. So far, no harmful effects on the unborn child have been observed in the treatment of the expectant mother.

Budesonide can also be used while breastfeeding. There have been no reports of side effects in the breastfed infant.

How to get medication with budesonide

Every medicinal product with 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 mainly affects rectal foams and nasal sprays with budesonide.

How long has budesonide been known?

In 1855, the scientist Thomas Addison described a hormone deficiency that could be treated with an extract from the adrenal cortex. As was discovered by researchers Kendall and Reichstein in 1936, this contained the glucocorticoid cortisol.

It was first replicated in the laboratory in 1948. This also opened up the possibility of modifying the structure of the active ingredient in order to change and improve its properties. A "predetermined breaking point" was specifically added to the active ingredient budesonide, which gives way as soon as the active ingredient leaves the site of action.

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