Betamethasone

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 betamethasone is a synthetic cortisol derivative (a glucocorticoid or corticosteroid). It has anti-inflammatory and anti-allergic effects and suppresses the immune system. It is used for numerous diseases, both chronic and acute. Here you can read everything interesting about the effect of betamethasone, side effects and use.

This is how betamethasone works

The natural hormone cortisol, also called hydrocortisone, has multiple effects in the human body. Colloquially, the hormone is also called "cortisone", but this is not correct because it is the inactivated (ineffective) form of cortisol.

Cortisol has the following functions in the body:

• It increases the production of blood sugar (glucose) in the liver in order to be able to provide the body with energy quickly in stressful situations.
• It accelerates protein turnover - the breakdown of protein also provides energy.
• It has a dampening effect on the immune system.

Betamethasone is a synthetic derivative of cortisol. It looks around 25 to 30 times stronger than its natural counterpart. All glucocorticoids are divided into classes from 1 (weakly effective) to 4 (very strongly effective) based on their potency - betamethasone is assigned to class 3 (highly effective).

Compared to cortisol, betamethasone is broken down or inactivated less quickly in the body because it cannot be broken down into cortisone by the body's own enzymes.

Breakdown and excretion of betamethasone

Betamethasone is quickly absorbed from the gastrointestinal tract after ingestion and reaches the highest blood levels after one to two hours. The biological half-life, i.e. the time in which the effect drops by half, is very long at 36 to 54 hours. For comparison: the half-life of cortisol is around ten hours.

The liver converts betamethasone into a more soluble compound. This is then excreted in the stool via the bile.

When is betamethasone used?

Betamethasone is applied locally to the skin for skin diseases such as psoriasis, neurodermatitis, allergic or itchy skin reactions (hives). Betamethasone ointment, gel or cream are used that contain the active ingredient as so-called esters: In these compounds, fatty acids are attached to the betamethasone in order to increase its absorption into the skin. Examples are betamethasone valerate and betamethasone dipropionate.

If betamethasone is to be administered as a syringe (injection) or taken in liquid form, betamethasone hydrogen phosphate is used. It has a much better water solubility than the pure active ingredient. The areas of application are even more extensive. Examples are:

• Buildup of fluid (with swelling) in the brain (cerebral edema)
• Initial treatment for severe skin conditions (see above)
• Rheumatoid arthritis
• more severe inflammatory reactions in the body

However, it is always important that it is not bacterial inflammation, as the dampening of the immune system by betamethasone could make the infections flare up particularly strongly.

The duration of the application varies from person to person.

This is how betamethasone is used

The most common application form of betamethasone is the local treatment with the help of betamethasone ointment for skin diseases. Due to the long duration of action, the ointment often only needs to be applied once a day.

In addition, betamethasone tablets are often used, which must be taken according to a doctor's therapy plan. In general, the dose is initially increased quickly, then kept constant (plateau phase) until the disease has subsided, and then slowly reduced in order to end the therapy. The tablets are usually taken in the morning, as the body's own cortisol levels are also highest in the morning after getting up.

What are the side effects of betamethasone?

Side effects are primarily only to be expected with internal use (e.g. betamethasone tablets or injections). When applied locally to the skin, only a negligibly small part of the active ingredient gets into the blood.

The side effects of betamethasone are dose dependent. With high dosages and / or long-term use, the following adverse reactions are possible:

• diabetes
• increased levels of fat and cholesterol in the blood
• Changes in blood electrolyte levels
• Muscle weakness
• Mood swings
• dizziness
• Indigestion
• Changes in the number of certain blood cells

Many of these side effects can be effectively avoided if a dose is given that is as high as necessary but as low as possible.

What should be considered when taking betamethasone?

Betamethasone is broken down by certain enzymes (mainly CYP3A4) in the body. Taking other medicines that stimulate these enzymes at the same time reduces the effect of betamethasone. Such drugs include the antibiotic rifampicin and the epilepsy drugs phenytoin, carbamazepine and phenobarbital.

Conversely, the simultaneous administration of drugs that inhibit the enzymes concerned can increase the effect of betamethasone. This applies, for example, to the antifungal agents ketoconazole and itraconazole).

In combination with ACE inhibitors (antihypertensive agents such as ramipril, enalapril, lisinopril), changes in the blood count can occur.

Betamethasone can reduce the blood sugar lowering effect of oral antidiabetic drugs.

Nonsteroidal anti-inflammatory drugs (ASA, ibuprofen, indomethacin), which are often taken as headache relievers, in combination with betamethasone can lead to increased gastrointestinal bleeding.

Glucocorticoids such as betamethasone cross the placental barrier and pass into breast milk, which is why they should not be used during pregnancy and breastfeeding. For medically justified delivery before the actual due date, betamethasone is used to stimulate the premature development of the lungs in the unborn child.

How to get medication with betamethasone

All drugs containing betamethasone are subject to a doctor's prescription.

Since when is betamethasone known?

As early as 1855, the scientist Thomas Addison (after whom Addison's disease was named, in which the cortisol-producing adrenal glands are underactive) described a disease that could be successfully treated with an adrenal extract. The hormone cortisol it contains was identified in 1936 by the research groups led by Kendall and Reichstein. In 1948 it was possible for the first time to manufacture cortisol in the laboratory. This also offered the opportunity to change its structure in order to optimize the duration of action and reduce the potential for side effects. This eventually led to the development of betamethasone.

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