Formoterol: Effects, Uses, Side Effects

How formoterol works

The active ingredient formoterol mimics the effect of the “stress hormones” adrenaline and noradrenaline in the body. These are released by the body in stressful situations or when the body has to perform (such as during sports) and ensure that the necessary organs are supplied with oxygen and nutrients in the best possible way: The heart beats faster, blood pressure rises, the bronchial tubes of the lungs expand, and the muscles are better supplied with blood. At the same time, energy-consuming processes such as digestion are slowed down.

Since the active ingredient formoterol is absorbed by inhalation, it acts mainly in the lungs, where it dilates the bronchial tubes, which should ensure better gas exchange. This is particularly important when the bronchi are permanently constricted or prone to constriction due to inflammatory or general pathological processes (as in COPD and asthma).

Absorption, breakdown and excretion of formoterol

Formoterol is largely broken down in the liver and then excreted via the kidneys. A small proportion (less than ten percent) is excreted unchanged. At high blood levels, excretion is quite rapid – half of the active substance is eliminated within two to three hours. At low blood levels, it is slower: it takes up to 14 hours for half of the active substance to leave the body again.

When is formoterol used?

The active ingredient formoterol is used to:

  • Treatment of moderate to severe asthma (in combination with a “cortisone” – i.e., a glucocorticoid)
  • @ treatment of chronic bronchitis

Formoterol is mainly used for longer-term preventive treatment – either continuously, as in chronic disease, or in phases, as in seasonal allergy-related asthma. Since the drug is effective for about twelve hours, it is usually used twice a day.

How formoterol is used

Formoterol is used by inhalation, as this achieves the highest concentration of active ingredient in the lungs. It is used as a compressed gas inhaler (the classic asthma spray) or in the form of capsules with powder for inhalation (with a suitable inhaler). The capsules are inserted into the inhaler individually and pricked. The powder is then transported into the lungs by the air suction during inhalation.

A single dose (spray puff or capsule for inhalation) contains four and a half to twelve micrograms of formoterol and is used twice daily. In severe cases, the dosage may be doubled, which corresponds to a maximum daily dose of 48 micrograms of formoterol.

What are the side effects of formoterol?

Side effects associated with formoterol treatment usually increase at the beginning of therapy and then improve progressively. If symptoms persist, it should be checked whether the inhalation is performed correctly.

One in ten to one hundred people treated experience formoterol side effects such as headache, tremor, palpitations and shortness of breath.

If the preparation also contains a glucocorticoid (colloquially “cortisone”), as is usual in asthma treatment, something must be eaten or drunk after inhalation to rinse the oral cavity – otherwise fungal infections in the oral cavity may occur.

What should be taken into account when using formoterol?

If other sympathomimetics (“stimulating” agents such as ephedrine) are taken during treatment with formoterol, this may increase the side effects.

When formoterol is taken at the same time as diuretic agents (diuretics such as hydrochlorothiazide/HCT, furosemide), steroids and xanthines (for example, caffeine, theophylline), low potassium blood levels (hypokalemia) may occur.

The effect of formoterol may be weakened or canceled when combined with beta-blockers (agents that lower the heart rate and thereby blood pressure), including in the form of eye drops (for glaucoma treatment).

Formoterol should not be used during pregnancy and lactation if it can be avoided. However, in urgent cases where the benefits and risks have been carefully weighed by a physician, it may be used.

Treatment with formoterol is approved in children and adolescents six years of age and older.

How to obtain medicines containing formoterol

Preparations containing the active ingredient formoterol are available only from pharmacies and on prescription.

How long has formoterol been known?

As early as 1903, scientists Bullowa and Kaplan discovered that adrenaline dilates the bronchial tubes and helps with acute asthma attacks. Later, attempts were made to optimize the short duration of action and the many side effects of epinephrine by making changes to its chemical structure. In 1977, formoterol was produced for the first time, but its full potential was not discovered until 1986. In 1997, formoterol was launched on the German market.