Umeclidinium bromide

Umeclidinium bromide is an active substance used to treat chronic obstructive pulmonary disease (COPD). Umeclidinium bromide belongs to the group of parasympatholytics and has a bronchodilator effect. Umeclidinium bromide can also be used as an inhaler in combination with vilanterol and/or fluticasone. It has a long duration of action and therefore has the advantage that it only needs to be used once a day. Umeclidinium bromide is chemically related to atropine and is a quinuclidine derivative. It is usually available as a white powder.

Umeclidinium bromide acts on the muscarinic receptors of the smooth muscles of the respiratory tract. It is a competitive antagonist and neutralizes the effects of acetylcholine there. Respiratory movements are controlled by the parasympathetic nervous system, which is activated by acetylcholine, resulting in a bronchodilator effect. Umeclidinium bromide mainly acts on the muscarinic 3 receptors (M3) and blocks the receptors there so that acetylcholine can no longer bind and therefore cannot exert its effect. As a competitive antagonist, the concentration of umeclidinium bromide must be greater than that of acetylcholine.

Acetylcholine acts by activating the M3 receptor. This activates the enzyme phospholipase C, which forms inositol 1,4,5-trisphophate, which in turn releases calcium into the cell. Calcium then triggers muscle contractions, which exacerbate the symptoms of COPD.

Umeclidinium bromide is broken down in the liver via the enzyme CYP2D6 and is excreted almost exclusively via faeces. The bioavailability, i.e. the percentage of the active substance available in the blood, is 13% on average. The half-life, i.e. the time the body needs to excrete half of the active substance, is approx. 11 hours. The maximum plasma concentration (Cmax), i.e. the maximum concentration of the active substance in the blood plasma (liquid cell-free part of the blood), is reached after 5-15 minutes.

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

The usual recommended dose is 55-62.5 micrograms per day, which corresponds to one inhalation.

The maximum dose per day is one spray. If your dose needs to be adjusted, you should never use more or less than one spray, but have a new inhaler with a different dosage prescribed.

The following side effects may occur:

Frequent:

• accelerated heartbeat
• Frequent and painful urination
• common cold
• Infection of the nose and throat
• cough
• sinusitis
• Headache

Occasionally:

• Irregular heartbeat
• constipation
• Dry mouth
• Skin rash
• Taste disturbances

Interactions may occur if the following medicines are taken at the same time:

• Medication for the treatment of respiratory problems such astiotropium

Umeclidinium bromide must NOT be taken in the following cases:

• in case of allergy to umeclidinium bromide

Umeclidinium bromide should not be used under the age of 18.

In older people, there is a possibility that umeclidinium bromide could have a stronger effect at the same dosage than in other people.

Umeclidinium bromide should only be used during pregnancy after consultation with a doctor. Animal studies with rats and rabbits did not reveal any increased risk of malformations. Reduced fertility was also not observed in animal studies.

Umeclidinium bromide should only be used during breastfeeding after consultation with a doctor. In animal studies with rats and rabbits, no transfer into breast milk was observed.

A decrease in fertility in men was not observed.