Domperidone
Updated onBenjamin 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.
More about the experts All content is checked by medical journalists.Domperidone is one of the most important medicines used to treat nausea and vomiting. Its effect is based among other things on an acceleration of the gastric passage. Since the active ingredient hardly crosses the blood-brain barrier, side effects in the central nervous system are very rare. Here you can read everything you need to know about the effects and use of domperidone, side effects and interactions.
This is how domperidone works
Domperidone is a so-called prokinetic. It inhibits certain docking points (receptors) of the messenger substance dopamine. Thereby it promotes the motility (mobility) of the stomach, stimulates gastric emptying and works against nausea and vomiting.
Dopamine, as a neurotransmitter, mediates communication between nerve cells. It has a variety of tasks in the central nervous system (brain and spinal cord):
Among other things, dopamine is involved in the control of movement processes, contributes to positive feelings as a so-called "happiness hormone", causes psychoses and delusions when levels are too high, and influences the prolactin level in the blood (prolactin promotes milk production in women in the breast).
Domperidone blocks the docking points of dopamine so that the messenger substance can no longer bind itself and develop its effect. However, since the active ingredient cannot or hardly cross the blood-brain barrier - the protective barrier against potentially harmful substances in the blood - it has no effect on the dopamine receptors in the central nervous system (CNS). This means that an effect on the ability to move in the brain controlled by dopamine, which it would otherwise suppress, and on the psyche is almost impossible.
The so-called vomiting center is an exception - a special part of the CNS that is located in the brain stem and the adjacent elongated spinal cord. Here the blood-brain barrier is "perforated", which means that this part can react very quickly to harmful substances, namely with nausea and vomiting, in order to prevent further absorption of the harmful substances.
Since the communication of the nerve cells in the vomiting center is also partly controlled by dopamine, domperidone can unfold its effect here - in other words: counteract nausea and vomiting.
Another positive side effect of domperidone, the origin of which is still unclear, is the accelerated emptying of the stomach in the direction of the intestines. This relieves the stomach, which can also reduce nausea and bloating.
Uptake, breakdown and excretion
After ingestion, domperidone is quickly absorbed into the blood in the intestine, where it reaches the highest active ingredient levels after half an hour to an hour.
However, a large part of the active ingredient is already broken down in the intestinal mucosa and in the liver, so that only about 15 percent of the active ingredient can reach the circulatory system and work.
After about seven to nine hours, half of domperidone is excreted - one third through the urine and two thirds through the stool.
When is domperidone used?
Domperidone is approved for the relief of symptoms of nausea and vomiting. As soon as the symptoms improve, the intake should be stopped. As a rule, domperidone should not be taken for longer than a week - unless specifically instructed by the attending physician.
Promoting milk production with domperidone and thereby being able to breastfeed more effectively is a so-called "off-label use" - a use outside of the approved areas of application. The active ingredient effectively stimulates milk production, has few side effects, hardly passes into breast milk and does not get into the CNS. It is therefore popular with mothers with breastfeeding problems.
This is how domperidone is used
Domperidone is taken in the form of tablets or a suspension (juice). If this is not possible due to severe vomiting, domperidone suppositories are used.
To improve absorption in the intestines, it is recommended to take the tablets or suspension half an hour to an hour before eating. Depending on the severity of the symptoms, one tablet of ten milligrams of domperidone three times a day is recommended. This corresponds to a maximum daily dose of 30 milligrams.
The duration of the intake should not exceed a week.
What side effects does domperidone have?
With short-term and low-dose use, the active ingredient domperidone has relatively few side effects:
One in ten to one hundredth people treated has a dry mouth.
One in hundred to one in a thousand patients may experience side effects such as headache, drowsiness, loss of libido, anxiety, diarrhea, rash, weakness, chest pain and increased milk flow from the mammary gland.
A rare but potentially dangerous side effect is the increase in what is known as the QT interval in the heart (a section of the EKG). There is a risk of a prolongation of the QT time, especially with prolonged intake of high doses.
What should be considered when taking domperidone?
Contraindications
Domperidone must not be taken if:
- Prolactinoma (prolactin-producing tumor of the pituitary gland)
- moderate to severe liver dysfunction
- Heart failure (heart failure)
- Extension of the QT interval
- Use of other drugs that may increase the QT interval
- Taking drugs that strongly inhibit a certain liver enzyme system (CYP3A4 inhibitors)
Interactions
Domperidone needs a sufficiently acidic gastric environment for absorption in the intestine. The additional intake of active ingredients that neutralize gastric acid or inhibit gastric acid production therefore significantly reduces the absorption of domperidone. Such active substances are, for example, H2 blockers (e.g. cimetidine, ranitidine) and proton pump inhibitors (e.g. omeprazole, pantoprazole).
Domperidone is broken down in the body by an enzyme system (CYP3A4), which also metabolizes numerous other active substances. If the active ingredients concerned are taken in addition, this can lead to a reduced breakdown and thus to increased levels of domperidone in the body.
Examples of such active ingredients include many antibiotics (e.g. erythromycin), agents against fungal infections (e.g. ketoconazole), antidepressants (e.g. amitriptyline, citalopram), pain relievers (e.g. tramadol), sedatives (e.g. diazepam) and agents against increased cholesterol levels (e.g. atorvastatin, simvastatin ).
If you are taking domperidone, you should inform a doctor who will prescribe other medication for you. You should also tell the pharmacist that you are using domperidone before buying any over-the-counter medication. He can then point out possible interactions.
Age restriction
Although studies have been carried out on the use of domperidone in infants from the age of six months, the active ingredient has so far only been approved for children from the age of twelve and a body weight of at least 35 kilograms.
pregnancy and breast feeding period
Previous data on the use of domperidone during pregnancy gave no indications of a foetotoxic risk (i.e. the risk of toxic effects on the unborn child). If you have severe pregnancy sickness, other measures such as meclozin should be tried first.
Significantly fewer data are available on the use of domperidone during breastfeeding. Due to the risk of side effects on the mother's heart, it is not recommended. However, if a doctor deems the use of domperidone to be necessary, the patient can still continue to breastfeed.
How to get drugs with domperidone
Medicines with this active ingredient are subject to pharmacy and prescription requirements in Germany, Austria and Switzerland.
Since when is domperidone known?
The active ingredient was developed in 1974 and approved in many European countries just a few years later. Initially, a domperidone injection solution was also put on the market, but it repeatedly led to severe cardiac arrhythmias. As a result, her license was withdrawn again in the end. In the USA, the approval for the active ingredient domperidone (also for other dosage forms) was never granted because of the said side effects on the heart.
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