| ATC Code | N05AD01 |
| CAS number | 52-86-8 |
| PUB number | 3559 |
| Drugbank ID | DB00502 |
| Empirical formula | C21H23ClFNO2 |
| Molar mass (g·mol−1) | 375,864 |
| Physical state | solid |
| Density (g·cm−3) | 1,2 |
| Melting point (°C) | 148-152 |
| Boiling point (°C) | 529 |
| PKS value | 8,66 |
| Solubility | 0.00446 mg/mL |
Haloperidol is an active substance that is used to treat psychotic illnesses as well as chronic pain and movement disorders. It belongs to the group of neuroleptics and has antipsychotic and antidopaminergic effects. Haloperidol is a pethidine derivative and is structurally very similar to loperamide. It is usually available as a white powder that is insoluble in water.
Haloperidol works by binding to the dopamine receptors, mainly D2. It inhibits the effects caused by dopamine. The exact mechanism of action has not yet been fully researched, but it is assumed that haloperidol binds to the postsynaptic dopamine 2 receptors, thereby displacing dopamine from the receptors and causing hallucinations or delusions to disappear. Haloperidol also has an influence on the 5-HT2 and alpha-1 receptors, but these are negligible for the effect of haloperidol.
Haloperidol is broken down in the liver, mainly by the enzymes CYP2D6 and CYP3A4. The bioavailability, i.e. the percentage of the active substance available in the blood, is 40-75%. The half-life of haloperidol, i.e. the time the body needs to excrete half of the active substance, is approx. 14.5-36.7 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 1.7-6.1 hours.
Always take haloperidol exactly as described in the package leaflet or as advised by your doctor.
The usual recommended dose for adults and children aged 13 years and over is 0.5-2 mg 2-3 times a day for moderate symptoms and 3-5 mg 2-3 times a day for severe symptoms.
The maximum dose is 20 mg per day.
The recommended dose for children aged 6 to 12 years is 0.5 mg daily. This should be divided into 2-3 doses per day.
The following side effects may occur:
Very common:
Common:
Occasionally:
Rarely:
Frequency unknown:
Interactions may occur if the following medicines are taken at the same time:
Haloperidol must NOT be taken in the following cases
Haloperidol can be used from the age of 6.
Haloperidol can be used during pregnancy after consultation with your doctor and if no alternative is possible.
No increased risk of malformations has been found in the 1st trimester of pregnancy.
In the 2nd and 3rd trimester of pregnancy, the newborn may experience adjustment disorders, which disappear again. This can lead to impaired breathing, gastrointestinal tract and brain function (affecting the nervous system). In addition to the adaptation disorders, extrapyramidal motor disorders may occur.
Haloperidol should only be used during breastfeeding after consultation with your doctor and with reservations.
Babies whose mothers take unusually high doses may suffer from psychomotor developmental disorders. If therapy has to be continued, it is advisable to have the infant's plasma levels determined after 2-3 weeks in order to see to what extent the infant is absorbing the active substance through breast milk.
Haloperidol was developed and subsequently marketed by Paul Janssen, the founder of the pharmaceutical company Janssen Pharmaceutica. It was first approved in Belgium in 1957.
Thomas Hofko
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