Antipsychotics or neuroleptics are one of the best known types of psychopharmaceuticals, after antidepressants and anti-anxiety drugs. It is a type of substance that allows fighting the symptoms of such disabling and severe disorders as schizophrenia, achieving that those who suffer it can control their symptoms and maintain a normative life.
But the formerly called major sedatives can have other uses as well, in some cases even being the major ones. This is the case of droperidol , an antipsychotic that we are going to talk about here.
Droperidol as a psychopharmaceutical
Droperidol is a drug with psychoactive properties that belongs to the group of antipsychotics or neuroleptics.
This substance, derived from tetrahydropyridine and part of the butyrophenones , is considered one of the typical or first generation antipsychotics.
These are drugs that are highly effective in the treatment of hallucinatory and delusional symptoms typical of the positive or productive symptoms of schizophrenia and other psychotic problems, but which have little effect on the negative ones (cognitive, affective and language impoverishment, among others) and which have a high potential for generating annoying and undesirable side effects.
In the case of droperidol, it is a highly potent drug but its effects are short lived (usually two to four hours).
However, beyond schizophrenia droperidol is well known in other fields more medical than psychiatric . It has a relevant anaesthetic and analgesic effect, as well as an antiemetic one (it makes vomiting difficult or prevents it). It is a substance with sedative properties, which is metabolised in the liver and eliminated through the urine.
Its main presentation is in the form of injectables , which are administered intravenously or intramuscularly, and are generally used in cases of emergency. Previously there was an oral presentation, but doubts and the danger of the drug in the long term in relation to coronary events led the pharmacist herself to withdraw this form of presentation from the market.
Mechanism of action
Droperidol affects the body through a mechanism of action based on dopamine antagonism , blocking the receptors of this neurotransmitter in a non-specific way throughout the brain.
This fact makes it effective in the treatment of her hallucinatory and delirious symptomatology as well as in the agitation typical of psychotic outbreaks, which are related to an excess of dopamine in the mesolimbic pathway.
However, its non-specific action on the entire brain makes it likely that side effects will appear , as it also decreases this day in areas where there is no excess and even in those where there is a deficit (as occurs in the mesocortical pathway in people with negative symptoms).
It also affects receptors in the aftermath area, which is linked to its ability to inhibit vomiting. Fortunately, unlike other antipsychotics, it has no effect on acetylcholine or histamine (an effect that could lead to other side effects). It does have an effect on adrenergic receptors, although this is not particularly potent.
Indications and uses of droperidol
Droperidol is an antipsychotic or neuroleptic drug , so one of its indications is the treatment of schizophrenia and other psychotic disorders.
However, its effects on the body are short lived, which makes it (along with its potential to generate arrhythmias and cardiac events) less than optimal for chronic treatment. Instead, is used to treat psychotic break in acute and emergency situations , and is usually not a first choice drug.
Where this drug is most often used, in fact, is in surgery : its powerful analgesic and sedative effect are used for inducing sleep and as a coadjutant drug for anaesthesia (either general or local). It is also used to reduce the usual anxiety before this type of intervention.
Its antiemetic effect also makes it useful for the treatment of nausea following chemotherapy. They are also used to treat nausea and vomiting following such interventions.
Although the use of droperidol is useful and relevant in the treatment of various problems, the truth is that, as with other drugs, it can also cause significant side effects and even risks to one’s physical integrity.
These side effects are not common, especially if use is limited to sporadic situations, but they should be taken into account.
The most common side effects include sedation and drowsiness , which is useful in certain situations but can be annoying and disabling for the user. It is also frequent to generate arterial hypotension and tachycardia, as well as dizziness.
It can also cause hallucinations, excess antidiuretic hormone or alterations in the levels of the different components of the blood (in terms of red blood cells, leukocytes or platelets) that can endanger survival.
Neuroleptic malignant syndrome may also appear, with a mortal potential (this, together with the mentioned risk of leukopenia among others, is one of the reasons why antipsychotics are introduced little by little and with great medical control).
It can also cause, in high doses, parkinsonian-type alterations, agitation, catalepsy, fever, alterations of consciousness such as stupor, convulsions, coma or sudden death.
A major side effect is the fact that it lengthens the QT interval, which can lead to cardiac disturbances such as arrhythmias . In extreme cases it can lead to cardiac arrest.
As we have seen, there are multiple risks that can arise from the use of droperidol, something that makes it necessary to take into account that there are different types of populations that are contraindicated to this drug .
To begin with, it should be avoided by those who are allergic to this drug or its components. Pregnant and lactating women should also avoid it, as there are not enough data regarding its safety for fetuses and infants. Women who are pregnant and who plan to become pregnant in the near future should discuss with their doctor whether or not to use this drug.
Great caution should be exercised in the use of other drugs. Alcohol, depressant substances, some antibiotics, antihypertensives or some drugs that alter the ability of the blood to clot can be examples of elements that can interact dangerously with droperidol. Other drugs such as glucocorticoids are directly contraindicated.
In general, you should discuss the use of this medication with others, given the risk of interaction.
People with angina pectoris, previous heart attacks or heart problems should avoid it , and those with liver or kidney problems and failure should be especially careful. It is contraindicated in subjects with epilepsy or a history of epilepsy, as well as in the population with Parkinson’s disease or severe depression.
People with low levels of potassium or sodium in the blood, bradycardia or arrhythmias or with adrenal tumors, have it contraindicated. Also in insulin-dependent diabetics, special care should be taken
- Spanish Agency for Medicines and Healthcare Products (AEMPS). (2017). Leaflet Droperidol Hikma 2.5 mg/ml solution for injection EFG. AEMPS. Available at: https://cima.aemps.es/cima/dochtml/p/82997/P_82997.html#4-posibles-efectos-adversos
- Cure, S., Rathbone, J., Carpenter, S. (2008). Droperidol for acute psychosis. In: The Cochrane Library Plus, Issue 3. This record should be cited as: Cure S, Rathbone J, Carpenter S. Droperidol for acute psychosis.
- (Translated from The Cochrane Library, Issue . Chichester, UK: John Wiley & Sons, Ltd.)
- Rathbone, J., Mandriota-Carpenter, S.L., Cure, S.J. (2009). Droperidol for schizophrenia. Cochrane Library. Available at: https://www.cochrane.org/es/CD002830/droperidol-para-la-esquizofrenia .