Droperidol: uses and side effects of this antipsychotic drug.

A drug against schizophrenia that is also used in certain medical contexts.

Antipsychotics or neuroleptics are one of the best known types of psychotropic drugs, after antidepressants and anxiolytics. They are a type of substance that can combat the symptoms of such disabling and severe disorders as schizophrenia, enabling sufferers to control their symptoms and maintain a normative life.

But the formerly also called major sedatives can also have other uses, in some cases even being the most common. This is the case of droperidolan antipsychotic of which we are going to speak here.

Droperidol as a psychotropic drug

Droperidol is a drug with psychoactive properties that belongs to the group of antipsychotics or neuroleptics.

This substance, derived from tetrahydropyridine and forming part of the butyrophenones, is considered one of the typical or first generation antipsychotics.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-type problems, but have little effect on the negative symptoms (cognitive, affective and language impoverishment, among others) and have a high potential for generating bothersome and undesirable side effects.

In the case of droperidol, it is a drug of high potency but whose effects are of short duration (usually between two and four hours).

However, beyond schizophrenia, droperidol is well known in other fields, more medical than psychiatric.. It has a relevant anesthetic and analgesic effect, as well as an antiemetic (it hinders or prevents vomiting). It is a substance with sedative properties, which is metabolized in the liver and eliminated through urine.

Its main presentation is in the form of injectables, which are administered via the urinary tract.which are administered intravenously or intramuscularly, and is generally used in emergency cases. Previously there was an oral presentation, but doubts and the danger of the drug in the long term in terms of coronary events made the pharmaceutical company itself withdraw this form of presentation from the market.

Mechanism of action

Droperidol affects the organism through a mechanism of action based on dopamine antagonism.blocking the receptors of this neurotransmitter in a non-specific way in the whole brain.

This fact makes it effective in the treatment of 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, However, its non-specific action in the whole brain makes it likely that side effects may appear, as it also decreases this day in areas of the brain where it is present.However, its non-specific action in the whole brain makes it likely that side effects will appear, as it also decreases 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 postrema area, something that is linked to its ability to inhibit vomiting. Fortunately, unlike other antipsychotics, it has no effects on acetylcholine or histamine (an effect that could generate other side effects). It does have an effect on adrenergic receptors, although it is not particularly potent.

Indications and uses of droperidol

Droperidol is an antipsychotic or neuroleptic drug.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) not optimal for chronic treatment. Instead, it is used to treat acute-phase psychotic breaks and in emergency situations, and is generally not an effective treatment for the acute phase of psychotic episodes.and is generally not a drug of first choice.

In fact, it is most commonly used in surgery.The most common use of this drug is in surgery: its potent analgesic and sedative effects are used for sleep induction and as an adjuvant drug for anesthesia (either general or local). It is also used to reduce the usual previous anxiety before this type of interventions.

Its antiemetic effect also makes it useful for the treatment of post-chemotherapy nausea. It is also used to treat nausea and vomiting after such interventions.

Side effects

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 relevant side effects and even risks to one's own physical integrity.

These side effects are not common, especially if the use is limited to sporadic situations, but they should be taken into account.

Among the most common side effects are sedation and drowsinesswhich 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, excesses of antidiuretic hormone or alterations in the levels of the different blood components (in terms of red blood cells, leukocytes or platelets) that can endanger survival.

Neuroleptic malignant syndrome may also appear.This, together with the aforementioned risk of leukopenia, among others, is one of the reasons why antipsychotics are introduced gradually 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 side effect of great relevance is the fact that it lengthens the QT interval, something that can generate cardiac alterations, such as can cause cardiac disturbances, such as arrhythmias.. In extreme cases it can cause cardiac arrest.

Contraindications

As we have seen, there are multiple risks that the use of droperidol may have, something that makes it necessary to take into account that there are different types of people who are contraindicated for this drug..

To begin with, it should be avoided by those who are allergic to this drug or its components. Pregnant women and nursing mothers should also avoid it, since there is insufficient data regarding its safety for fetuses and infants. Women who are pregnant or plan to become pregnant in the near future should discuss with their physician whether or not to use this drug.

Great caution should be exercised in the consumption of other drugs. Alcohol, depressant substances, some antibiotics, antihypertensives. or some drugs that alter the ability of blood to clot may be examples of elements that may interact dangerously with droperidol. Other drugs such as glucocorticoids are directly contraindicated.

In general, the use of this drug together with other drugs should be consulted with the physician, given the risk of interaction.

People with angina pectoris, previous heart attacks or heart problems should avoid this drug.and those with hepatic or renal problems and failures should be especially cautious. It is contraindicated in subjects with epilepsy or previous history of epilepsy, as well as in people with Parkinson's disease or severe depression.

People with low levels of potassium or sodium in blood, bradycardia or arrhythmias or with adrenal tumors, are contraindicated. Also in insulin-dependent diabetics, special care should be taken.

Bibliographic references:

• Spanish Agency of Medicines and Health Products (AEMPS). (2017). Package 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. Oxford, Update Software Ltd. Available at: http://www.update-software.com.
• (Translated from The Cochrane Library, Issue 3. 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.