Butyrophenones: Characteristics Of Atypical Antipsychotics
The discovery of the first antipsychotic in the early 1950s, chlorpromazine, represented a great revolution for the treatment of psychoses, especially schizophrenia.
In this article we will talk about a family of antipsychotics: butyrophenones Within it we find haloperidol (especially known for its usefulness in schizophrenia) and droperidol.
The beginning of research into butyrophenones begins with chlorpromazine.
Chlorpromazine was synthesized as an antihistamine by the French pharmaceutical industry and in 1950, Henri Laborit, a French surgeon, highlighted its sedative effect on psychotic patients. Two years later, in 1952, Delay, Deniker and Harl tested it at the Sainte Anne Hospital in Paris and confirmed its usefulness for the positive psychotic symptoms of schizophrenia
Since the introduction of the first typical antipsychotic, research on neuroleptics has focused on increasing their effectiveness in schizophrenia, reducing the negative symptoms of the disorder, and defining their mechanism of action.
Typical and atypical antipsychotics
Typical or first-generation antipsychotics have more side effects than second-generation or atypical antipsychotics. The latter appeared with the discovery of Clozapine in the 70s, which began to be marketed in Switzerland and Austria.
Currently, second generation or atypical antipsychotics already exist which also act on the negative symptoms of schizophrenia (something that the first generation did not do), in addition to the positive symptoms.
Their antipsychotic efficacy is similar to that of the typical ones, and they differ from them by presenting a lower incidence of EPS (Extrapyramidal Syndrome: set of motor symptoms) and hyperprolactinemia. (side or adverse effects).
Butyrophenones are a family of atypical antipsychotics. Antipsychotics are a type of medications or drugs that are used to treat schizophrenia and other psychotic disorders, as well as bipolar disorder, among others.
In general, antipsychotics reduce dopamine (DA), a brain neurotransmitter abnormally elevated in psychotic disorders.
Droperidol
One of the butyrophenone-type antipsychotics is Droperidol, very short-acting and strongly sedative and tranquilizing
Droperidol has high antiemetic activity (prevents vomiting and nausea). It acts as an antagonist of dopamine receptors, being partially selective for D2 receptors.
Its antiemetic action is produced by the antagonism of DA receptors in a very specific area of the vagus nerve. It is especially useful for the prevention and treatment of postoperative and/or opioid analgesic-induced nausea and vomiting.
It also has weak cholinergic receptor antagonist activity (acetylcholine) muscarinic. Acetylcholine is a neurotransmitter involved in the transmission of nerve impulses and movement.
Characteristics
Droperidol is used for the prevention and treatment of postoperative nausea and vomiting in adults, and as a second line, in children and adolescents. Also for vomiting and nausea induced by morphine derivatives.
Regarding the route of administration of this type of butyrophenone, it is done through the intravenous route.
Some of its contraindications are: cases of hypersensitivity to the drug or allergy to butyrophenones, bradykinesia (decrease in normal heart rate) and Parkinson’s disease.
Precautions
It should be taken into account that it is a medication that can increase the CNS depression produced by other depressant medications. Besides, Caution should be taken in cases of epilepsy, hypotension, cardiac arrhythmias and chronic alcoholism, among others. The appearance of unexplained fever may be a symptom of neuroleptic malignant syndrome.
The dose should be reduced in the elderly, as well as in those subjects with renal failure and/or liver failure. In patients with breast cancer or prolactin-dependent tumors, it can increase the levels of this hormone.
Haloperidol: another type of butyrophenone
Another of the butyrophenone-type neuroleptics is Haloperidol.
It acts the same as the previous one, so it is also a powerful antagonist of brain dopamine receptors. It is classified among highly potent neuroleptics It has no antihistamine or anticholinergic activity (therefore, no side effects of these two types).
The therapeutic indications for haloperidol are diverse. As a neuroleptic it is used in:
As a treatment for psychomotor agitation, some of its uses are for:
Like Droperidol, as an antiemetic it prevents vomiting and nausea of various etiologies.
It is contraindicated in cases of hypersensitivity to the drug, coma, depression of the central nervous system due to alcohol or other depressants, Parkinson’s and damage to the basal ganglia.
