Droperidol - AbsoluteAstronomy.com

Droperidol /droʊˈpɛrIdɔːl/ (Droleptan, Dridol, Inapsine, Xomolix, Innovar [combination with fentanyl]) is an antidopaminergic drug

Medication

A pharmaceutical drug, also referred to as medicine, medication or medicament, can be loosely defined as any chemical substance intended for use in the medical diagnosis, cure, treatment, or prevention of disease.- Classification :...

used as an antiemetic

Antiemetic

An antiemetic is a drug that is effective against vomiting and nausea. Antiemetics are typically used to treat motion sickness and the side effects of opioid analgesics, general anaesthetics, and chemotherapy directed against cancer....

and antipsychotic

Antipsychotic

An antipsychotic is a tranquilizing psychiatric medication primarily used to manage psychosis , particularly in schizophrenia and bipolar disorder. A first generation of antipsychotics, known as typical antipsychotics, was discovered in the 1950s...

. Droperidol is also often used for neuroleptanalgesic anesthesia and sedation in intensive-care treatment.

History and use

Discovered at Janssen Pharmaceutica

Janssen Pharmaceutica

Janssen Pharmaceutica is pharmaceutical company, established in Belgium in 1953 by Paul Janssen. Its headquarters are located in Beerse, in the Campine region of the province of Antwerp, Belgium. It was created not as a subsidiary of a chemical factory but solely with the aim of conducting...

in 1961, droperidol is a butyrophenone

Butyrophenone

Butyrophenone is a chemical compound ; some of its derivatives are used to treat various psychiatric disorders such as schizophrenia, as well as acting as antiemetics....

, and is a potent D₂ (dopamine receptor) antagonist with some histamine

Histamine

Histamine is an organic nitrogen compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter. Histamine triggers the inflammatory response. As part of an immune response to foreign pathogens, histamine is produced by...

and serotonin

Serotonin

Serotonin or 5-hydroxytryptamine is a monoamine neurotransmitter. Biochemically derived from tryptophan, serotonin is primarily found in the gastrointestinal tract, platelets, and in the central nervous system of animals including humans...

antagonist activity. It has a central antiemetic action and effectively prevents postoperative nausea and vomiting

Postoperative nausea and vomiting

Postoperative nausea and vomiting is an unpleasant complication affecting about a third of the 10% of the population undergoing general anaesthesia each year. This equates to about two million people in the United Kingdom annually.-Impact:...

in adults using doses as low as 0.625 mg. It has also been used as an antipsychotic in doses ranging from 5 to 10 mg given as an intramuscular injection, generally in cases of severe agitation in a psychotic patient who is refusing oral medication. Its use in intramuscular sedation has been replaced by intramuscular preparations of haloperidol

Haloperidol

Haloperidol is a typical antipsychotic. It is in the butyrophenone class of antipsychotic medications and has pharmacological effects similar to the phenothiazines....

, midazolam

Midazolam

Midazolam is a short-acting drug in the benzodiazepine class developed by Hoffmann-La Roche in the 1970s. The drug is used for treatment of acute seizures, moderate to severe insomnia, and for inducing sedation and amnesia before medical procedures. It possesses profoundly potent anxiolytic,...

, clonazepam

Clonazepam

Clonazepamis a benzodiazepine drug having anxiolytic, anticonvulsant, muscle relaxant, and hypnotic properties. It is marketed by Roche under the trade name Klonopin in the United States and Rivotril in Australia, Brazil, Canada and Europe...

and olanzapine

Olanzapine

Olanzapine is an atypical antipsychotic, approved by the FDA for the treatment of schizophrenia and bipolar disorder...

. Some practitioners recommend the use of 0.5 mg to 1 mg intravenously for the treatment of vertigo in an otherwise healthy elderly patients who have not responded to Epley maneuver

Epley maneuver

The Epley maneuver is a maneuver used to treat benign paroxysmal positional vertigo . It is often performed by a doctor, chiropractor, or a physical therapist, after confirmation of a diagnosis of BPPV using the Dix-Hallpike . This maneuver was developed by Dr. John Epley and first described in 1980...

Black box warning

In 2001, the FDA changed the labeling requirements for droperidol injection, to include a so-called "Black Box Warning", citing concerns of QT prolongation and torsades de pointes

Torsades de pointes

Torsades de pointes, or simply torsades, is a French term that literally means "twisting of the points". It was first described by Dessertenne in 1966 and refers to a specific, rare variety of ventricular tachycardia that exhibits distinct characteristics on the electrocardiogram .- Presentation...

. The evidence for this is disputed, with 9 reported cases of torsades in 30 years and all of those having received doses in excess of 5 mg. QT prolongation is a dose-related effect, and it appears that droperidol is not a significant risk in low doses.

Side effects

Dysphoria

Dysphoria is medically recognized as a mental and emotional condition in which a person experiences intense feelings of depression, discontent and indifference to the world around them.Mood disorders can induce dysphoria, often with a heightened risk of suicide, especially in...

, sedation, hypotension

Hypotension

In physiology and medicine, hypotension is abnormally low blood pressure, especially in the arteries of the systemic circulation. It is best understood as a physiologic state, rather than a disease. It is often associated with shock, though not necessarily indicative of it. Hypotension is the...

resulting from peripheral alpha adrenoceptor blockade, prolongation of QT interval which can lead to torsades de pointes

Torsades de pointes

, and extrapyramidal side effects

Extrapyramidal symptoms

The extrapyramidal system can be affected in a number of ways, which are revealed in a range of extrapyramidal symptoms , also known as extrapyramidal side-effects , such as akinesia and akathisia .Extrapyramidal symptoms are various movement disorders such as acute dystonic reactions,...

such as dystonic reactions

Dystonia

Dystonia is a neurological movement disorder, in which sustained muscle contractions cause twisting and repetitive movements or abnormal postures. The disorder may be hereditary or caused by other factors such as birth-related or other physical trauma, infection, poisoning or reaction to...

/neuroleptic malignant syndrome

Neuroleptic malignant syndrome

Neuroleptic malignant syndrome is a life- threatening neurological disorder most often caused by an adverse reaction to neuroleptic or antipsychotic drugs...

Chemistry

Droperidol is synthesized from 1-benzyl-3-carbethoxypiperidin-4-one,
which is reacted with o-phenylendiamine. Evidently, the first derivative that is formed under the reaction conditions, 1,5-benzdiazepine, rearranges into 1-(1-benzyl-1,2,3,6-tetrahydro-4-piridyl)-2-benzymidazolone. Debenzylation of the resulting product with hydrogen over a palladium catalyst, and subsequent alkylation of this using 4-chloro-4'-fluorobutyrophenone yields droperidol.

C. Janssen, NV Res. Lab., (1962).
Janssen, P. A. J.; 1963, Belgian Patent .
F.J. Gardocki, J. Janssen, (1964).
P.A.J. Janssen, (1964).

(See pimozide article for proposed mechanism of intramolecular

Intramolecular

Intramolecular in chemistry describes a process or characteristic limited within the structure of a single molecule, a property or phenomenon limited to the extent of a single molecule.- Examples :...

rearrangement.)

History and use

Black box warning

Side effects

Chemistry

Further reading