Bromperidol

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Not to be confused with Bromperamole.
Bromperidol
Structure of bromperidol.png
Systematic (IUPAC) name
4-[4-(4-bromophenyl)-4-hydroxy-1-piperidyl]-1-(4-fluorophenyl)butan-1-one
Clinical data
AHFS/Drugs.com International Drug Names
Legal status
?
Routes Oral
Identifiers
CAS number 10457-90-6 N
ATC code N05AD06
PubChem CID 2448
ChemSpider 2354 YesY
UNII LYH6F7I22E YesY
KEGG D01101 YesY
ChEMBL CHEMBL28218 YesY
Chemical data
Formula C21H23BrFNO2 
Mol. mass 420.315 g/mol
 N (what is this?)  (verify)

Bromperidol (marketed as Impromen, Bromodol) is a drug which is a butyrophenone derivative. It is a potent and long-acting neuroleptic, used as an antipsychotic in the treatment of schizophrenia. It was discovered at Janssen Pharmaceutica in 1966.

Medical Uses[edit]

Antipsychotic drugs such as Bromperidol have been used for treating patients with schizophrenia for many years. Long‐acting depot injections of these types of drugs are extensively used as a means of long‐term maintenance treatment.

Contraindications[edit]

Bromperidol is contraindicated in central nervous system depression, comatose states, and in those who have in the past been hypersensitive to any of the ingredients of the tablets or of the injection solution or to another butyrophenone such as haloperidol, droperidol and benperidol. Bromperidol is not intended for use in disorders dealing with depression.

Special warnings and special precautions for use[edit]

Increased Mortality in Elderly people with Dementia[edit]

Previous data has shown that elderly people with many forms of dementia who are treated with antipsychotics such as bromperidol are at an increased risk of death compared with those who are not treated with these types of antipsychotics. The cause of the increased risk is not known at this time.

Venous Thromboembolism (VTE)[edit]

Many cases of venous thromboembolism (VTE) have been studied and reported with antipsychotic drugs. Because of this possible risk factor preventative measures should be taken prior to and during bromperidol tratment.

Cerebrovascular Adverse Events (CVA)[edit]

Patients with dementia have a 3-fold increased risk of having cerebrovascular events after taking bromperidol according to controlled clinical trials held in the past. The mechanism for this increased risk is not known. An increased risk cannot be excluded for other antipsychotics or other patient populations. Bromperidol should be used with caution in patients with risk factors for stroke and heart disease.

Neuroleptic Malignant Syndrome[edit]

Like other antipsychotic drugs, adverse effects of Bromperidol can cause neuroleptic malignant syndrome: which is an idiosyncratic response characterized by hyperthermia, generalised muscle rigidity, autonomic instability, altered consciousness. Hyperthermia is often an early sign of this syndrome.

Tardive dyskinesia[edit]

As with all antipsychotic agents, tardive dyskinesia may appear in some patients on longterm therapy or after drug discontinuation. The syndrome is characterized by rhythmical involuntary twitching of the face. This disorder can possibly become permanent in some patients. If the onset of this disorder occurs treatment should be discontinued immediately. The risk of permanent tardive dyskinesia may be greater in elderly patients and patients with mental disorders.

Interaction with other medicinal products and other forms of interaction[edit]

Normally with other antipsychotics it is not reccommended to prescribe them with medications that have the ability to prolong the QT interval, the same should be followed with Bromperidol.

Effect of other drugs on bromperidol[edit]

Liver-enzyme induction by drugs (e.g., phenobarbital, carbamazepine, phenytoin) have the potential to metabolize neuroleptics. If Bromperidol is being taken in combination with these types of drugs the dosage should be heavily monitored and adjusted if necessary.

Pharmakokinetics[edit]

According to the Core Saftey report for bromperidol in a pharmacokinetic study, increased bromperidol concentrations have been reported when bromperidol was given concomitantly with itraconazole known as a potent inhibitor of CYP 3A4.

Effect of bromperidol on other drugs[edit]

As with other antipsychotics, bromperidol has the potential to cause sedation when used in combination with other drugs (e.g. barbiturates, benzodiazepines, antihistamines) and by alcohol. Bromperidol inhibits the action of dopamine agonists, such as bromocriptine, lisuride and L-dopa. It also has potential to increase the risk of hypotension in patients using antihypertensive drugs.

Pregnancy and lactation[edit]

Teratogenicity (potential for abnormalties in psychological development)was not found in studies using rats and rabbits. Although safety in pregnant women has not been unequivocally established. When there is a need to administer Bromperidol during pregnancy the risks should be weighed carefully against the expected therapeutic benefits. In rats Bromperidol is excreted in breast milk. If the use of Bromperidol is considered essential, breastfeeding should be highly discouraged.

Adverse Effects[edit]

The characteristics of the side-effects of bromperidol was investigated in 33 acutely exacerbated Schizophrenic patients. The most frequently observed side-effects were extrapyramidal symptoms. Acute dystonia developed in 10 of 33 patients, and the mean age was significantly lower (P < 0.05) in patients with dystonia (27.3 ± 6.2 years) than that in patients without dystonia (41.5 ± 12.9 years).These findings suggested that acute dystonia is affected by age factor, and that daily dosage or monitoring of drug concentration is unlikely to be a useful marker for the prediction of side effects during bromperidol treatment.

Effects on ability to drive and use machines[edit]

Patients who drive or operate machinery should be warned of the possibility of drowsiness and impaired mental alertness. Simultaneous intake of alcohol may potentiate these effects.

Marketing and Patents[edit]

Impromen is the marketed drug containing Bromperidol as the active ingredient. Impromen was acquired by Eumedica in 2013 from Janssen Pharmaceuticals(Johnson & Johnson) Pharmaceuticals. The drug is currently on the market for perscription use only as an antipsyhchotic.

Bromperidol can be found for sale through countries outside of the United States for research use but sales information for the prescription drug have not been reported.


A patent was filed for Bromperidol in 1980 stating that the drug is to be used for psychotropic therapy. It allows patients to return to a normal rhythm of life when they would otherwise be required to be hospitalized for long periods of time.

Research[edit]

In most drugs the therapeutic response is proportional to drug levels in the blood. This is not the case with many butyrophenones including haloperidol and bromperidol. It has been reported that when taken drug concentrations correlate well with concentrations in the brain but not in the blood. The availability of butyrophenones labeled with y-emitting radionuclides could provide an opportunity for investigators to establish a correlation between dose, blood levels, and brain levels in humans. Vincent et. al at the University of Kentucky synthesized a synthetic radio-labeled Bromperidol radioactive bromine 82^Br .

References[edit]

  • Poldinger W, Bures E, Haage H, Clinical study with bromperidol, a new butyrophenone derivative, Int Pharmacopsychiatry. 1977;12(1):20-4.
  • Dubinsky B, McGuire JL, Niemegeers CJ, Janssen PA, Weintraub HS, McKenzie BE, Bromperidol, a new butyrophenone neuroleptic: a review, Psychopharmacology (Berl). 1982;78(1):1-7.
  • Yasui-furukori, N., Kondo, T., & Ishida, M. (2002). The characteristics of side-effects of bromperidol in schizophrenic patients, (December 2000), 103–106.

External Links[edit]

http://www.eumedica.com/en/qui_sommes_nous.html

http://www.bfarm.de/SharedDocs/Downloads/EN/Drugs/vigilance/PSURs/csp/a-b/bromperidol.pdf;jsessionid=78307460BF62F875DBFB0638381171DD.1_cid340?__blob=publicationFile&v=2

https://www.google.com/patents/DE3024305C2?dq=bromperidol&ei=JgWGVLizNcWoNpH8gZgE&cl=en