DRUG INTERACTION

Actions and spectrum: 

Actions of benperidol: 

• Dopamine Receptor Blockade: benperidol exerts its therapeutic effects by blocking dopamine receptors in the brain. It has a higher affinity for D2 dopamine receptors, which are associated with the regulation of mood, behaviour, and perception. By blocking these receptors, benperidol helps to modulate dopamine neurotransmission and reduce the symptoms of psychosis. 
• Central Nervous System Depression: Like other antipsychotic medications, benperidol can produce sedation and central nervous system depression. This can contribute to its calming and tranquilizing effects, which may help alleviate agitation and aggressive behaviour in individuals with psychotic disorders. 

Spectrum of Use: 

benperidol is primarily indicated for the treatment of schizophrenia and other psychotic disorders. Its use is reserved for cases where other antipsychotic medications have been ineffective or when its specific properties are deemed advantageous. It is not typically used as a first-line treatment due to its potential side effects. benperidol is more commonly used in certain regions of the world, such as Europe, and may have limited availability in other areas. 

Frequency not defined 

Dizziness 

Excitement 

Insomnia 

Seizures 

Nausea 

Constipation 

Hyperprolactinemia 

Gynecomastia 

Amenorrhea 

Tachycardia
abnormal Liver function 

Rash 

Exanthema 

Blood dyscrasias 

Weight changes 

Ventricular fibrillation 

Torsades de pointes 

Dyskinesia 

Apathy 

Dry mouth 

Blurred vision 

ECG changes 

Agranulocytosis 

Photosensitivity 

Lens opacities 

Pulmonary embolism 

Thromboembolism 

Dizziness 

Akathisia

Black Box Warning: 

There are no known black box warnings specifically associated with the use of benperidol. 

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: benperidol should not be used in individuals who have a known hypersensitivity or allergy to the medication or any of its components. 
• QT Prolongation: benperidol can prolong the QT interval on an electrocardiogram (ECG), which can lead to a potentially serious heart arrhythmia known as torsades de pointes. Therefore, it should be used with caution or avoided in individuals with a history of QT prolongation, congenital long QT syndrome, recent myocardial infarction, heart failure, or other conditions that increase the risk of QT interval prolongation. 
• Severe Central Nervous System Depression: benperidol can cause sedation and central nervous system depression. It should be used cautiously or avoided in individuals who are severely depressed, have impaired consciousness, or are at risk of respiratory depression. 
• Parkinson’s Disease and Extrapyramidal Disorders: benperidol can exacerbate symptoms of Parkinson’s disease or other extrapyramidal disorders. It may not be suitable for individuals with these conditions, and careful monitoring is required if used. 
• Epilepsy and Seizure Disorders: benperidol can lower seizure threshold & increase the risk of seizures. It should be used cautiously in individuals with a history of epilepsy or seizure disorders.

Caution: 

• Extrapyramidal Symptoms (EPS): benperidol, like other antipsychotic medications, can potentially cause extrapyramidal symptoms such as dystonia, akathisia, parkinsonism, and tardive dyskinesia. Healthcare providers should monitor patients for these symptoms, especially during the initial treatment period, and adjust the dosage or consider alternative treatments if necessary. 
• Cardiac Effects: benperidol can prolong the QT interval on an electrocardiogram (ECG), which may increase the risk of a serious heart arrhythmia called torsades de pointes. Caution should be exercised when prescribing benperidol to individuals with a history of QT prolongation, cardiovascular disease, electrolyte imbalances, or those taking other medications that can prolong the QT interval. 
• Central Nervous System Depression: benperidol may cause sedation and central nervous system depression. Patients should be cautioned against activities like driving or operating machinery, especially during the initial stages of treatment. 
• Risk of Seizures: benperidol can lower the seizure threshold and increase the risk of seizures. Caution is advised in individuals with a history of epilepsy or seizure disorders. 
• Hyperprolactinemia: benperidol may lead to elevated levels of prolactin, a hormone that can cause side effects such as menstrual irregularities, galactorrhoea (abnormal milk production), and sexual dysfunction. 
• Anticholinergic Effects: benperidol has anticholinergic properties that can lead to side effects like dry mouth, blurred vision, constipation, and urinary retention. Caution is needed in individuals with pre-existing urinary or gastrointestinal conditions. 
• Elderly Population: Elderly individuals may be more sensitive to the sedative and anticholinergic effects of benperidol. Dosage adjustments and careful monitoring are often required. 
• Liver and Kidney Function: benperidol is metabolized by the liver and excreted through the kidneys. Caution should be exercised in individuals with impaired liver or kidney function, as dosing adjustments may be necessary. 
• Pregnancy and Breastfeeding: The use of benperidol during pregnancy and breastfeeding should be carefully considered, weighing the potential benefits against the potential risks. It should only be used if clearly needed and under medical supervision. 

Comorbidities: 

• Cardiovascular Conditions: The cardiovascular conditions like heart disease, arrhythmias, or a history of QT interval prolongation, may require cautious use of benperidol due to its potential to prolong the QT interval on an electrocardiogram (ECG). Close monitoring and ECG assessments may be necessary, and alternative antipsychotic options could be considered. 
• Epilepsy and Seizure Disorders: benperidol can lower seizure threshold & increase the risk of seizures. Individuals with a history of epilepsy or seizure disorders should be carefully evaluated before using benperidol, and the potential risks and benefits should be weighed. 
• Parkinson’s Disease and Movement Disorders: benperidol can exacerbate symptoms of Parkinson’s disease or movement disorders due to its dopamine receptor-blocking effects. Dosing adjustments and careful monitoring are important in individuals with these conditions. 
• Renal or Hepatic Impairment: benperidol is metabolized by the liver and excreted through the kidneys. patients with impaired liver or kidney function may require dose adjustments to prevent the accumulation of the medication and potential adverse effects. 
• Respiratory Conditions: benperidol can cause sedation and central nervous system depression, which may be of concern in individuals with respiratory conditions like chronic obstructive pulmonary disease (COPD) or sleep apnea. Monitoring and cautious use are advised. 
• Endocrine Disorders: benperidol can lead to elevated prolactin levels, potentially affecting individuals with endocrine disorders, such as hyperprolactinemia or hormonal imbalances. 
• Geriatric Patients: Elderly individuals may be more susceptible to the sedative and anticholinergic effects of benperidol. Lower initial doses and careful monitoring are often recommended. 
• Psychiatric Comorbidities: Individuals with comorbid psychiatric conditions, such as mood disorders or anxiety disorders, may require individualized treatment approaches, as antipsychotic medications like benperidol can influence mood and behaviour. 

Pregnancy consideration: pregnancy category C 

Lactation: excreted into human milk: yes  

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 
• Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 
• Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.   
• Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits. 
• Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women. 
• Category N: There is no data available for the drug under this category. 

Pharmacology: 

benperidol is a potent antipsychotic medication belonging to the butyrophenone class. Its pharmacology centers on dopamine receptor blockade, particularly D2 dopamine receptors in the brain. By inhibiting dopamine’s binding to these receptors, benperidol exerts its therapeutic effects, alleviating symptoms of psychosis such as hallucinations and delusions. Its high affinity for D2 receptors contributes to its potency.

benperidol’s actions also extend to other receptors, including alpha-adrenergic and histamine H1 receptors, accounting for its sedative and anticholinergic properties. Careful dosing is required due to the risk of extrapyramidal symptoms, sedation, and the potential to prolong the QT interval on an electrocardiogram. The pharmacology of benperidol underscores its role in managing psychotic disorders while necessitating vigilance for potential side effects and interactions.  

Pharmacodynamics: 

• Dopamine Receptor Blockade: benperidol is a potent antipsychotic medication that acts by blocking dopamine receptors in the brain, particularly D2 dopamine receptors. This blockade inhibits the binding of dopamine, a neurotransmitter associated with mood and behaviour regulation. By modulating dopamine activity, benperidol helps alleviate symptoms of psychosis, including hallucinations and delusions. 
• Central Nervous System Effects: The dopamine receptor blockade by benperidol has a range of central nervous system effects. It helps restore the balance of neurotransmitters involved in mood and thought processes, contributing to the reduction of psychotic symptoms. However, this action can also lead to potential side effects such as sedation, drowsiness, and cognitive effects. 
• Extrapyramidal Symptoms (EPS): While effective in treating psychosis, benperidol’s dopamine receptor antagonism can result in extrapyramidal symptoms, including dystonia, akathisia, parkinsonism, and tardive dyskinesia. These motor disturbances arise from alterations in the dopamine signaling pathways in the basal ganglia. 
• Alpha-Adrenergic and Histamine H1 Receptors: Beyond dopamine receptors, benperidol also interacts with alpha-adrenergic and histamine H1 receptors. This interaction contributes to its sedative and anticholinergic properties, which may lead to drowsiness, dry mouth, blurred vision, and other related effects. 
• QT Interval Prolongation: benperidol’s blockade of cardiac potassium channels can lead to QT interval prolongation on an electrocardiogram (ECG). This effect poses a risk for arrhythmias, particularly torsades de pointes. Monitoring of ECG and caution in patients with pre-existing cardiovascular conditions are essential.

Pharmacokinetics: 

Absorption 

benperidol is usually administered orally as tablets or liquid. It is well absorbed from the gastrointestinal tract, although absorption can vary among individuals. Food intake may affect the rate and extent of absorption. 

Distribution 

After absorption, benperidol is distributed throughout the body, including the central nervous system, due to its lipophilic nature. It crosses the blood-brain barrier and can bind to various receptors, particularly dopamine receptors in the brain. 

Metabolism 

benperidol undergoes hepatic metabolism primarily through the cytochrome P450 enzyme system, particularly CYP3A4. The metabolites formed are less pharmacologically active than the parent compound. Genetic and individual variations in metabolism can influence the rate at which benperidol is metabolized. 

Elimination and excretion 

Metabolized benperidol and its metabolites are primarily excreted in the urine. A small portion may be excreted in feces. The elimination half-life of benperidol varies and can be prolonged, especially in individuals with impaired liver function. 

Administration: 

Oral Administration: 

• Dosage Form: benperidol is available in various dosage forms, such as tablets or liquid.  
• Dosage: The dosage of benperidol is based on factors such as the severity of your symptoms, your medical history, and your response to the medication. It is important to take the medication exactly as prescribed. 
• Timing: benperidol is usually taken once or twice a day. It is important to follow the dosing schedule provided by your healthcare provider. 
• Swallowing: If you are taking tablets, swallow them whole with a glass of water.  
• Liquid Form: If you are prescribed the liquid form of benperidol, carefully measure the prescribed dose using a calibrated measuring device. Shake the liquid well before each use. 

Patient information leaflet 

Generic Name: benperidol 

Pronounced: (Ben-PEH-ri-dol)  

Why do we use benperidol? 

• Schizophrenia: benperidol is prescribed to manage the symptoms of schizophrenia, a chronic mental disorder characterized by distorted thinking, emotions, and perceptions. It helps reduce hallucinations, delusions, thought disturbances, and emotional withdrawal, allowing individuals to regain a more stable and functional state of mind. 
• Psychotic Disorders: Beyond schizophrenia, benperidol may be used to treat other psychotic disorders like schizoaffective disorder or delusional disorder. Its antipsychotic effects help address the core symptoms of these conditions, improving overall mental well-being. 
• Severe Agitation: benperidol can be employed to manage severe agitation and behavioural disturbances in individuals with psychotic disorders. Its calming and sedative properties contribute to stabilizing patients and preventing potential harm to themselves or others. 
• Treatment-Resistant Cases: In some instances, benperidol might be considered when other antipsychotic medications have not adequately controlled symptoms or when alternative treatment options are limited. It may be used cautiously and under close supervision in such cases.