acetophenazine

Action and Spectrum

Actions and Spectrum: 

acetophenazine is a typical antipsychotic medication with actions that help alleviate symptoms associated with psychotic disorders, particularly schizophrenia. It exerts its therapeutic effects through its antagonistic action on dopamine receptors in the brain. 

It can also alleviate negative symptoms like flattened affect (reduced emotional expression) and social withdrawal. However, it may be less effective in treating negative symptoms compared to newer atypical antipsychotics. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Sedation 

Urinary retention 

Restlessness 

Muscle stiffness 

Constipation 

Arrhythmias 

Blurred vision 

Dry mouth 

Breast enlargement 

Galactorrhea 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications 

• Hypersensitivity 
• Coma 
• Circulatory collapse 
• Subcortical brain damage 
• Blood dyscrasias 

Cautions 

• Elderly patients 
• Cardiovascular diseases 
• Renal impairment 
• Hepatic impairment 
• Respiratory diseases 
• Seizure disorders 

Pregnancy / Lactation

Pregnancy consideration:  

No data is available regarding the administration of the drug during pregnancy. 

Breastfeeding warnings:  

No data is available regarding the excretion of drugs in breast milk. 

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: No data is available for the drug under this category. 

Pharmacology

Pharmacology: 

The critical aspects of the pharmacology of acetophenazine: 

• Dopamine receptor blockade: acetophenazine primarily acts as a dopamine receptor antagonist, specifically targeting D2 receptors. Blocking these receptors in some areas of the brain helps reduce the excessive doAntagonizing these receptors helps disorders like schizophrenia. 
• Serotonin receptor blockade: acetophenazine also has a moderate affinity for serotonin receptors, particularly the 5-HT2A receptors. The antagonism of these receptors may contribute to the antipsychotic effects of the medication. 
• Adrenergic receptor blockade: acetophenazine exhibits antagonistic activity at alpha-adrenergic receptors, leading to various physiological effects, including hypotension (low blood pressure), sedation, and other autonomic effects. 
• Histamine receptor blockade: acetophenazine has antihistaminic properties, specifically antagonism of histamine H1 receptors. This activity contributes to the sedative and anticholinergic effects associated with the medication. 
• Other receptor interactions: acetophenazine may also interact with other receptors to varying degrees, including alpha-1 adrenergic, alpha-2 adrenergic, and other serotonin receptor subtypes. 

Pharmacodynamics: 

The critical pharmacodynamic aspects of acetophenazine: 

• Dopamine receptor antagonism: acetophenazine exerts its primary pharmacodynamic effect by blocking dopamine receptors, particularly the D2 receptors. Antagonizing these receptors helps modulate the excessive dopamine activity associated with psychotic disorders, such as schizophrenia. 
• Serotonin receptor antagonism: acetophenazine also exhibits moderate affinity for serotonin receptors, mainly the 5-HT2A receptors. Antagonism of these receptors contributes to its antipsychotic effects and may also help alleviate some adverse symptoms of schizophrenia. 
• Adrenergic receptor blockade: acetophenazine acts as an antagonist at alpha-adrenergic receptors, leading to various physiological effects. This includes vasodilation and decreased peripheral vascular resistance, which can result in lowered blood pressure. 
• Histamine receptor antagonism: acetophenazine has antihistaminic properties, blocking histamine H1 receptors. This activity contributes to the sedative effects of the medication. 

Pharmacokinetics: 

Absorption 

acetophenazine is well absorbed after oral administration. However, the absorption may be slower and less predictable than other antipsychotic medications. It is recommended to take acetophenazine with food to improve its absorption. 

Distribution 

acetophenazine has a high volume of distribution, indicating that it distributes widely throughout the body tissues. It readily crosses the blood-brain barrier, allowing it to affect the central nervous system. 

Metabolism 

acetophenazine undergoes extensive hepatic metabolism. It is primarily metabolized by the liver enzyme CYP2D6 to produce active and inactive metabolites. These metabolites are further metabolized through various pathways before being excreted from the body. 

Elimination and Excretion 

The elimination half-life of acetophenazine is relatively long, ranging from about 20 to 40 hours. This means it takes several days for the medication to be eliminated from the body. The elimination occurs primarily through hepatic metabolism and subsequent renal excretion of metabolites. 

Adminstartion

Administration: 

acetophenazine tablets are typically taken by mouth with water. Taking the medication with food is usually recommended to improve absorption and minimize stomach upset.

Take care of the instructions provided by your healthcare provider or the medication’s package insert regarding the dosage, frequency, and timing of administration. It’s important to swallow the tablets whole and not crush or chew them unless specifically instructed. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: acetophenazine 

Pronounced: be-TRIX-a-ban 

Why do we use acetophenazine? 

acetophenazine is primarily used in the treatment of psychotic disorders, particularly schizophrenia. The main reasons why acetophenazine is used: 

• Treatment of schizophrenia: acetophenazine is prescribed to manage the symptoms of schizophrenia, which is a chronic mental disorder characterized by distorted thinking, hallucinations, delusions, disorganized behavior, and reduced emotional expression. It helps to reduce or eliminate these symptoms, allowing individuals to function better in their daily lives. 
• Control of positive symptoms: acetophenazine targets the positive symptoms of schizophrenia, including hallucinations (perceiving things that are not there), delusions (false beliefs), and disorganized thinking. By blocking dopamine receptors in the brain, acetophenazine helps to reduce the excessive dopamine activity associated with these symptoms. 
• Adjunctive treatment: acetophenazine can be used as an adjunctive medication in combination with other antipsychotics or treatment modalities to enhance the management of symptoms in individuals with schizophrenia.