levomepromazine (methotrimeprazine)

Action and Spectrum

Actions and Spectrum: 

levomepromazine is a medication that belongs to the class of phenothiazine antipsychotics. It has a broad spectrum of actions, including sedative, hypnotic, anxiolytic, antipsychotic, and antiemetic effects. 

The sedative and hypnotic effects of levomepromazine make it helpful in treating insomnia and anxiety disorders.  

levomepromazine works by blocking action help to reduce symptoms of psychosis, anxiety, and agitation. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Angioedema 

Apathy 

Anxiety 

Confusion 

Dystonia 

Drowsiness 

Mood changes 

Tremor 

Cataract 

Respiratory depression 

Gastritis 

Seizure 

Delirium 

Tardive dyskinesia 

Black Box Warning

Black Box Warning: 

Geriatric patients who have psychosis related to dementia and undergo treatment with antipsychotic drugs are more prone to death as compared to placebo. 

Contraindication / Caution

Contraindication/Caution: 

levomepromazine is a medication with several contraindications and precautions. Some of the contraindications and precautions of levomepromazine include: 

• Hypersensitivity to levomepromazine or other phenothiazines: levomepromazine should not be used in individuals with a known allergy or hypersensitivity to levomepromazine or other phenothiazines. 
• Central nervous system (CNS) depression: levomepromazine can cause CNS depression, and caution should be taken when using this medication in individuals with a history of CNS depression, including alcohol or drug abuse, head injury, or coma. 
• Parkinson’s disease: levomepromazine can worsen the symptoms of Parkinson’s disease, and caution should be taken when using this medication in individuals with Parkinson’s disease. 
• Seizures: levomepromazine can lower the seizure threshold and increase the risk of seizures. Therefore, it should be used cautiously in individuals with a history of seizures or epilepsy. 
• Cardiovascular disease: levomepromazine can cause hypotension, including arrhythmias, heart failure, or myocardial infarction. 
• Liver or kidney disease: levomepromazine is metabolized in the liver and excreted in the urine. Therefore, individuals with liver or kidney disease should take the drug cautiously. 
• Elderly individuals: levomepromazine should be used cautiously in elderly individuals who are more sensitive to its effects and more likely to experience adverse effects, such as hypotension, extrapyramidal symptoms, or confusion. 

Pregnancy / Lactation

Pregnancy consideration:  

Other antipsychotic agents are preferred in the case of pregnancy.  

Breastfeeding warnings:  

The drug is excreted in the breastmilk 

Pregnancy category: 

• Category A: well-controlled and Satisfactory studies do not show risk to the fetus in the first/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

Pharmacology: 

levomepromazine is a medication that belongs to the class of phenothiazine antipsychotics. Its pharmacological effects are due to its ability to block the activity of certain neurotransmitters in the brain, such as dopamine and serotonin. This action helps to reduce symptoms of psychosis, anxiety, and agitation. 

The mechanism of action of levomepromazine is complex and needs to be fully understood.  By blocking dopamine receptors, levomepromazine can help reduce dopamine activity in certain parts of the brain, which can help alleviate symptoms of psychosis. 

In addition to its effects on dopamine, levomepromazine also blocks serotonin receptors in the brain. Serotonin is another neurotransmitter that regulates mood, appetite, and sleep. By blocking serotonin receptors, levomepromazine can help reduce serotonin activity in certain parts of the brain. 

levomepromazine is also a potent sedative due to its ability to block histamine receptors in the brain. By blocking histamine receptors, levomepromazine can induce drowsiness and promote sleep.  

Pharmacodynamics: 

The pharmacodynamics of levomepromazine refers to the drug’s effects on the body, including its mechanism of action, therapeutic effects, and adverse effects. 

Mechanism of Action: levomepromazine exerts its pharmacological effects by blocking the activity of certain neurotransmitters in the brain, including dopamine, serotonin, and histamine. It is believed that levomepromazine blocks dopamine receptors in the brain, which helps to reduce symptoms of psychosis. levomepromazine also blocks serotonin receptors, which helps reduce anxiety and agitation symptoms. The drug also blocks histamine receptors in the brain, which leads to its sedative effects.  

Pharmacokinetics: 

Absorption 

levomepromazine is typically administered orally but can also be given intramuscularly or intravenously. The drug is absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within 2 to 4 hours. 

Distribution 

levomepromazine has a high degree of protein binding (about 90%), primarily to albumin. The drug gets distributed in the body, including the brain, where it crosses the blood-brain barrier. 

Metabolism 

levomepromazine is extensively metabolized in the liver by the cytochrome P450 system, primarily by the CYP2D6 enzyme. The primary metabolite of levomepromazine is its sulfoxide metabolite, which has a pharmacological activity similar to the parent drug. 

Elimination/Excretion 

The elimination half-life of levomepromazine is approximately 20 to 30 hours. levomepromazine is primarily eliminated through the liver, with about 20% of the drug being excreted unchanged in the urine. 

Adminstartion

Administration: 

Oral Administration: The tablets or capsules should be gulped with a full glass of water.  

Intramuscular and Intravenous Administration: levomepromazine can also be administered by injection, either intramuscularly or intravenously. A healthcare professional typically gives the injection in a hospital or clinic setting. Intravenous administration is generally reserved for emergencies such as acute agitation or psychosis. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: levomepromazine 

Pronounced: lev-ome-pro-mazine. 

Why do we use levomepromazine? 

• Psychotic Disorders: levomepromazine is an antipsychotic medication commonly used to treat psychotic disorders. 
• Nausea and Vomiting: levomepromazine has antiemetic properties and prevents or treats nausea and vomiting associated with chemotherapy, radiation therapy, and surgery. 
• Agitation and Aggression: levomepromazine has sedative and calming effects and can manage agitation and aggression in patients with psychiatric or behavioral disorders. 
• Anxiety and Insomnia: levomepromazine can also manage anxiety and insomnia in patients who have not responded to other treatments. 
• Chronic Pain: levomepromazine has been used as an adjunctive treatment for chronic conditions such as cancer and neuropathic pain.