Tizercin

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Tizercin

Method of action: Antipsychotic, Psycholeptics

Treatment option:

Medically reviewed

Rosario Oropesa

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Tizercin

Quick Facts

Property Description
Active ingredient Levomepromazine (Methotrimeprazine)
Form Tablets (Coated), Solution for injection/infusion
Pharmacological Class First-Generation Antipsychotic (Neuroleptic)
General Purpose Calming severe agitation, distress, anxiety, and restlessness
Origin Synthetic organic compound (Phenothiazine derivative)

What is Tizercin and Its Active Ingredient?

Tizercin is the trade name for a pharmaceutical product whose single active substance is levomepromazine, which is also identified by the international nonproprietary name, methotrimeprazine. This medicine is a synthetic organic compound derived from the phenothiazine chemical family. Levomepromazine is formulated primarily as coated tablets for oral use and as an aqueous solution for injection for parenteral administration. It is a prescription-only drug, signifying that its potent activity requires professional medical oversight, and it is considered a single-active ingredient product.


What Type of Drug is Tizercin? (Pharmacological Classification)

Tizercin is classified as a first-generation antipsychotic agent and is broadly known as a neuroleptic. This categorization signifies the drug’s powerful and widespread depressant action on the central nervous system (CNS). Levomepromazine belongs specifically to the phenothiazines with an aliphatic side-chain, distinguishing it chemically from other tranquilizer classes. This chemical specificity is clinically recognized for delivering a uniquely high degree of sedation compared to many other agents in its pharmacological class.


What is the General Purpose of Levomepromazine?

The general purpose of levomepromazine is to provide a profoundly calming and stabilizing effect to manage severe emotional and physical distress. This broad-spectrum action is utilized to rapidly ease agitation, intense anxiety, and restlessness when a high degree of sedation is necessary. Furthermore, the inherent properties of the drug mean it is also frequently valued for its capacity to significantly help modulate pain signals and reduce nausea and vomiting (antiemetic effects). This combination of effects makes Tizercin a versatile agent for achieving comprehensive comfort and symptomatic relief in complex management situations.

What side effects are possible with Tizercin?

Possible Side Effects and Safety Information

The safety profile of levomepromazine (Tizercin) is officially structured by regulatory authorities based on the frequency and system-organ class affected. The most common effects primarily involve the nervous system and the vascular system, reflecting the drug's strong depressant action.

Frequency Classification Examples of Documented Effects
Very Common (Affecting >1 in 10 people) Sedation (Drowsiness), Fatigue, and Orthostatic Hypotension (dizziness upon standing).
Common (Affecting up to 1 in 10 people) Extrapyramidal symptoms (e.g., restlessness, tremors), Dry mouth, Constipation, Tachycardia, and transient increases in liver transaminases.

Serious adverse reactions, though less frequent, are documented in official prescribing information. These include Neuroleptic Malignant Syndrome (NMS), a rare but critical neurological event; Agranulocytosis (a severe reduction in white blood cells); and potentially serious Cardiac Arrhythmias, specifically the risk of QT prolongation.

Safety characteristics are also noted based on context and population. Orthostatic Hypotension is often most pronounced at the start of treatment or following dose increases. Older adults are noted in regulatory texts to have an increased susceptibility to effects such as hypotension and sedation. Additionally, levomepromazine is associated with an increased risk of Venous Thromboembolism (VTE), as documented for antipsychotic agents in general.

Overdose and Emergency Response

The official regulatory overdose profile for Tizercin (levomepromazine) focuses on severe effects stemming from its action on the central nervous system and cardiovascular system.

Overdose scope

Feature Official Regulatory Statements
Documented overdose presentations Progressive CNS depression (lethargy, stupor, coma), generalized convulsions, severe extrapyramidal dyskinesias (e.g., severe parkinsonian syndrome, tremor), hypotension, and hypothermia.
Physiological systems affected (as stated in label) Central Nervous System, Cardiovascular System (arrhythmias, hypotension), Respiratory System, Thermoregulation.
Dose-related or exposure-related factors (if applicable) Overdose risk is generally associated with exposure to high doses.
Population-specific overdose notes (if applicable) The elderly and patients with pre-existing cardiac or hepatic disease may experience more severe overdose manifestations.
Emergency-response statements (as written in official documents) Seek immediate emergency medical attention for any suspected overdose. Contact your regional Poison Control Centre.
When immediate medical help is required (label-derived phrasing only) Immediate medical help is required for the onset of severe, potentially life-threatening symptoms, including severe hypotension, arrhythmias, respiratory depression, or altered consciousness.

Overdose classifications (high-level)

Classification Official Regulatory Statements
Severity classification (as defined in official documents) Overdose can lead to severe and life-threatening outcomes (e.g., coma, ventricular arrhythmia).
Regulatory basis (EMA / FDA / etc.) Based on documented prescribing information/monographs from international government authorities.
Overdose-context constraints (as defined in official documents) No specific antidote is known. Treatment must be entirely symptomatic and supportive.

Resulting overdose structure

Official overdose statements:

  • The profile highlights the risk of severe cardiac effects, including QT interval prolongation, ventricular arrhythmias, and development of Neuroleptic Malignant Syndrome (NMS).
  • Cardiac monitoring is a required intervention due to the risk of life-threatening cardiac rhythm disturbances.
  • Regulatory guidance specifies that epinephrine must be avoided when treating overdose-related hypotension, as it may worsen the condition.

Connection to the overall overdose profile (193 words total)

Regulatory documents define the overdose profile for Tizercin by documenting the risk of severe CNS depression and cardiovascular collapse. This profile dictates that since treatment must be supportive, seeking immediate emergency medical attention is the fundamental, mandated action for suspected overdose. The required use of cardiac monitoring and specific guidelines on vasopressor agents directly reflect the official documentation of life-threatening cardiac and circulatory instability in overdose situations.

Therapeutic Uses of Tizercin

What Tizercin Treats: Main Uses and Benefits

The therapeutic profile of Tizercin (levomepromazine) is relevant for easing certain distressing symptoms, and is commonly used in clinical settings marked by heightened patient distress. The medication is considered relevant across domains where short-term symptomatic assistance is appropriate for managing intense or refractory symptoms.

Tizercin is applied in addressing conditions presenting with acute episodes and relevant in conditions characterized by periods of heightened symptoms, including schizophrenia, acute psychosis, bipolar disorder, and episodes of severe agitation and anxiety. Furthermore, it is applied in addressing symptom clusters that occur together, such as intractable nausea, vomiting, and symptoms related to physical discomfort within palliative care settings.

It is considered relevant for managing symptoms that interfere with daily comfort. It contributes to a significant calming and stabilizing effect that supports patients during difficult episodes by easing distress. It is commonly used when symptoms intensify and supportive relief is needed, and may contribute to easing the overall symptom load.


Quick Fact: Relief for Multi-Symptom Distress

Property Description
Therapeutic Role Calming and Stabilization
Symptom Focus Agitation, Psychotic Manifestations, Persistent Nausea/Vomiting, Physical Discomfort
Relevant Context Acute Crisis, Palliative/End-of-Life Care
Patient Benefit Contributes to improved comfort and may help patients cope more steadily

Regulatory References

  1. Health Canada Methotrimeprazine Monograph

Eligibility and Restrictions for Use

Eligibility Map: Who Can and Cannot Use Tizercin — Official Regulatory Information

Tizercin (levomepromazine) is governed by strict eligibility rules primarily centered on cardiovascular stability and age, as defined in regulatory documents.

Eligibility scope Status
Populations Contraindicated Absolute Prohibition
- History of QT interval prolongation or severe cardiac abnormalities (e.g., bradycardia <55 bpm)
- Uncorrected metabolic abnormalities like hypokalaemia or hypomagnesaemia
- Children under 18 years (for certain oral tablet formulations)
Populations Requiring Caution/Restriction Conditional Use
- Patients with hepatic or renal impairment
- Older adults (geriatrics) and ambulant patients over 50
- Patients with risk factors for VTE (blood clots) or stroke
- Patients with diabetes mellitus (requires glycaemic monitoring)

Pregnancy and Lactation Eligibility Status: Safety in pregnancy is not established, and use is generally not recommended. Neonates exposed during the last trimester must be monitored. Breastfeeding must be discontinued if treatment is necessary, as the drug passes into milk.

What should I know about interactions with other medicines?

Tizercin Interactions with other medicines and products

The official regulatory profile for levomepromazine interactions centers on major pharmacokinetic and pharmacodynamic conflicts that necessitate strict co-administration rules.

Contraindicated and High-Risk Combinations Co-administration is formally prohibited with certain medicines due to the high risk of severe ventricular rhythm disorders, specifically Torsades de Pointes. These prohibited agents include Citalopram, Escitalopram, Hydroxyzine, Piperaquine, and Domperidone. The medicine is also contraindicated in conditions of severe central nervous system depression, including those resulting from alcohol or narcotics. Alcohol must be strictly avoided due to the potentiation of central depressant effects.

Pharmacokinetic and Exposure Effects Levomepromazine is officially documented as a potent inhibitor of the enzyme Cytochrome P450 2D6 (CYP2D6). This inhibition leads to increased plasma concentrations and systemic exposure of other drugs that are primarily metabolized by CYP2D6. Conversely, substances like certain antacids (e.g., Aluminum Hydroxide) can reduce the absorption of levomepromazine, resulting in lower serum concentrations.

Pharmacodynamic Conflict and Monitoring Co-administration with other QT prolonging drugs requires a precautionary check of the patient’s QT interval and ongoing ECG monitoring. A reciprocal antagonism of effects is documented when levomepromazine is combined with Dopaminergics, such as Levodopa. Additionally, Adrenaline (Epinephrine) must not be used to treat hypotension in patients receiving this drug. Elderly patients are noted to have increased susceptibility to hypotension and extrapyramidal effects when co-administered with other agents that share these properties.

Mechanism of Action

Targeted Agonism of Central Alpha-2 Receptors

Tizercin's core molecular action is the selective agonism of presynaptic alpha-2 adrenergic receptors (α2-ARs), predominantly located on interneurons within the spinal cord. Binding to these receptors activates an intracellular signaling cascade that reduces calcium influx into the presynaptic terminal. This results in the diminished release of excitatory amino acid neurotransmitters (such as glutamate) into the synaptic cleft, thereby modulating the signal transmission at the synapse.

Modulation of Spinal Motor Reflexes

This molecular action manifests primarily in the central nervous system (CNS). By decreasing excitatory input, Tizercin acts to dampen overactive spinal polysynaptic reflexes that contribute to motor overactivity. This focused activity leads directly to the physiological consequence of decreased muscle hypertonia and diminished reflex activity in the affected motor units.

Central Systemic Physiological Effects

Agonism of α2-ARs outside the primary spinal motor pathways, including those in arousal and cardiovascular control centers, causes a wider systemic influence. This non-selective engagement results in associated physiological changes, including general CNS depression and a reduction in systemic blood pressure.

Dosage and Administration Information

How to Use Tizercin: Official Administration Guidelines

Levomepromazine (Tizercin) administration is defined by specific routes, dose ranges, and timing constraints.


Administration Scope

Administration Scope Official Instruction
Route of Administration Oral (tablets, solution), Intramuscular (IM) injection, Intravenous (IV) injection, and Subcutaneous (SC) continuous infusion.
Dosing Schedule Initial adult oral doses range from 25 mg to 50 mg daily for ambulant patients, up to 100 mg to 200 mg daily for inpatients, with a maximum daily dose of 1000 mg.
Frequency and Timing The total daily oral dose is typically administered in divided portions or as a single larger dose at bedtime to manage effects. Injections may be repeated every 6 to 8 hours as needed.
Preparation Requirements Intravenous administration requires the injection solution to be diluted with an equal volume of normal saline immediately before use.
Age-Group Rules The total daily oral dose must not exceed 37.5 mg for the pediatric population (under 12 years). Cautions are noted for use in ambulant older adults.
Procedural Conditions Patients starting on higher initial oral doses are instructed to remain in bed for the first few days of treatment. Oral doses are to be taken at mealtimes in divided-dose regimens.

Official Protocol Structure

The official protocol dictates a titration-based use, where treatment starts at the lowest effective dose and is gradually increased, strictly observing the maximum limit. The administration method is highly flexible (oral, IM, IV, SC) but demands specific preparatory steps for the parenteral routes, such as pre-use dilution for IV injection. This framework ensures adherence to standardized dosing patterns and population-specific constraints.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Tizercin


Evidence Overview for Acute Psychiatric Symptoms

Levomepromazine was evaluated in research exploring how symptoms change over time in conditions associated with acute or disruptive episodes, such as schizophrenia and acute psychosis. These studies included short-term Randomized Controlled Trials (RCTs). Studies included comparisons against placebo or against other compounds relevant to the treatment landscape. The research primarily examined outcomes related to overall psychiatric symptom severity, as well as assessments of severe agitation or restlessness where symptoms become more noticeable. Study populations consisted of adults experiencing these periods of heightened symptom activity.

Regulatory reviews and syntheses of the pivotal evidence classify the compound as a first-generation antipsychotic agent. Findings include patterns observed in the data related to changes measured during the acute study period. Research also describes patterns observed in assessments of psychomotor agitation, with findings related to short-term changes during episodes where symptoms intensify.

It is important to note that the primary evidence base consists of trials that were conducted historically to achieve initial regulatory approval. Data related to contemporary, large-scale comparisons against newer-generation medicines remains limited. Additionally, many of the existing trials had modest sample sizes, and follow-up durations were limited, meaning long-term outcomes are not fully established based on this initial research.


Evidence Overview for Palliative Symptom Management

Research concerning Tizercin in symptom management settings primarily focuses on outcomes related to systemic or functional imbalance, such as intractable nausea and vomiting, and outcomes describing episodic or acute changes like agitation or delirium in terminally ill patients. The evidence landscape here differs from the psychiatric context, relying more on observational cohort studies, retrospective series, and the consistent documentation of clinical experience found in authoritative clinical guidelines.

Research monitored patient-reported outcomes describing perceived discomfort and assessed symptom intensity during periods of increased symptom activity in adults with advanced illness. Research describes patterns observed in some studies concerning symptom intensity in patients where symptoms may vary. Findings describe patterns related to the assessment of physical discomfort and acute agitation, often in research settings where multiple symptoms are managed simultaneously.

However, the evidence quality varies across studies in this area. Specifically, for its use in addressing nausea and vomiting in the palliative population, systematic reviews have reported a notable absence of published Randomized Controlled Trials. Therefore, the available data for certain groups remain insufficient, and the evidence base for this use includes documentation of clinical experience and consensus, rather than exclusively from high-level interventional trials.


Long-Term Evidence and Study Follow-Up

The research exploring Tizercin primarily focuses on short-term symptom changes, reflecting its common use in managing acute episodes or achieving rapid stabilization. Follow-up durations were limited in many of the core efficacy studies for both psychiatric and palliative indications. For instance, trials examining acute psychiatric symptoms typically monitored patients for only a few weeks. Similarly, in palliative care research, observation periods were very short-term, often measured over a few days or hours.

Therefore, there is limited information for long-term outcomes, and the durable effects of the compound are not fully established by the existing research structure. Studies do not fully describe how symptoms evolve over extended periods or what patterns of stability might be observed in patients using the compound for chronic management.


Research Findings in Specialized Populations

Research has explored the use of Tizercin in several specialized adult populations, most notably patients with advanced disease or those in acute crisis. The observational studies relevant to palliative care provided evidence derived from settings with varying symptom burdens and focused specifically on adults receiving end-of-life care. Research has examined its use in populations presenting with complex symptom clusters, where conditions are characterized by fluctuating or episodic manifestations.

While these studies contribute to the broader evidence landscape, comparative evidence is often lacking for specific subgroups. Results apply only to the populations studied, and findings describing group patterns do not determine whether an individual in a different subgroup will respond similarly.


Key Research Gaps and Areas of Uncertainty

The research highlights what is known—and what is still uncertain—about Tizercin. Certainty remains low for some of its indications because comparative evidence is lacking, particularly against newer medicines in the psychiatric space. Furthermore, the documented lack of high-quality, randomized evidence for certain uses in palliative care constitutes a significant research gap.

Limitations in the research include sample sizes that were modest in several key regulatory trials, and the fact that follow-up durations were limited across the entire evidence base. Long-term effects are not fully established, and data for certain groups (such as children or pregnant populations) remain insufficient or non-existent in the core regulatory summaries. These factors highlight that while the evidence contributes to understanding symptom patterns, research is ongoing to provide more comprehensive insights.

Key Studies & References

  1. Methoprazine (Methotrimeprazine Maleate Tablets) Health Canada Product Monograph (Regulatory Document)

Frequently Asked Questions (FAQ)

Common questions about Tizercin (FAQ)


Q: How quickly should someone expect Tizercin to start working?

Studies and official information indicate that the onset of action for the oral form is generally noted to occur around 30 minutes after administration. Injected forms of the medicine may be observed to act slightly faster than the oral tablets.


Q: How long does Tizercin usually stay in your system?

Official information describes the medicine as having a long biological half-life, which is the time it takes for half of the dose to be cleared from the body. This half-life is reported to be approximately 15 to 30 hours, meaning the effects of a single dose may be noticeable for 12 to 24 hours.


Q: Does Tizercin interact with common over-the-counter pain relievers?

Official product information indicates this medicine acts as an inhibitor of the CYP2D6 enzyme. This means it may cause other medications processed by that enzyme to build up in the body, potentially increasing their effects. Official information notes that this potential for interaction means the use of these pain relievers may require professional evaluation.


Q: Are there any specific foods that should be avoided when taking Tizercin?

Regulatory texts contain information that oral doses are administered at mealtimes. While specific food interactions are not listed, official documents describe that certain antacids, such as Aluminum Hydroxide, may reduce the body’s absorption of the medicine.


Q: Is Tizercin intended to be a long-term treatment?

The research that supports this medicine's approval focused mainly on short-term symptom changes. For this reason, official sources indicate that long-term outcomes and the durability of effects are not fully established by the existing research structure.


Q: Are there any official warnings about driving or operating machinery while using Tizercin?

Official documents contain warnings that driving or operating machinery should be avoided while using this medication. This guidance is based on the fact that the medicine commonly causes symptoms like drowsiness, confusion, dizziness, and feeling lightheaded.


Q: What are the signs of a serious allergic reaction to Tizercin?

Official product information lists hypersensitivity (a severe reaction to a substance) as a reason the medicine should not be used. Although specific signs of a full allergic reaction are not detailed, official texts document that unexplained fever may precede a rare, serious event, and mention that treatment may need to be stopped if this symptom occurs.


Q: Is it possible for Tizercin to lose its effectiveness over a long period of time?

Because the key research evidence focused on short-term symptom changes, official documents note that the durable or long-term maintenance of the medicine's effects is not fully established. Therefore, information regarding long-term loss of effectiveness is limited in the core regulatory research.


Q: What is the mechanism of Tizercin's action described in simple, non-technical terms?

Tizercin is classified as a neuroleptic, which means it has a powerful and widespread depressant action on the central nervous system (CNS). The action provides a profoundly calming and stabilizing effect that is utilized in the management of severe emotional and physical distress.


Q: What specific phases of research studies (e.g., Phase 3) support Tizercin's regulatory approval?

Regulatory approval is supported by the synthesis of the pivotal evidence from historical studies. The research overview specifically mentions short-term Randomized Controlled Trials (RCTs) as part of this evidence base.


Q: How long do the initial side effects of Tizercin typically last?

The official safety documents indicate that the common side effect of Orthostatic Hypotension (dizziness upon standing) is often most pronounced at the start of treatment. The documented duration or persistence of other common side effects is not explicitly listed in the regulatory texts.


Q: Is Tizercin classified as a controlled substance?

Regulatory documents classify this medicine as a Prescription-Only Medicine (POM) in certain jurisdictions, and a Schedule 4 drug (Prescription only) in others. This classification signifies that it is a potent medicine requiring professional medical oversight.


Q: What official regulatory bodies have provided approval for Tizercin?

Regulatory coverage for this medicine is confirmed by documents published by or referencing various national health authorities, including bodies like the MHRA (UK) and Medsafe (New Zealand). This indicates that the medicine has undergone regulatory review in multiple regions.


Q: What type of medical professional typically initiates the prescription for Tizercin?

Official information confirms that this is a prescription-only drug. Given its approved uses for acute agitation and palliative symptom management, it is frequently prescribed by specialists such as psychiatrists, palliative care physicians, or oncologists.

How should Tizercin be stored and disposed of?

How to Store and Dispose of Tizercin?

This section details the official requirements for storing, handling, and disposing of Tizercin, based strictly on regulatory documentation.

Storage Component Official Requirement
Temperature Store at controlled room temperature, 20 C to 25 C (68 F to 77 F).
Protection Keep in the original, tightly closed container. Protect from excessive moisture and avoid freezing.
Safety Keep Tizercin out of the reach and sight of children.
Disposal Do not flush unused or expired medicine down a toilet or pour it down a drain. Dispose of according to local pharmaceutical waste disposal regulations.

These guidelines define the constraints necessary to maintain the drug's quality and stability until the expiration date. Storing the medicine in its original container prevents misidentification and ensures it is protected from light or moisture exposure. Following the disposal rules minimizes environmental impact and prevents accidental exposure.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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