tiapride

Action and Spectrum

Actions and Spectrum: 

• Dopamine D2 Receptor Antagonist: 

tiapride is primarily known as a dopamine D2 receptor antagonist. It acts by blocking the D2 dopamine receptors in the brain. This action is believed to be the basis for many of its therapeutic effects. 

• Antipsychotic Effects: 

tiapride treats various psychiatric conditions, including schizophrenia and other psychotic disorders. By antagonizing D2 receptors, it can help reduce the symptoms of psychosis. 

• Antidyskinetic Effects: 

tiapride is commonly used to manage movement disorders, particularly those associated with neuroleptic (antipsychotic) therapy. It can help alleviate extrapyramidal symptoms (movement-related side effects) caused by other antipsychotic medications, such as parkinsonism, dystonia, and akathisia. 

• Gastrointestinal Effects: 

tiapride also has effects on the gastrointestinal system. It can increase gastric motility and promote gastric emptying. This makes it helpful in managing certain gastrointestinal disorders, such as gastroparesis (delayed stomach emptying) and functional dyspepsia. 

• Sedative and Calming Effects: 

tiapride is known for its sedative and calming effects. It can help reduce anxiety and agitation in some individuals. This property can be beneficial in managing neuropsychiatric conditions characterized by agitation or anxiety. 

• Limited Extrapyramidal Side Effects: 

One of the advantages of tiapride is its relatively lower risk of causing extrapyramidal side effects compared to other antipsychotic medications. This makes it a preferred choice when minimizing movement-related side effects is a priority. 

• Narrow Therapeutic Spectrum: 

tiapride’s therapeutic spectrum is relatively narrow, primarily encompassing neuropsychiatric and gastrointestinal conditions. It is not typically used for a wide range of medical conditions. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Drowsiness 

Agitation 

Convulsions 

Insomnia 

Nasal congestion 

Depression 

ECG changes 

Cardiac arrhythmias 

Delirium 

Agitation 

Photosensitization 

Orthostatic hypotension 

Impotence 

Priapism 

Black Box Warning

Black Box Warning: 

None 

Contraindication / Caution

Contraindication/Caution: 

Contraindications: 

• Prolactin-dependent tumors 
• Hypersensitivity 
• Phaeochromocytoma 

Cautions: 

• Cardiovascular risk 
• Migraine 
• Renal impairment 
• Elderly patients 
• Parkinsons disease 
• Liver impairment 
• Seizures 
• Driving & operating machinery 

Pregnancy / Lactation

Pregnancy consideration:  

Administered to pregnant females, only if benefits outweigh the risks. 

Breastfeeding warnings:  

The drug is excreted in breast milk. The effect on lactating infants is not known.  

Pregnancy category: 

Category A: Well-controlled and satisfactory studies show no risk to the fetus in the initial 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:  

Dopamine D2 Receptor Antagonism: 

tiapride primarily acts as a selective antagonist of the dopamine D2 receptors in the brain. This means it blocks the effects of dopamine, which is involved in regulating behavior, mood, and exercise. 

By blocking D2 receptors, tiapride helps regulate dopamine signaling in the brain, which is particularly important in treating various neuropsychiatric conditions. 

Preferential Binding to Limbic D2 Receptors: 

tiapride has a unique feature: it has a higher affinity for dopamine D2 receptors in the limbic system than those in the striatum. This selective binding pattern is thought to be responsible for its neuroleptic effects, with a lower risk of extrapyramidal side effects (movement-related side effects) compared to some other antipsychotic medications. 

Antipsychotic Effects: 

tiapride is used in the management of psychotic disorders, such as schizophrenia. By blocking D2 receptors, it can reduce the positive symptoms of psychosis, including hallucinations and delusions. 

Pharmacodynamics: 

• Gastrointestinal Effects: 

tiapride can influence the gastrointestinal system by increasing gastric motility and promoting gastric emptying. This makes it helpful in managing certain gastrointestinal disorders, such as gastroparesis (delayed stomach emptying) and functional dyspepsia. 

• Sedative and Calming Effects: 

tiapride is known for its sedative and calming effects. It can help reduce anxiety, agitation, and emotional tension in some individuals. This property can be beneficial in managing neuropsychiatric conditions characterized by agitation or anxiety. 

• Limited Extrapyramidal Side Effects: 

One of the advantages of tiapride is its relatively lower risk of causing extrapyramidal side effects compared to other antipsychotic medications. This makes it a preferred choice when minimizing movement-related side effects is a priority. 

Pharmacokinetics: 

Absorption 

tiapride is well absorbed when administered orally, with peak blood concentrations typically reached within 1 to 3 hours after ingestion. 

Distribution 

tiapride is distributed throughout the body, with a moderate volume of distribution. This means that it can enter various tissues.  

Metabolism 

tiapride undergoes hepatic (liver) metabolism. The major metabolic pathway involves the enzyme cytochrome P450 2D6 (CYP2D6). 

Elimination and Excretion 

The elimination half-life of tiapride can vary but commonly ranges from 4 to 6 hours. This means it takes this amount of time for half of the drug to be cleared from the body. 

Adminstartion

Administration: 

The administration of tiapride is typically done orally in the form of tablets or capsules. The specific dosing instructions may vary based on the brand of tiapride and the condition being treated. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: tiapride 

Pronounced as: tia-pryd 

Why do we use tiapride? 

tiapride is a medication used for various medical purposes, primarily for its neuroleptic (antipsychotic) and antidyskinetic properties. Here are some common reasons why tiapride may be prescribed: 

• Treatment of Psychotic Disorders: tiapride is used to manage psychotic disorders, including schizophrenia. It helps reduce the positive symptoms of psychosis, such as hallucinations, delusions, and thought disorders. 
• Management of Movement Disorders: tiapride effectively treats movement disorders, especially those associated with neuroleptic (antipsychotic) therapy. It can alleviate extrapyramidal symptoms, which include parkinsonism (similar to Parkinson’s disease), dystonia (involuntary muscle contractions), and akathisia (restlessness). 
• Gastroparesis: tiapride is sometimes prescribed to individuals with gastroparesis, characterized by delayed stomach emptying. Promoting gastric motility can help alleviate symptoms like nausea, vomiting, and early satiety. 
• Functional Dyspepsia: tiapride may also be used to manage functional dyspepsia, a chronic or recurrent upper abdominal discomfort or pain. It can help improve gastric motility and reduce symptoms. 
• Adjunct to Withdrawal: tiapride may be an adjunctive treatment in individuals undergoing alcohol withdrawal. It helps in managing the withdrawal symptoms and reduces anxiety and agitation during detoxification. 
• Sedation: tiapride’s sedative properties can be useful in calming individuals with agitation, anxiety, or tension. 
• Limited Extrapyramidal Side Effects: tiapride is preferred over other antipsychotic medications when minimizing movement-related side effects is a priority. 
• Individualized Treatment: Sometimes, tiapride may be chosen when other antipsychotic medications have not provided the desired therapeutic effects or have led to undesirable side effects.