itopride

Action and Spectrum

Actions and Spectrum: 

itopride exerts its therapeutic effects through a combination of actions on the gastrointestinal tract: 

• Dopamine D2 Receptor Antagonism: itopride acts as a dopamine D2 receptor antagonist. By blocking dopamine receptors in the gastrointestinal tract, it inhibits the inhibitory effects of dopamine on gastrointestinal motility. This results in increased acetylcholine release and enhanced cholinergic activity, leading to improved gastrointestinal motility and acceleration of gastric emptying. 
• Acetylcholinesterase Inhibition: itopride also inhibits acetylcholinesterase, the enzyme responsible for breaking down acetylcholine in the gut. By preventing the degradation of acetylcholine, itopride enhances the action of acetylcholine, which further stimulates gastrointestinal motility and improves gastric emptying. 

itopride is primarily used for the treatment of functional dyspepsia and GERD, conditions characterized by symptoms such as: 

• Epigastric pain or discomfort 
• Early satiety 
• Fullness after eating 
• Heartburn 
• Regurgitation 

Drug Interaction

Adverse Reaction

Frequency not defined 

Diarrhoe 

Salivary hypersecretion 

Abdominal pain 

Dizziness 

Headache 

Black Box Warning

Black box warning: 

None 

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: itopride should not be used in individuals with a known hypersensitivity or allergy to itopride or its components. Allergic reactions can range from mild skin rashes to severe anaphylactic reactions. 
• Gastrointestinal Obstruction: itopride is intended to improve gastrointestinal motility. Therefore, it should not be used in individuals with mechanical gastrointestinal obstruction, as it may worsen the condition. 
• Gastrointestinal Hemorrhage or Perforation: itopride should be avoided in cases of gastrointestinal bleeding or perforation, as it may exacerbate these conditions. 
• Prolactin-Producing Tumors: itopride has the potential to increase serum prolactin levels. Therefore, it should be used cautiously or avoided in individuals with prolactin-producing tumors, such as prolactinomas. 
• Severe Liver Impairment: itopride is metabolized by the liver, and its pharmacokinetics can be altered in individuals with severe liver impairment. It should be used with caution or avoided in such cases. 

Caution: 

• Extrapyramidal Symptoms (EPS): itopride, like other medications that affect dopamine receptors, can rarely cause extrapyramidal symptoms such as tremors, muscle stiffness, or abnormal muscle movements. This risk may be higher in elderly individuals.  
• Elderly Patients: Elderly individuals may be more susceptible to specific side effects of itopride, including EPS. Dosing may need to be adjusted, and patients should be monitored closely for adverse effects. 
• Parkinson’s Disease: Patients with Parkinson’s disease or a history of Parkinsonism should use itopride cautiously due to the potential for exacerbating motor symptoms.  
• Seizure Disorders: itopride may lower the seizure threshold, which could concern individuals with a history of epilepsy or other seizure disorders. Careful monitoring and dose adjustment may be necessary in these cases. 
• Cardiovascular Conditions: Caution is advised when prescribing itopride to individuals with underlying heart conditions or a history of arrhythmias. 

Pregnancy / Lactation

Pregnancy consideration: N/A 

Lactation: N/A 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester. 

<b>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: 

itopride is a prokinetic medication used to treat gastrointestinal disorders, primarily functional dyspepsia and gastroesophageal reflux disease (GERD). Its pharmacology involves several mechanisms of action related to the gastrointestinal (GI) tract: 

• Dopamine D2 Receptor Antagonism: itopride is a selective antagonist of dopamine D2 receptors in the GI tract. By blocking these receptors, itopride reduces the inhibitory effect of dopamine on cholinergic neurons in the enteric nervous system. This, in turn, leads to increased release of acetylcholine, a neurotransmitter that enhances GI motility and gastric emptying. 
• Acetylcholinesterase Inhibition: In addition to its action on dopamine receptors, itopride inhibits acetylcholinesterase, the enzyme responsible for breaking down acetylcholine. By inhibiting acetylcholinesterase, itopride prolongs the effects of acetylcholine, further enhancing cholinergic stimulation of GI motility. 
• Enhanced Lower Esophageal Sphincter (LES) Tone: itopride has been shown to increase the tone of the lower esophageal sphincter (LES), which helps prevent the reflux of gastric contents into the esophagus. This effect is beneficial in treating GERD reducing heartburn and regurgitation. 

Pharmacokinetics: 

Absorption 

itopride is rapidly and almost completely absorbed from the gastrointestinal tract, indicating that it is well-absorbed after oral administration. Its bioavailability is approximately 60%, suggesting that about 60% of the dose administered reaches the systemic circulation. The time to reach peak plasma concentration (Tmax) typically occurs within 0.5 to 0.75 hours after oral administration, indicating a fast onset of action. 

Distribution 

itopride exhibits significant plasma protein binding, with approximately 96% of the drug binding to plasma proteins, mainly to albumin. This binding can influence the distribution of the drug within the body. 

Metabolism 

itopride undergoes extensive metabolism in the liver. The primary route of metabolism is via flavine monooxygenase (FMO) enzymes. FMOs are a group of enzymes responsible for the oxidative metabolism of various drugs and xenobiotics. 

Elimination and Excretion 

The elimination of itopride primarily occurs through the urine. This indicates that the kidneys excrete the drug and its metabolites. The terminal elimination half-life of itopride is approximately 6 hours. This means it takes about 6 hours for half of the drug concentration in the plasma to be eliminated from the body. 

Adminstartion

Administration: 

Oral administration 

itopride is typically administered orally in the form of tablets or capsules. itopride is often taken before meals, usually 15 to 30 minutes before each meal. Taking it with food can help enhance its prokinetic effects and alleviate symptoms associated with impaired gastric motility. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: itopride 

Why do we use itopride? 

itopride is a medication primarily used to treat gastrointestinal disorders, particularly those related to impaired gastrointestinal motility. Its main indications include: 

• Functional Dyspepsia: itopride is commonly prescribed for the treatment of functional dyspepsia. Functional dyspepsia is a chronic digestive disorder characterized by epigastric pain or discomfort, early satiety (feeling full after eating), fullness, and bloating. itopride helps by enhancing gastrointestinal motility and reducing these symptoms. 
• Gastroesophageal Reflux Disease (GERD): itopride can be used as part of the treatment regimen for GERD. GERD is when stomach acid frequently flows back into the esophagus, leading to symptoms like heartburn and regurgitation. itopride helps improve lower esophageal sphincter (LES) tone and gastric emptying, which can reduce the frequency and severity of reflux episodes.