clebopride

Action and Spectrum

Actions and spectrum: 

clebopride is a prokinetic agent that acts on the gastrointestinal (GI) tract. Its primary action is to increase the motility and coordination of GI smooth muscle, particularly in the stomach and small intestine. clebopride exerts its effects by antagonizing dopamine receptors in the GI tract, specifically the D2 receptors.

By blocking these receptors, clebopride enhances the release of acetylcholine, a neurotransmitter that stimulates GI smooth muscle contraction. This leads to improved GI motility and can be helpful in conditions characterized by slowed gastric emptying or impaired intestinal transit. 

The spectrum of clebopride’s action is focused on the GI system, and it is primarily used to treat conditions like gastroparesis (delayed stomach emptying), functional dyspepsia, and other GI motility disorders. It is not typically used for other medical conditions, as its effects are localized to the digestive system. 

Drug Interaction

Adverse Reaction

Frequency not defined 

Extrapyramidal symptoms 

drowsiness 

hypotension 

dizziness 

Depression 

restlessness 

Diarrhoea 

hypertension 

Headache 

galactorrhoea 

Black Box Warning

Black Box Warning: 

There is no specific black box warning associated with clebopride. 

Contraindication / Caution

Contraindication/Caution: 

Contraindication: 

• Hypersensitivity: clebopride should not be used in individuals who have a known hypersensitivity or allergy to the medication or any of its components. 
• Gastrointestinal Obstruction: It is typically contraindicated in individuals with mechanical gastrointestinal obstruction, as clebopride’s prokinetic effects may exacerbate the obstruction. 
• Gastrointestinal Perforation: clebopride should not be used in cases of gastrointestinal perforation or risk of perforation, as increased motility could potentially worsen this condition. 
• Seizure Disorders: clebopride may lower the seizure threshold, so it should be used cautiously or avoided in individuals with a history of seizure disorders. 
• Pregnancy and Lactation: The safety of clebopride during pregnancy and breastfeeding is not well established, and it is typically avoided unless the potential benefits outweigh the risks.

Caution: 

• Elderly Patients: Caution is advised when prescribing clebopride to elderly individuals, as they may be more sensitive to its effects, including potential side effects. Lower doses or closer monitoring may be necessary. 
• Renal Impairment: clebopride is primarily excreted through the kidneys. Patients with significant renal impairment may require dosage adjustments, as the drug’s elimination may be delayed. 
• Liver Impairment: Patients with severe liver impairment may require dosage adjustments, as the drug’s metabolism may be affected in these individuals. 
• Gastrointestinal Conditions: clebopride should be used cautiously in individuals with a history of gastrointestinal bleeding or ulcers. It may exacerbate these conditions due to its prokinetic effects. 
• Cardiac Conditions: clebopride can affect the QT interval in some individuals, potentially leading to arrhythmias. Caution is advised when using clebopride in patients with a history of cardiac arrhythmias or those taking medications that prolong QT interval. 
• Driving and Operating Machinery: clebopride may cause dizziness and affect mental alertness in some individuals. caution should be used while driving or operating heavy machinery.

Comorbidities: 

• Psychiatric Disorders: Patients with gastrointestinal motility disorders like IBS often have comorbid psychiatric conditions such as anxiety and depression. clebopride’s effects on the gastrointestinal system can indirectly benefit these comorbid psychiatric symptoms by alleviating gastrointestinal discomfort. 
• Cardiovascular Conditions: Patients with cardiovascular conditions such as hypertension or heart disease may also suffer from gastrointestinal motility disorders. When prescribing clebopride to individuals with cardiovascular comorbidities, healthcare providers should consider the medication’s potential effects on heart rate and rhythm, as it may prolong the QT interval in some cases. 
• Diabetes: Some patients with diabetes may develop gastrointestinal motility issues. clebopride’s prokinetic effects can help improve gastric emptying and reduce symptoms of gastroparesis, a common complication of diabetes. 
• Chronic Pain Conditions: Individuals with chronic pain conditions like fibromyalgia or chronic back pain, may experience exacerbated gastrointestinal symptoms due to stress or medication side effects. clebopride may provide relief for these comorbid gastrointestinal symptoms. 
• Inflammatory Bowel Disease (IBD): While clebopride is not typically used to treat IBD itself, some patients with IBD may have concurrent functional gastrointestinal disorders. clebopride might help manage the functional symptoms in these cases. 

Pregnancy / Lactation

Pregnancy consideration: pregnancy category: not assigned 

Lactation: excreted into breast milk: unknown  

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: 

clebopride is a medication with prokinetic properties primarily used to treat gastrointestinal disorders associated with impaired motility. It exerts its pharmacological effects by selectively blocking dopamine D2 receptors in the gastrointestinal tract, which in turn inhibits the inhibitory actions of dopamine on gut motility.

Additionally, clebopride acts as an agonist of serotonin (5-HT4) receptors in the GI tract, stimulating the release of acetylcholine and promoting smooth muscle contractions. These combined actions enhance gastric emptying, improve gastrointestinal transit, and alleviate symptoms like constipation, abdominal discomfort, and bloating in conditions such as irritable bowel syndrome with constipation (IBS-C) and gastroparesis. clebopride’s pharmacology is focused on restoring normal gut motility and relieving associated symptoms.  

Pharmacodynamics: 

• Dopamine D2 Receptor Antagonism: clebopride acts as a selective antagonist of dopamine D2 receptors in the GI tract. By blocking these receptors, it inhibits the inhibitory effects of dopamine on gut motility. This results in increased GI peristalsis and enhanced transit of food and digestive contents. Increased gut motility can help relieve symptoms such as bloating, abdominal discomfort, and constipation. 
• Serotonin (5-HT4) Receptor Agonism: clebopride also functions as an agonist of serotonin (5-HT4) receptors in the GI tract. Activation of these receptors stimulates acetylcholine release, a neurotransmitter that promotes smooth muscle contractions in the GI tract. This action further enhances gut motility and contributes to the drug’s prokinetic effects. 
• Enhanced Gastric Emptying: clebopride accelerates gastric emptying by stimulating smooth muscle contractions in the stomach and upper GI tract. This effect can be particularly beneficial in conditions associated with delayed gastric emptying, such as gastroparesis. 
• Improved Gastrointestinal Transit: clebopride’s prokinetic properties lead to improved transit of food and digestive contents through the entire GI tract. This helps to relieve symptoms of constipation and irritable bowel syndrome with constipation (IBS-C). 
• Reduction in Gastrointestinal Symptoms: The enhanced gut motility and transit facilitated by clebopride can alleviate symptoms like abdominal discomfort, bloating, and nausea associated with various GI disorders.

Pharmacokinetics: 

Absorption 

clebopride is well-absorbed from the gastrointestinal tract after oral administration. 

Distribution 

It has a moderate distribution volume in the body, indicating that it can distribute to various tissues. 

Metabolism 

clebopride undergoes extensive hepatic metabolism through the cytochrome P450 enzyme system, primarily CYP3A4. Metabolites are excreted in the urine. 

Elimination and excretion 

clebopride and its metabolites are excreted primarily through the urine. 

Adminstartion

Administration: 

• Dosage: The recommended dose can vary depending on the patient’s age, weight, and the condition being treated. Always take the prescribed amount as directed by your healthcare provider. 
• Timing: clebopride is usually taken before meals. This helps optimize its prokinetic effects on the gastrointestinal tract. 
• Duration: The duration of treatment also depends on the underlying condition. Follow your healthcare provider’s instructions regarding how long you should take clebopride. 
• Storage: Store clebopride as directed on the medication label. Typically, it should be kept at room temperature away from light and moisture. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: clebopride 

Pronounced: (klee-boe-pride)  

Why do we use clebopride? 

• Gastroparesis: clebopride is often prescribed to alleviate the symptoms of gastroparesis, a condition characterized by delayed stomach emptying. It can help improve gastric motility and reduce symptoms like nausea, vomiting, early satiety, and abdominal discomfort. 
• Functional Gastrointestinal Disorders: clebopride may be used to manage symptoms in functional gastrointestinal disorders, such as irritable bowel syndrome (IBS). It can help alleviate abdominal pain and discomfort associated with these conditions. 
• Nausea and Vomiting: clebopride may be prescribed to control nausea and vomiting caused by various factors, including postoperative recovery, chemotherapy, or radiation therapy. 
• Acute and Chronic Gastritis: In some cases, clebopride may be used to manage gastritis, both acute and chronic. It can help relieve symptoms like indigestion, heartburn, and bloating.