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prokinetic agents battle

Domperidone vs Itopride vs Levosulpiride-A prokinetic Guide

  • A prokinetic agent is a drug that enhances gastrointestinal (GI) motility by increasing the frequency or strength of contractions in the stomach and intestines, without disrupting their natural rhythm.

Most commonly used prokinetic agent includes:

  • Domperidone
  • itopride
  • Levosulpiride

A number of times the choice between these prokinetic agent becomes difficult, its because that we aren’t aware of their whole clinical insights which is essential to be known, by every physician and pharmacist, before initiating any of these reagent in any patient. 

Here is the comprehensive yet Quick overview of clinical insights of prokinetic agents. 

So, let’s began the battle!!!

Drug (domperidone) Clinical Characteristics Nature Antidopaminergic Therapeutic Class Prokinetic/Antiemetic agents Mechanism of action Block dopamine receptors (D2 and D3) in periphery to produce prokinetic effect and in chemoreceptor trigger zone (CTZ lie just outside the BBB, regulates vomiting) to produce anti-emetic effect. It’s also increase the level of prolactin in the body. Indication Dyspepsia, indigestion, epigastric sense of fullness, epigastric pain, regurgitation, diabetic gastroparesis, nausea, and vomiting. Dosage forms availability Oral, injection, and rectal Dosage and administration guidelines Oral Adult Dose: for all indications 10-20mg orally 3-4 times a day 30 minutes before meal, maximum 80mg/day. Must reevaluate the need for continuation of treatment after every 4 weeks Precautions Renal impairment, Electrolyte disturbance, Elderly (>60yrs) Contraindications Prolactinoma, GI haemorrhage, perforation, obstruction, hepatic impairment or Cardiac Dysfunction Adverse drug reactions Ventricular arrhythmias, QT interval prolongation, Sudden cardiac death, Galactorrhoea, gynecomastia, or menstrual irregularities. Interactions Ketoconazole, ritonavir, erythromycin Facts ● Don’t Cross BBB so, less EPS. ● Not US FDA approved due to high cardiac toxicity. ● Approval in other countries is restricted to short durations and lowest effective doses, with warnings about ECG monitoring in high-risk patients. Common Brands ● Motilium/Pelton (TABLET+SYRUP) ● Motilium V/Domel/Pelton V (Domperidone Maleate) ● Domflash ORO (Oro dispersible tablet) ● Pelton-C (Domperidone + Cinnarizine)
ADVERSE EFFECTS OF DOMPERIDONE
Drug (ITOPRIDE) Clinical Characteristics Nature Antidopaminergic + Cholinergic agent (decreases AchE) Therapeutic Class Prokinetic/Antiemetic agents Mechanism of action Itopride is basically a dopamine D2 receptor antagonist which by antagonizing D2 receptors, also decreases the inhibitory effects of dopamine on acetylcholine (Ach) release. It also inhibits the enzyme AchE (that break down Ach) which increases the concentration of Ach. Thus, the overall result of the itopride administration is boost up in the level of acetylcholine (Ach) that leads toward the promotion of gastric motility, increases the lower oesophageal sphincter pressure, enhances gastric emptying and improves gastro-duodenal coordination. This dual mode of action of Itopride is exceptional, making it a unique choice among other prokinetic agents. Indication Functional dyspepsia such as nausea and vomiting, non-ulcer dyspepsia (chronic gastritis), sensation of bloating, early satiety, upper abdominal pain, or discomfort, anorexia, and heart burn Dosage forms availability Tablet (50mg or 150mg) and Capsules (150mg) Dosage and administration guidelines Oral Adult Dose: 50mg orally 3 times a day 30 minutes before meal, or 150mg OD (once daily) 30 minutes before meal maximum 150mg/day. Not recommended in children. Precautions As it increases Ach level thus can causes cholinergic effects Contraindications GI haemorrhage, perforation, obstruction, or in cases where GI motility is harmful. Adverse drug reactions Diarrhea, Constipation, increase saliva, nausea, dizziness, headache, tremor, abdominal pain Interactions Anticholinergic Drugs Facts ● Don’t Cross BBB so, less EPS. Itopride is hydrophilic and is a substrate of P-glycoprotein (P-gp), which actively pumps it out of the CNS. ● Not US FDA approved due to lack of manufacturer’s interest ● Approved in other countries for the above-mentioned indication. ● No Cardiac Toxicity. Common Brands ● ITP 50mg OR ITP OD (150mg) ● Emptin-OD 150mg and Emptin 50mg ● Ganaton 50mg and Ganaton OD 150mg ● Tespral 50mg
ADVERSE EFFECTS OF ITOPRIDE
Drug (Levosulpiride ) Clinical Characteristics Drug category Antidopaminergic (Antipsychotic due to BBB penetration) Therapeutic Class Prokinetic/Antipsychotic Mechanism of action Levosulpiride acts as a selective antagonist of dopamine D₂ receptors, both centrally (in the brain) and peripherally (in the gastrointestinal tract) also act on CTZ, thus ● Produces antipsychotic effect, Increases prolactin levels, potential EPS ● increases the acetylcholine level and promote GI motility. ● produces anti-emetic effect Indication Dyspepsia, Nausea, vomiting, vertigo, Inflammatory bowel syndrome (IBS), Schizophrenia, Tourette’s Syndrome, depression with or without anxiety Dosage forms availability Tablet (25mg and 50mg) and Capsules (25,50 and 100mg) Dosage and administration guidelines Oral Adult Dose: 50mg -200mg daily However the dose for CNS disorder may vary depending upon condition: Schizophrenia: 3-5mg/kg daily to children over 14 yr of age. Adults: Initially, 200-400mg twice daily, Maximum 1.2g BD if necessary, especially in the case of patients with positive symptoms and Up to 800mg daily in the case of patient with negative symptoms In case of patient with neither predominating, are given usual dose of 400-600mg bd. Tourette’s Syndrome: Adolescents14-18 yr: 200-400mg bd. Precautions Should be careful while giving it to manic or hypomanic patient, as it can exacerbate the symptoms in such patients. Contraindications Comatose, CNS depression, pheochromocytoma Adverse drug reactions Extrapyramidal effects, cardiovascular effects, hypotension, sleep changes, over stimulation and agitation Interactions Anticholinergic Drugs, Alcohol, CNS depressants, guanethidine, antacids, NSAIDs Facts ● Cross BBB have EPS. ● Not US FDA approved due to lack of manufacturer’s interest ● Approved in other countries for the above-mentioned indication. Common Brands ● Sulvorid 25 and 50mg ● Motivo 25 and 50mg ● Lusell 25 and 100mg ● Scipride 50mg ● Sowel 25, 50 and 100mg
ADVERSE EFFECTS OF LEVOSULPIRIDE

So, what we get from the above clinical pearls is that one size doesn’t fits all.

Like if we see the safety profile of these prokinetic agents in patients suffering from cardiovascular disease we come to know that itopride has a good safety profile in cardiovascular patients. while domperidone can causes severe cardiac effect likewise levosulpiride also has negative effects on heart. which helps us choose the right medicine for the heart patients.

Similarly the decision to choose different prokinetic agents in different clinical scenario has been easy after having this comparison.

Unlock The Pearls of All Medcines to be an Expert!

References:

DrugBank. (n.d.). Itopride. DrugBank Online. Retrieved June 22, 2025, from https://go.drugbank.com/drugs/DB09217

PharmaGuide Publications. (2019). PharmaGuide: Pakistan drug directory (26th ed.). PharmaGuide Publications.

DrugBank. (n.d.). Domperidone. DrugBank Online. Retrieved June 22, 2025, from https://go.drugbank.com/drugs/DB01184

DrugBank. (n.d.). Levosulpiride. DrugBank Online. Retrieved June 22, 2025, from https://go.drugbank.com/drugs/DB12855

 

Disclaimer:

This information is for educational purposes only and is not intended to replace professional medical advice. Always consult your doctor or pharmacist before starting or changing any medication.

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