Indications
- Healing of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD).
- Maintenance of Healing of Erosive or Ulcerative Gastroesophageal Reflux Disease (GERD)
- Healing of Duodenal Ulcers
- Treatment of Pathological Hypersecretory Conditions, Including Zollinger-Ellison Syndrome.
- Irritable bowel syndrome
- Chronic Gastritis.
Mechanism of Action
Levosulpiride is more selective and acts primarily as a dopamine D2 antagonist. The prokinetic effect of Levosulpiride is mediated through the blockade of enteric (neuronal and muscular) inhibitory dopamine D2 receptors. Results also show that levosulpiride also acts as a moderate agonist at the 5-HT receptor. The serotonergic (5-HT4) component of Levosulpiride may enhance its therapeutic efficacy in gastrointestinal disorders. This property, together with antagonism at D2 receptors, may contribute to its gastrointestinal prokinetic effect.
Drug Interactions
Association with psycho pharmaceutical drugs require special precautions and monitoring to avoid undesired and unexpected effects because of interactions. High doses can produce hyperprolactinemia, therefore special control during treatment is advised.
Rabeprazole produces a profound increase in gastric pH and may affect drugs whose absorption is pH dependant, such as ketoconazole and digoxin. Concomitant administration decreases ketoconazole levels by 33% and increases digoxin trough levels by up to 22%.
Pharmacology
Pharmacodynamics:Rabeprazole prevents the production of acid in the stomach. It reduces symptoms and prevents injury to the esophagus or stomach in patients with gastroesophageal reflux disease (GERD) or ulcers. Rabeprazole is also useful in conditions that produce too much stomach acid such as Zollinger-Ellison syndrome. Levosulpiride acts as prokinetic agent.
Pharmacokinetics
Rabeprazole:Absorption: Absolute bioavailability is approximately 52%.
Route of Elimination:Following a single 20 mg oral dose of 14C-labeled rabeprazole, Approximately 90% of the drug was eliminated in the urine, primarily as thioether carboxylic acid; itslucuronide, and mercapturic acid metabolites.
Levosulpiride:Absorption: Oral bioavailability is about 30%; peak plasma concentrations after about 3hr.
Route of Elimination:Mainly via urine. Plasma half-life: 9.7 hr (oral); 4.3 hr (IV).
Side Effects
Contraindications
The drug should be used cautiously in pregnancy (only when it is expected to benefit the mother more than the possibility of risking the fetus).
The drug is known to be secreted in breast milk, so, its use should be restricted in breastfeeding women.
Warning & Precautions
The drug should be used cautiously in pregnancy (only when it is expected to benefit the mother more than the possibility of risking the fetus).
The drug is known to be secreted in breast milk, so, its use should be restricted in breastfeeding women.