DESCRIPTION
Pantoprazole -Pantoprazole is a proton pump inhibitor drug used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.Levosulpiride -Levosulpiride is a substituted benzamide antipsychotic, reported to be a selective antagonist of dopamine D2 receptor activity on both central and peripheral levels. It is an atypical neuroleptic and a prokinetic agent. Levosulpiride is also claimed to have mood elevating properties. Levosulpiride is used in the treatment of psychoses, particularly negative symptoms of schizophrenia, anxiety disorders, dysthymia, vertigo, dyspepsia, irritable bowel syndrome and premature ejaculation.
CATEGORIES
Pantoprazole -Anti-Ulcer Agents,Proton Pump Inhibitors.Levosulpiride -Antipsychotics.
CHEMICAL FORMULA
Pantoprazole -C16H15F2N3O4S.Levosulpiride -C15H23N3O4S.
COMPOSITION
Pantoprazole 40mg +Levosulpiride 75mg
INDICATION
Pantoprazole -Short-term (up to 16 weeks) treatment of erosive esophagitis. Levosulpiride -This medication is an antipsychotic and prokinetic agent, prescribed for dyspepsia, gastro-esophageal reflux disease, and irritable bowel syndrome.
PHARMACODYNAMICS
Pantoprazole -Pantoprazole is a substituted benzimidazole indicated for the short-term treatment (up to 16 weeks) in the healing and symptomatic relief of erosive esophagitis. Pantoprazole is a proton pump inhibitor (PPI) that suppresses the final step in gastric acid production. Levosulpiride -Sulpiride is a substituted benzamide derivative and a selective dopamine D2 antagonist with antipsychotic and antidepressant activity. Other benzamide derivatives include metoclopramide, tiapride, and sultopride.
MECHANISM
Pantoprazole -Pantoprazole is a proton pump inhibitor (PPI) that suppresses the final step in gastric acid production by forming a covalent bond to two sites of the (H+,K+ )- ATPase enzyme system at the secretory surface of the gastric parietal cell. This effect is dose- related and leads to inhibition of both basal and stimulated gastric acid secretion irrespective of the stimulus. Levosulpiride -In contrast to most other neuroleptics which block both dopamine D1 and D2 receptors, sulpiride is more selective and acts primarily as a dopamine D2 antagonist. Sulpiride appears to lack effects on norepinephrine, acetylcholine, serotonin, histamine, or gamma-aminobutyric acid (GABA) receptors.
ABSORPTION
Pantoprazole -Pantoprazole is well absorbed. It undergoes little first-pass metabolism resulting in an absolute bioavailability of approximately 77%.
VOLUME DISTRIBUTION
Pantoprazole -11.0 to 23.6 L.
METABOLISM
Pantoprazole -Pantoprazole is extensively metabolized in the liver through the cytochrome P450 (CYP) system. The main metabolic pathway is demethylation, by CYP2C19, with subsequent sulfation; other metabolic pathways include oxidation by CYP3A4. There is no evidence that any of the pantoprazole metabolites have significant pharmacologic activity.
ELIMINATION
Pantoprazole -After administration of a single intravenous dose of 14C-labeled pantoprazole to healthy, normal metabolizer subjects, approximately 71% of the dose was excreted in the urine with 18% excreted in the feces through biliary excretion.
HALF LIFE
Pantoprazole -1 hour.
TOXICITY
Pantoprazole -Single intravenous doses of pantoprazole at 378, 230, and 266 mg/kg (38, 46, and 177 times the recommended human dose based on body surface area) were lethal to mice, rats and dogs, respectively. The symptoms of toxicity included hypoactivity, ataxia, hunched sitting, limb-splay, lateral position, segregation, absence of ear reflex, and tremor. There is limited experience regarding cases of human overdosage, and treatment should be symptomatic and supportive.
FOOD INTERACTIONS
Pantoprazole -Take without regard to meals.
SIDE EFFECTS
Pantoprazole -Headache. Loose stools (diarrhea). Hip, spine, or wrist fractures may rarely happen.Levosulpiride -Amenorrhoea, gynaecomastia, changes in libido. Neuroleptic malignant syndrome.