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.Itopride-Itopride is a dopamine D2 antagonist with acetylcholinesterase inhibitory actions.
CATEGORIES
Pantoprazole-Anti-Ulcer Agents,Proton Pump Inhibitors.Itopride-GIT Regulators & Anti-Inflammatories.
CHEMICAL FORMULA
Pantoprazole-C16H15F2N3O4S.Itopride-C20H26N2O4.
COMPOSITION
Pantoprazole 40mg + Itopride 150mg
INDICATION
Pantoprazole-Short-term (up to 16 weeks) treatment of erosive esophagitis. Itopride-Investigated for use/treatment in gastrointestinal diseases and disorders (miscellaneous).
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.
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. Itopride-Itopride has anticholinesterase (AchE) activity as well as dopamine D2 receptor antagonistic activity. It is well established that M3 receptors exist on the smooth muscle layer throughout the gut and acetylcholine (ACh) released from enteric nerve endings stimulates the contraction of smooth muscle through M3 receptors. The enzyme AChE hydrolyses the released ACh, inactivates it and thus inhibits the gastric motility leading to various digestive disorders. Besides ACh, dopamine is present in significant amounts in the gastrointestinal tract and has several inhibitory effects on gastrointestinal motility, including reduction of lower esophageal sphincter and intragastric pressure. These effects appear to result from suppression of ACh release from the myenteric motor neurons and are mediated by the D2 subtype of dopamine receptors. Itopride, by virtue of its dopamine D2 receptor antagonism, removes the inhibitory effects on Ach release. It also inhibits the enzyme AchE which prevents the degradation of ACh. The net effect is an increase in ACh concentration, which in turn, promotes gastric motility, increases the lower esophageal sphincter pressure, accelerates gastric emptying and improves gastro-duodenal coordination. This dual mode of action of Itopride is unique and different from the actions of other prokinetic agents available in the market.
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. Itopride-Flavin-containing monooxygenase (FMO) is involved in N-oxygenation, the major metabolic pathway of itopride (PMID: 10997945).
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.Itopride-Rash, diarrhoea, constipation, abdominal pain, headache, sleeping disorders, dizziness, galactorrhea, gynecomastia.