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. Domperidone – A specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.
CATEGORIES
Pantoprazole – Anti-Ulcer Agents,Proton Pump Inhibitors.Domperidone – Antiemetics, GIT Regulators & Anti-Inflammatories .
CHEMICAL FORMULA
Pantoprazole – C16H15F2N3O4S,Domperidone – C22H24ClN5O2.
COMPOSITION
Pantoprazole 40mg+Domperidone30mg
INDICATION
Pantoprazole – Short-term (up to 16 weeks) treatment of erosive esophagitis.Domperidone -For management of dyspepsia, heartburn, epigastric pain, nausea, and vomiting.
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.Domperidone – Domperidone is a specific blocker of dopamine receptors. It speeds gastrointestinal peristalsis, causes prolactin release, and is used as antiemetic and tool in the study of dopaminergic mechanisms.
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.Domperidone – Domperidone acts as a gastrointestinal emptying (delayed) adjunct and peristaltic stimulant. The gastroprokinetic properties of domperidone are related to its peripheral dopamine receptor blocking properties. Domperidone facilitates gastric emptying and decreases small bowel transit time by increasing esophageal and gastric peristalsis and by lowering esophageal sphincter pressure. Antiemetic: The antiemetic properties of domperidone are related to its dopamine receptor blocking activity at both the chemoreceptor trigger zone and at the gastric level. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which – among others – regulates nausea and vomiting .
ABSORPTION
Pantoprazole – Pantoprazole is well absorbed. It undergoes little first-pass metabolism resulting in an absolute bioavailability of approximately 77%.Domperidone – Fast.
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. Domperidone – Hepatic and intestinal (first-pass) .
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. Domperidone – Breast milk, renal.
HALF LIFE
Pantoprazole – 1 hour.Domperidone – 7 hours.
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. Domperidone – Side effects include galactorrhea, gynecomastia, or menstrual irregularities.
FOOD INTERACTIONS
avoid alcohol
SIDE EFFECTS
Pantoprazole – Headache. Loose stools (diarrhea). Hip, spine, or wrist fractures may rarely happen.Domperidone – Headache. Dry mouth. Good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. See a dentist often