Diocid-DSR
Diocid-DSR Uses, Dosage, Side Effects, Food Interaction and all others data.
Domperidone is dopamine receptor (D2) antagonist which selectively inhibits dopamine at the D2 receptor. It acts principally at receptors in the chemoreceptor trigger zone (CTZ) and also at receptors in the stomach.
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.
Omeprazole belongs to a class of antisecretory compounds, the substituted benzimidazoles, that suppress gastric acid secretion by specific inhibition of the H+/K+ ATPase enzyme system at the secretory surface of the gastric parietal cell. Because this enzyme system is regarded as the acid (proton) pump within the gastric mucosa, omeprazole has been characterized as a gastric acid-pump inhibitor, in that it blocks the final step of acid production. This effect is dose-related and leads to inhibition of both basal and stimulated acid secretion irrespective of the stimulus.
Clinical advantage of omeprazole mups tablet compared to conventional modified-release omeprazole tablets and pellet-filled omeprazole capsules:
Ensures greater bioavailabilityEnsures uniform emptying of micro pellets from stomach into small intestine facilitates rapid dissolution of enteric coating and drug release resulting in early Tmax and Cmax (peak time and peak plasma concentration)Ensures lesser possibility of dose dumpingIs a combination of fast acting and sustained actionEnsures uniform drug releaseOnce daily dosingEnsures lesser chance of localized irritationEnsures better and more uniform drug absorptionBetter than capsules in reducing the esophageal residence timeMinimizes fluctuation in plasma concentration of drugEffects on gastric acid secretion
This drug decreases gastric acid secretion . After oral administration, the onset of the antisecretory effect of omeprazole is usually achieved within one hour, with the maximum effect occurring by 2 hours after administration. The inhibitory effect of omeprazole on acid secretion increases with repeated once-daily dosing, reaching a plateau after four days .
Trade Name | Diocid-DSR |
Generic | Domperidone + Omeprazole |
Type | |
Therapeutic Class | |
Manufacturer | |
Available Country | India |
Last Updated: | September 19, 2023 at 7:00 am |
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Uses
Stimulation of gut motility in-
- Non-ulcer dyspepsia
- Oesophageal reflux, reflux oesophagitis and gastritis
- Diabetic gastroparesis
- Functional dyspepsia
- Speeding barium transit in follow through radiological studies
Prevention and symptomatic relief of acute nausea and vomiting from any cause including cytotoxic therapy, radiotherapy and antiparkinsonism therapy.
In the prophylactic treatment of migraine.
Each film coated MUPS tablet contains 20 mg Omeprazole enteric coated micro pellets
Omeprazole (Multiple-Unit Pellet System) is indixated in-
- Duodenal and Gastric ulcers
- NSAID-induced gastric and duodenal ulcers
- Reflux Oesophagitis
- GERD (Gastroesophageal Reflux Disease)
- Eradication of H. pylori with appropriate antibiotics
- Zollinger-Ellison Syndrome
MUPS is abbreviation for Multiple-Unit Pellet System. However, from pharmaceutical industry and research perspective, the term in general refers to MUPS compacted into tablets. Thus, the resulting tablets prepared by compaction of modified release coated multiparticulates or pellets are called as MUPS. It is the more recent and challenging technology that combines the advantages of both tablets and pellet filled capsules in one dosage form.
MUPS ensure rapid and uniform gastric emptying and subsequently uniform drug dissolution of pellets in the gastrointestinal tract due to their small size and larger surface, uniform drug absorption is facilitated which results in consistent and controlled pharmacological action.
A further reduction in inter- and intra-subject variability in drug absorption and clinical response is facilitated since the number of pellets per MUPS dosage form is much more than a conventional pellet-filled capsule and possibility of dose dumping(in stomach) and incomplete drug release is further minimized.
Diocid-DSR is also used to associated treatment for these conditions: Diabetic Gastroparesis, Dyspepsia, Erosive Esophagitis, Gastrointestinal Symptoms, Non-erosive Reflux Esophagitis Disease (NERD), Upper gastrointestinal motility disordersAnkylosing Spondylitis (AS), Duodenal Ulcer, Erosive Esophagitis, Gastric Ulcer, Gastro-esophageal Reflux Disease (GERD), Healing, Heartburn, Helicobacter Pylori Infection, NSAID Associated Gastric Ulcers, Osteoarthritis (OA), Rheumatoid Arthritis, Zollinger-Ellison Syndrome, Hypersecretory conditions, Multiple endocrine adenomas
How Diocid-DSR works
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
Hydrochloric acid (HCl) secretion into the gastric lumen is a process regulated mainly by the H(+)/K(+)-ATPase of the proton pump , expressed in high quantities by the parietal cells of the stomach. ATPase is an enzyme on the parietal cell membrane that facilitates hydrogen and potassium exchange through the cell, which normally results in the extrusion of potassium and formation of HCl (gastric acid) .
Omeprazole is a member of a class of antisecretory compounds, the substituted benzimidazoles, that stop gastric acid secretion by selective inhibition of the H+/K+ ATPase enzyme system. Proton-pump inhibitors such as omeprazole bind covalently to cysteine residues via disulfide bridges on the alpha subunit of the H+/K+ ATPase pump, inhibiting gastric acid secretion for up to 36 hours . This antisecretory effect is dose-related and leads to the inhibition of both basal and stimulated acid secretion, regardless of the stimulus .
Mechanism of H. pylori eradication
Peptic ulcer disease (PUD) is frequently associated with Helicobacter pylori bacterial infection (NSAIDs) . The treatment of H. pylori infection may include the addition of omeprazole or other proton pump inhibitors as part of the treatment regimen , . H. pylori replicates most effectively at a neutral pH . Acid inhibition in H. pylori eradication therapy, including proton-pump inhibitors such as omeprazole, raises gastric pH, discouraging the growth of H.pylori . It is generally believed that proton pump inhibitors inhibit the urease enzyme, which increases the pathogenesis of H. pylori in gastric-acid related conditions .
Dosage
Diocid-DSR dosage
Adults: 10 - 20 mg every 4 - 8 hours daily
Children: 0.2 - 0.4 mg/kg every 4 - 8 hours daily.
Domperidone tablet and suspension should be taken 15 - 30 minutes before a meal. For acute nausea and vomiting, maximum period of treatment is 12 weeks.
Adult:
- GERD (Gastroesophageal Reflux Disease):20 mg Once daily for 4 weeks
- Gastric ulcer:20 mg Once daily for 4-8 weeks; in severe cases Twice daily
- Duodenal ulcer:20 mg Once daily for 2-4 weeks; in severe cases Twice daily
- NSAID-induced ulceration:20 mg Once daily for 4-8 weeks
- Reflux esophagitis:20 mg Once daily for 4-8 weeks; in severe cases Twice daily
- H. pylori eradication (Omeprazole MUPS tablet with Amoxicillin and Clarithromycin or Metronidazole):20 mg Twice daily for 1 week
- Zollinger-Ellison Syndrome:60 mg Once daily; Usual maintenance, 20-120mg daily
Children:
- Acid regurgitation in GERD (Gastroesophageal Reflux Disease):20 mg Once daily for 2-4 week
- Reflux esophagitis:20 mg Once daily for 4-8 weeks
Swallow the tablet whole with a glass of water. The tablet must not be chewed or crushed. OR
If the patients have trouble swallowing the tablets, put the tablet into a glass of water (Do not use other liquids). Stir the preparation until the tablets disintegrate. Then drink the liquid within 30 minutes. Stir the mixture just always before drinking.
Side Effects
Domperidone may produce hyperprolactinemia which may cause galactorrhea & breast enlargement, soreness and reduced libido. It may rarely cause dry mouth, thirst, headache, nervousness, drowsiness, diarrhea, skin rash and itching.
Toxicity
Side effects include galactorrhea, gynecomastia, or menstrual irregularities.
Oral acute (LD50): 4000 mg/kg (mouse), 2210 mg/kg (rat) .
Overdose
Symptoms of overdose include confusion, drowsiness, blurred vision, tachycardia, nausea, diaphoresis, flushing, headache, and dry mouth.
Carcinogenesis and mutagenesis
In 24-month studies in rats, a dose-related significant increase in gastric carcinoid tumors and ECL cell hyperplasia was seen in male and female animals. Carcinoid tumors have also been found in rats treated with a fundectomy or long-term treatment with other proton pump inhibitors, or high doses of H2-receptor antagonists .
Omeprazole showed positive clastogenic effects in an in vitro human lymphocyte chromosomal aberration study, in one of two in vivo mouse micronucleus tests, and in an in vivo bone marrow cell chromosomal aberration test. Omeprazole tested negative in the in vitro Ames test, an in vitro mouse lymphoma cell forward mutation assay, and an in vivo rat liver DNA damage assay .
The use in breastfeeding
Limited data indicate that omeprazole may be present in human milk. There is currently no information on the effects of omeprazole on the breastfed infant or production of milk. The benefits of breastfeeding should be considered along with the level of need for omeprazole and any potential adverse effects on the breastfed infant from omeprazole .
Effects on fertility
Effects of omeprazole at oral doses up to 138 mg/kg/day in rats (about 34 times an oral human dose) was found to have no impact on fertility and reproductive performance .
Precaution
Domperidone should be used with absolute caution in case of children because there may be an increased risk of extra-pyramidal reactions in young children because of an incompletely developed blood brain barrier.
Omeprazole tablet should be used carefully if the patient has severe liver dysfunction and severe renal impairment.
Interaction
Domperidone may reduce the hypoprolactinaemic effect of bromocriptine. Anti-muscarinics and opioid analgesics may antagonize the action of Domperidone on gastrointestinal function.
Omeprazole is metabolized through CYP2C19 . When starting or stopping treatment with Omeprazole should be taken into account potential interactions with medicines which are CYP2C19 metabolized.
Volume of Distribution
Approximately 0.3 L/kg, corresponding to the volume of extracellular water .
Elimination Route
Omeprazole delayed-release capsules contain an enteric-coated granule formulation of omeprazole (because omeprazole is acid-labile), so that absorption of omeprazole begins only after the granules exit the stomach .
Absorption of omeprazole occurs rapidly, with peak plasma concentrations of omeprazole achieved within 0.5-3.5 hours .
Absolute bioavailability (compared with intravenous administration) is approximately 30-40% at doses of 20-40 mg, largely due to pre-systemic metabolism. The bioavailability of omeprazole increases slightly upon repeated administration of omeprazole delayed-release capsules .
Half Life
7 hours
0.5-1 hour (healthy subjects, delayed-release capsule)
Approximately 3 hours (hepatic impairment)
Clearance
Healthy subject (delayed release capsule), total body clearance 500 - 600 mL/min
Geriatric plasma clearance: 250 mL/min
Hepatic impairment plasma clearance: 70 mL/min
Elimination Route
After a single dose oral dose of a buffered solution of omeprazole, negligible (if any) amounts of unchanged drug were excreted in urine. Most of the dose (about 77%) was eliminated in urine as at least six different metabolites. Two metabolites were identified as hydroxyomeprazole and the corresponding carboxylic acid. The remainder of the dose was found in the feces. This suggests significant biliary excretion of omeprazole metabolites. Three metabolites have been identified in the plasma, the sulfide and sulfone derivatives of omeprazole, and hydroxyomeprazole. These metabolites possess minimal or no antisecretory activity .
Pregnancy & Breastfeeding use
Use in pregnancy: The safety of this drug has not been established for pregnant women. So it is not recommended during pregnancy.
Use in lactation: Domperidone may precipitate galactorrhea and improve postnatal lactation, which is secreted in breast milk but in very small quantities insufficient to be considered harmful.
Not known to be harmful. Omeprazole can be used during pregnancy. Omeprazole is excreted in breast milk but is not likely to influence the child when therapeutic doses are used.
Contraindication
Domperidone is contraindicated to the patients who have hypersensitivity to this drug and in case of neonates.
Omeprazole is contraindicated in those patients who have known hypersensitivity to any other components of the formulation.
Acute Overdose
Overdose has been reported primarily in infants and children. Symptoms of overdosage may include disorientation, somnolence and extrapyramidal reactions. There is no specific antidote to domperidone, but in the event of overdose, the administration of activated charcoal may be useful. Anticholinergics, antiparkinson drugs may be useful in controlling extrapyramidal reactions. The patient should be observed closely and supportive measures employed.
Storage Condition
Store in a cool dry place protected from light. Keep out of reach of children.
Store in a cool (below 30° C) and dry place, protected from light and moisture.
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