Mepazole
Mepazole Uses, Dosage, Side Effects, Food Interaction and all others data.
Mepazole 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 | Mepazole |
| Availability | Rx and/or OTC |
| Generic | Omeprazole |
| Omeprazole Other Names | OMEP, Omeprazol, Omeprazole, Omeprazolum |
| Related Drugs | amoxicillin, famotidine, pantoprazole, metronidazole, Nexium, Pepcid, Protonix, esomeprazole, sucralfate, Prilosec |
| Type | |
| Formula | C17H19N3O3S |
| Weight | Average: 345.416 Monoisotopic: 345.114712179 |
| Protein binding | Approximately 95% bound to human plasma proteins . |
| Groups | Approved, Investigational, Vet approved |
| Therapeutic Class | Proton Pump Inhibitor |
| Manufacturer | |
| Available Country | Philippines |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Each film coated MUPS tablet contains 20 mg Mepazole enteric coated micro pellets
Mepazole (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.
Mepazole is also used to associated treatment for these conditions: Ankylosing 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 Mepazole works
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) .
Mepazole 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
Mepazole dosage
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 (Mepazole 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.
Toxicity
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 .
Mepazole 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. Mepazole 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
Mepazole tablet should be used carefully if the patient has severe liver dysfunction and severe renal impairment.
Interaction
Mepazole is metabolized through CYP2C19 . When starting or stopping treatment with Mepazole should be taken into account potential interactions with medicines which are CYP2C19 metabolized.
Food Interaction
- Take before a meal. Allow 30-60 minutes before a meal.
Mepazole Drug Interaction
Moderate: atorvastatin, levothyroxine, alprazolamMinor: aspirin, aspirin, duloxetine, cyanocobalaminUnknown: diphenhydramine, omega-3 polyunsaturated fatty acids, fluticasone nasal, pregabalin, metoprolol, metoprolol, acetaminophen, albuterol, montelukast, acetaminophen, ascorbic acid, cholecalciferol, cetirizine
Mepazole Disease Interaction
Volume of Distribution
Approximately 0.3 L/kg, corresponding to the volume of extracellular water .
Elimination Route
Mepazole 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
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
Not known to be harmful. Mepazole can be used during pregnancy. Mepazole is excreted in breast milk but is not likely to influence the child when therapeutic doses are used.
Contraindication
Mepazole is contraindicated in those patients who have known hypersensitivity to any other components of the formulation.
Storage Condition
Store in a cool (below 30° C) and dry place, protected from light and moisture.
Innovators Monograph
You find simplified version here Mepazole
Mepazole contains Omeprazole see full prescribing information from innovator Mepazole Monograph, Mepazole MSDS, Mepazole FDA label
FAQ
What is Mepazole used for?
Mepazole is used to treat conditions in which the stomach produces too much acid such as Zollinger-Ellison syndrome in adults. Prescription Mepazole is used to allow the esophagus to heal and prevent further damage to the esophagus in adults and children 1 year of age and older with GERD.
What are the side effects of taking Mepazole?
Mepazole side effects are Rare:
- Back, leg, or stomach pain
- bleeding or crusting sores on the lips
- blisters
- bloody or cloudy urine
- chills
- continuing ulcers or sores in the mouth
- difficult, burning, or painful urination
- fever
- frequent urge to urinate
- general feeling of discomfort or illness
- itching, skin rash
- joint pain
- loss of appetite
- muscle aches or cramps
- pain
- red or irritated eyes
- redness, tenderness, itching, burning, or peeling of the skin
- sore throat
- sores, ulcers, or white spots on the lips, in the mouth, or on the genitals
- unusual bleeding or bruising
- unusual tiredness or weakness
How long should I take Mepazole?
Mepazole is a delayed-release 20mg tablet, taken once a day (every 24 hours) for 14 days before eating. You should not take it for more than 14 days or repeat a 14-day course more often than every 4 months unless directed by a doctor. Do not crush, break, or chew the tablet.
Is it bad to take Mepazole every day?
Sometimes you might need to take it for longer, even for many years. Some people do not need to take Mepazole every day and take it only when they have symptoms. Once you feel better (often after a few days or weeks), you can stop taking it. But taking Mepazole in this way is not suitable for everyone.
What foods neutralize stomach acid?
Foods that may help reduce your symptoms
- Vegetables. Vegetables are naturally low in fat and sugar, and they help reduce stomach acid.
- Ginger.
- Oatmeal.
- Noncitrus fruits.
- Lean meats and seafood.
- Egg whites.
- Healthy fats.
How long before a meal should you take Mepazole?
Take Mepazole powder for oral suspension on an empty stomach at least 1 hour before a meal.
What can I take instead of Mepazole?
These include proton pump inhibitors such as esomeprazole, omeprazole, pantoprazole and lansoprazole. The others are antacids such as Maalox, Mylanta and Tums; and H2 (histamine) receptor antagonists such as famotidine, and cimetidine.
Can Mepazole make me gassy?
Common side effects may include: stomach pain, gas; nausea, vomiting, diarrhea; or. headache.
Why should not lie down after taking Mepazole?
Do not lie down immediately after taking medicine, to make sure the pills have gone through the esophagus into the stomach. Notify your healthcare provider if you experience painful swallowing or feel that the medicine is sticking in your throat.
Why is Mepazole taken before meals?
When therapy with Mepazole or lansop- razole is indicated, medication should be taken before a meal for optimal control of daytime gastric acidity. the parietal cell is maximally stimulated as it is after a meal.
How do I cure GERD permanently?
Try to:
- Maintain a healthy weight.
- Stop smoking.
- Elevate the head of your bed.
- Don't lie down after a meal.
- Eat food slowly and chew thoroughly.
- Avoid foods and drinks that trigger reflux. ..
- Avoid tight-fitting clothing.
Is it safe to take Mepazole long term?
If you take Mepazole for more than 3 months, the levels of magnesium in your blood may fall.
Low magnesium can make you feel tired, confused, dizzy and cause muscle twitches, shakiness and an irregular heartbeat. If you get any of these symptoms, tell your doctor.
Taking Mepazole for more than a year may increase your chances of certain side effects, including:
- bone fractures
- gut infections
- vitamin B12 deficiency – symptoms include feeling very tired, a sore and red tongue, mouth ulcers and pins and needles
If you take Mepazole for longer than 1 year, your doctor will regularly check your health to see if you should carry on taking it.
Should I stop taking Mepazole if I have diarrhea?
Stop using Mepazole and call your doctor at once if you have: severe stomach pain, diarrhea that is watery or bloody; new or unusual pain in your wrist, thigh, hip, or back; seizure (convulsions);
How long does it take for stomach acid to return to normal?
For most people acid levels return to normal within one to two weeks.
Are there any side effects when I stop taking Mepazole?
When Mepazole is stopped, a common side effect is rebound acid secretion, where the acid secretion in your stomach increases significantly. This should return to normal within 2 weeks.
Is Mepazole safe in pregnancy?
Usually, Mepazole is safe to take during pregnancy.
Is Mepazole safe during breastfeeding?
Usually, omeprazole is safe to take during breastfeeding.
How does Mepazole work?
Mepazole (Omeprazole) is a type of medicine called a proton pump inhibitor (PPI). Proton pumps are tiny substances in the lining of the stomach that help it make acid to digest food. Omeprazole prevents proton pumps working properly. This reduces the amount of acid the stomach makes.
When will I feel better after taking Mepazole?
You should start to feel better within 2 to 3 days. It may take up to 4 weeks for Mepazole to work properly, so you may still have some acid symptoms during this time. If you're self-treating, tell your doctor if you feel no better after taking Mepazole for 2 weeks. They may want to do tests or change you to a different medicine.
Can I take painkillers with Mepazole?
Yes, it's safe to take painkillers such as paracetamol or ibuprofen at the same time as Mepazole. It's best to take ibuprofen with, or just after, a meal so it does not upset your stomach.
Are there other medicines like Mepazole?
There are 4 other medicines that are similar to Mepazole. They are:
- lansoprazole
- esomeprazole
- pantoprazole
- rabeprazole
Can I take Mepazole with an antacid?
You can take Mepazole with an antacid (for example, Gaviscon) if you need to, but leave a gap of 2 hours between them.
Will Mepazole affect my fertility?
There's no clear evidence to suggest that taking Mepazole will reduce fertility in either men or women. But speak to a pharmacist or your doctor if you're trying to get pregnant. They may want to review your treatment.
Will Mepazole affect my contraception?
Mepazole does not affect any type of regular contraception, including the combined pill. But if Mepazole makes you sick (vomit), your contraceptive pills may not protect you from pregnancy. If this happens, follow the instructions in the leaflet that comes with your contraceptive pills.
