Jiracek-20 Davipharm medicine treats gastric ulcer, gastroesophageal reflux
Dosage form Box of 3 blisters x 10 tablets
Specifications Esomeprazole
Ingredient
| Composition information | Content |
| Esomeprazole | 20mg |
Uses
indicated
Adults:
Gastroesophageal reflux disease (GERD)
Patients need to continue treating with nonsteroidal anti -inflammatory drugs (NSAIDs):
Treatment of Zollinger-Elison syndrome.
Children ≥ 12 years:
Gastroesophageal reflux disease (GERD)
Pharmacology
Pharmacological group: Aggress inhibitors of the gastric acid belonging to the Proton pump inhibitor group.
ATC code: A02BC05.
Esomeprazol is the S isomorphic form of omeprazol, used similarly to Omeprazol in the treatment of gastric ulcer - duodenum and gastroesophageal reflux disease and Zollinger -Elison syndrome.
Esomeprazol is a weak base, attached to H+/K+-Aatpase (also known as proton pump) in the cell wall of the stomach, inactivating this enzyme system, preventing the final step of the excretion of hydrochloric acid in the stomach. Therefore, Esomeprazol has the effect of inhibiting the stomach secretion of basic acid and even when stimulated by any agent. The drug works strongly, lasting.
Proton pump inhibitors have an inhibitory but not except for Helicobacter pylori, so it is necessary to coordinate with antibiotics (such as amoxicillin, tetracycline and clarithromycin) to effectively deduct this bacteria.
Pharmacokinetics
absorption
Esomeprazol is an unstable substance in an acidic environment and is taken orally in the form of a tablet in the intestine. In Vivo, Esomeprazol is transferred to negligible r-Isomer isomer. Esomeprazol absorbs quickly after drinking, promoting within 1 hour, reaching the highest concentration in plasma after 1-2 hours. Esomeprazol's bioavailability increases according to the dose and when used to repeat: reaching about 50% after the single dose of 20 mg, increasing to 68% when the dose is repeated daily; 64% when using only 40 mg and up to 89% after daily dose use. Food slows down and reduces the absorption of Esomeprazol, but does not change the effect of the effect of the drug on the concentration of acid in the stomach. The area under the curve (AUC) after taking a single dose Esomeprazol 40 mg at meals compared to the hunger decreased from 43% to 53%. Therefore, Esomeprazol should drink at least 1 hour before meals.
Distribution
About 97% Esomeprazol attaches to plasma proteins. The volume of distribution when the drug concentration is stable in healthy volunteers of 0.22 l/kg body weight.
Metabolism
The main metabolic drug in the liver thanks to the cytochrom P450 enzyme system, isenzyme CYP2C19 into hydroxy and desmethyl metabolites is no longer active, the rest is converted through isoenzyme CYP3A4 into esomeprazol sulfon. When used repeated, initially metabolized through the liver and the clearance of the drug reduced, possibly due to the inhibited ISOENZYM CYP2C19. However, there is no phenomenon of accumulation of drugs when used once a day.
Elimination
The total removal of the drug in plasma is about 17 l/hour after taking the only dose and about 9 l/hour after taking the dose repeated. Selling time for plasma is about 1.3 hours. Esomeprazol is completely eliminated from the plasma between the doses and does not cause accumulation when taking the dose repeated once a day. The main metabolites of Esomeprazol does not affect stomach acid secretion. About 80% of oral doses are eliminated in the form of non -active metabolites in the urine, the rest is eliminated in the feces. Less than 1% of the drug is eliminated in urine.
Linear/non -linear:
Esomeprazol'spharmacokinetics has been studied with a dose of up to 40 mg x 2 times/day.
The area under the concentration curve over time (AUC) increases when using the repeated dose esomeprazol. This increase depends on the dose and leads to an increase in AUC at a larger rate than the dose increase after the dose is repeated. This time and dosage dependence is due to the first metabolism through the liver and the whole body clearance, possibly due to the effect of inhibiting CYP2C19 of Esomeprazol and/or its sulphon metabolism.
pharmacokinetics on special subjects
Poor metabolic people:
In some people because of the lack of CYP2C19 due to genetics (15-20% of Asians), they should slow down the metabolism of Esomeprazol. In these people, Esomeprazol's metabolism is mainly catalyzed by CYP3A4 enzyme. In a stable state, the AUC value in people deficient in CYP2C19 enzyme increases about 2 times compared to people with enough enzymes.
Sex:
After taking the single dose of Esomeprazol 40 mg, AUC in women is about 30%higher than men.
There is no difference between gender when using daily dose.
Hepatic failure:
Esomeprazol metabolism in people with medium and mild liver dysfunction may decrease. The metabolic rate decreases in patients with severe liver dysfunction that doubles the AUC of Esomeprazol. Therefore, do not use more than 20 mg of esomeprazol for patients with severe disorders. Esomeprazol and its main metabolites do not cause accumulation when used 1 time/ day.
kidney failure:
No studies have been conducted in patients with renal function.
Because the kidneys play the role of eliminating the metabolites of ecomeprazol but not the original active ingredient, the metabolism of Esomeprazol may not be changed in patients with impaired renal function.
Elderly:
Esomeprazol metabolism has not changed significantly on the object of the patient who is old 71 - 80 years old).
Children:
Adolescents 12-18 years old: After repeating Esomeprazol dose of 20 mg and 40 mg, AUC and TMAX in objects 12 - 18 years old similar to adults in both doses.
Before taking Jiracek-20 Davipharm medicine treats gastric ulcer, gastroesophageal reflux
How to use
Esomeprazole is not stable in acidic environment, so it is necessary to take the drug in the form of tablets in the intestine so that it will not be destroyed in the stomach and increase bioavailability. Must swallow the whole pill with water, do not be crushed, chewed or broken.
Take medicine at least 1 hour before meals. Can be used with antacids when necessary to relieve pain.
This form of preparation is not suitable for patients with difficulty swallowing or unable to swallow. Choose other forms of preparation more suitable for patients.
Dosage
Esomeprazol is used in Magnesi salt but the dose is calculated by esomeprazol:
Adults and children ≥ 12 years:
Gastroesophageal reflux disease (GERD)
Adults:
Used in combination with the appropriate antibiotic regimen to eradicate Helicobacter pylori and treat duodenal ulcerative ulcerative ulcerative by Helicobacter pylori and prevent the recurrence of stomach ulcers caused by Helicobacter Pylori 20 mg Esomeprazol + 1 g amoxicillin + 500 mg Clarithromycin, drink 2 times/day for 7 days.
Patients need to continue treating with nonsteroidal anti -inflammatory drugs (NSAIDs):
Treatment of stomach ulcers caused by NSAID: The usual dose is 20 mg x 1 time/day. Treatment for about 4 - 8 weeks.
Preventive stomach - duodenal ulcer prophylaxis due to NSAID in patients at risk: 20 mg x 1 time/day.
Prolonged treatment after Esomeprazol intravenous injection to prevent recurrent bleeding in stomach ulcers - duodenum 40 mg x times/day for 4 weeks after intravenous injection to prevent recurrent bleeding in stomach - duodenal ulcer.
Treatment of Zollinger Ellison syndrome
The recommended starting dose is 40 mg x 2 times/day. The following dose should be adjusted depending on the patient and continue treatment when there is clinical indications. Based on existing clinical data, most patients can control the disease at 80 - 160 mg/day. Doses greater than 80 mg/day should be divided into drinking 2 times/day.
Children:
Children ≥ 12 years:
Treatment of duodenal ulcerative by Helicobacter pylori
When choosing appropriate coordination therapy, it is necessary to consider the official guidelines of the nation, the region and the locality on antibacterial ability, treatment time (usually 7 days but sometimes up to 14 days), and use an antibiotic reasonable. The treatment should be monitored by a specialist.
The recommended dose is:Side Effects
The following unwanted effects have been identified or suspected in clinical trials and after bringing the drug to the market. There is no unwanted effect related to the dose.
Common, 1/100 ≤ ADR
The drug can cause other unwanted effects. It is recommended that patients immediately notify the doctor when they experience unwanted effects when taking the drug.
Instructions for handling ADR:
Must stop the drug when there is a heavy ADR manifestation
Warnings
Before using the drug you need to read the instructions carefully and refer to the information below.
contraindicated
hypersensitivity to Esomeprazol or other proton pump inhibitors, or benzimidazol -substances, or hypersensitivity to any ingredients of the drug.
Do not use drugs simultaneously with nelfinavir.
Caution when using
When there are warning symptoms (such as unintentional strong weight loss, vomiting, vomiting blood or bleeding) and when suspected or identifying stomach ulcers, eliminating the possibility of malignant disease because the drug can cover symptoms and slow diagnosis.
Be cautious when used in people with liver disease, pregnant or nursing.
Prolonged treatment patients (especially over 1 year): Should be monitored regularly.
The long -lastingusing ecomeprazol can cause gastric atrophy or an increased risk of infection (such as pneumonia in the community).
Patients treated as required: Should be instructed to contact the doctor if there is a change in the properties of symptoms. When using Esomeprazol on demand, it is necessary to consider the impact of interactions with other drugs due to the change of Esomeprazol concentration in plasma.
Helicobacter pylori:
It is necessary to consider the possibility of interacting with other drugs when taking Esomeprazol in the Helicobacter pylori kills. Clarithromycin is a powerful CYP3A4 inhibitor, so it should be noted for the contraindications and interactions of Clarithromycin when using Clarithromycin in the 3 -drug regimen for patients who are using concurrently metabolic drugs through CYP3A4 as Cisaprid.
Gastrointestinal infections:
Treatment with proton pump inhibitors may increase the risk of gastrointestinal infections such as Samonella and Campylobacter.
may increase the risk of diarrhea due to Clostridium difficile when using proton pump inhibitors.
Vitamin B12 absorption:
As other antacids, Esomeprazol can reduce the absorption of vitamin B12 (cyanocobalamin) due to the effect of reducing or deficiency of gastric acid. It is necessary to consider when taking the drug for patients with a reduced reserve of vitamin B12 or have risk factors that reduce the absorption of vitamin B12 when treated for a long time.
Hypotension (with or asymptomatic) rarely encountered in patients using prolonged proton pump inhibitors (at least 3 months or in most cases that last for more than 1 year).
There have been cases of severe magnesi in patients treated with proton pump inhibitors such as Esomeprazol for at least 3 months and in most cases that last for more than 1 year. The serious manifestation of the blood magnesi such as fatigue, spasticity, delirium, convulsions, dizziness and ventricular arrhythmia may occur, but these symptoms may not be clear and overlooked. In patients most affected, the condition of lowering blood magnesium can be improved after stopping the drug and replacing Magnesi.
For patients who are likely to be treated with prolonged proton pump inhibitors or use in combination with digoxin or other drugs that can cause other blood magnesium (such as diuretics), treatment doctors should conduct testing and evaluation of blood blood levels before starting treatment and periodically during treatment with proton pump inhibitors, including Esomeprazole.
Risk of fractures:
When using proton pump inhibitors, especially when taking high and prolonged doses (≥ 1 year), it may increase the risk of pelvic fractures, wrist or spine due to osteoporosis, mainly occurs in the elderly or people with risk factors available. The mechanism of this phenomenon has not been explained, but it may be due to reduction in unanimidated calcium absorption due to gastric pH increase.
The lowest dosage recommendation works in the shortest possible time, suitable for clinical status. Patients at risk of osteoporosis should use enough calcium and vitamin D, assess bone condition and manage as instructed.
Lupus erythematosus in the skin (SCLE):
Proton pump inhibitors are related to frequency of non -frequency SCLE. If the damage occurs, especially the skin in direct sun exposure to the sun, with joint pain, it is recommended that patients see a doctor and consider stopping the drug for the patient. The patient had a history of SCLE after taking a proton pump inhibitor that could increase the risk of SCLE with other proton pump inhibitors.
Use other drugs:
It is not recommended to simultaneously use Esomeprazol and Atazanavir. If required, it must be closely monitored, increasing the dose of Atazanavir to 400 mg in combination with 100 mg of ritonavir, should not use Esomeprazol more than 20 mg.
Esomeprazol is CYP2C19 inhibitor. When starting or ending treatment with esomeprazol, it is necessary to consider the interactions that may occur with metabolic drugs through CYP2C19. There have been drug interaction reports between clopidogrel and esomeprazol. The clinical relevance of this interaction is uncertain. Be careful with this interaction, not recommended to simultaneously use Esomeprazol and Clopidogrel.
Subclinical tests:
Increased chromographin A (CGA) can hinder the diagnosis of endocrine nerve tumors. To avoid this effect, stop Esomeprazol at least 5 days before CGA test.
Be cautious for excipients Magnesi Hydroxid
The drug contains magnesium magnesi laxative, which can lead to diarrhea.
Hypergathed blood (causing hypotension, mental impairment, coma), especially cautious when used for people with kidney failure.
To be out of reach of children.
The effect of the drug on driving and operating machinery
Esomeprazol slightly affects the ability to drive and operate machinery. Unwanted effects such as: headache, dizziness (rarely), drowsiness, reduction of vision (rare) ... Be careful when participating in dangerous activities that need alertness such as working on high, operating machinery or driving train.
Use drugs for women during pregnancy and lactation
pregnancy
There is no adequate study when using Esomeprazol in pregnant people. On animals, white rats oral Esomeprazol dose of 280 mg/ kg/ day (57 times the dose on humans calculated by the body surface area) and the oral rabbit dose of 86 mg/ kg/ day (35 times the dose on humans calculated by the surface area of the body) does not see evidence of reproductive or toxic fetus due to Esomeprazol. However, only use Esomeprazol during pregnancy when really necessary.
Breastfeeding period
It is not known whether esomeprazole will excrete in milk or not. However, omeprazol is distributed into breast milk.
Esomeprazol is likely to cause unwanted effects in breastfed babies, so it is necessary to decide to stop breastfeeding or stop the drug, depending on the importance of the medication for the mother.
Reproduction
Animal research with racemic mixture of omeprazol oral oral use is not visible on fertility.
Drug interaction
Esomeprazol's effect on the pharmacokinetics of other drugs:
Absorbed drug depends on pH
Inhibiting stomach acid secretion when treated with ecomeprazol or other proton pump inhibitors may increase or reduce the absorption of drugs that depend on the stomach pH. When treated with ecomeprazol, stomach acids reduce the absorption of some drugs such as ketoconazole, otraconazole and erlotinib and increase the absorption of drugs like Digoxin. Omeprazol simultaneous treatment (20 mg/ day) with digoxin in healthy people increases the bioavailability of digoxin to 10% (up to 30% in 2 of 10 users). The toxicity of Digoxin has been reported rare. However, it is necessary to be cautious when using high doses of Esomeprazol for the elderly. Closely monitor the treatment process with digoxin.
Protease inhibitors
There has been an interactive report between omeprazol and some protease inhibitors. Clinically importance and mechanism behind these interactions are not fully known.
Gastric pH increases during omeprazole treatment may change the absorption of protease inhibitors. Other mechanisms that can be explained to the above interaction are through CYP2C19 inhibition.
There have been reports to reduce serum levels of Atazanavir and Nelfinavir when used simultaneously with omeprazol, so this combination is not recommended. Simultaneous use of omeprazol (40 mg x 1 time/ day) with Atazanavir 300 mg/ ritonavir 100 mg in healthy volunteers significantly reduces Atazanavir concentration (reduced AUC, CMAX, CMIN by approximately 75%). Increasing the dose of Atazanavir to 400 mg is not sufficient to compensate for the effects of omeprazol on Atazanavir concentration. Simultaneous use of omeprazol (20 mg x 1 time/ day) with Atazanavir 400 mg/ ritonavir 100 mg in healthy volunteers reduces the level of Atazanavir levels approximately
30% compared to when using Atazanavir 300 mg/ ritonavir 100 mg x 1 time/ day. Sometimes, Omeprazol (40 mg x once a day) reduces AUC, CMAX and CMIN of Nelfinavir by 36 - 39% and AUC, CMAX and CMIN of metabolites with M8 activity decreased by about 75 - 92%. For Saquinavir (Ritonavir combination), there has been reports to increase serum concentration (80 - 100%) when using omeprazol simultaneously (40 mg x 1 time/ day). Treatment with Omeprazol 20 mg 1 time/ day does not affect the concentration of Darunavir (Ritonavir) and Amprenavir (Ritonavir combination). Treatment with Esomeprazol 20 mg 1 time/ day does not affect Amprenavir concentration (whether or not ritonavir). Treatment with omeprazol 40 mg x 1 time/day does not affect Lopinavir concentration (Ritonavir combination). Because Omeprazol and Esomeprazol are similar in terms of pharmacokinetics and pharmacokinetics, it is not recommended to simultaneously use Esomeprazol and Atazanavir and Conv Lend to simultaneously use Esomeprazol and Nelfinavir.
The drug is metabolized by CYP2C19
Esomeprazol inhibits CYP2C19, the main metabolic enzyme of Esomeprazol. Therefore, when used simultaneously, Esomeprazol with metabolic drugs by CYP2C19 such as Diazepam, Citalopram, Imipramin, Clomipramin, Phenitoin, ... will increase the concentration of the above drugs in plasma, which may need to reduce the dose. It should be noted when indicating Esomeprazol at the required treatment therapy.
Diazepam: Simultaneous use of 30 mg of Esomeprazol reduces 45% of the clearance of CYP2C19 Diazepam substrate.
Phenytoin: Simultaneously use 40 mg of Esomeprazol, which increases 13% of plasma phenytoin concentrations in epilepsy patients. Recommendation for monitoring phenytoin concentrations in plasma when starting or stopping treatment with Esomeprazol.
Voriconazole: Omeprazol (40 mg x 1 time/ day) increases CMAX and AUC of Voriconazole (a CYP2C19 substrate) 15% and 41% respectively.
warfarin: simultaneously use 40 mg of Esomeprazol for patients being treated with warfarin in clinical trials showing that blood clotting time is within the acceptable range. However, after bringing the drug to the market, there were some cases of significant Inr clinical increase in clinical treatment at the same time. The Inr monitoring recommendation at the beginning and at the end of Esomeprazol treatment simultaneously with Warfarin or other Coumarin derivatives.
cilostazol: Omeprazol and Esomeprazol both have CYP2C19 inhibitors. Using 40 mg dose Omeprazol in healthy people increases CMAX and AUC of Cilostazol 18% and 26% respectively, and of a metabolite with its activity about 29% and 69% respectively.
Cisaprid: In healthy volunteers, simultaneously used with Esomeprazol 40 mg increases 32% AUC and prolongs the sale time of 31% but does not significantly increase the peak concentration in the plasma of Cisaprid. There has been a report that extends the mild QT period after using only Cisaprid and does not last longer when using Cisaprid with Esomeprazol.
Clopidogrel: In a cross -clinical study, Clopidogrel (attack dose of 300 mg/maintenance dose of 75 mg/day) alone and omeprazol combination (80 mg, used at the same time with clopidogrel) used for 5 days. The concentration of the active metabolites of clopidogrel decreased by about 46% (day 1) and 42% (day 5) when using clopidogrel with omeprazol. The inhibition of platelets (IPA) decreased by about 47% (24 hours) and 30% (day 5) when using clopidogrel with omeprazol. Another study showed that the use of clopidogrel and omeprazol at different times did not prevent the interaction between them, may be due to the inhibitory effect of CYP2C19 of Omeprazol. The data is not consistent with the clinical effects of this PK/PD interaction of Esomeprazol for large cardiovascular events that have been reported from description and clinical studies.
Use Esomeprazol with CYP2C19 and CYP3A4 induction drugs such as rifampin reduces Esomeprazol levels, avoiding simultaneous use.
amoxicillin and quinidine: There is no influence of ecomeprazol on pharmacokinetics of amoxicillin, clinical quinidine.
Naproxen or Rofecoxib: In short -term studies, simultaneous use of Esomeprazol with Naproxen or Rofecoxib does not see clinical pharmacokinetic interactions.
Unknown mechanism:
methotrexate: Increased methotrexate levels in some patients when using proton pump inhibitors simultaneously. Consider temporary suspension of Esomeprazol when indicating high doses of methotrexate for patients.
tacrolimus:
There have been reports to increase serum tacrolimus concentration when using Esomeprazol simultaneously. Tacrolimus concentration should be closely monitored as well as monitoring the patient's kidney function (CLCR), adjusting the tacrolimus dose if necessary.
Effect of other drugs on Esomeprazol's pharmacokinetics:
CYP2C19 and/or CYP3A4 inhibitors:
Esomeprazol metabolized by CYP2C19 and CYP3A4. Concomitant use of Esomeprazol and a CYP3A4 inhibitor such as Clarythromycin (500 mg x 2 times/ day) double the AUC of Esomeprazol. Simultaneous use of Esomeprazol and an inhibitor both CYP2C19 and CYP3A4 may increase more than the AUC of Esomeprazol.
Voriconazole inhibits CYP2C19 and CYP3A4, increasing the AUC of Esomeprazole about 280%.
In these cases, the adjustment of the dose may not be necessary. However, considering adjusting the dose when taking drugs for patients with severe hepatic failure or being indicated for prolonged treatment.
CYP2C19 and/ or CYP3A4 induction drugs:
CYP2C19 or CYP3A4 induction drugs or both (such as rifampicin and st John’s Wort) can reduce serum ecomeprazol levels due to increased Esomeprazol metabolism.
Other interactions:may increase the risk of hypoglycemia when taking ecomeprazol and drugs that also causes hypotension such as thiazid diuretics, strap diuretic. Check blood magnesium levels before taking proton pump inhibitors and periodically.
Digoxin: Lowering blood magnesia due to prolonged use of proton pump inhibitors that cause heart muscle to increase sensitivity to digoxin, which can increase the risk of toxicity to Digoxin's heart. In patients who are using digoxin, check the magnesium concentration before starting to use proton pump inhibitors and periodically later.
Sucralfate: Inhibition of absorption and reducing the bioavailability of proton pump inhibitors. Use proton pump inhibitors at least 30 minutes before using sucralfat.
Children:
Esomeprazol interactive studies have only been done on adults.
Storage
Leave a cool place, avoid light, temperatures below 30⁰C.
To be out of reach of children, read the instructions carefully before use.
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