Kagasdine medicine 20mg khapharco treatment of gastric ulcer, duodenal ulcer, gastric reflux - esophagus (1000 tablets)

Children from 1 year of age and over and ≥ 10 kg

ATC code: A02BC01.

Mechanism of action: Omeprazol is a racemic mixture of two isomers that reduce the secretion of gastric acid through the acting mechanism at the destination. The specific inhibitor of acid pumps on the walls of the walls. The drug has a quick acting and controlling impact through reversible inhibition of gastric acid secretion with daily dose.

Omeprazol is a weak base, concentrated and transformed into an active form in the high acidic environment of the cell into, where H'K'atpase inhibitors are inhibitors. The drug acts at the end of the process of gastric acid secretion, this effect depends on the dose and inhibiting both basic acid secretion and acid secretion due to stimulation, regardless of the stimulating agent causing acid secretion.

Pharmacological impact: All pharmacological effects observed can be explained by the effects of omeprazol on acid secretion. Take a single dose of 20mg of omeprazole to create a strong and effective stomach acid secretion. The maximum effect is achieved after 4 days of treatment. In patients with duodenal ulcer can maintain a 80% reduction in gastric acid in 24 hours.

Omeprazole can inhibit Helicobacter pylori bacteria in people with duodenal ulcers and/or reflux contaminated with this bacteria. Combining omeprazol with some antibiotics (such as clarithromycin, amoxicillin) can be exposed to H.pylori accompanied by an ulcer and remission for a long time.

Dynamic pharmacokinetics

absorption: Omeprazol is destroyed in an acidic environment. The drug is formulated in the form of tablets in the intestine to avoid the destruction of the acid pH of the stomach.

Omeprazol absorbs quickly after drinking, reaching the peak concentration after about 1-2 hours.

Omeprazol is usually completely absorbed in the small intestine after drinking for 3 to 6 hours. Concomitance with food does not affect the bioavailability of the drug.

Birth of omeprazol after taking the only dose is about 40%. After taking the dose repeated 1 time/day, bioavailability increases to about 60%.

Distribution: Omeprazol's distribution volume in healthy people is approximately 0.3 I/kg body weight. About 97% Omeprazol attached to plasma proteins.

Metabolism: Omeprazol is almost completely metabolized in the liver, mainly thanks to the cytochrom P450 isoenzyme to become hydroxy omeprazol, and a small part is transformed through CYP3A4 to form omeprazolsulfon. These metabolites are not active.

Elimination: Omeprazol's plasma sale time is usually less than 1 hour even after taking the only dose and the dose is repeated once a day. Omeprazol is completely eliminated from plasma between doses, not causing accumulation when taken 1 time/day. About 80% of the oral dose of omeprazol is eliminated in the form of metabolites through the urine, the rest is eliminated through feces, mainly due to the secretion of bile.

Linear/non -linear:

ome of omeprazol increases when the dose is repeated. This increase depends on the dose and leading to non -linear AUC with the dose after repeated use. This time and dose dependence is due to the first decrease in the liver and the whole body, possibly due to the CYP2C19 inhibitors of Omeprazol and/or its metabolites (such as sulfon metabolites). No metabolites work any effect on gastric acid secretion.

pharmacokinetics on special subjects:

Poor drug metabolic: In some people because the lack of CYP2C19 is active due to genetics (15 - 20% of Asians), should slow down the metabolism of omeprazol. In these people, the metabolism of omeprazol is mainly catalyzed by CYP3A4 enzyme. After using omeprazol 20mg repeated 1 time/day, AUC in people with drug metabolism increased by 5-10 times compared to normal people. The peak concentration in plasma is also 3-5 times higher. This does not affect the dose of omeprazol.

Hepatic failure: Omeprazol metabolism in people with impaired liver dysfunction leads to an increase in AUC. Omeprazol does not cause accumulation at a dose/day.

Kidney failure: Omeprazol pharmacokinetic parameters include systemic bioavailability and excretion rate, unchanged in patients with renal function impairment.

Elderly: Omeprazol metabolism decreases slightly in the elderly (75 - 79 years).

Children: During treatment at the recommended dose for children over 1 year of age, the concentration of drugs in plasma is similar to adults. In children under 6 months old, low omeprazol clearance due to poor conversion of omeprazol.

Treatment of heartburn and acid reflux in patients with gastroesophageal reflux: 2-4 weeks. It is advisable to conduct further review if it is not possible to improve symptoms after 2-4 weeks.

Children and teenagers over 4 years old:

Treatment of duodenal ulcerative ulcerative ulcer: When choosing suitable combination therapy for patients, they should consider official instructions in countries, regions and localities on bacterial resistance, treatment time (usually 7 days but sometimes up to 14 days) and use reasonable antibiotics. Treatment should be conducted under the supervision of a doctor. The recommended dose is as follows:

do when overdose? The overdose symptoms have been reported: nausea, vomiting, dizziness, abdominal pain, diarrhea and headache. There are also symptoms such as indifference, depression and confusion have also been described in some single cases.

Management: Omeprazol overdose symptoms are described as fleeting and no serious consequences are reported. The rate of elimination of drugs is constant when the dose increases. Symptomatic treatment if necessary.

When overdose, only symptomatic treatment, no specific treatment.

What to do when you forget a dose? However, if close to the next dose, skip the forgotten dose and take the next dose at the time as planned. Note that it should not be used double the prescribed dose.

When experiencing side effects of the drug, it is necessary to stop using and notify the doctor or go to the nearest medical facility for timely treatment.

Caution when using

When there are warning symptoms (such as unintentional weight loss, periodic recurrent vomiting, difficulty swallowing, vomiting of blood, anemia or defecation of black stool) and when suspected or gastric ulcer, it is necessary to eliminate the possibility of malignant diseases (such as cancer) because the drug can cover symptoms and slow diagnosis.

Do not recommend using Atazanavir with proton pump inhibitors.

In case the coordination is inevitable, it should be closely monitored when increasing the dose of Atazanavir to 400mg in combination with Ritonavir 100mg; Do not exceed the dose of 20mg of omeprazol. Omeprazol, as well as other acid secretions, can reduce the absorption of vitamin B12 (cyanocobalamin) due to reduced or deficient gastric acid. This should be considered in patients who reduce reserve or have the risk of reducing vitamin B12 absorption when long -term treatment.

omeprazol is a CYP2C19 inhibitor. When starting or ending treatment with omeprazol should consider potential interactions with metabolic drugs through CYP2C19. There has been an interaction between clopidogrel and omeprazol. It is unclear clinical correlation of this interaction. For careful purposes, should not be used simultaneously omeprazol and clopidogrel.

Serious blood magnesia reduction has been reported in patients treated with proton pump inhibitors such as omeprazol for at least three months, and in most cases is 1 year. The serious symptoms of the blood magnesi are like fatigue, muscle spasms, delirium, convulsions, dizziness, and ventricular arrhythmias may occur, but these manifestations may be silently and not concerned. In most cases, the condition of hypoglycemia can be improved when supplemented with magnesi and ppi stops.

For patients who need long -term treatment or patients who use ppi with digoxin or drugs that can cause blood magnesium (such as diuretics), medical experts should consider measuring blood magnesium levels before starting PPI treatment and periodically during treatment.

Proton pump inhibitors, especially when using high doses and for a long time (> 1 year), can slightly increase the risk of hip fractures, wrist bones and spine, especially the elderly or those with known risk factors.

Observatory studies show that proton pump inhibitors may increase the overall risk of fractures by about 10 - 40%. Part of this increase may be due to other risk factors. Patients at risk of osteoporosis should be taken care of under the current clinical instructions and should be used just enough vitamin D and calcium.

Select Lupus Lupus (SCLE): There is a SCLE report in patients who are taking proton pump inhibitors. If the damage occurs, especially the skin in direct contact with the sun, with joint pain, it is recommended that patients come to the doctor and consider stopping the drug.

Patients who have a history of being scratched after taking a proton pump inhibitor may increase the risk of SCLE with other proton pump inhibitors.

affect tests: increased chromographin (CGA) levels may affect the detection of endocrine nerve tumors. In order to avoid this intervention, omeprazol should be stopped at least 5 days before CGA measurement.

Some children with chronic diseases may need prolonged treatment, although not recommended.

Treatment with proton pump inhibitors may increase the risk of gastrointestinal infections such as Salmonella and Campylobacter, in boarding patients may have the risk of clostridium difficile infection.

When long -term treatment, especially when it lasts over 1 year, patients should be monitored regularly.

The ability to drive and operate machinery

omeprazole hardly affects the ability to drive and operate machinery. However, unwanted effects such as dizziness, visual disorders may occur. Therefore, if these reactions occur, patients should not drive or control machines.

Use drugs for women during pregnancy and lactation

Pregnant women: Results from some epidemiological studies show that there is no unwanted effect of omeprazol in pregnant women or the health of the fetus/babies. Omeprazol can be used during pregnancy.

Lactating women: Omeprazol is secreted into breast milk but hardly affects breastfed babies while taking the drug at the dose of treatment.

Reproductive ability: Animal research with racemic isomers of omeprazol oral use does not see the fertility effect.

Drug interaction

Omeprazol's effect on the pharmacokinetics of other drugs:

Absorbing drugs dependent pH:

Reducing stomach acid when treated with omeprazol and other ppi can reduce or increase the absorption of other drugs with a mechanism of absorption dependent on gastric pH.

Nelfinavir, Atazanavir: The concentration of these two drugs may be reduced when used simultaneously with omeprazol. Contrain to the simultaneous use of Omeprazol and Nelfinavir, this interaction may be related to CYP2C19 inhibitors. Do not recommend simultaneous use of omeprazol and atazanavir.

Digoxin: simultaneous treatment of omeprazol (20mg/day) and digoxin can increase the bioavailability of digoxin to 10%. Rare Digoxin poisoning has been reported.

Be cautious when using high -dose omeprazol in the elderly. Strengthen monitoring when treating with digoxin.

Clopidogrel: The result of studies on healthy subjects has shown that the pharmacokinetic/pharmaceutical interaction between clopidogrel (loaded dose of 300mg/maintenance dose 75mg/day) and omeprazol (80mg/day of oral) leads to the reduction of the active metabolic level of clopidogrel average 46% and maximum inhibition of plasma collection (causing by ADP) The inconsistent data in the clinical publications of Omeprazol's pharmaceutical/pharmaceutical interactions on the main cardiovascular events have been reported in both clinical observation and clinical research studies. For careful purposes, should not be used simultaneously omeprazol and clopidogrel

Other drugs: The absorption of Posaconazole, Erlotinib, Ketoconazole and Itraconazole is severely reduced and therefore clinical efficiency can also be affected. For Posaconazol and Erlotinib, avoid simultaneously with omeprazol.

Metabolic drugs by CYP2C19:

Omeprazol is a medium inhibitor CYP2C19, the main metabolic enzyme of omeprazol. Therefore, the metabolism of combined drugs is also metabolized via CYP2C19 can decrease and increase AUC such as R-Warfarin and other anti-vitamin K drugs, Cilostazol, Diazepam and Phenytoin.

cilostazol: Concentrated with omeprazol increases the concentration of Cilostazol and its active metabolites.

Phenytoin: Need to monitor plasma phenytoin concentrations for the first 2 weeks after the beginning of treatment with omeprazol and monitor if adjusting the phenytoin dose, continue to adjust the phenytoin dose at the end of treatment with omeprazol.

Unknown mechanism:

saquinavir: Concomitance of Omeprazol and Saquinavir/Ritonavir increases the plasma saquinavir levels to 70% related to good tolerance in HIV patients.

tacrolimus: simultaneously used with omeprazol increases the concentration of tacrolimus in serum. Need to closely monitor Tacrolimus concentration as well as monitor the patient's kidney function, adjust the dose of Tacrolimus if necessary.

methotrexate: Increased methotrexate levels in some patients when used simultaneously with proton pump inhibitors. Consider temporary suspension Omeprazol when using high doses of methotrezat in patients.

Effect of other drugs on omeprazol pharmacokinetics:

CYP2C19 and or CYP3A4 inhibitors: Because Omeprazol is metabolized by CYP2C19 and CYP3A4, when used simultaneously with CYP2C19 or CYP3A4 inhibitors (such as Clarithromycin, Voriconazole) can increase serum omeprazole due to Esomeprazole reduction. Treatment in combination with voriconazole can double the AUC of Omeprazol. Because high doses Omeprazol have good tolerance, the adjustment of the dose is unnecessary. However, the dose should be considered in patients with severe liver failure and are indicated for treatment in a long time.

CYP2C19 and/ or CYP3A4 induction drugs: CYP2C19 or CYP3A4 induction drugs or both (such as rifamicin and st.john (hypericum performance)) can reduce serum omeprazol levels due to increased metabolism
omeprazol.

Due to the lack of studies on the correlation of the drug, not mixing this drug with other drugs.