Rabiswift 20 CPC1HN Treatment of active duodenal ulcer (3 blisters x 10 tablets)

Anti -secretion activity: After the dose of 20 mg of sodium Rabeprazol, the anti -secret effect appears within 1 hour, the maximum efficiency is achieved within 2 to 4 hours. After the first dose of 23 hours, the basic acid secretion is 69 % and acid secretion inhibits stimulated by food is 82 %, the inhibitor time lasts up to 48 hours. The time for the drug has a much longer pharmacological effect compared to the semi -cancellation time (about 1 hour), may be due to the prolonged link with the enzyme H/K - ATPASE in the stomach wall. The acid secretion effect of Rabeprazol sodium increases slightly when used next day and stable after 3 days ..

Effects on serum gastrin: In clinical studies on patients treated with 20 mg of sodium Rabeprazol sodium once a day, lasting up to 24 months. The serum gastrin increases in the first 2 to 8 weeks, showing the inhibitory effect on acid secretion. Gastrin returns as before treatment, usually within 1 black 2 weeks after stopping the drug.

Effect of killing H. pylori:

The gastric biopsy samples from the caves and the bottom of more than 500 patients using Rabeprazol or the control treatment for 8 weeks are not detected the hypopathinal change of ECL cells, the degree of gastritis, the incidence of gastritis, intestinal transmission or the distribution of H. pylori infection. In more than 250 patients monitoring in 36 months of continuous treatment, there is no significant change in the initial survey detection that has been observed.

Studies on healthy objects have shown that sodium rabeprazol has no significant clinical interactions with Amoxicillin. Rabeprazole does not affect the concentration of amoxicillin in plasma or clarithromycin when combined with the purpose of killing H. pylori in the stomach - intestines.

Dynamic pharmacokinetics

absorption: Rabeprazol sodium is formulated in the form of tablets soluble in the intestine due to the characteristic of being decomposed by acid. Therefore, the absorption of Rabeprazole only happens after the drug leaves the stomach. The drug is fast absorbing, with peak concentration in plasma about 3.5 hours after taking 20 mg dose. The peak concentration in plasma (CMAX) and AUC is linearly between 10 mg to 40 mg. The absolute bioavailability of the 20 mg oral dose (compared to intravenously) is about 52% due to a large part of the drug. In addition, bioavailability does not seem to increase after repeating the dose. In healthy people, plasma disposal time is about 1 hour (from 0.7 to 1.5 hours), and the body clearance is estimated at 283 ± 98 ml/min. There is no interaction with clinical food. Both food and medication time do not affect the absorption of Rabeprazol sodium ..

Distribution: Rabeprazole is attached to plasma proteins about 97%.

Metabolism and excretion: Sodium Rabeprazol as well as other proton pump inhibitors (PPI) metabolized through the drug metabolism system through cytochrom P450 (CYP450). In vitro studies in human liver microsom shows that Sodium Rabeprazol is metabolized by the CYP450 isoenzyme (CYP2C19 and CYP3A4). In these studies, at the desired drug concentration in serum, Rabeprazole does not cause induction nor inhibited CYP3A4; And although in vitro studies do not always predict in vivo results, the results of these studies allows predicting no interaction between rabeprazol and cyclosporin, in people the main metabolites in plasma are thioether (ml) and carboxylic acid (M6) and auxiliary transformations with lower concentrations of sulphon (M2), Desmethyl-Desmethyl-Phaioether (M4) and M4) Combined with mercapturic acid (M5). Only Desmethyl metabolism (M3) has antimicrobial activity, but does not appear in plasma.

After taking a single dose of 20 mg of sodium Rabeprazol is marked by 14C, no non -metabolic drug is found in urine. About 90% of the drug is excreted in urine mainly 2 metabolites: associated with mercapturic acid (M5) and carboxylic acid (M6), and two unknown metabolites. The rest is found in stool.

Sex: adjusted to height and body weight, there is no significant difference in pharmacokinetic parameters after taking a single dose of 20 mg of sodium Rabeprazol.

Renal failure: In patients with end -stage renal impairment, regular hemorrhage is absorbing (creatinine clearance

Liver failure: In mild to moderate liver failure, after using a single dose of 20 mg Rabeprazol, AUC doubled and the selling time increased by 2-3 times higher than healthy volunteers. However, after taking a dose of 20 mg within 7 days, AUC only increased by 1.5 times and CMAX increased by 1.2 times. Rabeprazol's waste sale time in patients with hepatic impairment is 12.3 hours compared to 2.1 hours in healthy volunteers. Responding to pharmacological resources (gastric pH control) in both groups is clinically equivalent.

Elderly: Rabeprazol elimination decreases slightly in the elderly. After 7 days of using Rabeprazol sodium 20 mg, AUC increased approximately, CMAX increased by about 60% and the sale time increased by about 30% compared to healthy young volunteers. However, there is no evidence of drug accumulation.

CYP2C19 diversity: After using Rabeprazol 20 mg/day for 7 days, people with CYP2C19 are slowly transformed, with AUC and the sale time of about 1.9 and 1.6 times compared to people with fast transformation, while CMAX only increases 40%.

Be cautious when using

Patients should be recommended not to chew or crush the pill but must swallow whole tablets.

Improving symptoms through sodium Rabeprazol does not rule out the presence of stomach or esophagus cancer, so it is necessary to eliminate malignant possibility before starting treatment. Patients with long -term treatment (especially for more than 1 year treatment) need to be tested regularly.

Do not recommend using drugs in children, because there is no experience in this age group.

There have been reports when circulating in the market for hematopoietic disorders (platelets and neutrophils. In most cases, it is impossible to identify other causes, this event has no complications and out of the drug.

The liver enzyme abnormalities have been encountered in clinical trials and has also been reported since the saving is allowed to circulate. In most cases, there is no other cause, this incident has no complications when the drug is stopped.

There is no evidence of drug safety issues in a study on patients with mild liver failure on average with age and gender control. However, there is no clinical data on the use of drugs in patients with severe liver failure or prescriptions should be cautious when treating for the first time in these patients.

Simultaneous use of sodium and Atazanavir rabeprazol is not recommended.

Treatment with proton pump inhibitors may increase the risk of digestive infections such as Salmonella, Campylobacter and Clostridium difficile.

Proton pump inhibitors, especially if high doses and long -term doses (> 1 year), may increase the risk of cracking hip, wrist and spine fractures. Observatory studies show that proton pump inhibitors can increase the risk of a crack by 10-40 %. Some of these increase may be due to other risk factors. Patients at risk of osteoporosis need to be cared for under the current clinical instructions and may provide additional vitamin D and calcium.

Serious blood magnesia reduces have been reported in patients treated with proton pump inhibitors for at least 3 months, and in most cases of 1 year use. The serious manifestation of blood magnesium reduces includes fatigue, spasticity, delirium, convulsions, dizziness and ventricular arrhythmia but can also cure the head quietly and be overlooked, reduce blood magnesium improved after replacing magnesium and stopping the drug.

For patients who will treat long -term or patients taking proton pump inhibitors with digoxin or drugs that cause blood magnesium (eg diuretics), testing magnesi levels in the blood before the beginning of treatment and periodically during treatment.

The effect of the drug on the ability to drive and operate machines

Based on the pharmacological properties and the side effects show that Rabeprazole does not reduce the ability to drive or use machinery. However, if sleepy reduces sensitivity, avoid driving or operating complex machinery.

Use drugs for women during pregnancy and lactation

Pregnant women:

There is no safety data on pregnant women. Studies on reproduction conducted on rats and rabbits show that there is no evidence of reproductive decline or affecting the embryo due to sodium rabeprazol, although there is a decrease in metabolism between placenta and fetus in mice. Contraindicated in pregnant women

breastfeeding women:

It is unclear whether Rabeprazol sodium is secreted into breast milk or not. There is no research on breastfeeding women. Rabeprazol sodium has excretion in milk in the mouse. So do not take the drug while breastfeeding.

Drug interaction

Rabeprazol sodium that inhibits acid secretion of strong and prolonged stomach acid. The interaction between the drug and the absorption of pH may occur. Simultaneous use of sodium rabeprazole and ketoconazole or otraconazole can significantly reduce antifungal concentration in plasma. Therefore, each patient needs to be monitored to decide whether it is necessary to reduce the dose when used simultaneously with ketoconazole and otraconazole.

In clinical trials, simultaneous antacids with sodium Rabeprazol and in a specific medication-interactive study, do not observe interactions with liquid acid resistance.

Sometimes, Atazanavir 300 mg/ritonavir 10 mg with omeprazol (40 mg/day) or Atazanavir 400 mg with Lansoprazol (60 mg/day) with a healthy volunteer leads to a decrease. Rabeprazole may increase the concentration/effect of drugs that are CYP2C19, CYP2C8 (high risk level), Metrothrexat, Saquinavir, Voriconazol.