Raso, 20 mg 30 pcs.

Pharmacodynamics

Mechanism of action

Rabeprazole belongs to the class of antisecretory drugs which are chemically substituted benzimidazoles. Rabeprazole inhibits the activity of the enzyme H+/K+ATPase (“proton pump”), thus blocking the final stage of hydrochloric acid synthesis. This effect is dose-dependent and leads to inhibition of both basal and stimulated hydrochloric acid secretion regardless of the irritant.

Rabeprazole has no anticholinergic properties.

Antisecretory activity

After oral administration of 20 mg rabeprazole the antisecretory effect occurs within one hour. Inhibition of basal and stimulated hydrochloric acid secretion 23 h after the first dose of rabeprazole is 62% and 82%, respectively, and continues until 48 h. This duration of pharmacokinetic action is much longer than that predicted by the half-life (T1/2), which is approximately 1 h.

Indications

Gastric and duodenal ulcer, reflux esophagitis, Nausea, Sour belching, GI infections caused by Helicobacter pylori, Abdominal bloating

• Gastric ulcer in the acute stage and anastomosis ulcer;

• acute duodenal ulcer;

Active ingredient

Rabeprazole

Composition

Each enteric-coated tablet, 20 mg contains:

Active ingredient:

Rabeprazole sodium 20 mg

Associates:

Mannitol

Hyprolose low substituted

Magnesium oxide heavy

Hypromellose (5cps)

Sodium lauryl sulfate

Talc

Magnesium stearate

Shell:

Zein

Triethylcitrate

Encoating:

Methacrylic acid and ethyl acrylate copolymer [1:1] (methacrylic acid copolymer (type C))

Triethylcitrate

Talc

Shell:

Opadray Yellow OY-52945 (Hypromellose 5 cP, Titanium Dioxide (E171) MacroGol-400 Dye Iron Oxide Yellow (E172))

The composition of the red ink for writing on the 20 mg tablet:

Shellac glaze 45%

Dye red charming (E129)

H-butanol

Denatured ethanol

How to take, the dosage

Razo® tablets are taken orally without chewing or crushing. It was found that neither time of day nor food intake affects rabeprazole activity.

In acute peptic ulcer disease and anastomosis ulcer it is recommended to take orally 20 mg once a day. Usually the cure comes after 6 weeks of therapy, but in some cases the duration of treatment may be extended.
In acute duodenal ulcer, it is recommended to take orally 20 mg once a day. The duration of treatment is from 2 to 4 weeks. If necessary, the treatment duration can be prolonged for 4 more weeks.

In treatment of erosive and ulcerative gastroesophageal reflux disease or reflux esophagitis it is recommended to take orally 20 mg once a day. The duration of treatment is from 4 to 8 weeks. If necessary, the duration of treatment may be prolonged for 8 more weeks.

In maintenance therapy of gastroesophageal reflux disease it is recommended to take orally 20 mg once a day. The duration of treatment depends on the patient’s condition.

In non-erosive gastroesophageal reflux disease it is recommended to take orally 20 mg once a day.
If after four weeks of treatment the symptoms have not disappeared, a further examination of the patient should be conducted. After the relief of symptoms to prevent their subsequent occurrence the drug should be taken orally once a day on demand.

For the treatment of Zollinger-Ellison syndrome and other conditions characterized by pathological hypersecretion, the dose is selected individually. The initial dose is 60 mg per day, then the dose is increased and the drug is prescribed at a dose of up to 100 mg per day at a single dose or 60 mg twice a day. For some patients, fractional dosing is preferable. Treatment should be continued as clinically necessary. In some patients with Zollinger-Ellison syndrome treatment duration of rabeprazole may be up to one year.

For eradication of Helicobacter pylori it is recommended to take by mouth 20 mg twice a day according to a certain scheme with appropriate antibiotic combination. The duration of treatment is 7 days.

Patients with renal and hepatic impairment

No dose adjustment is required in patients with renal impairment.

In patients with mild to moderate hepatic impairment the blood concentration of rabeprazole is usually higher than in healthy patients.
Caution should be exercised when prescribing Razo® in patients with severe hepatic impairment.

Elderly patients

No dose adjustment is required.

Children

The safety and efficacy of rabeprazole in children aged 12 years and older is established for short-term (up to 8 weeks) treatment of GERD. The recommended dose for children aged 12 years and older is 20 mg once daily for up to 8 weeks. Safety and efficacy of rabeprazole in pediatric patients for other indications have not been established.

Interaction

Concomitant use with digoxin may increase (mild to moderate) plasma concentrations of digoxin.

Concomitant use with ketoconazole decreases its bioavailability.

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Special Instructions

Patient response to rabeprazole therapy does not exclude the presence of malignant neoplasms in the stomach.

Tablets of the drug Razo® must not be chewed or crushed. The tablets should be swallowed whole. It was found that neither time of day nor food intake influence activity of rabeprazole.

In a special study in patients with mild or moderate hepatic impairment no significant difference of frequency of side effects of rabeprazole from that in healthy individuals of similar sex and age was found, but, nevertheless, caution is recommended during first use of rabeprazole in patients with severe liver impairment. The AUC of rabeprazole in patients with severe hepatic impairment is approximately twice as high as in healthy patients.
Patients with renal or hepatic impairment do not require dose adjustment of rabeprazole.

Hypomagnesemia

When treated with proton pump inhibitors for at least 3 months, cases of symptomatic or asymptomatic hypomagnesemia have rarely been reported. Most of these cases were reported one year after therapy. Serious adverse events were tetany, arrhythmias, and seizures. Most patients required treatment for hypomagnesemia, which included magnesium replacement and withdrawal of proton pump inhibitor therapy. In patients who will receive long-term treatment or who take proton pump inhibitors with drugs such as digoxin or drugs that may cause hypomagnesemia (e.g., diuretics), health care providers should monitor magnesium levels before treatment with proton pump inhibitors and during treatment.

Patients should not take other acid-reducing agents, such as H2-receptor blockers or proton pump inhibitors, simultaneously with rabeprazole.

Bone fractures

Observational studies suggest that therapy with proton pump inhibitors may increase the risk of osteoporosis-related fractures of the hip, wrist, or spine. The risk of fractures was increased in patients who received high-dose PPIs for a long period of time (one year or more).

Simultaneous use of rabeprazole with methotrexate

. According to the literature data, concomitant use of PPIs with methotrexate (especially in high doses) can lead to increased concentration of methotrexate and/or its metabolite hydroxytetrexate and longer elimination half-life, which can lead to methotrexate toxicity. If high doses of methotrexate are necessary, temporary discontinuation of PPI therapy may be considered.

Clostridium difficile

PPI therapy may result in an increased risk of gastrointestinal infections such as Clostridium difficile.
Based on the peculiarities of the pharmacodynamics of rabeprazole and its profile of adverse effects, it is unlikely that rabeprazole affects the ability to drive vehicles and perform other activities requiring concentration and rapid psychomotor reactions. However, in case of drowsiness or dizziness, these activities should be avoided.

Contraindications

Hypersensitivity to rabeprazole, substituted benzimidazoles or excipients of the drug; pregnancy;

Breast-feeding period;

Children under 12 years of age.

With caution:

Severe renal insufficiency, childhood (over 12 years).

Side effects

Rabeprazole is generally well tolerated by patients.

Side effects are generally mild to moderate and transient.

The following side effects were noted during clinical trials while taking rabeprazole: headache, abdominal pain, diarrhea, flatulence, constipation, dry mouth, dizziness, rash, peripheral edema.

Frequency of side effects is stated according to the following gradation: very frequently (>1/10);

• frequently (1/10 – 1/100);

• infrequently (1/100 – 1/1000);

• frequently (1/1000 – 1/10000);

• very rarely (< 1/10000).

immune system disorders

• Rarely, acute systemic allergic reactions.

• Disorders of the blood and lymphatic system

• Rarely – thrombocytopenia, neutropenia, leukopenia.

• Metabolic and nutrition disorders

• Rarely – hypomagnesemia.

Hepatobiliary system disorders

Rarely – increased activity of “liver” enzymes, hepatitis, jaundice, hepatic encephalopathy.

Renal and urinary tract disorders

• very rarely – interstitial nephritis.

Dermatological and subcutaneous tissue disorders

• Rarely – bullous rashes, urticaria;
• very rarely – erythema multiforme, toxic epidermal necrolysis, Stevens-Johnson syndrome.

Muscular and connective tissue disorders

• Rarely – myalgia, arthralgia.

Reproductive system disorders

• Very rare – gynecomastia.

Changes in laboratory parameters during rabeprazole administration have not been observed.

The risk of bone fractures may increase when taking proton pump inhibitors (see section “Special Precautions”).

Pregnancy use

There are no data on the safety of rabeprazole during pregnancy.

Reproduction studies in rats and rabbits have shown no evidence of fertility impairment or fetal defects due to rabeprazole; however, in rats in small amounts the drug penetrates the placental barrier. Razo® should not be used during pregnancy unless the expected benefits to the mother outweigh the possible harm to the fetus.

It is unknown whether rabeprazole penetrates into breast milk. Relevant studies in breastfeeding women have not been conducted. However, rabeprazole is found in the milk of lactating rats, therefore the drug should not be used in lactating women.

Similarities

Pariet, Zulbecs, Hirabezol, Rabelock, Rabeprazol, Rabiet , Irritable bowel