Composition, form of production and packaging
The tablets covered with a cover of white color, round, biconcave, with engraving "GX EC2" on the one hand.
1 tab.
ranitidine (in the form of hydrochloride) 150 mg
Excipients: microcrystalline cellulose, magnesium stearate, methylhydroxypropylcellulose, titanium dioxide, triacetin.
10 pieces. - blisters (2) - packs of cardboard.
The tablets covered with a cover of white color, oval, biconcave, with engraving "GX EC3" on the one hand.
1 tab.
ranitidine (in the form of hydrochloride) 300 mg
Excipients: microcrystalline cellulose, magnesium stearate, sodium croscarmellose, methylhydroxypropylcellulose, titanium dioxide, triacetin.
10 pieces. - blisters (1) - packs of cardboard.
The tablets are effervescent round, flat, with beveled edges, from light yellow to almost white.
1 tab.
ranitidine (in the form of hydrochloride) 150 mg
Excipients: sodium monocitrate anhydrous, sodium hydrogen carbonate, aspartame, povidone K30, sodium benzoate, orange flavor, grapefruit flavor (sodium content 14.3 mEq (328 mg) / 1 tab.)
6 pcs. - blisters of aluminum (1) - packs of cardboard.
6 pcs. - blisters from aluminum (2) - packs cardboard.
10 pieces. - blisters of aluminum (1) - packs of cardboard.
10 pieces. - blisters from aluminum (2) - packs cardboard.
15 pcs. - polypropylene tubes (1) - cardboard packs.
The tablets are effervescent round, flat, with beveled edges, from light yellow to almost white.
1 tab.
ranitidine (in the form of hydrochloride) 300 mg
Excipients: sodium monocitrate anhydrous, sodium hydrogen carbonate, aspartame, povidone K30, sodium benzoate, orange flavor, grapefruit flavor (sodium content 20.8 mEq (479 mg) / 1 tab.).
6 pcs. - blisters of aluminum (1) - packs of cardboard.
6 pcs. - blisters from aluminum (2) - packs cardboard.
10 pieces. - blisters of aluminum (1) - packs of cardboard.
10 pieces. - blisters from aluminum (2) - packs cardboard.
15 pcs. - polypropylene tubes (1) - cardboard packs.
The injection solution is clear, colorless or light yellow in color.
1 ml of 1 amp.
ranitidine (in the form of hydrochloride) 25 mg 50 mg
Excipients: sodium chloride, potassium dihydroorthophosphate, sodium hydroorthophosphate, disubstituted anhydrous, nitrogen, water d / u.
2 ml - ampoules (5) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The description of the drug was approved by the manufacturer for the 2006 print edition.
PHARMACHOLOGIC EFFECT
The blocker of histamine H 2 -receptors. Reduces the basal and stimulated by stimulation of baroreceptors, food load, the action of histamine, gastrin and other biogenic stimulants secretion of hydrochloric (hydrochloric) acid.
Reduces both the amount of secretion and the content of hydrochloric acid (hydrochloric acid) and pepsin in it. Promotes an increase in the pH of gastric contents, which leads to a decrease in the activity of pepsin. The duration of action of ranitidine after a single dose is 12 hours.
Helicobacter pylori is defined in approximately 95% of patients with duodenal ulcers and in 80% of patients with gastric ulcers. When ranitidine is combined with amoxicillin and metronidazole, eradication of Helicobacter pylori occurs in approximately 90% of cases. This combination of drugs significantly reduces the frequency of exacerbations of duodenal ulcer.
PHARMACOKINETICS
Suction
When administered orally, the bioavailability of ranitidine is approximately 50%. After ingestion of the drug in a dose of 150 mg C max is achieved after 2-3 hours and is 300-550 ng / ml.
After the / m administration, C max is reached within 15 minutes after administration and is 300-500 ng / ml.
Distribution
Binding to plasma proteins does not exceed 15%. Ranitidine penetrates the placental barrier. Excreted in breast milk (concentration in breast milk is higher than in plasma). Badly penetrates the BBB.
Metabolism
Not subjected to intensive metabolism. The metabolism of ranitidine does not differ with parenteral administration and ingestion and proceeds with the formation of small amounts of N-oxide (6%), S-oxide (2%), desmethylaritidine (2%) and furoic acid analogue (1-2%).
Excretion
T 1/2 is 2-3 hours.
After taking 3 H-ranitidine in a dose of 150 mg, 60-70% of the drug is excreted in the urine and 26% - with feces; 35% of the dose taken is excreted unchanged in the urine.
After intravenous administration of 3 H-ranitidine in a dose of 150 mg, 93% of the drug is excreted in the urine and 5% - with feces; in the first 24 hours 70% of the dose is excreted unchanged in the urine.
Pharmacokinetics in special clinical cases
With pronounced disturbances of kidney function, the concentration of ranitidine in the plasma increases.
INDICATIONS
- ulcers of the duodenum and benign ulcers of the stomach, incl. associated with the administration of NSAIDs;
- prevention of duodenal ulcers caused by NSAIDs (including acetylsalicylic acid), especially in patients with a history of peptic ulcer;
- duodenal ulcers associated with infection with Helicobacter pylori;
- Postoperative ulcers;
- gastroesophageal reflux disease;
- reflux esophagitis;
- relief of pain syndrome in gastroesophageal reflux disease;
- Zollinger-Ellison syndrome;
- chronic episodic dyspepsia, characterized by epigastric or chest pain, which is associated with eating or disturbing sleep, but does not belong to the above conditions;
- prevention of stressful stomach ulcers in critically ill patients;
- prevention of recurrence of bleeding from peptic ulcers;
- Prevention of Mendelssohn syndrome (aspiration of acidic stomach contents during anesthesia).
DOSING MODE
Tablets and tablets are effervescent
Inside adults with exacerbation of duodenal ulcer and benign gastric ulcer appoint 150 mg 2 times / day or 300 mg per night. In most cases, duodenal ulcers and benign gastric ulcers heal within 4 weeks. In patients with nevrubtsevshimisya for this period of ulceration, healing usually occurs against the background of continuing treatment for the next 4 weeks. When treating duodenal ulcers, taking the drug at a dose of 300 mg 2 times / day is more effective than taking doses of 150 mg 2 times / day or 300 mg 1 time per night. Increasing the dose does not lead to an increase in the incidence of side effects.
With prolonged prophylaxis of relapses, ulcers of the duodenum and stomach are prescribed 150 mg 1 time / day (overnight). For smokers, it is more preferable to increase the dose to 300 mg per night (since smoking is associated with a higher incidence of ulcer relapses).
To treat ulcers associated with taking NSAIDs , appoint 150 mg 2 times / day or 300 mg per night for 8-12 weeks, for prevention - 150 mg 2 times / day during treatment with NSAIDs.
To treat ulcers of the duodenum associated with Helicobacter pylori, 150 mg 2 times / day (morning and evening) or 300 mg once a day (at night) in combination with amoxicillin 750 mg 3 times / day and metronidazole 500 mg 3 times / day for 2 weeks. Treatment with Zantakom should continue for another 2 weeks. This scheme significantly reduces the frequency of recurrences of duodenal ulcers.
With postoperative ulcers appoint 150 mg 2 times / day for 4 weeks. In patients with nevrubtsevshimisya for this period of ulceration, healing usually occurs against the background of continuing treatment for the next 4 weeks.
In gastroesophageal reflux disease , 150 mg 2 times / day or 300 mg per night for 8 weeks are prescribed for the treatment of acute reflux esophagitis ; If necessary, the course of treatment can be extended to 12 weeks. With a moderate and severe course of reflux esophagitis, the dose can be increased to 150 mg 4 times / day with a treatment duration of up to 12 weeks. When conducting preventive therapy with reflux-esophagitis, the recommended dose is 150 mg 2 times / day.
For relief of pain in gastroesophageal reflux disease , 150 mg 2 times / day are prescribed for 2 weeks. With insufficient effectiveness, treatment can be continued at the same dose for the next 2 weeks.
With Zollinger-Ellison syndrome, the initial dose is 150 mg 3 times / day, if necessary, the dose may be increased. Doses up to 6 g / day were tolerated well.
In chronic episodes of dyspepsia, Zantac is prescribed 150 mg 2 times / day for 6 weeks. In the absence of a positive effect of treatment, as well as in case of deterioration in the background of treatment should be a thorough examination.
To prevent bleeding from stress ulcers in severely ill patients, as well as to prevent recurrent bleeding from peptic ulcers after the patient is able to take food through the mouth, parenteral use of Zantak can be replaced by the administration of the drug inside at a dose of 150 mg 2 times / day.
To prevent the development of Mendelssohn syndrome, Zantak is prescribed at a dose of 150 mg for 2 hours before anesthesia, and also, preferably, 150 mg the night before. Perhaps parenteral application of Zantak.
For the prevention of Mendelssohn's syndrome , 150 mg are given every 6 hours during labor , but in case general anesthesia is required, water-soluble antacids (eg sodium citrate) should be used simultaneously with Zantak.
Children for the treatment of peptic ulcers recommended a dose of 2-4 mg / kg 2 times / day; the maximum daily dose is 300 mg.
In patients with severe renal insufficiency (CC less than 50 ml / min) cumulation and increased plasma concentrations of ranitidine are noted. The recommended dose is 150 mg 1 time / day.
Patients who are on long-term outpatient peritoneal dialysis or long-term hemodialysis , the drug is prescribed at a dose of 150 mg immediately after the end of the dialysis session.
The injection solution can be introduced as:
- slow (more than 2 minutes) IV injection 50 mg, which is diluted to a volume of 20 ml and injected every 6-8 hours;
- Intermittent intravenous infusion at a rate of 25 mg / h for 2 hours, with repeated administration after 6-8 hours;
- In / m injections in a dose of 50 mg every 6-8 hours.
To prevent bleeding from stress ulcers and recurrences of bleeding from the peptic ulcer in seriously ill patients, Zantak is administered at an initial dose of 50 mg in the form of a slow intravenous injection, followed by a prolonged IV infusion at a rate of 0.125-0.250 mg / kg / h. Parenteral therapy continues until the patient can not eat. Then you can go to Zantak's reception inside.
For the prevention of Mendelssohn syndrome, the recommended dose is 50 mg IM or slowly IV for 45-60 minutes before anesthesia.
Patients with renal insufficiency with CC less than 50 ml / min the recommended dose of Zantak for parenteral use is 25 mg.
SIDE EFFECT
On the part of the digestive system: nausea, dry mouth, constipation, vomiting, abdominal pain, transient and reversible changes in functional hepatic tests; in some cases - the development of hepatitis (hepatocellular, cholestatic or mixed), accompanied or not accompanied by jaundice (usually reversible); rarely - diarrhea, acute pancreatitis.
On the part of the hematopoiesis system: leukopenia, thrombocytopenia; rarely - agranulocytosis, pancytopenia, sometimes - hypo- and aplasia of the bone marrow, immune hemolytic anemia.
On the part of the cardiovascular system: lowering blood pressure, arrhythmia, bradycardia, AV blockade; rarely - vasculitis.
From the side of the central nervous system: headache (sometimes severe), dizziness, fatigue, drowsiness; rarely - irritability, noise in the ears, blurred vision, possibly associated with a change in accommodation, involuntary reversible motor disorders, involuntary movements; mainly in seriously ill patients and elderly patients - confusion, depression and hallucinations.
From the musculoskeletal system: rarely - arthralgia, myalgia.
Dermatological reactions: alopecia.
Allergic reactions: skin rash, erythema multiforme, urticaria, angioedema, anaphylactic shock, bronchospasm, arterial hypotension, fever, chest pain.
On the part of the endocrine system: hyperprolactinaemia, gynecomastia, amenorrhea, decreased libido; rarely - reversible impotence, the appearance of swelling or a feeling of discomfort in the mammary glands of men.
CONTRAINDICATIONS
- acute porphyria (including in the anamnesis);
- Pregnancy;
- lactation period (breastfeeding);
- children's age till 12 years;
- Hypersensitivity to ranitidine and other components of the drug.
With caution should prescribe the drug in renal and hepatic insufficiency, with cirrhosis of the liver with portosystemic encephalopathy in the anamnesis.
PREGNANCY AND LACTATION
Ranitidine penetrates the placenta and is excreted in breast milk (concentration in breast milk is higher than in plasma).
The use of the drug during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus.
If it is necessary to prescribe the drug during lactation, the question of stopping breastfeeding should be solved.
APPLICATION FOR FUNCTIONS OF THE LIVER
In patients with severe renal insufficiency (CC less than 50 ml / min) cumulation and increased plasma concentrations of ranitidine are noted. The recommended dose is 150 mg 1 time / day.
Patients who are on long-term outpatient peritoneal dialysis or long-term hemodialysis , the drug is prescribed at a dose of 150 mg immediately after the end of the dialysis session.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution should prescribe the drug for liver failure, with cirrhosis of the liver with portosystemic encephalopathy in history.
APPLICATION FOR CHILDREN
The drug is contraindicated for children under 12 years.
APPLICATION IN ELDERLY PATIENTS
It is necessary to regularly monitor elderly patients taking ranitidine in combination with NSAIDs.
SPECIAL INSTRUCTIONS
Treatment with Zantakom can mask the symptoms associated with carcinoma of the stomach. Therefore, in patients with gastric ulcers (and in patients of middle and advanced age when changing or appearing new symptoms of dyspepsia), before starting treatment with Zantak it is necessary to exclude the possibility of malignancy.
The drug should not be abruptly abolished, there is a risk of a syndrome of "bounce".
With long-term treatment of weakened patients under stress, bacterial lesions of the stomach are possible with the subsequent spread of infection.
It is necessary to regularly monitor patients (especially the elderly and patients with a history of peptic ulcer disease) who take ranitidine in combination with NSAIDs.
There have been isolated reports that ranitidine may contribute to the development of an acute attack of porphyria, and therefore it is necessary to avoid its use in patients with acute porphyria in the anamnesis.
Zantac's effervescent tablets contain sodium, so caution should be exercised in the treatment of patients who show a restriction on sodium intake.
In connection with the fact that Zantak effervescent tablets contain aspartame, they should be used with caution in patients with phenylketonuria.
It is known about rare cases of bradycardia with rapid parenteral administration of Zantac, which was usually observed in patients with predisposing factors to the development of cardiac arrhythmias. Do not exceed the recommended rate of drug administration.
It should be noted that ranitidine is excreted through the kidneys, and therefore the level of the drug in the plasma increases with renal failure of severe degree.Therefore, it is necessary to adjust the dosing regimen.
When parenteral administration of the drug in high doses more than 5 days, an increase in the activity of hepatic enzymes may be observed.
Zantac should be taken 2 hours after taking itraconazole or ketoconazole in order to avoid a significant decrease in their absorption.
Against the background of taking the drug may increase the activity of glutamate transpeptidase.
Receiving Zantaka can cause a false positive response to a sample for the presence of protein in the urine.
The blockers of histamine H 2 receptors (including Zantac) can counteract the effects of pentagastrin and histamine on the acid-forming function of the stomach, so it is not recommended to use Zantac for 24 hours prior to the test.
The blockers of histamine H 2 -receptors can suppress the skin reaction to histamine, thus leading to false negative results. Therefore, before performing diagnostic skin tests to detect an allergic skin reaction of the immediate Zantac type, it should be discarded.
During treatment, avoid eating foods, beverages and other medications that can cause irritation of the gastric mucosa.
Smoking reduces the effectiveness of Zantak.
Unused mixtures should be disposed of within 24 hours after preparation.
Since compatibility studies of solutions were carried out only in polyvinyl chloride infusion packets (in glass for sodium bicarbonate) and polyvinyl chloride systems, it is assumed that adequate stability can be achieved with the use of polyethylene bags.
Use in Pediatrics
Safety and effectiveness of Zantac in children under the age of 12 years are not established.
Impact on the ability to drive vehicles and manage mechanisms
During the period of Zantak drug intake, it is necessary to refrain from practicing potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.
OVERDOSE
Symptoms: convulsions, bradycardia, ventricular arrhythmias.
Treatment: conduct symptomatic therapy; with the development of convulsions - diazepam iv, with bradycardia and ventricular arrhythmias - enter atropine, lidocaine.Ranitidine can be removed from the plasma during hemodialysis.
DRUG INTERACTION
With the simultaneous use of Zantac with antacids, sucralfate in high doses (2 g), a violation of the absorption of ranitidine is possible, so the interval between doses of these drugs should be at least 2 hours.
With the simultaneous administration of Zantak and drugs that depress the bone marrow, the risk of developing neutropenia increases.
Zantak does not suppress the activity of cytochrome P 450 isoenzymes, so it does not enhance the effects of drugs metabolized with the participation of this enzyme system, such as diazepam, lidocaine, phenytoin, propranolol, theophylline, warfarin.
Ranitidine inhibits the metabolism of phenazone, aminophenazone, hexobarbital, indirect anticoagulants, glipizide, buformin, calcium antagonists.
Because of increasing pH of stomach contents while receiving with Zantac may decrease the absorption of itraconazole and ketoconazole.
At reception on the background Zantac increased AUC and concentration of metoprolol in the blood serum (respectively 80% and 50%), while T 1/2 metoprolol increased from 4.4 to 6.5 hours.
There was no interaction ranitidine with metronidazole and amoxicillin.
Pharmaceutical interaction
Zantac Injection solution suitable for infusion solutions: 0.9% sodium chloride solution, 5% dextrose, 0.18% chloride and 4% sodium solution dextrose solution, 4.2% sodium bicarbonate solution, Hartman solution.
TERMS AND CONDITIONS OF STORAGE
Tablets should be stored in reach of children at a temperature not higher than 30 В° C. It is tightly closed with a cover tube effervescent tablets.
Shelf life 150 mg tablets - 5 years, tablets 300 mg - 3 years, effervescent tablets - 2 years.
A solution for injection should be stored in reach of children at a temperature not higher than 25 В° C. Shelf life - 3 years.
Conditions of leave from pharmacies
The drug is released by prescription.
