Zantak

General characteristics. Structure:

Tablets, coated white color, round, biconvex, with the engraving "GX EC2" about one Active ingredient: ranitidine (in the form of a hydrochloride) 150 mg

Excipients: cellulose microcrystallic, magnesium stearate, methylhydroxypropyl cellulose, titanium dioxide, triacetin.

Tablets, coated white color, oval, biconvex, with the engraving "GX EC3" on the one hand.

Active ingredient: ranitidine (in the form of a hydrochloride) 300 mg

Excipients: cellulose microcrystallic, magnesium stearate, sodium of a kroskarmelloz, methylhydroxypropyl cellulose, titanium dioxide, triacetin.

Tablets are sparkling round, flat, with slanted edges, from light yellow till almost white color.

Active ingredient: ranitidine (in the form of a hydrochloride) 150 mg

Excipients: sodium monocitrate anhydrous, Natrii hydrocarbonas, aspartame, K30 povidone, Natrium benzoicum, orange fragrance, grapefruit fragrance (content of sodium 14.3 Mack (328 mg) of/1 tablet)

Tablets are sparkling round, flat, with slanted edges, from light yellow till almost white color.

Active ingredient: ranitidine (in the form of a hydrochloride) 300 mg

Excipients: sodium monocitrate anhydrous, Natrii hydrocarbonas, aspartame, K30 povidone, Natrium benzoicum, orange fragrance, grapefruit fragrance (content of sodium 20.8 Mack (479 mg) of/1 tablet).

Solution for injections transparent, colourless or light yellow color.

Active ingredient: ranitidine (in the form of a hydrochloride) 25 mg 50 mg

Excipients: sodium chloride, potassium dihydroortho-phosphate, sodium hydroortho-phosphate disubstituted anhydrous, nitrogen, water for and.

Pharmacological properties:

Blocker histamine H2 receptors. Reduces basal and stimulated irritation of baroreceptors, food loading, action of a histamine, gastrin and other biogenic stimulators secretion of hydrochloric (hydrochloric) acid.

Reduces both the secret volume, and contents in it hydrochloric (hydrochloric) acid and pepsin. Promotes increase рН gastric contents that leads to pepsin decrease of the activity. Duration of effect of ranitidine after a single dose - 12 h.

Helicobacter pylori decides approximately at 95% of patients on ulcers of a duodenum and at 80% of patients on stomach ulcers. At a ranitidine combination to amoxicillin and metronidazole approximately in 90% of cases Helicobacter pylori eradikation is noted. Such combination of drugs considerably reduces the frequency of aggravations of a peptic ulcer of a duodenum.

Pharmacokinetics. Absorption

At intake bioavailability of ranitidine makes about 50%. After intake of drug in a dose of 150 mg of Cmax it is reached in 2-3 h and makes 300-550 ng/ml.

After introduction in oil Cmax is reached within 15 min. after introduction and makes 300-500 ng/ml.

Distribution

Linkng with proteins of plasma does not exceed 15%. Ranitidine gets through a placental barrier. It is allocated with breast milk (concentration in breast milk higher, than in plasma). Badly gets through GEB.

Metabolism

Is not exposed to intensive metabolism. Metabolism of ranitidine does not differ at parenteral administration and at intake and the desmetilranitidina (2%) and an analog of furoyevy acid (1-2%) proceeds with formation of small amounts of N-oxide (6%), S-oxide (2%).

Removal

T1/2 makes 2-3 h.

After reception of 3H-ranitidine in a dose of 150 mg of 60-70% of drug also 26% - with a stake are removed with urine; and 35% of the accepted dose are removed with urine in not changed look.

Later in/in administrations of 3H-ranitidine in a dose of 150 mg of 93% of drug also 5% - with a stake are allocated with urine; in the first 24 h 70% of the accepted dose it is removed with urine in not changed look.

Pharmacokinetics in special clinical cases

At the expressed renal failures concentration of ranitidine in plasma increases.

Indications to use:

— ulcers of a duodenum and benign stomach ulcers, including connected with reception of NPVS;

— prevention of the ulcers of a duodenum caused by NPVS (including acetylsalicylic acid), especially at patients with a peptic ulcer in the anamnesis;

— the duodenum ulcers connected with infection of Helicobacter pylori;

— postoperative ulcers;

— gastroesophageal reflux disease;

— reflux esophagitis;

— stopping of a pain syndrome at a gastroesophageal reflux disease;

— Zollingera-Ellison's syndrome;

— the chronic incidental dyspepsia which is characterized by epigastric or retrosternal pains which are connected with meal or interrupt a sleep, but do not treat above-mentioned states;

— prevention of stressful stomach ulcers at seriously ill patients of patients;

— prevention of a recurrence of bleeding from round ulcers;

— prevention of a syndrome of Mendelssohn (aspiration of acid contents of a stomach during an anesthesia).

Route of administration and doses:

Tablets and tablets sparkling

Inside the adult at an exacerbation of an ulcer of a duodenum and benign stomach ulcer appoint on 150 mg 2 or 300 mg to night. In most cases ulcers of a duodenum and benign stomach ulcers heal within 4 weeks. At patients healing usually happens to the ulcers which did not cicatrize for this term against the background of continuation of treatment within the next 4 weeks. At treatment of an ulcer of a duodenum administration of drug in a dose of 300 mg 2 is more effective, than reception of doses on 150 mg of 2 or 300 mg of 1 times for the night. Increase in a dose does not lead to increase in frequency of emergence of side effects.

At long prevention of a recurrence of ulcers of a duodenum and stomach appoint 150 mg of 1 times / (to night). Increase in a dose up to 300 mg for the night is more preferable to the smoking patients (since smoking is associated with the bigger frequency of a recurrence of ulcers).

For treatment of the ulcers connected with reception of NPVS appoint on 150 mg 2 or 300 mg to night within 8-12 weeks, for prevention - on 150 mg 2 during treatment of NPVS.

For treatment of the ulcers of a duodenum associated with Helicobacter pylori appoint on 150 mg 2 (in the morning and in the evening) or 300 mg of 1 times / (to night) in combination with amoxicillin in a dose of 750 mg 3 and metronidazole of 500 mg 3 within 2 weeks. Treatment by Zantak has to continue within the next 2 weeks. This scheme considerably reduces the frequency of a recurrence of ulcers of a duodenum.

At postoperative ulcers appoint on 150 mg 2 within 4 weeks. At patients healing usually happens to the ulcers which did not cicatrize for this term against the background of continuation of treatment within the next 4 weeks.

At a gastroesophageal reflux disease for treatment acute the reflux esophagitis is appointed on 150 mg of 2 or 300 mg to night within 8 weeks; if necessary the course of treatment can be prolonged up to 12 weeks. At a medium-weight and heavy current a reflux esophagitis the dose can be increased to 150 mg 4 lasting treatment up to 12 weeks. When performing preventive therapy at a reflux esophagitis the recommended dose makes 150 mg 2

For stopping of a pain syndrome at a gastroesophageal reflux disease appoint on 150 mg 2 within 2 weeks. At insufficient efficiency treatment can be continued in the same dose within the next 2 weeks.

At Zollingera-Ellison's syndrome the initial dose makes 150 mg 3, if necessary the dose can be increased. Doses to 6 g / were transferred well.

At chronic episodes of dyspepsia Zantak appoint on 150 mg 2 within 6 weeks. In case of lack of positive effect from treatment, and also in case of an aggravation of symptoms against the background of treatment it is necessary to conduct careful examination.

For prevention of bleedings from stressful ulcers at seriously ill patients of patients, and also for prevention of recurrent bleedings from round ulcers after the patient is able to eat food through a mouth, parenteral use of Zantak can be replaced with purpose of drug inside in a dose of 150 mg 2

For prevention of development of a syndrome of Mendelssohn appoint Zantak in a dose 150 mg for 2 h to an anesthesia, and also, it is desirable, 150 mg the night before. Perhaps parenteral use of Zantak.

For prevention of a syndrome of Mendelssohn to women in labor at the time of delivery appoint on 150 mg in each 6 h, but if carrying out the general anesthesia is required, then before it it is necessary to apply water-soluble antacids along with Zantak (for example, sodium citrate).

The dose of 2-4 mg/kg 2 is recommended to children for treatment of a round ulcer; the maximum daily dose - 300 mg.

At patients with a renal failure of heavy degree (KK less than 50 ml/min.) notes cumulation and increase in plasma concentration of ranitidine. The recommended dose makes 150 mg of 1 times /

The patient who is on long out-patient peritoneal dialysis or on a long hemodialysis, drug appoint in a dose 150 mg right after the end of a session of dialysis.

Solution for injections can be entered in a look:

— slow (over 2 min.) in/in an injection in a dose of 50 mg which gets divorced up to the volume of 20 ml and is entered each 6-8 h;

— intermittent in/in infusion with a speed of 25 mg/h during 2 h, with repeated introduction in 6-8 h;

— injections in oil in a dose of 50 mg each 6-8 h.

For prevention of bleeding from stressful ulcers and a recurrence of bleedings from a round ulcer at seriously ill patients of patients Zantak enter in an initial dose 50 mg in the form of slow into injections, and then carry out long to infusion with a speed of 0.125-0.250 mg/kg/h. Parenteral therapy continues until the patient is not able to eat food. Further transition to Zantak's reception inside is possible.

For prevention of a syndrome of Mendelssohn the recommended dose makes 50 mg in oil or slowly in/in in 45-60 min. prior to anesthesia.

To patients with a renal failure at KK less than 50 ml/min. the recommended Zantak's dose for parenteral use - 25 mg.

Features of use:

Treatment by Zantak can mask the symptoms connected with a stomach carcinoma. Therefore at patients with stomach ulcer (and at patients of middle and advanced age at change or emergence of new symptoms of dyspepsia) before an initiation of treatment Zantak it is necessary to exclude a possibility of a malignancy.

Drug should not be cancelled sharply, there is a danger of emergence of a syndrome of "ricochet".

At prolonged treatment of the weakened patients in the conditions of a stress bacterial damages of a stomach with the subsequent spread of an infection are possible.

Regular observation of the patients (especially elderly and sick with a peptic ulcer in the anamnesis) accepting ranitidine in combination with NPVS is necessary.

There are separate messages that ranitidine can promote development of a bad attack of a porphyria in this connection it is necessary to avoid its use for patients with an acute porphyria in the anamnesis.

Sparkling tablets Zantak contain sodium therefore it is necessary to be careful at treatment of patients to which sodium reception restriction is shown.

Because sparkling tablets Zantak contain aspartame, they should be applied with care at patients with a fenilketonuriya.

It is known of exceptional cases of bradycardia at bystry parenteral administration of Zantak that was usually observed at patients with the contributing factors to development of disturbances of a cordial rhythm. It is not necessary to exceed the recommended drug rate of administering.

It is necessary to consider that ranitidine is removed through kidneys and therefore drug level in plasma increases at a renal failure of heavy degree. Therefore it is necessary to adjust the dosing mode.

At parenteral administration of drug in high doses more than 5 days increase in activity of liver enzymes can be observed.

Zantak it is necessary to accept in 2 h after reception of an itrakonazol or a ketokonazol in order to avoid considerable reduction of their absorption.

Against the background of administration of drug activity of a glutamattranspeptidaza can increase.

Zantak's reception can be the cause of false positive reaction to conducting test on availability of protein in urine.

Blockers histamine H2 receptors (including Zantak) can counteract influence of Pentagastrinum and histamine on acid-forming function of a stomach therefore during 24 h preceding the test it is not recommended to apply Zantak.

Blockers histamine H2 receptors can suppress skin reaction to a histamine, resulting thus in false-negative results. Therefore before conducting diagnostic skin tests for identification of allergic skin reaction of immediate type Zantak it is necessary to cancel.

During treatment it is necessary to avoid the use of food stuffs, drinks and other medicines which can cause irritation of a mucous membrane of a stomach.

Smoking reduces efficiency of use of Zantak.

Unused mixes have to be destroyed during 24 h after preparation.

As researches on compatibility of solutions were conducted only in polyvinyl chloride infusional packages (in glass for sodium bicarbonate) and polyvinyl chloride systems, it is supposed that adequate stability can be reached also at use of plastic bags.

Use in pediatrics

Safety and efficiency of use of Zantak for children aged up to 12 years are not established.

Influence on ability to driving of motor transport and to control of mechanisms

During administration of drug Zantak it is necessary to refrain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions.

Side effects:

From the alimentary system: nausea, dryness in a mouth, a lock, vomiting, abdominal pains, passing and reversible changes of functional hepatic tests; in some cases - development of the hepatitis (hepatocellular, cholestatic or mixed) which is followed or not followed by jaundice (as a rule, reversible); seldom - diarrhea, acute pancreatitis.

From system of a hemopoiesis: leukopenia, thrombocytopenia; seldom - an agranulocytosis, a pancytopenia, sometimes - hypo - and a marrow aplasia, immune hemolitic anemia.

From cardiovascular system: decrease in the ABP, arrhythmia, bradycardia, AV blockade; seldom - a vasculitis.

From TsNS: headache (sometimes strong), dizziness, increased fatigue, drowsiness; seldom - irritability, a sonitus, the sight illegibility which is perhaps connected with accommodation change, involuntary reversible motive disturbances, the involuntary movements; preferential at seriously ill patients and elderly patients - confusion of consciousness, a depression and hallucination.

From a musculoskeletal system: seldom - an arthralgia, a mialgiya.

Dermatological reactions: alopecia.

Allergic reactions: skin rash, multiformny erythema, small tortoiseshell, Quincke's disease, acute anaphylaxis, bronchospasm, arterial hypotension, fever, thorax pains.

From endocrine system: giperprolaktinemiya, gynecomastia, amenorrhea, decrease in a libido; seldom - reversible impotence, emergence of swelling or a sensation of discomfort in chest glands at men.

Interaction with other medicines:

At simultaneous use of Zantak with antacids, sukralfaty in high doses (2 g) ranitidine absorption disturbance therefore the interval between receptions of these drugs has to make not less than 2 h is possible.

At the concomitant use of Zantak and drugs oppressing marrow the risk of development of a neutropenia increases.

Zantak does not suppress activity of isoenzymes of system of P450 cytochrome therefore it does not strengthen effect of the drugs which are metabolized with the participation of this fermental system such as diazepam, lidocaine, Phenytoinum, propranolol, theophylline, warfarin.

Ranitidine oppresses metabolism of phenazone, Aminophenazonum, hexobarbital, indirect anticoagulants, a glipizida, Buforminum, antagonists of calcium.

Owing to increase in pH of contents of a stomach at a concomitant use with Zantak absorption of an itrakonazol and ketokonazol can decrease.

At reception against the background of Zantak AUC and concentration of a metoprolol in blood serum increases (respectively by 80% and 50%), at this T1/2 of a metoprolol raises from 4.4 to 6.5 h.

Interaction of ranitidine with metronidazole and amoxicillin is noted.

Pharmaceutical interaction

Zantak's solution for injections is compatible to the following infusion solutions: 0.9% solution of sodium of chloride, 5% solution of a dextrose, 0.18% solution of sodium of chloride and 4% solution of a dextrose, 4.2% sodium bicarbonate solution, Hartman's solution.

Contraindications:

— an acute porphyria (including in the anamnesis);

— pregnancy;

— period of a lactation (breastfeeding);

— children's age up to 12 years;

— hypersensitivity to ranitidine and other components of drug.

With care it is necessary to appoint drug at a renal and liver failure, at cirrhosis with portosistemny encephalopathy in the anamnesis.

Use of the drug ZANTAK® at pregnancy and feeding by a breast

Ranitidine gets through a placenta and is emitted with breast milk (concentration in breast milk higher than in plasma).

Use of drug at pregnancy is possible only in that case when the estimated advantage for mother exceeds potential risk for a fruit.

In need of purpose of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Use at abnormal liver functions
With care it is necessary to appoint drug at a liver failure, at cirrhosis with portosistemny encephalopathy in the anamnesis.

Use at renal failures
At patients with a renal failure of heavy degree (KK less than 50 ml/min.) notes cumulation and increase in plasma concentration of ranitidine. The recommended dose makes 150 mg of 1 times /

The patient who is on long out-patient peritoneal dialysis or on a long hemodialysis, drug appoint in a dose 150 mg right after the end of a session of dialysis.

Use for elderly patients
Regular observation of the elderly patients accepting ranitidine in combination with NPVS is necessary.

Use for children
Drug is contraindicated to children up to 12 years.

Overdose:

Symptoms: spasms, bradycardia, ventricular arrhythmias.

Treatment: carry out symptomatic therapy; at development of spasms - diazepam in/in, at bradycardia and ventricular arrhythmias - is entered by atropine, lidocaine. Ranitidine can be removed from plasma at a hemodialysis.

Storage conditions:

Tablets should be stored in the place, unavailable to children, at a temperature not above 30 °C. It is necessary to close densely a cover a tuba with sparkling tablets.

Period of validity of tablets of 150 mg - 5 years, tablets of 300 mg - 3 years, tablets sparkling - 2 years.

Solution for injections should be stored in the place, unavailable to children, at a temperature not above 25 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

10 - blisters (2) - packs cardboard.
10 - blisters (1) - packs cardboard.

6 - blisters from aluminum (1) - packs cardboard.
6 - blisters from aluminum (2) - packs cardboard.
10 - blisters from aluminum (1) - packs cardboard.
10 - blisters from aluminum (2) - packs cardboard.
15 - polypropylene (1) - packs cardboard.

2 ml - ampoules (5) - packs cardboard.