Ranitidine - instructions for use, dose, side effects, contraindications

Each tablet contains 150 mg of ranitidine (as hydrochloride), auxiliary substances: microcrystalline cellulose, povidone (polyvinylpyrrolidone), low molecular weight, magnesium stearate, methyl methacrylate, dimethylaminoethyl methacrylate and butyl methacrylate copolymer (Eudragit E 100), titanium dioxide, talc, macrogol- 4000 (polyethylene glycol-4000).

Description:

Tablets coated with a film coat, white or white with a creamy shade of color, round, biconvex.

Pharmacotherapeutic group:glands of the stomach secretion reducing agent - H2-histamine receptor blocker.

ATX: & nbsp

A.02.B.A Blockers of histamine H2-receptors

A.02.B.A.02 Ranitidine

Pharmacodynamics:

Blocker H2-gistaminoreceptors of the second generation. The mechanism of action is associated with blockade of H2-histamine-receptor membranes of parietal cells of the gastric mucosa.Suppresses the day and night secretion of hydrochloric acid, as well as basal and stimulated, reduces the amount of gastric juice caused by stretching the stomach food load, the action of hormones and biogenic stimulants (gastrin, histamine, acetylcholine, pentagastrin, caffeine). Reduces the amount of hydrochloric acid in the gastric juice, virtually not suppressing the "liver" enzymes associated with cytochrome P450, does not affect the concentration of gastrin in the plasma, the production of mucus. Reduces the activity of pepsin.

Does not affect the concentration of Ca²⁺ in the blood serum. After oral administration in therapeutic doses does not affect the concentration of prolactin in the blood serum.

It has no effect on the release of pituitary hormones: gonadotropin, thyroid hormone, and growth hormone. Does not affect the concentration of cortisol, aldosterone, androgens and estrogens, the motility of spermatozoa, the amount and composition of sperm, and also does not have an antiandrogenic effect. May attenuate the release of vasopressin.

Strengthens the mechanisms of protection of the gastric mucosa and promotes the healing of its damage associated with exposure HCL (incl.cessation of gastrointestinal bleeding and cicatrization of stress ulcers), by increasing the formation of gastric mucus, the content of glycoproteins in it, stimulating the secretion of hydrocarbonate by the gastric mucosa, endogenous synthesis of prostaglandins and the rate of regeneration.

In a dose of 150 mg suppresses the secretion of gastric juice for 8-2 hours. Inhibits microsomal enzymes (weaker than cimetidine).

Pharmacokinetics:

Quickly absorbed, eating does not affect the degree of absorption. When ingested 150 mg bioavailability 50%, C_max 36-94 ng / ml; TS_max - 2-Hrs .; Relationship with blood plasma proteins -15%. Poorly penetrates the blood-brain barrier; penetrates the placental barrier and into breast milk (concentration in breast milk during lactation is higher than in plasma).

It is slightly metabolized in the liver with the formation of desmethyranitidine and S- ranitidine oxide. Has the effect of "first pass" through the liver. The rate and degree of elimination depend little on the condition of the liver. The half-life period after ingestion with a normal CC-2.5 hours, with a CC of 20-30 ml / min, is 8-9 hours.

It is excreted by the kidneys 60-70% and through the intestines.

Indications:

Treatment and prevention - peptic ulcer and duodenal ulcer, NSAID-gastropathy, heartburn (associated with hyperchlorhydria), hypersecretion of gastric juice, symptomatic ulcers, stress ulcers of the gastrointestinal tract, erosive esophagitis, reflux esophagitis, Zollinger-Ellison syndrome, systemic mastocytosis, polyendocrine adenomatosis; dyspepsia characterized by epigastric or chest pain associated with eating or disturbing sleep, but not due to the above conditions; treatment of bleeding from the upper sections of the gastrointestinal tract, prevention of recurrences of gastric bleeding in the postoperative period; prevention of aspiration of gastric juice in patients undergoing general anesthesia surgery (Mendelssohn syndrome), aspiration pneumonitis (prophylaxis), rheumatoid arthritis (as an auxiliary therapy).

Contraindications:

Hypersensitivity, lactation period

Carefully:

Renal and / or hepatic insufficiency, cirrhosis of the liver with portosystemic encephalopathy (in the anamnesis), acute porphyria (including in the anamnesis), children's age (up to 12 years), pregnancy.

Dosing and Administration:

Inside. Stomach ulcer and duodenal ulcer (in the phase of exacerbation), postoperative ulcers - 150 mg 2 times a day or 300 mg at night for 4-8 weeks. In patients with untreated for this period of ulcers - continued treatment for the next 4 weeks.

Prevention of relapse - 150 mg at night; for smokers, 300 mg. NSAIDs-gastropathy - 150 mg 2 times a day or 300 mg at night for 8-12 weeks; prophylaxis - 150 mg twice a day.

Erosive reflux esophagitis - 150 mg 2 times a day or 300 mg per night for 8 weeks; if necessary, the course of treatment is extended to 12 weeks. At the Fifth Mig. the severity of the reflux esophagitis dose is increased to 600 mg / day in 4 divided doses for 12 weeks. Prolonged preventive therapy-150 mg 2 times a day.

Zollinger-Ellison syndrome-the initial dose of 150 mg 3 times a day, if necessary, up to 6 g / day.

In chronic episodes of dyspepsia - 150 mg twice a day for 6 weeks. Children for the treatment of peptic ulcer-in, 2-4 mg / kg 2 times a day; with reflux esophagitis -2-8 mg / kg 3 times a day; the maximum daily dose of 300 mg. Patients with impaired renal function require a correction of the dosing regimen. If there is concomitant liver damage, a dose reduction may be required.

Patients who are on hemodialysis, the next dose is prescribed immediately after the end of hemodialysis.

Side effects:

On the part of the digestive system are possible: nausea, dry mouth, constipation, vomiting, diarrhea, abdominal pain, increased activity of "liver" transaminases, rarely - hepatocellular, cholestatic or mixed hepatitis, acute pancreatitis. From the hematopoiesis are possible: leukopenia, thrombocytopenia, agranulocytosis, pancytopenia, neutropenia, hypo- and aplasia of the bone marrow, immune hemolytic anemia.

From the cardiovascular system are possible: lowering blood pressure, bradycardia, arrhythmia, atrioventricular blockade, vasculitis.

From the nervous system are possible: headache, dizziness, hypertension, emotional lability, anxiety, anxiety, depression, excessive fatigue, drowsiness; rarely - confusion, tinnitus, irritability, hallucinations (mainly in elderly patients and seriously ill patients), involuntary movements.

From the senses are possible: blurred vision, paresis of accommodation.

From the musculoskeletal system are possible: arthralgia, myalgia.

From the endocrine system are possible: hyperprolactinemia, gynecomastia, amenorrhea, decreased libido, decreased potency.

Allergic reactions are possible: urticaria, skin rash, angioedema, anaphylactic shock, bronchospasm, multiforme exudative erythema, including Stevens-Johnson syndrome, exfoliative dermatitis, toxic epidermal necrolysis.

Other: alopecia.

Overdose:

Symptoms: convulsions, bradycardia, ventricular arrhythmias.

Treatment is symptomatic. With the development of seizures - diazepam in / in, with bradycardias - atropine, ventricular arrhythmias - lidocaine. Hemodialysis is effective

Interaction:

Increases AUC and the concentration of metoprolol in the serum (respectively, 80% and 50%), while the half-life of metoprolol increased from 4.4 to 6.5 hours.

Reduces the absorption of itraconazole and ketoconazole.

Inhibits the metabolism in the liver of phenazone, aminophenazone, diazepam, lidocaine, phenytoin, theophylline, aminophylline, indirect anticoagulants, glipizide, buformin, metronidazole, BCCC.

Antacids, sucralfate slow the absorption of ranitidine (with the simultaneous use of a break between the intake of antacids and ranitidine should be at least 1-2 hours).

Drugs that depress the bone marrow increase the risk of neutropenia.

Smoking reduces the effectiveness of ranitidine.

Special instructions:

Ranitidine treatment can mask the symptoms associated with carcinoma of the stomach, so before starting treatment it is necessary to exclude the presence of malignant neoplasm.

Ranitidine, like everyone else H2-histaminoblockers, it is undesirable to abruptly cancel ("ricochet syndrome").

With long-term treatment of weakened patients under stress, bacterial lesions of the stomach are possible with the subsequent spread of infection. Blockers H₂-gistaminoreceptors should be taken 2 hours after taking itraconazole or ketoconazole in order to avoid a significant reduction in their absorption. May be the cause of a false positive reaction when carrying out a sample for protein in the urine.

Blockers H2-gistaminoreceptors can counteract the influence of pentagastrin and histamine on the acid-forming function of the stomach, therefore, within 24 hours preceding the test, use blockers H2-gistaminoreceptors is not recommended.

Blockers H2-histaminoreceptors can suppress the skin reaction to histamine, thus leading to false negative results (before conducting diagnostic skin tests to detect an allergic skin reaction of immediate type, the use of blockers H2-histaminoreceptors it is recommended to stop).

During treatment, avoid eating foods, beverages and other medications that can cause irritation of the gastric mucosa.

During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions.

Effect on the ability to drive transp. cf. and fur:During the treatment period, care must be taken when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets, film-coated 150 mg. For 10 tablets in a planar cell package.2 contour mesh packs together with instructions for use are placed in a pack of cardboard.

Packaging:For 10 tablets in a planar cell package. 2 contour mesh packages together with instructions for use are placed in a pack of cardboard

Storage conditions:

In a dry, dark place, at a temperature of no higher than 25 ⁰ C. Keep out of reach of children.

Shelf life:3 years. Do not use after the expiry date stated on the package

Terms of leave from pharmacies:Without recipe

Registration number:LSR-007987/08

Date of registration:09.10.2008

The owner of the registration certificate:TATHIMFARMPREPARATY, JSC TATHIMFARMPREPARATY, JSC Russia

Manufacturer: & nbsp

TATHIMFARMPREPARATY, JSC Russia

Information update date: & nbsp09.10.2008

Illustrated instructions

Instructions

Ranitidine (Ranitidine)