Ranitidine

General characteristics. Structure:

Active agent: ranitidine a hydrochloride — 168 mg, in terms of ranitidine — 150 mg.

Excipients (kernel): cellulose microcrystallic — 83,76 mg, potato starch — 28,0 mg, magnesium stearate — 3,0 mg, silicon dioxide colloid — 1,0 mg, povidone (polyvinylpirrolidone) — 16,24 mg.

Excipients (cover): gipromello-for — 5,217 mg, a macrogoal — 1,742 mg, titanium dioxide — 2,781 mg, talc — 0,26 mg.

Pharmacological properties:

Ranitidine is an antagonist histamine H2 receptors of covering cells of a mucous membrane of a stomach. Reduces the basal and stimulated secretion of hydrochloric acid caused by irritation of baroreceptors, food loading, effect of hormones and biogenic stimulators (gastrin, a histamine, Pentagastrinum). Ranitidine reduces the volume of a gastric juice and content of hydrochloric acid in it, raises рН stomach contents that leads to pepsin decrease of the activity. After oral administration in therapeutic doses does not influence prolactin level. Inhibits microsomal enzymes. Action duration after a single dose till 12 o'clock.

Pharmacokinetics. It is quickly soaked up, meal does not influence extent of absorption. At intake bioavailability of ranitidine makes about 50%. The maximum concentration in plasma are reached in 2-3 hours after reception. Linkng with proteins of plasma does not exceed 15%. It is slightly metabolized in a liver with formation of a desmetilranitidin and S-oxide of ranitidine. Has effect of "the first passing" through a liver. Speed and extent of elimination depend on a condition of a liver a little.
Elimination half-life after intake — 2,5 hours, at clearance of creatinine of 20-30 ml/min. — 8-9 hours. The insignificant quantity — with a stake is removed generally with urine in an invariable look. Badly gets through a blood-brain barrier. Gets through a placenta. It is allocated with breast milk (concentration in breast milk at women in the period of a lactation higher, than in plasma).

Indications to use:

Treatment and prevention of aggravations of a peptic ulcer of a stomach and duodenum; stomach ulcer and a 12-perstny gut, connected with reception of non-steroidal anti-inflammatory drugs (NPVP); reflux esophagitis, erosive esophagitis; Zollingera-Ellison's syndrome; treatment and prevention of postoperative, "stressful" ulcers of upper parts of digestive tract; prevention of a recurrence of bleedings from upper parts of digestive tract; prevention of aspiration of a gastric juice at operations under the general anesthesia (Mendelssohn's syndrome).

Route of administration and doses:

Ranitidine is accepted irrespective of meal, without chewing, washing down with a small amount of liquid.
Adults and children are more senior than 12 years: Peptic ulcer of a stomach and 12-perstny gut. For baking of aggravations appoint 0,15 g 2 times a day (in the morning and in the evening) or 0,3 g to night. If necessary — on 0,3 g 2 times a day. Baking course duration — 4-8 weeks. For prevention of aggravations appoint 0,15 g to night.
The ulcers connected with reception of NPVP. Appoint 0,15 g 2 times a day or 0,3 g to night within 8-12 weeks. Prevention of formation of ulcers at reception of NPVP — on 0,15 g 2 times a day.
Postoperative "stressful" ulcers. Appoint 0,15 g 2 times a day within 4-8 weeks. Reflux esophagitis, erosive esophagitis. Appoint 0,15 g 2 times a day or 0,3 g to night. If necessary the dose can be increased to 0,15 g 4 times a day. Course of treatment of 8-12 weeks.
Zollingera-Ellison's syndrome. The initial dose makes 0,15 g 3 times a day, if necessary the dose can be increased.
Prevention of recurrent bleedings. On 0,15 g 2 times a day.
Prevention of development of a syndrome of Mendelssohn. Appoint in a dose 0,15 g in 2 hours prior to an anesthesia, and also, 0,15 g the night before are desirable. In the presence of the accompanying abnormal liver function the dose decline can be required. The patient with a renal failure at clearance of creatine less than 50 ml/min. the recommended dose makes 0,15 g a day.
The patient who is on a hemodialysis, the next dose is appointed right after the termination of a hemodialysis.

Features of use:

Treatment by ranitidine can mask the symptoms connected with a stomach carcinoma therefore before an initiation of treatment it is necessary to exclude existence of cancer ulcer.
Ranitidine, as well as all H2-gistaminoblokatory, is undesirable to cancel sharply (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.
Safety and efficiency of ranitidine at children are younger than 12 years are not established. There are data that ranitidine can cause bad attacks of a porphyria.
During treatment it is necessary to abstain from occupations potentially dangerous types of activity demanding the increased concentration of attention and speed of psychomotor reactions. Blockers H2-gistaminoretseptorov should be accepted in 2 hours after reception of an itrakonazol or a ketokonazol in order to avoid considerable reduction of their absorption.
Can increase activity of a glutamattranspeptidaza. Can be the cause of false positive reaction to carrying out an albumin test in urine. Blockers H2-gistaminoretseptorov can counteract influence of Pentagastrinum and histamine on acid-forming function of a stomach therefore within 24 hours preceding the test it is not recommended to apply blockers H2-gistaminoretseptorov. Symptoms of a peptic ulcer of a 12-perstny gut can disappear within 1-2 weeks, therapy should be continued until scarring is not confirmed with data of an endoscopic or X-ray analysis.
Efficiency of drug in inhibition of night secretion of acid in a stomach can decrease as a result of smoking.
Ranitidine increases the level of creatinine, gamma глутамилтрансферазы (GGT) and transaminases in blood serum.
Blockers H2-gistaminoretseptorov can suppress skin reaction to a histamine, resulting, thus in false positive results (before conducting diagnostic skin tests for identification of allergic skin reaction of immediate type use of blockers H2-gistaminoretseptorov is recommended to be stopped).
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.

Side effects:

- From the alimentary system: nausea, dryness in a mouth, a lock, vomiting, diarrhea, abdominal pains; seldom — the hepatocellular, cholestatic or mixed hepatitis, acute pancreatitis.
- From bodies of a hemopoiesis: a leukopenia, thrombocytopenia, an agranulocytosis, a pancytopenia, hypo - and a marrow aplasia, immune hemolitic anemia, a neutropenia.
- From cardiovascular system: lowering of arterial pressure, bradycardia, arrhythmia, atrioventricular block, tachycardia, vasculitis.
- From a nervous system: increased fatigue, drowsiness, headache, dizziness, hyperthermia, concern, alarm, depression; seldom — confusion of consciousness, a sonitus, irritability, hallucinations (generally at elderly patients and heavy patients), the involuntary movements.
- From sense bodys: illegibility of visual perception, accommodation paresis.
- From a musculoskeletal system: arthralgia, mialgiya.
- From endocrine system: giperprolaktinemiya, gynecomastia, amenorrhea, decrease in a libido, impotence.
- Allergic reactions: urticaria, skin rash, Quincke's disease, acute anaphylaxis, bronchospasm, multiformny erythema, toxic epidermal necrolysis.
- Other: alopecia, giperkreatininemiya.

Interaction with other medicines:

Smoking reduces efficiency of ranitidine. Increases AUC and concentration of a metoprolol in blood serum (respectively by 80% and 50%), at this T1/2 of a metoprolol raises from 4,4 to 6,5 h. Owing to increase рН stomach contents at a concomitant use absorption of an itrakonazol and ketokonazol can decrease. Metabolism in a liver of phenazone, Aminophenazonum, diazepam, hexobarbital, propranolol, diazepam, lidocaine, Phenytoinum, theophylline, Aminophyllinum, indirect anticoagulants, a glipizida, Buforminum, metronidazole, antagonists of calcium oppresses. The medicines oppressing marrow increase risk of a neutropenia.
At simultaneous use with antacids, sou-kralfatom in high doses ranitidine absorption delay therefore the break between reception of these drugs has to be not less than 2 hours is possible.

Contraindications:

Hypersensitivity to ranitidine or other components of drug. Pregnancy, lactation. Children's age up to 12 years.

With CARE — a renal and/or liver failure, cirrhosis with portosistemny encephalopathy in the anamnesis, an acute porphyria (including in the anamnesis), immunity oppression.

Overdose:

Symptoms: spasms, bradycardia, ventricular arrhythmias.
Treatment: symptomatic. At development of spasms — diazepam in/in, at bradycardia or ventricular arrhythmias — atropine, lidocaine. The hemodialysis — is effective.

Storage conditions:

List B. To store in the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children.

Issue conditions:

According to the recipe

Packaging:

Tablets, film coated, on 150 mg. On 10 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished
On 10, 20, 30 tablets in a container polymeric. The free space in a container is filled with hygroscopic medical cotton.
One container or 1, 2, 3, 6 or 10 blister strip packagings together with the application instruction place in a pack from a cardboard.