Ranitidin-Darnitsa

General characteristics. Structure:

Active ingredient: ranitidine;

1 tablet contains hydrochloride ranitidine in terms of ranitidine 150 mg;

excipients: cellulose microcrystallic, povidone, lactose monohydrate, potato starch, talc, magnesium stearate, опадрай AMB 80 W yellow.

Pharmacological properties:

Pharmacodynamics. Ranitidine – antiulcerous means, the antagonist of H2-histamine receptors. The mechanism of action is caused by competitive inhibition of H2-histamine receptors of membranes of covering cells of a mucous membrane of a stomach. Reduces basal and stimulated secretion of hydrochloric acid, reducing the volume of the gastric juice caused by irritation of baroreceptors (stomach stretching), food loading, effect of hormones and biogenic stimulators (gastrin, a histamine, Pentagastrinum). Ranitidine reduces amount of hydrochloric acid in a gastric juice, does not influence concentration of gastrin in a blood plasma, and also on products of slime. Ranitidine is characterized by long action.

Ranitidine does not influence enzymatic system of P450 cytochrome of a liver.

Pharmacokinetics. After oral administration ranitidine is quickly soaked up in
digestive tract. Bioavailability – about 50%. The maximum concentration in blood is reached in 2-3 hours and makes 478 ng/ml. It is partially metabolized in a liver to N-oxide (the main metabolite, 4% of a dose), S-oxide and it demetilirutsya.

Elimination half-life (after intake) at normal clearance of creatinine – 
2-3 hours, at lowered (20-30 ml/min.) – 8-9 hours. It is excreted by kidneys within 24 hours, in not changed look about 30% of orally accepted dose are removed.
Gets through gistogematichesky barriers, including through placental, but it is bad – through a blood-brain barrier. Rather significant concentration are defined in breast milk. Speed and extent of elimination depend on a condition of a liver a little and are connected generally with function of kidneys.

Pharmaceutical characteristics.

Main physical and chemical properties: tablets of a round form with a biconvex surface, coated, from yellow till yellow-orange color. On cross section two layers are visible.

Indications to use:

– The round ulcer of a stomach and duodenum which is not associated with Helicobacter pylori (in an aggravation phase), including the ulcer connected with reception of non-steroidal anti-inflammatory drugs (NPVS);

– functional dyspepsia;

– chronic gastritis with the increased acid-forming function of a stomach in a stage
 aggravations;

– a gastroesophageal reflux disease (for relief of symptoms) or a reflux esophagitis.

Route of administration and doses:

Appoint to adults and children 12 years are more senior. Accept inside, without chewing, washing down with a small amount of water, irrespective of meal.

The round ulcer of a stomach and duodenum which is not associated with Helicobacter pylori (in an aggravation phase). Appoint 150 mg (1 tablet) 2 times a day in the morning and in the evening or 300 mg (2 tablets) once to night within 4 weeks. If ulcers did not cicatrize, to continue treatment within the next 4 weeks.

Prevention of the petichesky stomach ulcer and duodenum associated with reception of NPVS. Appoint 150 mg (1 tablet) 2 times a day in the morning and in the evening for therapy of NPVS.

Functional dyspepsia. Appoint 150 mg (1 tablet) 2 times a day in the morning and in the evening within 2-3 weeks.

Chronic gastritis with the increased acid-forming function of a stomach in an aggravation stage. Appoint 150 mg (1 tablet) 2 times a day in the morning and in the evening during
2-4 weeks.

Gastroesophageal reflux disease. For relief of symptoms appoint 150 mg (1 tablet) 2 times a day in the morning and in the evening within 2 weeks, if necessary continue a course of treatment.

For prolonged treatment and at an exacerbation of a gastroesophageal reflux disease
 appoint 150 mg (1 tablet) 2 times a day in the morning and in the evening or 300 mg (2 tablets) once in days to night within 8 weeks, if necessary continue a course of treatment up to 12 weeks.

Patients with the expressed renal failure (clearance of creatinine less than 50 ml/min.). A daily dose of drug for this category of patients – 1 tablet (150 mg of ranitidine).

Features of use:

Use during pregnancy or feeding by a breast.

Drug is contraindicated during pregnancy.

In need of use of drug it is necessary to stop feeding by a breast.

Children.

To children 12 years are more senior use of drug is shown for the purpose of reduction of terms of treatment of a peptic ulcer of a stomach and a duodenum, for treatment of a gastroesophageal reflux disease, including a reflux esophagitis, and for relief of symptoms of a gastroesophageal reflux disease.

In the presence of an allergy to other drugs of group of blockers H2 receptors of a histamine allergic reactions to ranitidine therefore with hypersensitivity to other drugs of this group it is necessary to use drug with care are possible.

With care use drug at a porphyria (including in the anamnesis), an immunodeficiency.
Ranitidine is removed by kidneys therefore at patients with the expressed renal failure its level in plasma is increased (see a dosage for such patients in the section "Route of Administration and Doses").

At patients of advanced age with abnormal liver functions or kidneys disturbance (confusion) of consciousness is possible that causes need of a dose decline.

Treatment by drug can mask stomach carcinoma symptoms therefore before an initiation of treatment it is necessary to exclude existence of malignant new growths in a stomach.

Regular observation of patients (especially advanced age and with instructions in the anamnesis on a round ulcer of a stomach and/or duodenum), accepting ranitidine together with non-steroidal anti-inflammatory drugs is necessary.
At patients of advanced age, persons with chronic diseases of lungs, a diabetes mellitus or at persons with the weakened immunity the increased tendency to community-acquired pneumonia development was observed.

Treatment by drug is cancelled gradually because of risk of development of a syndrome of "ricochet" at sharp cancellation.

Ability to influence speed of response at control of motor transport or work with other mechanisms.

Considering that sensitive patients at use of drug can have side reactions (dizziness, hallucinations, accommodation disturbance), during administration of drug it is necessary to refrain from control of vehicles or work with other mechanisms.

Side effects:

From system of blood: very seldom – a leukopenia, reverse thrombocytopenia, an agranulocytosis or a pancytopenia, sometimes with a hypoplasia or an aplasia of marrow, a neutropenia, immune hemolitic and aplastic anemia (usually reversible).

From immune system: seldom – a small tortoiseshell, a Quincke's disease, an acute anaphylaxis, a bronchospasm, a multiformny exudative erythema, exfoliative dermatitis, Stephens-Johnson's syndrome, a toxic epidermal necrolysis, a hyperthermia.

From mentality: very seldom – increased fatigue, reversible confusion of consciousness, drowsiness, sleeplessness, emotional lability, concern, alarm, a depression, nervousness, hallucinations, a sonitus, irritability, a disorientation. These manifestations are observed preferential at seriously ill patients or patients of advanced age.

From a nervous system: very seldom – a headache, dizziness and reversible involuntary motive frustration.

From organs of sight: illegibility of visual perception, accommodation disturbance.
From cardiovascular system: very seldom – a lowering of arterial pressure, bradycardia, tachycardia, an asystolia, an atrioventricular block, a vasculitis, a stethalgia, arrhythmia, premature ventricular contraction.

From a digestive tract: seldom – dryness in a mouth, nausea, vomiting, a lock, diarrhea, an abdominal pain, acute pancreatitis, a loss of appetite.

From gepatobiliarny system: seldom – passing and reversible changes of indicators of function of a liver, it is very rare – the hepatocellular, cholestatic or mixed hepatitis, jaundice.

From skin and hypodermic fabric: hyperemia, itch; seldom – skin rash, it is very rare – a multiformny erythema, an alopecia.

From a musculoskeletal system: very seldom – an arthralgia, a mialgiya.

From an urinary system: very seldom – acute intersticial nephrite.
From reproductive system: very seldom – a giperprolaktinemiya, a galactorrhoea, a gynecomastia, an amenorrhea, decrease in a potentiality and/or libido.

Interaction with other medicines:

Ranitidine can influence absorption, metabolism and renal excretion of other medicines.

Ranitidine in therapeutic doses does not change activity of fermental system of P450 cytochrome and does not exponentiate effect of the medicines which are metabolized this system (diazepam, lidocaine, Phenytoinum, propranolol, theophylline, etc.).

Ranitidine, changing acidity of a stomach, can influence bioavailability of some medicines. It leads or to increase in their absorption (to triazoles, midazolam, глипизид) or to decrease in their absorption (кетоконазол, итраконазол, атазанавир, гефитиниб).
Antacids and сукральфат slow down ranitidine absorption owing to what the interval between reception of these medicines and ranitidine has to make not less than 1-2 hours.
Simultaneous use with metoprololy can lead to increase in concentration of a metoprolol in blood serum.

Ranitidine at simultaneous use with coumarinic anticoagulants (warfarin) can change a prothrombin time (monitoring of a prothrombin time is recommended).
High doses of ranitidine can slow down removal of procaineamide and N-atsetilprokainamida that leads to increase in their level in a blood plasma.

Data on interaction between ranitidine and amoxicillin or metronidazole are absent.

Contraindications:

The increased individual sensitivity to ranitidine and to other components of drug; existence of malignant diseases of a stomach, cirrhosis with portosistemny encephalopathy in the anamnesis.

Overdose:

Strengthening of side reactions is possible.

Treatment: if necessary carry out an adequate symptomatic and maintenance therapy.

Storage conditions:

Period of validity. 2 years. To store in the place, unavailable to children, in original packaging at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging; on 1 or 2 blister strip packagings in a pack.