Ranitidine

General characteristics. Structure:

Active ingredient: ranitidine a hydrochloride that is equivalent to ranitidine of 150 mg.

Excipients: microcrystallic cellulose, sodium of a kroskamelloz, magnesium stearate, a component for a covering - Opadry II 85G53691 orange (FD&C Blue No. 2 Aluminium Lake (AL5096), FD&C Yellow No. 6 Aluminium Lake (AL5197), FD&C Yellow No. 6 Aluminium Lake (3862), lecithin, polyethyleneglycol, polyvinyl alcohol, понсо 4R, Aluminium Lake, talc, titanium dioxide).

Pharmacological properties:

Pharmacodynamics. Ranitidine is an antagonist of H2-histamine receptors. Competitively reversibly contacting H2-histamine receptors of covering cells of a mucous membrane of a stomach, oppresses basal and stimulated secretion of hydrochloric acid and reduces activity of pepsin, raises рН stomach contents. Reduces the volume of the gastric juice caused by irritation of baroreceptors (stomach stretching), food loading, effect of hormones and biogenic stimulators (gastrin, a histamine, пенгастрин, caffeine). Duration of effect of drug after single use makes about 12 hours.

Pharmacokinetics. Ranitidine is quickly soaked up during intake. Absorption does not depend on meal. The peak of concentration in plasma within 300 – 500 mkg/ml is reached in 1 – 3 hour after oral administration of 150 mg of drug. Bioavailability of ranitidine of 50%. Concentration to Ranitidine in plasma is proportional to the accepted dose. Linkng with proteins of plasma makes 15%. It is partially metabolized in a liver.
Removal of drug is carried out preferential by kidneys (60 – 70% of a peroral dose) and 26% with excrements. The elimination half-life makes 2 – 3 hours. About 30% of a peroral dose are allocated in not changed state.

Indications to use:

Round ulcer of a stomach and duodenum in cases of lack of H. pylori or at impossibility of an eradikation of H. pylori as preventive treatment; GERB (gastroesophageal reflux disease); Zollingera-Ellison's syndrome; chronic gastritis with the increased acid-forming function of a stomach in an aggravation stage; not ulcer dyspepsia.

Route of administration and doses:

Adults.
- A round ulcer of a stomach in the absence of H. pylori or at impossibility of an eradikation of H. pylori as preventive treatment – on 150 mg 2 times a day or 300 mg of 1 times a day 4-8 weeks.
- A round ulcer of a duodenum in the absence of H. pylori or at impossibility of an eradikation of H. pylori as preventive treatment – on 150 mg 2 times a day or 300 mg of 1 times a day 4 – 6 weeks.
- The Gastroesophageal Reflux Disease (GRD) - 150 mg 4 times a day 4 - 8 weeks. A maintenance therapy at GERB – on 150 mg of 1 times a day up to 12 months.
- Zollingera-Ellison's syndrome - the initial dose makes 150 mg 4 times a day, but in case of need the dose can be increased. Selection of a dose individual.
- For patients with not ulcer dyspepsia the course on 150 mg 2 times a day 2–4 weeks or 300 mg of 1 times in sugk is recommended.
- Chronic gastritis with the increased acid-forming function of a stomach in an aggravation stage – on 150 mg 2 times a day 2 – 4 weeks or 300 mg of 1 times a day.
- The renal failure At patients with severe damage of kidneys (clearance of creatinine less than 50 ml/min.) is possible ranitidine cumulation. For such patients the recommended dose of 150 mg once a day. To the patients undergoing continuous out-patient peritoneal dialysis or a constant hemodialysis, it is necessary to accept ranitidine (150 mg) right after dialysis session.

Features of use:

Prior to treatment it is necessary to exclude a possibility of existence of malignant new growths of a stomach as treatment by ranitidine can mask symptoms of development of a tumor in a stomach.
Ranitidine is emitted with kidneys therefore drug level in plasma increases at patients with severe damages of kidneys. The drug dose for such patients has to be respectively modified.
In case of bystry drug withdrawal development of a syndrome of a ricochet is possible. In case of need drug withdrawals should be done it gradually. It is not necessary to appoint drug sick to an acute porphyria.
Pregnancies and period of a lactation. Ranitidine passes through a placenta and gets to breast milk of the woman. Similar to other drugs it can be applied during pregnancy only in urgent cases. When feeding children a breast it is necessary to stop administration of drug.

Side effects:

At an insignificant part of patients the headache and dizziness, drowsiness, uneasiness, excitement were observed. There are messages on isolated cases of developing of hallucinations, first of all at seriously ill patients and patients of advanced age. There were several messages on reversible opacification of sight, it is possible in connection with change of accommodation of an eye.
Dryness in a mouth, a lock or diarrhea, nausea, vomiting, an abdominal pain can be observed.
Reversible changes of laboratory indicators in analyses of function of a liver are possible. There are separate messages on hepatitises (with jaundice or without), as a rule, reversible.
It was reported about a possibility of development of acute pancreatitis.
Changes in blood, as a rule, reversible (a leukopenia, thrombocytopenia, a granulocytopenia, aplastic anemia) took place at some patients. It was reported about separate cases of an agranulocytosis or a pancytopenia, sometimes with a marrowy hypoplasia or an aplasia. As well as in a case with other antagonists of H2 receptors, and at use of ranitidine separate messages on a possibility of development of arrhythmias (bradycardia or tachycardia, an ekstratsistoliya), atrioventricular blocks take place.
There are messages on a joint pain and muscles.
Increase in creatinine of blood, increase in level of prolactin, gynecomastia, amenorrhea, alopecia can be observed.
Allergic reactions are seldom possible: small tortoiseshell, Quincke's disease, bronchospasm, acute anaphylaxis, thorax pain, arterial hypotension.

Interaction with other medicines:

At reception of the standard recommended ranitidine doses drug does not influence P450 cytochrome - the related functional oxidizing system in a liver. Respectively, ranitidine in the standard therapeutic dosages does not potentsiirut effect of drugs which are inactivated to these enzymes, it concerns diazepam, lidocaine, Phenytoinum, propranolol, theophylline and warfarin.
At simultaneous use with antacids the break between reception of antacids and Ranitidine has to be not less than 1 - 2 hours.
At simultaneous use of high doses of a sukralfat (2 g) and ranitidine absorption of the last can decrease. The effect is not swept up if сукральфат to accept after a 2-one-hour break.
Constant observation of the patients accepting non-steroidal anti-inflammatory drugs along with ranitidine, especially for elderly people and patients with a round ulcer in the anamnesis is recommended.

Contraindications:

Hypersensitivity to drug components. Existence of malignant diseases of a stomach. A serious illness of kidneys and a liver, cirrhosis with portosistemny encephalopathy in the anamnesis. Periods of pregnancy and lactation. Children's age (up to 14 years).

Overdose:

There are no data on life-threatening effects of overdose. In cases of overdose it is necessary to wash out a stomach and to carry out symptomatic therapy. If necessary drug can be removed from plasma by means of a hemodialysis.

Storage conditions:

To store in unavailable to children, the dry place at a temperature not above 25 °C. A period of validity – 3 years.

Issue conditions:

According to the recipe

Packaging:

 On 10 tablets at a strip No. 10; 10 strips in a cardboard box (No. 10х10).