Pharmacological properties

Pharmakodinamichesky parameters. ranitidine — pharmaceutical active ingredient of medicament — is an antagonist of n2-receptors. ranitidine competitively and reversibly blocks impact on the specified receptors of parietal glandulotsit of the histamine released by enterokhromaffinopodobny cells of a stomach.

Effects of ranitidine:

• reduction of volume of gastric juice;
• decrease in concentration of HCl in gastric juice;
• decrease in secretion of HCl (basal, night and stimulated);
• decrease in pepsinia.

it is essential

that ranitidine:

• does not influence gastrin content in blood plasma and products of slime stomach glands;
does not change
• secretion by a pancreas of bicarbonate or enzymes in response to stimulation by secretin and pancreozymin;
• does not make significant impact on CYP P450.

Pharmacokinetic parameters. After oral introduction are quickly absorbed irrespective of meal or antacids (the bioavailability is about 50%). The C _max in blood of 440-545 ng/ml is reached in 2–3 h after introduction of 150 mg of ranitidine. Distribution volume — about 1.4 l/kg. Linking with proteins of blood plasma on average — 15%.

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it is Partially metabolized in a liver (to N- and S-oxides and a desmetilranitidin). Renal clearance — about 410 ml/min. (points to active canalicular excretion). The t _½ makes 2.5-3 h (in a renal failure increases to 4–5 h)

Main way of excretion — with urine (at the same time about 30% of orally entered dose are removed in not changed look). An insignificant part is removed with a stake.

Well gets through gistogematichesky barriers (an exception — GEB). In significant quantities it is allocated in breast milk.

At patients with cirrhosis in compensation stage the little change of parameters of pharmacokinetics of ranitidine has no clinical importance.

considerable linear correlation between orally entered dose (up to 300 mg) and the inhibiting impact of ranitidine on secretion of hydrochloric acid Exists. Concentration of ranitidine in blood plasma of 50 ng/ml renders to 50% the inhibiting effect concerning stimulated secretion of HCl.

After oral introduction of 150 mg of ranitidine its concentration in blood plasma exceeding the EU ₅₀ (36–94 ng/ml), remains during 8 h. At the same time in 12 h the medicament level in blood plasma remains rather high to make the considerable inhibiting impact on gastric secretion. At patients with a duodenum ulcer the oral administration of ranitidine in a dose of 150 mg each 12 h considerably reduces average 24-hour activity of ions of hydrogen by 69% and night secretion of hydrochloric acid for 90%.

Besides, 300 mg of ranitidine at oral introduction for the night also effectively reduce acidity of gastric contents during 24 h, as well as reception of 150 mg of ranitidine 2 times a day.

Results of long researches on animals on studying toxic, cancerogenic and mutagen effects of ranitidine assume lack of those at the person at administration of medicament in therapeutic doses.

Indication

round ulcer of a stomach and duodenum which is not associated with helicobacter pylori (including npvp-induced), an aggravation phase; chronic gastritis (with the raised kislotoproduktion), an aggravation stage; gastroesophageal reflux disease; reflux esophagitis; functional dyspepsia.

Use

Adults and children at the age of 12 years: per os, without chewing (to wash down with the insignificant volume of water), regardless of meal. in case of use 2 times a day take the medicament in the morning and in the evening. at single use in day the medicament is taken for the night.

• round ulcer of a stomach and duodenum which is not associated with Helicobacter pylori (including NPVP-indutsirovannuyu), an aggravation phase:

on 150 mg 2 times a day (or 300 mg of 1 times a day), a course — 4 weeks. In case of insufficient effective healing duration of therapy Prevention of emergence NPVP-indutsirovannykh of stomach ulcers and a duodenum increase by 4 weeks

• :

on 150 mg 2 times a day. A course — during the period of use by the patient of NPVP.

• Functional dyspepsia:

on 150 mg 2 times a day. A course — 2–3 weeks

• Chronic gastritis (the raised kislotoproduktion), an aggravation stage:

on 150 mg 2 times a day. A course — 2–4 weeks

• Gastroesophageal reflux disease:

— for simplification of expressiveness of symptomatology: on 150 mg 2 times a day. A course — 2 weeks (to prolong if it is necessary);

— long therapy or in case of aggravation: on 150 mg 2 times a day (or 300 mg of 1 times a day). A course — 8 weeks, (to prolong up to 12 weeks if it is necessary).

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Sick with the profound renal failure (clearance of creatinine of 50 ml/min.) ranitidine appoint in a dose 150 mg/days

Contraindication

Individual hypersensitivity to active ingredient of medicament or other its components; the cirrhosis (complicated by hepatic encephalopathy); renal failure of heavy degree; malignant new growths of a stomach.

Side effects

– reduction of quantity of leukocytes in peripheral blood (4 109/l), reversible decrease in quantity of thrombocytes (150 109/l), an agranulocytosis or decrease in maintenance of all uniform elements of blood, in some cases against the background of hypo - or a marrow aplasia, a neutropenia; as a rule, reversible anemia (hemolytic immune or aplastic).

– Reactions of hypersensitivity (among other things urticaria, a Quincke's edema, an acute anaphylaxis, a spasm of bronchial tubes, exfoliative dermatitis, a multiformny exudative erythema, Lyell's diseases, Stephens — Johnson), a hyperthermia.

— Increased fatigue, confusion of consciousness (reversible), drowsiness, a condition of excitement, insomnia, emotional lability, feeling of alarm, concern, a depression, irritability, nervousness, hallucinations, tinnitus, a condition of a disorientation or confusion (mainly at elderly patients or patients with heavy pathology).

– the Headache, dizziness, involuntary motive disturbances (reversible).

– Illegibility of visual perception, accommodation disorder.

– Arterial hypotension, decrease in ChSS (40 ud. / mines), increase in ChSS (90 ud. / mines), asystolia, AV blockade, vasculitis, stethalgia, disturbances of a warm rhythm, premature ventricular contraction.

– the Loss of appetite, nausea, vomiting, dryness in a mouth, a meteorism, a constipation, diarrhea, an abdominal pain, acute pancreatitis.

– Tranzitorny deviations of indicators of hepatic tests (reversible character), hepatitis (including anicteric forms).

– Hyperaemia, an itching, rash, xeroderma, an alopecia.

– muscle, joints Pain.

– Acute defeat of interstitial tissue of kidneys, decrease in renal functions.

– the Gynecomastia, an amenorrhea, increase in level of prolactin in blood, a galactorrhoea, reversible decrease in erectile function and/or sexual desire.

Special instructions

likelihood of development of allergic reactions at intake of ranitidine in case of an allergy for the patient to other β-antagonists of n2-receptors Is available.

At patients with decrease in immune responsiveness, at patients with a sharp porphyria (in the anamnesis or now) at use of ranitidine it is necessary to observe discretion.

Dose should be lowered in case of development of confusion of consciousness in elderly patients with a liver or renal failure.

At intake of ranitidine the reduction of expressiveness of manifestations of malignant new growths of a stomach is possible

.

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At use of ranitidine noted increase in probability of emergence of community-acquired pneumonia at the immunokomprometirovanny or elderly patients sick with diabetes or persons with chronic pulmonary pathology.

should not stop sharply therapy by ranitidine.

Sick with a lactose intolerance, a galactosemia, disturbance of absorption of glucose and a galactose needs to take presence of lactose in medicament into account.

during pregnancy and feeding a breast medicament is not appointed.

As the likelihood of developing disorders of accommodation, dizziness and hallucinations is available, during ranitidine use the control of vehicles and work with other mechanisms are excluded.

Interaction

Intake of ranitidine increases absorption in a GIT of a glipizid, midazolam and a triazolam.

At the combined use with ranitidine the absorption in a GIT of a gefitinib, itrakonazol, ketokonazol, atazanavir decreases.

Absorption of ranitidine in a GIT slows down at simultaneous use with antacids (the due interval makes ≥1–2 h).

increase in blood plasma of maintenance of a metoprolol at its combined use with ranitidine Is possible

.

Protrombiny time can change at the combined use of ranitidine with warfarin.

increase in time of excretion of procaineamide and N-atsetilprokainamida at the combined use with high doses of ranitidine Is possible

.

Efficiency of ranitidine decreases when smoking.

Overdose

in case of excess use strengthening of expressiveness of side reactions is possible

.

Storage conditions

At a temperature of ≤25 °C in original packing.