Famotidine

General characteristics. Structure:

Active ingredient: 20 mg or 40 mg of famotidine in 1 tablet.

Excipients: cellulose microcrystallic, aerosil (silicon dioxide colloid), potato starch, maltodextrin, magnesium stearate, sodium of a kroskarmelloz.

Excipients for a cover: Опадрай II (series 85) [polyvinyl alcohol, macrogoal (polyethyleneglycol), talc, titanium dioxide].

Pharmacological properties:

Blocker of H2-histamine receptors of the III generation. Suppresses basal and stimulated a histamine, gastrin and acetylcholine products of hydrochloric acid. At the same time with decrease in products of hydrochloric acid and increase рН also activity of pepsin decreases. Significantly does not change concentration of gastrin in plasma.

Poorly inhibits oksidazny system of P450 cytochrome in a liver. After intake action begins in 1 hour, reaches a maximum within 3 hours. Duration of effect of drug at a single dose depends on a dose and makes from 12 to 24 hours.

Pharmacokinetics. After intake it is quickly absorbed from digestive tract. The maximum concentration in a blood plasma is reached within 1–3,5 hours. Bioavailability of famotidine makes 40-45%, slightly changes in the presence of food and decreases against the background of reception of antacids. Communication with proteins of plasma – 15-20%. 30-35% of famotidine are metabolized in a liver (with formation of S-oxide).

Elimination, generally happens through kidneys, 27-40% of drug are removed with urine in not changed look. The elimination half-life – 2,5-4 hours, at patients with clearance of creatinine lower than 30 ml/min. increases till 10-12 o'clock. At patients with a heavy renal failure (the clearance of creatinine is lower than 10 ml/min.) it increases till 20 o'clock.

Gets through a placental barrier and it is allocated with breast milk.

Indications to use:

- Treatment and prevention of a recurrence of a peptic ulcer of a stomach and 12-perstny gut.
- Treatment and prevention of the symptomatic stomach ulcers and a 12-perstny gut (connected with reception of non-steroidal anti-inflammatory drugs (NPVP), stressful, postoperative ulcers).
- Erosive gastroduodenit.
- The functional dyspepsia associated with the increased secretory function of a stomach (including heartburn, an acid eructation).
- Reflux esophagitis.
- Zollingera-Ellison's syndrome.
- Prevention of a recurrence of bleedings from upper parts of the digestive tract (DT).
- The prevention of aspiration of a gastric juice at the general anesthesia (Mendelssohn's syndrome).

Route of administration and doses:

Inside, without chewing, washing down with enough water.

At a peptic ulcer of a stomach and a 12-perstny gut in an aggravation phase, symptomatic ulcers, an erosive gastroduodenit usually appoint 20 mg 2 times a day or on 40 mg of 1 times a day to night. If necessary the daily dose can be increased to 80-160 mg. A course of treatment – 4-8 weeks. At the dyspepsia connected with the increased secretory function of a stomach appoint 20 mg 1-2 times a day.

For prevention of a recurrence of a round ulcer of a stomach and a duodenum: 20 mg once before going to bed.

At a reflux esophagitis – 20-40 mg 2 times a day within 6-12 weeks.

At Zollingera-Ellison's syndrome the dose of drug and duration of a course of treatment are established individually. The initial dose usually makes 20 mg each 6 hours and can be increased to 160 mg each 6 hours.

For prevention of aspiration of a gastric juice at the general anesthesia appoint 40 mg in the evening and/or in the morning before operation. At a renal failure if the clearance of creatinine makes less than 30 ml/min. or the content of creatinine in blood serum more than 3 mg / 100 ml, it is necessary to reduce a daily dose of drug to 20 mg.

For prevention of a recurrence of bleedings from upper parts of a GIT – on 20 mg 2 times a day within 3-4 weeks.

Features of use:

Use at pregnancy and the lactation period: Use at pregnancy is possible only if the potential advantage for mother exceeds risk for a fruit. Gets into breast milk. In the period of a lactation it is necessary to cancel use of drug or to stop feeding by a breast.

Symptoms of a peptic ulcer 12 - a 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. Can mask the symptoms connected with a stomach carcinoma therefore before an initiation of treatment it is necessary to exclude existence of a malignant new growth. Cancel gradually because of risk of development of a syndrome of "ricochet" at sharp cancellation.

At prolonged treatment of the weakened patients, and also at a stress bacterial damages of a stomach with the subsequent spread of an infection are possible.

H2 blockers - histamine receptors should be accepted in 2 h after reception of an itrakonazol or a ketokonazol in order to avoid considerable reduction of their absorption.

Counteracts influence of Pentagastrinum and histamine on acid-forming function of a stomach.

Suppresses skin reaction to a histamine, resulting, thus, in false-negative results (before conducting diagnostic skin tests for identification of allergic skin reaction of immediate type use of blockers of H2 - histamine receptors is recommended to be stopped).

During treatment it is necessary to avoid the use of food stuffs, drinks and other medicines (M) which can cause irritation of a mucous membrane of a stomach.

Efficiency of drug in inhibition of night secretion of acid in a stomach can decrease as a result of smoking.

Increase in a dose of drug owing to the increased clearance can be required by patients with burns.

In case of the admission of a dose, it needs to be accepted as soon as possible; not to accept if there came time of reception of the following dose; not to double a dose.

Influence on ability to drive the car and other mechanisms. There are no data on influence of drug on ability to manage vehicles or to perform the work requiring concentration and special attention.

Side effects:

From the alimentary system: dryness in a mouth, nausea, vomiting, abdominal pains, appetite loss. In some cases increase in activity of transaminases in a blood plasma.

From a nervous system: headache, dizziness, sonitus, passing mental disturbances.

From cardiovascular system: seldom – arrhythmias.

From bodies of a hemopoiesis: seldom – a leukopenia, thrombocytopenia, an agranulocytosis, a pancytopenia.

From reproductive system: at long reception of high doses – a giperprolaktinemiya, a gynecomastia, an amenorrhea, decrease in a libido, impotence.

From sense bodys: paresis of accommodation, an illegibility of visual perception, a ring in ears.

Allergic reactions: urticaria, a skin itch, skin rash, a bronchospasm are possible.
Others: fever, arthralgia, mialgiya.

Interaction with other medicines:

Owing to increase рН stomach contents at a concomitant use absorption of a ketokonazol and itrakonazol can decrease.

At simultaneous use with antiacid means, sukralfaty there is a decrease in intensity of absorption of famotidine therefore the break between reception of these drugs has to make not less than 1-2 hours.

Metabolism in a liver of phenazone, Aminophenazonum, diazepam, hexobarbital, propranolol, a metoprolol, lidocaine, Phenytoinum, theophylline, indirect anticoagulants, a glipizida, Buforminum, metronidazole, caffeine, blockers of "slow" calcium channels, tricyclic antidepressants oppresses.

Increases absorption of amoxicillin and clavulanic acid.

The medicines oppressing marrow increase risk of development of a neutropenia.

Contraindications:

Children's age up to 12 years (due to the lack of sufficient experience of use of drug), individual hypersensitivity to drug components.

With care: a liver failure, cirrhosis with portosistemny encephalopathy in the anamnesis, a renal failure, an immunodeficiency, advanced age.

Overdose:

Symptoms: vomiting, motive excitement, tremor, lowering of arterial pressure, tachycardia, collapse.

Treatment: gastric lavage, symptomatic therapy, hemodialysis.

Storage conditions:

List B. In the dry, protected from light place at a temperature not above 25 °C. To store in the place, unavailable to children. A period of validity - 2 years. Not to apply after the period of validity specified on packaging.

Issue conditions:

Without recipe

Packaging:

Tablets, film coated, 20 mg and 40 mg. On 7, 10, 14 or 20 tablets in a blister strip packaging from a film of the polyvinyl chloride and printing aluminum foil varnished. On 1, 2, 3, 4 or 10 blister strip packagings with the application instruction in a pack from a cardboard.