Famotidine

General characteristics. Structure:

Active ingredient: 20 mg or 40 mg of famotidine.

Excipients: lactose, calcium phosphate double-base, starch corn, povidone, Natrium benzoicum, talc, magnesium stearate, sodium glikolit starch, colloid anhydride of silicon.

Pharmacological properties:

Pharmacodynamics. A blocker of N 2 - histamine receptors of the III generation. Suppresses basal and stimulated a histamine, gastrin and acetylcholine products of hydrochloric acid. Reduces activity of pepsin. Strengthens protective mechanisms of a mucous membrane of a stomach and promotes healing of its damages connected with influence of hydrochloric acid (including to the termination of gastrointestinal bleedings and scarring of stressful ulcers) by increase in formation of gastric slime, the maintenance in it of glycoproteins, stimulation of secretion of a hydrocarbonate a mucous membrane of a stomach, endogenous synthesis in it of prostaglandins and speeds of regeneration. Significantly does not change gastrin level 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 a GIT. After intake the maximum concentration in a blood plasma is reached within 1–3,5 hours. Bioavailability – 40-45%, increases at reception with 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:

- A peptic ulcer of a 12-perstny gut and a stomach in an aggravation phase, prevention of a recurrence. - Treatment and prevention of the symptomatic stomach ulcers and a 12-perstny gut (connected with reception of NPVP, stressful, postoperative ulcers).

- Erosive gastroduodenit.

- The functional dyspepsia associated with the increased secretory function of a stomach.

- Reflux esophagitis.

- Zollingera-Ellison's syndrome.

- Prevention of a recurrence of bleedings from upper parts of a GIT.

- The prevention of aspiration of a gastric juice at the general anesthesia (Mendelssohn's syndrome).

Route of administration and doses:

At a peptic ulcer of a stomach and a 12-perstny gut in an aggravation phase, symptomatic ulcers, an erosive gastroduodenit usually appoint 0,02 g 2 times a day or on 0,04 g of 1 times a day to night. If necessary the daily dose can be increased till 0,08-0,16. A course of treatment - 4-8 weeks. At the dyspepsia connected with the increased secretory function of a stomach appoint 0,02 g 1-2 times a day.

For the purpose of prevention of a recurrence of a peptic ulcer appoint 0,020 g of 1 times a day before going to bed.

At a reflux esophagitis - 0,02-0,04 two 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 0,02 g each 6 hours and can be increased to 0,160 g each 6 hours.

For prevention of aspiration of a gastric juice at the general anesthesia appoint 0,040 g in the evening and/or in the morning before operation. Tablets of Famotidine should be swallowed without chewing, washing down with enough water.

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 0,02 g.

Features of use:

Before an initiation of treatment it is necessary to exclude a possibility of existence of a malignant disease of a gullet, stomach or duodenum. Famotidine, as well as all H2-gistaminoblokatory, is undesirable to cancel sharply (a syndrome of "ricochet"). At prolonged treatment at the weakened patients, in the conditions of a stress, bacterial damages of a stomach with the subsequent spread of an infection are possible.

With care apply at patients at an abnormal liver function. Blockers of N 2 - gistaminoretseptor 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.

Blockers H2-gistaminoretseptorov can suppress 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 N 2 - gistaminoretseptor 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: are possible - dryness in a mouth, nausea, vomiting, abdominal pains, it is rare - appetite loss, increase in activity of "hepatic" transaminases; development of hepatitis, acute pancreatitis is in some cases possible.

From a nervous system: headache, dizziness; cases of development of hallucinations, confusion of consciousness, an illegibility of visual perception are described.

From cardiovascular system: very seldom - decrease in the ABP, bradycardia.

From bodies of a hemopoiesis: seldom - a leukopenia, thrombocytopenia; in isolated cases - an agranulocytosis, a pancytopenia, a hypoplasia, a marrow aplasia.

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

Interaction with other medicines:

Owing to increase рН stomach contents at a concomitant use absorption of a ketokonazol 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 oppresses.

Increases absorption of amoxicillin and clavulanic acid.

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

Overdose:

Symptoms: aggravation of side effects is possible.

Treatment: gastric lavage, symptomatic therapy, hemodialysis.

Storage conditions:

List B. To store in the place protected from moisture and light at a temperature not above +25 °C. To store in the place, unavailable to children. Not to use after the term specified on packaging. Period of validity 3 years.

Issue conditions:

According to the recipe

Packaging:

On 10, 20, 30 or 50 tablets in banks polymeric. On 10 tablets in a blister strip packaging from a film of polyvinyl chloride and aluminum foil. Bank or 1, 2, 3, 5 blister strip packagings together with a leaf insert in a cardboard pack.