Famotidine-Akri^® (Tablets) Instructions for Use

Marketing Authorization Holder

Akrikhin Chemical and Pharmaceutical Plant, JSC (Russia)

ATC Code

A02BA03 (Famotidine)

Active Substance

Famotidine (Rec.INN registered by WHO)

Dosage Form

Famotidine-Akri®

Film-coated tablets, 20 mg: 20 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white or white with a greyish or yellowish tint; on the break – white or almost white.

Excipients: lactose, potato starch, colloidal silicon dioxide (aerosil), talc, magnesium stearate.

Shell composition: hypromellose (hydroxypropyl methylcellulose), macrogol, glycerol, talc, titanium dioxide, lactose.

10 pcs. – blister packs (2) – cardboard packs.

Clinical-Pharmacological Group

Histamine H₂-receptor blocker. Antiulcer drug

Pharmacotherapeutic Group

H2 histamine receptor blocker

Pharmacological Action

Third-generation H₂-histamine receptor blocker. Suppresses basal and histamine-, gastrin-, and acetylcholine-stimulated hydrochloric acid production. Reduces pepsin activity.

Enhances the protective mechanisms of the gastric mucosa and promotes the healing of its lesions associated with the effects of hydrochloric acid (including cessation of gastrointestinal bleeding and scarring of stress ulcers) by increasing gastric mucus formation, its glycoprotein content, stimulating bicarbonate secretion by the gastric mucosa, its endogenous prostaglandin synthesis, and the regeneration rate.

Does not significantly change plasma gastrin concentration. Weakly inhibits the cytochrome P450 oxidase system in the liver.

After oral administration, the effect begins within 1 hour, reaching a maximum within 3 hours. The duration of the drug’s effect after a single dose depends on the dose and ranges from 12 to 24 hours.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract. After oral administration, C_max in blood plasma is reached within 1-3.5 hours. Bioavailability is 40-45 %, increases when taken with food and decreases against the background of antacid intake. Plasma protein binding is 15-20%.

30-35% of famotidine is metabolized in the liver (forming S-oxide). Elimination occurs mainly through the kidneys: 27-40% of the drug is excreted unchanged in the urine. T_1/2 is 2.5-4 hours, in patients with CrCl below 30 ml/min it increases to 10-12 hours.

In patients with severe renal failure (CrCl below 10 ml/min), it increases to 20 hours. Crosses the placental barrier and is excreted in breast milk.

Indications

• Duodenal and gastric ulcer in the acute phase, prevention of relapses;
• Treatment and prevention of symptomatic gastric and duodenal ulcers (associated with the use of non-steroidal anti-inflammatory drugs, stress, postoperative ulcers);
• Functional dyspepsia associated with increased gastric secretory function;
• Reflux esophagitis, erosive esophagitis;
• Zollinger-Ellison syndrome;
• Erosive gastroduodenitis;
• Prevention of recurrence of bleeding from the upper gastrointestinal tract;
• Prevention of gastric juice aspiration during general anesthesia (Mendelson’s syndrome).

ICD codes

Dosage Regimen

Orally. For gastric and duodenal ulcer in the acute phase, symptomatic ulcers, erosive gastroduodenitis, 20 mg 2 times/day or 40 mg once/day at night is usually prescribed. If necessary, the daily dose can be increased to 80-160 mg. The course of treatment is 4-8 weeks.

For dyspepsia associated with increased gastric secretory function, 20 mg 1-2 times/day is prescribed.

For the prevention of peptic ulcer relapses, 20 mg once/day before bedtime is prescribed.

For reflux esophagitis – 20-40 mg 2 times/day for 6-12 weeks.

For Zollinger-Ellison syndrome, the drug dose and duration of the treatment course are set individually. The initial dose is usually 20 mg every 6 hours and can be increased to 160 mg every 6 hours.

In renal failure, if the creatinine clearance is less than 30 ml/min or the serum creatinine content is more than 3 mg/100 ml, the daily dose of the drug must be reduced to 20 mg.

Adverse Reactions

From the digestive system: dry mouth, nausea, vomiting, abdominal pain, loss of appetite, increased activity of liver transaminases, constipation, diarrhea, jaundice, hepatitis, acute pancreatitis.

From the nervous system: headache, dizziness, asthenia, drowsiness, insomnia, fatigue, anxiety, depression, nervousness, psychosis, hyperthermia; cases of hallucinations, confusion, blurred vision have been described.

From the cardiovascular system: decreased blood pressure, atrioventricular block, bradycardia, arrhythmia, vasculitis.

Allergic reactions: urticaria, itching, bronchospasm, angioedema, erythema multiforme, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis, anaphylactic shock.

From the hematopoietic organs: rarely – leukopenia, neutropenia, thrombocytopenia; in isolated cases – agranulocytosis, pancytopenia, hypoplasia, bone marrow aplasia.

From the reproductive system: with long-term use of large doses – hyperprolactinemia, gynecomastia, amenorrhea, decreased libido, impotence.

From the senses: accommodation paresis, tinnitus.

Other: rarely – fever, arthralgia, myalgia, alopecia, dry skin.

Contraindications

• Pregnancy;
• Lactation period;
• Hepatic insufficiency;
• Childhood;
• Hypersensitivity to the drug components.

With caution: liver cirrhosis with a history of portosystemic encephalopathy, impaired liver function, renal failure, immunodeficiency.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation.

Use in Hepatic Impairment

Contraindication: hepatic insufficiency.

Use in Renal Impairment

In renal failure, if the creatinine clearance is less than 30 ml/min or the serum creatinine content is more than 3 mg/100 ml, the daily dose of the drug must be reduced to 20 mg.

Pediatric Use

Contraindication: childhood

Special Precautions

Before starting treatment, it is necessary to exclude the possibility of a malignant disease of the esophagus, stomach, or duodenum. Famotidine-Akri^®, like all H₂-histamine blockers, should not be abruptly discontinued (“rebound” syndrome).

During long-term treatment in debilitated patients, under stress, bacterial lesions of the stomach with subsequent spread of infection are possible.

H₂-histamine receptor blockers may counteract the effect of pentagastrin and histamine on gastric acid-forming function, so it is not recommended to use H₂-histamine receptor blockers within 24 hours preceding the test.

H₂-histamine receptor blockers may suppress the skin reaction to histamine, thus leading to false-negative results (before performing diagnostic skin tests to detect an immediate-type allergic skin reaction, it is recommended to discontinue the use of H₂-histamine receptor blockers).

During treatment, consumption of foods, beverages, and other medications that may cause irritation of the gastric mucosa should be avoided.

Overdose

Symptoms: vomiting, motor restlessness, tremor, decreased blood pressure, tachycardia, collapse.

Treatment: gastric lavage, symptomatic therapy, hemodialysis.

Drug Interactions

Due to an increase in the pH of gastric contents upon simultaneous administration, the absorption of ketoconazole may decrease.

With simultaneous use with antacids, sucralfate, the intensity of famotidine absorption decreases, so the interval between taking these drugs should be at least 1-2 hours.

Inhibits the metabolism in the liver of phenazone, aminophenazone, diazepam, hexobarbital, propranolol, metoprolol, lidocaine, phenytoin, theophylline, indirect anticoagulants, glipizide, buformin, metronidazole, caffeine, slow calcium channel blockers.

Increases the absorption of amoxicillin and clavulanic acid.

Drugs that suppress the bone marrow increase the risk of neutropenia.

Storage Conditions

List B. In a dry, light-protected place, at a temperature not exceeding 25°C (77°F). Keep out of reach of children.

Shelf Life

Shelf life 3 years. Do not use after the expiration date

Dispensing Status

By prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.