Ranitidine (Tablets) Instructions for Use

ATC Code

A02BA02 (Ranitidine)

Active Substance

Ranitidine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Histamine H₂-receptor blocker. Antiulcer drug

Pharmacotherapeutic Group

H2 histamine receptor blocker

Pharmacological Action

Ranitidine blocks histamine H₂-receptors of parietal cells of the gastric mucosa, reduces basal and stimulated secretion of hydrochloric acid, caused by baroreceptor irritation, food load, action of hormones and biogenic stimulants (gastrin, histamine, pentagastrin).

Ranitidine reduces the volume of gastric juice and the content of hydrochloric acid in it, increases the pH of the gastric contents, which leads to a decrease in pepsin activity. After oral administration in therapeutic doses, it does not affect prolactin levels. It inhibits microsomal enzymes.

The duration of action after a single dose is up to 12 hours.

Pharmacokinetics

It is rapidly absorbed; food intake does not affect the degree of absorption. When taken orally, the bioavailability of ranitidine is approximately 50%. C_max in plasma is reached 2-3 hours after administration.

Plasma protein binding does not exceed 15%. It is slightly metabolized in the liver to form desmethylranitidine and ranitidine S-oxide.

It has a first-pass effect through the liver. The rate and extent of elimination are slightly dependent on the state of the liver.

T_1/2 after oral administration is 2.5 hours, with a creatinine clearance of 20-30 ml/min it is 8-9 hours. It is excreted mainly in the urine (60-70%, unchanged – 35%), a small amount – in the feces. It poorly penetrates the blood-brain barrier. It crosses the placenta. It is excreted in breast milk (the concentration in breast milk in lactating women is higher than in plasma).

Indications

• Treatment and prevention of exacerbations of gastric and duodenal ulcers;
• Gastric and duodenal ulcers associated with NSAID use;
• Reflux esophagitis, erosive esophagitis;
• Zollinger-Ellison syndrome;
• Treatment and prevention of postoperative, “stress” ulcers of the upper gastrointestinal tract;
• Prevention of recurrence of bleeding from the upper gastrointestinal tract;
• Prevention of gastric juice aspiration during operations under general anesthesia (Mendelson’s syndrome).

ICD codes

Dosage Regimen

Tablets

Ranitidine is taken regardless of meals, without chewing, with a small amount of liquid.

Adults and children over 12 years old

Gastric and duodenal ulcer. For the treatment of exacerbations, 150 mg 2 times/day (in the morning and evening) or 300 mg at night is prescribed. If necessary – 300 mg 2 times/day. The duration of the treatment course is 4-8 weeks. For the prevention of exacerbations, 150 mg at night is prescribed, for smoking patients – 300 mg at night.

Ulcers associated with NSAID use. 150 mg 2 times/day or 300 mg at night is prescribed for 8-12 weeks. Prevention of ulcer formation when taking NSAIDs – 150 mg 2 times/day.

Postoperative and “stress” ulcers. 150 mg 2 times/day is prescribed for 4-8 weeks.

Erosive reflux esophagitis. 150 mg 2 times/day or 300 mg at night is prescribed. If necessary, the dose can be increased to 150 mg 4 times/day. The course of treatment is 8-12 weeks. Long-term preventive therapy – 150 mg 2 times/day.

Zollinger-Ellison syndrome. The initial dose is 150 mg 3 times/day, if necessary the dose can be increased.

Prevention of recurrent bleeding. 150 mg 2 times/day.

Prevention of the development of Mendelson’s syndrome. It is prescribed at a dose of 150 mg 2 hours before anesthesia, and also preferably 150 mg the night before.

In the presence of concomitant impaired liver function, a dose reduction may be required.

For patients with renal failure with creatinine clearance less than 50 ml/min, the recommended dose is 150 mg/day.

Adverse Reactions

From the digestive system nausea, dry mouth, constipation, vomiting, diarrhea, abdominal pain; rarely – hepatocellular, cholestatic or mixed hepatitis, acute pancreatitis.

From the hematopoietic organs leukopenia, thrombocytopenia, agranulocytosis, pancytopenia, hypo- and aplasia of the bone marrow, immune hemolytic anemia.

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

From the nervous system increased fatigue, drowsiness, headache, dizziness; rarely – confusion, tinnitus, irritability, hallucinations (mainly in elderly patients and severely ill patients), involuntary movements.

From the sensory organs blurred vision, accommodation paresis.

From the musculoskeletal system arthralgia, myalgia.

From the endocrine system hyperprolactinemia, gynecomastia, amenorrhea, decreased libido, impotence.

Allergic reactions urticaria, skin rash, angioedema, anaphylactic shock, bronchospasm, erythema multiforme.

Other alopecia, hypercreatininemia.

Contraindications

• Pregnancy;
• Lactation;
• Children under 12 years of age;
• Hypersensitivity to ranitidine or other components of the drug.

With caution – renal and/or hepatic insufficiency, liver cirrhosis with a history of portosystemic encephalopathy, acute porphyria (including history).

Use in Hepatic Impairment

In the presence of concomitant impaired liver function, a dose reduction may be required.

Use in Renal Impairment

For patients with renal failure with creatinine clearance less than 50 ml/min, the recommended dose is 150 mg/day.

Pediatric Use

Contraindication: children under 12 years of age.

Special Precautions

Treatment with ranitidine may mask symptoms associated with gastric carcinoma, so before starting treatment, it is necessary to exclude the presence of cancer-ulcer.

Ranitidine, like all H₂-histamine blockers, should not be abruptly discontinued (“rebound” syndrome).

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

There is evidence that Ranitidine can cause acute attacks of porphyria.

H₂-histamine receptor blockers should be taken 2 hours after taking itraconazole or ketoconazole to avoid a significant reduction in their absorption.

May increase glutamyltranspeptidase activity.

May be the cause of a false-positive reaction when performing a urine protein test.

H₂-histamine receptor blockers may counteract the effect of pentagastrin and histamine on the acid-forming function of the stomach, therefore, 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-positive results (before conducting diagnostic skin tests to detect an immediate allergic skin reaction, it is recommended to discontinue the use of H₂-histamine receptor blockers).

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

Use in pediatrics

The safety and efficacy of ranitidine in children under 12 years of age have not been established.

Effect on ability to drive vehicles and machinery

During the treatment period, it is necessary to refrain from engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Overdose

Symptoms: convulsions, bradycardia, ventricular arrhythmias.

Treatment symptomatic. For developing convulsions – diazepam IV, for bradycardia or ventricular arrhythmias – atropine, lidocaine. Hemodialysis is effective.

Drug Interactions

Smoking reduces the effectiveness of ranitidine.

Increases the concentration of metoprolol in blood serum (by 80% and 50%, respectively), while the half-life of metoprolol increases from 4.4 to 6.5 hours.

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

Inhibits the metabolism in the liver of phenazone, aminophenazone, diazepam, hexobarbital, propranolol, diazepam, lidocaine, phenytoin, theophylline, aminophylline, indirect anticoagulants, glipizide, buformin, metronidazole, calcium antagonists.

Medicines that inhibit the bone marrow increase the risk of neutropenia.

With simultaneous use with antacids, sucralfate in high doses, a slowdown in the absorption of ranitidine is possible, so the interval between taking these drugs should be at least 2 hours.

Storage Conditions

Store in a dry place, out of reach of children, at a temperature from 15°C (59°F) to 30°C (86°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is dispensed 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.