Ranitidine

When ATH:
A02BA02

Characteristic.

H antagonist gistaminovыh₂-receptors.

Ranitidine hydrochloride - white or pale yellow granular powder slightly bitter taste with the smell of sulfur. Hygroscopic, sensitive to light. Easily soluble in acetic acid and water, Soluble in methanol, sparingly soluble in ethanol, practically insoluble in chloroform, pH 1% solution 4.5-6.0. pKa 8, 2 and 2,7. Molecular weight 350,87.

Pharmacological action.
Antiulcer.

Application.

Treatment and prevention — disease hospital of stomach and duodenal ulcers, NSAID-gastropathy, heartburn (associated with hyperacidity), hypersecretion of gastric juice, symptomatic GI ulcers, erosive esophagitis, reflux esophagitis, Zollinger-Ellison, systemic mastocytosis, multiple endocrine adenomatosis; hronicheskaya dyspepsia, characterized by epigastric or retrosternal pain, associated with eating or sleep disturbances; treatment of bleeding from the upper gastrointestinal tract, prevention of recurrence of gastric bleeding in the postoperative period, prevention of aspiration of gastric juice in patients, which operations are carried out under general anesthesia (Mendelson's syndrome), aspiration pneumonitis (prevention).

Contraindications.

Hypersensitivity.

Restrictions apply.

Cirrhosis of the liver with portosystemic encephalopathy history, kidney and / or liver failure, acute porphyria (incl. history), childhood (to 12 years).

Pregnancy and breast-feeding.

In experiments in rats and rabbits, receiving ranitidine doses, to 160 times the human dose, adverse effects on the fetus revealed no.

Ranitidine crosses the placenta. Application during pregnancy is possible only in case of, if the effect of therapy outweighs the potential risk to the fetus (adequate and well-controlled studies of the safety of use in pregnant women were not conducted).

Category actions result in FDA - B. (The study of reproduction in animals revealed no risk of adverse effects on the fetus, and adequate and well-controlled studies in pregnant women have not done.)

Ranitidine passes into breast milk and, perhaps, it creates a higher concentration, than in blood plasma. Do not take while breastfeeding. The appointment should decide the issue of termination of breastfeeding.

Side effects.

From the nervous system and sensory organs: headache, feeling tired, dizziness, drowsiness, insomnia, vertigo, alarm, depression; rarely - confusion, hallucinations (particularly in elderly and debilitated patients), reversible blurred vision, ccomodation eye.

Cardio-vascular system and blood (hematopoiesis, hemostasis): arrhythmia, tachycardia / bradycardia, OF блокада, decrease in blood pressure; reversible leukopenia, thrombocytopenia, granulocytopenia; seldom-agranulozitos, pancytopenia, sometimes with bone marrow hypoplasia, aplasticheskaya anemia; sometimes immune hemolytic anemia.

From the digestive tract: nausea, vomiting, constipation / diarrhea, abdominal discomfort / pain; rarely, pancreatitis. Sometimes hepatocellular, cholestatic hepatitis, or mixed with / without jaundice (in such cases the receiving ranitidine must be stopped immediately). These effects are usually reversible, but in rare cases may lead to death. It is also noted rare cases of liver failure. In healthy volunteers, the concentration was increased AST, at least, in 2 fold relative to the level before treatment, 6 from 12 man, receiving 100 mg 4 times / in for 7 days, and 4 from 24 people, receiving 50 mg 4 times / in for 5 days.

On the part of the musculoskeletal system: seldom-artralgia, myalgia.

Allergic reactions: skin rash, bronchospasm, fever, eozinofilija; rarely mnogoformnaya Erythema, anaphylactic shock, angioedema.

Other: rarely — alopecia, vasculitis; in some cases, gynecomastia, reduced potency and / or libido. With prolonged use may develop in₁₂-deficiency anemia.

Cooperation.

Antacids, sucralfate in high doses (2 g) slow down the absorption of ranitidine (while the application of the break between taking antacids and ranitidine should be at least 1-2 hours). Smoking decreases the effectiveness of ranitidine. It reported a further lengthening of the PX when used together with warfarin ranitidine; however, in pharmacokinetic studies in humans at a dose of ranitidine 400 mg / day interactions were observed; ranitidine had no effect on the clearance of warfarin and PV; possibility of interaction with warfarin at doses above 400 mg / day has not been studied. When receiving ranitidine twice daily and triazolam triazolam plasma concentrations were higher, than when one triazolam. Triazolam AUC values ​​in people 18-60 years were 10 and 28% higher after receiving ranitidine tablets 75 and 150 mg, than after administration of triazolam. Patients older 60 years AUC values ​​were approximately 30% higher after taking the pills 75 and 150 mg ranitidine. Ranitidine increases AUC (on 80%) and concentration (on 50%) metoprolol serum, wherein T_1/2 metoprolol increased from 4,4 to 6,5 no. Reduces the absorption of itraconazole and ketoconazole (ranitidine should be taken through 2 hours after administration). It inhibits metabolism of phenazone, geksoʙarʙitala, Glipizide, ʙuformina, BCC. Compatible with 0,9% sodium chloride solution, 5% dextrose, 0,18% sodium chloride solution and 4% dextrose, 4,2% solution of sodium bicarbonate. Together with the admission PM, depressing the bone marrow, increased risk of neutropenia. Perhaps the interaction with alcohol.

Overdose.

Symptoms: convulsions, bradycardia, ventricular arrhythmias.

Treatment: induction of vomiting or gastric lavage, simptomaticheskaya therapy. Cramps-diazepam in/in, When bradikardii-atropine, in jeludockovh aritmiah-lidocaine.

Dosing and Administration.

Inside, parenterally (I /, / m). The dosage regimen and duration of treatment is determined individually. Inside, daily, usually 300 mg in 1-2 reception, maximum dose for adults is 6 g / day. To prevent the recurrence of diseases 150 mg at night; for smokers- 300 mg at night.

Children: 1.25-2.5 mg/kg (the maximum dose - 300 mg / day) 1-2 reception.

/ M, I / (bolus and infusion) by 50 mg every 6-8 hours. Children-in/drip in 0.75-1.5 mg/kg (maximum — 0,4 g / day).

Patients with impaired renal function requires correction mode. When creatinine clearance <50 mL/min when injecting introduction- 50 mg every 18-24 hours; if necessary to increase the frequency of administration 2 once a day every 12 h or more; If ingestion is 150 mg / day. In the presence of concomitant liver dysfunction may necessitate further dose reduction. Patients, hemodialysis, another dose administered immediately after hemodialysis.

Precautions.

Before treatment, exclude malignant tumors in the stomach and duodenum (may mask the symptoms of stomach cancer). The risk of cardiotoxicity is increased in patients with heart disease, With the rapid on / in the introduction and use of high doses of. It is undesirable to abruptly cancel the ranitidine at risk of acute condition. Prolonged treatment of patients with weakened under stress may be bacterial lesions of the stomach and then spread infection.

It may increase the activity of glutamyl. In the treatment of ranitidine possible false positive reaction during the tests for protein in the urine.

Cooperation