Alisazim is a blocker of histamine H2-receptors. Inhibits basal and stimulated by histamine, gastrin and acetylcholine (to a lesser extent) the secretion of hydrochloric acid. Increases the pH of gastric contents and reduces the activity of pepsin. The duration of action of Alisazim with a single admission - 12 hours.
After oral administration, Alisazim is rapidly absorbed from the gastrointestinal tract. Eating and antacids significantly affect the extent of absorption. Subjected to the effect of "first passage" through the liver. Cmax in plasma is reached within 2 h after a single oral administration. After IM injection Alisazim rapidly and almost completely absorbed from the injection site. Cmax achieved within 15 min.
Protein binding - 15%. Vd - 1.4 L / kg. Alisazim is excreted in breast milk.
T1/2 is 2-3 h. About 30% of the dose excreted in the urine in unchanged form. Elimination rate decreases with abnormal liver function or renal function.
Why is Alisazim prescribed?
Gastric ulcer and duodenal ulcer in acute phase; prevention of relapse of peptic ulcer; symptomatic ulcer; erosive and reflux esophagitis; Zollinger-Ellison syndrome; prevention of "stress" ulcers of the gastrointestinal tract, postoperative ulcers, recurrent bleeding from upper gastrointestinal tract; prevention of aspiration of gastric juice during operations under general anesthesia.
Dosage and administration
Individual. For oral administration for treatment of adults and children over 14 years daily Alisazim dose is 300-450 mg; if necessary, the daily dose was increased to 600-900 mg; multiplicity of administration is 2-3 times / day. For the prevention of exacerbations of disease are used by 150 mg / day at bedtime. The duration of treatment is determined by the indications for use.
The dose of Alisazim for patients with renal insufficiency at the level of creatinine more than 3.3 mg / 100 ml is 75 mg 2 times / day.
IV or IM by 50-100 mg every 6-8 hours.
Alisazim side effects, adverse reactions
Cardio-vascular system: in a few cases (for IV administration) - AV-blockade.
Digestive system: rarely - diarrhea, constipation, and in isolated cases - hepatitis.
CNS: Rarely - headache, dizziness, fatigue, blurred vision, and in isolated cases (at seriously ill patients) - confusion, hallucinations.
Hematopoietic system: rarely - thrombocytopenia, prolonged use at high doses - leukopenia.
Metabolism: rarely - a slight increase of creatinine in serum at the beginning of treatment.
Endocrine system: long-term use in high doses may increase the content of prolactin, gynecomastia, amenorrhea, impotence, decreased libido.
From the musculoskeletal system: very rarely - arthralgia, myalgia.
Allergic reactions: rarely - a skin rash, urticaria, angioedema, anaphylactic shock, bronchospasm, hypotension.
Other: rarely - recurrent parotitis, and in isolated cases - hair loss.
Pregnancy, lactation (breastfeeding), increased sensitivity to ranitidine.
Using during pregnancy and breastfeeding
Adequate and well controlled studies of the safety of Alisazim during pregnancy has not been conducted, therefore the use during pregnancy is contraindicated.
If necessary the use of Alisazim during lactation should stop breastfeeding.
With careful use in patients with impaired renal excretory function.
Before treatment with Alisazim is necessary to exclude the possibility of a malignant disease of the esophagus, stomach or duodenum.
With long-term treatment of debilitated patients under stress conditions may be bacterial lesions of the stomach with subsequent spread of infection.
Undesirable abrupt discontinuation of Alisazim because of the risk of recurrence of peptic ulcer. Effectiveness of prophylactic treatment of peptic ulcer above while taking Alisazim courses for 45 days in spring and autumn than during the reception. Quick intravenous injection of Alisazim in rare cases cause bradycardia, usually in patients predisposed to cardiac arrhythmias.
There are a few reports that Alisazim might contribute to the development of acute attacks of porphyria, in connection with what is necessary to avoid its use in patients with acute porphyria in history.
Therapy with Alisazim possible distortions of laboratory data: increased creatinine, the activity of gamma-glutamyl transpeptidase and liver transaminases in the blood plasma.
In cases where Alisazim is used in combination with antacids, the break between taking antacids and Alisazim should be at least 1-2 hours (antacids may cause undesired absorption of ranitidine).
Clinical data on the safety of Alisazim in pediatric patients is limited.
Alisazim drug interactions
In an application with antacids may decrease absorption of ranitidine.
In an application of Alisazim with anticholinergics may be in breach of memory and attention in elderly patients.
Probably that histamine H2-blockers reduce receptor ulcerogenic action of NSAIDs on the gastric mucosa.
In an application with warfarin may decrease clearance of warfarin. There is one case of gipoprotrombinemiey and bleeding in patients receiving warfarin.
In an application with bismuth tripotassium dicitrate may increase unwanted absorption of bismuth, with glyburide - described the cases of hypoglycemia, with ketoconazole, itraconazole - decreased absorption of ketoconazole, itraconazole.
In an application with metoprolol may increase the plasma concentrations and increased AUC and T1 / 2 of metoprolol.
In an application with sucralfate in high doses (2 g) possible violation of the absorption of ranitidine.
In an application Alisazim with procainamide may be decrease excretion of procainamide by the kidneys which leads to an increase in its concentration in blood plasma.
There is a data of increased absorption of triazolam in its simultaneous application, apparently due to changes in pH of gastric contents under the influence of ranitidine.
Probably that while the application with phenytoin may increase the concentration of phenytoin in plasma and increased risk of toxicity.
In an application with furosemide moderately expressed increasing the bioavailability of furosemide.
There is a described case of ventricular arrhythmias (bigeminy) with simultaneous application of quinidine, with cisapride - described a case of cardiotoxicity.
It can not be excluded some increase in cyclosporine concentration in blood plasma in its simultaneous application with ranitidine.
Alisazim in case of emergency / overdose
Symptoms: seizures, bradycardia, ventricular arrhythmias.
Treatment: induction of vomiting or gastric lavage, symptomatic therapy. In convulsions - diazepam IV, bradycardia - atropine, ventricular arrhythmias - lidocaine.