Pharmacotherapeutic group Omeprazole 40 mg
For the treatment of peptic ulcers. Inhibitors “of the proton pump.”
Pharmacodynamics Omeprazole 40 mg:
Omeprazole belongs to the antiulcer antisecretory drugs. It easily penetrates the parietal cells of gastric mucosa, is concentrated in and activated by acid pH. Active metabolite – sulfenamide inhibits H +, K +-ATPase of the secretory membrane of parietal cells (proton pump), stopping the output of hydrogen ions into the cavity of the stomach and blocking the final stage of hydrochloric acid secretion. Dose-dependent decreases the level of basal and stimulated secretion, the total volume of gastric secretion and isolation of pepsin. Effectively inhibits both night and day production of hydrochloric acid.
Has a bactericidal effect on Helicobacter pylori. Eradication of H. pylori, while the application of omeprazole and antibiotics to quickly arrest the symptoms of the disease, a high degree of healing of damaged mucosa and persistent long-term remission, reduces the likelihood of bleeding from the gastrointestinal tract.
If reflux esophagitis ulcerative normalization of acid exposure in the esophagus and the maintenance of intragastric pH> 4.0 for 24 hours with a decrease of damaging nature of the contents of the stomach (pepsinogen inhibition of transition in pepsin) helps to reduce symptoms and complete healing of esophageal lesions (healing rate exceeds 90%). Highly effective in the treatment of severe and complicated forms of erosive and ulcerative esophagitis resistant to H2-histamine receptor blockers. Long-term maintenance therapy prevents relapse of reflux esophagitis and reduces the risk of complications. With gastroesophageal reflux disease provides remission for 1 year in 85% of patients.
Pharmacokinetics Omeprazole 40 mg:
After oral administration, the drug quickly and adequately absorbed from the gastrointestinal tract, but the bioavailability of not more than 50 – 55% (effect of “first pass” through the liver). Binding to plasma proteins (albumin and alpha1-acid glycoprotein) is very high – 95%.
After a single dose of 20 mg omeprazole inhibition of gastric secretion occurs during the first hour, reaching a peak after 2 hours and lasts about 24 hours, the severity of the effect depends on the dose. Ability of parietal cells produce hydrochloric acid is restored within 3 – 5 days after therapy.
Drug biotransformation in the liver to form, at least
6 metabolites, characterized by the virtual absence of antisecretory activity.
Excreted in the kidneys as metabolites (72 – 80%) and through the gut
(18 – 23%). The half-life is 0.5 – 1 hour (normal liver function) or
3 hours (with chronic liver diseases).
Elderly patients may be some increase bioavailability and decrease the rate of excretion.
Method of use and dose Omeprazole 40 mg
Is the inside before eating, not chewing and damaging the capsule, squeezed a small amount of liquid.
Adults and children over 14 years taking omeprazole:
• gastric ulcer, duodenal ulcer and reflux esophagitis, 20 mg 1 time a day if necessary increase the dose to 40 mg (1 capsule morning and evening).
The duration of treatment for an ulcer 12 duodenal ulcer is 2 – 4 weeks, and gastric ulcer and reflux esophagitis, respectively, 4 – 8 weeks;
• in Zollinger-Ellison syndrome starting dose is 20 – 60 mg / day, if necessary it was increased to 120 mg / day. The daily dose of 80 mg or more should be administered in divided doses on 2 receptions for 2 – 8 weeks;
• with peptic ulcer caused by Helicobacter pylori, Helicobacter pylori eradication for omeprazole is prescribed in combination with antibiotics, metronidazole, bismuth preparations and other drugs;
• for resistance to other antiulcer drugs omeprazole should be administered, ranging from 40 mg / day;
• at gastroenteropathy associated with use of nonsteroidal anti-inflammatory drugs (NSAIDs), prescribed to 20 1 mg once daily for 4 – 8 weeks.
Side Effects Omeprazole 40 mg
When receiving omeprazole are possible:
• from the gastro-intestinal tract: nausea, diarrhea, constipation, abdominal pain, flatulence, dry mouth, loss of appetite;
• by the Nervous System: headache, dizziness, fatigue (including muscle), sleep disturbance, drowsiness, depression, anxiety;
• by the musculoskeletal system: in some cases – arthralgia, muscle weakness, myalgia;
• from the hemopoietic system: in some cases – anemia, eosinophilia, thrombocytopenia;
• Allergic reactions: skin rash.
Omeprazole. Indications for Use
- Stomach ulcer, duodenal ulcer, erosive-ulcerative esophagitis at exacerbation;
• eradication of Helicobacter pylori;
• Pathological hypersecretory conditions (Zollinger-Ellison syndrome, multiple endocrine adenomatosis, systemic mastocytosis, stress ulcers);
• erosive and ulcerative lesions of gastric and duodenal ulcers associated with taking non-steroidal anti-inflammatory drugs (NSAIDs);
• non-ulcer dyspepsia.
Interaction with other drugs Omeprazole 40 mg
Alter the bioavailability of any drug, absorption depends on pH (ketoconazole, iron salts). Omeprazole may increase the half-life and duration of action of drugs metabolized in the liver by oxidation (diazepam, warfarin), strengthens the effect of coumarin anticoagulants and difenina; slows for benzodiazepine tranquilizers (sibazon). Increases the (relative) concentration in the blood of clarithromycin.
With the simultaneous application of omeprazole with antacid drug interactions were observed.
Overdose Omeprazole 40 mg
Symptoms: blurred vision, confusion, headache, increased sweating, drowsiness, dry mouth, nausea, flushing, and tachycardia.
Treatment: symptomatic.
Features of use
Advised to take prescription-only and under the supervision of a physician specialist.
The drug is not recommended for children due to lack of clinical experience with omeprazole in these patients.
Before starting treatment should be to exclude the presence of malignant neoplasms in the gastrointestinal tract, especially gastric ulcer.
In patients with severe hepatic insufficiency the dose should not exceed 20 mg / day (due to increased bioavailability and half-life).
In the application of omeprazole may be distorted laboratory results of liver function and gastrin concentrations in blood plasma.
