Mix: instructions for using the medicine, structure, Contraindications
Active material: Omeprazole
When ATH: A02BC01
CCF: Inhibitor N+-K+-ATPase. Anti-ulcer drug
ICD-10 codes (testimony): E16.8, J95.4, K21.0, K25, K26, K27
When CSF: 11.01.03
Manufacturer: DR. REDDY`S LABORATORIES LTD. (India)
Mix: dosage form, composition and packaging
Valium for solution for infusion in the form of a homogeneous porous cakes or pieces or as a powder of white or almost white.
| 1 fl. | |
| omeprazole | 40 mg |
Excipients: Sodium hydroxide, disodium эdetat.
Bottles of colorless glass (1) – packs cardboard.
Mix: pharmachologic effect
Anti-ulcer drug, a specific inhibitor of proton pump. Inhibits the activity of H+-K+-ATPase in gastric parietal cells, blocking the final stage of hydrochloric acid secretion, thereby, reduces acid production. It reduces basal and stimulated secretion regardless of the nature of the stimulus.
Omeprazole is a prodrug and activated in an acidic environment of the secretory canaliculi of gastric parietal cells.
Antisecretory effects after taking a dose of 20 mg occurs within the first hour, maximum action – through 2 no. Inhibition 50% maximum secretion continues 24 no.
A single dose per day provides a rapid and effective inhibition of daytime and nighttime gastric secretion, reaches its maximum at 4 days of treatment and disappear by the end of 3 – 4 days after the deadline.
In patients with duodenal ulcer reception 20 mg omeprazole maintains the pH in the stomach level 3 during 17 no.
Mix: pharmacokinetics
Distribution and metabolism
Associated with the plasma protein by 90-95% (albumin and alpha-acid glycoprotein).
Almost completely metabolized in the liver involving the cytochrome P450 enzyme system to form 6 pharmacologically active metabolites (incl. gidroksiomeprazol, sulfide and sulfone derivatives). A significant part of the metabolism of omeprazole is dependent on polymorphonuclear expressible specific isoform CYP2C19 ( S-hydroxylase mefenitoin), responsible for education gidroksiomeprazol, the main plasma metabolite. It is an inhibitor of the isozyme CYP2C19.
Deduction
T1/2 for the final phase of the AUC after i / v administration of omeprazole is approximately 40 m (hepatic failure – 3 no); total clearance of plasma is from 0.3 to 0.6 l / min. Changes of T1/2 in the course of treatment does not occur.
Excreted in the urine (70-80%) and the bile (20-30%).
Pharmacokinetics in special clinical situations
In chronic renal insufficiency excretion is reduced in proportion to the decrease in creatinine clearance.
In elderly patients, excretion is reduced, increased bioavailability.
Mix: testimony
- Gastric ulcer and duodenal ulcer (incl. relapse prevention);
- Reflux esophagitis;
- Hypersecretory conditions (Zollinger-Ellison, stress ulcers GIT, multiple endocrine adenomatosis, systemic mastocytosis);
- NSAID-gastropathy;
- Prevention of aspiration of acidic stomach contents into the airway during general anesthesia (Mendelson's syndrome).
Mix: dosing regimen
At severe exacerbation of peptic ulcer disease, reflux esophagitis and NSAID-gastropathy, patients, which is not shown oral formulation, the recommended daily dose Omez® is 40 mg for administration in the form of I / infusion.
At Zollinger-Ellison syndrome the drug is prescribed in an initial dose 60 mg / day. The dose should be individualized, possible appointment to the higher doses (80-120 mg / day). When the daily dose is from above 60 mg, it should be divided into 2-3 infusion for days.
At Mendelson's syndrome drug prescribed for the night in a dose of 40 mg and less than 2 hours before anesthesia / surgery dose 40 mg.
In elderly patients there is no need to adjust the dose.
Rules of drug infusion solution
Solution / in infusion is prepared immediately before use. To prepare the solution for / in infusion use only 5% Dextrose (Glucose) without preservatives. To dissolve 40 mg lyophilized powder in a vial is added omeprazole least 5 ml solvent and gently shaken until complete dissolution of lyophilizate. The prepared solution, comprising 40 mg omeprazole, diluted before administration 100 ml 5% dextrose (Glucose) without preservatives for / in infusion for at least 30 m. Prior to the introduction should ensure that no solution of suspended particles. Chemical and physical stability of the prepared solution of omeprazole is observed within 6 h with time simply entails omeprazole in 5% dextrose (Glucose).
Mix: side effects
From the hematopoietic system: in some cases – leukopenia, thrombocytopenia, agranulocytosis, pancytopenia.
On the part of the digestive system: diarrhea or constipation, abdominal pain, nausea, vomiting, flatulence; rarely – increase in liver enzymes, taste disturbances; in some cases – dry mouth, stomatitis, in patients with severe liver disease prior – hepatitis (incl. with jaundice), abnormal liver function.
CNS: in patients with severe concomitant somatic diseases – dizziness, headache, excitation, depression; in patients with severe liver disease prior – encephalopathy.
On the part of the musculoskeletal system: in some cases – arthralgia, myasthenia, myalgia.
Dermatological reactions: rarely – skin rash and / or itching; in some cases – photosensitivity, erythema multiforme exudative, alopecia.
Allergic reactions: hives, angioedema, fever, bronchospasm, interstitsialynыy jade and anafilakticheskiy shock.
Other: rarely – gynecomastia, malaise, visual impairment, peripheral edema, increased sweating, the formation of gastric glandular cysts during long-term treatment (a consequence of inhibiting the secretion of hydrochloric acid, It is a benign reversible).
Mix: Contraindications
- Children's age;
- Pregnancy;
- Lactation;
- Hypersensitivity to the drug.
FROM caution should be prescribed in patients with renal and / or hepatic insufficiency.
Mix: Pregnancy and lactation
Use of the drug Omez® Pregnancy and lactation (breast-feeding) contraindicated.
Mix: Special instructions
Before therapy is necessary to exclude the presence of malignant process (especially gastric ulcer), since treatment, maskyruya symptoms, may delay the correct diagnosis.
Effects on ability to drive vehicles and management mechanisms
During the period of treatment must be careful when driving and occupation of other potentially hazardous activities, require high concentration and speed of psychomotor reactions.
Mix: overdose
According to clinical studies with a / in the introduction of a dose of omeprazole 270 mg / day and at a dose of 650 mg for 3 day dose-related side effects have been observed.
Symptoms: confusion, blurred vision, drowsiness, dry mouth, headache, nausea, tachycardia, arrhythmia.
Treatment: symptomatic. Hemodialysis is not effective enough.
Mix: drug interaction
In an application Omez® may reduce the absorption of ampicillin esters, iron salts, itraconazole and ketoconazole, tk. omeprazole gastric pH increases.
As an inhibitor of cytochrome P450, omeprazole may increase concentration and reduce the excretion of diazepam, antykoahulyantov indirect actions (varfarina), phenytoin (preparations, metabolized in the liver with CYP2C19), that in some cases may require reducing the dose of these drugs.
At the same time, prolonged use of omeprazole dose 20 mg 1 time / day in combination with caffeine, theophylline, piroksikamom, diclofenac, naproxen, metoprolol, propranolol, ethanol, cyclosporine, lidokainom, quinidine and estradiol did not change their plasma concentration.
Concentrations of omeprazole and clarithromycin plasma increases during joint oral these drugs, while evidence interaction of omeprazole with metronidazole and amoxicillin have been identified.
Mix: terms of dispensing from pharmacies
The drug is released under the prescription.
Mix: terms and conditions of storage
List B. The drug should be stored in a dry, protected from light, inaccessible to children at temperature not exceeding 25 ° C. Shelf life – 2 year.
