Ortanol
Ortanol: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. For violations of liver function
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Ortanol
ATX code: A02BC01
Active ingredient: omeprazole (omeprazole)
Manufacturer: SANDOZ, dd (Slovenia)
Description and photo update: 2019-14-08
Prices in pharmacies: from 69 rubles.
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Ortanol is an inhibitor of H + -K + -ATPase, an antiulcer agent.
Release form and composition
Ortanol dosage forms:
- Capsules size No. 3: solid, with a body and cap of light pinkish-brown color, on which there is an inscription "OME 10" in black; contents - granules of light yellow color (7 pcs. in blisters, 1, 2 or 4 blisters in a package);
- Capsules size No. 2: solid, with a white body and lid, on which there is an inscription "OME 20" in black; contents - granules of light yellow color (7 pcs. in blisters, 1, 2 or 4 blisters in a package);
- Capsules size 1: solid, with a light pinkish-brown body and a white cap, on which there is an inscription "OME 40" in black; contents - granules of light yellow color (7 pcs. in blisters, 1, 2 or 4 blisters in a package);
- Lyophilisate for preparation of solution for infusion: powder or mass of almost white or white color (40 mg each in transparent glass vials, in a cardboard box 1, 5 or 10 vials).
The active substance of Ortanol is omeprazole:
- 1 capsule - 10 mg (size # 3), 20 mg (size # 2) or 40 mg (size # 1);
- 1 bottle of lyophilisate - 40 mg.
Auxiliary components of capsules: anhydrous lactose, microcrystalline cellulose, croscarmellose sodium, low-substituted hyprolose, povidone, hypromellose phthalate, polysorbate 80, talc, dibutylsebakate.
The composition of the capsule shell:
- Capsules 10 mg: hypromellose, carrageenan, potassium chloride, titanium dioxide, water, iron (III) oxide yellow and oxide red; ink for inscriptions - shellac, propylene glycol, anhydrous isopropanol, anhydrous ethanol, ammonium hydroxide, potassium hydroxide, purified water, iron (III) oxide black (E172);
- Capsules 20 mg: titanium dioxide, carrageenan, hypromellose, water, potassium chloride; ink for the inscription - ammonium hydroxide, anhydrous ethanol, butanol, anhydrous isopropanol, shellac, potassium hydroxide, propylene glycol, purified water, iron (III) oxide black (E172);
- Capsules 40 mg: potassium chloride, carrageenan, titanium dioxide, hypromellose, water, iron (III) oxide red and oxide yellow; ink for inscriptions - ammonium hydroxide, butanol, potassium hydroxide, anhydrous ethanol, propylene glycol, shellac, anhydrous isopropanol, purified water, iron (III) oxide black (E172).
Auxiliary components of the lyophilisate: disodium edetate dihydrate, sodium hydroxide.
Pharmacological properties
Pharmacodynamics
The mechanism of action of the drug
Omeprazole is a racemic mixture of two enantiomers that causes a decrease in gastric acid secretion through a highly selective mechanism of action. Being a weak base, omeprazole accumulates in the secretory tubules of the parietal cells of the stomach and is activated by inhibiting the enzyme H +, K + -ATPase. The degree of influence of the active substance on the formation of hydrochloric acid is dose-dependent. As a result, regardless of the stimulating factor, the basal and stimulated secretion of hydrochloric acid is inhibited. After a single oral administration, omeprazole begins to act within the first hour. The action of Ortanol lasts for 1 day. The maximum effect is achieved 2 hours after taking omeprazole. After stopping the use of Ortanol, the complete restoration of secretory activity occurs in 3-5 days.
Influence on the secretion of hydrochloric acid
In the case of oral administration of omeprazole once a day, day and night secretion of gastric juice is quickly and effectively inhibited. The maximum effect is achieved with treatment for 3-5 days. In case of duodenal ulcer, taking omeprazole at a dose of 20 mg leads to a decrease in daily gastric acidity by 80%. On average, the maximum acid secretion following stimulation with pentagastrin after 24 hours is approximately 70%. In such patients, when omeprazole is taken orally at a dose of 20 mg, the intragastric pH value averages> 3 for 17 hours a day.
The inhibition of acid secretion is influenced by the area under the concentration-time curve (AUC) and is not influenced by the plasma concentration of omeprazole at a particular point in time.
Effects on Helicobacter pylori
In vitro, omeprazole has a bactericidal effect on H. pylori. In the case of the combined use of omeprazole and antibacterial drugs, H. pylori eradication occurs, as a result of which symptoms are quickly eliminated, a high degree of healing of defects in the gastrointestinal tract is ensured. Also, the result is a long-term remission of peptic ulcer disease, which reduces the likelihood of bleeding and other complications with the same effectiveness as with constant maintenance therapy.
Other effects due to inhibition of acid secretion
There is evidence that with prolonged treatment, the frequency of the formation of glandular cysts in the stomach slightly increases. Such changes, which are the result of inhibition of the secretion of hydrochloric acid, are classified as benign and are reversible with continued therapy.
With a decrease in the secretion of hydrochloric acid in the stomach under the influence of proton pump inhibitors or other acid-inhibiting factors, the risk of developing intestinal infections may slightly increase, which are caused by the following pathogens: Campylobacter spp., Salmonella spp. and possibly Clostridium difficile.
When using drugs that reduce the secretion of gastric glands, the serum gastrin content increases. Due to a decrease in the concentration of hydrochloric acid, the concentration of chromogranin A in the blood plasma increases, which can cause false positive results in the diagnosis of neuroendocrine tumors. To prevent this effect, therapy with proton pump inhibitors should be suspended no later than 5-14 days before the study of the concentration of chromogranin A. If during the specified period the indicators have not returned to normal levels, the study should be repeated.
With prolonged use of omeprazole in adults and children, an increase in the number of enterochromaffin-like cells was recorded, possibly due to an increase in the content of gastrin in the blood serum. This phenomenon has no clinical significance.
Pharmacokinetics
Omeprazole is rapidly absorbed from the gastrointestinal tract. The time to reach the maximum plasma concentration is 1–2 hours. The antisecretory effect occurs within the first hour after oral administration and reaches a maximum after 2 hours. Omeprazole is absorbed in the small intestine, the process is completely completed in 3-6 hours. About 50% of the maximum secretion is inhibited within 1 day. After taking a single dose, bioavailability ranges from 30 to 40%, with repeated administration it increases to 60%. 97% binds to blood plasma proteins. The volume of distribution is 0.3 l / kg.
In the liver, with the help of cytochrome P 450 (CYP) isoenzymes, omeprazole is almost completely metabolized, resulting in the formation of six pharmacologically inactive enzymes. The main metabolic pathway is interaction with the isoenzyme CYP2C19. Another way is with the help of the cytochrome CYP3A4 isoenzyme. As a result of the high affinity for the CYP2C19 isoenzyme, competitive inhibition and metabolic interactions of omeprazole with other substrates of the CYP2C19 isoenzyme are possible. At the same time, due to the low affinity for the CYP3A4 isoenzyme, the active substance does not inhibit the metabolism of other substrates of the CYP3A4 isoenzyme. Also, omeprazole does not have an inhibitory effect on the main isoenzymes of the cytochrome CYP system.
In about 15–20% of Asians and 3% of Caucasians, the activity of the CYP2C19 isoenzyme is reduced, that is, they are "slow" metabolizers. In this case, the metabolism of omeprazole is probably predominantly via the CYP3A4 isoenzyme. In the case of repeated use of omeprazole at a dose of 20 mg once a day in "slow" metabolizers, the average AUC is 5-10 times higher than in patients in whom the activity of the CYP2C19 isoenzyme is normal. In these cases, the mean peak plasma concentrations were also 3–5 times higher. The given data do not affect the dosage regimen of Ortanol.
The half-life is from 0.5 to 1 hour. It is excreted by the kidneys in the form of metabolites (from 70 to 80%) and in the bile (from 20 to 30%).
Total plasma clearance is from 0.3 to 0.6 l / min.
When liver function is impaired, the bioavailability of omeprazole increases, and plasma clearance decreases significantly.
In case of impaired renal function, significant changes in the pharmacokinetics of omeprazole were not recorded. In patients with chronic renal failure, excretion decreases in proportion to the decrease in creatinine clearance.
The metabolic rate of omeprazole in elderly patients (over 75 years old) is slightly reduced.
Indications for use
- Peptic ulcer and 12 duodenal ulcer (including prevention of relapse);
- Hypersecretory conditions (stress ulcers of the gastrointestinal tract, Zollinger-Ellison syndrome, systemic mastocytosis, polyendocrine adenomatosis);
- Reflux esophagitis;
- Gastroesophageal reflux (symptomatic treatment);
- Eradication of Helicobacter pylori in infected patients with gastric ulcer and 12 duodenal ulcer (as one of the components of combination therapy);
- Treatment and prevention of damage to the mucous membrane of the stomach and duodenum 12 (dyspepsia, peptic ulcer, erosion of the mucous membrane) due to the intake of non-steroidal anti-inflammatory drugs (NSAIDs).
Contraindications
Absolute:
- Age under 18;
- Lactation;
- Concomitant use of atazanavir, erlotinib, nelfinavir, posaconazole;
- Hypersensitivity to any component of Ortanol or substituted benzimidazoles.
According to the instructions, Ortanol should be used with caution in the following cases:
- Renal / hepatic impairment;
- Osteoporosis;
- The presence of "alarming symptoms": repeated vomiting, vomiting of blood, discoloration of feces (melena), swallowing disorders, significant weight loss, vitamin B 12 deficiency;
- Pregnancy period;
- Simultaneous use of St. John's wort, rifampicin, voriconazole, clarithromycin, diazepam, warfarin, clopidogrel, saquinavir, cilostazol, itraconazole, tacrolimus, phenytoin.
Instructions for the use of Ortanol: method and dosage
Capsules
Ortanol is taken orally before meals, with a single use - preferably before breakfast: the capsules are swallowed whole and washed down with a sufficient amount of water.
For patients who have difficulty swallowing, the capsules can be dissolved in a small amount of fruit juice (such as orange or apple juice) or water.
Recommended dosage regimens of Ortanol, depending on the indications:
- Duodenal ulcer: 20 mg 1 time per day for 2 weeks. If complete scarring after the end of therapy is not noted, another 2-week course is carried out;
- Duodenal ulcer disease resistant to therapy: 40 mg 1 time per day for 2-4 weeks;
- Peptic ulcer: 20 mg once a day for 4 weeks. If complete scarring after the end of therapy is not noted, another 4-week course is carried out;
- Peptic ulcer, resistant to therapy: 40 mg 1 time per day for 4-8 weeks;
- Hypersecretory states: the dose is selected individually, the recommended initial dose is 60 mg once a day, the maximum daily dose is 120 mg. If the dose exceeds 80 mg per day, it should be divided into several doses;
- Eradication of Helicobacter pylori (in combination with antibacterial agents): 20 mg 2 times a day for 2 weeks;
- Reflux esophagitis: 20 mg once a day for a 4-week course. If a complete cure does not occur after the end of therapy, a repeated 4-week course is carried out. In severe forms of the disease, the duration of treatment can be extended to 8 weeks;
- Damage to the mucous membrane of the gastrointestinal tract due to the use of NSAIDs: prevention - 20 mg 1 time per day during the entire course of NSAID use, treatment - 20 mg 1 time per day for 4-8 weeks.
There is no need to adjust the dose in patients with impaired renal function. Patients with severe liver disease and the elderly should not exceed a dose of 20 mg per day.
Lyophilisate for preparation of solution for infusion
Oratnol is administered intravenously for 20-30 minutes.
In this dosage form, the drug is prescribed when it is impossible to conduct oral therapy.
Patients with reflux esophagitis, gastric ulcer and 12 duodenal ulcer are prescribed 40 mg once a day.
For patients with Zollinger-Ellison syndrome, the recommended dose is 60 mg once a day. If necessary, it is increased to 80-120 mg per day, but in this case it is divided into 2 administrations.
In case of impaired liver function, the maximum daily dose of Ortanol is 20 mg.
Rules for the preparation of a solution for injection (for 1 vial of lyophilisate, 100 ml of glucose solution 5% or sodium chloride 0.9% is required):
- From a vial with a solvent or an infusion bag, draw 5 ml of solution into a syringe;
- Introduce the solvent into the vial with Ortanol lyophilizate and mix thoroughly until the powder is completely dissolved;
- Draw up omeprazole solution into a syringe and transfer it to an infusion bag or vial with solvent;
- Repeat the first three steps until all of the omeprazole has been transferred.
An alternative method for preparing solutions for infusion in soft containers using a double-sided needle adapter:
- Insert one end of the needle into the vial with lyophilisate, and attach the other to the infusion bag with the solution for infusion;
- Dissolve the lyophilisate by pumping the infusion solution between the bag and the vial;
- Make sure that the powder is completely dissolved, then disconnect the empty bottle and remove the needle from the bag.
The resulting solution cannot be reused. Its physical and chemical stability is maintained for 4 hours when stored in a dark place at temperatures up to 25 ºС.
From a microbiological point of view, the diluted solution should be used immediately.
Side effects
- From the hematopoietic system: in individual cases - thrombocytopenia, agranulocytosis, pancytopenia, leukopenia;
- From the nervous system: in the presence of concomitant severe somatic diseases - headache; rarely - vertigo, insomnia, drowsiness, impaired taste, paresthesia; very rarely - reversible confusion, agitation, depression; in patients with severe liver disease - encephalopathy;
- From the digestive system: rarely - flatulence, diarrhea / constipation, abdominal pain, nausea and / or vomiting; very rarely - increased activity of hepatic transaminases and alkaline phosphatase, stomatitis, dry mouth; after severe liver diseases - liver dysfunction, hepatitis; with long-term treatment - the formation of reversible benign gastric glandular cysts;
- From the musculoskeletal system: arthralgia, myalgia; in individual cases, muscle weakness;
- On the part of the skin: increased sweating, photosensitivity, alopecia, erythema multiforme exudative;
- Allergic reactions: rarely - itching, urticaria; very rarely - fever, interstitial nephritis, eosinophilia, anaphylactoid reactions, bronchospasm, angioedema;
- Others: blurred vision, peripheral edema, gynecomastia.
The side effects arising from taking Ortanol are usually mild and transient.
Overdose
A single intake of omeprazole at a dose of 560 mg in adult patients caused symptoms of moderate intoxication. A case of a single dose of 2400 mg omeprazole without severe toxic symptoms was also described. In the case of increasing the dose, the rate of elimination of omeprazole did not change (first-order kinetics). In these cases, no specific treatment was required.
Symptoms: nausea, vomiting, dry mouth, diarrhea, flatulence, headache, increased sweating, dizziness, drowsiness, blurred vision, confusion, tachycardia.
Treatment: symptomatic. There is no specific antidote. Hemodialysis is ineffective due to the high degree of protein binding.
special instructions
Before prescribing Ortanol, the patient must undergo an examination to exclude the presence of a malignant process, since omeprazole can mask symptoms and thereby delay the timely diagnosis.
With long-term treatment, patients should be under constant medical supervision.
Ortanol can reduce the absorption of vitamin B 12 due to hypo- or achlorhydria, which should be considered when treating patients with cyanocobalamin deficiency or at risk of developing it.
During treatment with Ortanol, the concentration of chromogranin A in the blood plasma may increase, which may lead to false-positive results when diagnosing patients with suspected neuroendocrine tumors. For this reason, 5-14 days before the prescribed study, it is necessary to suspend omeprazole therapy.
For patients at risk of developing osteoporosis, additional prescription of calcium and vitamin D preparations is recommended, since long-term use of proton pump inhibitors can lead to a moderate increase in the risk of vertebral, hip and wrist fractures, especially in the elderly and in patients with other known factors risk.
During treatment with Ortanol, it is recommended to be careful when driving a car and performing work that requires increased attention and a high reaction rate.
Application during pregnancy and lactation
The use of Ortanol during pregnancy is not recommended. If it is necessary to take the drug during lactation, it is recommended to stop breastfeeding.
Pediatric use
It is forbidden to use Ortanol for the treatment of patients under the age of 18 years.
For violations of liver function
According to the instructions, Ortanol is prohibited for use in chronic liver diseases (including a history).
Drug interactions
Omeprazole can increase the half-life and increase the concentration of phenytoin, diazepam, warfarin and other drugs that are metabolized in the liver with the participation of the isoenzyme CYP2C19, and therefore their blood levels should be monitored and the dose should be reduced if necessary.
With simultaneous use of omeprazole increases the bioavailability of digoxin by 10%.
In the case of a combined appointment, a violation of the absorption of drugs is possible, the bioavailability of which is determined mainly by the acidity of gastric juice, for example, cyanocobalamin, iron salts, ampicillin esters, itraconazole, ketoconazole.
Ortanol can enhance the inhibitory effect on the hemostasis system of other drugs.
No clinically significant interaction with lidocaine, caffeine, ethanol, propranolol, theophylline, metoprolol, quinidine, antacids has been established.
Analogs
Ortanol analogs are: Omez, Gasek, Loseprazole, Omelic, Omeprazole, Omeprazole-Akrikhin, Ultop.
Terms and conditions of storage
Store in a place protected from light, out of reach of children, at temperatures up to 25 ° C.
Shelf life is 2 years.
The solution prepared from the lyophilisate can be stored for no more than 4 hours at temperatures up to 25 ºС.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Ortanol
Reviews of Ortanol indicate that, due to the strong action of the drug, to achieve the desired result and prevent side effects, the drug should be taken only after consulting a doctor.
Ortanol price in pharmacies
The approximate price for Ortanol: 14 capsules 10 mg - 107 rubles, 28 capsules 10 mg - 181 rubles, 14 capsules 20 mg - 110 rubles, 28 capsules 20 mg - 156 rubles, 7 capsules 40 mg - 140 rubles, 28 capsules 40 mg - 388 rubles.
Ortanol: prices in online pharmacies
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Drug name Price Pharmacy |
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Ortanol 20 mg capsules 14 pcs. RUB 69 Buy |
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Ortanol capsules 20mg 14 pcs. RUB 80 Buy |
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Ortanol 10 mg capsules 14 pcs. RUB 90 Buy |
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Ortanol 10 mg capsules 28 pcs. RUB 100 Buy |
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Ortanol 20 mg capsules 28 pcs. 102 RUB Buy |
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Ortanol 40 mg capsules 14 pcs. 125 RUB Buy |
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Ortanol capsules 20mg 28 pcs. 139 RUB Buy |
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Ortanol capsules 10mg 28 pcs. RUB 150 Buy |
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Ortanol 40 mg capsules 28 pcs. RUB 318 Buy |
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Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
