Lansazole
Lansazol: 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. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Lansazol
ATX code: A02BC03
Active ingredient: lansoprazole (Lansoprazole)
Manufacturer: JSC "Borisov Plant of Medical Products" (JSC "BZMP") (Republic of Belarus)
Description and photo update: 2019-09-07
Lansazole is an antiulcer drug, proton pump inhibitor.
Release form and composition
The drug is available in the form of capsules: No. 0, hard gelatinous, cylindrical, white, the ends of the capsules are hemispherical (10 pcs. In blisters, 2 packs in a cardboard box and instructions for use of Lansazol).
1 capsule contains:
- active substance: lansoprazole - 30 mg (in the form of lansoprazole pellets 8.5%);
- auxiliary components: lactose, sucrose, mannitol, calcium carboxymethyl cellulose, povidone S-630, hydroxypropyl methylcellulose, magnesium carbonate, methacrylic acid L30D, cetyl alcohol, tween-80, propylene glycol, sodium hydroxide, titanium dioxide;
- capsule composition: gelatin, titanium dioxide.
Pharmacological properties
Pharmacodynamics
Lansazole is an anti-ulcer drug intended for the treatment of conditions associated with a violation of acidity levels and in gastroesophageal reflux disease. Its active ingredient, lansoprazole, inhibits the H + / K + adenosine triphosphatase (H + / K + ATPase) enzyme in the parietal cells of the stomach or a proton pump, blocking the synthesis of hydrochloric acid at the final stage of formation. Regardless of the reason for the increased production of gastric juice, it helps to reduce the level of basal and stimulated secretion. The effect on the secretion of hydrochloric acid occurs as a result of the accumulation of lansoprazole in parietal cells, where it is activated under the influence of their acidic environment and reacts with sulfhydryl groups H +/ 1SATP-ases, inhibiting the activity of the enzyme.
Lansoprazole at a dose of 30 mg after oral administration causes inhibition of pentagastrin-stimulated secretion of hydrochloric acid in the stomach by about 80%, a decrease in basal secretion by 70%, which provides rapid relief of symptoms. Against the background of regular administration of the drug for 7 days, the synthesis of induced hydrochloric acid is inhibited by 90%. Taking 1 capsule per day in the treatment of gastric ulcer and duodenal ulcer in most cases provides recovery within 14 days, with gastric ulcer and reflux esophagitis - within 28 days.
Reducing the acidity of gastric juice increases the effectiveness of the corresponding antibacterial agents against Helicobacter pylori.
The inhibition of the secretion of hydrochloric acid is accompanied by an increase in the concentration of gastrin in the blood serum. It should be borne in mind that a decrease in gastric acidity causes an increase in chromogranin A (CgA), which distorts the results of studies in the diagnosis of neuroendocrine neoplasms. Therefore, Lansazole should be discontinued 5-14 days prior to the CgA study.
Pharmacokinetics
Lansoprazole is a racemate of two active enantiomers, biotransformed in the acidic medium of parietal cells into an active form. Under the influence of hydrochloric acid, it is quickly inactivated, therefore it is taken internally in the form of enteric coated pellets. Possesses high bioavailability - 80-90%. The maximum concentration (C max) in the blood plasma is reached within 1.5–2 hours. Simultaneous food intake reduces bioavailability and slows down the rate of absorption by 50%.
The protein binding of lansoprazole is high - at the level of 97%.
The substance is actively metabolized in the liver, mainly with the participation of CYP2C19 and CYP3A4 enzymes with the formation of the following inactive metabolites: 5-hydroxyl lansoprazole, sulfone, sulfide.
The half-life (T 1/2) after a single dose is 1-2 hours, it does not cumulate in the body.
Up to 35% is excreted through the kidneys, the rest of the dose taken through the intestines.
In elderly patients, there is a decrease in the clearance of lansoprazole and an increase in T 1/2 by 1–2 hours, C max does not increase.
With a mild degree of liver failure, the effect of Lansazole is doubled, with a moderate and severe degree of liver failure, the effect of the drug is significantly increased.
In individuals homozygous for the mutant CYP2C19 allele and lacking a functional CYP2C19 enzyme, the effect of Lansazole is several times stronger than that of fast metabolizers.
Indications for use
- peptic ulcer of the stomach and duodenum;
- treatment and prevention of erosive and ulcerative lesions of the stomach and duodenum caused by the use of non-steroidal anti-inflammatory drugs (NSAIDs);
- treatment and prevention of reflux esophagitis;
- symptomatic gastroesophageal reflux disease;
- Zollinger-Ellison syndrome;
- eradication of Helicobacter pylori infection (as part of antibacterial combination therapy).
Contraindications
Absolute:
- malignant neoplasms of the gastrointestinal tract;
- concomitant therapy with nelfinavir;
- fructose intolerance, sucrase-isomaltase deficiency, glucose-galactose malabsorption syndrome;
- period of pregnancy;
- breast-feeding;
- age up to 18 years;
- hypersensitivity to the components of Lansazole.
With caution, Lansazol capsules should be prescribed for moderate and severe liver dysfunction, as well as in elderly patients.
Lansazol, instructions for use: method and dosage
Lansazol capsules are taken orally, swallowing whole 0.5 hours before meals, with a sufficient amount of liquid.
If the patient is unable, for a number of reasons, to swallow the capsule whole, the drug can be taken by mixing the contents of the capsule with 1 tablespoon of yogurt, apple or tomato juice. In addition, it is possible to administer a solution of 40 ml of apple juice and the contents of one capsule through a nasogastric tube.
The suspension or mixture should be used immediately after preparation. If it is necessary to prescribe at a dose below 30 mg, it is recommended to use another dosage form.
The recommended dosage regimen of Lansazol, depending on the indications:
- peptic ulcer of the stomach and duodenum: 30 mg (1 pc.) 1 time per day. Course duration - 14 days, in case of resistance - up to 28 days;
- erosive-ulcerative esophagitis, acute period of gastric ulcer: 30 mg 1 time per day for 28 days. In the absence of a sufficient therapeutic effect, treatment can be extended up to 56 days;
- prevention of esophagitis: 15 mg once a day, if necessary, the initial dose can be increased to 30 mg;
- eradication of Helicobacter pylori: 30 mg 2 times a day. The duration of the course of treatment is 7-14 days. Lansazole is taken in combination with the following antibiotic doses: clarithromycin (250-500 mg 2 times a day) + amoxicillin (1000 mg 2 times a day) or clarithromycin (250 mg 2 times a day) + metronidazole (400-500 mg 2 times a day) day);
- treatment of erosive and ulcerative lesions of the stomach and duodenum caused by taking NSAIDs: 30 mg 1 time per day for 28–56 days. If the body is resistant to the therapy, the dose and the period of treatment are increased;
- symptomatic gastroesophageal reflux disease: 15–30 mg once a day for 28 days;
- Zollinger-Ellison syndrome: the initial dose is 60 mg once a day, then the dose is selected individually. The maximum daily dose is 180 mg. If the daily dose exceeds 120 mg, it should be divided into 2 doses.
Anti-relapse treatment of gastric ulcer and duodenal ulcer caused by taking NSAIDs in patients with a history of ulcerative pathologies and over the age of 65 is carried out at a dose of 15 mg 1 time per day, if necessary, the dose can be increased to 30 mg.
In renal failure, dose adjustment of Lansazole is not required.
In moderate or severe liver dysfunction, it is recommended to use 15 mg of lansoprazole per day and close monitoring of the patient's condition.
In elderly patients, the dose of Lansazol is selected individually, it must strictly correspond to the clinical indications.
Side effects
- from the gastrointestinal tract: often - stomach pain, dry mouth or throat, diarrhea, constipation, nausea, vomiting, benign stomach polyps; rarely - a violation of taste, esophageal candidiasis, glossitis, pancreatitis; very rarely - stomatitis, colitis;
- from the hepatobiliary system: often - an increase in the level of liver enzymes; rarely - jaundice, hepatitis;
- from the lymphatic system and blood: infrequently - leukopenia, thrombocytopenia, eosinophilia; rarely - anemia; very rarely - pancytopenia, agranulocytosis;
- from the psyche: infrequently - depression; rarely - insomnia, confusion, hallucinations;
- from the nervous system: often - headache, dizziness; rarely - drowsiness, restlessness, vertigo, paresthesia, tremor;
- dermatological reactions: often - itching, rash, urticaria; rarely - erythema, petechiae, hair loss, purpura, photosensitivity; very rarely - toxic epidermal necrolysis, Stevens-Johnson syndrome;
- from the musculoskeletal system: infrequently - arthralgia, myalgia, fracture of the wrist, hip and / or spine;
- from the urinary system: rarely - interstitial nephritis;
- from the reproductive system: rarely - gynecomastia, impotence;
- on the part of the visual system: rarely - visual disturbances;
- general disorders: often - fatigue; infrequently - edema; rarely - hyperhidrosis, fever, angioedema, anorexia; very rarely - anaphylactic shock;
- on the part of metabolic processes and nutrition: the frequency is not established - hypomagnesemia;
- laboratory parameters: very rarely - hyponatremia, increased triglyceride and cholesterol levels.
Overdose
Cases of overdose of lansoprazole have not been established. A single intake of the drug in a dose of 600 mg was not accompanied by clinical symptoms of an overdose.
If you suspect a significant excess of the permissible dose, it is recommended to monitor the patient's condition, prescribe symptomatic therapy.
Hemodialysis is not effective.
special instructions
Lansoprazole can mask the symptoms of malignant neoplasms of the stomach and postpone the correct diagnosis. To exclude the presence of a tumor, endoscopic studies of the gastrointestinal tract must be performed before the appointment of Lansazol.
A decrease in gastric acidity while taking Lansazole increases the number of bacteria in the gastrointestinal tract, which may increase the risk of infections caused by Salmonella and Campylobacter.
It should be borne in mind that in case of gastric ulcer and duodenal ulcer, Helicobacter pylori infection can be an etiological factor.
Combined antibiotic therapy for the eradication of Helicobacter pylori should be accompanied by careful monitoring.
If severe or persistent diarrhea occurs, it is recommended to consider discontinuing Lansazole.
When Lansazole is prescribed for the prevention of peptic ulcer disease caused by prolonged use of NSAIDs, patients who have to take NSAIDs in the highest possible doses for a long time are primarily at risk of complications. In addition, elderly patients with a history of gastrointestinal bleeding, the presence of perforations, ulcers or other concomitant pathologies, who are on concomitant therapy with corticosteroids or anticoagulants.
Treatment with proton pump inhibitors can often cause hypomagnesemia in the patient, symptoms of which are fatigue, ventricular arrhythmia, convulsions, and dizziness. With long-term therapy with Lansazole in combination with diuretics and other drugs that cause hypomagnesemia, regular monitoring of the level of magnesium in the blood should be ensured and an additional intake of magnesium preparations should be prescribed.
In order to reduce the risk of fractures of the hip, wrist or spine, patients who take high doses of Lansazole for a long time are advised to take vitamin D and calcium supplements at the same time.
Application during pregnancy and lactation
The use of Lansazol is contraindicated during the period of gestation and breastfeeding.
Pediatric use
Lansazole is contraindicated for the treatment of patients under the age of 18 years.
With impaired renal function
Patients with renal impairment do not need to adjust the Lansazole dosage regimen.
For violations of liver function
Lansazole should be used with caution to treat patients with moderate to severe hepatic impairment.
Use in the elderly
Care should be taken when prescribing Lansazole to elderly patients.
Drug interactions
The following reactions of drug / drug interactions are possible when used simultaneously with Lansazole:
- atazanavir, ketoconazole, itraconazole, digoxin: lansoprazole causes a malabsorption of these drugs, due to the fact that their bioavailability depends on the acidity of gastric juice. So the exposure of atazanavir is significantly reduced, and the level of concentration of ketoconazole, itraconazole or digoxin increases. Therefore, it is recommended to avoid the combination of lansoprazole with atazanavir, ketoconazole and itraconazole. In the case of combined use with digoxin, its level in blood plasma should be monitored and the dose adjusted if necessary;
- substances transported with the participation of P-glycoprotein: the ability of lansoprazole to inhibit the transport of P-glycoprotein has been established in vitro, but the clinical significance of this effect has not been established;
- drugs whose metabolism occurs with the participation of CYP3A4 enzymes: it is necessary to take these drugs with a narrow therapeutic range simultaneously with lansoprazole with caution, since it significantly changes their plasma concentrations, for example, theophylline - its level in plasma decreases and the clinical effect is weakened; tacrolimus - plasma concentrations of the substance increase to 81%, which requires monitoring of its plasma content at the beginning of simultaneous use with Lansazole and at the end of combination therapy;
- CYP2C19 enzyme inhibitor fluvoxamine: promotes a fourfold increase in the plasma concentration of lansoprazole, therefore, when combined, lower doses of Lansazole should be used;
- inducers of enzymes CYP2C19 and CYP3A4, for example, rifampicin, St. John's wort: can cause a decrease in the level of lansoprazole in plasma;
- warfarin: the combination with warfarin should be accompanied by monitoring of the International Normalized Ratio (INR) and prothrombin time;
- antacids, including sucralfate: it should be borne in mind that antacids reduce the bioavailability of lansoprazole, therefore, capsules should be taken no earlier than 1 hour after taking antacids;
- NSAIDs: no clinically significant interaction with lansoprazole has been established, but specific studies of this combined use have not been conducted.
Analogs
Lansazol analogues are Lansoprazole, Lanzoptol, Lancid, Epicur, Akrilanz, Helikol, Lanzabel, Lanzap, Lansoprazole Stada, Lansofed, Loenzar-sanovel, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C, protected from moisture and light.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Lansazole
The few reviews about Lansazole are positive. Patients recommend using the drug only as directed by a doctor. They indicate the high efficiency of the drug, the relief of pain within an hour after taking the first pill, as well as its low cost.
Medical experts say that side reactions when taking Lansazol are extremely rare.
The price of Lansazol in pharmacies
The price of Lansazole is currently not known due to the lack of the drug in the pharmacy chain.
Estimated cost of direct analogues of the drug with an identical active ingredient:
- Epicurus, capsules of 14 pcs. in a package, dosage 30 mg - 396 rubles;
- Lancid, capsules of 30 pcs. in the package: dosage 30 mg - 378 rubles; dosage 15 mg - 276 rubles.
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, 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!
