Lansoprol

Lansoprol is a proton pump inhibitor.

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Indications Lansoprol

Shown for:

• benign form of duodenal ulcer or gastric ulcer (also associated with the use of NSAIDs);
• development of GERD;
• ulcerogenic adenoma of the pancreas;
• elimination of the microorganism Helicobacter pylori (in combination with the use of antibiotics).

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Release form

It is produced in capsules of 7 pieces per blister (the pack contains 2 or 4 blister plates). Also, there can be 14 capsules on 1 blister (in this case, there will be 1 or 2 blister plates in the pack). Sometimes the blister consists of 4 capsules (in this case, one package will contain 1 blister plate).

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Pharmacodynamics

Lansoprazole inhibits the active action of the H ⁺ K ⁺ ATPase proton pump inside the parietal cells of the gastric mucosa. This allows the drug to suppress the process of gastric acid production occurring at the final stage and reduces its acidity and quantity inside the gastric juice. Due to such actions, the negative impact of gastric juice on the mucosa is significantly reduced.

The strength of activity suppression depends on the duration of the treatment process, as well as the size of the drug dose. Even with a single dose of 30 mg of the drug, gastric juice secretion is suppressed by approximately 70-90%. Lansoprazole begins to act approximately 1-2 hours after administration. The effect of the drug dose lasts for 1 day.

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Pharmacokinetics

The substance is absorbed inside the intestine. The peak plasma level in volunteers who took 30 mg of the drug was 0.75-1.15 mg/l, and it took 1.5-2 hours to reach it. Plasma values and bioavailability levels depend on individual characteristics of a person, so they do not change in relation to the frequency of drug use.

The drug is 98% synthesized with protein.

Lansoprazole is excreted with bile and urine (exclusively in the form of decay products - lansoprazole sulfone with hydroxylansoprazole). About 21% of the drug is excreted in urine per day.

The half-life is 1.5 hours. This period becomes longer in people with severe liver dysfunction and in elderly patients (over 69 years of age). In case of renal dysfunction, the absorption rates of the active substance remain almost unchanged.

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Dosing and administration

The drug is taken orally. The dosage is usually 30 mg once a day (30-40 minutes before meals). The capsule should be taken with water (150-200 ml) without chewing. If it is not possible to take the medicine in this way, the capsule can be opened and then the powder inside dissolved in apple juice (1 full spoon is enough), then swallowed immediately without chewing the mixture. A similar procedure is also carried out when administering the drug through a nasogastric tube.

Regarding the duration of the therapeutic course, as well as the dose sizes, they are determined by the attending physician, taking into account the nature of the pathology, as well as the clinical picture.

No more than 60 mg of the drug can be taken per day, and for people with liver disorders - no more than 30 mg. For people with ulcerogenic adenoma of the pancreas, the dosage may be increased.

If you need to take 2 daily doses, you need to take one of them in the morning, before breakfast, and the second in the evening, before dinner.

If you do not take the medicine during the prescribed period, you must take the capsule as soon as possible after this period. But if there is little time left before taking the next capsule, you do not need to take the missed dose.

In case of duodenal ulcer: active phases of the pathology are treated with 30 mg once a day for 0.5-1 month. In case of ulcers caused by NSAIDs, the dosage is the same as indicated above, and the treatment period is 1-2 months.

For the prevention of ulcers caused by long-term use of NSAIDs, people from the risk category (over 65 years old or with a history of duodenal ulcer or gastritis) - the daily dose is 15 mg. If there is no effect, it should be increased to 30 mg.

Benign form of gastric ulcer: when eliminating the active phase, it is necessary to drink 30 mg of the drug per day once for 2 months. During the treatment of ulcers that arose due to the use of NSAIDs, the drug in the same dose is used for a period of 1-2 months.

For the treatment of GERD: it is recommended to drink 15-30 mg per day. With such treatment, the condition improves quickly. Individual dosages are also considered. If there is no improvement after 1 month of using the drug in a daily dose of 30 mg, additional testing is required.

In case of treatment of severe or moderate esophagitis, it is required to take 30 mg of the medicine per day once during the first month. If the pathology is not eliminated during the specified period of time, the course can be extended for another month.

For long-term prevention of relapse of erosive esophagitis, a single daily dose is 15-30 mg. The effectiveness and safety of maintenance treatment in such doses over a period of 12 months has been confirmed.

Destruction of the Helicobacter pylori microbe: take 30 mg of the medicine in the morning and evening (both times before meals). The capsules should be taken for 1-2 weeks in combination with antibiotics in accordance with the selected treatment regimen.

Ulcerogenic adenoma of the pancreas: the dosage is determined individually, taking into account that the basal acid secretion rate is not higher than 10 mmol/hour. At the beginning of treatment, it is recommended to drink 60 mg once a day before the morning meal. In case of using more than 120 mg per day, half of the dosage should be taken before breakfast, and the second part - before the evening meal. The course lasts until the symptoms of the disease disappear.

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Use Lansoprol during pregnancy

The medicine is not prescribed to pregnant women or lactating women. If the medicine must be taken during lactation, breastfeeding should be stopped for the duration of treatment.

Contraindications

Among the contraindications:

• hypersensitivity to lansoprazole or other components of the drug;
• combined use with atazanavir;
• the presence of malignant tumors in the digestive tract;
• childhood.

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Side effects Lansoprol

During the therapy period, there are often reports of diarrhea (most often), as well as nausea and abdominal pain. Headaches are also often observed. Among other side effects:

• cardiovascular system organs: development of vasodilation, angina pectoris, myocardial infarction, shock, as well as palpitations and cerebrovascular changes, as well as an increase/decrease in blood pressure;
• Digestive tract organs: vomiting or constipation, anorexia, cholelithiasis, cardiospasm, hepatitis with hepatotoxicity, and jaundice. Thirst and dry mouth mucous membranes, candidiasis inside the digestive tract (on the mucous membranes), belching, swallowing disorder, esophageal stenosis, and bloating may also develop. Dyspeptic symptoms, gastric polyps, esophagitis, colitis with gastroenteritis, and changes in feces color are possible. In addition, the following may appear: vomiting with blood, bleeding in the gastrointestinal tract or in the anus, worsening or increasing appetite, increased salivation, stomatitis, melena, pancreatitis with glossitis, ulcerative colitis, taste disorder, and tenesmus;
• metabolic processes: development of hypomagnesemia;
• endocrine system organs: the appearance of goiter, the development of diabetes mellitus, as well as hyper- or hypoglycemia;
• lymph and hematopoietic system: development of anemia (also its hemolytic or aplastic forms), agranulocytosis, neutro-, thrombocyto-, leukopenia- and pancytopenia, as well as eosinophilia, hemolysis and thrombotic, as well as thrombocytopenic forms of purpura;
• skeletal and muscular structure: muscle or joint pain, arthritis, musculoskeletal pain;
• organs of the nervous system: the appearance of amnesia, dizziness, hallucinations, as well as feelings of fear, depression, apathy, nervousness and hostility. In addition, drowsiness or insomnia appears, increased excitability, vertigo, paresthesia with tremor, hemiparesis, and confusion develop. Fainting and mental disorders appear, libido decreases;
• respiratory system organs: the appearance of cough, dyspnea, hiccups, development of runny nose, asthma and pharyngitis. Infectious processes also occur in the lower and upper respiratory system (pneumonia and bronchitis), bleeding from the nose and in the lungs;
• subcutaneous tissue with skin: Lyell's and Stevens-Johnson syndromes, Quincke's edema, acne, erythema multiforme, hair loss, rashes with itching and urticaria, facial hyperemia, photophobia, petechiae, purpura, and increased sweating;
• sensory organs: eye pain, speech problems, development of deafness or otitis media, blurred vision, defects in the visual fields, taste bud disorders, tinnitus;
• urogenital system organs: tubulointerstitial nephritis (may develop into renal failure), formation of kidney stones, problems with urination, albuminuria or hematuria with glucosuria, development of impotence, menstrual irregularities, pain in the mammary glands, enlargement of the mammary glands or gynecomastia;
• with triple therapy using clarithromycin, lansoprazole and amoxicillin: most often during a 2-week period, diarrhea, changes in taste sensations, and headaches are observed; with double therapy with a combination of lansoprazole and amoxicillin: development of headaches, as well as diarrhea. Such manifestations are short-lived and pass without stopping the course of treatment;
• analysis data: increase in ALP, ALT with AST, as well as globulins, creatinine and γ-GTP, as well as imbalance in the proportions of albumins with globulins. Along with this, there is a decrease / increase in the leukocyte index, eosinophilia with bilirubinemia and hyperlipidemia, as well as a change in the number of erythrocytes. In addition, the electrolyte index decreases / increases, cholesterol decreases / increases, urea or potassium values u200bu200bincrease, hemoglobin decreases, glucocorticoids or low-density lipoproteins increase. An increase in gastrin values, a decrease / increase in platelet levels, as well as a positive test result for occult blood are possible. In the urine - the development of hematuria, albuminuria or glucosuria, as well as the appearance of salts. There is information about an increase in liver enzyme values (3 times higher than the maximum normal limit) by the end of the treatment course, but without the development of jaundice;
• other: anaphylaxis, anaphylactoid manifestations, development of candidiasis, asthenia, fever. In addition, there is also increased fatigue, swelling, pain in the sternum, bad breath, development of flu-like syndrome, infectious processes, as well as a feeling of weakness.

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Interactions with other drugs

Lansoprol, like other proton pump inhibitors, reduces the level of atazanavir (a substance that inhibits HIV protease), the absorption of which depends on the level of stomach acidity, which is why this can affect the therapeutic properties of atazanavir and at the same time cause resistance to HIV infection. As a result, combining the above drugs is prohibited.

Lansoprazole can increase the plasma level of drugs that are metabolized by CYP3A4 (drugs such as warfarin with indomethacin, antipyrine, phenytoin, diazepam with ibuprofen, clarithromycin, propranolol, terfenadine or prednisolone).

Medicines that inhibit 2C19 function (such as fluvoxamine) significantly increase the plasma level of Lansoprol (4-fold). Therefore, if they are combined, the dose of the latter must be adjusted.

Inducers of 2C19 elements, as well as CYP3A4 (such as St. John's wort or rifampicin) can significantly reduce the lansoprazole index in plasma. The combination of these drugs requires a correction of the dosage of the latter.

Lansoprazole suppresses the process of gastric secretion for a long time, which is why it can theoretically affect the bioavailability of those drugs for which the pH level is important for absorption (such as digoxin, ketoconazole and ampicillin esters with itraconazole and iron salts).

Combined use with digoxin may increase its plasma level. Therefore, when combining these drugs, constant monitoring of digoxin levels will be required, followed by dose adjustment (if necessary, and also after cessation of lansoprazole use).

Combination with antacids or sucralfate may reduce the bioavailability of lansoprazole, so the latter should be taken at least 1 hour after using these drugs.

Combined administration with theophylline (CYP1A2 and CYP3A elements) moderately increases the clearance of the latter (up to 10%), but at the same time, a medicinally significant interaction between the drugs is unlikely. Although, to maintain the theophylline level in medicinally effective values, dosage adjustment may sometimes be required at the initial stage or after completion of lansoprazole use.

Lansoprazole has no effect on the pharmacokinetic properties of warfarin, nor on its prothrombin time.

An increase in INR and PT can cause bleeding and, in the worst cases, death.

Combination of lansoprazole with tacrolimus may increase the plasma level of the latter. This is especially true for people who have had an organ transplant. Therefore, it is necessary to monitor the plasma levels of tacrolimus at the beginning of treatment and then after stopping lansoprazole.

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Storage conditions

The medicine is kept in a place closed to children. The temperature indicators cannot exceed 25°C.

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Shelf life

Lansoprol is permitted to be used for 3 years from the date of release of the drug.

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