Lancerol

Lancerol is a proton pump inhibitor used to treat GERD and ulcerative pathologies.

Indications Lancerola

Shown for:

• duodenal ulcer or gastric ulcer (benign forms), also in the treatment of these diseases that have arisen as a result of taking NSAIDs;
• treatment of GERD;
• treatment of gastrinoma,
• to destroy the pathogenic bacterium Helicobacter pylori (combining the drug with antibiotics).

Release form

Available in capsules, 1 blister contains 10 pieces. Inside one pack is 1 blister plate.

Pharmacodynamics

Lansoprazole inhibits the processes of action of the H ⁺ K ⁺ -ATPase proton pump inside the parietal cells of the gastric mucosa. This allows the drug to suppress the final stage of acid formation inside the gastric juice. Such an effect reduces its acidity and reduces the volume of acid contained in it. As a result, the negative effect of the juice on the gastric mucosa becomes much weaker.

The strength of suppression depends on the duration of the course of therapy, as well as the size of the dose. Even the use of a single dose of the drug (30 mg) reduces the secretion of gastric juice by 70-90%. The effect of the drug begins after 1-2 hours, and then continues throughout the day.

Pharmacokinetics

The component is absorbed inside the intestine. After a healthy person takes 30 mg of the drug, the peak plasma level reaches 0.75-1.15 mg/l after 1-2 hours. The level of bioavailability, as well as peak plasma indicators, do not change in accordance with the frequency of drug use; the change in values in this case depends on the individual characteristics of the person.

The synthesis of the active substance with plasma protein is 98%.

Lansoprazole is excreted in urine and bile (exclusively in the form of decay products, such as lansoprazole sulfone with hydroxylansoprazole). During the day, 21% of the drug is excreted (in urine). The half-life is 1.5 hours. This indicator increases in people suffering from severe liver dysfunction, as well as in elderly patients (over 69 years of age). In case of renal dysfunction, the absorption rates of the drug remain almost unchanged.

Dosing and administration

It is taken orally. The standard dosage of the drug is 30 mg once a day (before meals, 30-40 minutes). The capsules are washed down with water (150-200 ml) and are not chewed. If it is impossible to perform such manipulation, it is allowed to open the capsule and then dissolve the substance contained in it in apple juice (1 tablespoon of the drink is enough). A similar procedure is required for the introduction of the drug using a nasogastric tube.

The duration of therapy and dosage are prescribed by the doctor, taking into account the patient’s characteristics, the course of the pathology, and the clinical picture of the disease.

No more than 60 mg of the drug is allowed per day, and people with liver disorders - no more than 30 mg. For people with gastrinoma, the dose sizes may be increased.

If it is necessary to take 2 daily doses, it is necessary to divide the intake into 2 times - in the morning before breakfast and in the evening before dinner.

If you miss a dose of the medicine, you should try to take the capsule as soon as possible. However, if there is very little time left before the next dose, you must not use the previous missed capsule.

During treatment of duodenal ulcer: the active phase should be treated with a single dose of 30 mg of the drug over a period of 0.5-1 month. When eliminating ulcers caused by the use of NSAIDs, the dosage is similar, but the course of treatment itself lasts 1-2 months.

In the treatment of benign gastric ulcers: the active phase is treated with 30 mg of the drug (once a day) for 2 months. To get rid of ulcers caused by the use of NSAIDs, a similar dosage of the drug should be used for 1-2 months.

During the treatment of GERD: severe and moderate stages of the disease are treated during the 1st month (taking 30 mg of the drug once a day). If there is no result after 4 weeks of taking, the therapy period should be doubled. With long-term prevention of relapse of the pathology, you should also take 30 mg once a day. Information has been confirmed that maintenance treatment for 1 year is effective and safe for health.

Destruction of the pathogenic bacterium Helicobacter pylori: 2-time daily use of the drug in a dose of 30 mg (before breakfast and before dinner) is required. The drug should be taken in combination with selected antibiotics according to a pre-selected scheme (in a period of 1-2 weeks).

Treatment of gastrinoma: dosages are prescribed individually, taking into account the prevention of exceeding the basal secretion of acid (10 mmol/hour). Often the size of the initial dose is 60 mg per day (once before breakfast). In case of taking the drug in the amount of more than 120 mg, it is necessary to drink 1 part of the dose before breakfast, and the 2nd - before dinner. The course lasts until the symptoms of the disease completely disappear.

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Use Lancerola during pregnancy

Taking Lancerol capsules by pregnant women is prohibited.

If you need to take the medicine during the lactation period, you should stop breastfeeding for this period.

Contraindications

Among the main contraindications of the drug:

• severe intolerance to lansoprazole or other components contained in the capsules;
• combination of the drug with the substance atazanavir;
• the presence of malignant tumors in the digestive tract;
• the patient's childhood.

Side effects Lancerola

When treating with Lancerol, side effects such as nausea, abdominal pain and diarrhea (most often) usually occur. In some cases, headaches have also occurred. Other adverse reactions:

• cardiovascular system organs: shock, decrease/increase in blood pressure, myocardial infarction, development of angina pectoris, palpitations, cerebrovascular changes, and vasodilation;
• Digestive tract organs: development of vomiting, constipation, anorexia, cholelithiasis, cardiospasm, hepatotoxicity, and hepatitis with jaundice. In addition, thirst, dry mouth, mucous candidiasis inside the gastrointestinal tract, belching with dysphagia, and dyspeptic symptoms occur. Colitis, esophagitis, esophageal ulcer/stenosis, bloating, gastroenteritis, gastric polyps, and gastrointestinal bleeding may also occur. There is a change in the color of feces, worsening/increasing appetite, taste bud disorder, vomiting with blood, increased salivation, melena, glossitis with stomatitis, ulcerative colitis, pancreatitis, and tenesmus, as well as bleeding from the anus;
• endocrine system organs: development of hypo- or hyperglycemia, goiter, and diabetes mellitus;
• lymph and hematopoietic system: development of neutro-, leukopenia-, thrombocyto- or pancytopenia, hemolysis, anemia (also hemolytic or aplastic forms of the disease), eosinophilia with agranulocytosis, as well as thrombocytopenic/thrombotic purpura;
• connective tissues, as well as musculoskeletal organs: development of myalgia or arthralgia/arthritis, pain in the skeleton and muscles;
• organs of the nervous system: development of apathy, amnesia, depression, increased agitation, vertigo. In addition, the appearance of fainting or dizziness, hallucinations, feelings of fear, nervousness, hostility and drowsiness. The occurrence of tremor, hemiplegia, paresthesia, insomnia, confusion, as well as disorder of thought processes and decreased libido;
• respiratory system organs: the appearance of a runny nose, hiccups, cough, dyspnea, the development of pharyngitis, asthma, infectious processes in the lower and upper respiratory tract (pneumonia or bronchitis), bleeding in the lungs or from the nose;
• subcutaneous layer and skin: development of erythema multiforme, Quincke's edema, Lyell's or Stevens-Johnson syndromes, facial hyperemia, as well as itching with acne and erythema multiforme. Also, a rash with purpura occurs, alopecia begins, photosensitivity, urticaria, and in addition, increased sweating and petechiae;
• sense organs: the appearance of pain in the eyes, deterioration of visual clarity, as well as defects of the visual fields. In addition, tinnitus, development of otitis media or deafness. Speech disorders may develop and taste perception may change;
• urogenital system organs: development of tubulointerstitial nephritis, which can develop into renal failure, urinary retention, formation of stones inside the kidneys, appearance of hematuria, glucosuria or albuminuria. Possible development of impotence, enlargement (gynecomastia) or tenderness of the mammary glands, menstrual irregularities;
• combined use of lansoprazole with amoxicillin, as well as clarithromycin: most often, with triple treatment using the above-mentioned drugs, headaches, diarrhea, and taste disorders develop over a period of 2 weeks. In the case of using lansoprazole only with amoxicillin, often only headaches and diarrhea appear. These reactions are short-term and go away on their own, without discontinuing therapy;
• changes in test results: increased levels of alkaline phosphatase and ALT with AST, as well as globulins with creatinine and γ-GTP, as well as an imbalance of albumins with globulins. In addition, a decrease/increase in leukocyte values, eosinophilia and bilirubinemia with hyperlipidemia develop, the number of erythrocytes changes, platelet values, electrolytes or cholesterol increase/decrease, gastrin, urea and potassium levels increase, as well as lipoproteins (with low density) and glucocorticoids. The hemoglobin level also decreases, and the occult blood test gives a positive result. In the urine, the appearance of salts is observed, as well as hematuria, albuminuria or glucosuria. There is information about an increase in liver enzyme values at the final stage of therapy (more than three times exceeding the maximum permissible normal limit), but jaundice did not develop;
• Others: occurrence of anaphylaxis, asthenia, anaphylactoid manifestations, candidiasis, swelling, chest pain, bad breath. In addition, increased fatigue, fever, development of infections, feelings of weakness and flu-like syndrome are noted.

Interactions with other drugs

Lansoprazole, like other proton pump inhibitors, reduces the levels of atazanavir (which is an HIV protease inhibitor), the absorption of which is associated with gastric acidity. As a result, Lancerol may affect the effectiveness of atazanavir and also contribute to the development of resistance to HIV. For this reason, combining these drugs is prohibited.

The drug is capable of increasing plasma levels of drugs whose metabolism is carried out with the help of the CYP3A4 element (such as ibuprofen and prednisolone with warfarin, as well as antipyrine with phenytoin and indomethacin, propranolol with clarithromycin and terfenadine with diazepam).

Drugs that inhibit 2C19 (eg, fluvoxamine) can greatly increase (approximately fourfold) the plasma level of lansoprazole, so when combined with them, the dose of the latter must be adjusted.

Inducers of elements 2C19, as well as CYP3A4 (among them St. John's wort with rifampicin) are capable of significantly reducing plasma values of lansoprazole, therefore, when combined with them, the dose of Lancerol must be adjusted.

Lansoprazole is capable of suppressing the secretory function of the stomach for a long time, which is why, in theory, it can affect the level of bioavailability of drugs for the absorption of which acidity indicators are important (among them digoxin with ketoconazole, iron salts with itraconazole, as well as ampicillin esters).

Antacids and sucralfate can reduce the bioavailability of the drug, which is why it must be taken at least 1 hour after using the above-mentioned drugs.

Combination of the drug with theophylline (CYP1A2 and CYP3A elements) causes a moderate increase (no more than 10%) in the clearance rate of this substance, but the likelihood that such interaction will have medicinal significance is very low. It should be noted that some people need to adjust the dosage of theophylline at the initial stage of combination therapy and after completion of Lancerol use in order to maintain medicinally effective values of theophylline.

Lansoprazole does not affect the prothrombin time or the pharmacokinetic properties of warfarin.

An increase in the PT and INR values can cause bleeding and, in the future, even provoke a fatal outcome.

Combined administration with digoxin promotes an increase in plasma levels of this substance.

Combined use with tacrolimus increases its plasma levels (especially in individuals who have undergone organ transplants).

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Storage conditions

The medicine must be kept in a place inaccessible to small children, in conditions suitable for medicines. The temperature value is a maximum of 25°C.

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Shelf life

Lancerol is permitted for use for a period of 2 years from the date of manufacture of the drug.