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Lansoprol
Lansoprol is an inhibitor of the "proton pump".
Release form
Available in capsules of 7 pieces per blister (in the pack contains 2 or 4 blister plates). Also on the 1st blister there can be 14 capsules (in this case there will be 1 or 2 blister plates in the bundle). Sometimes the blister consists of 4 capsules (one package will contain 1 blister plate).
Pharmacodynamics
Lansoprazole oppresses the active action of the proton pump's H + K + ATPase within the parietal cells of the gastric mucosa. This allows the drug to suppress the process of producing gastric acid occurring at the final stage and reduces its acidity and the amount inside the gastric juice. Due to such actions, the negative effect of gastric juice on the mucous membrane decreases significantly.
The strength of inhibition of activity depends on the duration of the treatment process, as well as the dose size of the drug. Even with a single intake of 30 mg of the drug, suppression of gastric juice secretion is approximately 70-90%. Lansoprazole begins to act about 1-2 hours after taking. The effect of a dose of drugs lasts for 1 day.
Pharmacokinetics
Absorption of the substance takes place inside the intestine. Peak plasma index in volunteers who took 30 mg LS was 0.75-1.15 mg / l, and it took 1.5-2 hours to achieve it. Plasma values and the level of bioavailability are dependent on the individual characteristics of a person, so they do not change in proportion to the frequency of drug use.
With protein, the drug is synthesized at 98%.
Excretion of lansoprazole occurs with bile, as well as urine (exclusively in the form of decay products - lansoprazolesulfone with hydroxylansoprazole). About 21% of the drug is excreted per day with urine.
Half-life lasts 1.5 hours. This period becomes longer in people with severe disorders in the liver, as well as in elderly patients (over 69 years of age). In disorders of renal function, the absorption of the active substance is almost unchanged.
Side effects of the lansoprol
During the period of therapy, there is often information about the development of diarrhea (most often), as well as nausea and abdominal pain. Headaches are often observed. Among other side effects:
- CAS organs: development of vasodilation, angina pectoris, myocardial infarction, shock state, and also heart rate and cerebrovascular changes, as well as increase / decrease in blood pressure;
- organs of the digestive tract: the occurrence of vomiting or constipation, the development of anorexia, cholelithiasis, cardiospasm, hepatitis with hepatotoxicity, and jaundice. In addition, thirst and dryness of oral mucous membranes, candidiasis inside the digestive tract (on mucous membranes), eructation, swallowing disorder, esophageal form of stenosis, bloating may develop. Possible dyspeptic phenomena, gastric polyps, esophagitis, colitis with gastroenteritis and a change in the color of feces. In addition, vomiting with blood, bleeding in the gastrointestinal tract, or in the anus, worsening or increased appetite, increased salivation, stomatitis, melena, pancreatitis with glossitis, ulcerative colitis, a disorder of taste sensations and tenesmus may appear;
- metabolic processes: development of hypomagnesemia;
- organs of the endocrine system: the appearance of goiter, the development of diabetes, as well as hyper- or hypoglycemia;
- lymph and hematopoietic system: the development of anemia (also its hemolytic or aplastic form), agranulocytosis, neutro-, thrombocyto-, leuko- and pancytopenia, and in addition eosinophilia, hemolysis and thrombotic, as well as thrombocytopenic forms of purpura;
- structure of the skeleton and musculature: muscle or joint pain, arthritis, musculoskeletal pain;
- organs of the National Assembly: the emergence of amnesia, dizziness, hallucinations, as well as feelings of fear, depression, apathy, nervousness and hostility. In addition, drowsiness or insomnia develops, increased excitability, vertigo, paresthesia with tremor, hemiparesis, as well as confusion. There are fainting and thinking disorders, libido decreases;
- organs of the respiratory system: the appearance of cough, dyspnoea, hiccoughs, development of the common cold, asthma and pharyngitis. There are also infectious processes in the lower and upper parts of the respiratory system (inflammation of the lungs and bronchitis), bleeding from the nose and into the lungs;
- subcutaneous tissue with skin: Lyell's and Stevens-Johnson's syndromes, Quincke's edema, acne, erythema polyforma, hair loss, itching and urticaria, facial hyperemia, photophobia, petechiae, purpura, and increased sweating;
- sensory organs: pain in the eyes, speech problems, development of deafness or otitis media, visual fuzziness, defects in the fields of vision, disorders of taste buds, tinnitus;
- organs of the urogenital system: tubulointerstitial nephritis (can develop into kidney failure), kidney stones, urinary problems, albuminuria or hematuria with glucosuria, impotence, menstrual disorder, chest pains, mammary gland enlargement or gynecomastia;
- with triple treatment using clarithromycin, lansoprazole and amoxyllicin: most often in the period of 2 weeks there is diarrhea, changes in taste, as well as headaches; with double treatment with the combination of lansoprazole and amoxicillin: the development of headaches, as well as diarrhea. Such manifestations are brief and pass without stopping the treatment course;
- data analysis: an increase in the parameters of alkaline phosphatase, ALT with AST, and in addition globulins, creatinine and γ-GTP, as well as an imbalance of the proportions of albumins with globulins. At the same time, there is a decrease / increase in the white blood cell count, eosinophilia with bilirubinemia and hyperlipidemia, and a change in the number of red blood cells. In addition, the number of electrolytes decreases / increases, cholesterol decreases / increases, urea or potassium values increase, hemoglobin decreases, glucocorticoids or low density lipoproteins increase. It is possible to increase the values of gastrin, decrease / increase in the level of platelets, as well as a positive test result for hidden blood. Inside the urine - the development of hematuria, albuminuria or glucosuria, and in addition the occurrence of salts. There is information about an increase in the values of hepatic enzymes (above the maximum limit of the norm 3 times) at the end of the treatment course, but without the development of jaundice;
- Other: anaphylaxis, anaphylactoid manifestations, development of candidiasis, asthenia, fever. In addition, also increased fatigue, swelling, pain in the sternum, a bad smell from the mouth, the development of influenza-like syndrome, infectious processes, and a sense of weakness.
Dosing and administration
The use is by oral route. Basically, the dosage is 30 mg once a day (before meals, for 30-40 minutes). Capsule should be consumed by washing with water (150-200 ml), without chewing. If it is impossible to take the medicine in this way, you can open the capsule, and then dissolve the powder in it in the apple juice (enough 1 full spoonful), then immediately swallow, without chewing the mixture. A similar procedure is carried out when the drug is administered by a nasogastric tube.
Regarding the duration of the therapeutic course, as well as the size of the doses - they are determined by the attending doctor, taking into account the nature of the course of the pathology, as well as the clinical picture.
During the day, you can take no more than 60 mg LS, and for people with disorders in the liver - no more than 30 mg. Dosages can be increased in people with ulcerogenic pancreatic adenoma.
If you need to take 2-day doses, you need to drink one of them in the morning, before breakfast, and the second - in the evening, before dinner.
In case of non-use of medicines in the prescribed period, it is required to drink the capsule as soon as possible after this period. But if there is not enough time to consume the next capsule, it is not necessary to take the missed dosage.
With an ulcer of the duodenum: the active phases of the pathology are treated with 30 mg once a day for the 0.5-1 month. When eliminating ulcers, provoked by the use of NSAIDs, the dosage is the same as indicated above, and the treatment period is 1-2 months.
In the prevention of ulcers that have appeared due to prolonged use of NSAIDs, people at risk (over 65 years of age or having an ulcer of duodenum gut or gastritis) - daily dose is 15 mg. If there is no effect, increase it to 30 mg.
Benign form of the gastric ulcer: when eliminating the active phase, it is necessary to drink 30 mg of LS per day only for 2 months. During the therapy of ulcers that have arisen because of the use of NSAIDs, the drug in the same dose is applied in the period of 1-2 months.
When treating GERD: it is recommended to drink 15-30 mg per day. With such treatment, the condition improves rapidly. Individual dosage is also considered. If there is no improvement after the first month of using drugs in a daily dose of 30 mg, additional testing is required.
In the case of treatment of severe or moderate esophagitis, it is required to take 30 mg of medication per day once during the first month. If the pathology is not eliminated for the specified period of time, the course can be extended for another 1 month.
With prolonged prevention of relapse of the erosive form of esophagitis, a single daily dose is 15-30 mg. The efficacy and safety of maintenance treatment at such doses in the 12-month period is confirmed.
Destruction of the microbe Helicobacter pylori: taking in the morning and evening (both times before meals) 30 mg of the drug. Use capsules is required in the period of 1-2 weeks in combination with antibiotics in accordance with a selected treatment regimen.
Ulcerogenic pancreatic adenoma: the dosage size is determined individually, taking into account that the basal acid extraction index is not higher than 10 mmol / h. At the beginning of treatment it is recommended to drink once a day for 60 mg before the morning meal. In case of daily intake of more than 120 mg, half the dosage should be consumed before breakfast, and the second part before the evening meal. The course lasts until the symptoms of the disease disappear.
Interactions with other drugs
Lansoprol, like other proton pump inhibitors, lowers the level of atazanavir (a substance that slows the HIV protease), the absorption of which is dependent on the level of gastric acidity, which can affect the therapeutic properties of atazanavir and, at the same time, cause resistance to infection HIV. Because of this, it is forbidden to combine the above preparations.
Lansoprazole is able to increase the plasma level of drugs that are metabolized by CYPCA4 (drugs such as warfarin with indomethacin, antipyrine, phenytoin, diazepam with ibuprofen, clarithromycin, propranolol, terfenadine, or prednisolone).
Drugs that inhibit the function of 2S19 (such as fluvoxamine), significantly increase the plasma level of lansoprol (4 times). Therefore, if they are combined, you need to adjust the dose of the latter.
Inductors of elements 2S19, as well as CYPZA4 (such as the herb of St. John's wort or rifampicin) are capable of greatly reducing the amount of lansoprazole inside the plasma. The combination of these drugs requires correction of the dosage of the latter.
Lansoprazole for a long time suppresses the process of gastric secretion, because of what theoretically can affect the bioavailability of those drugs for which absorption is important pH level (such as digoxin, ketoconazole and ampicillin esters with itraconazole and iron salts).
Combined use with digoxin can increase its plasma value. Because of this, when combining these drugs will need constant monitoring of digoxin and subsequent correction of its dose (if necessary, as well as after the application of lansoprazole).
Combination with antacids or sucralfate may reduce the bioavailability of lansoprazole, so the latter should be consumed at least 1 hour after using these drugs.
Combined therapy with theophylline (elements CYP1A2 and CYRZA) moderately increases the clearance of the latter (up to 10%), but drug-significant interaction between drugs is unlikely. Although to maintain the level of theophylline in drug-effective values, it may sometimes be necessary to adjust the dosage at the initial stage or upon completion of the use of lansoprazole.
Lansoprazole has no effect on the pharmacokinetic properties of warfarin, as well as its prothrombin time.
The increase in INR, as well as PTV, can cause bleeding and, in the worst cases, death.
Due to the combination of lansoprazole with tacrolimus, an increase in the plasma level of the latter is possible. In particular, this applies to people who underwent organ transplantation. Therefore, it is necessary to monitor the plasma values of tacrolimus at the initial stage of treatment, and then after the application of lansoprazole.