Dexilant capsules 30 mg 28 pcs
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Active ingredients
Dexlansoprazole
Release form
Capsules
Composition
Active ingredient: Dexlansoprazole (Dexlansoprazole) Active ingredient concentration (mg): 30
Pharmacological effect
Proton pump inhibitor. It inhibits the secretion of gastric juice by inhibiting H + / K + -ATP-ase in the parietal cells of the stomach. Blocks the final stage of the secretion of hydrochloric acid. The capsule of the drug Dexilant disintegrates in the stomach and contains two types of enteric-coated granules that release the active substance depending on the pH in different areas of the small intestine. This combination helps to prolong the action of dexlansoprazole and helps to reduce the secretion of gastric juice for a long time.
Pharmacokinetics
Absorption Dekslansoprazol well absorbed when taken orally. Its bioavailability is 76% or more. The bicomponent composition of the drug Dexilant causes absorption in the form of two pH-dependent phases. The first peak concentration of the active substance occurs in the range from 1 to 2 hours after ingestion (1 phase release of the active substance) and 4 to 5 hours (2 phase release of the active substance), respectively. After 5 days of administration of dexlansoprazole in the dosage of 30 mg and 60 mg Cmax in the blood plasma is 658 ng / ml and 1397 ng / ml, respectively. AUC is 3275 ng × h / ml and 6529 ng × h / ml after 5 days of administration of dexlansoprazole at dosages of 30 mg and 60 mg, respectively. as a result of oxidation, reduction and subsequent formation of sulfate, glucoronid and glutathione compounds. The oxidation is carried out with the help of the cytochrome P450 enzyme system, which participates both in the hydroxylation process (mainly CYP2C19 isoenzyme) and in the oxidation process (CYP3A4 isoenzyme). CYP2C19 isoenzyme is a polymorphic hepatic isoenzyme that exists in 3 fractions that exhibit different properties in the metabolism of substrates: fast, moderate and slow metabolisers. Dexansoprazole is the main component in the blood plasma, regardless of the type of metabolizer according to the CYP2C19 isoenzyme.In the case of medium and strong metabolisers of the CYP2C19 isoenzyme, the main metabolite in the blood plasma is 5-hydroxydexanesoprazole and its glucuronic compound. With weak metabolisers on the isoenzyme CYP2C19 - dexlansoprazole sulfone. Output T1 / 2 is 1-2 hours. Clearance after 5 days of dexansoprazole is 11.4 and 11.6 l / h for dosages of 30 mg and 60 mg, respectively. The drug is excreted by the kidneys (about 51%) and 48% is excreted through the intestines. Since the drug is extensively metabolized in the liver, with the use of dexlansoprazole in patients with impaired renal function, no dose reduction is required. As in patients with normal renal function, a change in pharmacokinetics is not expected.
Indications
Treatment of erosive esophagitis of any severity; - supportive therapy after treatment of erosive esophagitis and relief of heartburn; - symptomatic treatment of gastroesophageal reflux disease GERD (ie, NERD - non-erosive reflux disease).
Contraindications
Hypersensitivity to any component of the drug; - combined use with HIV protease inhibitors (atazanavir, nelfinavir); - age up to 18 years; - pregnancy; - lactation period. The preparation contains sucrose, therefore its use is not recommended for patients with hereditary fructose intolerance, glucose -alactose malabsorption or succinic-isomaltase deficiency.
Precautionary measures
Do not exceed recommended doses.
Use during pregnancy and lactation
The use of the drug Dexilant during pregnancy is contraindicated. If necessary, the use of the drug during lactation should stop breastfeeding.
Dosage and administration
Inside: the capsule is taken entirely regardless of the meal. You can also open the capsule, pour the granules from it into a tablespoon and mix them with applesauce; then immediately, without chewing, swallow. The treatment of erosive esophagitis of any severity: the recommended dose is 60 mg 1 time / day. The course of treatment is 8 weeks. Supportive therapy after treatment of erosive esophagitis and relief of heartburn manifestations: the recommended dose is 30 mg 1 time / day. In the conducted studies, the course of treatment was up to 6 months. In case of moderate and severe erosive esophagitis, the recommended dose is 60 mg 1 time / day. In the conducted studies, the treatment course was up to 6 months. Symptomatic treatment of gastroesophageal reflux disease of GERD (i.e.NERD - non-erosive reflux disease): the recommended dose is 30 mg 1 time / day. The course of treatment is 4 weeks. In patients with impaired liver function of moderate severity (Child-Pugh class B), the daily dose should not exceed 30 mg of dexlansoprazole. Clinical data on the administration of the drug in patients with severe disorders (Child-Pugh class C ) are absent. Dose correction in elderly patients, patients with impaired renal function and with impaired liver function of mild severity (Child-Pugh class A) is not required.
Side effects
Most often (at least 2%): diarrhea, flatulence, abdominal pain, nausea, vomiting, upper respiratory tract infections. Determining the frequency of adverse reactions: very often (≥1 / 10), often (≥1 / 100 and <1 / 10), infrequently (≥1 / 1000 and <1/100), rarely (≥1 / 10 000 and <1/1000), very rarely (<1/10 000, including individual cases), the frequency is unknown (it is impossible to estimate based on the available data). From the side of the immune system: frequency is unknown - hypersensitivity (including anaphylactic reactions), malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal n Ecrolysis, exfoliative dermatitis, anaphylactic shock. Metabolism: frequency unknown - hypomagnesemia, hyponatremia. On the digestive system: often diarrhea, discomfort and abdominal pain, constipation, flatulence, nausea, vomiting; infrequently - dry mouth; rarely - oral candidiasis; frequency unknown - swelling of the oral mucosa, pancreatitis. From the urinary system: frequency unknown - acute renal failure. From the liver and biliary tract: infrequently - change in the indicators of the functional activity of the liver; frequency is unknown - drug hepatitis. On the side of the skin and subcutaneous tissues: infrequently - rash, urticaria, itching; frequency is unknown - leukocytoclastic vasculitis, generalized rash. On the respiratory system: often - infectious diseases of the upper respiratory tract; infrequently - cough; frequency unknown - laryngeal edema, feeling of tightness in the throat. From the side of the blood and lymphatic system: unknown frequency - autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura. From the musculoskeletal system: unknown frequency - fractures. From the cardiovascular system: infrequently - hot flashes (hot flashes), increased blood pressure. From the nervous system: often - headache; infrequently - dizziness, dysgeusia; rarely - paresthesia, convulsions; frequency unknown - stroketransient ischemic attack. For the organ of vision: rarely - visual impairment; frequency is unknown - visual impairment (misting). On the part of the organ of hearing and labyrinth disorders: rarely - vertigo; frequency is unknown - decrease in hearing. Psychiatric disorders: infrequently - insomnia, depression; rarely, auditory hallucinations. General disorders: infrequently, weakness, changes in appetite; frequency unknown - swelling of the face.
Overdose
There were no reports of significant cases of overdose as a result of using the drug Dexilant. Symptoms: repeated administration of a dose of 120 mg and a single dose of 300 mg did not cause serious side effects. When taking the drug Dexilant 60 mg 2 times / day there was an increase in blood pressure of more than 140/90 mm Hg. Treatment: in the case of overdose and only in the presence of clinical manifestations symptomatic therapy is carried out. Dexansoprazole is not excreted by hemodialysis.
Interaction with other drugs
Dexansoprazole can be administered without the risk of drug interaction to patients taking clopidogrel. In the case of co-administration, correction of the dose of clopidogrel is not required. There is also a lack of clinically significant drug interaction with phenytoin, theophylline and diazepam. Simultaneous use of dexansoprazole may affect the absorption of drugs whose bioavailability depends on the pH of the gastric environment (for example, ampicillin esters, digoxin, salts iron, ketoconazole, erlotinib). Simultaneous administration with tacrolimus can lead to an increase in plasma tacrolimus concentration, especially in patients after trans splantation, which are moderate or slow metabolisers of the CYP2C19 isoenzyme. When taken simultaneously with fluvoxamine, there is a possibility of an increase in systemic exposure to dexlansoprazole. Simultaneous administration of dexlansoprazole and methotrexate can lead to an increase and maintenance of a high serum concentration of methotrexate and / or its metabolite in the serum, which leads to an increase in the serum levels of methotrexate and / or its metabolite. may lead to the development of toxicity of methotrexate. If you need to receive high doses of methotrexate, it is recommended to temporarily discontinue dexlansoprazole.
special instructions
Before the treatment of dexlansoprazole, the possibility of a malignant neoplasm should be excluded, since the drug can mask the symptoms and delay the correct diagnosis. If the symptoms persist despite adequate treatment, further examination should be carried out. When taking proton pump inhibitors, which include dexlansoprazole, the risk of gastrointestinal intestinal infections, accompanied by diarrhea, the causative agents of which are bacteria of the genus Clostridium difficile, especially in hospitalized patients This should be taken into account if the patient's condition does not improve during the treatment of diarrhea. Patients in this case are advised to take the minimum effective dose of dexlansoprazole with the shortest duration of treatment. Patients receiving high doses of the drug or with long-term therapy with proton pump inhibitors (IPN) in over the course of a year or more, the risk of osteoporotic fractures of the hips, hands, and spine increases. Patients with the risk of osteoporotic fractures should adhere to the recommended doses. In rare cases, patients experienced symptomatic and asymptomatic hypomagnesemia when taking drugs IIT for at least 3 months, and in most cases - when taking for a year. Symptoms of hypomagnesemia are tetany, arrhythmia, and seizures. Treatment is the replenishment of magnesium and the discontinuation of taking drugs IDU. In patients who need long-term treatment or simultaneously taking drugs with digoxin or other drugs that can cause hypomagnesemia (for example, diuretics), it is necessary to control the concentration of magnesium in serum before and during treatment. Impact on ability to drive and control mechanisms - due to the likelihood of dizziness and visual impairment, patients during the treatment period should refrain from driving and other mechanisms that require high attention.