Dexilant capsules 30mg #14Dexilant Pharmachologic Effect:
Mode of action - inhibiting the proton pump, antiulcer.
Dekslansoprazol is a proton pump inhibitor, suppresses gastric acid secretion by inhibiting H + / K + -ATPase in the parietal cells of the stomach. Blocks the final stage of hydrochloric acid secretion.
Dexilant® capsule formulation contains two types of granules, enteric-coated, which release capsules after the dissolution of the active substance in the stomach as a function of pH in different areas of the small intestine. This helps to prolong the effect of a combination dekslansoprazola and reduces gastric acid secretion for an extended time.
Dekslansoprazol well absorbed when taken orally. Its bioavailability is 76% or more. Two part Dexilant® drug absorption causes a pH-dependent two phases. The first peak of the active substance concentration occurs in the range of 1 to 2 hours after oral administration (1st phase release of active ingredient) and the second - in the range of 4 to 5 hours (2nd phase the release of active substance), respectively. After 5 days of dekslansoprazol in doses of 30 and 60 mg in a plasma Cmax of 658 and 1397 ng / ml, respectively.
AUC is 3275 ng-hr / mL and 6529 ng · h / mL after 5 days of dekslansoprazol in doses of 30 and 60 mg, respectively.
Dekslansoprazola Binding to plasma proteins is 96,1-98,8%.
Dekslansoprazol extensively metabolized in the liver to inactive metabolites as a result of oxidation, reduction and the subsequent formation of sulfate, glucuronide and glutathione compounds.
The oxidation is carried out by the enzyme cytochrome P450, which participates in the process of hydroxylation (preferably isoenzyme CYP2C19), and in the oxidation process (isoenzyme CYP3A4). CYP2C19 isozyme hepatic isoenzyme is polymorphic, existing in three fractions exhibiting different properties in the metabolism of substrates (fast, moderate and slow metabolizers). In the case of medium and strong metabolizers by isoenzyme CYP2C19, a major metabolite in plasma is 5 and glucuronic gidroksidekslansoprazol compound. In poor metabolizers by isoenzyme CYP2C19 - dekslansoprazola sulfone.
T1 / 2 of the drug - 1-2 hours.
Clearance after 5 days of dekslansoprazola is 11.4 and 11.6 l / h for dosing of 30 and 60 mg, respectively.
The drug is eliminated via the kidneys (approximately 51%) and 48% is excreted through the intestines.
Since the drug is extensively metabolized in the liver, when applying dekslansoprazola in patients with impaired renal function dose reduction is required. As in patients with normal renal function is not expected to alter the pharmacokinetics.
Indications Dexilant® drug:
- treatment of erosive esophagitis any severity;
- maintenance therapy after treatment of erosive esophagitis and heartburn relief manifestations;
- symptomatic treatment of gastroesophageal reflux disease (GERD, including NERD - non-erosive reflux disease).
- hypersensitivity to any component of the drug;
- concomitant use with HIV protease inhibitors (atazanavir, nelfinavir);
- patients with hereditary fructose intolerance, glucose-galactose malabsorption or saharazno-izomaltaznoy insufficiency (the drug contains sucrose);
- age 18 years.
concomitant use of tacrolimus; isoenzyme inhibitors CYP2C19 (such as fluvoxamine); warfarin (under the control of PT and INR); methotrexate.
Pregnancy and breast-feeding:
Application Dexilant® drug during pregnancy is contraindicated. If necessary, use during lactation should stop breastfeeding.
Dexilant Side Effects:
The most common (more than 2%) undesirable adverse reactions are diarrhea, flatulence, abdominal pain, nausea, vomiting, upper respiratory tract infection.
Below are details about the unwanted side reactions, depending on their frequency of occurrence: very common - ≥ 1/10; often - ≥1 / 100 and <1/10; infrequently - ≥1 / 1000 and <1/100; rarely - ≥1 / 10,000 to <1/1000; very rarely - <1/10000, including isolated cases; Frequency not known (can not be estimated from the available data).
- On the part of the immune system: the frequency is unknown - hypersensitivity (including anaphylaxis), malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis, exfoliative dermatitis, anaphylactic shock.
- On the part of metabolism and nutrition: the frequency is unknown - hypomagnesemia, hyponatremia.
- On the part of the digestive tract: often - diarrhea, discomfort and abdominal pain, constipation, flatulence, nausea, vomiting; Infrequent - dry mouth; rarely - oral candidiasis; the frequency is unknown - swelling of the mouth, pancreatitis.
- On the part of the kidney and urinary tract: the frequency is unknown - acute renal failure.
- On the part of the liver and biliary tract: rarely - to change the parameters of the functional activity of the liver; the frequency is unknown - drug-induced hepatitis.
- Skin and subcutaneous tissue disorders: rare - rash, hives, itching; the frequency is unknown - leukocytoclastic vasculitis, generalized rash.
- The respiratory system, organs, thoracic and mediastinal disorders: often - infections of the upper respiratory tract; infrequently - cough; the frequency is unknown - swelling of the throat, tightness in the throat.
- From the blood and lymphatic system: the frequency is unknown - autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura.
- On the part of the musculoskeletal and connective tissue disorders: Frequency not known - fractures.
- On the part of the vessels: seldom - an attack of heat (flushing), increased blood pressure.
- From the nervous system: often - headache; Infrequent - dizziness, dysgeusia; rarely - paresthesia, convulsions; the frequency is unknown - stroke, transient ischemic attack.
- On the part of the organ of vision: rarely - visual impairment; the frequency is unknown - misting.
- On the part of the organ of hearing and labyrinth disorders: rare - vertigo; the frequency is unknown - hearing loss.
- Mental disorders: rarely - insomnia, depression; rarely - auditory hallucinations.
- General disorders: rarely - weakness, changes in appetite; the frequency is unknown - swelling of the face.
Dekslansoprazol can be assigned without the risk of drug interactions in patients receiving clopidogrel. In the case of co-administration of clopidogrel dose adjustments required. It is also noted the absence of clinically significant drug interactions with phenytoin, theophylline and diazepam.
Simultaneous application dekslansoprazola can affect the absorption of drugs, bioavailability depends on the pH of the gastric environment (e.g. ampicillin complex esters, digoxin, iron salts, ketoconazole, erlotinib).
Simultaneous treatment with tacrolimus may increase tacrolimus concentrations in blood plasma, particularly after transplantation in patients who are slow metabolizers moderate or isoenzyme by CYP2C19.
When concomitantly with fluvoxamine is likely to increase systemic exposure dekslansoprazol.
Simultaneous reception dekslansoprazola and methotrexate can lead to higher and higher concentrations of methotrexate conservation and / or its metabolite in the blood serum. If you want to receive high-dose methotrexate is recommended to cancel the temporary reception dekslansoprazola.
Dosing and Administration:
Inside, a capsule taken as a whole, regardless of the meal.
You can also open the capsule, pour out of it in a tablespoon of granules and mix them with applesauce; then immediately, without chewing, swallowing.
Treatment of erosive esophagitis of any severity. The recommended dose is 60 mg 1 time per day. The course of treatment - 8 weeks.
Maintenance therapy after treatment of erosive esophagitis and heartburn relief manifestations. The recommended dose is 30 mg 1 time per day. In the study treatment was up to 6 months.
Patients with erosive esophagitis moderate and severe recommended dose is 60 mg 1 time per day. In the study treatment was up to 6 months.
Symptomatic treatment of gastroesophageal reflux disease (GERD, including NERD - non-erosive reflux disease). The recommended dose is 30 mg 1 time per day. The course of treatment - 4 weeks.
In patients with impaired function of the liver moderate (Class B for Child-Pugh) daily dose should not exceed 30 mg dekslansoprazola. Clinical data on the admission of the drug in patients with severe impairment of patients (class C Child-Pugh) are absent.
Correction of the dose in elderly patients, patients with impaired renal function and in violation of mild liver function (class A on Child-Pugh) is not required.
Posts on significant cases of overdose Dexilant® was no preparation. Multiple receiving doses of 120 mg and a single dose of 300 mg did not cause severe side effects. There has been a side effect of raising blood pressure above 140/90 mm Hg Dexilant® when taking the drug, 60 mg 2 times a day.
However, in case of overdose only when clinical manifestations symptomatic therapy.
Dekslansoprazol not output through hemodialysis.
Before treatment dekslansoprazolom to exclude the possibility of malignant neoplasms of the gastrointestinal tract, since the drug may mask the symptoms and delay the correct diagnosis.
If symptoms persist despite adequate treatment, it should be further examination.
When receiving proton pump inhibitors, which include dekslansoprazol, increased risk of gastrointestinal infections, diarrheal pathogens that are bacteria of the genus Clostridium difficile, especially in hospitalized patients. It must be taken into account if the patient's condition does not improve the treatment of diarrhea. Patients in this case it is recommended to take the lowest effective dose dekslansoprazola at least the duration of treatment.
In patients receiving high doses or prolonged therapy, proton pump inhibitors (PPIs) for a year or more increases the risk of osteoporotic hip fractures, wrist and spine. Patients at risk for osteoporotic fractures should adhere to the recommended dosage (see. "Dosage and administration").
In rare cases, patients had symptomatic and asymptomatic hypomagnesemia while taking PPI drugs for at least 3 months, and in most cases - for admission to the course of the year. Symptoms are hypomagnesemia tetany, arrhythmias and seizures. Treatment - magnesium replenishment and cancel receiving PPI medication. In patients who need long-term treatment or concurrently taking drugs PPIs with digoxin or other drugs that can cause hypomagnesemia (eg diuretics) should be monitored in serum magnesium concentration before and during treatment.
Effects on ability to drive vehicles / machinery. Because of the likelihood of dizziness and blurred vision should refrain from driving and other mechanisms that require attention.
The modified-release capsules, 30 mg and 60 mg. At 14 or 28 capsules. Modified release HDPE vial, sealed with aluminum foil and sealed with a polypropylene screw cap. In the bottle is placed a container with a desiccant containing silica gel. On 1 vial. placed in a cardboard box.