Dexilant® [Dexlansoprazole]

Brand Takeda GmbH

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Available since: 2019-09-19

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Clinical Pharmacology

Dexilant - proton pump inhibitor, anti-ulcer.

Pharmacodynamics

Dexansoprazole is a proton pump inhibitor that inhibits the secretion of gastric juice by inhibiting H⁺/ K⁺-ATPase in the parietal cells of the stomach. Blocks the final stage of the secretion of hydrochloric acid.

Dexilant Capsule^® contains two types of enteric-coated granules, which after the disintegration of capsules in the stomach 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

Suction

Dexlansoprazole is well absorbed when taken orally. Its bioavailability is 76% or more. Two-component 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 (1st phase release of the active substance) and the second in the range from 4 to 5 hours (2nd phase release of the active substance), respectively. After 5 days of taking dexlansoprazole in dosages of 30 and 60 mg C_max in blood plasma is 658 and 1397 ng / ml, respectively.

AUC is equal to 3275 ng · h / ml and 6529 ng · h / ml after 5 days of administration of dexlansoprazole in dosages of 30 and 60 mg, respectively.

Distribution

The binding of dexlansoprazole to plasma proteins is 96.1–98.8%.

Metabolism

Dexansoprazole is extensively metabolized in the liver to inactive metabolites as a result of oxidation, reduction, and subsequent formation of sulfate, glucuronide, 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). 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. In weak metabolizers of the isoenzyme CYP2C19 - dexlansoprazole sulfone.

Removal

T_1/2 drug - 1-2 hours

Clearance after 5 days of dexansoprazole is 11.4 and 11.6 l / h for dosages of 30 and 60 mg, respectively.

The drug is excreted through the kidneys (about 51%) and 48% is excreted through the intestines.

Since the drug is extensively metabolized in the liver, dose reduction is not required when using dexlansoprazole in patients with impaired renal function. As in patients with normal renal function, a change in pharmacokinetics is not expected.

Indications

treatment of erosive esophagitis of any severity;
maintenance therapy after treatment of erosive esophagitis and relief of heartburn;
symptomatic treatment of gastroesophageal reflux disease (GERD, including NERD - non-erosive reflux disease).

Composition

Active ingredient: dexlansoprazole 30 mg

Auxiliary substances: sugar grits from 500 to 710 microns; magnesium carbonate; sucrose; low-level hyprolosis; hyprolosis; hypromellose 2910; talc; titanium dioxide; dispersion of methacrylic acid copolymer (methacrylic acid, ethyl acrylate, sodium lauryl sulfate, polysorbate 80); macrogol 8000; polysorbate 80; colloidal silicon dioxide; methacrylic acid and methyl methacrylate copolymer (1: 2); methacrylic acid and methyl methacrylate copolymer (1: 1); triethyl citrate;

Shell: carrageenan; potassium chloride; titanium dioxide; dye FD & C blue No. 2 aluminum varnish; iron dye black oxide; hypromellose; peeled gray ink for labeling (iron dye red oxide, iron dye yellow oxide, dye FD & C blue No. 2 aluminum varnish, carnauba wax, shellac, glyceryl monooleate).

Dexlansoprazole is marketed under different brands and generic names, and comes in different dosage forms:

Brand name	Manufacturer	Country	Dosage form
Dexilant	Takeda GmbH	Japan	capsules
Dexdor	Orion Corporation	Finland	solution

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Dosage and Administration

Orally, 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 swallow immediately, without chewing.

Treatment of erosive esophagitis of any severity. The recommended dose is 60 mg 1 time per day. The course of treatment is 8 weeks.

Maintenance therapy after treatment of erosive esophagitis and relief of heartburn. The recommended dose is 30 mg 1 time per day. In the studies, the course of treatment was up to 6 months.

For patients with moderate and severe erosive esophagitis, the recommended dose is 60 mg 1 time per day. In the studies, the course of 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 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 admission of the drug in patients with severe disorders (class C on Child-Pugh) are missing.

Dose adjustment in elderly patients, patients with impaired renal function and with impaired liver function of mild severity (Child-Pugh class A) is not required.

Adverse reactions

On the part of the immune system: the frequency is unknown - hypersensitivity (including anaphylactic reactions), malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis, exfoliative dermatitis, anaphylactic shock.

On the part of metabolism and nutrition: the frequency is unknown - hypomagnesaemia, hyponatremia.

On the part of the digestive tract: often - diarrhea, discomfort and abdominal pain, constipation, flatulence, nausea, vomiting; infrequently - dry mouth; rarely - oral candidiasis; frequency is unknown - swelling of the oral mucosa, pancreatitis.

On the part of the kidneys and urinary tract: the frequency is unknown - acute renal failure.

On the part of the liver and biliary tract: infrequently - a change in the indicators of the functional activity of the liver; frequency unknown - drug hepatitis.

On the part of the skin and subcutaneous tissues: infrequently - rash, hives, itching; frequency is unknown - leukocytoclastic vasculitis, generalized rash.

On the part of the respiratory system, chest organs and mediastinum: often - infectious diseases of the upper respiratory tract; infrequently - cough; frequency is unknown - swelling of the larynx, feeling of tightness in the throat.

On the part of the blood and lymphatic system: the frequency is unknown - autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura.

From the musculoskeletal and connective tissue: the frequency is unknown - fractures.

On the part of the vessels: infrequently - the attack of heat (tides), increased blood pressure.

On the part of the nervous system: often - headache; infrequently - dizziness, dysgeusia; rarely - paresthesia, convulsions; frequency unknown - stroke, transient ischemic attack.

On the part of the organ of vision: rarely - visual impairment; frequency unknown - misting.

On the part of the organ of hearing and labyrinth disturbances: rarely - vertigo; frequency is unknown - decrease in hearing.

Mental Disorders: Infrequently - insomnia, depression; rarely - auditory hallucinations.

General disorders: infrequently - weakness, changes in appetite; frequency unknown - swelling of the face.

With care: taking tacrolimus at the same time; CYP2C19 isoenzyme inhibitors (such as fluvoxamine); warfarin (controlled by PF and INR); methotrexate.

Drug interactions

Dexansoprazole can be prescribed without the risk of drug interaction to patients taking clopidogrel. In the case of co-administration of a dose adjustment, clopidogrel is not required.The absence of clinically significant drug interactions with phenytoin, theophylline and diazepam was also noted.

The simultaneous use of dexlansoprazole may affect the absorption of drugs, the bioavailability of which depends on the pH of the stomach (for example, ampicillin esters, digoxin, iron salts, ketoconazole, erlotinib).

Simultaneous administration with tacrolimus can lead to an increase in plasma tacrolimus concentration, especially in post-transplant patients who are moderate or slower metabolizers of the CYP2C19 isoenzyme.

When taken simultaneously with fluvoxamine, there is a possibility of an increase in systemic exposure to dexlansoprazole.

The simultaneous administration of dexlansoprazole and methotrexate can lead to an increase and maintenance of a high concentration of methotrexate and / or its metabolite in the blood serum. If it is necessary to take high doses of methotrexate, temporary withdrawal of dexlansoprazole is recommended.

Pregnancy and Lactation

Use of the drug Dexilant^® during pregnancy is contraindicated. If necessary, the use of the drug during lactation should stop breastfeeding.

Special instructions

Before starting treatment with dexlansoprazole, the possibility of a malignant neoplasm of the gastrointestinal tract should be excluded, since the drug can mask the symptoms and delay the correct diagnosis.

If symptoms persist despite adequate treatment, further examination should be carried out.

When taking proton pump inhibitors, which include dexlansoprazole, increases the risk of gastrointestinal 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 in the treatment of diarrhea. Patients in this case it is recommended to take the minimum effective dose of dexlansoprazole with the shortest duration of treatment.

In patients receiving high doses of the drug or with prolonged therapy with proton pump inhibitors (AITs) for a year or more, the risk of osteoporotic fractures of the thighs, hands and spine increases. Patients at risk for osteoporotic fractures should adhere to the recommended dosages (see “Dosage and Administration”).

In rare cases, patients experienced symptomatic and asymptomatic hypomagnesemia when taking drugs with IIT for at least 3 months, and in most cases, when taken 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 at the same time taking drugs with digoxin or other drugs that can cause hypomagnesemia (such as diuretics), it is necessary to control the concentration of magnesium in the serum before and during treatment.

Impact on the ability to drive vehicles / mechanisms. Because of the likelihood of dizziness and visual impairment, you should refrain from driving and other mechanisms that require increased attention.