Universal reference book for medicines
Product name: DEXILANT ® (DEXILANT)

Active substance: dexlansoprazole

Type: H + -K + -ATPase inhibitor

Manufacturer: TAKEDA PHARMACEUTICALS USA, Inc.
(USA) manufactured by TAKEDA PHARMACEUTICAL COMPANY (Japan) issuing quality control TAKEDA PHARMACEUTICAL COMPANY (Japan)

Capsules with a modified release with an opaque blue lid and an opaque gray body;
The cap is marked with a dark-gray ink logo "TAP", on the body - the inscription "30"; the contents of the capsules are white to almost white granules.
1 caps.

dexlensoprazole 30 mg

Auxiliary substances: sugar grits (from 500 microns to 710 microns) - 28.8 mg (sucrose 18-26.352 mg, corn starch 2.448-10.8 mg), magnesium carbonate - 11.5 mg, sucrose - 41.5 mg, low-substituted giprolose 8.64 mg, giprolose - 0.34 mg, hypromellose 2910 - 7.54 mg, talc - 16.64 mg, titanium dioxide 5.5 mg, dispersion of methacrylic acid copolymer 9.66 mg (methacrylic acid 4.4436 mg, ethyl acrylate 4.2504 mg, sodium lauryl sulfate 0.2254 mg, polysorbate 80 0.7046 mg ), macrogol 8000 - 0.96 mg, polysorbate 80 - 0.44 mg, silicon dioxide colloid - 0.09 mg, copolymer of methacrylic acid and methyl methacrylate
[1: 2] - 15.95 mg, copolymer of methacrylic acid and methyl methacrylate [1: 1] - 5.32 mg, triethyl citrate - 2.12 mg.
The composition of the shell capsules: carrageenan - 0.192-0.624 mg, potassium chloride - 0.144-0.48 mg, titanium dioxide - 2.4768 mg, dye FD & C blue No. 2 aluminum lacquer - 0.3456 mg, iron dye oxide black - 0.0576 mg, hypromellose qs up 48 mg, gray ink cleaned for marking - trace amounts.

Composition of gray ink purified: iron oxide red oxide, iron oxide yellow oxide, dye FD & C blue No. 2 aluminum varnish, carnauba wax, shellac, glyceryl monooleate.

14 pcs.
- blisters AL / PVC (1) - packs cardboard.
14 pcs.
- blisters AL / PVC (2) - packs cardboard.
14 pcs.
- polyethylene bottles (1) - cardboard packs.
28 pcs.
- polyethylene bottles (1) - cardboard packs.
Capsules with modified release with opaque blue lid and body;
The cap is marked with a dark-gray ink logo "TAP", on the body - the inscription "60"; the contents of the capsules are white to almost white granules.
1 caps.

dexlansoprazole 60 mg

Auxiliary substances: sugar grits (from 500 microns to 710 microns) - 40 mg (sucrose 25-36.6 mg, corn starch 3.4-15 mg), magnesium carbonate - 16 mg, sucrose - 39.52 mg, low-substituted giprolose - 12 mg, giprolose - 0.48 mg, hypromellose 2910-105067 mg, talcum 27.5499 mg, titanium dioxide 6.9933 mg, dispersion of methacrylic acid copolymer 7.02 mg (methacrylic acid 3.2292 mg, ethyl acrylate 3.0888 mg, sodium lauryl sulfate 0.1638 mg, polysorbate 80 0.5382 mg ), macrogol 8000 - 0.7 mg, polysorbate 80 - 0.32 mg, silicon colloidal dioxide - 0.13 mg, copolymer of methacrylic acid and methyl methacrylate [1:
2] - 31.9 mg, a copolymer of methacrylic acid and methyl methacrylate [1: 1] - 10.64 mg, triethyl citrate - 4.24 mg.
The composition of the capsule shell: carrageenan 0.24-0.78 mg, potassium chloride 0.18-0.6 mg, titanium dioxide 2.52 mg, dye FD & C blue No. 2 aluminum lacquer 1.08 mg, hypromellose qs up to 60 mg, gray ink cleaned for labeling trace amounts.

Composition of gray ink purified: iron oxide red oxide, iron oxide yellow oxide, dye FD & C blue No. 2 aluminum varnish, carnauba wax, shellac, glyceryl monooleate.

14 pcs.
- blisters AL / PVC (1) - packs cardboard.
14 pcs.
- blisters AL / PVC (2) - packs cardboard.
14 pcs.
- polyethylene bottles (1) - cardboard packs.
28 pcs.
- polyethylene bottles (1) - cardboard packs.
INSTRUCTION FOR THE SPECIALIST.

Description of the drug approved by the manufacturer for the printed edition of 2017.

PHARMACHOLOGIC EFFECT

Proton pump inhibitor.
Suppresses the secretion of gastric juice by inhibiting H + / K + -ATP-ase in parietal cells of the stomach. It blocks the final stage of hydrochloric acid secretion.
The capsule of Dexilant ® disintegrates in the stomach and contains two types of enteric coated granules that release the active substance depending on the pH in various areas of the small intestine.
This combination helps prolong the effect of dexlansoprazole and helps reduce gastric juice secretion for a long time.
PHARMACOKINETICS

Suction

Dexlansoprazole is well absorbed when ingested.
Its bioavailability is 76% or more.
The two-component formulation of the Dexylant ® prepares absorption in the form of two pH-dependent phases.
The first peak of the concentration of the active substance occurs between 1 and 2 hours after ingestion (1 phase of release of the active substance) and 4 to 5 hours (2 phase of release of the active substance), respectively. After 5 days of taking dexlansoprazole in doses of 30 mg and 60 mg C max in 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 dexlansoprazole at 30 mg and 60 mg, respectively.
Distribution

Binding dexlansoprazole to plasma proteins is 96.1-98.8%.

Metabolism

Dexlensoprazole is extensively metabolized in the liver to inactive metabolites as a result of oxidation, reduction and subsequent formation of sulfate, glucuronide and glutathione compounds.
Oxidation is carried out with the help of the cytochrome P450 enzyme system, which is involved both in the hydroxylation process (mainly the isoenzyme CYP2C19) and in the oxidation process (isoenzyme CYP3A4). The CYP2C19 isoenzyme is a polymorphic hepatic isoenzyme that exists in 3 fractions exhibiting different properties in the metabolism of substrates: fast, moderate and slow metabolizers. Dexlensoprazole is the main component in blood plasma, regardless of the type of metabolizer for the isoenzyme CYP2C19. In the case of medium and strong metabolizers for the isoenzyme CYP2C19, the main metabolite in the blood plasma is 5-hydroxydeclansoprazole and its glucuronic compound. At weak metabolizers on isoenzyme CYP2C19 - dexlansoprazole sulfone.
Excretion

T 1/2 is 1-2 hours. The clearance after 5 days of taking dexlansoprazole is 11.4 and 11.6 l / h for a dosage of 30 mg and 60 mg, respectively.
The drug is excreted by the kidneys (about 51%) and 48% is excreted through the intestine. Because the drug is intensively metabolized in the liver, with the use of dexlansoprazole in patients with impaired renal function, dose reduction is not required. 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 of GERD (ie NERB - non-erosive reflux disease).

DOSING MODE

Inside: the capsule is taken entirely regardless of the food intake.
Also, you can open the capsule, pour the granules out of it into a tablespoon and mix them with apple puree; then immediately, without chewing, swallow.
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 symptoms: the recommended dose is 30 mg 1 time / day.
In the studies, the course of treatment was up to 6 months.
With erosive esophagitis of medium and severe degree, the recommended dose is 60 mg 1 time / day.
In the studies, the course of treatment was up to 6 months.
Symptomatic treatment of gastroesophageal reflux disease GERD (ie NERB - 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 (class B by Child-Pugh), the daily dose should not exceed 30 mg of dexlansoprazole.

Clinical data on the administration of the drug in patients with severe disorders (class C according to Child-Pugh) are absent.

Dose adjustments in elderly patients, patients with impaired renal function and with mild liver function disorder (Child-Pugh class A) are not required.

SIDE EFFECT

Most often (at least 2%): diarrhea, flatulence, abdominal pain, nausea, vomiting, upper respiratory tract infection.

Determination of 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 available data).

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.

From the side of metabolism: the frequency is unknown - hypomagnesemia, hyponatremia.

On the part of the digestive system: often - diarrhea, discomfort and abdominal pain, constipation, flatulence, nausea, vomiting;
infrequently dry mouth; rarely - candidiasis of the oral cavity; frequency unknown - edema of the oral mucosa, pancreatitis.
From the side of the urinary system: the frequency is unknown - acute renal failure.

From the side of the liver and bile ducts: infrequently - a change in the indices of the functional activity of the liver;
frequency unknown - drug-induced hepatitis.
From the skin and subcutaneous tissues: infrequently - rash, hives, itching;
frequency unknown - leukocytoclastic vasculitis, generalized rash.
From the respiratory system: often - infectious diseases of the upper respiratory tract;
infrequently - cough; the frequency is unknown - the laryngeal edema, a 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 system: the frequency is unknown - fractures.

From the side of the cardiovascular system: infrequently -
a fit of fever ("hot flashes"), an increase in blood pressure.
From the nervous system: often - headache;
infrequently - dizziness, dysgeusia; rarely - paresthesia, convulsions; frequency unknown - stroke, transient ischemic attack.
From the side of the organ of vision: rarely - visual impairment;
frequency unknown - visual impairment (fogging).
From the side of the hearing organ and labyrinthine disturbances: rarely - vertigo;
frequency unknown - hearing loss.
Disorders of the psyche: infrequently - insomnia, depression;
rarely - auditory hallucinations.
General disorders: infrequent - weakness, changes in appetite;
frequency unknown - swelling of the face.
CONTRAINDICATIONS

- hypersensitivity to any of the components of the drug;

- combined use with HIV protease inhibitors, the absorption of which depends on the pH of the stomach (such as atazanavir, nelfinavir) due to a significant reduction in their bioavailability;

- age up to 18 years;

- Pregnancy;

lactation period.

The drug contains sucrose, so its use is not recommended for patients with hereditary intolerance to fructose, glucose-galactose malabsorption or sucrose-isomaltase deficiency.

Carefully:

- patients taking tacrolimus;

- patients taking inhibitors of the isoenzyme CYP2C19, such as fluvoxamine;

- patients taking warfarin (under the control of prothrombin time and MHO);

- patients taking methotrexate.

PREGNANCY AND LACTATION

The use of the drug Dexylant ® during pregnancy is contraindicated.
If it is necessary to use the drug during lactation, breastfeeding should be stopped.
APPLICATION FOR FUNCTIONS OF THE LIVER

Correction of the dose in patients with impaired renal function is not required.

APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS

In patients with impaired liver function of moderate severity (class B but Child-Pugh), the daily dose should not exceed 30 mg of dexlansoprazole.

Clinical data on the administration of the drug in patients with severe disorders (class C according to Child-Pugh) are absent.

Dose adjustments in patients with mild liver function disorder (Child-Pugh class A) are not required.

APPLICATION FOR CHILDREN

Contraindicated for children under 18 years.

APPLICATION IN ELDERLY PATIENTS

Dose adjustments in elderly patients are not required.

SPECIAL INSTRUCTIONS

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

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

When taking proton pump inhibitors, such as dexlansoprazole, increases the risk of gastrointestinal infections accompanied by diarrhea, caused by 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 are recommended to take a minimally effective dose of dexlansoprazole with the shortest duration of treatment.

In patients receiving high doses of the drug or prolonged therapy with proton pump inhibitors (PIDs) for a year or more, the risk of osteoporotic fractures of the hips of the hips, brushes and spine increases.
Patients with a risk of osteoporotic fractures should adhere to recommended doses.
In rare cases, symptomatic and asymptomatic hypomagnesemia was observed in patients receiving IPN drugs for at least 3 months, and in most cases - with admission during the year.
Symptoms of hypomagnesemia are tetany, arrhythmia and convulsions. Treatment - the replacement of magnesium and the withdrawal of drugs IPN. In patients who require long-term treatment or who simultaneously take IPN medications with digoxin or other drugs that can cause hypomagnesemia (eg, diuretics), it is necessary to monitor the magnesium concentration in the serum prior to and during treatment.
Impact on the ability to drive vehicles and manage mechanisms

Because of the likelihood of dizziness and visual impairment, patients during the treatment period should refrain from managing vehicles and other mechanisms requiring increased attention.

OVERDOSE

No significant cases of overdose have been reported as a result of the use of Dexilant ® .

Symptoms: multiple doses 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 more than 140/90 mm Hg.
Treatment: in case of an overdose and only in the presence of clinical manifestations, symptomatic therapy is performed.
Dexlansoprazole is not excreted by hemodialysis.
DRUG INTERACTION

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

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

Simultaneous administration with tacrolimus may lead to an increase in tacrolimus concentration in the blood plasma, especially in patients after transplantation, which are moderate or slow metabolizers for the CYP2C19 isoenzyme.

With simultaneous administration with fluvoxamine, there is a possibility of increasing the systemic effect of dexlansoprazole.

Simultaneous administration of dexlansoprazole and methotrexate may lead to an increase and retention of a high concentration of methotrexate and / or its metabolite in the blood serum, which, accordingly, may lead to the development of methotrexate toxicity.
If it is necessary to take high doses of methotrexate, a temporary withdrawal of dexlansoprazole is recommended.
TERMS OF RELEASE FROM PHARMACY

The drug is released by prescription.

TERMS AND CONDITIONS OF STORAGE

The drug should be stored out of reach of children, dry place at a temperature of no higher than 25 ° C.
Shelf life in packing in vials - 4 years, when packing in blisters - 3 years. Do not use after the expiration date printed on the package.
The information is provided for your information, do not self-medicate, it is dangerous for your health.

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