Dekslansoprazole - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Proton pump inhibitors

Included in the formulation

Dexylant®

capsules inwards

Takeda Pharmaceuticals USA, Inc. USA

АТХ:

A.02.B.C Proton pump inhibitors

A.02.B.C.06 Dexlensoprazole

Pharmacodynamics:

The drug is an inhibitor of the proton pump, suppressing the secretion of gastric juice by inhibiting H + / K + -ATPase in parietal cells of the stomach. It blocks the final stage of hydrochloric acid secretion.

The capsule of the preparation contains two types of enteric coated beads that release the active substance after the capsules in the stomach have dissolved, depending on the pH in various regions of the small intestine. This combination helps prolong the effect of dexlansoprazole and helps reduce gastric juice secretion for a long time.

Pharmacokinetics:

Absorbed by 76% or more, the connection with plasma proteins is 96.1-98.8%.

The two-component formulation of the drug causes absorption in the form of two pH-dependent phases. The first peak of the concentration of the active substance occurs in the interval from 1 to 2 hours after ingestion (the first phase of the release of the active substance) and the second in the range of 4 to 5 hours (the 2nd phase of release of the active substance), respectively.

Metabolized in the liver, half-life - 1-2 hours.Excreted by the kidneys approximately 51% and the gastrointestinal tract 48%.

The onset of action for 1 hour, duration of action up to 72 hours, complete recovery of hydrochloric acid production after 4 days.

Indications:

- Gastroesophageal reflux disease (symptomatic treatment);

- Supportive therapy after treatment of erosive esophagitis;

- Relief of heartburn;

- Erosive esophagitis of any severity.

ICD-10

XI.K20-K31.K20 Esophagitis

XI.K20-K31.K21 Gastroesophageal reflux

XI.K20-K31.K21.0 Gastroesophageal reflux with esophagitis

XVIII.R10-R19.R12 Heartburn

Contraindications:

- Pregnancy and breastfeeding;

- Age to 18 years;

- Joint use of human immunodeficiency virus protease inhibitors (atazanavir, nelfinavir);

- Hypersensitivity.

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:

Simultaneous administration of inhibitors CYP2C19 (fluvoxamine), tacrolimus, warfarin (under the control of prothrombin time and MNO), methotrexate.

Pregnancy and lactation:

Category FDA - B. The use of the drug during pregnancy is contraindicated. If it is necessary to use the drug during lactation, breastfeeding should be stopped.

Dosing and Administration:

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.

60 mg once a day, treatment for 8 weeks, with maintenance therapy, recommended taking the drug at a dose of 30 mg per day, the duration of treatment - up to 6 months.

Side effects:

From the side of metabolism and nutrition: hyponatremia, hypomagnesemia.

From the immune system: malignant exudative erythema, exfoliative dermatitis, toxic epidermal necrolysis, anaphylactic shock, hypersensitivity.

From the side of the urinary system: acute renal failure.

From the gastrointestinal tract: candidiasis of the oral cavity, edema of the oral mucosa, pancreatitis, diarrhea, abdominal pain, vomiting, nausea, flatulence, constipation, dry mouth, candidiasis of the mouth.

From the cardiovascular system: increased blood pressure, autoimmune hemolytic anemia, attacks of heat ("hot flashes"), idiopathic thrombocytopenic purpura.

From the nervous system: dizziness, headache, stroke, dysgeusia, insomnia, auditory hallucinations, depression, seizures, paresthesia, stroke, transient ischemic attack, auditory hallucinations.

From the respiratory system: upper respiratory tract infection, cough, throat tightness, laryngeal edema.

From the musculoskeletal system: fractures.

From the skin and subcutaneous tissue: itching, urticaria, rash, generalized rash, leukocytoclastic vasculitis.

On the part of the organs of vision: blurring, various violations.

Hearing impairment: Vertigo.

From the side of the liver: drug hepatitis, changes in liver function.

Other: a change in appetite, weakness, swelling of the face.

Overdose:

There is no information, treatment is symptomatic. Dexlansoprazole is not excreted by hemodialysis.

Interaction:

The drug affects the absorption of other drugs, the bioavailability of which depends on pH gastric juice (for example, ampicillin esters, digoxin, iron salts, ketoconazole, erlotinib).

The drug increases the concentration of tacrolimus (a moderate or slow metabolizer for the isoenzyme CYP2C19) and methotrexate in the blood.

Fluvoxamine (inhibitor isoenzyme CYP2C19) increases the systemic effects of dexlansoprazole.

Special instructions:

Before taking the drug, it is necessary to exclude neoplasms of the gastrointestinal tract.

The drug increases the risk of gastrointestinal infections, the causative agents of which are Clostridium difficile.

In patients receiving high doses of the drug or prolonged therapy with proton pump inhibitors 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 the recommended dosages.

In rare cases, patients experienced symptomatic and asymptomatic hypomagnesemia in admission proton pump inhibitors for at least 3 months, and in most cases - during admission during the year. Symptoms of hypomagnesemia are tetany, arrhythmia and convulsions.Treatment - magnesium supplementation and withdrawal of admission proton pump inhibitors. In patients who need long-term treatment or at the same time proton pump inhibitors with digoxin or other drugs that can cause hypomagnesemia (eg, diuretics), it is necessary to monitor the concentration of magnesium in the serum before and during treatment.

Impact on the ability to drive vehicles / machinery. Due to the likelihood of dizziness and visual impairment, one should refrain from managing vehicles and other mechanisms requiring increased attention.

Instructions

Dexlensoprazole (Dexlansoprazolum)