Dexilant 60 mg

Active substance:

Content

Pharmacological group

Nosological classification (ICD-10)

3D images

Description of the dosage form

Capsules, 30 mg: with an opaque blue cap and an opaque gray body. On the lid in dark gray ink affixed logo “TAR”, on the case – the inscription “30”.

Capsules, 60 mg: with opaque blue cap and body. The TAR logo is affixed to the lid in dark gray ink; the inscription “60” is affixed to the case.

The contents of the capsules are white to almost white granules.

pharmachologic effect

Pharmacodynamics

Dexansoprazole is a proton pump inhibitor (PPI), inhibiting the secretion of gastric juice by inhibiting the H + / K + -ATP-ase in the parietal cells of the stomach. Blocks the final stage of the secretion of hydrochloric acid.

When using antisecretory drugs, the level of gastrin in the blood serum increases in response to a decrease in the secretion of gastric juice. There is also an increase in chromogranin A (CgA) as a result of decreased acidity in the stomach. Elevated CgA levels may interfere with the diagnosis of neuroendocrine tumors.

Published data suggest that the use of PPI should be discontinued 5–14 days before determining the level of CgA, this allows you to return to the rate of falsely elevated levels of CgA concentration that occurs after taking the PPI.

The capsule of the drug Dexilant ® contains two types of granules, enteric-coated, 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

Dexlansoprazole is well absorbed when taken orally. Its bioavailability is 76% or more. The two-component composition of the drug Dexilant ® determines the 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 administration of dexlansoprazole in plasma dosages of 30 and 60 mg Cmax 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.

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

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. 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.

T1 / 2 drug – 1–2 h.

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

Dexilant 60 mg

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 of drug Dexilant ®

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, in

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 environment (such as atazanavir, nelfinavir), due to a significant decrease in their bioavailability;

Dexilant 60 mg

age up to 18 years.

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

With caution, Dexilant ® may be prescribed:

– patients taking tacrolimus;

– patients taking CYP2C19 isoenzyme inhibitors, such as fluvoxamine;

– patients taking warfarin, under the control of PV and INR;

– patients taking methotrexate.

Use during pregnancy and lactation

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

Side effects

The most frequent (at least 2%) undesirable side reactions are diarrhea, flatulence, abdominal pain, nausea, vomiting, infections of the upper respiratory tract.

The following are data on adverse reactions, depending on the frequency of their occurrence: very often – ≥ 1/10; often – ≥1 / 100 and ® were not noted. Repeated doses of 120 mg and a single dose of 300 mg did not cause serious side effects. There was a side effect in the form of increased blood pressure above 140/90 mm

However, in the case of overdose, symptomatic therapy is carried out only in the presence of clinical manifestations.

Dexansoprazole is not excreted by hemodialysis.

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 long-term treatment of IPS for a year or more, the risk of osteoporotic fractures of the thighs, hands and spine increases. Patients with the risk of osteoporotic fractures should adhere to the recommended dosages (see the section “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.

The use of IIT may be associated with very rare cases of the development of subacute lupus erythematosus (PKKV). When a nidus appears, especially in areas of skin exposed to sunlight, and if there is pain in the joints, the patient should immediately consult a doctor, and it is recommended to stop the use of Dexilant ®. It should be noted that in the case of the development of PKKV after the treatment of IPN, the risk of the development of PKKV with the use of other APIs may further increase.

It must be borne in mind that elevated CgA levels may interfere with the diagnosis of neuroendocrine tumors. In order to eliminate this effect, the use of the drug Dexilant ® should be discontinued at least 5 days prior to determining the level of CgA. If the levels of CgA and gastrin do not return to normal values ​​after the first determination, the analysis should be repeated 14 days after discontinuation of the IIT.

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.

Release form

Modified release capsules, 30 mg and 60 mg. On 14 or 28 caps. with a modified release in a bottle of HDPE, sealed with aluminum foil and sealed with a screw-on cap of polypropylene; a container with a desiccant containing silica gel is placed in the vial; 1 fl. placed in a carton box.

14 caps. with modified release in Al. / PVC blister; 1 or 2 blisters are placed in a carton box.

Manufacturer

Registration Certificate Holder: Takeda Pharmaceuticals USA, Inc. One Takeda Parkway, Deerfield, Illinois, 60015, USA.

Takeda Pharmaceuticals USA, Inc. One Takeda Parkway, Deerfield, IL 60015, USA.

Manufacturer: Takeda Pharmaceutical Company Limited, a plant in Osaka.

Dexilant 60 mg

17-85, Yusohonmachi 2-chome, Yodogawa-ku, Osaka 532-8686, Japan.

Takeda Pharmaceutical Company Limited, Osaka Plant.

17-85, Jusohonmachi 2-chome, Yodogawa-ku, Osaka 532-8686, Japan.

Quality Control Issuer: Takeda Pharmaceutical Company Limited, Plant in Osaka.

17-85, Yusohonmachi 2-chome, Yodogawa-ku, Osaka 532-8686, Japan.

Takeda Pharmaceutical Company Limited, Osaka Plant.

17-85, Jusohonmachi 2-chome, Yodogawa-ku, Osaka 532-8686, Japan.

Or (only for blisters in a carton box) Delpharm Novara

Delpharm novara

The claims of consumers should be sent to: Takeda Pharmaceuticals LLC: 119048, Moscow, ul. Usacheva, 2, p. 1.

Tel: (495) 933-55-11; fax: (495) 502-16-25.

Pharmacy sales terms

Storage conditions of the drug Dexilant ®

Keep out of the reach of children.

Shelf life drug Dexilant ®

30 mg modified release capsules – 3 years.

30 mg modified release capsules – 3 years.

60 mg modified release capsules – 3 years.

60 mg modified release capsules – 3 years.

Do not use after the expiration date printed on the package.

Like this post? Please share to your friends:
Leave a Reply