Dexilant caps. 60 mg No. 28 (dexlansoprazole)

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Dexilant caps. 60 mg No. 28 (dexlansoprazole)

Full description

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Tradename

Dexilant™

International nonproprietary name

Dexlansoprazole

Dosage form

Modified release capsules 30 mg and 60 mg

Composition

One capsule contains

active ingredients: dexlansoprazole 30 mg or 60 mg

excipients: granulated sugar, magnesium carbonate, sucrose, low-substituted hyprolose, hyprolose, hypromellose 2910, talc, titanium dioxide (E 171), methacrylic acid copolymer dispersion, macrogol 8000, polysorbate 80, colloidal anhydrous silicon dioxide, methacrylic acid copolymer (type B), methacrylic acid copolymer (type A), triethyl citrate

Capsule shell:

Carrageenan, potassium chloride, titanium dioxide (E 171), FD&C blue dye

No. 2 aluminum varnish (E132), black iron oxide (E 172), hypromellose, purified gray ink

 — composition of granulated sugar: sucrose, corn starch;

** - composition of methacrylic acid copolymer dispersion: methacrylic acid, ethyl acrylate, sodium lauryl sulfate, polysorbate;

*** — composition of purified gray ink: red iron oxide (E 172), yellow iron oxide (E 172), FD&C blue dye No. 2, aluminum varnish (E 132), carnauba wax, shellac, glycerol monooleate.

Description

Capsules with an opaque blue cap and an opaque gray body. The “TAR” logo is applied to the cap in dark gray ink, and the inscription “30” is printed on the body. The contents of the capsules are white to almost white granules

(for a dosage of 30 mg)

Capsules with opaque blue cap and body. The “TAR” logo is applied to the cap in dark gray ink, and the inscription “60” is printed on the body. The contents of the capsules are white to almost white granules (for a dosage of 60 mg)

Pharmacotherapeutic group

Drugs for the treatment of diseases associated with acidity disorders. Antiulcer drugs and drugs for the treatment of gastroesophageal reflux. Proton pump inhibitors. Dexlansoprazole.

ATX code A02BC06

Pharmacological properties

Pharmacokinetics

Dexilant™ is a dual sustained release drug that results in two different peak plasma concentrations; the first peak occurs within one to two hours after ingestion, followed by a second peak within four to five hours. The half-life of dexlansoprazole is about one to two hours in healthy people and in patients with symptoms of gastroesophageal reflux disease (GERD). There was no accumulation of dexlansoprazole after multiple or single doses of Dexilant™ 30 mg or 60 mg, although the mean area under the curve (AUCt) and maximum drug concentration achieved in plasma (Cmax) of dexlansoprazole were slightly higher (less than 10%) at 5 -th day than on the 1st day.

The pharmacokinetics of dexlansoprazole are highly variable, with coefficient of variation (CV%) values ​​for Cmax, AUC, and oral clearance (CL/F) greater than 30% percent (see Table 1).

Absorption

Following oral administration of 30 mg or 60 mg of Dexilant™ to healthy individuals and patients with symptomatic GERD, the mean Cmax and AUC of dexlansoprazole increased approximately proportionally to the dose.

When Dexilant™ 60 mg granules are mixed with water and administered through a nasogastric tube or orally syringed, the bioavailability (Cmax and AUC) of dexlansoprazole is similar to that of Dexilant™ 60 mg administered as an unopened capsule.

Distribution

Plasma protein binding of dexlansoprazole in healthy volunteers ranged from 96% to 99% and was independent at concentrations of 0.01-20 μg/L. In patients with symptomatic gastroesophageal reflux disease, the apparent volume of distribution (Vz/F) after multiple doses was 40 L.

Metabolism

Dexlansoprazole is extensively metabolized in the liver by oxidation, reduction and subsequent formation of sulfate, glucuronide and glutathione compounds to inactive metabolites. Oxidative metabolites are formed through the cytochrome P450 (CYP) enzyme system, including hydroxylation, mainly by CYP2C19, and oxidation to sulfone by CYP3A4.

The CYP2C19 isoenzyme is a polymorphic hepatic isoenzyme that exhibits three phenotypes when metabolizing CYP2C19 substrates; rapid metabolizers (*1/*1), intermediate metabolizers (*1/mutant) and poor metabolizers (mutant/mutant). Dexlansoprazole is the major component circulating in plasma, regardless of CYP2C19 metabolizer status. In intermediate and rapid metabolizers of the CYP2C19 isoenzyme, the main metabolite in the blood plasma is 5-hydroxydexlansoprazole and its glucuronic compound, while in slow metabolizers of CYP2C19 the sulfone is the main metabolite in the blood plasma.

Selection

After administration of Dexilant™, dexlansoprazole is not excreted unchanged in the urine. After administration of 14C-labeled dexlansoprazole to six healthy volunteers, approximately 50.7% (standard deviation (SD): 9.0%) of the administered radioactivity was excreted in the urine and 47.6% (SD: 7.3%) in the feces. Oral clearance in healthy individuals was 11.4-11.6 l/h, respectively, after 5 days of use at doses of 30 mg or 60 mg once daily.

Impact of food intake

In meal studies with healthy volunteers, taking Dexilant™ after a meal was compared with taking the drug on an empty stomach; the increase in Cmax ranged from 12% to 55%, the increase in AUC ranged from 9% to 37%, and Tmax also varied (ranging from a decrease of up to 0.7 hours to an increase of up to three hours).

Special patient groups

Childhood

The pharmacokinetics of dexlansoprazole in patients under 18 years of age have not been studied.

Elderly age

In the elderly, compared with the young, the terminal half-life is significantly longer (2.2 and 1.5 hours, respectively). Systemic exposure (AUC) of dexlansoprazole in elderly patients was significantly higher than in younger patients (34% higher).

Floor

When a single 60 mg oral dose of Dexilant™ was administered to 12 healthy men and 12 healthy women, women had a higher systemic exposure (AUC) (43% higher) than men. This difference does not pose a significant safety concern.

Kidney failure

Dexlansoprazole is extensively metabolized in the liver to inactive metabolites, and the parent substance is not detectable in urine after oral administration of dexlansoprazole. Therefore, the pharmacokinetics of dexlansoprazole is not expected to change in patients with impaired renal function. No studies have been conducted in patients with impaired renal function. In addition, the pharmacokinetics of lansoprazole were not clinically different in patients with mild, moderate or severe renal impairment compared with healthy subjects with normal renal function.

Liver dysfunction

In 12 patients with moderate hepatic impairment (Child-Pugh B) who received a single 60 mg oral dose of Dexilant™, the systemic exposure (AUC) of bound and unbound dexlansoprazole was approximately twice that of patients with normal liver function. liver function. This difference in exposure was not due to differences in protein binding. Studies have not been conducted in patients with severe liver dysfunction.

Pharmacodynamics

Mechanism of action

Dexlansoprazole belongs to the class of antisecretory drugs, is a benzimidazole derivative that suppresses the secretion of gastric juice by inhibiting H+/K+-ATPase in the parietal cells of the stomach. Since this enzyme is considered to be the acid (-proton) pump in the parietal cells, dexlansoprazole is characterized as an inhibitor of the gastric proton pump, since it blocks the final stage of acid formation.

Antisecretory activity

In a crossover study in healthy subjects, the antisecretory effect on 24-hour intragastric pH was assessed when Dexilant™ 60 mg (n = 20) and lansoprazole 30 mg (n = 23) were administered once daily for five days. The results are shown in Table 2.

Effect on serum gastrin levels

The effect of Dexilant™ on serum gastrin concentrations was assessed in approximately 3460 patients in clinical studies lasting up to eight weeks, and in 1023 patients lasting six to 12 months. The mean fasting gastrin concentration increased compared to the control group during treatment with Dexilant™ 30 mg and 60 mg. In patients treated for more than six months, mean serum gastrin levels increased during approximately the first three months of treatment and were stable for the remainder of treatment. Mean serum gastrin levels returned to pre-treatment levels within one month of drug cessation.

Increased gastrin causes hyperplasia of enterochromaffin-like cells (ECL) and serum chromogranin A (CgA) levels. Elevated CgA levels may cause false-positive results in diagnostic tests for neuroendocrine tumors.

Effect on enterochromaffin-like cells (ECL)

When using Dexilant™ 30 mg, 60 mg or 90 mg for up to 12 months, there were no reports of ECL cell hyperplasia based on gastrobiopsy specimens. When lansoprazole was administered to rats up to 150 mg/kg/day throughout life, the development of hypergastrinemia was observed, followed by proliferation of ECL cells and the formation of carcinoid tumors, especially in females.

Effect on cardiac repolarization

At doses up to five times the maximum recommended dosage, dexlansoprazole does not prolong the QT interval to any clinically significant extent.

Indications for use

• treatment of erosive esophagitis of any severity;
• maintenance therapy of treated erosive esophagitis and relief of heartburn;
• for the treatment of heartburn associated with symptomatic nonerosive gastroesophageal reflux disease (GERD)

Directions for use and doses

Important information for use

• Missed Doses: If a dose is missed, take the capsule as soon as possible. However, if the next scheduled dose is already due, do not take the missed dose, but take the next dose on time. Do not take two doses at the same time to make up for a missed dose.
• Dexilant™ can be taken with or without food.
• Swallow whole; do not chew.
• For patients with swallowing problems, Dexilant™ capsules may be opened and taken with applesauce as follows:

1. Place one tablespoon of applesauce in a clean container.

2. Open the capsule.

3. Sprinkle granules into applesauce.

4. Immediately swallow the applesauce granules. Do not chew the granules. Do not store applesauce granules for later use.

• Alternatively, the capsules may be administered with water, an oral syringe, or a nasogastric tube.

Administration with water using an oral syringe

1. Open the capsule and pour the granules into a clean container with 20 ml of water.

2. Place the entire mixture into the syringe.

3. Gently mix the contents of the syringe to prevent the granules from settling.

4. Immediately put the mixture into your mouth. Do not store the mixture of water and granules for later use.

5. Refill the syringe with 10 ml of water, shake gently and insert into the mouth.

6. Refill the syringe again with 10 ml of water, shake gently and insert into the mouth.

Administration with water through a nasogastric tube (>16 French gauge)

1. Open the capsule and pour the granules into a clean container with 20 ml of water.

2. Place the entire mixture into a syringe with a catheter at the end.

7. Gently mix the contents of the syringe to prevent sedimentation of the granules and immediately inject the mixture into the stomach through a nasogastric tube. Do not store the mixture of water and granules for later use.

3. Refill the syringe with 10 ml of water, shake gently and pour into the probe.

4. Refill the syringe with 10 ml of water, shake gently and inject into the stomach.

Dexilant™ is available as capsules in 30 mg and 60 mg doses. Dosage recommendations for adults are given in Table 3.

*Controlled studies lasted no more than 6 months

Dose adjustment in adult patients with erosive esophagitis and liver dysfunction

In patients with moderate hepatic impairment (Child-Pugh class B), the daily dose should not exceed 30 mg of dexlansoprazole once daily for up to 8 weeks.

The use of Dexilant™ is not recommended in patients with severe liver dysfunction (Child-Pugh class C).

Side effects

The following serious adverse reactions are described below and elsewhere in the instructions:

• Acute interstitial nephritis
• Cyanocobalamin (vitamin B12) deficiency
• Clostridial diarrhea
• Bone fracture
• Hypomagnesemia

Clinical research experience

Because clinical trials are conducted under different conditions, the proportion of adverse reactions observed during trials cannot be directly compared with the proportion of reactions in clinical trials with another drug. In addition, they may not reflect the frequency found in practice.

The safety of Dexilant™ was assessed in 4,548 patients in controlled and uncontrolled clinical studies, including 863 patients treated for at least six months and 203 patients treated for one year. The studies included patients aged 18 to 90 years (mean age 48 years), 54% women, 85% Caucasian, 8% black, 4% Asian, and 3% other races. Six randomized controlled clinical trials were conducted on the treatment of erosive esophagitis, maintenance therapy of treated erosive esophagitis and symptomatic GERD. They included 896 patients receiving placebo, 455 patients receiving Dexilant™ 30 mg, 2218 patients receiving 60 mg and 1363 patients receiving lansoprazole 30 mg once daily.

The most common (at least 2%) unwanted side effects are diarrhea, flatulence, abdominal pain, nausea, vomiting, and upper respiratory tract infections.

Adverse reactions leading to discontinuation of therapy

In controlled clinical studies, the most common reaction leading to discontinuation of Dexilant™ was diarrhea (0.7%).

Less frequent adverse reactions

Other adverse reactions reported in controlled studies with an incidence of less than 2% are listed below by body system:

Circulatory and lymphatic system disorders: anemia, lymphadenopathy

Cardiac disorders: angina pectoris, arrhythmia, bradycardia, chest pain, edema, myocardial infarction, palpitations, tachycardia

Hearing and balance disorders: ear pain, tinnitus, dizziness

Endocrine system disorders: goiter

Eye disorders: eye irritation, eye swelling

Gastrointestinal Disorders: Abdominal discomfort, abdominal tenderness, abnormal bowel movements, anal discomfort, Barrett's esophagus, bezoar, abnormal bowel sounds, breath odor, microscopic colitis, colon polyp, constipation, dry mouth , duodenitis, dyspepsia, dysphagia, enteritis, belching, esophagitis, gastric polyp, gastritis, gastroenteritis, gastrointestinal disorders, gastrointestinal hyperkinetic disorders, GERD, gastrointestinal ulcers and perforation, hematemesis, bloody stools, hemorrhoids, impaired gastric emptying, syndrome irritable bowel disease, mucous stools, blistering of the oral mucosa, painful bowel movements, proctitis, oral paresthesia, rectal hemorrhage, retching

General and administration site conditions: adverse drug reaction, asthenia, chest pain, chills, abnormal sense of touch, inflammation, mucosal inflammation, nodular thickening, pain, hyperthermia

Disorders of the liver and biliary tract: biliary colic, cholelithiasis, hepatomegaly

Immune system disorders: hypersensitivity

Infectious and parasitic diseases: candidiasis, influenza, nasopharyngitis, oral herpes, pharyngitis, sinusitis, viral infection, vulvo-vaginal infections

Injuries, poisoning and complications of procedures: falls, fractures, joint dislocations, overdose, pain during the procedure, sunburn

Laboratory tests: increased alkaline phosphatase, increased alanine aminotransferase (ALT), increased aspartate aminotransferase (AST), increased/decreased bilirubin, increased blood creatinine, increased blood gastrin, increased blood glucose, increased blood potassium, abnormal liver function tests , decreased platelet count, increased total protein, weight gain

Metabolic and nutritional disorders: changes in appetite, hypercalcemia, hypokalemia

Skeletal muscle and connective tissue disorders: arthralgia, arthritis, muscle cramps, musculoskeletal pain, myalgia

Nervous system disorders: changes in taste, convulsions, dizziness, headaches, migraines, memory impairment, paresthesia, psychomotor hyperactivity, tremor, trigeminal neuralgia

Mental disorders: unusual dreams, anxiety, depression, insomnia, changes in libido

Renal and urinary tract disorders: dysuria, urinary urgency

Reproductive system and breast disorders: dysmenorrhea, dyspareunia, menorrhagia, menstrual irregularities

Respiratory, thoracic and mediastinal disorders: aspiration, asthma, bronchitis, cough, dyspnea, hiccups, hyperventilation, airway congestion, sore throat

Skin and subcutaneous tissue disorders: acne, dermatitis, erythema, itching, rash, skin lesions, urticaria

Cardiovascular system disorders: deep vein thrombosis, hot flashes, hypertension

Additional adverse reactions reported in a long-term, uncontrolled study and considered by the treating physician to be related to Dexilant™ included: anaphylaxis, auditory hallucinations, B-cell lymphoma, bursitis, central obesity, acute cholecystitis, dehydration, diabetes mellitus, dysphonia, epistaxis, folliculitis, gout, herpes zoster, hyperlipidemia, hypothyroidism, increased number of neutrophils, decreased average hemoglobin concentration in erythrocytes, neutropenia, painful urge to defecate, restless leg syndrome, drowsiness, tonsillitis.

Post-registration experience

The following adverse reactions were identified during post-registration use of the drug Dexilant™. Because these reactions have been reported voluntarily from the public to an unknown extent, it is not always possible to reliably estimate the frequency of their occurrence or establish a causal relationship to drug exposure.

Circulatory and lymphatic system disorders: autoimmune hemolytic anemia, idiopathic thrombocytopenic purpura

Hearing and balance disorders: deafness

Visual disorders: blurred vision

Gastrointestinal disorders: oral edema, pancreatitis

General and injection site conditions: facial swelling

Liver and biliary tract disorders: drug-induced hepatitis

Immune system disorders: anaphylactic shock (requiring emergency intervention), exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis (sometimes fatal)

Infectious and parasitic diseases: clostridial diarrhea

Metabolic and nutritional disorders: hypomagnesemia, hyponatremia

Musculoskeletal disorders: bone fracture

Nervous system disorders: cerebrovascular accident, transient ischemic attack

Renal and urinary tract disorders: acute renal failure

Respiratory, thoracic and mediastinal disorders: laryngeal edema, throat constriction

Skin and subcutaneous tissue disorders: generalized rash, leukocytoclastic vasculitis

Contraindications

• hypersensitivity to any of the components of the drug
• combined use with drugs containing rilpivirine
• acute interstitial nephritis
• children under 18 years of age

Drug interactions

Tables 4 and 5 describe clinically significant drug interactions with Dexilant™, interactions between diagnostic tests and Dexilant™, and recommendations for preventing complications.

Effect of dexlansoprazole on other drugs

Cytochrome P 450

Dexlansoprazole is partially metabolized by CYP2C19 and CYP3A4.

In vitro studies have shown that dexlansoprazole does not inhibit CYP isoforms 1A1, 1A2, 2A6, 2B6, 2C8, 2C9, 2D6, 2E1 or 3A4. Therefore, any clinically significant interactions with drugs that are metabolized by these CYP enzymes are not expected. In addition, in vivo studies have shown that Dexilant™ does not affect the pharmacokinetics of phenytoin (CYP2C9 substrate) or theophylline (CYP1A2 substrate). Although in vitro studies have shown that Dexilant™ may inhibit CYP2C19 in vivo; An in vivo drug interaction study among extensive and intermediate metabolizers of CYP2C19 showed that Dexilant™ does not affect the pharmacokinetics of diazepam (a CYP2C19 substrate).

Clopidogrel

Clopidogrel is partially metabolized to its active metabolite by CYP2C19. A study was conducted in healthy subjects who were extensive metabolizers of CYP2C19 and took clopidogrel 75 mg alone or concomitantly with Dexilant™ 60 mg (n = 40), once daily for nine days. The mean AUC of the active metabolite of clopidogrel was reduced by approximately 9% when clopidogrel was administered with Dexilant™. Concomitant administration of dexlansoprazole and clopidogrel in healthy subjects did not have a clinically significant effect on exposure to the active metabolite of clopidogrel or clopidogrel-induced platelet inhibition.

Effect of other drugs on dexlansoprazole

Because dexlansoprazole is metabolized by CYP2C19 and CYP3A4, inducers and inhibitors of these enzymes may potentially alter the exposure of dexlansoprazole.

special instructions

Gastric neoplasms

A symptomatic response to Dexilant™ does not exclude the presence of gastric malignancy.

Acute interstitial nephritis

Acute interstitial nephritis has been observed in patients taking PPIs, including lansoprazole. Acute interstitial nephritis can occur at any time during PPI therapy, usually associated with an idiopathic hypersensitivity reaction. If acute interstitial nephritis develops, treatment with Dexilant™ should be discontinued.

Cyanocobalamin (vitamin B12) deficiency

Daily treatment with any acid-suppressing drugs for a long period of time (for example, more than 3 years) can lead to impaired absorption of cyanocobalamin (vitamin B12), caused by hypo- or achlorhydria. Rare reports of cyanocobalamin deficiency due to acid suppression therapy have been described. This diagnosis should be considered in patients taking Dexilant™ if clinical symptoms suggestive of cyanocobalamin deficiency are observed.

Clostridial diarrhea

Published observational studies suggest that PPI therapy, such as Dexilant™ therapy, may be associated with an increased risk of clostridial diarrhea, particularly in hospitalized patients. This diagnosis should be considered for diarrhea that does not improve.

Patients should use the lowest dose and shortest duration of PPI therapy appropriate for the condition being treated.

Bone fracture

A number of published observational studies suggest that PPI therapy may be associated with an increased risk of hip, wrist, or spine fractures associated with osteoporosis. The risk of fracture is increased in patients receiving high doses, determined by