Eltium 50

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ELTIUM 50

Keep out of reach of children

Read the directions carefully before use.

Please consult a physician for more information.

For prescription only.

QUALITATIVE AND QUANTITATIVE COMPOSITION

Active ingredient: Itopride hydrochloride 50 mg

Excipients: Lactose monohydrate, microcrystalline cellulose M101, povidone K30, magnesium stearate, sodium starch glycolate, colloidal silicon dioxide, titanium dioxide, hypromellose 606, hypromellose 615, polyethylene glycol 6000, talc.

PHARMACEUTICAL FORM: Film coated tablet.

Product description: A white to off-white, round, film-coated tablet, plain on both sides, intact edges.

THERAPEUTIC INDICATIONS

Gastrointestinal symptoms in chronic gastritis (bloating feeling, upper abdominal pain, anorexia, heartburn, nausea and vomiting).

POSOLOGY AND METHOD OF ADMINISTRATION

The usual adult dosage for oral use is 150 mg of itopride hydrochloride (3 tablets) daily in three divided doses before meals. The dose may be reduced according to patient’s age and symptoms.

CONTRAINDICATIONS

Itopride hydrochloride is contraindicated in the patients with a history of hypersensitivity to any ingredients of this product. It should not be used during pregnancy unless really necessary.

SPECIAL WARNINGS AND PRECAUTIONS:

Important precautions

- Itopride hydrochloride should be used with caution since it enhances the action of acetylcholine.

- This product should not be used continuously for an extended period when no improvement of gastrointestinal symptoms is observed.

Precautions concerning use

Precautions regarding dispensing: For drugs that are dispensed in a press-through package (FTP), instruct the patient to remove the drug from the package prior to use. (It has been reported that, if the PTP sheet is swallowed, the sharp corners of the sheet may puncture the esophageal mucosa, resulting in severe complications).

USE IN PREGNANCY AND LACTATION

- This medicine should be used in pregnant women or in women who may possibly be pregnant only If the expected therapeutic benefits outweigh the possible risks associated with treatment, (The safety of this product in pregnant women has not been established).

- It is ideal not to use this product in women during lactation, but if it Is necessary, breast feeding should be avoided during the treatment of this product. (It has been reported that itopride hydrochloride Is excreted in breast milk in the animal experiments (rats)). (See “Pharmacokinetic properties” section)

PEDIATRIC USE

The safety of this product in children has not been established (There are a few clinical experiences).

USE IN THE ELDERLY

Since the elderly often have a physiological hypo-function, adverse reactions are liable to appear. The patients receiving this product, therefore, should be carefully observed, if any adverse reactions appear, appropriate measures such as reduction or interruption of the drug should be taken.

EFFECTS ON THE ABILITY TO DRIVE AND USE MACHINES

Adverse drug reactions such as dizziness may occur. Under these conditions the ability to react may be decreased.

INTERACTIONS

Precautions for co-administration with the following drugs:

Drugs

Signs, symptoms, and treatment

Mechanism and risk factors

Anticholinergic drugs:

 Tiquizium bromide, scopolamine butyl bromide, timepidium bromide, etc.

Symptoms:

There is a possibility of reducing the action of this product that activates gastrointestinal motility (cholinergic action).

Mechanism:

Inhibitory action of anticholinergic agent may pharmacologically opposes the action of this product

UNDESIRABLE EFFECTS

At the approval in Japan: Adverse reactions were observed in 14 (2.45%) of 572 patients (19 cases, 3.32%). The major adverse reactions were diarrhea (4 cases, 0.70%), headache (2 cases, 0,35%), abdominal pain (2 cases, 0.35%), Abnormalities in laboratory data were leucopenia (4 cases), increased prolactin (2 cases), etc.

At the end of reexamination: Adverse reactions were observed in 74 (1.25%) of 5,913 patients (104 cases, 1.76%). The major adverse reactions containing abnormalities in laboratory data were diarrhea (13 cases, 0.22%), abdominal pain (8 cases, 0.14%), constipation (8 cases, 0.14%), increased AST (GOT) (8 cases, 0.14%) increased ALT (GPT) (8 cases, 0.14%), etc.

Clinically significant adverse reactions

- Shock and anaphylactoid reaction (incidence unknown): Shock and anaphylactoid reaction may occur, and the patient should be carefully monitored. If any signs of shock and anaphylactoid reaction such as hypotension, dyspnoea, larynx oedema, urticaria, pallor and diaphoresis etc. occur, the drug should be discontinued and appropriate therapeutic measures implemented.

- Hepatic function disorder and jaundice (incidence unknown): Hepatic function disorder and jaundice with increased AST (GOT), ALT(GPT) and γ -GTP etc., may occur, and the patient should be carefully monitored. If such abnormalities occur, the drug should be discontinued and appropriate therapeutic measures implemented.

Other adverse reactions (AR)

 

0.1% < AR < 5%

AR < 0.1%

Incidence unknown (1)

Hypersensitivity (2)

   

Rash, redness, itching, etc.

Extrapyramidal symptoms (2)

 

Tremor, etc.

 

Endocrine (2)

 

Increased prolactin, etc.

Gynecomastia

Hematologic (2)

 

Thrombocytopenia, leucopenia, etc.

 

Gastrointestinal

Diarrhea, constipation, abdominal pain, etc.

Nausea, increased saliva, etc.

 

Psychoneurologic

 

Headache, irritated feeling, sleep disorder, dizziness, etc.

 

Hepatic

Increased AST (GOT), increased ALT (GPT), etc.

Increased γ -GTP, Increased Al-P, etc.

 

Renal

 

Increased BUN. Increased creatinine, etc.

 

Others

 

Chest or back pain, fatigue

 

Note:

(1) Incidence is unknown due to spontaneous reports.

(2) If any abnormality is observed, appropriate measures, such as discontinuation of the medication, should be taken.

PHARMACODYNAMIC PROPERTIES

Mechanism of action

Itopride hydrochloride enhances the release of acetylcholine (ACh) through dopamine D2-receptor antagonistic action and inhibits decomposition of released ACh through its acetylcholine esterase (AChE) inhibitory action, resulting in enhancement of gastrointestinal motility.

Enhancement of the gastrointestinal motility activation

- Enhancement of the gastric motility activation.

Itopride hydrochloride activates the gastric motility dose-dependently in conscious dogs.

- Activation of the gastric emptying ability

Itopride hydrochloride activates gastric emptying ability in humans, dogs and rats

Alleviation of vomiting

Itopride hydrochloride inhibits apomorphine-induced vomiting in dogs in dose-dependent manner.

PHARMACOKINETIC PROPERTIES

Serum concentrations

The serum concentrations and pharmacokinetic parameters in healthy adults, after single oral administration of 50 mg of itopride hydrochloride in the fasting state, are shown in the following Figure 1 and Table 1.

Figure 1: Serum concentrations after a single oral administration of 50 mg of itopride hydrochloride (healthy adults in the fasting state, mean ±S.E)

Table 1: Pharmacokinetic parameters

Dose (mg)

Cmax (µg/ mL)

Tmax (hr)

AUC (µg.hr/ mL)

T1/2β (hr)

50

0,28 ± 0,02

0,58 ± 0,08

0,75 ± 0,05

5,77 ± 0,33

Mean value ± standard deviation, n = 6

Distribution

Results of animal experiments

- The concentrations reached the maximum in almost all tissues at 1 to 2 hours after a single oral dose of 5 mg/kg of 14C-itopride hydrochloride to rats, and the level at 2 hours after administration was high in the kidneys, small intestines, liver, adrenal glands, and stomach in the order of the level (high to low) and the transfer into the central nervous system, such as brain and spinal marrow, was minimal.

- In intraduodenal administration of 5 mg/kg of 14C-itoprlde hydrochloride to rats, the radioactivity concentrations in the gastric muscular layers were about twice as high as those in the blood.

- Excretion in breast milk; When 5 mg/kg of 14C-itopride hydrochloride was orally administered to rats, concentrations of radioactivity in breast milk in comparison to serum concentrations of radioactivity were 1.2 times higher in Cmax, 2.6 times higher in AUC, and 2.1 times higher in T1/2

Metabolism and excretion

- At a single oral administration of 100 mg of itopride hydrochloride was orally administered to healthy adults (6 men) in the fasting state, the urinary excretion rate within 24 hours after administration was highest in the N-oxide form [67.54 % of the dose (89.41% of the urinary excretion)] and in the unchanged compound (4.14%) and in the others were minimal.

- In the experiments using microsomes that express a human CYP or flavine monooxygenase (FMO), it was found that FM01 and FM03 were involved in the production of main metabolic N-oxide form. However, no N-oxygenase activity of CYP1A2, -2A6, -2B6, -2C8, -2C9, 2C19, 2D6. 2E1, or 3A4 was detected.

Others

Serum protein binding ratio: Serum protein binding ratio was 96% after a single oral administration of 100mg of itopride hydrochloride to healthy adults (6 men) in the fasting state.

CLINICAL STUDIES

Open clinical studies and double-blind comparative studies of itopride hydrochloride were conducted. As the results, the efficacy rate (in the “moderately improved” or better cases) of itopride hydrochloride for gastrointestinal symptoms in chronic gastritis was 77.6% (277/357 patients). (At the approval)

PRESENTATION

Box of 5 blisters x 10 tablets.

Box of 10 blisters x 10 tablets.

SHELF-LIFE: 36 months from the manufacturing date.

STORAGE CONDITIONS: Store in dry places, not exceeding 30oC, protect from light.

SPECIFICATIONS: Manufacturer’s.

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