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Drug ELTHON 50mg have composition itopride hydrochloride, Indication for Gastrointestial symptoms in chronic gastritis : feeling of enlarged abdomen, upper abdominal pain, anorexia, heartburn, nausea and vomiting

MEPRAZ treat of for Gastric ulcer, Gastroesophageal Reflux Disease

Maalox treatment of Gastritis,  Dyspepsia, Peptic ulcer, Hiatal hernia

OpeCipro 500mg is indicated for severe infections

PHYSICOCHEMISTRY

Nonproprietary name: ELTHON 50mg ( itopride hydrochloride ) Chemical name: N-[4-[2-(Dimethylamino) ethoxy]benzyl]-3,4- dimethoxybenzamide monohydrochloride Molecular formula: C20H26N2O4, HCL

Description: itopride hydrochloride occurs as white to pale yellowish white crystals or crystalline powder. It is odorless and has a bitter taste. It is very soluble in water, freely soluble in methanol or in glacial acetic acid, sparingly soluble in ethanol and practically in-soluble in acetic anhydride or in ether. The pH of the solution (1->10) is 4.0 to 5.0.

Melting point: 193 to 198°C

Partition coefficient: 5.7 [pH7.4, 1-octanol/buffer]

ELTHON 50mg Tablet - Itopride hydrochloride

PHARMACOKINETIC:

1. 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.

Fig. 1: Serum Concentrations after single oral administration of 50mg of itopride hydrochloride (Healthy adults in the fasting state, mean +- S.E.)

2. 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 two times 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 in breast milk in comparison to serum concentrations of radioactivity were 1.2 times higher in C max, 2.6 times higher in AUC, and 2.1 times higher in T 1/2

3. Metabolism and Excretion

–  Al a single dose of 100 mg of itopride hydrochloride was orally administered to

healthy adults (6 men) In the fasting stale 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 was the second (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, -2C6, -2C9, 2C19, 2D6. 2E1, or 3A4 was detected.

4. Others

Serum protein binding ratio: Serum protein binding ratio was 96% after orally administration at a single dose 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 ELTHON 50mg were conducted. As the results, the efficacy rate (in the “moderately improved” or better cases) of ELTHON 50mg for gastrointestinal symptoms in chronic gastritis was 77.6% (277/357 patients). (At the approval)

PHARMACOLOGY:

1. Mechanism of action

ELTHON 50mg increases the release of acetylcholine (ACh) through dopamine D2-receptor antagonistic action and inhibits decomposing released ACh through its acetylcholine esterase (AChE) inhibitory action, resulting in enhancement of gastrointestinal motility.

2. Enhancement of the Gastrointestinal Motility Activation of the gastric motility

ELTHON 50mg ( Itopride hydrochloride ) activates the gastric motil-ity dose-dependently in conscious dogs.

– Activation of the gastric emptying ability itopride hydrochloride activates gastric emptying ability in humans, dogs and rats

3. Alleviation of Vomiting

ELTHON 50mg ( Itopride hydrochloride ) inhibits apomorphine-induced vomiting dose-dependently in dogs

INDICATIONS

Gastrointestial symptoms in chronic gastritis ( feeling of enlarged abdomen, upper abdominal pain, anorexia, heartburn, nausea and vomiting )

CONTRAINDICATIONS:

ELTHON is contraindicated in the patients with a history of hypersensitivity to any ingredients of this product. It should not be used during pregnancy unless benefits outweigh the potential risk.

DOSAGE AND 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.

PRECAUTIONS:

1. Important precautions

– ELTHON 50mg should be used with caution since it enhances the action of acetylcholine.

– This product should not be used aimlessly for a long term when no improvement of gastrointestinal symptoms is observed.

2. Drug Interactions

Precautions for co-administration (ELTHON should be administered with care when co-administered with the following drugs.)

Drugs Signs, symptoms, and treatment Mechanism and risk factors
Anticholinergic Drugs: Tiquizlum 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 work against the action of this product

3. Adverse Reactions

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

At the end of reexamination:

Adverse reactions were observed in 74 (1.25%) of 5,913 patients (104 events, 1.76%). The major adverse reactions containing abnormalities in laboratory data were diarrhea (13 events, 0.22%), abdominal pain (8 events, 0.14%), constipation (8 events, 0.14%), increased AST (GOT) (8 events, 0.14%) increased ALT (GRT) (8 events, 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., are observed, administration of the drug should be discontinued and appropriate therapeutic measures taken.

–        Hepatic function disorder and Jaundice (incidence unknown): Hepatic function disorder and jaundice with increased AST (GOT), ALT(GPT) and 7-GTP etc., may occur, and the patient should be carefully monitored. If such abnormalities are observed, administration of the drug should be discontinued and appropriate theraoeutic measures taken.

* Other adverse reactions (AR)

0,1% <= AR < 5% AR <0,1% Incidence

unknown

Hypersensitivity Rash, redness, itching, etc
Exlrnpyramidal symptoms Tremor, etc.
Endocrine Increased prolactin, etc Gynecomastia

etc.

Hematologic 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 y-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,

4. 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.

5. Use during Pregnancy, Delivery or Lactation

– ELTHON 50mg 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 “PHARMACOKINETICS” section]

6. Pediatric Use

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

7. 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.

8. 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 comers of the sheet may puncture the esophageal mucosa, resulting in severe complications such as medi-astinitis.)

PACKAGING: Box of 2 blisters x 10 tablets,

STORAGE: Store below 30eC, protect from light. Keep out of reach of children

SHELF LIFE:

3 years from the date of production. Don’t use beyond the expiry date Specification: Manufacturer’s.

Manufactured by: Abbott Japan Co., Ltd.

Read carefully the package Insert before use your doctor if you need any further information.

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