Gaslon N OD Tablets

Irsogladine maleate.

Gaslon N OD Tablets 2 mg: Each tablet contains 2 mg of irsogladine maleate (INN: irsogladine). (See Table 1.)

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Gaslon N OD Tablets 4 mg: Each tablet contains 4 mg of irsogladine maleate (INN: irsogladine). (See Table 2.)

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Nonproprietary name: Irsogladine maleate (JAN).
INN: Irsogladine.
Chemical name: 2,4-Diamino-6-(2,5-dichlorophenyl)-s-triazine maleate.
Molecular formula: C₉H₇Cl₂N₅·C₄H₄O₄.
Molecular weight: 372.16.
Irsogladine maleate occurs as white crystals or crystalline powder. It is odorless, and has a slightly bitter taste. It is sparingly soluble in 2-methoxyethanol, in glacial acetic acid and in ethylene glycol, slightly soluble in ethanol, and practically insoluble in water.
Melting point: 175-183°C (decomposition).
Partition coefficient: 1.4 [n-octanol/buffered solution (pH 1.2)]; 54.0 [n-octanol/buffered solution (pH 6.8)].
Excipients/Inactive Ingredients: Lactose hydrate, D-mannitol, corn starch, hydroxypropylcellulose, magnesium stearate and yoghurt flavor (aroma chemicals, glycerin and dextrin).

Agents for peptic ulcer (Other) group.
Pharmacology: Pharmacodynamics: Mechanism of action: Irsogladine, a mucosal protective agent, has effect based on a mechanism apparently different from those of antisecretory drugs.
Irsogladine increased intercellular cyclic adenosine 3',5'-monophosphate (cAMP) content via non-selective inhibition of phosphodiesterase (PDE) isozymes and exhibited gastric cytoprotection partly mediated by endogenous nitric oxide (NO).
These effects may account for variety actions of Irsogladine in the gastrointestinal tract, including facilitation of gap junctional intercellular communication (GJIC), inhibition of the reduced gastric mucosal blood flow response, suppression of reactive oxygen generation).
Pharmacodynamic effects: Effects on experimentally-induced ulcer: Irsogladine maleate showed antiulcer effects dose-dependently at low doses of 1-10 mg/kg in acute experimental ulcers such as water-immersion stress-induced ulcers in rats, ethanol-induced ulcers in rats, Shay ulcers in rats, indomethacin-induced ulcers in rats, histamine-induced ulcers in guinea pigs and rats, and aspirin-induced ulcers in rats, monochloramine-induced ulcers in rats and ischemia-reperfusion induced-injury of gastric mucosa in rats and in chronic experimental ulcers such as acetic acid-induced ulcers in rats and electric thermocauterization ulcers in dogs.
Effects on experimentally-induced gastritis: Irsogladine maleate showed the effects that this drug dose-dependently inhibited or promoted the healing for the ethanol-induced gastritis, taurocholic acid-induced atrophic gastritis and NH₄OH-induced gastric mucosa lesion in rats.
Cytoprotective effect: Irsogladine maleate inhibited the desquamation and exfoliation of gastric mucosal epithelial cells induced by intragastric infusion of 0.2N hydrochloric acid and inhibits the expansion of intercellular spaces in rats.
Irsogladine maleate inhibited the exfoliation and desquamation of gastric mucosal epithelial cells induced by oral administration of dehydrated ethanol in rats.
Irsogladine maleate inhibited the penetration of gastric mucosal lesion-inducing substances such as 0.2N hydrochloric acid, ethanol and etc. through the gastric mucosa in rats.
Improving effect on blood flow rate of gastric mucosa: Irsogladine maleate increased dose-dependently mucosal blood flow at the marginal area of acetic acid-induced ulcer in dogs. Irsogladine maleate also inhibited monochloramine-induced decrease of gastric mucosal blood flow in rats.
Anti-inflammatory effects: Irsogladine maleate inhibited the production of reactive oxygen species induced by stimulants in activated human neutrophil (in vitro).
Irsogladine maleate inhibited the production of TNF-α in gastric mucosa injured by ischemia-reperfusion and also inhibited the infiltration of inflammatory cells into gastric mucosa in rats indicated with MPO activity.
Irsogladine maleate inhibited dose-dependently the production of IL-8 and RANTES in co-cultivation of human gastric mucosa epithelial cells and Helicobacterium pylori (in vitro).
Effect on activation of intercellular communication: Irsogladine maleate activated the intercellular communication in Dye Coupling method using rabbit fetal gastric mucosa epithelial cells (in vitro).

Gastric ulcer.
Improvement of gastric mucosal lesion (erosion, hemorrhage, redness and edema) caused by the following diseases: Acute gastritis and acute exacerbation stage of chronic gastritis.

For adults, usually 4 mg daily as irsogladine maleate (two tablets of Gaslon N OD Tablets 2 mg or one tablet of Gaslon N OD Tablets 4 mg) is orally administered in 1 to 2 divided doses. Usage in pediatric patient has not been established.
The dosage may be adjusted according to the age of patients and severity of symptoms.
This drug disintegrates in the oral cavity, but is not absorbed from the oral mucosa. It should therefore be swallowed with saliva or water.

In the event of overdosage general symptomatic and general supportive measures are indicated as required.

In patient with hypersensitivity to irsogladine or to any of the excipients.

Use in Children: Safety in pediatric patients has not been established (insufficient clinical experience).
Use in the Elderly: Since the elderly patients often have a physiological hypofunction, this drug should be carefully administered such as starting at a low dose (e.g. 2 mg/day) while closely monitoring the patient's condition.

Safety of this drug in pregnant women has not been established.

Adverse drug reactions to this drug, including abnormalities in laboratory data, were reported in 64 of 10,176 patients (0.63%). The most frequently observed adverse drug reactions were hepatic function abnormal in 12 patients (0.12%), increased ALT (GPT) in 12 patients (0.12%), increased AST (GOT) in 7 patients (0.07%), constipation in 6 patients (0.06%), rash in 5 patients (0.05%), itching, diarrhea and increased ALP in each 3 patients (0.03%).
(At the end of the reexamination period of Gaslon N Tablets and Fine Granules.) (See Table 3.)

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There have not been any studies to confirm Irsogladine causes drug interactions with other drugs.

Precaution in dispensing: For drugs that are dispensed in press-through package (PTP), 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 puncture the esophageal mucosa, resulting in severe complications such as mediastinitis.)
Precaution in administration: Since this drug disintegrates when it was infiltrated with saliva on tongue, it can be taken without water. It is also possible to take it with water.
Incompatibilities: Not applicable.

Store below 30°C.
Store in a tight container. Avoid humidity at room temperature.

Antacids, Antireflux Agents & Antiulcerants

A02BX16 - irsogladine ; Belongs to the class of other drugs used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).

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