Selbex

Selbex

teprenone

Manufacturer:

Eisai

Distributor:

DKSH
Full Prescribing Info
Contents
Teprenone.
Description
Each hard capsule contains 50 mg of teprenone.
Physicochemistry: Nonproprietary name: Teprenone (JAN, INN).
Chemical Name: 3:2 (5E:5Z) geometrical mixture of (9E, 13E)-6,10,14,18-tetramethyl-5,9,13,17-nonadecatetraen-2-one.
Molecular Formula: C23H38O.
Molecular Weight: 330.55.
Teprenone occurs as colorless or pale yellow, oily liquid. It has a slight characteristic odor, and is tasteless. It is miscible with methanol, with ethanol (95), with acetone, chloroform and with hexane, and practically insoluble in water.
It is affected by air.
Refractive Index: nD20: 1.485-1.491.
Specific Gravity: d2020: 0.882-0.89.
Excipients/Inactive Ingredients: FD&C Yellow No. 6 (Sunset Yellow FCF), hydrated silicon dioxide, glycine, FD&C Blue No. 1 (Brilliant Blue FCF), talc, corn starch, tocopherol, macrogol 6000, D-mannitol and sodium lauryl sulfate.
Action
Pharmacotherapeutic Group: Gastritis and gastric ulcer treatment.
Pharmacology:
Terpenes are naturally-occurring organic substances that are found in essential oils and in tree and plant resins. They have long been known for their ability to aid in tissue repair.
Teprenone, the active ingredient of SELBEX, is a terpene analogue. It accelerates the biosynthesis of high molecular weight glycoproteins and phospholipids - major components of gastric mucosa and mucus that are involved in the regeneration and defense of gastric mucosa. Teprenone also increases bicarbonate concentrations in gastric mucus. In addition, it prevents or reverses reductions in proliferative capacity of mucosal cells that can be caused by gastric mucosal lesions and promotes repairing of mucosal lesions.
Teprenone has been found to have excellent clinical efficacy in the treatment of acute gastritis, acute exacerbation of chronic gastritis and gastric ulcers.
Anti-ulcer effect: Teprenone has been demonstrated to show a potent anti-ulcer effect against various experimental ulcers in rats (caused by cold-restraint, indomethacin, aspirin, prednisolone, reserpine, acetic acid, thermocautery or aspirin-cold-restraint) and to be very effective against various experimental gastric mucosal lesions (caused by hydrochloric acid, aspirin, ethanol, or radiation).
Further, in an experiment using rats, teprenone has been demonstrated to inhibit gastric mucosal lesions due to compound 48/80 or platelet activating factor (PAF) in which active oxygen is thought to be involved.
Increase of gastric mucus: Teprenone promotes mucus synthesis and secretion in cultured gastric mucosal epithelial cells of rat origin.
When present in the superficial mucous cells and neck cells, teprenone increases the output of mucus from these cells in rats.
Teprenone increases activities of synthetases mediating the biosynthesis of high-molecular glycoprotein in rats and phospholipids in guinea pigs, the main factors for gastric mucosal regeneration and protection, and promotes the synthesis and secretion of high-molecular glycoprotein and phospholipids in rats and humans.
In addition, it has also been demonstrated in rats and rabbits that teprenone increases the bicarbonate content of the gastric mucus.
Cytoprotect effect due to induction of heat shock proteins (HSP) genesis: Teprenone induces genesis of HSP60, 70, 90 in gastric mucosal cells and shows cytoprotect effect in guinea pigs.
Increase of gastric mucosal prostaglandins: Teprenone increases the content of prostaglandin E2 and I2 in the gastric mucus of rats. In rats, the mechanism for this has been demonstrated to be an increase in prostaglandin synthetase activity.
Increase and improvement of gastric mucosal blood flow: Teprenone increases gastric mucosal blood flow in humans. Teprenone rectifies the decrease in gastric mucosal blood flow in water-immersion restrained rats.
Protection of the gastric mucosa: Teprenone inhibits ethanol-induced injury of the gastric mucosa in rats.
Teprenone inhibits ethanol-induced injury of the gastric mucosa in healthy adult male volunteers.
Maintenance of the homeostasis of the gastric mucosal cell proliferation zone: Teprenone enhances gastric mucosal cell proliferation which has been reduced by hydrocortisone in mice, thus helping to maintain the homeostasis of the gastric mucosal cell proliferation zone. Teprenone promotes gastric mucosal regeneration and injured gastric mucosal repair in acetic acid ulcers in rats.
Inhibition of lipid peroxidation: Teprenone inhibits both gastric mucosal injury due to burning as well as increases in lipid peroxide levels in the gastric mucosa in rats.
Clinical Studies: Clinical Efficacy: SELBEX was useful for treatment of acute gastritis and acute exacerbation stage of chronic gastritis in a double-blind clinical trial. The General Improvement Rating (GIR) of SELBEX for patients with gastritis was "markedly improved" in 48% (12/25) and "moderately improved" or better in 92% (23/25).
GIR was determined from the improvement rating for endoscopic findings and the improvement rating for subjective or objective symptoms.
SELBEX was useful for treatment of peptic ulcers in a double-blind clinical trial. The Final Global Improving Ratio (FGIR) of SELBEX for patients with gastric ulcers was "markedly improved" in 47% (61/131) and "slightly improved" or better in 93% (122/131).
FGIR was evaluated by coordinating the findings of endoscopy and roentgenography with the degree of improvement of subjective and objective symptoms.
Pharmacokinetics: Blood concentration: Three capsules of SELBEX Capsules or 1.5 g of SELBEX Fine Granules 10% (150 mg of teprenone) were administered orally to twelve healthy adult male volunteers after a meal in a cross-over design. The serum teprenone concentrations were determined and are shown in the following figure (see Figure 1). The maximum drug concentrations (Cmax) and the area under the plasma concentration curve (AUC0-32) are shown in the following table (see Table 2). There was no significant difference in Cmax or AUC0-32 between the 2 dosage forms. (See Figure 1 and Table 1.)

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Click on icon to see table/diagram/image

Effect of meal: Three capsules of SELBEX Capsules (150 mg of teprenone) were administered orally to eighteen healthy adult male volunteers at 30 min. 1 hr or 3 hr after a meal in a cross-over design. The plasma teprenone concentrations were determined and are shown in the following figure and table (see Figure 2 and Table 2). The area under the plasma concentration-time curve (AUC) at 30 min after a meal is comparable with that at 1 hr after a meal. The AUC at 3 hr after a meal was 23% lower than that at 30 min after a meal. (See Figure 2 and Table 2.)

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Click on icon to see table/diagram/image
Indications/Uses
Improvement of gastric mucosal lesions (erosion, hemorrhage, redness and edema) associated with the following diseases: acute gastritis and acute exacerbation of chronic gastritis.
Gastric ulcers.
Dosage/Direction for Use
The usual dose for adults is 50 mg (1 capsule) three times daily after meals (daily dose: 150 mg of teprenone). The dose should be adjusted according to the age of the patient and the severity of symptoms.
Overdosage
There is no experience to date with deliberate overdose.
No specific antidote is known.
Contraindications
Patients with a history of hypersensitivity to Teprenone.
Special Precautions
Use in Children: The safety in children has not been established (insufficient clinical experience).
Use in the Elderly: Since the elderly often have a physiological hypofunction, it is advisable to take measures, such as reduction in dosage under careful supervision.
Use In Pregnancy & Lactation
SELBEX should only be used for pregnant women or women suspected of being pregnant, if the expected therapeutic benefits are evaluated to outweigh the possible risk of treatment.
(The safety of SELBEX has not been established in pregnant women.)
Adverse Reactions
Adverse reactions were reported in 52 of 10,914 patients (0.48%). (At the end of the reexamination period.)
Clinically significant adverse reactions (incidence unknown): Hepatic function disorders and jaundice: Hepatic function disorders accompanied by elevation of AST (GOT), ALT (GPT), γ-GTP or Al-P, or jaundice may occur. In the event of such abnormal findings, administration should be discontinued and appropriate measures should be taken.
Other adverse reactions: (see Table 3).

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Drug Interactions
No any specific drug interaction has been reported.
Caution For Usage
Caution in handling over drug (capsules): For drugs that are dispensed in a 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 may puncture the esophageal mucosa, causing perforation and resulting in serious complications such as mediastinitis.]
Storage
SELBEX Capsules should be preserved at room temperature not exceeding 30°C.
ATC Classification
A02BX - Other drugs for peptic ulcer and gastro-oesophageal reflux disease (GORD) ; Used in the treatment of peptic ulcer and gastro-oesophageal reflux disease (GERD).
Presentation/Packing
Cap 50 mg (opaque grayish blue-green/light orange, debossed with
Click on icon to see table/diagram/image
, 14.3 mm in length, 160 mg in weight, size no. 4) x 3 x 10's.
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