Coliopan

Coliopan

Manufacturer:

Eisai

Distributor:

DKSH
Full Prescribing Info
Contents
Butropium bromide.
Description
Each tablet of Coliopan contains 5mg of Butropium bromide.
Physico-chemical Properties of Active Ingredients:
Generic name: Butropium bromide.
Chemical name: 8-( p-butoxybenzy l)-3α-hydroxy-lα H , 5α H-tropanium bromide(-)-tropate.
Molecular formula: C28H38BrNO4.
Molecular weight: 532.52.
Butropium bromide occurs as a white crystal or crystalline powder with a bitter taste. It is freely soluble in methanol, formic acid and glacial acetic acid, soluble in chloroform and dimethylformamide, sparingly soluble in ethanol, slightly soluble in water and practically insoluble in acetone, either and acetic anhydride.
Action
Coliopan a hyoscyarnine derivative originally developed by Eisai Research Laboratories is a parasympatbolytic agent. Coliopan possesses antispasmodic action on smooth muscle, acts to inhibit gastric secretion and has anti-ulcer effects. Coliopan is also reported lo act to normalize gastric emptying and to increase blood flow in gastric mucosa. Double blind controlled clinical trials have proven its effectiveness in relieving spasmodic pain associated with gastrointestinal disorders and peptic ulcers.
Pharmacology:
Pharmacodynamics: Inhibition of gastrointestinal motility: Butropium bromide reduces the tone and motility of parasympathetically innervated smooth muscle of the gastrointestinal tract by acting on the acethylcholine receptors as the nerve endings. Experiments on the isolated jejunum of rabbits, the isolated proximal colon of mice, and the isolated gallbladder of guinea pigs indicate that butropium bromide is more effective than atropine in inhibiting the motility of smooth muscle. In experiments with the isolated ileum of mice, Butropium bromide exhibited a papaverine like action. In clinical studies, Butropium administered into the duodenum decreased the intestinal motility within 15 minutes after administration.
Anti-ulcer effect: Butropium bromide administered orally to rats decreased incidence of pyloric ligation-induces ulceration. Specific experimental observations from these experiments include an increase in intragastric pH, a reduction in the volume of gastric juice, a lower total acidity and suppression of pepsin secretion. In rats pretreated orally with Butropium bromide is considered to be as potent as that of atropine.
Inhibition of Gastric Secretion: The oral administration of Coliopan was found to significantly inhibit gastric secretion in healthy men.
Normalization of Gastric Secretion: Clinical studies have shown that Butropium bromide normalizes delayed or accelerated gastric emptying in patients with digestive ulcers. In general, high doses of Butropium bromide normalize gastric emptying by accelerating that which is delayed and delaying that which is accelerated.
Clinical Studies: Clinical Effects: Double-blind controlled studies have shown Coliopan to be effective and symptomatic relief of spasmodic pain. Relief of abdominal pain began in an average of 39 minutes after oral administration of 10mg Coliopan, and this effect was sustained for 24 minutes.
Adverse Reactions: In a survey 2,057 patients treated orally with Coliopan, adverse effects were reported for 189 patients (9.19%). The most common untoward effects were dryness of the mouth (121 patients: 5.88%), constipation (19 patients: 0.92%), impaired ocular accomodation (10 patients: 0.49%), tachycardia (10 patients: 0.49%) and urinary retention (10 patients: 0.49%).
Animal Studies: Absorption, Distribution and Excretion: Oral doses of 3mg/kg of 3H-labelled butoxybenzyl hyoscyamine bromide were administered to rats and guinea pigs. Peak plasma concentration of 0.012g/mL and 0.013g/mL, respectively, occured 1 hour after administration and gradually declined there after. Tissue distributor in animal models showed that radioactivity was high in the gut and stomach, and secondly in the liver and kidneys. No radioactivity was detected in the brain. Compared with guinea pigs, radioactivity in the pancreas and adrenal glands was markedly higher in rats.
The radioactivity in the tissues of rats and guinea pigs disappeared within 3 to 11 days after administration. Approximately 1% of the administered radioactivity was excreted in the urine and 98 to 99% was excreted during the first 5 days after oral administration.
Acute Toxicity (LD 30mg/kg): (See table).

Click on icon to see table/diagram/image

Subacute Toxicity: Butropium bromide was administered orally in doses of 63, 125, 250 and 500mg/kg/day to male and female rats for 5 consecutive weeks. Butropium bromide was well tolerated and no abnormal findings were noted in body weight, organ weights, blood and urinary tests and pathological examination. Mydriasis and sluggish movements, however, were observed at the doses greater than 125mg/kg/day.
Chronic Toxicity: Male and female rats given 6, 125, 100 and 400 mg/kg/day of Butropium bromide orally for 25 consecutive weeks showed no sign of toxicity, with the exception that mydriasis and sluggish movements were observed in some animals receiving a daily dose of 100mg/kg.
Reproduction Toxicity: Butropium bromide, administered orally in doses of 60, 240 and 500mg/kg/day to pregnant mice and rats during organogenesis, caused a decrease in weight gain or death in some mice receiving the higher doses of 240 or 500mg/kg/day dose, and death in some rats at highest dose level. Neither an increase in fetal resorption nor dysmorphologic effects were induced, although a decrease in the mean fetal weight and retarded ossification were noted in the live fetuses form the late stage of gestation. Postnatal growth was not effected.
Indications/Uses
Spasmodic pains associated with gastritis, enteritis, gastric ulcer, cholelithiasis and cholecystopathy (including cholecystitis, cholecystic and biliary dyskinesia).
Dosage/Direction for Use
Adults: 2 tablets 3 times daily (30 mg of Butropium bromide) per oral. The dose should be adjusted according to the age of patient and severity of symptoms.
Contraindications
Coliopan is contraindicated in patients with glaucoma, impaired urination due to prostatomegaly severe heart disease, paralytic ileus pyloric stenosis or a history of hypersensitivity to Coliopan.
Special Precautions
Coliopan should be used with caution in patients with prostatomegaly, congestive heart failure, arrhythmia, ulcerative colitis (possibility of inducing toxic megacolon colitis), or hyperthyroidism.
Cautions should be taken when administering Coliopan to patients where the environmental temperature is high.
Coliopan may produce impaired visual accommodation, drowsiness or dizziness; patients should be warned against engaging in occupations or activities requiring alertness such as driving a vehicle or operating hazardous machinery.
Use in children: Safe use of Coliopan in children has not yet been established. (Adequate clinical use has not yet been performed.)
Use In Pregnancy & Lactation
Use in Pregnancy: Safe use of Coliopan during pregnancy has not yet been established. The drug should be administered to patients who are pregnant or are suspected to be pregnant only if the expected therapeutic benefit is thought to outweigh any possible risk.
Adverse Reactions
Eyes: Symptoms of impaired ocular accommodation may occasionally occur.
Gastrointestinal: Dryness of the mouth, nausea, vomiting or constipation may occasionally occur.
Genito-urinary: Impaired urination may occasionally result.
Psychoneurotic: Symptoms such as headache, drowsiness or dizziness may occasionally occur.
Cardiovascular: Tachycardia or hypotension may occasionally occur.
Hypersensitivity: Hypersensitivity reactions such as skin rash may occur in rare cases, the medication should be discontinued if such signs develop.
Others:
Flushing or redness of the face or unusual tiredness may occasionally occur.
Drug Interactions
Concurrent use of the following drugs may intensify actions of Coliopan: Tricyclic antidepressants, Phenothiazines, Monoamine oxidase (MAO) inhibitors, Antihistamines.
Storage
Store below 30 degree celcius.
Coliopan tablets should be protected from moisture.
MIMS Class
ATC Classification
A03BB - Belladonna alkaloids, semisynthetic, quaternary ammonium compounds ; Used in the treatment of functional gastrointestinal disorders.
Presentation/Packing
Tab 5 mg (hard white, odorless with a bitter taste) x 180's.
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