SUMMARY PRODUCT INFORMATION 3 INDICATIONS AND CLINICAL USE 3 CONTRAINDICATIONS 4 WARNINGS AND PRECAUTIONS 4 ADVERSE REACTIONS 6 DRUG INTERACTIONS 6 DOSAGE AND ADMINISTRATION 8 OVERDOSAGE 9 ACTION AND CLINICAL PHARMACOLOGY 9 STORAGE AND STABILITY 10 DOSAGE FORMS, COMPOSITION AND PACKAGING 10

PART II: SCIENTIFIC INFORMATION 11

PART III: CONSUMER INFORMATION. 12

Buscopan(r) Hyoscine Butylbromide, Tablets Boehringer Ingelheim Standard, 10 mg Hyoscine Butylbromide Injection, 20 mg/mL

PART I: HEALTH PROFESSIONAL INFORMATION SUMMARY PRODUCT INFORMATION

INDICATIONS AND CLINICAL USE

BUSCOPAN (hyoscine butylbromide) tablets are indicated for:

The relief of smooth muscle spasm of the gastrointestinal and genitourinary systems.

BUSCOPAN ampoules are indicated for: The relief of acute genitourinary or gastrointestinal spasm (e.g., renal or biliary colic), or to produce smooth muscle relaxation prior to radiological procedures such as pyelography or other diagnostic procedures where spasm may be a problem (e.g., gastro-duodenal endoscopy).

Geriatrics:

No data is available

Pediatrics:

No data is available

CONTRAINDICATIONS

Hypersensitivity to hyoscine butylbromide, or atropinics (see WARNINGS AND PRECAUTIONS) or to any of the product excipients (See Dosage Forms, Composition and Packaging). BUSCOPAN (hyoscine butylbromide) tablets are contraindicated in patients with myasthenia gravis, megacolon, glaucoma or obstructive prostatic hypertrophy. Parenteral administration is contraindicated in patients with myasthenia gravis, untreated narrow angle glaucoma, prostatic hypertrophy with urinary retention, stenotic lesions of the gastrointestinal tract, tachycardia, angina, cardiac failure and megacolon. BUSCOPAN(r) ampoules should not be given by intramuscular injection to patients being treated with anticoagulant drugs since intramuscular haematoma may occur. In these patients, the subcutaneous or intravenous routes may be used.

WARNINGS AND PRECAUTIONS

Therapy should be discontinued if the patient reports any unusual visual disturbances or pressure pain within the eye. Patients intolerant of one belladonna alkaloid or derivative may also be intolerant of other belladonna alkaloids or derivatives such as hyoscine butylbromide. After parenteral administration of BUSCOPAN, cases of anaphylaxis, including episodes of shock have been observed. As with all drugs causing such reactions, patients receiving BUSCOPAN by injection should be kept under observation. BUSCOPAN (hyoscine butylbromide) tablets and ampoules should be used with caution in patients with prostatic enlargement. BUSCOPAN may precipitate or aggravate urinary retention in patients with the following conditions: nonobstructive prostatic hypertrophy, urinary retention (or the predisposition to) or obstructive uropathy such as a bladder neck obstruction due to prostatic hypertrophy (see CONTRAINDICATIONS). In addition, exercise caution in patients inclined to tachyarrhythmia. One sugar-coated tablet of 10 mg contains 41.2 mg sucrose, resulting in 411.8 mg sucrose per maximum recommended daily dose. Patients with the rare hereditary condition of fructose intolerance should not take this medicine.

As large doses of anticholinergics/systemic antispasmodics may cause an increase in heart rate, due care is necessary in patients with cardiac disease, especially cardiac arrhythmias, congestive heart failure, coronary artery disease and mitral stenosis. The increase in heart rate may also be undesirable in patients with unstable cardiovascular status in an acute hemorrhage situation.

Exercise caution in patients with reflux esophagitis or gastrointestinal tract obstructive disease (i.,e., achalasia and pyloroduodenal stenosis) due to the ability of anticholinergics/systemic antispasmodics to decrease smooth muscle motility and tone resulting in gastric retention. Anticholinergics may aggravate hiatal hernia associated with reflux esophagitis, myasthenia gravis or pyloric obstruction. In patients with ulcerative colitis, large anticholinergic doses may suppress intestinal motility, possibly causing paralytic ileus or resulting in obstruction; also, use may precipitate or aggravate toxic megacolon.

The parenteral administration of hyoscine butylbromide, particularly of higher doses, has been reported to cause transient disturbances of accommodation which recede spontaneously. Therefore, patients should be cautioned about potential visual problems and the need to exercise care while driving or operating machinery after receiving BUSCOPAN ampoules. The mydriatic effect of anticholinergics/systemic antispasmodics may result in increased intraocular pressure. BUSCOPAN should be used with caution in patients with angle-closure glaucoma or with this predisposition, as anticholinergics/systemic antispasmodics may precipitate an acute angle-closure glaucoma attack (see CONTRAINDICATIONS). Patients should seek urgent ophthamological advice in case they should develop a painful eye with loss of vision after injection of BUSCOPAN.

Pregnant Women:

Safety during pregnancy has not yet been established. Limited preclinical data has not indicated a hazard; nevertheless, the usual precautions regarding the use of drugs during pregnancy, especially during the first trimester, should be observed.

Nursing Women:

Safety during lactation has not been established. No specific studies have been conducted on the excretion of this drug in breast milk. The benefits of hyoscine butylbromide use during lactation should therefore be weighed against possible effects on the infant.

Pediatrics:

Geriatrics:

Geriatric patients are especially susceptible to the anticholinergic side effects of constipation, dryness of mouth and urinary retention (especially in males). If these side effects continue or are severe, discontinuation of medication should be considered. Due care is necessary when anticholinergics are administered to geriatric patients due to the danger of precipitating undiagnosed glaucoma. Administration of anticholinergics/systemic antispasmodics to elderly patients with intestinal atony or in debilitated patients may result in obstruction.

ADVERSE REACTIONS

Adverse Drug Reaction Overview

Many of the listed undesirable effects can be assigned to the anticholinergic properties of BUSCOPAN(r). Anticholinergic side effects of BUSCOPAN(r) are generally mild and self- limited. Accumulated clinical and postmarketing experience indicates that the following adverse reactions can be expected with the use of BUSCOPAN Ampoules and Tablets: Xerostomia (dry mouth), dyshidrosis, visual accomodation disorders, tachycardia, dyspnea, and urinary retention. There have been rare reports of dizziness, blood pressure decreased and flushing. Skin reactions and other hypersensitivity, angioedema and fixed drug eruptions have been reported rarely. There have been very rare reports of anaphylactic reactions and anaphylactic shock including fatal outcome. Adverse events reported during therapy with BUSCOPAN include increased pulse rate, diarrhea, nausea, retinal pigmentation, and glaucoma.

DRUG INTERACTIONS

As hyoscine butylbromide can reduce the motility and secretory activity of the gastrointestinal system, the systemic absorption and pharmacologic effects of other oral medications may be delayed.

DOSAGE AND ADMINISTRATION

Individual response to BUSCOPAN (hyoscine butylbromide) may vary and doses should be adjusted accordingly.

Tablets: One to two 10 mg tablets per day up to a maximum of 6 tablets per day. In prolonged illness which requires repeated dosing, 1 tablet 3 to 5 times a day is recommended. Ampoules: One half (10 mg/0.5mL) to one ampoule (20 mg/1mL) administered parenterally by intramuscular, subcutaneous, or intravenous routes, at an injection rate of 1 mL/min. No dilution of the ampoule is necessary prior to administration. The maximum dose should not exceed 100 mg/day (5 ampoules).

In case a dose has been missed, take the next dose as scheduled. Do not double the dose.

Tablets should be swallowed whole with a glass of water. The rapid action of injected BUSCOPAN is advantageous in acutely ill patients and in those situations where prompt spasmolytic activity facilitates diagnostic procedures such as radiological examinations. BUSCOPAN ampoules may also be used intramuscularly 10-15 minutes before radiological examinations of the stomach to slow peristaltic movements.

Dilution and Stability of Parenteral BUSCOPAN:

Although dilution prior to administration is not required, BUSCOPAN solution is compatible with the following solutions, should dilution be desirable: Ringers Solution Ringers Lactate NaCl 0.9% Laevulose 5% Glucose 10% Solutions must be mixed under sterile conditions and are stable for 8 hours.

OVERDOSAGE

Single oral doses of up to 590 mg and quantities of active drug up to 1090 mg within 5 hours have produced dry mouth, tachycardia, slight drowsiness and transient visual disorders. Other symptoms include urinary retention, reddening of the skin, and inhibition of gastrointestinal motility. Other symptoms which occurred in animals and which may be encountered in humans include: shock, Cheyne-Stokes respiration, respiratory paralysis, clonic spasms, paresis of the striated muscle, coma, paralytic ileus and cystoparalysis.

In the case of an oral overdose, perform gastric lavage with activated charcoal followed by magnesium sulfate (15%). BUSCOPAN overdose symptoms respond to parasympathomimetics. For patients with glaucoma, administer pilocarpine locally. If necessary, parasypathomimetics should be administered, e.g. neostigmine 0.5-2.5 mg i.m. or i.v.. Cardiovascular complications should be treated according to usual therapeutic principles. In case of respiratiory paralysis: intubation, artificial respiration. Catheterisation may be required for urinary retention. Other overdosage symptoms should be treated with standard supportive therapy.

ACTION AND CLINICAL PHARMACOLOGY

BUSCOPAN (hyoscine butylbromide) is an antispasmodic agent which relaxes the smooth muscle of the gastrointestinal, biliary and urinary tracts. It is believed to act predominantly at the parasympathetic ganglia in the walls of the viscera of these organs. Structurally, BUSCOPAN exists as a quaternary ammonium compound and as a single positively charged cation throughout the entire pH range.

Absorption:

BUSCOPAN undergoes rapid tissue absorption after oral administration. In the rat, it concentrates in the gastrointestinal tract, liver and kidney tissues.

Distribution: .

The high tissue affinity of the substance is further reflected in the extremely short distribution half-life (t1/2a) in the plasma of approximately 2-3 minutes. Despite low systemic bioavailability, hyoscine butylbromide remains available in high concentrations at the site of action. Plasma levels of radioactivity in man peak within 3 hours of enteral administration

Metabolism:

Protein binding in the human plasma occurs at 8-13% and in a 4.4% human serum albumin solution at 3-11%. Hyoscine butylbromide does not readily cross the blood brain barrier.

Excretion: A high portion of the absorbed hyoscine butylbromide (14C) undergoes elimination in an unchanged form within the first few hours of administration in man and animals. Later in elimination, the metabolized portion predominates. In man, following the administration of intravenous 14C-labelled substance, the elimination followed a three-phase course: t1/2a = 3.5 min., t1/2b = 0.8 hours; t1/2 = 14.0 hours. Following oral administration, the terminal elimination half-life is 4.8 hours. Metabolites from rat urine detected in quantities ranging from 4 to 44% include three main metabolites (phenyl acetic acid-scopine ester-butochloride, 4-hydroxytropic acid-scopine ester-butochloride, scopine butobromide) and four minor metabolites (including AD 12 and Ba 790).

STORAGE AND STABILITY

BUSCOPAN tablets and ampoules should be protected from light and heat. BUSCOPAN ampoules should be protected from freezing. Products should be stored at room temperature and are stable up to the expiration date indicated on the label.

DOSAGE FORMS, COMPOSITION AND PACKAGING

Tablets: Round, white, sugar-coated tablets each containing 10 mg of hyoscine butylbromide. Ampoules: Containing 20 mg of hyoscine butylbromide in 1 mL aqueous solution.

Tablets: hyoscine-N-butylbromide. Non-medicinal ingredients include acacia, carnauba wax, castor oil, lactose, magnesium stearate, maize starch, sucrose, polyethylene glycol, shellac, talc, tartaric acid, titanium dioxide, and white wax. Ampoules: hyoscine-N-butylbromide. Non-medicinal ingredients include sodium chloride and water for injection.

PHARMACEUTICAL INFORMATION

Drug Substance

Proper name: hyoscine butylbromide Chemical name: (1S,3S,5R,6R,7S)-8-Butyl-6,7-epoxy-3-[(S)-tropoyloxy] tropanium bromide Molecular formula and molecular mass: C21H30BrNO4, 440.4 Physicochemical properties: A white or almost white, odourless or almost odourless, powder, soluble 1 to 1 in water, 1 in 50 of alcohol, and 1 in 5 of chloroform. 10% solution in water has a pH of 5.5 to 6.5.

This leaflet is part III of a three-part "Product Monograph" published when BUSCOPAN was approved for sale in Canada and is designed specifically for Consumers. This leaflet is a summary and will not tell you everything about BUSCOPAN. Contact your doctor or pharmacist if you have any questions

BUSCOPAN ampoules are used for relief of acute genitourinary or gastrointestinal spasm, or to produce smooth muscle relaxation prior to radiological procedures where spasm may be a problem.

Stomach cramps are caused by sudden, irregular tightening up of muscles in the wall of the intestine. BUSCOPAN works by

You have myasthenia gravis (a muscle wasting disease) untreated narrow angle glaucoma or obstructive prostatic hypertrophy (enlarged and blocked prostate).

You have myasthenia gravis, untreated narrow angle glaucoma, difficulty in urination due to inflammation of the prostate, stenotic lesions (narrowing of a duct/canal) of the gastrointestinal tract, tachycardia (fast heartbeat), angina, heart failure and megacolon (enlarged colon).

Tablets: acacia, carnauba wax, castor oil, lactose, magnesium stearate, maize starch, sucrose, polyethylene glycol, shellac, talc,

you are hypersensitive or "allergic" to hyoscine-N- butylbromide or any of the other ingredients

antihistamines, antivirals, dopamine antagonists (e.g. metoclopramide) or medicines to treat heart problems

Exercise care in driving or operating machinery until you know how Buscopan may affect your vision.

Drugs that may interact with BUSCOPAN include: tricyclic antidepressants, antihistamines, quinidine, disopyramide, amantadine, MAO inhibitors, anticholinergics, dopamine antagonists such as metoclopramide, beta-adrenergic agents, antacids or adsorbent antidiarrheals.

Tablets: One to two 10 mg tablets per day up to a maximum of 6 tablets per day. In prolonged illness, which requires repeated

dosing, one tablet 3 to 5 times a day is recommended. Swallow tablets whole with a glass of water.

Ampoules: One half (10 mg/0.5 mL) to one ampoule (20 mg/mL) administered parenterally by intramuscular, subcutaneous, or intravenous routes, at an injection rate of 1 mL/min. No dilutions of the ampoule is necessary prior to administration. The maximum dose should not exceed 100 mg/day (5 ampoules).

listed below may be observed. In this situation, a doctor must be consulted or the Poison Control Center should be contacted immediately.

Your doctor will advise you that certain antacids or adsorbent antidiarrheals should be taken at least one hour before Buscopan.

To monitor drug safety, Health Canada collects information on serious and unexpected effects of drugs . If you suspect you have had a serious or unexpected reaction to this drug you may notify Health Canada by:

All medicines sometimes cause side-effects. BUSCOPAN may occasionally cause a dry mouth, blurred vision, diarrhea, nausea,

Other possible rare side-effects include, dizziness, flushing, allergic reactions (particularly skin rash and itching) and difficulty in breathing (usually in patients who suffer with asthma or allergy).

If you experience any of these effects and they persist or become troublesome, consult your doctor.

Should you suffer from a painful red eye with loss of vision, seek urgent medical advice.

If you experience any other effects not mentioned above, consult your doctor or pharmacist.

This is not a complete list of side effects. For any unexpected effects while taking BUSCOPAN, contact your doctor or pharmacist.

NOTE: Before contacting Health Canada, you should contact your physician or pharmacist.

This document plus the Prescribing Information, prepared for health professionals can be found at:

This leaflet was prepared by Boehringer Ingelheim (Canada) Ltd. Last revised: April 30, 2008

BUSCOPAN ampoules should be protected from freezing. Products should be stored at room temperature and are stable up to

Route of Administration	Dosage Form / Strength	Clinically Relevant Nonmedicinal Ingredients
Oral Parenteral	Tablets, 10 mg Ampoules, 20 mg/mL	acacia, carnauba wax, castor oil, lactose, magnesium stearate, maize starch, sucrose, polyethylene glycol, shellac, talc, tartaric acid, titanium dioxide, and white wax sodium chloride and water for injection

Hyoscine Butylbromide	Effect	Clinical comment
Tricyclic antidepressants	Can potentiate the anticholinergic effect of parenterally administered hyoscine butylbromide .
Antihistamines	Can potentiate the anticholinergic effect of parenterally administered hyoscine butylbromide .
Quinidine	Can potentiate the anticholinergic effect of parenterally administered hyoscine butylbromide .
Disopyramide	Can potentiate the anticholinergic effect of parenterally administered hyoscine butylbromide .
Amantadine	Can potentiate the anticholinergic effect of parenterally administered hyoscine butylbromide .
MAO inhibitors	May result in intensified anticholinergic side effects of hyoscine butylbromide. Also, may block detoxification of anticholinergics thus potentiating their action.
Anticholinergics	May intensify anticholinergic effects. May increase the severity of potassium chloride induced gastrointestinal lesions.
Dopamine antagonists such as metoclopramide.	May result in diminution of the effects of both drugs on the gastrointestinal tract.
Beta-adrenergic agents	May enhanced tachycardic effects.
Antacids or adsorbent antidiarrheals	May reduce the absorption of anticholinergics, resulting in decreased therapeutic effectiveness.	Anticholinergics such as hyoscine butylbromide should be given at least one hour before these medications.

Submission Control Number: 121001

PART I: HEALTH PROFESSIONAL INFORMATION 3

PART II: SCIENTIFIC INFORMATION 11

PART III: CONSUMER INFORMATION. 12

PART I: HEALTH PROFESSIONAL INFORMATION SUMMARY PRODUCT INFORMATION

INDICATIONS AND CLINICAL USE

Geriatrics:

Pediatrics:

CONTRAINDICATIONS

WARNINGS AND PRECAUTIONS

Pregnant Women:

Nursing Women:

Pediatrics:

Geriatrics:

ADVERSE REACTIONS

DRUG INTERACTIONS

DOSAGE AND ADMINISTRATION

Dilution and Stability of Parenteral BUSCOPAN:

OVERDOSAGE

ACTION AND CLINICAL PHARMACOLOGY

Absorption:

Distribution: .

Metabolism:

STORAGE AND STABILITY

DOSAGE FORMS, COMPOSITION AND PACKAGING

PHARMACEUTICAL INFORMATION

Drug Substance