For the treatment of mild to moderate spasm of the gastrointestinal tract and for the treatment of spas- modic abdominal pain in irritable bowel syndrome

Posology:
Adults and children aged 6 years and over: 1 - 2 tablets 3 times daily
(Single dose: 10 - 20 mg hyoscine butylbromide; maximum daily dose: 60 mg hyoscine butylbromide)
The package leaflet informs patients that Buscopan sugar-coated tablets should not be taken for more than 5 days unless the cause of the symptoms has been medically investigated.
Method of administration: Oral use
The tablets should be swallowed whole with sufficient liquid.

• Hypersensitivity to the active substance or to any of the excipients listed in section 6.1 • Mechanical stenosis of the gastrointestinal tract • Megacolon • Paralytical or obstructive ileus • Urinary retention with subvesical obstruction (e.g. benign prostatic hyperplasia) • Narrow-angle glaucoma • Tachycardia and tachyarrhythmia • Myasthenia gravis

Medical advice should be sought immediately if severe abdominal pain persists or worsens, or occurs in conjunction with symptoms such as fever, nausea, vomiting, changes in intestinal motility, abdomi- nal tenderness, decreased blood pressure, fainting or blood in the stools.
This medicine contains sucrose (approx. 41 mg per tablet). Patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency should not take Buscopan sugar-coated tablets.
Buscopan should be used with caution in conditions characterised by tachycardia such as thyrotoxicosis, cardiac insufficiency or failure and in cardiac surgery where it may further accelerate the heart rate. Due to the risk of anticholinergic complications, caution should be used in patients susceptible to intestinal or urinary outlet obstructions.
Because of the possibility that anticholinergics may reduce sweating, Buscopan should be administered with caution to patients with pyrexia.
Elevation of intraocular pressure may be produced by the administration of anticholinergic agents such as Buscopan in patients with undiagnosed and therefore untreated narrow angle glaucoma. Therefore, patients should seek urgent ophthalmological advice in case they should develop a painful, red eye with loss of vision whilst or after taking Buscopan.

Buscopan may enhance the anticholinergic effects of other anticholinergics (such as tiotropium, ipra- tropium and atropine-like compounds), amantadine, tricyclic and tetracyclic antidepressants, quinidi- ne, antihistamines, antipsychotics, disopyramide and other drugs, as well as the tachycardic effect of
β-adrenergic agents.
Coadministration of Buscopan with dopamine antagonists such as metoclopramide may result in a re- duction of the effect of both drugs on gastrointestinal motility.

Pregnancy:
There has been very limited or no experience to date with the use of hyoscine butylbromide in preg- nant women. Animal studies are insufficient with respect to reproductive toxicity (see section 5.3). As a precaution, the use of Buscopan sugar-coated tablets should be avoided during pregnancy.
Lactation:
Anticholinergics may inhibit lactation. It is not known whether hyoscine butylbromide or its metabo- lites are excreted in breast milk. Newborns have shown an increased response to some anticholinerg- ics. A risk to the newborns/infants cannot be excluded.
A decision must be made whether to discontinue breast-feeding or to discontinue/abstain from therapy with Buscopan sugar-coated tablets taking into account the benefit of breast-feeding for the child and the benefit of therapy for the woman.
Fertility:
No studies on the effects on human fertility have been conducted (see section 5.3).

No studies on the effects on the ability to drive and use machines have been performed.
No impairment would normally be expected to occur in patients taking Buscopan sugar-coated tablets at the intended dose. However, if symptoms such as tiredness, dizziness or near-vision impairment oc- cur, the ability to drive and use machines may be impaired.

Many of the known undesirable effects are due to the anticholinergic properties of Buscopan. These anticholinergic effects are generally mild and self-limiting.
The following categories are used to rank the undesirable effects by frequency of occurrence:

Very common	≥ 1/10
Common	≥ 1/100 - < 1/10
Uncommon	≥ 1/1000 - < 1/100
Rare	≥ 1/10,000 - < 1/1000
Very rare	< 1/10,000
Not known	Frequency cannot be estimated from the available data

Immune system disorders
Uncommon: Skin reactions (such as urticaria and pruritus)
Not known: Hypersensitivity reactions, dyspnoea, anaphylactic reactions, anaphylactic shock with flushing and decreased blood pressure, rash, cutaneous erythema
Cardiac disorders
Uncommon: Tachycardia
Vascular disorders
Uncommon: Decreased blood pressure, dizziness
Eye disorders
Very rare: Accommodation disturbances, especially in hypermetropic patients whose defect has not been adequately corrected; acute glaucoma attack
Gastrointestinal disorders
Uncommon: Dry mouth (reduced salivary secretion), diarrhoea, nausea, vomiting, gastric discomfort
Skin and subcutaneous tissue disorders
Uncommon: Dry skin (reduced sweating)
Renal and urinary disorders
Rare: Micturition difficulties (such as urinary retention and dysuria)
General disorders
Uncommon: Tiredness
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It al- lows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professi- onals are asked to report any suspected adverse reactions to the national pharmacovigilance and drug safety center (NPC).
To report any side effect(s):
• Saudi Arabia:
− The National Pharmacovigilance and Drug Safety Centre (NPC)
o Fax: +966-11-205-7662
o Call NPC at +966-11-2038222, Exts: 2317-2356-2353-2354-2334-2340.
o Toll free phone: 8002490000
o Calling: 19999
o E-mail: npc.drug@sfda.gov.sa
o Website: www.sfda.gov.sa/npc

• Other GCC States:

− Please contact the relevant competent authority.

Symptoms
Signs of poisoning following acute overdose have not been observed in man to date.
Overdose is likely to give rise to anticholinergic symptoms such as visual disturbances, tachycardia, dry mouth, urinary retention and cutaneous erythema.

In animal studies, ataxia, tremor, convulsions, dyspnoea and anticholinergic effects (mydriasis, muc- osal dryness, tachycardia and reduced gastrointestinal motility with accumulation of food in the stom- ach and intestine) occurred following extremely high doses. Death occurred as a result of respiratory paralysis.
Treatment
As there are no known cases of Buscopan poisoning to date, the measures listed below are based on theoretical considerations:
In the event of oral poisoning, gastrointestinal decontamination is indicated. For patients with glauc- oma, topical pilocarpine should be administered and an ophthalmologist should be consulted immedi- ately. Patients with urinary retention should be catheterised.
If necessary, parasympathomimetic agents should be given (neostigmine 0.5 - 2.5 mg i.m. or i.v.). Ca- rdiovascular complications should be treated according to usual therapeutic principles. Intubation and artificial respiration are required in cases of respiratory paralysis.

Pharmacotherapeutic group: Antispasmodics ATC code: A03BB01
Hyoscine butylbromide is a semi-synthetic derivative of scopolamine, a naturally-occurring substance of plant origin. As a quaternary ammonium compound, hyoscine butylbromide does not enter the cen- tral nervous system on systemic administration. It does, however, have peripheral anticholinergic eff- ects, which are due to both inhibition of ganglionic transmission and inhibition of muscarinic receptors in smooth muscle cells.
Hyoscine butylbromide administered orally or rectally reduces smooth muscle tone in the gastrointes- tinal tract and thus exerts an antispasmodic effect.
The clinically proven efficacy of the drug in spasmodic abdominal pain is due to its specific local eff- ect on nicotinic and muscarinic acetylcholine receptors in the muscle layer of the gastrointestinal tract.

Absorption
Because of its quaternary nitrogen atom, hyoscine butylbromide is only absorbed to a limited extent following oral and rectal administration. The median absolute bioavailability of 100 mg hyoscine bu- tylbromide (administered as e.g. film-coated tablets, suppositories or drops) is less than 1%. Findings from animal studies suggest that the effects of orally and rectally administered hyoscine butylbromide are due to a specific local action.
Distribution
Hyoscine butylbromide has a high affinity for muscarinic and nicotinic acetylcholine receptors and, following parenteral administration, it is predominantly distributed in the smooth muscle cells and in- tramural ganglia of the abdominal and pelvic organs. Plasma protein binding is approximately 4.4%. It has been shown in animal studies that hyoscine butylbromide does not cross the blood-brain barrier, although no clinical data to this effect are available. Hyoscine butylbromide interacts weakly with the choline transport system in cultured epithelial cells of the human placenta (Ki = 0.63 mM/L).
Metabolism and elimination

Following oral administration of single doses between 100 and 400 mg, the terminal elimination half- lives ranged from 6.2 to 10.6 hours. The main metabolic pathway for hyoscine butylbromide is hydro- lytic cleavage of the ester bond. Orally administered hyoscine butylbromide is excreted in the faeces and the urine. Following oral administration, approximately 90% of radioactivity was recovered in the faeces; recovery of radioactivity in the urine was variable depending on the route of administration but did not exceed 5%. Mean clearance values after oral doses of 100 to 400 mg ranged from 881 to 1420 L/min, whilst the volumes of distribution after these doses were between 6.13 and 11.3 x 105 L (presu- mably due to low systemic availability). The metabolites excreted in the urine have a low affinity for muscarinic receptors and therefore probably do not contribute to the effect of the drug.

Acute and chronic toxicity
Acute and chronic toxicity studies did not show any effects relevant to the therapeutic use of hyoscine butylbromide. The NOAEL following oral administration in a 39-week toxicity study in dogs was 30 mg/kg.
Mutagenic and tumorigenic potential
Hyoscine butylbromide showed no mutagenic or clastogenic properties in the Ames test, in an in-vitro gene mutation assay in V79 cells or in an in-vitro chromosome aberration test in human lymphocytes. In vivo, the drug was not genotoxic in the rat bone marrow micronucleus assay.
No long-term animal studies investigating tumorigenic potential have been performed.
However, no evidence of tumorigenic potential was seen in two chronic toxicity studies carried out in rats over 26 weeks at doses of up 1000 mg/kg.
Reproductive toxicity
Hyoscine butylbromide did not show any teratogenic effects in embryotoxicity studies in rats and rab- bits. Fertility was not impaired in rats. No studies on pre- or postnatal development have been carried out with hyoscine butylbromide.

Sucrose, calcium hydrogen phosphate, maize starch, talc, colloidal anhydrous silica, acacia, povidone, tartaric acid (Ph. Eur.), stearic acid, macrogol 6000, carnauba wax, white beeswax, titanium dioxide (E 171)

Not applicable

3 years Medicines must not be used after the expiry date.

Store below 30ºC.

Sealed PVC/aluminium blister packs
Original pack containing 20 sugar-coated tablets Original pack containing 50 sugar-coated tablets Hospital pack containing 500 sugar-coated tablets
Not all pack sizes may available in your country.

No special requirements