1.
Name of the Medicinal Product
HYOSCINE BUTYLBROMIDE INJECTION BP
1.1. Strength
20 mg/ml
1.2 Pharmaceutical Dosage Form
Liquid Injection
1. Qualitative And Quantitative Composition
Qualitative Declaration
Hyoscine Butylbromide Injection BP contains Hyoscine Butylbromide BP.
Quantitative Declaration
Each ml contains:
Hyoscine Butylbromide BP 20 mg
Water for Injections BP q.s
3. Pharmaceutical Form
Liquid Injection
4. Clinical Particulars
4.1 Therapeutic Indications
Hyoscine Butylbromide Injections are indicated in acute spasm, as in renal or biliary colic, in
radiology for differential diagnosis of obstruction and to reduce spasm and pain in pyelography,
and in other diagnostic procedures where spasm may be a problem, e.g. gastro-duodenal
endoscopy.
4.2 Posology and Method of Administration
Adults:
One ampoule (20 mg) intramuscularly or intravenously, repeated after half an hour if necessary.
Intravenous injection should be performed 'slowly' (in rare cases a marked drop in blood
pressure and even shock may be produced by Hyoscine). When used in endoscopy this dose
may need to be repeated more frequently.
Maximum daily dose of 100mg.
Special populations
Elderly: No specific information on the use of this product in the elderly is available. Clinical
trials have included patients over 65 years and no adverse reactions specific to this age group
have been reported.
Summary of Product Characteristics
Paediatric population
Not recommended for children.
Hyoscine Butylbromide Injection should not be taken on a continuous daily basis or for
extended periods without investigating the cause of abdominal pain.
Dosage: For IM/IV use only.
4.3 Contraindications
Hyoscine Butylbromide injections are contraindicated in patients with:
Hypersensitivity to the active substance or to any of the excipients
Narrow angle glaucoma
Hypertrophy of the prostate with urinary retention
Mechanical stenosis in the gastrointestinal tract
Paralytical or obstructive ileus
Megacolon
Tachycardia
Myasthenia gravis
Hyoscine Butylbromide injections should not be given by intramuscular injection to patients
being treated with anticoagulant drugs since intramuscular haematoma may occur.
4.4 Special Warning and Precautions for Use
In case severe, unexplained abdominal pain persists or worsens, or occurs together with
symptoms like fever, nausea, vomiting, changes in bowel movements, abdominal tenderness,
decreased blood pressure, fainting, or blood in stool, appropriate diagnostic measures are
needed to investigate the aetiology of the symptoms.
Hyoscine Butylbromide injections can cause tachycardia, hypotension and anaphylaxis,
therefore use with caution in patients with cardiac conditions such as cardiac failure, coronary
heart disease, cardiac arrhythmia or hypertension, and in cardiac surgery. Monitoring of these
patients is advised.
Because of the possibility that anticholinergics may reduce sweating, Hyoscine Butylbromide
injections should be administered with caution to patients with pyrexia.
Elevation of intraocular pressure may be produced by the administration of anticholinergic
agents such as Hyoscine Butylbromide injection 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 after the injection of
Hyoscine Butylbromide injections.
Summary of Product Characteristics
4.5 Interaction with Other Medicinal Products and Other Forms of Interaction
The anticholinergic effect of drugs such as tri- and tetracyclic antidepressants, antihistamines,
quinidine, amantadine, antipsychotics (e.g. phenothiazines, butyrophenones), disopyramide and
other anticholinergics (e.g. tiotropium, ipratropium, atropine-like compounds) may be
intensified by Hyoscine Butylbromide injections.
The tachycardic effects of beta-adrenergic agents may be enhanced by Hyoscine Butylbromide
injections.
Concomitant treatment with dopamine antagonists such as metoclopramide may result in
diminution of the effects of both drugs on the gastrointestinal tract
4.6 Fertility, pregnancy and lactation
Pregnancy
There are limited data from the use of hyoscine butylbromide in pregnant women. Animal
studies are insufficient with respect to reproductive toxicity. As a precautionary measure
Hyoscine Butylbromide is not recommended during pregnancy.
Lactation
There is insufficient information on the excretion of hyoscine butylbromide and its metabolites
in human milk. A risk to the breastfeeding child cannot be excluded. Use of hyoscine
butylbromide during breastfeeding is not recommended.
Fertility
No studies on the effects on human fertility have been conducted.
4.7 Effects on Ability to Drive and Use Machines
No studies on the effects on the ability to drive and use machines have been performed.
However, patients should be advised that they may experience undesirable effects such as
accommodation disorder or dizziness during treatment with hyoscine butylbromide ampoules.
Therefore, caution should be recommended when driving a car or operating machinery. If
patients experience accommodation disorder or dizziness, they should avoid potentially
hazardous tasks such as driving or operating machinery.
4.8 Undesirable Effects
Many of the listed undesirable effects can be assigned to the anticholinergic properties of
hyoscine butylbromide.
Adverse events have been ranked under headings of frequency using the following convention:
Very common ≥ 1/10
Common ≥ 1/100, < 1/10
Summary of Product Characteristics
Uncommon ≥ 1/1,000, <1/100
Rare ≥ 1/10,000, <1/1,000
Very rare <1/10,000
Not known cannot be estimated from the available data
Immune system disorders
Not known*: anaphylactic shock including cases with fatal outcome, anaphylactic reactions,
dyspnoea, skin reactions (e.g. urticaria, rash, erythema, pruritus) and other hypersensitivity.
Cardiac disorders
Common: tachycardia
Vascular disorders
Common: dizziness
Not known*: blood pressure decreased, flushing
Gastrointestinal disorders
Common: dry mouth
Constipation
Skin and subcutaneous tissue disorders
Not known*: dyshidrosis
Renal and urinary disorders
Not known*: urinary retention
*This adverse reaction has been observed in post-marketing experience. With 95% certainty,
the frequency category is not greater than common, but might be lower. A precise frequency
estimation is not possible as the adverse drug reaction did not occur in a clinical trial database
of 185 patients.
4.9 Overdose
Symptoms
Serious signs of poisoning following acute overdosage have not been observed in man. In the
case of overdosage, anticholinergic symptoms such as urinary retention, dry mouth, reddening
of the skin, tachycardia, inhibition of gastrointestinal motility and transient visual disturbances
may occur, and Cheynes-Stokes respiration has been reported.
Therapy
Summary of Product Characteristics
Symptoms of Hyoscine Butylbromide injection overdosage respond to parasympathomimetics.
For patients with glaucoma, pilocarpine should be given locally. Cardiovascular complications
should be treated according to usual therapeutic principles. In case of respiratory paralysis:
intubation, artificial respiration should be considered. Catheterisation may be required for
urinary retention.
5.0 Pharmacological Properties
5.1 Pharmacodynamic properties
Hyoscine butylbromide is an antispasmodic agent which relaxes smooth muscle of the organs of
the abdominal and pelvic cavities. It is believed to act predominantly on the intramural
parasympathetic ganglia of these organs
5.2 Pharmacokinetic properties
Absorption and distribution
After intravenous administration hyoscine butylbromide is rapidly distributed (t½α= 4 min, t½β=
29 min) into the tissues. The volume of distribution (Vss) is 128 L (corresponding to approx.
1.7 L/kg). Because of its high affinity for muscarinic receptors and nicotinic receptors, hyoscine
butylbromide is mainly distributed on muscle cells of the abdominal and pelvic area as well as
in the intramural ganglia of the abdominal organs. Plasma protein binding (albumin) of
hyoscine butylbromide is approximately 4.4%. Animal studies demonstrate that hyoscine
butylbromide does not pass the blood-brain barrier, but no clinical data to this effect is
available. Hyoscine butylbromide (1 mM) has been observed to interact with the choline
transport (1.4 nM) in epithelial cells of human placenta in vitro.
Metabolism and elimination
The main metabolic pathway is the hydrolytic cleavage of the ester bond. The half-life of the
terminal elimination phase (t½γ) is approximately 5 hours. The total clearance is 1.2 L/min.
Clinical studies with radiolabeled hyoscine butylbromide show that after intravenous injection
42 to 61% of the radioactive dose is excreted renally and 28.3 to 37% faecally. The portion of
unchanged active ingredient excreted in the urine is approximately 50%. The metabolites
excreted via the renal route bind poorly to the muscarinic receptors and are therefore not
considered to contribute to the effect of the hyoscine butylbromide.
5.3 Preclinical Safety Data
In limited reproductive toxicity studies hyoscine butylbromide showed no evidence of
teratogenicity in rats at 200 mg/kg in the diet or in rabbits at 200 mg/kg by oral gavage or 50
mg/kg by subcutaneous injection. Fertility in the rat was not impaired at doses of up to 200
mg/kg in the diet.
Summary of Product Characteristics
6. Pharmaceutical Particulars
6.1 List of Excipients
Sodium Metabisulphate
Trisodium Citrate
Chlorobutanol Hemihydrate
Disodium Edetate
Water for Injections
6.2 Incompatibilities
None known.
6.3 Shelf Life
36 Months
6.4 Special Precautions for Storage
Store at a temperature not exceeding 30°C. Protect from light.
Keep all medicines out of the reach of children.
6.5 Nature and Contents of Container
10x1ml amber coloured ampoules packed in a unit carton along with pack insert.
6.6 Special Precautions for Disposal and Other Handling
For single use only. Any unused solution should be discarded
7. Registrant/Sole Agent
EMBASSY PHARMACEUTICAL & CHEMICAL LTD.
41, Ademola street, South West Ikoyi, Lagos, Nigeria, Tel: 01-2900791
8. Manufacturer
LABORATE PHARMACEUTICALS INDIA LIMITED
31, Rajban Road,Nariwala, Paonta Sahib, Himachal Pradesh (India)
HO: E-11, Indl, Area, Panipat- 132103
Summary of Product Characteristics