Hyoscine -n- butyl bromide 20 mg/1 ml Solution for I.V., I.M. or S.C. injection Name of the medicinal product: Spasmocin Qualitative and quantitative composition: Each 1 ml solution in ampoule contains: Active ingredient: Hyoscine -n- butyl bromide 20 mg Inactive ingredients: Sterile Water for injection. Pharmaceutical form: Clear colourless solution in an amber glass ampoules. Indications/applications: Cramps and motility disorders of the gastrointestinal tract, spastic constipation, cramps and dyskinesias of the biliary and urinary tract, spasms of the muscular soft tissues during childbirth, dysmenorrhoeic complaints. For diagnostic measures such as x-rays and endoscopies (IV). Dosage/Application: Adults and adolescents over 12 years old 1-2 ampoules (20-40 mg) slowly IV, IM or SC several times a day. The daily dose should not exceed 100 mg. Children over 6 years In severe cases, 0.3–0.6 mg/kg body weight slowly IV, IM or SC several times a day The daily dose of 1.5 mg/kg body weight should not be exceeded. HYOSCINE -N- BUTYL BROMIDE should not be used on a continuous daily basis or over a longer period of time without clarifying the cause of the symptoms. Contraindications: HYOSCINE -N- BUTYL BROMIDE is contraindicated in: •Patients with known hypersensitivity to Hyoscine -n- butyl bromide or any other component of the drug; •untreated angle-closure glaucoma; •Prostatic hyperplasia with urinary retention; •mechanical stenoses in the gastrointestinal tract; •paralytic or obstructive ileus; •Megacolon; •Tachycardia; •Myasthenia gravis. Intramuscular administration of HYOSCINE -N- BUTYL BROMIDE ampoules is contraindicated in patients treated with anticoagulants because intramuscular hematoma may occur. In these patients the preparation can be administered subcutaneously or intravenously. Warnings and Precautions: Caution is advised when using HYOSCINE -N- BUTYL BROMIDE parenterally in patients with previous cardiac illnesses. These patients should be monitored. If severe abdominal pain of unexplained origin persists, worsens or occurs in conjunction with other symptoms, such as fever, nausea, vomiting, stool changes, painful tension in the abdominal wall, a decrease in blood pressure, loss of consciousness or blood in the stool, appropriate diagnostic measures should be taken to fully elucidate their cause. Due to the potential risks of anticholinergic complications, caution is advised in patients with a tendency to the following conditions: narrow-angle glaucoma, intestinal and urinary tract obstructions as well as tachyarrhythmia (e.g. hyperthyroidism, heart failure). The administration of anticholinergics can lead to an increase in intraocular pressure in patients who do not know they have angle-closure glaucoma and are therefore untreated. Patients experiencing eye pain or eye redness with changes in visual acuity after injection of HYOSCINE -N- BUTYL BROMIDE should consult an ophthalmologist without delay. Cases of anaphylaxis with episodes of shock have occurred following parenteral administration of HYOSCINE -N- BUTYL BROMIDE. As with all medicines that can trigger such reactions, patients should be monitored after an injection of SPASMOCIN. Interactions: The anticholinergic effects of drugs such as tri- and tetracyclic antidepressants, antihistamines, antipsychotics, quinidine, amantadine, disopyramide and other anticholinergics (e.g. tiotropium, ipratropium, related substances atropine) can be potentiated by HYOSCINE -N- BUTYL BROMIDE. Concomitant treatment with dopamine antagonists, such as metoclopramide, may result in reversing the effects of both preparations on the gastrointestinal tract. HYOSCINE -N- BUTYL BROMIDE may also enhance the tachycardia effects of beta-adrenergics. Pregnancy, breastfeeding: Pregnancy There are no controlled studies in pregnant women. As a precaution, the use of HYOSCINE -N- BUTYL BROMIDE should be avoided during pregnancy. Breastfeeding It is not known whether Hyoscine and its metabolites are excreted in breast milk. HYOSCINE -N- BUTYL BROMIDE should therefore not be used while breastfeeding. Effects on the ability to drive and operate machines: No relevant studies have been conducted. Patients should be informed that undesirable effects such as accommodation disorders and dizziness may occur during treatment with HYOSCINE -N- BUTYL BROMIDE. Because of possible accommodation disorders after parenteral administration of HYOSCINE -N- BUTYL BROMIDE, patients should only drive a vehicle or operate machines after their visual acuity has normalized. Undesirable effects: Many of the undesirable effects mentioned can be attributed to the anticholinergic properties of HYOSCINE -N- BUTYL BROMIDE. The anticholinergic side effects of HYOSCINE -N- BUTYL BROMIDE are generally mild and transient. The following list of side effects is based on the analysis of pooled, placebo-controlled studies with a total of 185 patients receiving HYOSCINE -N- BUTYL BROMIDE and post-marketing studies: Frequency information used: “common” (<1/10, ≥1/100), frequency not known* (cannot be determined). Immune system disorders Frequency not known*: Hypersensitivity reactions, anaphylactic reactions and anaphylactic shock including fatal consequences, dyspnea, skin reactions such as urticaria, rash, erythema, pruritus. Eye disorders Common: accommodation disorders. Frequency not known*: mydriasis, increase in intraocular pressure. Heart disorders Common: tachycardia. Vascular disorders Common: dizziness. Frequency not known*: drop in blood pressure, flushing. Gastrointestinal tract disorders Common: Inhibition of saliva secretion. Skin and subcutaneous tissue disorders Frequency not known*: dyshidrosis. Kidneys and urinary tract disorders Frequency not known*: Urinary retention. * This side effect was observed during the post-marketing period. An exact frequency estimate is not possible because the adverse effect did not occur in the clinical studies (185 patients in total). Overdose: Symptoms In case of overdose, anticholinergic symptoms such as urinary retention, dry mouth, skin flushing, tachycardia, inhibition of gastrointestinal motility, temporary visual disturbances may occur. Treatment If necessary, parasympathomimetics should be administered. Patients with glaucoma should seek immediate ophthalmological advice. Cardiovascular complications should be treated according to standard therapeutic principles. Measures for respiratory paralysis: intubation, artificial ventilation. If urinary retention occurs, catheterization may be necessary. In addition, appropriate supportive measures are indicated as required. Properties/Effects: HYOSCINE -N- BUTYL BROMIDE has an antispasmodic effect on the smooth muscles of the gastrointestinal tract, bile ducts and urogenital tract. The peripheral anticholinergic effect occurs due to visceral ganglion blockade and antimuscarinic activity. Pharmacokinetics: Absorption After intravenous administration, Hyoscine -n- butyl bromide is rapidly distributed into the tissues (t ½α = 4 min., t ½β = 29 min.). As a quaternary ammonium compound, Hyoscine -n- butyl bromide is highly polar and is therefore only partially absorbed after oral or rectal administration (8% and 3%, respectively). Distribution The steady-state volume of distribution (V ss) is 128 l (corresponds to approximately 1.7 l/kg). Because of its high affinity for muscarinic and nicotinic receptors, Hyoscine -n- butyl bromide is distributed primarily into the muscle cells of the abdomen and pelvis and into the intramural ganglia of the abdominal organs. The plasma protein binding (albumin) of Hyoscine -n- butyl bromide is approximately 4%. Metabolism Hydrolytic cleavage of the ester bond is the main metabolic pathway. The proportion of unchanged active ingredient in the urine is approx. 50%. The renally excreted metabolites are only bound to the muscarinic receptors to a small extent, which makes a contribution to the effect of Hyoscine -n- butyl bromide unlikely. Elimination The half-life of the terminal phase (t ½γ ) is approximately 5 hours. The total clearance after IV administration is 1.2 l/min. Clinical studies with radiolabeled Hyoscine -n- butyl bromide show that after intravenous administration, 42% to 61% of the radioactive dose is excreted via the kidneys and 28% to 37% via the feces. Storage conditions: Store at a temperature not exceeding 30°C. Shelf life: 3 years Package: Carton box containing 6 amber glass (Type I) ampoules (its capacity 1.85ml) in a tray, each of 1 ml and an inner leaflet.
