TRADE NAME: Spasmocin suppository GENERIC NAME: Hyoscine - N- butyl bromide COMPOSITION: Each suppository contains: Active ingredient: Hyoscine -N- butyl bromide 15 mg : Excipients Suppocire A PHARMACEUTICAL FORM: suppositories. PHARMACOLOGICAL ACTION: PHARMACODYNAMICS: Pharmacotherapeutic group: Semi-synthetic alkaloids of Belladonna, quaternary ammonium compounds. Spasmocin performs a spasmolytic action on the smooth muscle of the gastrointestinal tracts, biliary and genito-urinary tracts. Due to the structure of quaternary ammonium derivatives, hyoscine-N- butylbromide does not pass into the central nervous system and consequently there are no anticholinergic side effects at the level of the central nervous system. A peripheral anticholinergic action may occur as a result of a ganglionic blocking action at the visceral wall level as well as antimuscarinic activity. PHARMACOKINETICS: Absorption As a quaternary ammonium compound, hyoscine-N-butylbromide is highly polar and therefore only partially absorbed orally (8%) or rectally (3%). Following oral administration of single doses of 20 to 400 mg hyoscine-N- butylbromide, peak plasma concentrations were found between 0.11 ng /mL and 2.72 ng /mL at approximately 2 hours. At the same dose range, mean values of AUC0-tz ranged from 0.37 to 14.7 ng h/ ml. The average absolute bio-availabilities of different pharmaceutical forms, i.e. coated tablets, suppositories and oral solution, each containing 100 mg of hyoscine-N- butylbromide, were less than 1%. Distribution Due to its high affinity for muscarinic and nicotinic receptors, hyoscine-N-butylbromideis mainly distributed to the muscle cells of the pelvic and abdominal areas as well as the intramural ganglia of the abdominal organs. The plasma protein binding (albumin) of hyoscine-N- butylbromide is approximately 4.4%. Animal studies show that hyoscine-N- butylbromide does not cross the blood-brain barrier but no clinical data are available. Hyoscine-N- butylbromide (1 mM) has been shown to interact in vitro with choline transport (1.4 nM) in human placenta epithelial cells. Metabolism and elimination Following oral administration of single doses of between 100 and 400 mg, terminal elimination half-lives range from 6.2 to 10.6 hours. The main metabolic pathway is the hydrolytic breakage of the ester-like junctions. Hyoscine-N-butyl bromide administered orally is eliminated in feces and urine. Studies in people show that between 2% and 5% of the radioactive dose is eliminated via renal administration after oral administration and between 0.7% and 1.6% after rectal administration. Approximately 90% of recovered radioactivity is found in stool following oral administration. Urinary elimination of hyoscine-N-butylbromide is less than 0.1% of the dose. Oral apparent clearance following oral doses of 100-400 mg varied between 881 and 1420 l/min, while the corresponding volumes of distribution for the same range ranged from 5.77 to 11.3 x 105 1, probably due to a very low systemic availability. Renally eliminated metabolites bind poorly to muscarinic receptors and are therefore not considered to contribute to the effect of hyoscine-N- butyl bromide. INDICATIONS: Spasms of the gastrointestinal tract, biliary spasms and dyskinesias, genitourinary tract spasms, in adults and children over 6 years. DOSAGE AND ADMINISTRATION: The recommended dose for adults and children over 6 years of age is 1 to 2 suppositories, 2 to 3 times a day. The maximum daily dose is 100 mg for adults and children over 6 years should not be exceeded. The optimal duration of symptomatic treatment depends on the indication. No limit has been established for the duration of treatment. Spasmocin should not be administered continuously or for long periods of time without knowing the cause of abdominal pain. Pediatric caution Because the dose is not indicated in children under 6 years. Patients with renal and/ or hepatic failure No dose adjustment is required in patients with renal and/ or hepatic failure. Form of administration: By rectal route. CONTRAINDICATIONS: Spasmocin is contraindicated in the following situations: - Hypersensitivity to the active substance or to any of the excipients - Untreated narrow angle glaucoma - Prostate hypertrophy - Urinary retention for any urethro-prostatic pathology - Mechanical stenosis of the gastrointestinal tract - Pyloric stenosis - Paralytic ileus - Tachycardia - Megacolon - Myasthenia gravis
