International generic name

Hyoscine

Drug form and composition

Solution for injection. One ampoule of 1 ml contains 20 mg Hyoscine butylbromide (20 mg/ml). Coated tablets. One coated tablet contains 10 mg Hyoscine butylbromide.

Indications

In gastrointestinal diseases - stomach and duodenal ulcer; esophageal and cardia spasms; pylor spasm; vomiting; biliary colic; biliary dyskinesia; cholecystitis. Diseases of the urogenital system - renal colic; urinary bladder tenesmus; spasm in urolithiasis. In obstetrics and gynecology - spastic dysmenorrhoea; as an additional medicine in incipient and incomplete abortion; spasms of the delivery pathways during the parturition; manual extraction of the placenta.

Dosage and administration

Ampoules: In case of acute spastic pain, in adult patients 10-20 mg of preparation is injected intramuscularly or intravenously 2-4 times daily. Intravenously the preparation may be used as an infusion, diluted in some parenteral solution. Maximal dose in adults is 100 mg/24 h. In children older than 6 years Buscolysin is administered intramuscularly and intravenously in dose 5-10 mg, 2-4 times daily. Coated tablets: Recommended daily dose in adults and children older than 12 years is 1-2 tablets, 3-4 times daily (1-2 tablets). In children older than 6 years - 1 tablet, 3 times daily.

Contraindications

Hypersensitivity to the preparation; myasthenia gravis.

Special warnings and precautions

Buscolysin should be used with care in patients with rhythm disorders, as a risk of development of high frequency tachycardia and tachyarrhythmia exists, although the preparation, compared with atropine, possesses more weak cholinolytic effect on the heart. Although the preparation exerts weaker anticholinergic effect, compared with atropine, it should be administered with care in patients with glaucoma and fever. Buscolysin is used carefully in persons with xerostomia, rhinitis sicca, hypertension, and hyperthyroidism. It is advisable the preparation to be used in children over 6 years. In elderly patients, patients with metabolite, liver, and renal function disorders it should be used with care. Buscolysin passes the placentar barrier, so it should be administered with care in pregnant women during the first trimester. The preparation may reduce the mother milk secretion, and it is partially secreted in the milk, so for nursing women it should be used only in case of exceptional indications. Buscolysin is used with care in drivers, because it may cause mydriasis and cycloplegia, with resultant close distance vision disorders.

Drug interactions

M-cholinolytic action of Buscolysin is antagonised by cholinergic preparations, including pylocarpine and anti-cholinesterase agents (galantamine, fisostigmine, pyridostigmin), due to the functional antagonism. The preparation enhances anti-cholinergic effects of amantadine, chinidine, three- and fourcycled antidepressants, neuroleptics, antihistamine and antiparkinson preparations. Buscolysin, depressing gastrointestinal motor function, increases absorbtion and serum concentration of digoxin (by 1/3), and may lead to relative overdosage. Combined administration of corticosteroids (locally or systemic) and Buscolysisn leads to an increase of the risk of elevation of the ocular pressure and glaucoma development. Excretion of the preparation may be retarded by urine alkalizing agents - antiacid preparations, citrate, etc. Concomitant administration of Buscolysin and ketoconazole or metoclopramide may lead to a reduction of the therapeutic activity of the later.

Adverse reactions

Buscolysin depresses secretion of the endocrine glands. This is clinically manifested by xerostomia and skin redness. Buscolysin causes accommodation disorders - mydriasis and cycloplegia. It may provoke a glaucoma attack, because of elevation of the intraocular pressure. Following CNS manifestations may be seen: anxiety and hallucinations. Such symptoms are more frequent in case of overdosage, and in children and elderly patients. Occasionally Buscolysin may cause tachycardia or tachyarrhythmia, as well as hypersensitivity manifestations - rush, urticaria. Frequent side effects are miction disorders and urine retention, particularly in elderly men with prostatic gland hypertrophy.

Pharmacological mechanisms

Buscolysin, being a scopolamine derivative, belongs to the group of the M-cholinolytic agents influencing the vegetative system. It possesses a prominent spasmolytic action on the smooth muscle of the gastrointestinal tract, biliary and urinary tract. Buscolysin blocks predominantly the peripheral pre- and postsynapse muscarine receptors, whereas nicotine cholinergic receptors are less influenced. Buscolysin exerts some N-cholinolytic effect on the parasympathetic and sympathetic ganglia. Its effects on the salivary glands, the heart, and the eye are comparatively weak. Compared with atropine, the preparation depresses slightly degestive glands secretion - in parenteral application reduces slightly hydrochloric acid secretion in the stomach, as well as the pathologic night secretion of the stomach glands. Due to the quaterner nitric atom existence, the preparation does not pass hematoencephal barrier, and has no effect on the CNS.

Supplied

10 or 100 ampoules of 1 ml (20 mg). 20 or 800 coated tablets of 10 mg.

Expiry

Solution for injection - 5 years. Coated tablets - 3 years.