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Scopolamine (Scopolamine Hydrobromide) - Description and Clinical Pharmacology



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Scopolamine Hydrobromide Injection, USP is a sterile solution of scopolamine hydrobromide (C17H21NO4 • HBr • 3H2O) in Water for Injection.  The injection is preserved with methylparaben 0.18% and propylparaben 0.02%.  Scopolamine Hydrobromide Injection is intended for intramuscular, intravenous and subcutaneous use.  The pH (3.5-6.5) is adjusted with hydrobromic acid if necessary.

The structural formula is:




Scopolamine hydrobromide is one of the major antimuscarinic agents that inhibit the action of acetylcholine (ACh) on autonomic effectors innervated by postganglionic cholinergic nerves as well as on smooth muscles that lack cholinergic innervation.  It exerts little effects on the actions of ACh at nicotinic receptor sites such as autonomic ganglia.  The major action of this antimuscarinic agent is a surmountable antagonism to ACh and other muscarinic agents.

As compared with atropine, scopolamine differs only quantitatively in antimuscarinic actions.  Scopolamine has a stronger action on the iris, ciliary body and certain secretory glands such as salivary, bronchial and sweat.  Scopolamine, in therapeutic doses, normally causes drowsiness, euphoria, amnesia, fatigue and dreamless sleep with a reduction in rapid-eye-movement sleep.  However, the same doses occasionally cause excitement, restlessness, hallucinations or delirium, especially in the presence of severe pain.  Scopolamine depresses the EEG arousal response to photostimulation.  It is more potent than atropine on the antitremor activity (parkinsonism) in animals induced by surgical lesions.  Scopolamine is effective in preventing motion sickness by acting on the maculae of the utricle and saccule.

Scopolamine, although less potent than atropine, has been used frequently in preanesthetic medication for the purpose of inhibiting the secretions of the nose, mouth, pharynx and bronchi and reduces the occurrence of laryngospasm during general anesthesia.  Scopolamine is less potent in the decrease of cardiac rate, but not in the changes of blood pressure or cardiac output.  Like other antimuscarinic agents, scopolamine has been used widely in the treatment of peptic ulcers and as an antispasmodic agent for G.I. disorders.  This is due to the fact that scopolamine reduces salivary secretion, the gastric secretion (both the volume and acid content), and also it inhibits the motor activity of the stomach, duodenum, jejunum, ileum and colon, characterized by a decrease in tone, amplitude and frequency of peristaltic contractions.

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