Scopolamine Hydrobromide Trihydrate, also known as Hyoscine Hydrobromide Trihydrate, is a chemical compound belonging to the alkaloid class of compounds. It is a derivative of scopolamine, a naturally occurring plant alkaloid extracted primarily from the Solanaceae family, particularly from the plant Datura stramonium, commonly known as Jimsonweed or devil's trumpet. It consists of a tropane ring system with an ester linkage to a tropic acid moiety, where the amine group is protonated with a hydrobromide ion, and it exists in a hydrated form with three molecules of water of crystallization. It is a competitive antagonist of muscarinic acetylcholine receptors (mAChRs), with an IC50 value of 55.3 nM. This property makes it useful in various medical applications. It possesses sedative, hypnotic, and anticholinergic effects, inhibiting the secretion of sweat, relaxing muscles, and having anesthesia-like properties.
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Chemical Formula |
C17H28BrNO7 |
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Exact Mass |
437.10 |
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Molecular Weight |
438.32 |
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m/z |
437.10 (100.0%), 439.10 (97.3%), 440.11 (17.9%), 438.11 (16.2%), 438.11 (2.2%), 439.11 (1.4%), 441.11 (1.4%), 441.11 (1.2%), 439.11 (1.1%) |
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Elemental Analysis |
C, 46.58; H, 6.44; Br, 18.23; N, 3.20; O, 25.55 |
Bronchodilator
COPD Treatment: It has been studied as a bronchodilator for the maintenance treatment of chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema. It helps in the management of dyspnea associated with these conditions and prevents acute exacerbations.
Motion Sickness
Transdermal Patch: There is potential for the use in the development of transdermal patches for the management of motion sickness. Its anticholinergic properties may help alleviate symptoms caused by motion or visual stimuli.
Muscarinic Receptor Antagonist
As a competitive antagonist of muscarinic acetylcholine receptors (mAChR), it is a valuable tool in pharmacology and neuroscience research. Its ability to block the action of acetylcholine at these receptors makes it useful in studying the role of mAChR in various physiological and pathological processes.
Memory and Cognitive Function
It has been extensively used in research to induce memory impairments in animals, which helps scientists understand the mechanisms underlying memory formation and retrieval.
Ophthalmic Preparations
There is ongoing research into the use in the development of ophthalmic formulations. Its ability to influence the action of acetylcholine in the eye may have therapeutic implications for certain eye conditions.
Anesthesia Adjunct
Although not as commonly used, it has also been studied as an adjunct to anesthesia, particularly in pediatric patients, to reduce the incidence of postoperative nausea and vomiting.
Contraindications
- Patients who are allergic to scopolamine hydrobromide should not use it. Allergic reactions may include but are not limited to severe symptoms such as rash, urticaria, and difficulty breathing.
- Breastfeeding women: Since the drug may be passed to the baby through breast milk, breastfeeding women should avoid using it.
- Glaucomatous patients: Scopolamine hydrobromide may aggravate glaucoma symptoms and cause increased intraocular pressure, so it is contraindicated for glaucoma patients.
- Patients with intestinal obstruction and pyloric obstruction: Such patients may aggravate obstruction symptoms after use, so it is contraindicated.
- Patients with dysuria caused by prostate diseases, etc.: The drug may aggravate dysuria, so it should be used with caution or prohibited.
- Pregnant women: Although specific contraindications may vary depending on the condition and medication needs, pregnant women are generally advised to use it with caution to avoid potential risks.
- Scopolamine hydrobromide may interact with other drugs, especially anticholinergic drugs, antidepressants, antihistamines, etc. Consult a doctor or pharmacist before use to ensure there is no risk of drug interaction.
- For patients with serious heart disease, high blood pressure, hyperthyroidism and other diseases, scopolamine hydrobromide should be used with special caution and follow the doctor's advice.
The synthesis method of Scopolamine Hydrobromide Trihydrate, specifically the formation of its trihydrate form, is not typically detailed in a straightforward manner due to the complexity involved in the synthesis of the base compound, Scopolamine, and its subsequent conversion to the hydrobromide salt with hydration. However, I can outline a general approach to synthesizing Scopolamine Hydrobromide, which may then be subjected to conditions that favor the formation of the trihydrate.
Synthesis Method
The synthesis of Scopolamine Hydrobromide, typically starts from naturally occurring alkaloids or via semi-synthetic routes.
Extraction or Synthesis of Base Compound
Scopolamine (or its precursor alkaloid) is extracted from plant sources such as the nightshade family (Solanaceae) or synthesized via chemical methods.
Reaction with Hydrobromic Acid
The base compound (e.g., Scopolamine) is reacted with hydrobromic acid (HBr) in a suitable solvent. This reaction typically occurs under controlled conditions to ensure the formation of the desired hydrobromide salt.
Isolation and Purification
The resulting Scopolamine Hydrobromide salt is isolated from the reaction mixture and purified to remove impurities. This may involve filtration, crystallization, and/or other separation techniques.
Formation of the Trihydrate
The formation of the trihydrate form of Scopolamine Hydrobromide is likely a result of hydration of the anhydrous salt under specific conditions.
Hydration Conditions
The anhydrous Scopolamine Hydrobromide salt is exposed to controlled humidity or moisture levels, often in a solvent that promotes hydration. The solvent and temperature conditions are adjusted to favor the formation of the trihydrate crystal structure.
Crystallization
Crystallization of the hydrated salt is carefully controlled to ensure the formation of pure, crystalline Scopolamine Hydrobromide Trihydrate. This may involve slow cooling of a supersaturated solution or other crystallization techniques.
harm
After taking an overdose of scopolamine hydrobromide, various toxic symptoms appeared. Three hours after taking 12 tablets of scopolamine hydrobromide, seek medical attention. The dose of scopolamine hydrobromide is 150 μ g, equivalent to 1.8mg or 108 μ g/kg. Unable to answer simple questions and do not know familiar people. Start to become active, distracted, have speech disorders, and experience visual hallucinations. About an hour after ingestion, it becomes drowsy and falls asleep. Symptoms include incoherent speech, imbalance, low blood pressure, and palpitations. The neurological examination showed ataxia, but strength, sensation, pitch, and upper and lower limb reflexes were normal. An hour later, hypocalcemia appeared. In addition, there may be a phenomenon called "anticholinergic syndrome".
Testers placed experimental mice in a simple maze. After the mice became familiar with the maze path, administering 1mg/kg of scopolamine hydrobromide to the mice resulted in them being unable to find the familiar maze exit, indicating that taking a certain dose of scopolamine hydrobromide caused memory impairment in the mice.
When accidentally infected with scopolamine hydrobromide in the eyes, it can cause pupil dilation and blurred vision, but still has the ability to move the eyes without ptosis. It can be cured in 2 days. From this, it can be seen that scopolamine hydrobromide should not come into contact with the eyes.
The route and dosage of accepting scopolamine hydrobromide are not specified. A week later, confusion, suspicion, paranoia, and inappropriate behavior appeared, and blood pressure increased. In the following days, mental illness and eczema worsened, causing swelling and ulcers in the legs and feet, leading to rhabdomyolysis and deep vein thrombosis.
In 1987, it was common to rinse with scopolamine hydrobromide for 5 minutes before dental surgery, which can significantly reduce saliva in the mouth and facilitate operations without being affected by the patient's saliva secretion.
Storage Conditions
Temperature:
Low Temperature:
Ideally, it should be stored at a temperature range of 2-8°C. This low temperature helps to minimize degradation and maintain the stability of the compound.
Avoid High Temperatures:
Prolonged exposure to high temperatures can lead to degradation of the compound, therefore, storage areas should be well-insulated and equipped with temperature control systems.
Humidity and Moisture:
Dry Environment: Maintaining a dry environment is crucial to prevent hydration or dehydration of the trihydrate form. Ensure that storage containers are tightly sealed and the storage area is free from moisture sources.
Light Sensitivity:
Protect from Light: Scopolamine Hydrobromide Trihydrate should be stored in light-resistant containers or packaging to prevent photodegradation. Store in areas with minimal light exposure and avoid direct sunlight.
Packaging:
Airtight Containers:
Store the compound in airtight containers to prevent exposure to air and moisture.
Label Clearly:
Clearly label the containers with the name of the compound, its concentration, storage conditions, and any special handling instructions.
Transportation Conditions
Temperature Control:
Cold Chain Transportation: Use cold chain transportation methods to maintain the temperature range of 2-8°C during transit. This may involve the use of insulated containers with ice packs or refrigerated vehicles.
Packaging for Transport:
Sturdy Packaging:
Ensure that the packaging used for transportation is sturdy and can withstand the rigors of transport without damaging the product.
Shock-Resistant:
Use packaging materials that are shock-resistant to minimize the risk of breakage or leakage during transit.
Labeling and Documentation:
Proper Labeling:
Clearly label the transport containers with the name of the compound, hazard warnings, storage conditions, and any special handling instructions.
Shipping Documents:
Prepare shipping documents that include all relevant information about the compound, its classification, and any necessary safety precautions.
Emergency Procedures:
Spill Containment:
Have spill containment materials available in case of leaks or spills during transportation.
Emergency Response Plan:
Have an emergency response plan in place in case of accidents or incidents during transportation.
FAQ
What is scopolamine hydrobromide trihydrate used for?
Scopolamine hydrobromide trihydrate is an alkaloid from Solanaceae. It is used for the treatment of excessive salivation, colicky abdominal pain, bradycardia, sialorrhoea, diverticulitis, irritable bowel syndrome and motion sickness.
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