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Atropine sulfate monohydrate is an organic compound with the chemical formula C17H23NO3 · H2SO4 · H2O, CAS 5908-99-6. A colorless to white sparkling crystalline powder that typically appears delicate and odorless in appearance, but may have a slight bitterness when used in high concentrations or large quantities. The solubility in water is extremely high, belonging to the category of highly soluble. In addition, it can also be easily soluble in ethanol, but not in organic solvents such as ether or chloroform.
This solubility characteristic gives atropine sulfate greater flexibility in the preparation of drug formulations, allowing for the selection of appropriate solvents for dissolution and preparation as needed. Good stability to light, air, and heat, and can be stored for a long time at room temperature.
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Chemical Formula |
C17H27NO8S |
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Exact Mass |
405 |
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Molecular Weight |
405 |
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m/z |
405 (100.0%), 406 (18.4%), 407 (4.5%), 407 (1.6%), 407 (1.6%) |
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Elemental Analysis |
C, 50.36; H, 6.71; N, 3.45; O, 31.57; S, 7.91 |
Atropine sulfate monohydrate is an anticholinergic drug that blocks the binding of acetylcholine to its receptors. It reduces or eliminates autonomic nervous system responses such as slowed heart rate, contraction of smooth muscle in the digestive tract, and slowed breathing. Eucalyptus sunwood, including eucalyptus leaves and bark, is one of the natural sources of product.
A an important anticholinergic drug, has a wide range of applications in the medical field. Its unique pharmacological effects make it play a crucial role in multiple therapeutic fields.
Anticholinergic effect
As a competitive non-selective anticholinergic agent, it exerts its pharmacological effects by competitively binding to muscarinic acetylcholine receptors in the body. It effectively blocks the binding of endogenous acetylcholine to target receptors, thereby antagonizing the overexcited parasympathetic nerve function. This core mechanism inhibits excessive contraction of visceral smooth muscles and suppresses the hypersecretion of various exocrine glands, including gastric glands, salivary glands, bronchial glands, and sweat glands.
By regulating smooth muscle tension and glandular secretory levels, the drug relieves visceral spastic pain, reduces abnormal bodily secretions, and stabilizes autonomic nervous system function. This broad-spectrum anticholinergic property serves as the fundamental pharmacological basis for its extensive clinical application in gastrointestinal, respiratory, circulatory, and toxicological diseases, achieving targeted therapeutic effects on multiple parasympathetic hyperactivity disorders.
Gastrointestinal diseases treatment
In gastroenterology, it is a classic first-line adjuvant drug for spastic and ulcerative gastrointestinal disorders. It acts directly on the smooth muscle of the gastrointestinal tract, relieving persistent spastic contraction of the gastric and intestinal smooth muscles caused by parasympathetic hyperactivity, inflammation stimulation, or irritable bowel lesions. For common clinical conditions including gastric ulcers, duodenal ulcers, acute and chronic gastrointestinal spasms, and abdominal colic induced by gastroenteritis, the drug can rapidly alleviate paroxysmal abdominal pain, cramping discomfort, and gastrointestinal hyperperistalsis.
Additionally, its inhibitory effect on gastric gland secretion effectively reduces excessive gastric acid and pepsin production, which relieves mucosal irritation, reduces ulcer erosion stimulation, and creates a favorable repair environment for damaged gastrointestinal mucosal tissues, significantly improving patients' abdominal distension, pain, and abnormal defecation symptoms.
Pain relief for visceral colic
Beyond gastrointestinal pain, the drug possesses significant analgesic effects on various refractory visceral colic caused by smooth muscle spasm. It is widely used in the clinical relief of renal colic, biliary colic, and intestinal colic.
Renal colic induced by ureteral smooth muscle spasm due to urinary calculi, as well as biliary colic caused by gallbladder and biliary duct spasm from gallstones and cholecystitis, can be effectively relieved by atropine.By relaxing the overly contracted smooth muscles of the urinary and biliary tracts, it eliminates mechanical spastic compression and nerve stimulation, rapidly alleviates severe paroxysmal colic, and relieves patients' intense pain and autonomic reactions such as nausea and vomiting accompanied by colic. Notably, it targets the root cause of smooth muscle spasm rather than merely masking pain, delivering stable and sustained analgesic effects for visceral spastic pain.
Ophthalmic applications
Atropine sulfate monohydrate is an essential pharmaceutical agent in clinical ophthalmology, mainly applied in pupil dilation and cycloplegic refraction examinations. By blocking the muscarinic receptors of the iris sphincter muscle and ciliary muscle, it relaxes the contracted iris sphincter to achieve mydriasis and paralyzes the spastic ciliary muscle to eliminate regulatory accommodation spasm. During fundus examinations, full pupil dilation eliminates visual field obstruction caused by small pupils, enabling ophthalmologists to comprehensively and clearly observe the optic disc, retina, blood vessels, and macular lesions, greatly improving the detection rate of subtle fundus lesions.
In pediatric and adolescent optometry, its powerful cycloplegic effect can completely paralyze eye accommodation, eliminate pseudomyopia interference caused by accommodation spasm, and improve the accuracy of diopter measurement, providing reliable basis for accurate glasses matching and myopia diagnosis and intervention.
Treatment of infectious diseases
Relying on its unique anticholinergic and microcirculation-regulating activity, it plays a critical auxiliary therapeutic role in severe infectious diseases and critical syndrome treatment.
It is clinically applicable to infectious toxic shock and acute cardiogenic ischemic syndrome induced by antimony preparations, severe bacterial and viral infections.In critical infectious states, excessive release of inflammatory mediators and abnormal excitation of the parasympathetic nerve will cause microvascular spasm, microcirculation disturbance, and tissue ischemia and hypoxia. Atropine can dilate microvessels, relieve vascular smooth muscle spasm, improve systemic microcirculation and tissue blood perfusion, correct ischemic and hypoxic damage to vital organs such as the heart, brain, and kidneys, and inhibit excessive inflammatory stress response.
It effectively stabilizes vital signs, prevents the progression of shock and ischemic lesions, and significantly reduces the mortality of severe infectious critical illnesses, serving as an important microcirculation regulatory drug in emergency critical care.
Rescue of organic phosphorus poisoning
It is the core first-aid drug for clinical rescue of organophosphorus pesticide poisoning. Organophosphorus compounds can inhibit the activity of human cholinesterase, leading to massive accumulation of acetylcholine in synaptic clefts, causing continuous excitation of muscarinic, nicotinic and central nervous system, and resulting in a series of severe poisoning symptoms such as profuse sweating, salivation, bronchial spasm, pulmonary edema, muscle tremor and coma.
Atropine competitively blocks peripheral and central muscarinic acetylcholine receptors, cuts off the pathological excitation signal caused by accumulated acetylcholine, and rapidly relieves critical poisoning symptoms including respiratory secretion hyperactivity, bronchospasm, bradycardia and hypotension. However, it only antagonizes the toxic effects of acetylcholine overaccumulation and cannot reactivate inhibited cholinesterase or eliminate residual organophosphorus toxins.
Therefore, for moderate and severe organophosphorus poisoning, atropine must be used in combination with cholinesterase reactivators such as pralidoxime to achieve thorough detoxification and improve the success rate of rescue.
Pre anesthesia administration
As a routine pre-anesthetic medication, it is widely used in various surgical anesthesia preparations to ensure perioperative patient safety. Under anesthesia stimulation, patients are prone to parasympathetic nerve excitation, leading to excessive secretion of respiratory tract and oral glands, which may cause airway obstruction, aspiration pneumonia and respiratory distress risks.
Atropine can significantly inhibit the hypersecretion of salivary glands, bronchial glands and respiratory mucosal glands, reduce oral and respiratory tract secretions, and keep the airway dry and unobstructed throughout the anesthesia and operation process. Meanwhile, it can block the vagal reflex induced by anesthesia and surgical traction, prevent bradycardia, hypotension and cardiac arrhythmia caused by vagal overexcitation, stabilize the patient's cardiovascular and respiratory functions, reduce anesthesia complications, and provide a safe and stable physiological condition for smooth surgical operation and postoperative recovery.
There are many synthetic methods of Atropine sulfate monohydrate, three typical synthetic methods will be introduced below.
Method 1: Using isopropanol as solvent:
First add isopropanol to the kettle, then add Atropine and excess sodium hydroxide and stir until dissolved in the reaction mixture. The temperature was raised until the reaction mixture began to boil, and bromoacetic acid was added at the same time, and then the reaction mixture was kept boiling for about 10 h. After the reaction was completed, the filter residue was removed by filtration, and the filtrate was added to sulfuric acid and continued to stir for 20 min to obtain a solid of it. Its reaction equation is as follows:
(1R,3r,5S)-8-Methyl-8-azabicyclo[3.2.1]oct-3-yl(S)-tropate + NaOH + BrCH2COOH → Atropine bromide
Atropine bromide + Na2SO4 + H2SO4 + H2O → C17H25NO7S.
Method 2: Using benzene as a solvent:
Benzene was added to the kettle, followed by Atropine and excess NaOH and stirred until dissolved in the reaction mixture. Heated to 90°C, while adding bromoacetic acid, and then kept the reaction mixture at 90-95°C for 24 h. After the reaction was completed, the filter residue was removed by filtration, and the filtrate was added to sulfuric acid and continued to stir for 20 min to obtain a solid of product. Its reaction equation is as follows:
(1R,3r,5S)-8-Methyl-8-azabicyclo[3.2.1]oct-3-yl(S)-tropate + NaOH + BrCH2COOH → Atropine bromide
Atropine bromide + Na2SO4 + H2SO4 + H2O → C17H25NO7S
Method 3: Using dodecylbenzenesulfonic acid as a catalyst:
Below, I will provide a detailed description of the steps of the synthesis method, accompanied by corresponding chemical equations.
Step 1: Add atropine and sulfuric acid to the reactor
1.1 Stir the reactor with a clean glass rod to ensure a clean surface.
1.2 Add atropine (chemical formula C17H23NO3) and sulfuric acid (H2SO4) to the reactor and stir thoroughly with a glass rod until dissolved. The reaction equation is as follows:C17H23NO3+H2SO4 → [C17H23NO3]+[HSO4]-
Step 2: Add dodecylbenzenesulfonic acid and heat it up
2.1 Add dodecylbenzenesulfonic acid to the reactor and stir evenly again.
2.2 Turn on the heating equipment, raise the temperature to 90-110 ℃, and maintain the reaction temperature for 24 hours. During this process, dodecylbenzenesulfonic acid acted as a catalyst to promote the formation of product. The reaction may take several steps, but overall it can be described as follows:[C17H23NO3]+[HSO4]-+HSO4- → [C17H23NO3]+[HSO4]-[HSO4]-
Step 3: Cooling, filtering, and neutralization
After the reaction is completed, turn off the heating equipment and cool the reactor to room temperature.
3.1 Filter the reaction mixture with appropriate equipment to remove filter residue. Obtain the filtrate after filtration.
3.2The unreacted sulfuric acid in the filtrate needs to be neutralized. Neutralize the sulfuric acid in the filtrate with an appropriate amount of alkali to produce. The neutralization reaction equation can be expressed as:[C17H23NO3]+[HSO4]-[HSO4]-+NaOH → [C17H23NO3]+Na++H2O+SO4-2
The final product is the solid, which can be obtained through crystallization or other separation methods.
This synthesis method utilizes dodecylbenzenesulfonic acid as a catalyst to promote the synthesis of product, which has certain experimental application significance.
Recent Advances and Future Directions
► Low-Dose Atropine for Myopia
The ATOM2 trial demonstrated that 0.01% atropine eye drops reduce myopia progression by 50% with minimal rebound or side effects, revolutionizing pediatric ophthalmology. Ongoing research explores combination therapies with orthokeratology or defocus lenses.
► Nanotechnology-Based Delivery
Liposomal and nanocrystal formulations enhance ocular bioavailability, enabling sustained release and reduced dosing frequency.
For example, atropine-loaded chitosan nanoparticles show prolonged mydriasis in rabbit models.
► Novel Indications
COVID-19-Associated ARDS: Early studies suggest atropine may reduce bronchial secretions in mechanically ventilated patients, though evidence remains inconclusive.
FAQ
What is atropine sulphate monohydrate used for?
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Atropine sulfate eye drops is used to dilate the pupil before eye exams. It is also used to treat an eye condition called amblyopia (lazy eyes) and other eye conditions (eg, cycloplegia).
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