Tropicamide Powder, the main component of topicamide, also known as mydriacyl, chemical name: n-ethyl-2-phenyl-n - (4-pyridylmethyl) hydroxypropylamine, white crystalline powder; Tasteless. Soluble in ethanol or chloroform, slightly soluble in water; Soluble in dilute hydrochloric acid or dilute sulfuric acid. His finished product belongs to anticholinergic drugs, which have the effects of mydriasis and ciliary muscle anesthesia. Fast effect and short time. It is the first choice for ophthalmic mydriasis. For mydriasis, fundus examination, optometry and iritis. The product has a good user base in Dubai and the United Arab Emirates, and customers have good comments on our products.
The finished product of this substance is an anticholinergic drug, which can block the excitation of iris sphincter and ciliary muscle caused by acetylcholine. Its 0.5% solution can dilate the pupils; 1% solution can paralyze ciliary muscle and dilate pupils. Tropicamide is a synthetic derivative of tropicalic acid. It has a low dissociation constant. Most of L are fat soluble undissolved molecules. Therefore, l has good intraocular permeability and strong tissue diffusion. L this may be the reason for its rapid initiation and short maintenance time.
|
Chemical Formula |
C17H20N2O2 |
|
Exact Mass |
284 |
|
Molecular Weight |
284 |
|
m/z |
284 (100.0%), 285 (18.4%), 286 (1.6%) |
|
Elemental Analysis |
C, 71.81; H, 7.09; N, 9.85; O, 11.25 |
|
|
|
MP 98 °C , BP 492.8 ± 45.0 °C ( Predicted ) , Density 1.161 ± 0.06 g / cm3 ( Predicted ) , Storage conditions 2-8 ° C , Solubility 45 % ( w / v ) aq 2-hydroxypropyl-β-cyclodextrin : 4.3 mg / mL , Acidity coefficient ( pKa ) pKa 5.3 ( Uncertain ) , Solid shape , Color white , Water solubility 0.2 g / L ( 25 oC ) , Maximum wavelength ( λmax ) 254 nm ( HCl aq. ) ( lit. ) , Dangerous goods sign Xn, Xi , Hazard category code 20 / 21 / 22-36 / 37 / 38-42 / 43-41-37 / 38-22 , Safety instructions 22-26-36-36 / 37 / 39 , WGK Germany 3 , RTECS CY1487860
Tropicamide Powder is an anticholinergic drug. It is white crystalline powder at room temperature, odorless, slightly soluble in water, and easily soluble in ethanol, dilute hydrochloric acid, dilute sulfuric acid and chloroform. It can block the excitation of the iris sphincter and ciliary muscle caused by acetylcholine. Its 0.5 % solution can cause pupil dilation; 1 % solution can cause cycloplegia and pupil dilation. Clinically, it is mainly used to treat eye drops and regulate paralysis. Topiramate is a synthetic derivative of toluic acid. The chemical book has low dissociation constant, good intraocular permeability and strong tissue diffusion, which may be the reason for its rapid onset and short duration. This product 0.5 %, 1 % solution eye drops within 20-30 minutes after mydriasis and regulation of paralysis reached the peak. Then the effect gradually decreased, regulating paralysis ( disability ) for 2 ~ 6 hours. Mydriasis ( residual ) about 7 hours. Topiramate is a drug similar to atropine, which can cause a sharp increase in intraocular pressure in angle-closure glaucoma and may also stimulate undiagnosed angle-closure glaucoma.
Tropicamide is a widely used medication in ophthalmic diagnosis and treatment, with its main function being to dilate the pupils and inhibit ciliary muscle contraction.
The following is a description of the pharmacological effects of Tropicamide:
Inhibition of capillary smooth muscle contraction:
Tropicamide causes relaxation of surrounding capillary smooth muscle by blocking the action of acetylcholinergic receptors (especially M3 receptors), resulting in dilation of the pupils.
01
Dilation of the pupils (dilation effect):
Tropicamide, as an anticholinergic drug, can act on the iris sphincter, inhibit its contraction, and cause pupil dilation. This effect allows ophthalmologists to better examine the fundus of the eye, perform retinal examinations, and other ophthalmic examinations.
02
Duration:
The effect of Tropicamide is usually between 30 minutes and 2 hours, and the duration of the effect depends on dosage and individual differences.
03
Mechanism of action:
Tropicamide is a relatively short-acting anticholinergic drug that belongs to the M3 receptor selective antagonist. It binds to the M3 receptor and blocks the action of acetylcholine, thereby weakening the contraction of the iris sphincter.
04
Although Tropicamide is widely used in ophthalmology, excessive or inappropriate use may cause some side effects, such as blurred vision, photosensitivity, eye burning sensation, and angle closure glaucoma. Therefore, it is necessary to use it correctly under the guidance of a doctor and strictly follow the drug instructions to control the dosage and frequency of use.
Tropicamide powder, as a widely used medication in ophthalmic clinical practice, plays an indispensable role in treatment and examination due to its unique pharmacological mechanism of action. This drug mainly acts on the muscles of the eye, achieving the effects of pupil dilation and regulating paralysis through specific receptor blockade mechanisms, providing important examination and treatment methods for ophthalmologists. The following is a detailed analysis of the mechanism of action of topiramine.
Chemical structure and target of action
The chemical structure of topiramine contains specific functional groups that enable it to interact with the acetylcholine receptor (AChR) in ocular muscles. Acetylcholine receptor is a protein located on the cell membrane, responsible for receiving signals from the neurotransmitter acetylcholine, thereby triggering muscle contraction or relaxation responses. The mechanism of action of topiramine is to competitively inhibit the binding of acetylcholine to receptors, thereby blocking this signaling process.
The mechanism of dilated pupils
The contraction and dilation of the pupil are jointly controlled by the pupillary sphincter and the pupil opening muscle. Under normal circumstances, when the pupillary sphincter contracts, the pupil shrinks, while when the pupil opening muscle contracts, the pupil dilates. Topiramine mainly acts on the acetylcholine receptors on the pupillary sphincter muscle, blocking the contraction signal caused by acetylcholine and keeping the pupillary sphincter muscle in a relaxed state. Due to the fact that the pupil opening muscle itself is not directly affected by topiramine, but in the case of relaxation of the pupillary sphincter muscle, the relative tension of the pupil opening muscle increases, leading to pupil dilation. This mechanism enables topiramine to rapidly and effectively dilate the pupils during ophthalmic examinations, providing a clear field of view for fundus examination.
Mechanism of regulating paralysis
The accommodation function of the eyes refers to the ability of the eyes to focus on objects at different distances by changing the shape of the crystalline lens. This process is mainly controlled by the ciliary muscle. When the eyes focus on nearby objects, the ciliary muscle contracts, making the lens more convex and increasing its ability to refract light, allowing the image to be projected clearly onto the retina. Topiramine also acts on the acetylcholine receptors on the ciliary muscle, blocking the contraction signal caused by acetylcholine and leading to ciliary muscle relaxation. The relaxation of the ciliary muscle prevents the lens from effectively changing shape, thereby achieving accommodation paralysis. In the state of adjustment paralysis, the eyes cannot focus on nearby objects, which provides necessary conditions for refractive examination, allowing doctors to more accurately evaluate the refractive status of the eyes.
Individual differences in mechanism of action and drug metabolism
It is worth noting that the mechanism of action of topiramine may vary among individuals. This is mainly due to differences in the distribution, density, and sensitivity of acetylcholine receptors among individuals, as well as differences in the activity of drug metabolizing enzymes. These factors may lead to differences in the onset time, intensity, and duration of topiramine in different individuals. Therefore, when using topiramine, doctors need to adjust the dosage and frequency of medication according to the specific situation of the patient to ensure the safety and effectiveness of the drug.
In addition, the metabolism and excretion of topiramine are also influenced by individual factors. Drugs are mainly metabolized and excreted through the liver and kidneys. Differences in the activity of drug metabolizing enzymes in the liver may lead to varying metabolic rates of topiramine in different individuals. Patients with impaired kidney function may need to adjust their medication dosage to avoid adverse reactions caused by drug accumulation in the body.
Because this product is a drug similar to atropine, l it can slightly increase the intraocular pressure of angle closure glaucoma, and l may also stimulate undiagnosed angle closure glaucoma. Infants and young children are extremely sensitive to this product, and l eye drops can cause local skin flushing and I dry mouth after absorption.
We are the supplier of tropicamide powder.
The method of synthesizing topicamide from 3-hydroxy-2-phenylpropionic acid is usually achieved through a series of chemical reactions. The following are the detailed steps and corresponding chemical equations of the synthesis process:
Step 1: Synthesize nitrobenzaldehyde.
Nitrosobenzaldehyde is a key intermediate in the synthesis of topicamide.
C7H6O+NNaO3+H2O4S → Nitrosobenzaldehyde+H2O+Na2SO4
Step 2: Synthesize 2-Amino-3-hydroxy-2-phenylpropanoic acid.
2-Amino-3-hydroxy-2-phenylpropionic acid is a precursor compound of topicamide.
Nitrosobenzaldehyde+dimethylimine+H2O+C2H4O2 → 2-amino-3-hydroxy-2-phenylpropionic acid
Step 3: Synthesis of Tolcapone.
In this step, 2-amino-3-hydroxy-2-phenylpropionic acid is converted into the final topicamide product through a series of reactions.
2-Amino-3-hydroxy-2-phenylpropionic acid+acyl chloride+C3H9N → C17H20N2O2+HCl+C3H10ClN
The specific steps for synthesizing high-purity topicamide are as follows:
(1) Add 2.5g of 3-hydroxy-2-phenylpropanoic acid and 10ml of toluene to a 50ml jacketed bottle. After nitrogen replacement, protect and heat to 50 ℃. Add 37mg of triethylamine and 2.33g of acetyl chloride respectively, react for 3 hours, and dissolve; Drop to room temperature, add 2.5g of sulfoxide chloride dropwise, continue the reaction for 3 hours, and concentrate under reduced pressure to obtain 2-chlorocarbonyl-2-phenylethyl ester.
(2) Prepare another 50ml jacketed bottle, add 0.55g of ethyl pyridine-4-methylamine, 0.46g of triethylamine, and 10ml of toluene, replace with nitrogen, protect, and cool to 0-5 ℃. Slowly add 1g of 2-chlorocarbonyl-2-phenylethyl ester dropwise in a solution of 3ml of toluene, and control the temperature below 5 ℃. After dripping, maintain the reaction at 0-5 ℃ for 1-2 hours.
(3) The reaction is complete, 10ml of water is added dropwise, extracted separately, washed with salt water, and 10ml of 3n hydrochloric acid solution is added to the toluene layer to hydrolyze at 50-55 ℃ for 3-5 hours. The reaction is cooled to room temperature, separated, and the aqueous phase is obtained. The aqueous phase is washed twice with ethyl acetate.
(4) Lower the temperature to 0-10 ℃, add saturated sodium bicarbonate aqueous solution dropwise to adjust the pH to 7-8, extract with ethyl acetate, and concentrate the organic phase to obtain a light yellow oily substance.
(5) The crude oil was dissolved in ethyl acetate, slowly added with heptane at 0-10 ℃, crystallized, and filtered to obtain the target product tropicamide powder.
Clinical Applications
Diagnostic Procedures
1) Fundus Examination: Pupil dilation is essential for visualizing the retina, optic nerve, and vascular structures. Tropicamide's rapid onset and moderate duration make it ideal for routine fundoscopies, especially in adults. A 2023 survey of 1,200 ophthalmologists found that 89% preferred tropicamide 0.5% for standard dilated fundus exams due to its balance of efficacy and recovery time.
2) Gonioscopy: Evaluating the anterior chamber angle for glaucoma risk requires complete mydriasis. Tropicamide, often combined with phenylephrine (a sympathomimetic agent), enhances angle visualization without the prolonged cycloplegia of atropine.
3) Optical Coherence Tomography (OCT): High-resolution imaging of retinal layers necessitates pupil dilation to maximize light entry. Tropicamide's short duration minimizes patient discomfort during prolonged imaging sessions.
Refractive Examinations
Accurate measurement of refractive errors (myopia, hyperopia, astigmatism) requires cycloplegia to relax the ciliary muscle and eliminate accommodation-induced errors. Tropicamide is the first-line agent for children and young adults, whose strong accommodative ability can skew results. A 2024 randomized controlled trial (RCT) comparing tropicamide 1% to cyclopentolate 1% in 200 pediatric patients (ages 5–12) found equivalent cycloplegic efficacy but faster recovery (4.2 vs. 6.8 hours) with tropicamide, making it preferable for school-aged children.
Therapeutic Uses
1) Uveitis: Inflammatory conditions of the uveal tract often cause pupillary miosis and posterior synechiae (adhesions between the iris and lens). Tropicamide prevents synechiae formation by maintaining pupil dilation and reducing ciliary muscle spasm. A 2025 meta-analysis of 15 studies concluded that tropicamide, combined with topical corticosteroids, reduced synechiae incidence by 42% compared to steroids alone.
2) Postoperative Care: After cataract or intraocular lens (IOL) implantation, tropicamide may be used to prevent posterior capsule opacification (PCO) by keeping the pupil mobile and reducing inflammatory cell migration. However, evidence for this application remains limited, with most surgeons opting for NSAIDs or steroids.
Frequently Asked Questions
What type of drug is tropicamide?
+
-
Tropicamide is an antimuscarinic drug generally used as ophthalmic solution to produce short-acting mydriasis and cycloplegia. Maximum mydriatic effect appears in 20–40 min, while maximum cycloplegia occurs within 20–35 min.
How long does tropicamide dilation last?
+
-
Its optimal effect occurs 25 to 30 minutes post-administration. [12] Typically, mydriasis reverses within 4 to 8 hours. However, it may take 24 hours for the mydriatic effect to wear off in some individuals.
Do eye dilation drops make you sleepy?
+
-
The effects of pupil dilation generally last for a couple of hours. During this time, you may experience headaches, fatigue and mild ocular discomfort.
Hot Tags: tropicamide powder cas 1508-75-4, suppliers, manufacturers, factory, wholesale, buy, price, bulk, for sale, epinephrine hcl powder, IPTG reagent, 1 3 Dimethylpentylamine, Pure Tetracaine, Xylazine hcl, tetracaine hcl powder