Atropine Sulfate Hydrate 0.025% 0.3mL x 30 drops (Santen Myopia Relief Eye Drops 0.025%)

Atropine sulfate hydrate 0.025% is an anticholinergic eye drop that works by blocking cholinergic receptors in the eye, thus exerting mydriatic and accommodation-paralyzing effects. It is suitable for children's refractive examinations, cycloplegic refraction, and relieving ocular inflammation such as iridocyclitis.

I. Basic Drug Information

1. Common name: Atropine sulfate hydrate
2. English name: Atropine Sulfate Hydrate
3. Product Name: RYJUSEA Mini Ophthalmic Solution 0.025%, Un Yasan 2 Ophthalmic Solution 0.025%
4. Dosage form: eye drops
5. Indications: Inhibition of myopia progression
6. Element:
   • Active ingredient: Each 1 mL contains 0.25 mg of atropine sulfate hydrate.
   • Additives: concentrated glycerol, sodium dihydrogen phosphate hydrate, sodium citrate hydrate, hydroxyethyl cellulose, pH adjuster
7. Characteristics:
   • pH: 4.0~4.6
   • Osmotic pressure ratio: 0.9~1.1
   • Appearance: Colorless, clear, sterile aqueous eye drops

II. Usage and Dosage

III. Taboos

1. Patients with a history of allergy to any of the ingredients in this product.
2. Patients with glaucoma and those with factors that cause increased intraocular pressure, such as narrow angle-closure glaucoma or shallow anterior chamber, may be at risk of acute angle-closure glaucoma attacks.

IV. Precautions

1. Special populations:
   • Breastfeeding women: The benefits of treatment and the nutritional benefits of breast milk should be considered together to weigh whether to continue or stop breastfeeding.
   • Children, etc.: No clinical trials were conducted on low birth weight infants, newborns, infants, or children under 5 years old.
2. Medication instructions:
   • After applying eye drops, photophobia and blurred vision may occur due to pupil dilation. Before the symptoms subside, avoid using playground equipment that may cause a fall, riding a bicycle/car, or operating machinery. If necessary, wear sunglasses and avoid looking directly into sunlight or strong light.
   • When using, the first 1-2 drops should be discarded and not instilled into the eye; when instilling the drops, be careful not to let the tip of the container directly touch the eye; after instilling the drops, open the eyelids and instill the solution into the conjunctival sac, close the eyes and press on the lacrimal sac for 1-5 minutes before opening the eyes again.
   • When used in combination with other eye drops, an interval of at least 5 minutes is required.
   • This product contains no preservatives and should be used only once after opening. Any remaining liquid should be discarded.
3. Medication storage:
   • Store at room temperature and keep away from light.
   • After opening the aluminum-plastic packaging, it should be placed in the accompanying light-proof medicine bag, stored at room temperature, and used within 3 months.

V. Adverse Reactions

1. Allergic reactions: Not explicitly mentioned.
2. Digestive system reactions: Not explicitly mentioned.
3. Other reactions:
   • Eyes: More than 5% experience photophobia; 1% to 5% experience visual impairment, blurred vision, and pupillary obstruction; less than 1% experience accommodation disorder, eyelid eczema, and itchy eyes.
   • Nervous system: 1%~5% experience headaches.

VI. Drug Interactions

VII. Pharmacological effects

1. Moderating biomembrane function: Not explicitly mentioned.
2. Improvement of metabolic abnormalities: Not explicitly mentioned.
3. Regulating blood lipids: Not explicitly mentioned.
4. Protecting blood vessels: Not explicitly mentioned.
5. Other uses:
   • Mechanism of action: Atropine may participate in scleral remodeling directly or indirectly through muscarinic receptors in the retina or sclera, thereby inhibiting axial elongation.
   • It has non-selective affinity for muscarinic receptors (M1, M2, M3, M4, M5 subtypes) (in vitro assay).
   • Inhibition of myopia progression: The progression of experimental myopia can be inhibited by intravitreal administration to monkeys and by eye drops to guinea pigs, porcupines, and mice.

VIII. Pharmacokinetics

1. Absorption: A study of 10 myopic patients aged 5-15 years, who used one drop once daily for 7 consecutive days, showed that on day 1, the peak plasma concentration (Cmax) was 19.7±7.0 pg/mL, the median time to peak concentration (tmax) was 60 minutes (range 5.0-60 minutes), and the area under the curve (AUC0-60min) was 939±370 pg・min/mL; on day 7, the Cmax was 16.5±3.6 pg/mL, the median tmax was 60 minutes (range 30-60 minutes), and the AUC0-60min was 798±188 pg・min/mL.
2. Excretion: In healthy adult males, 88% of 14C-atropine 2 mg was excreted in the urine within 48 hours, of which about 50% was atropine unchanged and less than 2% was troponic acid; 14C was not detected in breath and only a small amount (less than 0.5% of the administered dose) was detected in feces.
3. Distribution: After a single instillation of 2% 3H-atropine solution into both eyes of white guinea pigs, the highest concentration of 3H in the eye tissues was observed 1 hour later. The concentrations, from highest to lowest, were found in the cornea, sclera, iris ciliary body, aqueous humor, choroid, retina, and vitreous body. After a single instillation of 2% 3H-atropine solution into both eyes of colored and white guinea pigs, the concentration of 3H in the iris of colored guinea pigs was approximately 8 times that of white guinea pigs at 96 hours, suggesting that atropine may bind to melanin.
4. Metabolism: Atropine can be N-demethylated to noratropine, oxidized to atropine-N-oxide, and hydrolyzed to tropine and tropine acid (based on foreign data).

IX. Clinical Research

10. Packaging Specifications

XI. Production Information

Manufacturer: Santen Pharmaceutical Co., Ltd.